GI DRUGS & Disorders Flashcards Preview

Pharmacology > GI DRUGS & Disorders > Flashcards

Flashcards in GI DRUGS & Disorders Deck (1522):
1

Goal of tx for N/V :

Treat cause but often have to treat symptoms

2

For N/V, HX is critical. What are 5 essentials in getting a good HX?

1. Onset
2. PMH
3. LMP(females)
4. Appearance of emesis (coffee grounds or undigested food)
5. recent bowel habits

3

N/V diagnostics :

X-ray
KUB
Ultrasound
labs: LFT's

4

3 types of med can choose for N/V:

1. Serotonin 5-HT Receptor antagonists (Zofran, Aloxi)
2. Antidopaminergics
3. Pepto

5

Causes of N/V:

1. GI DISORDER: GERD, gastritis, constipation, pancreatitis, hepatitis
2. Intracerebral / CNS / ⬆️ ICP
3. Illness: microbial; H. Pylori
4. Medications: Oc's, antidepressants (like Celexa), antibiotics, chemo

6

How do the Serotonin 5 HT 3 receptor antagonists work (method of action/MOA)?

Selective 5-Ht3receptor antagonist, binds in both periphery and CNS, Reducing intestinal vagus nerve stimulation.
Not clear if result of CNS or peripheral antagonism.
*blocks different NT than Compazine and Phenergan*

7

Pharmacokinetics of 5ht receptor antagonists:

Well absorbed po
Enhanced with food
SL And IV preps available
Metab via liver
70% protein bound
Excreted via urine

8

Name 2 5Ht receptor antagonists:

Zofran and Aloxi

9

Adverse effects of 5ht receptor antagonists:

Headache
Diarrhea
Dizziness
Constipation **
QTprolongation **

10

5ht receptor antagonists
Contraindicated in:

Congenital Long QT syndrome
Allergy

11

Who might not tolerate Zofran due to the side effect of constipation?

A pregnant pt with morning sickness

12

Pepto bismol (Bismuth Subsalicylate): MOA

= a derivative of salicylic acid, related to aspirin
- works to ⬇️ GI irritation >> ⬇ ️nausea
- also antidiarrheal properties / reduces bowel irritation (weak bacteriocidal activities for infectious diarrhea )
- also antacid properties

13

Pharmacokinetics Pepto Bismol:

Bismuth poorly absorbed but coats ulcers well
Subsalicylate hydrolyzed in stomach to salicylate
Bismuth is excreted in stool ** Can CAUSE BLACK STOOLS!**
Sub salicylate excreted in urine as salicylate

14

Side effects of PeptoBismol

Nausea
Constipation
Discolored tongue
Black stools

15

Contraindications for Pepto Bismol

Pediatrics (risk of Reye Syndrome)
Allergy

16

Phenothiazines: Phenergan, Compazine

MOA
-antidopaminergic / blocks dopamine receptors in brain thus blocking vagus nerve in GI tract
-Phenergan also has antihistamine effect on H 1 receptors

17

Phenothiazine
Pharmacokinetics / pharmacodynamics

Metabolized by liver
Excreted in stool

18

Side effects of phenothiazine

Sedation, dizziness, mood changes,constipation

19

Contraindications of Phenothiazines

Allergy
Severe HTN
BPH
PTS

20

Acid Reflux/ Gastritis:
prevalence, probable causes?

Very prevalent (10%) US pop
Several probable causes:
1. Transient lower esophageal sphincter relaxtion
2. Low resting lower esophageal sphincter
3. Poor esophageal acid clearance
4. Defects in esophagastric motility
5. Impaired mucosal resistance and over protective defenses

21

Descriptions and symptoms of gastritis

Burning sensation, nausea, chest pain, or globus (broad) sensation.
* can be very much like an MI ; differentiating SX - SOB, diaphoresis

22

Other contributing factors to gastritis?

Intake of acidic foods; treatment begins with removing these offenders / lifestyle modifications then mess

23

4 Types acid reflux/ gastritis meds

1. Antacids
2. Carafate
3. H2 receptor antagonists
4. PPI's

24

Antacids: sodium bicarbonate, calcium carbonate, magnesium hydroxide, aluminum hydroxide
MOA?

These are weak bases that fact with gastric acid to form a salt and water, therefore decreasing gastric acidity

25

Pharmokinetics/ dynamics of antacids

-Some po absorption; 25-35 % availability
-bicarbonate preps (bioavailability) improves with food bu hydroxide preparations poorly absorbed
-carbonate excreted via stool
-aluminum and mag excreted via urine

26

Pregnancy category of antacids

B, safe for breastfeeding as well

27

Antacids: adverse effects

N/V, constipation, dependence

28

Contraindications for taking antacids:

Renal Failure (for those with aluminum and magnesium) - ie, the re ally excreted ones

29

Carafate: MOA

Positively charged sucrose sulfate binds to negatively charged proteins in base of ulcers, forms an ADHERENT/ PROTECTIVE barrier from gastric acids and bile salts

30

Carafate: pharmacokinetics

-very little absorption, so not metabolized
-excreted in stool

31

Carafate: adverse effects

CONSTIPATION! Gotta love it!

32

Contraindications for use of Carafate-

Allergy; may use with caution with other meds... Can affect absorption

33

Carafate pregnancy category:

B ( off label for peds)

34

H2 receptor antagonists: Zantac, Pepcid, Tagamet
MOA?

Competitive inhibitors of H2 receptors in gastric parietal cells causing a decrease in gastric acid. No H1 or H3 efficacy (therefore not sedating).

35

H2 receptor antagonists: pharmacokinetics

-good po absorption
-metabolized via liver
-excreted in urine

36

H2 receptor antagonists
Adverse Effects

H/A, dizziness, confusion in elderly,
.....GYNECOMASTIA (for real!?!?!)

37

H2 receptor antagonists- contraindications

Potent P450 inhibitor!
Use Tagamet with caution in elderly

38

Pregnancy category for H2 receptor antagonists

B - also safe in peds

39

Proton Pump Inhibitors- Prilosec / omeprazole, Prevacid / lansoprazole, Protonix / pantoprazole, Nexium/ esomeprazole
MOA?

Binds irreversibly to H+/ K+ exchanging ATPase pumps (proton pumps) in gastric parietal cells, decreasing both basal and stimulated gastric acid secretion

40

PPI's: pharmacokinetics/ dynamics

-PRODRUG: must survive the acidic environment of stomach to be absorbed into small bowel
-all have fairly good bioavailability, decreased with po intake
-metab in liver / inhibits CYP2C19
-excreted in stool; **dose-adjust for hepatic disease**
-little renal excretion

41

PPI's: adverse effects

H/A, diarrhea, constipation, nausea, increased risk C. diff infection, ⬇️Mg with prolonged use,
⬆️ risk osteoporosis-related fractures with prolonged use

42

PPI's: contraindications

Allergy

43

Types of laxatives:

1. Bulk (Metamucil, fibercon)
2. Osmotic laxatives ( milk of mag, lactulose, mg citrate, polyethylene glycol (miralax)

44

Osmotic laxatives MOA:

Causes water retention in stool; soluble but no absorbable compounds

45

Pharmacokinetics of osmotic laxatives

NO PO absorption/ excreted in stool unchanged

46

Adverse effects of osmotic laxatives:

Diarrhea
abdominal complaints

47

Contraindications of osmotic laxatives:

-Existing electrolyte abnormality
-Age under 2 yo

48

Osmotic laxatives: great option for long or short term relief?

No adverse effects shown up to 12 months of daily use

49

Bulk laxatives - MOA?
Pharmacokinetics

Absorb water and enlarge stools which stimulates propulsive movement through the lower GI tract
-no po absorption; excreted through stool as unchanged drug

50

Adverse effects of bulk laxatives:

N/V, abdominal fullness

51

Contraindications of bulk laxatives:

Bowel obstruction, under age of 6

52

Pregnancy Category bulk laxatives

B; safe in pregnancy and breastfeeding

53

Gastric motility agent (Metoclopramide/ Reglan) MOA

Binds to dopamine D2 receptors in CNS, as well as some 5-HT3 antagonism: gastric motility is caused by the D2 antagonism

54

Reglan: pharmacokinetics

Well-absorbed PO, 65-90% bioavailability
Metabolized via liver
Excreted via urine (decrease dose in renal insufficiency

55

Reglan: adverse effects

EPS secondary to dopamine blockade;
Elevated prolactin;
Galactorrhea;
GYNECOMASTIA 😜
Irreversible tardiness dyskinesia

56

Contraindications in Reglan

Allergy
Concurrent use of drugs capable of causing EPS/TD

57

Reglan in pregnancy and breastfeeding?

Safe in pregnancy; off-label use in peds; not safe in breast feeding

58

Other thoughts about Reglan and drug / drug interactions:

Do not use Reglan and Compazine together related to both act on dopamine receptors

59

Constipation fun facts

= decreased passage of stool, straining, pellet-like stools,unable to pass
Causes can be related to MEDS, MEALS, Or METS (side effects, diet, tumors)
**MIRAlax= first line of TX

60

Even funner diarrhea facts

= loose liquid stools / defined as 3 + / day
Causes:
Infections
Meds
Inflammatory bowel diseases

61

Antidiarrheals: opioid agonists
(Loperamide /Immodium)
MOA?

Slows intestinal motility through opioid receptor activation, also reduces fecal volume and increases viscosity

62

Antidiarrheal
Pharmacokinetics

-little po absorption
-significant first pass metab**
-excreted in stool

63

Adverse effects of antidiarrheals:

Fatigue, dizziness, constipation, nausea

64

Contraindications for antidiarrheals:

High fever
Bloody diarrhea
Acute UC flare
Age les than 2 yo

65

Pregnancy and antidiarrheals?

Safe in pregnancy unknown if distributed in breastmilk

66

Irritable Bowel Syndrome Basics

= functional GI DISORDER; no identifiable causes
>>Dx of exclusion, once other GI problems ruled out
3 types:
1. Diarrhea -predominant
2. Constipation-predominant
3. Mixed
Tx>> often lifestyle modifications, but some meds available

67

Meds for Irritable Bowel Syndrome

1. Antispasmodics
2. 5HT3 antagonists

68

Antispasmodics for Irritable Bowel Syndrome:
MOA?

Dicyclomine, hyoscyamine
"Levsin"*** can be used in all 3 presentations of IBS!***
-inhibits cholinergic receptors on smooth muscle
-not specific to GI smooth muscle so at high doses have significant anti cholinergic side effects (dry mouth, dry mucous, urinary retention...it is NON selective)

69

5HT3 antagonist (Alosetron/ Lotronex)
MOA?

Modulates enteric nervous system slows GI activity
**for diarrhea-predominant IBS ONLY**

70

Inflammatory Bowel Disease:
What two diseases make up this category?

1. Crohn's Disease "TOP TO BOTTOM" can affect any portion of GI TRACT
2. Ulcerative Colitis (COLON ONLY)

71

What is the first line of TX For Inflammatory Bowel Disease?

Steroid

72

For inflammatory bowel disease, remission maintenance meds =

First line is Aminosalicylates;
immunomodulators becoming popular because may allow pt to avoid a steroid

73

For Inflammatory Bowel- acute phase med & MOA

GLUCOCORTICOIDS FOR ACUTE FLARE
MOA= anti-inflammatory corticosteroids, reduces inflammation by suppressing migration of polymorphonuclear leukocyte so, decreases prostaglandin synthesis

74

Glucocorticoid-
Pharmacokinetics

-not well absorbed, Enterocort has max 21% bioavailability
-metabolized extensively in liver
-excreted in urine

75

Glucocorticoid
Adverse effects

H/A, N/V

76

Contraindications
Glucocorticoid

Allergy

77

Glucocorticoids in Irritable Bowel Syndrome:
What phase again?

ACUTE PHASE NOT FOR DISEASE REMISSION

78

Enterocort- 2 facts:

1. High fat meal will delay Enterocort absorption
2. Rectal preparations are the first line for UC FLARE

79

Inflammatory Bowel Disease:
Maintenance meds are called- and MOA-

sulfasalazine (Azulfidine), mesalamine (ASACOL! ☎️! Your ass is calling!), balsalazide (Cozaal)
MOA is uncertain with these meds but thought to block prostaglandin synthesis,may also inhibit cellular functions of NK Cells, mucosal lymphocytes and macrophages

80

Aminosalicylates
Pharmacokinetics

Well absorbed in small intestine but not much colonic absorption
Up to 78% protein bound
Metab via liver
Excreted via stool

81

Aminosalicylates
Adverse effects

nausea, GI upset, H/A, **bone marrow suppression** ( leukopenia, anemia, thrombocytopenia)

82

Given that Aminosalicylates can cause bone marrow suppression, how can a provider determine if this is a med-related adverse event?

Establish a timeline- when started drug RX vs. when abnormal labs began

83

Inflammatory Bowel Disease: meds,MOA

Azathioprine (imuran), 6-MP (purinethol)
MOA: leads to immunocompromise, reduces immune response. Does this by blocking synthesis of purine, which then hinders DNA, RNA, and protein synthesis in fast growing cells like lymphocytes

84

Purine Analogs: pharmacokinetics

Imuran better absorbed than 6 MP
APPROX 30% protein bound
Metab via liver
Excreted via urine

85

Purine Analogs: adverse effects

**PANCYTOPENIA**, infection, hepatotoxicity, pancreatitis

86

Purine Analogs: contraindications

Pregnancy, breastfeeding;
Active malignancy

87

Long term use of purine analogs can lead to

Malignancies, especially lymphoma

88

Acid Reflux/ Gastritis:
prevalence, probable causes?

Very prevalent (10%) US pop
Several probable causes:
1. Transient lower esophageal sphincter relaxtion
2. Low resting lower esophageal sphincter
3. Poor esophageal acid clearance
4. Defects in esophagastric motility
5. Impaired mucosal resistance and over protective defenses

89

Descriptions and symptoms of gastritis

Burning sensation, nausea, chest pain, or globus (broad) sensation.
* can be very much like an MI ; differentiating SX - SOB, diaphoresis

90

Other contributing factors to gastritis?

Intake of acidic foods; treatment begins with removing these offenders / lifestyle modifications then mess

91

4 Types acid reflux/ gastritis meds

1. Antacids
2. Carafate
3. H2 receptor antagonists
4. PPI's

92

Antacids: sodium bicarbonate, calcium carbonate, magnesium hydroxide, aluminum hydroxide
MOA?

These are weak bases that fact with gastric acid to form a salt and water, therefore decreasing gastric acidity

93

Pharmokinetics/ dynamics of antacids

-Some po absorption; 25-35 % availability
-bicarbonate preps (bioavailability) improves with food bu hydroxide preparations poorly absorbed
-carbonate excreted via stool
-aluminum and mag excreted via urine

94

Pregnancy category of antacids

B, safe for breastfeeding as well

95

Antacids: adverse effects

N/V, constipation, dependence

96

Contraindications for taking antacids:

Renal Failure (for those with aluminum and magnesium) - ie, the re ally excreted ones

97

Carafate: MOA

Positively charged sucrose sulfate binds to negatively charged proteins in base of ulcers, forms an ADHERENT/ PROTECTIVE barrier from gastric acids and bile salts

98

Carafate: pharmacokinetics

-very little absorption, so not metabolized
-excreted in stool

99

Carafate: adverse effects

CONSTIPATION! Gotta love it!

100

Contraindications for use of Carafate-

Allergy; may use with caution with other meds... Can affect absorption

101

Carafate pregnancy category:

B ( off label for peds)

102

H2 receptor antagonists: Zantac, Pepcid, Tagamet
MOA?

Competitive inhibitors of H2 receptors in gastric parietal cells causing a decrease in gastric acid. No H1 or H3 efficacy (therefore not sedating).

103

H2 receptor antagonists: pharmacokinetics

-good po absorption
-metabolized via liver
-excreted in urine

104

H2 receptor antagonists
Adverse Effects

H/A, dizziness, confusion in elderly,
.....GYNECOMASTIA (for real!?!?!)

105

H2 receptor antagonists- contraindications

Potent P450 inhibitor!
Use Tagamet with caution in elderly

106

Pregnancy category for H2 receptor antagonists

B - also safe in peds

107

Proton Pump Inhibitors- Prilosec / omeprazole, Prevacid / lansoprazole, Protonix / pantoprazole, Nexium/ esomeprazole
MOA?

Binds irreversibly to H+/ K+ exchanging ATPase pumps (proton pumps) in gastric parietal cells, decreasing both basal and stimulated gastric acid secretion

108

PPI's: pharmacokinetics/ dynamics

-PRODRUG: must survive the acidic environment of stomach to be absorbed into small bowel
-all have fairly good bioavailability, decreased with po intake
-metab in liver / inhibits CYP2C19
-excreted in stool; **dose-adjust for hepatic disease**
-little renal excretion

109

PPI's: adverse effects

H/A, diarrhea, constipation, nausea, increased risk C. diff infection, ⬇️Mg with prolonged use,
⬆️ risk osteoporosis-related fractures with prolonged use

110

PPI's: contraindications

Allergy

111

Types of laxatives:

1. Bulk (Metamucil, fibercon)
2. Osmotic laxatives ( milk of mag, lactulose, mg citrate, polyethylene glycol (miralax)

112

Osmotic laxatives MOA:

Causes water retention in stool; soluble but no absorbable compounds

113

Pharmacokinetics of osmotic laxatives

NO PO absorption/ excreted in stool unchanged

114

Adverse effects of osmotic laxatives:

Diarrhea
abdominal complaints

115

Contraindications of osmotic laxatives:

-Existing electrolyte abnormality
-Age under 2 yo

116

Osmotic laxatives: great option for long or short term relief?

No adverse effects shown up to 12 months of daily use

117

Bulk laxatives - MOA?
Pharmacokinetics

Absorb water and enlarge stools which stimulates propulsive movement through the lower GI tract
-no po absorption; excreted through stool as unchanged drug

118

Adverse effects of bulk laxatives:

N/V, abdominal fullness

119

Contraindications of bulk laxatives:

Bowel obstruction, under age of 6

120

Pregnancy Category bulk laxatives

B; safe in pregnancy and breastfeeding

121

Gastric motility agent (Metoclopramide/ Reglan) MOA

Binds to dopamine D2 receptors in CNS, as well as some 5-HT3 antagonism: gastric motility is caused by the D2 antagonism

122

Reglan: pharmacokinetics

Well-absorbed PO, 65-90% bioavailability
Metabolized via liver
Excreted via urine (decrease dose in renal insufficiency

123

Acid Reflux/ Gastritis:
prevalence, probable causes?

Very prevalent (10%) US pop
Several probable causes:
1. Transient lower esophageal sphincter relaxtion
2. Low resting lower esophageal sphincter
3. Poor esophageal acid clearance
4. Defects in esophagastric motility
5. Impaired mucosal resistance and over protective defenses

124

Descriptions and symptoms of gastritis

Burning sensation, nausea, chest pain, or globus (broad) sensation.
* can be very much like an MI ; differentiating SX - SOB, diaphoresis

125

Other contributing factors to gastritis?

Intake of acidic foods; treatment begins with removing these offenders / lifestyle modifications then mess

126

4 Types acid reflux/ gastritis meds

1. Antacids
2. Carafate
3. H2 receptor antagonists
4. PPI's

127

Antacids: sodium bicarbonate, calcium carbonate, magnesium hydroxide, aluminum hydroxide
MOA?

These are weak bases that fact with gastric acid to form a salt and water, therefore decreasing gastric acidity

128

Pharmokinetics/ dynamics of antacids

-Some po absorption; 25-35 % availability
-bicarbonate preps (bioavailability) improves with food bu hydroxide preparations poorly absorbed
-carbonate excreted via stool
-aluminum and mag excreted via urine

129

Pregnancy category of antacids

B, safe for breastfeeding as well

130

Antacids: adverse effects

N/V, constipation, dependence

131

Contraindications for taking antacids:

Renal Failure (for those with aluminum and magnesium) - ie, the re ally excreted ones

132

Carafate: MOA

Positively charged sucrose sulfate binds to negatively charged proteins in base of ulcers, forms an ADHERENT/ PROTECTIVE barrier from gastric acids and bile salts

133

Carafate: pharmacokinetics

-very little absorption, so not metabolized
-excreted in stool

134

Carafate: adverse effects

CONSTIPATION! Gotta love it!

135

Contraindications for use of Carafate-

Allergy; may use with caution with other meds... Can affect absorption

136

Carafate pregnancy category:

B ( off label for peds)

137

H2 receptor antagonists: Zantac, Pepcid, Tagamet
MOA?

Competitive inhibitors of H2 receptors in gastric parietal cells causing a decrease in gastric acid. No H1 or H3 efficacy (therefore not sedating).

138

H2 receptor antagonists: pharmacokinetics

-good po absorption
-metabolized via liver
-excreted in urine

139

H2 receptor antagonists
Adverse Effects

H/A, dizziness, confusion in elderly,
.....GYNECOMASTIA (for real!?!?!)

140

H2 receptor antagonists- contraindications

Potent P450 inhibitor!
Use Tagamet with caution in elderly

141

Pregnancy category for H2 receptor antagonists

B - also safe in peds

142

Proton Pump Inhibitors- Prilosec / omeprazole, Prevacid / lansoprazole, Protonix / pantoprazole, Nexium/ esomeprazole
MOA?

Binds irreversibly to H+/ K+ exchanging ATPase pumps (proton pumps) in gastric parietal cells, decreasing both basal and stimulated gastric acid secretion

143

PPI's: pharmacokinetics/ dynamics

-PRODRUG: must survive the acidic environment of stomach to be absorbed into small bowel
-all have fairly good bioavailability, decreased with po intake
-metab in liver / inhibits CYP2C19
-excreted in stool; **dose-adjust for hepatic disease**
-little renal excretion

144

PPI's: adverse effects

H/A, diarrhea, constipation, nausea, increased risk C. diff infection, ⬇️Mg with prolonged use,
⬆️ risk osteoporosis-related fractures with prolonged use

145

PPI's: contraindications

Allergy

146

Types of laxatives:

1. Bulk (Metamucil, fibercon)
2. Osmotic laxatives ( milk of mag, lactulose, mg citrate, polyethylene glycol (miralax)

147

Osmotic laxatives MOA:

Causes water retention in stool; soluble but no absorbable compounds

148

Pharmacokinetics of osmotic laxatives

NO PO absorption/ excreted in stool unchanged

149

Adverse effects of osmotic laxatives:

Diarrhea
abdominal complaints

150

Contraindications of osmotic laxatives:

-Existing electrolyte abnormality
-Age under 2 yo

151

Osmotic laxatives: great option for long or short term relief?

No adverse effects shown up to 12 months of daily use

152

Bulk laxatives - MOA?
Pharmacokinetics

Absorb water and enlarge stools which stimulates propulsive movement through the lower GI tract
-no po absorption; excreted through stool as unchanged drug

153

Adverse effects of bulk laxatives:

N/V, abdominal fullness

154

Contraindications of bulk laxatives:

Bowel obstruction, under age of 6

155

Pregnancy Category bulk laxatives

B; safe in pregnancy and breastfeeding

156

Gastric motility agent (Metoclopramide/ Reglan) MOA

Binds to dopamine D2 receptors in CNS, as well as some 5-HT3 antagonism: gastric motility is caused by the D2 antagonism

157

Reglan: pharmacokinetics

Well-absorbed PO, 65-90% bioavailability
Metabolized via liver
Excreted via urine (decrease dose in renal insufficiency

158

Acid Reflux/ Gastritis:
prevalence, probable causes?

Very prevalent (10%) US pop
Several probable causes:
1. Transient lower esophageal sphincter relaxtion
2. Low resting lower esophageal sphincter
3. Poor esophageal acid clearance
4. Defects in esophagastric motility
5. Impaired mucosal resistance and over protective defenses

159

Descriptions and symptoms of gastritis

Burning sensation, nausea, chest pain, or globus (broad) sensation.
* can be very much like an MI ; differentiating SX - SOB, diaphoresis

160

Other contributing factors to gastritis?

Intake of acidic foods; treatment begins with removing these offenders / lifestyle modifications then mess

161

4 Types acid reflux/ gastritis meds

1. Antacids
2. Carafate
3. H2 receptor antagonists
4. PPI's

162

Antacids: sodium bicarbonate, calcium carbonate, magnesium hydroxide, aluminum hydroxide
MOA?

These are weak bases that fact with gastric acid to form a salt and water, therefore decreasing gastric acidity

163

Pharmokinetics/ dynamics of antacids

-Some po absorption; 25-35 % availability
-bicarbonate preps (bioavailability) improves with food bu hydroxide preparations poorly absorbed
-carbonate excreted via stool
-aluminum and mag excreted via urine

164

Pregnancy category of antacids

B, safe for breastfeeding as well

165

Antacids: adverse effects

N/V, constipation, dependence

166

Contraindications for taking antacids:

Renal Failure (for those with aluminum and magnesium) - ie, the re ally excreted ones

167

Carafate: MOA

Positively charged sucrose sulfate binds to negatively charged proteins in base of ulcers, forms an ADHERENT/ PROTECTIVE barrier from gastric acids and bile salts

168

Carafate: pharmacokinetics

-very little absorption, so not metabolized
-excreted in stool

169

Carafate: adverse effects

CONSTIPATION! Gotta love it!

170

Contraindications for use of Carafate-

Allergy; may use with caution with other meds... Can affect absorption

171

Carafate pregnancy category:

B ( off label for peds)

172

H2 receptor antagonists: Zantac, Pepcid, Tagamet
MOA?

Competitive inhibitors of H2 receptors in gastric parietal cells causing a decrease in gastric acid. No H1 or H3 efficacy (therefore not sedating).

173

H2 receptor antagonists: pharmacokinetics

-good po absorption
-metabolized via liver
-excreted in urine

174

H2 receptor antagonists
Adverse Effects

H/A, dizziness, confusion in elderly,
.....GYNECOMASTIA (for real!?!?!)

175

H2 receptor antagonists- contraindications

Potent P450 inhibitor!
Use Tagamet with caution in elderly

176

Pregnancy category for H2 receptor antagonists

B - also safe in peds

177

Proton Pump Inhibitors- Prilosec / omeprazole, Prevacid / lansoprazole, Protonix / pantoprazole, Nexium/ esomeprazole
MOA?

Binds irreversibly to H+/ K+ exchanging ATPase pumps (proton pumps) in gastric parietal cells, decreasing both basal and stimulated gastric acid secretion

178

PPI's: pharmacokinetics/ dynamics

-PRODRUG: must survive the acidic environment of stomach to be absorbed into small bowel
-all have fairly good bioavailability, decreased with po intake
-metab in liver / inhibits CYP2C19
-excreted in stool; **dose-adjust for hepatic disease**
-little renal excretion

179

PPI's: adverse effects

H/A, diarrhea, constipation, nausea, increased risk C. diff infection, ⬇️Mg with prolonged use,
⬆️ risk osteoporosis-related fractures with prolonged use

180

PPI's: contraindications

Allergy

181

Types of laxatives:

1. Bulk (Metamucil, fibercon)
2. Osmotic laxatives ( milk of mag, lactulose, mg citrate, polyethylene glycol (miralax)

182

Osmotic laxatives MOA:

Causes water retention in stool; soluble but no absorbable compounds

183

Pharmacokinetics of osmotic laxatives

NO PO absorption/ excreted in stool unchanged

184

Adverse effects of osmotic laxatives:

Diarrhea
abdominal complaints

185

Contraindications of osmotic laxatives:

-Existing electrolyte abnormality
-Age under 2 yo

186

Osmotic laxatives: great option for long or short term relief?

No adverse effects shown up to 12 months of daily use

187

Bulk laxatives - MOA?
Pharmacokinetics

Absorb water and enlarge stools which stimulates propulsive movement through the lower GI tract
-no po absorption; excreted through stool as unchanged drug

188

Adverse effects of bulk laxatives:

N/V, abdominal fullness

189

Contraindications of bulk laxatives:

Bowel obstruction, under age of 6

190

Pregnancy Category bulk laxatives

B; safe in pregnancy and breastfeeding

191

Gastric motility agent (Metoclopramide/ Reglan) MOA

Binds to dopamine D2 receptors in CNS, as well as some 5-HT3 antagonism: gastric motility is caused by the D2 antagonism

192

Reglan: pharmacokinetics

Well-absorbed PO, 65-90% bioavailability
Metabolized via liver
Excreted via urine (decrease dose in renal insufficiency

193

Acid Reflux/ Gastritis:
prevalence, probable causes?

Very prevalent (10%) US pop
Several probable causes:
1. Transient lower esophageal sphincter relaxtion
2. Low resting lower esophageal sphincter
3. Poor esophageal acid clearance
4. Defects in esophagastric motility
5. Impaired mucosal resistance and over protective defenses

194

Descriptions and symptoms of gastritis

Burning sensation, nausea, chest pain, or globus (broad) sensation.
* can be very much like an MI ; differentiating SX - SOB, diaphoresis

195

Other contributing factors to gastritis?

Intake of acidic foods; treatment begins with removing these offenders / lifestyle modifications then mess

196

4 Types acid reflux/ gastritis meds

1. Antacids
2. Carafate
3. H2 receptor antagonists
4. PPI's

197

Antacids: sodium bicarbonate, calcium carbonate, magnesium hydroxide, aluminum hydroxide
MOA?

These are weak bases that fact with gastric acid to form a salt and water, therefore decreasing gastric acidity

198

Pharmokinetics/ dynamics of antacids

-Some po absorption; 25-35 % availability
-bicarbonate preps (bioavailability) improves with food bu hydroxide preparations poorly absorbed
-carbonate excreted via stool
-aluminum and mag excreted via urine

199

Pregnancy category of antacids

B, safe for breastfeeding as well

200

Antacids: adverse effects

N/V, constipation, dependence

201

Contraindications for taking antacids:

Renal Failure (for those with aluminum and magnesium) - ie, the re ally excreted ones

202

Carafate: MOA

Positively charged sucrose sulfate binds to negatively charged proteins in base of ulcers, forms an ADHERENT/ PROTECTIVE barrier from gastric acids and bile salts

203

Carafate: pharmacokinetics

-very little absorption, so not metabolized
-excreted in stool

204

Carafate: adverse effects

CONSTIPATION! Gotta love it!

205

Contraindications for use of Carafate-

Allergy; may use with caution with other meds... Can affect absorption

206

Carafate pregnancy category:

B ( off label for peds)

207

H2 receptor antagonists: Zantac, Pepcid, Tagamet
MOA?

Competitive inhibitors of H2 receptors in gastric parietal cells causing a decrease in gastric acid. No H1 or H3 efficacy (therefore not sedating).

208

H2 receptor antagonists: pharmacokinetics

-good po absorption
-metabolized via liver
-excreted in urine

209

H2 receptor antagonists
Adverse Effects

H/A, dizziness, confusion in elderly,
.....GYNECOMASTIA (for real!?!?!)

210

H2 receptor antagonists- contraindications

Potent P450 inhibitor!
Use Tagamet with caution in elderly

211

Pregnancy category for H2 receptor antagonists

B - also safe in peds

212

Proton Pump Inhibitors- Prilosec / omeprazole, Prevacid / lansoprazole, Protonix / pantoprazole, Nexium/ esomeprazole
MOA?

Binds irreversibly to H+/ K+ exchanging ATPase pumps (proton pumps) in gastric parietal cells, decreasing both basal and stimulated gastric acid secretion

213

PPI's: pharmacokinetics/ dynamics

-PRODRUG: must survive the acidic environment of stomach to be absorbed into small bowel
-all have fairly good bioavailability, decreased with po intake
-metab in liver / inhibits CYP2C19
-excreted in stool; **dose-adjust for hepatic disease**
-little renal excretion

214

PPI's: adverse effects

H/A, diarrhea, constipation, nausea, increased risk C. diff infection, ⬇️Mg with prolonged use,
⬆️ risk osteoporosis-related fractures with prolonged use

215

PPI's: contraindications

Allergy

216

Types of laxatives:

1. Bulk (Metamucil, fibercon)
2. Osmotic laxatives ( milk of mag, lactulose, mg citrate, polyethylene glycol (miralax)

217

Osmotic laxatives MOA:

Causes water retention in stool; soluble but no absorbable compounds

218

Pharmacokinetics of osmotic laxatives

NO PO absorption/ excreted in stool unchanged

219

Adverse effects of osmotic laxatives:

Diarrhea
abdominal complaints

220

Contraindications of osmotic laxatives:

-Existing electrolyte abnormality
-Age under 2 yo

221

Osmotic laxatives: great option for long or short term relief?

No adverse effects shown up to 12 months of daily use

222

Bulk laxatives - MOA?
Pharmacokinetics

Absorb water and enlarge stools which stimulates propulsive movement through the lower GI tract
-no po absorption; excreted through stool as unchanged drug

223

Adverse effects of bulk laxatives:

N/V, abdominal fullness

224

Contraindications of bulk laxatives:

Bowel obstruction, under age of 6

225

Pregnancy Category bulk laxatives

B; safe in pregnancy and breastfeeding

226

Gastric motility agent (Metoclopramide/ Reglan) MOA

Binds to dopamine D2 receptors in CNS, as well as some 5-HT3 antagonism: gastric motility is caused by the D2 antagonism

227

Reglan: pharmacokinetics

Well-absorbed PO, 65-90% bioavailability
Metabolized via liver
Excreted via urine (decrease dose in renal insufficiency

228

Acid Reflux/ Gastritis:
prevalence, probable causes?

Very prevalent (10%) US pop
Several probable causes:
1. Transient lower esophageal sphincter relaxtion
2. Low resting lower esophageal sphincter
3. Poor esophageal acid clearance
4. Defects in esophagastric motility
5. Impaired mucosal resistance and over protective defenses

229

Descriptions and symptoms of gastritis

Burning sensation, nausea, chest pain, or globus (broad) sensation.
* can be very much like an MI ; differentiating SX - SOB, diaphoresis

230

Other contributing factors to gastritis?

Intake of acidic foods; treatment begins with removing these offenders / lifestyle modifications then mess

231

4 Types acid reflux/ gastritis meds

1. Antacids
2. Carafate
3. H2 receptor antagonists
4. PPI's

232

Antacids: sodium bicarbonate, calcium carbonate, magnesium hydroxide, aluminum hydroxide
MOA?

These are weak bases that fact with gastric acid to form a salt and water, therefore decreasing gastric acidity

233

Pharmokinetics/ dynamics of antacids

-Some po absorption; 25-35 % availability
-bicarbonate preps (bioavailability) improves with food bu hydroxide preparations poorly absorbed
-carbonate excreted via stool
-aluminum and mag excreted via urine

234

Pregnancy category of antacids

B, safe for breastfeeding as well

235

Antacids: adverse effects

N/V, constipation, dependence

236

Contraindications for taking antacids:

Renal Failure (for those with aluminum and magnesium) - ie, the re ally excreted ones

237

Carafate: MOA

Positively charged sucrose sulfate binds to negatively charged proteins in base of ulcers, forms an ADHERENT/ PROTECTIVE barrier from gastric acids and bile salts

238

Carafate: pharmacokinetics

-very little absorption, so not metabolized
-excreted in stool

239

Carafate: adverse effects

CONSTIPATION! Gotta love it!

240

Contraindications for use of Carafate-

Allergy; may use with caution with other meds... Can affect absorption

241

Carafate pregnancy category:

B ( off label for peds)

242

H2 receptor antagonists: Zantac, Pepcid, Tagamet
MOA?

Competitive inhibitors of H2 receptors in gastric parietal cells causing a decrease in gastric acid. No H1 or H3 efficacy (therefore not sedating).

243

H2 receptor antagonists: pharmacokinetics

-good po absorption
-metabolized via liver
-excreted in urine

244

H2 receptor antagonists
Adverse Effects

H/A, dizziness, confusion in elderly,
.....GYNECOMASTIA (for real!?!?!)

245

H2 receptor antagonists- contraindications

Potent P450 inhibitor!
Use Tagamet with caution in elderly

246

Pregnancy category for H2 receptor antagonists

B - also safe in peds

247

Proton Pump Inhibitors- Prilosec / omeprazole, Prevacid / lansoprazole, Protonix / pantoprazole, Nexium/ esomeprazole
MOA?

Binds irreversibly to H+/ K+ exchanging ATPase pumps (proton pumps) in gastric parietal cells, decreasing both basal and stimulated gastric acid secretion

248

PPI's: pharmacokinetics/ dynamics

-PRODRUG: must survive the acidic environment of stomach to be absorbed into small bowel
-all have fairly good bioavailability, decreased with po intake
-metab in liver / inhibits CYP2C19
-excreted in stool; **dose-adjust for hepatic disease**
-little renal excretion

249

PPI's: adverse effects

H/A, diarrhea, constipation, nausea, increased risk C. diff infection, ⬇️Mg with prolonged use,
⬆️ risk osteoporosis-related fractures with prolonged use

250

PPI's: contraindications

Allergy

251

Types of laxatives:

1. Bulk (Metamucil, fibercon)
2. Osmotic laxatives ( milk of mag, lactulose, mg citrate, polyethylene glycol (miralax)

252

Osmotic laxatives MOA:

Causes water retention in stool; soluble but no absorbable compounds

253

Pharmacokinetics of osmotic laxatives

NO PO absorption/ excreted in stool unchanged

254

Adverse effects of osmotic laxatives:

Diarrhea
abdominal complaints

255

Contraindications of osmotic laxatives:

-Existing electrolyte abnormality
-Age under 2 yo

256

Osmotic laxatives: great option for long or short term relief?

No adverse effects shown up to 12 months of daily use

257

Bulk laxatives - MOA?
Pharmacokinetics

Absorb water and enlarge stools which stimulates propulsive movement through the lower GI tract
-no po absorption; excreted through stool as unchanged drug

258

Adverse effects of bulk laxatives:

N/V, abdominal fullness

259

Contraindications of bulk laxatives:

Bowel obstruction, under age of 6

260

Pregnancy Category bulk laxatives

B; safe in pregnancy and breastfeeding

261

Gastric motility agent (Metoclopramide/ Reglan) MOA

Binds to dopamine D2 receptors in CNS, as well as some 5-HT3 antagonism: gastric motility is caused by the D2 antagonism

262

Reglan: pharmacokinetics

Well-absorbed PO, 65-90% bioavailability
Metabolized via liver
Excreted via urine (decrease dose in renal insufficiency

263

Acid Reflux/ Gastritis:
prevalence, probable causes?

Very prevalent (10%) US pop
Several probable causes:
1. Transient lower esophageal sphincter relaxtion
2. Low resting lower esophageal sphincter
3. Poor esophageal acid clearance
4. Defects in esophagastric motility
5. Impaired mucosal resistance and over protective defenses

264

Descriptions and symptoms of gastritis

Burning sensation, nausea, chest pain, or globus (broad) sensation.
* can be very much like an MI ; differentiating SX - SOB, diaphoresis

265

Other contributing factors to gastritis?

Intake of acidic foods; treatment begins with removing these offenders / lifestyle modifications then mess

266

4 Types acid reflux/ gastritis meds

1. Antacids
2. Carafate
3. H2 receptor antagonists
4. PPI's

267

Antacids: sodium bicarbonate, calcium carbonate, magnesium hydroxide, aluminum hydroxide
MOA?

These are weak bases that fact with gastric acid to form a salt and water, therefore decreasing gastric acidity

268

Pharmokinetics/ dynamics of antacids

-Some po absorption; 25-35 % availability
-bicarbonate preps (bioavailability) improves with food bu hydroxide preparations poorly absorbed
-carbonate excreted via stool
-aluminum and mag excreted via urine

269

Pregnancy category of antacids

B, safe for breastfeeding as well

270

Antacids: adverse effects

N/V, constipation, dependence

271

Contraindications for taking antacids:

Renal Failure (for those with aluminum and magnesium) - ie, the re ally excreted ones

272

Carafate: MOA

Positively charged sucrose sulfate binds to negatively charged proteins in base of ulcers, forms an ADHERENT/ PROTECTIVE barrier from gastric acids and bile salts

273

Carafate: pharmacokinetics

-very little absorption, so not metabolized
-excreted in stool

274

Carafate: adverse effects

CONSTIPATION! Gotta love it!

275

Contraindications for use of Carafate-

Allergy; may use with caution with other meds... Can affect absorption

276

Carafate pregnancy category:

B ( off label for peds)

277

H2 receptor antagonists: Zantac, Pepcid, Tagamet
MOA?

Competitive inhibitors of H2 receptors in gastric parietal cells causing a decrease in gastric acid. No H1 or H3 efficacy (therefore not sedating).

278

H2 receptor antagonists: pharmacokinetics

-good po absorption
-metabolized via liver
-excreted in urine

279

H2 receptor antagonists
Adverse Effects

H/A, dizziness, confusion in elderly,
.....GYNECOMASTIA (for real!?!?!)

280

H2 receptor antagonists- contraindications

Potent P450 inhibitor!
Use Tagamet with caution in elderly

281

Pregnancy category for H2 receptor antagonists

B - also safe in peds

282

Proton Pump Inhibitors- Prilosec / omeprazole, Prevacid / lansoprazole, Protonix / pantoprazole, Nexium/ esomeprazole
MOA?

Binds irreversibly to H+/ K+ exchanging ATPase pumps (proton pumps) in gastric parietal cells, decreasing both basal and stimulated gastric acid secretion

283

PPI's: pharmacokinetics/ dynamics

-PRODRUG: must survive the acidic environment of stomach to be absorbed into small bowel
-all have fairly good bioavailability, decreased with po intake
-metab in liver / inhibits CYP2C19
-excreted in stool; **dose-adjust for hepatic disease**
-little renal excretion

284

PPI's: adverse effects

H/A, diarrhea, constipation, nausea, increased risk C. diff infection, ⬇️Mg with prolonged use,
⬆️ risk osteoporosis-related fractures with prolonged use

285

PPI's: contraindications

Allergy

286

Types of laxatives:

1. Bulk (Metamucil, fibercon)
2. Osmotic laxatives ( milk of mag, lactulose, mg citrate, polyethylene glycol (miralax)

287

Osmotic laxatives MOA:

Causes water retention in stool; soluble but no absorbable compounds

288

Pharmacokinetics of osmotic laxatives

NO PO absorption/ excreted in stool unchanged

289

Adverse effects of osmotic laxatives:

Diarrhea
abdominal complaints

290

Contraindications of osmotic laxatives:

-Existing electrolyte abnormality
-Age under 2 yo

291

Osmotic laxatives: great option for long or short term relief?

No adverse effects shown up to 12 months of daily use

292

Bulk laxatives - MOA?
Pharmacokinetics

Absorb water and enlarge stools which stimulates propulsive movement through the lower GI tract
-no po absorption; excreted through stool as unchanged drug

293

Adverse effects of bulk laxatives:

N/V, abdominal fullness

294

Contraindications of bulk laxatives:

Bowel obstruction, under age of 6

295

Pregnancy Category bulk laxatives

B; safe in pregnancy and breastfeeding

296

Gastric motility agent (Metoclopramide/ Reglan) MOA

Binds to dopamine D2 receptors in CNS, as well as some 5-HT3 antagonism: gastric motility is caused by the D2 antagonism

297

Reglan: pharmacokinetics

Well-absorbed PO, 65-90% bioavailability
Metabolized via liver
Excreted via urine (decrease dose in renal insufficiency

298

Acid Reflux/ Gastritis:
prevalence, probable causes?

Very prevalent (10%) US pop
Several probable causes:
1. Transient lower esophageal sphincter relaxtion
2. Low resting lower esophageal sphincter
3. Poor esophageal acid clearance
4. Defects in esophagastric motility
5. Impaired mucosal resistance and over protective defenses

299

Descriptions and symptoms of gastritis

Burning sensation, nausea, chest pain, or globus (broad) sensation.
* can be very much like an MI ; differentiating SX - SOB, diaphoresis

300

Other contributing factors to gastritis?

Intake of acidic foods; treatment begins with removing these offenders / lifestyle modifications then mess

301

4 Types acid reflux/ gastritis meds

1. Antacids
2. Carafate
3. H2 receptor antagonists
4. PPI's

302

Antacids: sodium bicarbonate, calcium carbonate, magnesium hydroxide, aluminum hydroxide
MOA?

These are weak bases that fact with gastric acid to form a salt and water, therefore decreasing gastric acidity

303

Pharmokinetics/ dynamics of antacids

-Some po absorption; 25-35 % availability
-bicarbonate preps (bioavailability) improves with food bu hydroxide preparations poorly absorbed
-carbonate excreted via stool
-aluminum and mag excreted via urine

304

Pregnancy category of antacids

B, safe for breastfeeding as well

305

Antacids: adverse effects

N/V, constipation, dependence

306

Contraindications for taking antacids:

Renal Failure (for those with aluminum and magnesium) - ie, the re ally excreted ones

307

Carafate: MOA

Positively charged sucrose sulfate binds to negatively charged proteins in base of ulcers, forms an ADHERENT/ PROTECTIVE barrier from gastric acids and bile salts

308

Carafate: pharmacokinetics

-very little absorption, so not metabolized
-excreted in stool

309

Carafate: adverse effects

CONSTIPATION! Gotta love it!

310

Contraindications for use of Carafate-

Allergy; may use with caution with other meds... Can affect absorption

311

Carafate pregnancy category:

B ( off label for peds)

312

H2 receptor antagonists: Zantac, Pepcid, Tagamet
MOA?

Competitive inhibitors of H2 receptors in gastric parietal cells causing a decrease in gastric acid. No H1 or H3 efficacy (therefore not sedating).

313

H2 receptor antagonists: pharmacokinetics

-good po absorption
-metabolized via liver
-excreted in urine

314

H2 receptor antagonists
Adverse Effects

H/A, dizziness, confusion in elderly,
.....GYNECOMASTIA (for real!?!?!)

315

H2 receptor antagonists- contraindications

Potent P450 inhibitor!
Use Tagamet with caution in elderly

316

Pregnancy category for H2 receptor antagonists

B - also safe in peds

317

Proton Pump Inhibitors- Prilosec / omeprazole, Prevacid / lansoprazole, Protonix / pantoprazole, Nexium/ esomeprazole
MOA?

Binds irreversibly to H+/ K+ exchanging ATPase pumps (proton pumps) in gastric parietal cells, decreasing both basal and stimulated gastric acid secretion

318

PPI's: pharmacokinetics/ dynamics

-PRODRUG: must survive the acidic environment of stomach to be absorbed into small bowel
-all have fairly good bioavailability, decreased with po intake
-metab in liver / inhibits CYP2C19
-excreted in stool; **dose-adjust for hepatic disease**
-little renal excretion

319

PPI's: adverse effects

H/A, diarrhea, constipation, nausea, increased risk C. diff infection, ⬇️Mg with prolonged use,
⬆️ risk osteoporosis-related fractures with prolonged use

320

PPI's: contraindications

Allergy

321

Types of laxatives:

1. Bulk (Metamucil, fibercon)
2. Osmotic laxatives ( milk of mag, lactulose, mg citrate, polyethylene glycol (miralax)

322

Osmotic laxatives MOA:

Causes water retention in stool; soluble but no absorbable compounds

323

Pharmacokinetics of osmotic laxatives

NO PO absorption/ excreted in stool unchanged

324

Adverse effects of osmotic laxatives:

Diarrhea
abdominal complaints

325

Contraindications of osmotic laxatives:

-Existing electrolyte abnormality
-Age under 2 yo

326

Osmotic laxatives: great option for long or short term relief?

No adverse effects shown up to 12 months of daily use

327

Bulk laxatives - MOA?
Pharmacokinetics

Absorb water and enlarge stools which stimulates propulsive movement through the lower GI tract
-no po absorption; excreted through stool as unchanged drug

328

Adverse effects of bulk laxatives:

N/V, abdominal fullness

329

Contraindications of bulk laxatives:

Bowel obstruction, under age of 6

330

Pregnancy Category bulk laxatives

B; safe in pregnancy and breastfeeding

331

Gastric motility agent (Metoclopramide/ Reglan) MOA

Binds to dopamine D2 receptors in CNS, as well as some 5-HT3 antagonism: gastric motility is caused by the D2 antagonism

332

Reglan: pharmacokinetics

Well-absorbed PO, 65-90% bioavailability
Metabolized via liver
Excreted via urine (decrease dose in renal insufficiency

333

Acid Reflux/ Gastritis:
prevalence, probable causes?

Very prevalent (10%) US pop
Several probable causes:
1. Transient lower esophageal sphincter relaxtion
2. Low resting lower esophageal sphincter
3. Poor esophageal acid clearance
4. Defects in esophagastric motility
5. Impaired mucosal resistance and over protective defenses

334

Descriptions and symptoms of gastritis

Burning sensation, nausea, chest pain, or globus (broad) sensation.
* can be very much like an MI ; differentiating SX - SOB, diaphoresis

335

Other contributing factors to gastritis?

Intake of acidic foods; treatment begins with removing these offenders / lifestyle modifications then mess

336

4 Types acid reflux/ gastritis meds

1. Antacids
2. Carafate
3. H2 receptor antagonists
4. PPI's

337

Antacids: sodium bicarbonate, calcium carbonate, magnesium hydroxide, aluminum hydroxide
MOA?

These are weak bases that fact with gastric acid to form a salt and water, therefore decreasing gastric acidity

338

Pharmokinetics/ dynamics of antacids

-Some po absorption; 25-35 % availability
-bicarbonate preps (bioavailability) improves with food bu hydroxide preparations poorly absorbed
-carbonate excreted via stool
-aluminum and mag excreted via urine

339

Pregnancy category of antacids

B, safe for breastfeeding as well

340

Antacids: adverse effects

N/V, constipation, dependence

341

Contraindications for taking antacids:

Renal Failure (for those with aluminum and magnesium) - ie, the re ally excreted ones

342

Carafate: MOA

Positively charged sucrose sulfate binds to negatively charged proteins in base of ulcers, forms an ADHERENT/ PROTECTIVE barrier from gastric acids and bile salts

343

Carafate: pharmacokinetics

-very little absorption, so not metabolized
-excreted in stool

344

Carafate: adverse effects

CONSTIPATION! Gotta love it!

345

Contraindications for use of Carafate-

Allergy; may use with caution with other meds... Can affect absorption

346

Carafate pregnancy category:

B ( off label for peds)

347

H2 receptor antagonists: Zantac, Pepcid, Tagamet
MOA?

Competitive inhibitors of H2 receptors in gastric parietal cells causing a decrease in gastric acid. No H1 or H3 efficacy (therefore not sedating).

348

H2 receptor antagonists: pharmacokinetics

-good po absorption
-metabolized via liver
-excreted in urine

349

H2 receptor antagonists
Adverse Effects

H/A, dizziness, confusion in elderly,
.....GYNECOMASTIA (for real!?!?!)

350

H2 receptor antagonists- contraindications

Potent P450 inhibitor!
Use Tagamet with caution in elderly

351

Pregnancy category for H2 receptor antagonists

B - also safe in peds

352

Proton Pump Inhibitors- Prilosec / omeprazole, Prevacid / lansoprazole, Protonix / pantoprazole, Nexium/ esomeprazole
MOA?

Binds irreversibly to H+/ K+ exchanging ATPase pumps (proton pumps) in gastric parietal cells, decreasing both basal and stimulated gastric acid secretion

353

PPI's: pharmacokinetics/ dynamics

-PRODRUG: must survive the acidic environment of stomach to be absorbed into small bowel
-all have fairly good bioavailability, decreased with po intake
-metab in liver / inhibits CYP2C19
-excreted in stool; **dose-adjust for hepatic disease**
-little renal excretion

354

PPI's: adverse effects

H/A, diarrhea, constipation, nausea, increased risk C. diff infection, ⬇️Mg with prolonged use,
⬆️ risk osteoporosis-related fractures with prolonged use

355

PPI's: contraindications

Allergy

356

Types of laxatives:

1. Bulk (Metamucil, fibercon)
2. Osmotic laxatives ( milk of mag, lactulose, mg citrate, polyethylene glycol (miralax)

357

Osmotic laxatives MOA:

Causes water retention in stool; soluble but no absorbable compounds

358

Pharmacokinetics of osmotic laxatives

NO PO absorption/ excreted in stool unchanged

359

Adverse effects of osmotic laxatives:

Diarrhea
abdominal complaints

360

Contraindications of osmotic laxatives:

-Existing electrolyte abnormality
-Age under 2 yo

361

Osmotic laxatives: great option for long or short term relief?

No adverse effects shown up to 12 months of daily use

362

Bulk laxatives - MOA?
Pharmacokinetics

Absorb water and enlarge stools which stimulates propulsive movement through the lower GI tract
-no po absorption; excreted through stool as unchanged drug

363

Adverse effects of bulk laxatives:

N/V, abdominal fullness

364

Contraindications of bulk laxatives:

Bowel obstruction, under age of 6

365

Pregnancy Category bulk laxatives

B; safe in pregnancy and breastfeeding

366

Gastric motility agent (Metoclopramide/ Reglan) MOA

Binds to dopamine D2 receptors in CNS, as well as some 5-HT3 antagonism: gastric motility is caused by the D2 antagonism

367

Reglan: pharmacokinetics

Well-absorbed PO, 65-90% bioavailability
Metabolized via liver
Excreted via urine (decrease dose in renal insufficiency

368

Acid Reflux/ Gastritis:
prevalence, probable causes?

Very prevalent (10%) US pop
Several probable causes:
1. Transient lower esophageal sphincter relaxtion
2. Low resting lower esophageal sphincter
3. Poor esophageal acid clearance
4. Defects in esophagastric motility
5. Impaired mucosal resistance and over protective defenses

369

Descriptions and symptoms of gastritis

Burning sensation, nausea, chest pain, or globus (broad) sensation.
* can be very much like an MI ; differentiating SX - SOB, diaphoresis

370

Other contributing factors to gastritis?

Intake of acidic foods; treatment begins with removing these offenders / lifestyle modifications then mess

371

4 Types acid reflux/ gastritis meds

1. Antacids
2. Carafate
3. H2 receptor antagonists
4. PPI's

372

Antacids: sodium bicarbonate, calcium carbonate, magnesium hydroxide, aluminum hydroxide
MOA?

These are weak bases that fact with gastric acid to form a salt and water, therefore decreasing gastric acidity

373

Pharmokinetics/ dynamics of antacids

-Some po absorption; 25-35 % availability
-bicarbonate preps (bioavailability) improves with food bu hydroxide preparations poorly absorbed
-carbonate excreted via stool
-aluminum and mag excreted via urine

374

Pregnancy category of antacids

B, safe for breastfeeding as well

375

Antacids: adverse effects

N/V, constipation, dependence

376

Contraindications for taking antacids:

Renal Failure (for those with aluminum and magnesium) - ie, the re ally excreted ones

377

Carafate: MOA

Positively charged sucrose sulfate binds to negatively charged proteins in base of ulcers, forms an ADHERENT/ PROTECTIVE barrier from gastric acids and bile salts

378

Carafate: pharmacokinetics

-very little absorption, so not metabolized
-excreted in stool

379

Carafate: adverse effects

CONSTIPATION! Gotta love it!

380

Contraindications for use of Carafate-

Allergy; may use with caution with other meds... Can affect absorption

381

Carafate pregnancy category:

B ( off label for peds)

382

H2 receptor antagonists: Zantac, Pepcid, Tagamet
MOA?

Competitive inhibitors of H2 receptors in gastric parietal cells causing a decrease in gastric acid. No H1 or H3 efficacy (therefore not sedating).

383

H2 receptor antagonists: pharmacokinetics

-good po absorption
-metabolized via liver
-excreted in urine

384

H2 receptor antagonists
Adverse Effects

H/A, dizziness, confusion in elderly,
.....GYNECOMASTIA (for real!?!?!)

385

H2 receptor antagonists- contraindications

Potent P450 inhibitor!
Use Tagamet with caution in elderly

386

Pregnancy category for H2 receptor antagonists

B - also safe in peds

387

Proton Pump Inhibitors- Prilosec / omeprazole, Prevacid / lansoprazole, Protonix / pantoprazole, Nexium/ esomeprazole
MOA?

Binds irreversibly to H+/ K+ exchanging ATPase pumps (proton pumps) in gastric parietal cells, decreasing both basal and stimulated gastric acid secretion

388

PPI's: pharmacokinetics/ dynamics

-PRODRUG: must survive the acidic environment of stomach to be absorbed into small bowel
-all have fairly good bioavailability, decreased with po intake
-metab in liver / inhibits CYP2C19
-excreted in stool; **dose-adjust for hepatic disease**
-little renal excretion

389

PPI's: adverse effects

H/A, diarrhea, constipation, nausea, increased risk C. diff infection, ⬇️Mg with prolonged use,
⬆️ risk osteoporosis-related fractures with prolonged use

390

PPI's: contraindications

Allergy

391

Types of laxatives:

1. Bulk (Metamucil, fibercon)
2. Osmotic laxatives ( milk of mag, lactulose, mg citrate, polyethylene glycol (miralax)

392

Osmotic laxatives MOA:

Causes water retention in stool; soluble but no absorbable compounds

393

Pharmacokinetics of osmotic laxatives

NO PO absorption/ excreted in stool unchanged

394

Adverse effects of osmotic laxatives:

Diarrhea
abdominal complaints

395

Contraindications of osmotic laxatives:

-Existing electrolyte abnormality
-Age under 2 yo

396

Osmotic laxatives: great option for long or short term relief?

No adverse effects shown up to 12 months of daily use

397

Bulk laxatives - MOA?
Pharmacokinetics

Absorb water and enlarge stools which stimulates propulsive movement through the lower GI tract
-no po absorption; excreted through stool as unchanged drug

398

Adverse effects of bulk laxatives:

N/V, abdominal fullness

399

Contraindications of bulk laxatives:

Bowel obstruction, under age of 6

400

Pregnancy Category bulk laxatives

B; safe in pregnancy and breastfeeding

401

Gastric motility agent (Metoclopramide/ Reglan) MOA

Binds to dopamine D2 receptors in CNS, as well as some 5-HT3 antagonism: gastric motility is caused by the D2 antagonism

402

Reglan: pharmacokinetics

Well-absorbed PO, 65-90% bioavailability
Metabolized via liver
Excreted via urine (decrease dose in renal insufficiency

403

Acid Reflux/ Gastritis:
prevalence, probable causes?

Very prevalent (10%) US pop
Several probable causes:
1. Transient lower esophageal sphincter relaxtion
2. Low resting lower esophageal sphincter
3. Poor esophageal acid clearance
4. Defects in esophagastric motility
5. Impaired mucosal resistance and over protective defenses

404

Descriptions and symptoms of gastritis

Burning sensation, nausea, chest pain, or globus (broad) sensation.
* can be very much like an MI ; differentiating SX - SOB, diaphoresis

405

Other contributing factors to gastritis?

Intake of acidic foods; treatment begins with removing these offenders / lifestyle modifications then mess

406

4 Types acid reflux/ gastritis meds

1. Antacids
2. Carafate
3. H2 receptor antagonists
4. PPI's

407

Antacids: sodium bicarbonate, calcium carbonate, magnesium hydroxide, aluminum hydroxide
MOA?

These are weak bases that fact with gastric acid to form a salt and water, therefore decreasing gastric acidity

408

Pharmokinetics/ dynamics of antacids

-Some po absorption; 25-35 % availability
-bicarbonate preps (bioavailability) improves with food bu hydroxide preparations poorly absorbed
-carbonate excreted via stool
-aluminum and mag excreted via urine

409

Pregnancy category of antacids

B, safe for breastfeeding as well

410

Antacids: adverse effects

N/V, constipation, dependence

411

Contraindications for taking antacids:

Renal Failure (for those with aluminum and magnesium) - ie, the re ally excreted ones

412

Carafate: MOA

Positively charged sucrose sulfate binds to negatively charged proteins in base of ulcers, forms an ADHERENT/ PROTECTIVE barrier from gastric acids and bile salts

413

Carafate: pharmacokinetics

-very little absorption, so not metabolized
-excreted in stool

414

Carafate: adverse effects

CONSTIPATION! Gotta love it!

415

Contraindications for use of Carafate-

Allergy; may use with caution with other meds... Can affect absorption

416

Carafate pregnancy category:

B ( off label for peds)

417

H2 receptor antagonists: Zantac, Pepcid, Tagamet
MOA?

Competitive inhibitors of H2 receptors in gastric parietal cells causing a decrease in gastric acid. No H1 or H3 efficacy (therefore not sedating).

418

H2 receptor antagonists: pharmacokinetics

-good po absorption
-metabolized via liver
-excreted in urine

419

H2 receptor antagonists
Adverse Effects

H/A, dizziness, confusion in elderly,
.....GYNECOMASTIA (for real!?!?!)

420

H2 receptor antagonists- contraindications

Potent P450 inhibitor!
Use Tagamet with caution in elderly

421

Pregnancy category for H2 receptor antagonists

B - also safe in peds

422

Proton Pump Inhibitors- Prilosec / omeprazole, Prevacid / lansoprazole, Protonix / pantoprazole, Nexium/ esomeprazole
MOA?

Binds irreversibly to H+/ K+ exchanging ATPase pumps (proton pumps) in gastric parietal cells, decreasing both basal and stimulated gastric acid secretion

423

PPI's: pharmacokinetics/ dynamics

-PRODRUG: must survive the acidic environment of stomach to be absorbed into small bowel
-all have fairly good bioavailability, decreased with po intake
-metab in liver / inhibits CYP2C19
-excreted in stool; **dose-adjust for hepatic disease**
-little renal excretion

424

PPI's: adverse effects

H/A, diarrhea, constipation, nausea, increased risk C. diff infection, ⬇️Mg with prolonged use,
⬆️ risk osteoporosis-related fractures with prolonged use

425

PPI's: contraindications

Allergy

426

Types of laxatives:

1. Bulk (Metamucil, fibercon)
2. Osmotic laxatives ( milk of mag, lactulose, mg citrate, polyethylene glycol (miralax)

427

Osmotic laxatives MOA:

Causes water retention in stool; soluble but no absorbable compounds

428

Pharmacokinetics of osmotic laxatives

NO PO absorption/ excreted in stool unchanged

429

Adverse effects of osmotic laxatives:

Diarrhea
abdominal complaints

430

Contraindications of osmotic laxatives:

-Existing electrolyte abnormality
-Age under 2 yo

431

Osmotic laxatives: great option for long or short term relief?

No adverse effects shown up to 12 months of daily use

432

Bulk laxatives - MOA?
Pharmacokinetics

Absorb water and enlarge stools which stimulates propulsive movement through the lower GI tract
-no po absorption; excreted through stool as unchanged drug

433

Adverse effects of bulk laxatives:

N/V, abdominal fullness

434

Contraindications of bulk laxatives:

Bowel obstruction, under age of 6

435

Pregnancy Category bulk laxatives

B; safe in pregnancy and breastfeeding

436

Gastric motility agent (Metoclopramide/ Reglan) MOA

Binds to dopamine D2 receptors in CNS, as well as some 5-HT3 antagonism: gastric motility is caused by the D2 antagonism

437

Reglan: pharmacokinetics

Well-absorbed PO, 65-90% bioavailability
Metabolized via liver
Excreted via urine (decrease dose in renal insufficiency

438

Acid Reflux/ Gastritis:
prevalence, probable causes?

Very prevalent (10%) US pop
Several probable causes:
1. Transient lower esophageal sphincter relaxtion
2. Low resting lower esophageal sphincter
3. Poor esophageal acid clearance
4. Defects in esophagastric motility
5. Impaired mucosal resistance and over protective defenses

439

Descriptions and symptoms of gastritis

Burning sensation, nausea, chest pain, or globus (broad) sensation.
* can be very much like an MI ; differentiating SX - SOB, diaphoresis

440

Other contributing factors to gastritis?

Intake of acidic foods; treatment begins with removing these offenders / lifestyle modifications then mess

441

4 Types acid reflux/ gastritis meds

1. Antacids
2. Carafate
3. H2 receptor antagonists
4. PPI's

442

Antacids: sodium bicarbonate, calcium carbonate, magnesium hydroxide, aluminum hydroxide
MOA?

These are weak bases that fact with gastric acid to form a salt and water, therefore decreasing gastric acidity

443

Pharmokinetics/ dynamics of antacids

-Some po absorption; 25-35 % availability
-bicarbonate preps (bioavailability) improves with food bu hydroxide preparations poorly absorbed
-carbonate excreted via stool
-aluminum and mag excreted via urine

444

Pregnancy category of antacids

B, safe for breastfeeding as well

445

Antacids: adverse effects

N/V, constipation, dependence

446

Contraindications for taking antacids:

Renal Failure (for those with aluminum and magnesium) - ie, the re ally excreted ones

447

Carafate: MOA

Positively charged sucrose sulfate binds to negatively charged proteins in base of ulcers, forms an ADHERENT/ PROTECTIVE barrier from gastric acids and bile salts

448

Carafate: pharmacokinetics

-very little absorption, so not metabolized
-excreted in stool

449

Carafate: adverse effects

CONSTIPATION! Gotta love it!

450

Contraindications for use of Carafate-

Allergy; may use with caution with other meds... Can affect absorption

451

Carafate pregnancy category:

B ( off label for peds)

452

H2 receptor antagonists: Zantac, Pepcid, Tagamet
MOA?

Competitive inhibitors of H2 receptors in gastric parietal cells causing a decrease in gastric acid. No H1 or H3 efficacy (therefore not sedating).

453

H2 receptor antagonists: pharmacokinetics

-good po absorption
-metabolized via liver
-excreted in urine

454

H2 receptor antagonists
Adverse Effects

H/A, dizziness, confusion in elderly,
.....GYNECOMASTIA (for real!?!?!)

455

H2 receptor antagonists- contraindications

Potent P450 inhibitor!
Use Tagamet with caution in elderly

456

Pregnancy category for H2 receptor antagonists

B - also safe in peds

457

Proton Pump Inhibitors- Prilosec / omeprazole, Prevacid / lansoprazole, Protonix / pantoprazole, Nexium/ esomeprazole
MOA?

Binds irreversibly to H+/ K+ exchanging ATPase pumps (proton pumps) in gastric parietal cells, decreasing both basal and stimulated gastric acid secretion

458

PPI's: pharmacokinetics/ dynamics

-PRODRUG: must survive the acidic environment of stomach to be absorbed into small bowel
-all have fairly good bioavailability, decreased with po intake
-metab in liver / inhibits CYP2C19
-excreted in stool; **dose-adjust for hepatic disease**
-little renal excretion

459

PPI's: adverse effects

H/A, diarrhea, constipation, nausea, increased risk C. diff infection, ⬇️Mg with prolonged use,
⬆️ risk osteoporosis-related fractures with prolonged use

460

PPI's: contraindications

Allergy

461

Types of laxatives:

1. Bulk (Metamucil, fibercon)
2. Osmotic laxatives ( milk of mag, lactulose, mg citrate, polyethylene glycol (miralax)

462

Osmotic laxatives MOA:

Causes water retention in stool; soluble but no absorbable compounds

463

Pharmacokinetics of osmotic laxatives

NO PO absorption/ excreted in stool unchanged

464

Adverse effects of osmotic laxatives:

Diarrhea
abdominal complaints

465

Contraindications of osmotic laxatives:

-Existing electrolyte abnormality
-Age under 2 yo

466

Osmotic laxatives: great option for long or short term relief?

No adverse effects shown up to 12 months of daily use

467

Bulk laxatives - MOA?
Pharmacokinetics

Absorb water and enlarge stools which stimulates propulsive movement through the lower GI tract
-no po absorption; excreted through stool as unchanged drug

468

Adverse effects of bulk laxatives:

N/V, abdominal fullness

469

Contraindications of bulk laxatives:

Bowel obstruction, under age of 6

470

Pregnancy Category bulk laxatives

B; safe in pregnancy and breastfeeding

471

Gastric motility agent (Metoclopramide/ Reglan) MOA

Binds to dopamine D2 receptors in CNS, as well as some 5-HT3 antagonism: gastric motility is caused by the D2 antagonism

472

Reglan: pharmacokinetics

Well-absorbed PO, 65-90% bioavailability
Metabolized via liver
Excreted via urine (decrease dose in renal insufficiency

473

Acid Reflux/ Gastritis:
prevalence, probable causes?

Very prevalent (10%) US pop
Several probable causes:
1. Transient lower esophageal sphincter relaxtion
2. Low resting lower esophageal sphincter
3. Poor esophageal acid clearance
4. Defects in esophagastric motility
5. Impaired mucosal resistance and over protective defenses

474

Descriptions and symptoms of gastritis

Burning sensation, nausea, chest pain, or globus (broad) sensation.
* can be very much like an MI ; differentiating SX - SOB, diaphoresis

475

Other contributing factors to gastritis?

Intake of acidic foods; treatment begins with removing these offenders / lifestyle modifications then mess

476

4 Types acid reflux/ gastritis meds

1. Antacids
2. Carafate
3. H2 receptor antagonists
4. PPI's

477

Antacids: sodium bicarbonate, calcium carbonate, magnesium hydroxide, aluminum hydroxide
MOA?

These are weak bases that fact with gastric acid to form a salt and water, therefore decreasing gastric acidity

478

Pharmokinetics/ dynamics of antacids

-Some po absorption; 25-35 % availability
-bicarbonate preps (bioavailability) improves with food bu hydroxide preparations poorly absorbed
-carbonate excreted via stool
-aluminum and mag excreted via urine

479

Pregnancy category of antacids

B, safe for breastfeeding as well

480

Antacids: adverse effects

N/V, constipation, dependence

481

Contraindications for taking antacids:

Renal Failure (for those with aluminum and magnesium) - ie, the re ally excreted ones

482

Carafate: MOA

Positively charged sucrose sulfate binds to negatively charged proteins in base of ulcers, forms an ADHERENT/ PROTECTIVE barrier from gastric acids and bile salts

483

Carafate: pharmacokinetics

-very little absorption, so not metabolized
-excreted in stool

484

Carafate: adverse effects

CONSTIPATION! Gotta love it!

485

Contraindications for use of Carafate-

Allergy; may use with caution with other meds... Can affect absorption

486

Carafate pregnancy category:

B ( off label for peds)

487

H2 receptor antagonists: Zantac, Pepcid, Tagamet
MOA?

Competitive inhibitors of H2 receptors in gastric parietal cells causing a decrease in gastric acid. No H1 or H3 efficacy (therefore not sedating).

488

H2 receptor antagonists: pharmacokinetics

-good po absorption
-metabolized via liver
-excreted in urine

489

H2 receptor antagonists
Adverse Effects

H/A, dizziness, confusion in elderly,
.....GYNECOMASTIA (for real!?!?!)

490

H2 receptor antagonists- contraindications

Potent P450 inhibitor!
Use Tagamet with caution in elderly

491

Pregnancy category for H2 receptor antagonists

B - also safe in peds

492

Proton Pump Inhibitors- Prilosec / omeprazole, Prevacid / lansoprazole, Protonix / pantoprazole, Nexium/ esomeprazole
MOA?

Binds irreversibly to H+/ K+ exchanging ATPase pumps (proton pumps) in gastric parietal cells, decreasing both basal and stimulated gastric acid secretion

493

PPI's: pharmacokinetics/ dynamics

-PRODRUG: must survive the acidic environment of stomach to be absorbed into small bowel
-all have fairly good bioavailability, decreased with po intake
-metab in liver / inhibits CYP2C19
-excreted in stool; **dose-adjust for hepatic disease**
-little renal excretion

494

PPI's: adverse effects

H/A, diarrhea, constipation, nausea, increased risk C. diff infection, ⬇️Mg with prolonged use,
⬆️ risk osteoporosis-related fractures with prolonged use

495

PPI's: contraindications

Allergy

496

Types of laxatives:

1. Bulk (Metamucil, fibercon)
2. Osmotic laxatives ( milk of mag, lactulose, mg citrate, polyethylene glycol (miralax)

497

Osmotic laxatives MOA:

Causes water retention in stool; soluble but no absorbable compounds

498

Pharmacokinetics of osmotic laxatives

NO PO absorption/ excreted in stool unchanged

499

Adverse effects of osmotic laxatives:

Diarrhea
abdominal complaints

500

Contraindications of osmotic laxatives:

-Existing electrolyte abnormality
-Age under 2 yo

501

Osmotic laxatives: great option for long or short term relief?

No adverse effects shown up to 12 months of daily use

502

Bulk laxatives - MOA?
Pharmacokinetics

Absorb water and enlarge stools which stimulates propulsive movement through the lower GI tract
-no po absorption; excreted through stool as unchanged drug

503

Adverse effects of bulk laxatives:

N/V, abdominal fullness

504

Contraindications of bulk laxatives:

Bowel obstruction, under age of 6

505

Pregnancy Category bulk laxatives

B; safe in pregnancy and breastfeeding

506

Gastric motility agent (Metoclopramide/ Reglan) MOA

Binds to dopamine D2 receptors in CNS, as well as some 5-HT3 antagonism: gastric motility is caused by the D2 antagonism

507

Reglan: pharmacokinetics

Well-absorbed PO, 65-90% bioavailability
Metabolized via liver
Excreted via urine (decrease dose in renal insufficiency

508

Acid Reflux/ Gastritis:
prevalence, probable causes?

Very prevalent (10%) US pop
Several probable causes:
1. Transient lower esophageal sphincter relaxtion
2. Low resting lower esophageal sphincter
3. Poor esophageal acid clearance
4. Defects in esophagastric motility
5. Impaired mucosal resistance and over protective defenses

509

Descriptions and symptoms of gastritis

Burning sensation, nausea, chest pain, or globus (broad) sensation.
* can be very much like an MI ; differentiating SX - SOB, diaphoresis

510

Other contributing factors to gastritis?

Intake of acidic foods; treatment begins with removing these offenders / lifestyle modifications then mess

511

4 Types acid reflux/ gastritis meds

1. Antacids
2. Carafate
3. H2 receptor antagonists
4. PPI's

512

Antacids: sodium bicarbonate, calcium carbonate, magnesium hydroxide, aluminum hydroxide
MOA?

These are weak bases that fact with gastric acid to form a salt and water, therefore decreasing gastric acidity

513

Pharmokinetics/ dynamics of antacids

-Some po absorption; 25-35 % availability
-bicarbonate preps (bioavailability) improves with food bu hydroxide preparations poorly absorbed
-carbonate excreted via stool
-aluminum and mag excreted via urine

514

Pregnancy category of antacids

B, safe for breastfeeding as well

515

Antacids: adverse effects

N/V, constipation, dependence

516

Contraindications for taking antacids:

Renal Failure (for those with aluminum and magnesium) - ie, the re ally excreted ones

517

Carafate: MOA

Positively charged sucrose sulfate binds to negatively charged proteins in base of ulcers, forms an ADHERENT/ PROTECTIVE barrier from gastric acids and bile salts

518

Carafate: pharmacokinetics

-very little absorption, so not metabolized
-excreted in stool

519

Carafate: adverse effects

CONSTIPATION! Gotta love it!

520

Contraindications for use of Carafate-

Allergy; may use with caution with other meds... Can affect absorption

521

Carafate pregnancy category:

B ( off label for peds)

522

H2 receptor antagonists: Zantac, Pepcid, Tagamet
MOA?

Competitive inhibitors of H2 receptors in gastric parietal cells causing a decrease in gastric acid. No H1 or H3 efficacy (therefore not sedating).

523

H2 receptor antagonists: pharmacokinetics

-good po absorption
-metabolized via liver
-excreted in urine

524

H2 receptor antagonists
Adverse Effects

H/A, dizziness, confusion in elderly,
.....GYNECOMASTIA (for real!?!?!)

525

H2 receptor antagonists- contraindications

Potent P450 inhibitor!
Use Tagamet with caution in elderly

526

Pregnancy category for H2 receptor antagonists

B - also safe in peds

527

Proton Pump Inhibitors- Prilosec / omeprazole, Prevacid / lansoprazole, Protonix / pantoprazole, Nexium/ esomeprazole
MOA?

Binds irreversibly to H+/ K+ exchanging ATPase pumps (proton pumps) in gastric parietal cells, decreasing both basal and stimulated gastric acid secretion

528

PPI's: pharmacokinetics/ dynamics

-PRODRUG: must survive the acidic environment of stomach to be absorbed into small bowel
-all have fairly good bioavailability, decreased with po intake
-metab in liver / inhibits CYP2C19
-excreted in stool; **dose-adjust for hepatic disease**
-little renal excretion

529

PPI's: adverse effects

H/A, diarrhea, constipation, nausea, increased risk C. diff infection, ⬇️Mg with prolonged use,
⬆️ risk osteoporosis-related fractures with prolonged use

530

PPI's: contraindications

Allergy

531

Types of laxatives:

1. Bulk (Metamucil, fibercon)
2. Osmotic laxatives ( milk of mag, lactulose, mg citrate, polyethylene glycol (miralax)

532

Osmotic laxatives MOA:

Causes water retention in stool; soluble but no absorbable compounds

533

Pharmacokinetics of osmotic laxatives

NO PO absorption/ excreted in stool unchanged

534

Adverse effects of osmotic laxatives:

Diarrhea
abdominal complaints

535

Contraindications of osmotic laxatives:

-Existing electrolyte abnormality
-Age under 2 yo

536

Osmotic laxatives: great option for long or short term relief?

No adverse effects shown up to 12 months of daily use

537

Bulk laxatives - MOA?
Pharmacokinetics

Absorb water and enlarge stools which stimulates propulsive movement through the lower GI tract
-no po absorption; excreted through stool as unchanged drug

538

Adverse effects of bulk laxatives:

N/V, abdominal fullness

539

Contraindications of bulk laxatives:

Bowel obstruction, under age of 6

540

Pregnancy Category bulk laxatives

B; safe in pregnancy and breastfeeding

541

Gastric motility agent (Metoclopramide/ Reglan) MOA

Binds to dopamine D2 receptors in CNS, as well as some 5-HT3 antagonism: gastric motility is caused by the D2 antagonism

542

Reglan: pharmacokinetics

Well-absorbed PO, 65-90% bioavailability
Metabolized via liver
Excreted via urine (decrease dose in renal insufficiency

543

Acid Reflux/ Gastritis:
prevalence, probable causes?

Very prevalent (10%) US pop
Several probable causes:
1. Transient lower esophageal sphincter relaxtion
2. Low resting lower esophageal sphincter
3. Poor esophageal acid clearance
4. Defects in esophagastric motility
5. Impaired mucosal resistance and over protective defenses

544

Descriptions and symptoms of gastritis

Burning sensation, nausea, chest pain, or globus (broad) sensation.
* can be very much like an MI ; differentiating SX - SOB, diaphoresis

545

Other contributing factors to gastritis?

Intake of acidic foods; treatment begins with removing these offenders / lifestyle modifications then mess

546

4 Types acid reflux/ gastritis meds

1. Antacids
2. Carafate
3. H2 receptor antagonists
4. PPI's

547

Antacids: sodium bicarbonate, calcium carbonate, magnesium hydroxide, aluminum hydroxide
MOA?

These are weak bases that fact with gastric acid to form a salt and water, therefore decreasing gastric acidity

548

Pharmokinetics/ dynamics of antacids

-Some po absorption; 25-35 % availability
-bicarbonate preps (bioavailability) improves with food bu hydroxide preparations poorly absorbed
-carbonate excreted via stool
-aluminum and mag excreted via urine

549

Pregnancy category of antacids

B, safe for breastfeeding as well

550

Antacids: adverse effects

N/V, constipation, dependence

551

Contraindications for taking antacids:

Renal Failure (for those with aluminum and magnesium) - ie, the re ally excreted ones

552

Carafate: MOA

Positively charged sucrose sulfate binds to negatively charged proteins in base of ulcers, forms an ADHERENT/ PROTECTIVE barrier from gastric acids and bile salts

553

Carafate: pharmacokinetics

-very little absorption, so not metabolized
-excreted in stool

554

Carafate: adverse effects

CONSTIPATION! Gotta love it!

555

Contraindications for use of Carafate-

Allergy; may use with caution with other meds... Can affect absorption

556

Carafate pregnancy category:

B ( off label for peds)

557

H2 receptor antagonists: Zantac, Pepcid, Tagamet
MOA?

Competitive inhibitors of H2 receptors in gastric parietal cells causing a decrease in gastric acid. No H1 or H3 efficacy (therefore not sedating).

558

H2 receptor antagonists: pharmacokinetics

-good po absorption
-metabolized via liver
-excreted in urine

559

H2 receptor antagonists
Adverse Effects

H/A, dizziness, confusion in elderly,
.....GYNECOMASTIA (for real!?!?!)

560

H2 receptor antagonists- contraindications

Potent P450 inhibitor!
Use Tagamet with caution in elderly

561

Pregnancy category for H2 receptor antagonists

B - also safe in peds

562

Proton Pump Inhibitors- Prilosec / omeprazole, Prevacid / lansoprazole, Protonix / pantoprazole, Nexium/ esomeprazole
MOA?

Binds irreversibly to H+/ K+ exchanging ATPase pumps (proton pumps) in gastric parietal cells, decreasing both basal and stimulated gastric acid secretion

563

PPI's: pharmacokinetics/ dynamics

-PRODRUG: must survive the acidic environment of stomach to be absorbed into small bowel
-all have fairly good bioavailability, decreased with po intake
-metab in liver / inhibits CYP2C19
-excreted in stool; **dose-adjust for hepatic disease**
-little renal excretion

564

PPI's: adverse effects

H/A, diarrhea, constipation, nausea, increased risk C. diff infection, ⬇️Mg with prolonged use,
⬆️ risk osteoporosis-related fractures with prolonged use

565

PPI's: contraindications

Allergy

566

Types of laxatives:

1. Bulk (Metamucil, fibercon)
2. Osmotic laxatives ( milk of mag, lactulose, mg citrate, polyethylene glycol (miralax)

567

Osmotic laxatives MOA:

Causes water retention in stool; soluble but no absorbable compounds

568

Pharmacokinetics of osmotic laxatives

NO PO absorption/ excreted in stool unchanged

569

Adverse effects of osmotic laxatives:

Diarrhea
abdominal complaints

570

Contraindications of osmotic laxatives:

-Existing electrolyte abnormality
-Age under 2 yo

571

Osmotic laxatives: great option for long or short term relief?

No adverse effects shown up to 12 months of daily use

572

Bulk laxatives - MOA?
Pharmacokinetics

Absorb water and enlarge stools which stimulates propulsive movement through the lower GI tract
-no po absorption; excreted through stool as unchanged drug

573

Adverse effects of bulk laxatives:

N/V, abdominal fullness

574

Contraindications of bulk laxatives:

Bowel obstruction, under age of 6

575

Pregnancy Category bulk laxatives

B; safe in pregnancy and breastfeeding

576

Gastric motility agent (Metoclopramide/ Reglan) MOA

Binds to dopamine D2 receptors in CNS, as well as some 5-HT3 antagonism: gastric motility is caused by the D2 antagonism

577

Reglan: pharmacokinetics

Well-absorbed PO, 65-90% bioavailability
Metabolized via liver
Excreted via urine (decrease dose in renal insufficiency

578

Acid Reflux/ Gastritis:
prevalence, probable causes?

Very prevalent (10%) US pop
Several probable causes:
1. Transient lower esophageal sphincter relaxtion
2. Low resting lower esophageal sphincter
3. Poor esophageal acid clearance
4. Defects in esophagastric motility
5. Impaired mucosal resistance and over protective defenses

579

Descriptions and symptoms of gastritis

Burning sensation, nausea, chest pain, or globus (broad) sensation.
* can be very much like an MI ; differentiating SX - SOB, diaphoresis

580

Other contributing factors to gastritis?

Intake of acidic foods; treatment begins with removing these offenders / lifestyle modifications then mess

581

4 Types acid reflux/ gastritis meds

1. Antacids
2. Carafate
3. H2 receptor antagonists
4. PPI's

582

Antacids: sodium bicarbonate, calcium carbonate, magnesium hydroxide, aluminum hydroxide
MOA?

These are weak bases that fact with gastric acid to form a salt and water, therefore decreasing gastric acidity

583

Pharmokinetics/ dynamics of antacids

-Some po absorption; 25-35 % availability
-bicarbonate preps (bioavailability) improves with food bu hydroxide preparations poorly absorbed
-carbonate excreted via stool
-aluminum and mag excreted via urine

584

Pregnancy category of antacids

B, safe for breastfeeding as well

585

Antacids: adverse effects

N/V, constipation, dependence

586

Contraindications for taking antacids:

Renal Failure (for those with aluminum and magnesium) - ie, the re ally excreted ones

587

Carafate: MOA

Positively charged sucrose sulfate binds to negatively charged proteins in base of ulcers, forms an ADHERENT/ PROTECTIVE barrier from gastric acids and bile salts

588

Carafate: pharmacokinetics

-very little absorption, so not metabolized
-excreted in stool

589

Carafate: adverse effects

CONSTIPATION! Gotta love it!

590

Contraindications for use of Carafate-

Allergy; may use with caution with other meds... Can affect absorption

591

Carafate pregnancy category:

B ( off label for peds)

592

H2 receptor antagonists: Zantac, Pepcid, Tagamet
MOA?

Competitive inhibitors of H2 receptors in gastric parietal cells causing a decrease in gastric acid. No H1 or H3 efficacy (therefore not sedating).

593

H2 receptor antagonists: pharmacokinetics

-good po absorption
-metabolized via liver
-excreted in urine

594

H2 receptor antagonists
Adverse Effects

H/A, dizziness, confusion in elderly,
.....GYNECOMASTIA (for real!?!?!)

595

H2 receptor antagonists- contraindications

Potent P450 inhibitor!
Use Tagamet with caution in elderly

596

Pregnancy category for H2 receptor antagonists

B - also safe in peds

597

Proton Pump Inhibitors- Prilosec / omeprazole, Prevacid / lansoprazole, Protonix / pantoprazole, Nexium/ esomeprazole
MOA?

Binds irreversibly to H+/ K+ exchanging ATPase pumps (proton pumps) in gastric parietal cells, decreasing both basal and stimulated gastric acid secretion

598

PPI's: pharmacokinetics/ dynamics

-PRODRUG: must survive the acidic environment of stomach to be absorbed into small bowel
-all have fairly good bioavailability, decreased with po intake
-metab in liver / inhibits CYP2C19
-excreted in stool; **dose-adjust for hepatic disease**
-little renal excretion

599

PPI's: adverse effects

H/A, diarrhea, constipation, nausea, increased risk C. diff infection, ⬇️Mg with prolonged use,
⬆️ risk osteoporosis-related fractures with prolonged use

600

PPI's: contraindications

Allergy

601

Types of laxatives:

1. Bulk (Metamucil, fibercon)
2. Osmotic laxatives ( milk of mag, lactulose, mg citrate, polyethylene glycol (miralax)

602

Osmotic laxatives MOA:

Causes water retention in stool; soluble but no absorbable compounds

603

Pharmacokinetics of osmotic laxatives

NO PO absorption/ excreted in stool unchanged

604

Adverse effects of osmotic laxatives:

Diarrhea
abdominal complaints

605

Contraindications of osmotic laxatives:

-Existing electrolyte abnormality
-Age under 2 yo

606

Osmotic laxatives: great option for long or short term relief?

No adverse effects shown up to 12 months of daily use

607

Bulk laxatives - MOA?
Pharmacokinetics

Absorb water and enlarge stools which stimulates propulsive movement through the lower GI tract
-no po absorption; excreted through stool as unchanged drug

608

Adverse effects of bulk laxatives:

N/V, abdominal fullness

609

Contraindications of bulk laxatives:

Bowel obstruction, under age of 6

610

Pregnancy Category bulk laxatives

B; safe in pregnancy and breastfeeding

611

Gastric motility agent (Metoclopramide/ Reglan) MOA

Binds to dopamine D2 receptors in CNS, as well as some 5-HT3 antagonism: gastric motility is caused by the D2 antagonism

612

Reglan: pharmacokinetics

Well-absorbed PO, 65-90% bioavailability
Metabolized via liver
Excreted via urine (decrease dose in renal insufficiency

613

Acid Reflux/ Gastritis:
prevalence, probable causes?

Very prevalent (10%) US pop
Several probable causes:
1. Transient lower esophageal sphincter relaxtion
2. Low resting lower esophageal sphincter
3. Poor esophageal acid clearance
4. Defects in esophagastric motility
5. Impaired mucosal resistance and over protective defenses

614

Descriptions and symptoms of gastritis

Burning sensation, nausea, chest pain, or globus (broad) sensation.
* can be very much like an MI ; differentiating SX - SOB, diaphoresis

615

Other contributing factors to gastritis?

Intake of acidic foods; treatment begins with removing these offenders / lifestyle modifications then mess

616

4 Types acid reflux/ gastritis meds

1. Antacids
2. Carafate
3. H2 receptor antagonists
4. PPI's

617

Antacids: sodium bicarbonate, calcium carbonate, magnesium hydroxide, aluminum hydroxide
MOA?

These are weak bases that fact with gastric acid to form a salt and water, therefore decreasing gastric acidity

618

Pharmokinetics/ dynamics of antacids

-Some po absorption; 25-35 % availability
-bicarbonate preps (bioavailability) improves with food bu hydroxide preparations poorly absorbed
-carbonate excreted via stool
-aluminum and mag excreted via urine

619

Pregnancy category of antacids

B, safe for breastfeeding as well

620

Antacids: adverse effects

N/V, constipation, dependence

621

Contraindications for taking antacids:

Renal Failure (for those with aluminum and magnesium) - ie, the re ally excreted ones

622

Carafate: MOA

Positively charged sucrose sulfate binds to negatively charged proteins in base of ulcers, forms an ADHERENT/ PROTECTIVE barrier from gastric acids and bile salts

623

Carafate: pharmacokinetics

-very little absorption, so not metabolized
-excreted in stool

624

Carafate: adverse effects

CONSTIPATION! Gotta love it!

625

Contraindications for use of Carafate-

Allergy; may use with caution with other meds... Can affect absorption

626

Carafate pregnancy category:

B ( off label for peds)

627

H2 receptor antagonists: Zantac, Pepcid, Tagamet
MOA?

Competitive inhibitors of H2 receptors in gastric parietal cells causing a decrease in gastric acid. No H1 or H3 efficacy (therefore not sedating).

628

H2 receptor antagonists: pharmacokinetics

-good po absorption
-metabolized via liver
-excreted in urine

629

H2 receptor antagonists
Adverse Effects

H/A, dizziness, confusion in elderly,
.....GYNECOMASTIA (for real!?!?!)

630

H2 receptor antagonists- contraindications

Potent P450 inhibitor!
Use Tagamet with caution in elderly

631

Pregnancy category for H2 receptor antagonists

B - also safe in peds

632

Proton Pump Inhibitors- Prilosec / omeprazole, Prevacid / lansoprazole, Protonix / pantoprazole, Nexium/ esomeprazole
MOA?

Binds irreversibly to H+/ K+ exchanging ATPase pumps (proton pumps) in gastric parietal cells, decreasing both basal and stimulated gastric acid secretion

633

PPI's: pharmacokinetics/ dynamics

-PRODRUG: must survive the acidic environment of stomach to be absorbed into small bowel
-all have fairly good bioavailability, decreased with po intake
-metab in liver / inhibits CYP2C19
-excreted in stool; **dose-adjust for hepatic disease**
-little renal excretion

634

PPI's: adverse effects

H/A, diarrhea, constipation, nausea, increased risk C. diff infection, ⬇️Mg with prolonged use,
⬆️ risk osteoporosis-related fractures with prolonged use

635

PPI's: contraindications

Allergy

636

Types of laxatives:

1. Bulk (Metamucil, fibercon)
2. Osmotic laxatives ( milk of mag, lactulose, mg citrate, polyethylene glycol (miralax)

637

Osmotic laxatives MOA:

Causes water retention in stool; soluble but no absorbable compounds

638

Pharmacokinetics of osmotic laxatives

NO PO absorption/ excreted in stool unchanged

639

Adverse effects of osmotic laxatives:

Diarrhea
abdominal complaints

640

Contraindications of osmotic laxatives:

-Existing electrolyte abnormality
-Age under 2 yo

641

Osmotic laxatives: great option for long or short term relief?

No adverse effects shown up to 12 months of daily use

642

Bulk laxatives - MOA?
Pharmacokinetics

Absorb water and enlarge stools which stimulates propulsive movement through the lower GI tract
-no po absorption; excreted through stool as unchanged drug

643

Adverse effects of bulk laxatives:

N/V, abdominal fullness

644

Contraindications of bulk laxatives:

Bowel obstruction, under age of 6

645

Pregnancy Category bulk laxatives

B; safe in pregnancy and breastfeeding

646

Gastric motility agent (Metoclopramide/ Reglan) MOA

Binds to dopamine D2 receptors in CNS, as well as some 5-HT3 antagonism: gastric motility is caused by the D2 antagonism

647

Reglan: pharmacokinetics

Well-absorbed PO, 65-90% bioavailability
Metabolized via liver
Excreted via urine (decrease dose in renal insufficiency

648

Acid Reflux/ Gastritis:
prevalence, probable causes?

Very prevalent (10%) US pop
Several probable causes:
1. Transient lower esophageal sphincter relaxtion
2. Low resting lower esophageal sphincter
3. Poor esophageal acid clearance
4. Defects in esophagastric motility
5. Impaired mucosal resistance and over protective defenses

649

Descriptions and symptoms of gastritis

Burning sensation, nausea, chest pain, or globus (broad) sensation.
* can be very much like an MI ; differentiating SX - SOB, diaphoresis

650

Other contributing factors to gastritis?

Intake of acidic foods; treatment begins with removing these offenders / lifestyle modifications then mess

651

4 Types acid reflux/ gastritis meds

1. Antacids
2. Carafate
3. H2 receptor antagonists
4. PPI's

652

Antacids: sodium bicarbonate, calcium carbonate, magnesium hydroxide, aluminum hydroxide
MOA?

These are weak bases that fact with gastric acid to form a salt and water, therefore decreasing gastric acidity

653

Pharmokinetics/ dynamics of antacids

-Some po absorption; 25-35 % availability
-bicarbonate preps (bioavailability) improves with food bu hydroxide preparations poorly absorbed
-carbonate excreted via stool
-aluminum and mag excreted via urine

654

Pregnancy category of antacids

B, safe for breastfeeding as well

655

Antacids: adverse effects

N/V, constipation, dependence

656

Contraindications for taking antacids:

Renal Failure (for those with aluminum and magnesium) - ie, the re ally excreted ones

657

Carafate: MOA

Positively charged sucrose sulfate binds to negatively charged proteins in base of ulcers, forms an ADHERENT/ PROTECTIVE barrier from gastric acids and bile salts

658

Carafate: pharmacokinetics

-very little absorption, so not metabolized
-excreted in stool

659

Carafate: adverse effects

CONSTIPATION! Gotta love it!

660

Contraindications for use of Carafate-

Allergy; may use with caution with other meds... Can affect absorption

661

Carafate pregnancy category:

B ( off label for peds)

662

H2 receptor antagonists: Zantac, Pepcid, Tagamet
MOA?

Competitive inhibitors of H2 receptors in gastric parietal cells causing a decrease in gastric acid. No H1 or H3 efficacy (therefore not sedating).

663

H2 receptor antagonists: pharmacokinetics

-good po absorption
-metabolized via liver
-excreted in urine

664

H2 receptor antagonists
Adverse Effects

H/A, dizziness, confusion in elderly,
.....GYNECOMASTIA (for real!?!?!)

665

H2 receptor antagonists- contraindications

Potent P450 inhibitor!
Use Tagamet with caution in elderly

666

Pregnancy category for H2 receptor antagonists

B - also safe in peds

667

Proton Pump Inhibitors- Prilosec / omeprazole, Prevacid / lansoprazole, Protonix / pantoprazole, Nexium/ esomeprazole
MOA?

Binds irreversibly to H+/ K+ exchanging ATPase pumps (proton pumps) in gastric parietal cells, decreasing both basal and stimulated gastric acid secretion

668

PPI's: pharmacokinetics/ dynamics

-PRODRUG: must survive the acidic environment of stomach to be absorbed into small bowel
-all have fairly good bioavailability, decreased with po intake
-metab in liver / inhibits CYP2C19
-excreted in stool; **dose-adjust for hepatic disease**
-little renal excretion

669

PPI's: adverse effects

H/A, diarrhea, constipation, nausea, increased risk C. diff infection, ⬇️Mg with prolonged use,
⬆️ risk osteoporosis-related fractures with prolonged use

670

PPI's: contraindications

Allergy

671

Types of laxatives:

1. Bulk (Metamucil, fibercon)
2. Osmotic laxatives ( milk of mag, lactulose, mg citrate, polyethylene glycol (miralax)

672

Osmotic laxatives MOA:

Causes water retention in stool; soluble but no absorbable compounds

673

Pharmacokinetics of osmotic laxatives

NO PO absorption/ excreted in stool unchanged

674

Adverse effects of osmotic laxatives:

Diarrhea
abdominal complaints

675

Contraindications of osmotic laxatives:

-Existing electrolyte abnormality
-Age under 2 yo

676

Osmotic laxatives: great option for long or short term relief?

No adverse effects shown up to 12 months of daily use

677

Bulk laxatives - MOA?
Pharmacokinetics

Absorb water and enlarge stools which stimulates propulsive movement through the lower GI tract
-no po absorption; excreted through stool as unchanged drug

678

Adverse effects of bulk laxatives:

N/V, abdominal fullness

679

Contraindications of bulk laxatives:

Bowel obstruction, under age of 6

680

Pregnancy Category bulk laxatives

B; safe in pregnancy and breastfeeding

681

Gastric motility agent (Metoclopramide/ Reglan) MOA

Binds to dopamine D2 receptors in CNS, as well as some 5-HT3 antagonism: gastric motility is caused by the D2 antagonism

682

Reglan: pharmacokinetics

Well-absorbed PO, 65-90% bioavailability
Metabolized via liver
Excreted via urine (decrease dose in renal insufficiency

683

Acid Reflux/ Gastritis:
prevalence, probable causes?

Very prevalent (10%) US pop
Several probable causes:
1. Transient lower esophageal sphincter relaxtion
2. Low resting lower esophageal sphincter
3. Poor esophageal acid clearance
4. Defects in esophagastric motility
5. Impaired mucosal resistance and over protective defenses

684

Descriptions and symptoms of gastritis

Burning sensation, nausea, chest pain, or globus (broad) sensation.
* can be very much like an MI ; differentiating SX - SOB, diaphoresis

685

Other contributing factors to gastritis?

Intake of acidic foods; treatment begins with removing these offenders / lifestyle modifications then mess

686

4 Types acid reflux/ gastritis meds

1. Antacids
2. Carafate
3. H2 receptor antagonists
4. PPI's

687

Antacids: sodium bicarbonate, calcium carbonate, magnesium hydroxide, aluminum hydroxide
MOA?

These are weak bases that fact with gastric acid to form a salt and water, therefore decreasing gastric acidity

688

Pharmokinetics/ dynamics of antacids

-Some po absorption; 25-35 % availability
-bicarbonate preps (bioavailability) improves with food bu hydroxide preparations poorly absorbed
-carbonate excreted via stool
-aluminum and mag excreted via urine

689

Pregnancy category of antacids

B, safe for breastfeeding as well

690

Antacids: adverse effects

N/V, constipation, dependence

691

Contraindications for taking antacids:

Renal Failure (for those with aluminum and magnesium) - ie, the re ally excreted ones

692

Carafate: MOA

Positively charged sucrose sulfate binds to negatively charged proteins in base of ulcers, forms an ADHERENT/ PROTECTIVE barrier from gastric acids and bile salts

693

Carafate: pharmacokinetics

-very little absorption, so not metabolized
-excreted in stool

694

Carafate: adverse effects

CONSTIPATION! Gotta love it!

695

Contraindications for use of Carafate-

Allergy; may use with caution with other meds... Can affect absorption

696

Carafate pregnancy category:

B ( off label for peds)

697

H2 receptor antagonists: Zantac, Pepcid, Tagamet
MOA?

Competitive inhibitors of H2 receptors in gastric parietal cells causing a decrease in gastric acid. No H1 or H3 efficacy (therefore not sedating).

698

H2 receptor antagonists: pharmacokinetics

-good po absorption
-metabolized via liver
-excreted in urine

699

H2 receptor antagonists
Adverse Effects

H/A, dizziness, confusion in elderly,
.....GYNECOMASTIA (for real!?!?!)

700

H2 receptor antagonists- contraindications

Potent P450 inhibitor!
Use Tagamet with caution in elderly

701

Pregnancy category for H2 receptor antagonists

B - also safe in peds

702

Proton Pump Inhibitors- Prilosec / omeprazole, Prevacid / lansoprazole, Protonix / pantoprazole, Nexium/ esomeprazole
MOA?

Binds irreversibly to H+/ K+ exchanging ATPase pumps (proton pumps) in gastric parietal cells, decreasing both basal and stimulated gastric acid secretion

703

PPI's: pharmacokinetics/ dynamics

-PRODRUG: must survive the acidic environment of stomach to be absorbed into small bowel
-all have fairly good bioavailability, decreased with po intake
-metab in liver / inhibits CYP2C19
-excreted in stool; **dose-adjust for hepatic disease**
-little renal excretion

704

PPI's: adverse effects

H/A, diarrhea, constipation, nausea, increased risk C. diff infection, ⬇️Mg with prolonged use,
⬆️ risk osteoporosis-related fractures with prolonged use

705

PPI's: contraindications

Allergy

706

Types of laxatives:

1. Bulk (Metamucil, fibercon)
2. Osmotic laxatives ( milk of mag, lactulose, mg citrate, polyethylene glycol (miralax)

707

Osmotic laxatives MOA:

Causes water retention in stool; soluble but no absorbable compounds

708

Pharmacokinetics of osmotic laxatives

NO PO absorption/ excreted in stool unchanged

709

Adverse effects of osmotic laxatives:

Diarrhea
abdominal complaints

710

Contraindications of osmotic laxatives:

-Existing electrolyte abnormality
-Age under 2 yo

711

Osmotic laxatives: great option for long or short term relief?

No adverse effects shown up to 12 months of daily use

712

Bulk laxatives - MOA?
Pharmacokinetics

Absorb water and enlarge stools which stimulates propulsive movement through the lower GI tract
-no po absorption; excreted through stool as unchanged drug

713

Adverse effects of bulk laxatives:

N/V, abdominal fullness

714

Contraindications of bulk laxatives:

Bowel obstruction, under age of 6

715

Pregnancy Category bulk laxatives

B; safe in pregnancy and breastfeeding

716

Gastric motility agent (Metoclopramide/ Reglan) MOA

Binds to dopamine D2 receptors in CNS, as well as some 5-HT3 antagonism: gastric motility is caused by the D2 antagonism

717

Reglan: pharmacokinetics

Well-absorbed PO, 65-90% bioavailability
Metabolized via liver
Excreted via urine (decrease dose in renal insufficiency

718

Acid Reflux/ Gastritis:
prevalence, probable causes?

Very prevalent (10%) US pop
Several probable causes:
1. Transient lower esophageal sphincter relaxtion
2. Low resting lower esophageal sphincter
3. Poor esophageal acid clearance
4. Defects in esophagastric motility
5. Impaired mucosal resistance and over protective defenses

719

Descriptions and symptoms of gastritis

Burning sensation, nausea, chest pain, or globus (broad) sensation.
* can be very much like an MI ; differentiating SX - SOB, diaphoresis

720

Other contributing factors to gastritis?

Intake of acidic foods; treatment begins with removing these offenders / lifestyle modifications then mess

721

4 Types acid reflux/ gastritis meds

1. Antacids
2. Carafate
3. H2 receptor antagonists
4. PPI's

722

Antacids: sodium bicarbonate, calcium carbonate, magnesium hydroxide, aluminum hydroxide
MOA?

These are weak bases that fact with gastric acid to form a salt and water, therefore decreasing gastric acidity

723

Pharmokinetics/ dynamics of antacids

-Some po absorption; 25-35 % availability
-bicarbonate preps (bioavailability) improves with food bu hydroxide preparations poorly absorbed
-carbonate excreted via stool
-aluminum and mag excreted via urine

724

Pregnancy category of antacids

B, safe for breastfeeding as well

725

Antacids: adverse effects

N/V, constipation, dependence

726

Contraindications for taking antacids:

Renal Failure (for those with aluminum and magnesium) - ie, the re ally excreted ones

727

Carafate: MOA

Positively charged sucrose sulfate binds to negatively charged proteins in base of ulcers, forms an ADHERENT/ PROTECTIVE barrier from gastric acids and bile salts

728

Carafate: pharmacokinetics

-very little absorption, so not metabolized
-excreted in stool

729

Carafate: adverse effects

CONSTIPATION! Gotta love it!

730

Contraindications for use of Carafate-

Allergy; may use with caution with other meds... Can affect absorption

731

Carafate pregnancy category:

B ( off label for peds)

732

H2 receptor antagonists: Zantac, Pepcid, Tagamet
MOA?

Competitive inhibitors of H2 receptors in gastric parietal cells causing a decrease in gastric acid. No H1 or H3 efficacy (therefore not sedating).

733

H2 receptor antagonists: pharmacokinetics

-good po absorption
-metabolized via liver
-excreted in urine

734

H2 receptor antagonists
Adverse Effects

H/A, dizziness, confusion in elderly,
.....GYNECOMASTIA (for real!?!?!)

735

H2 receptor antagonists- contraindications

Potent P450 inhibitor!
Use Tagamet with caution in elderly

736

Pregnancy category for H2 receptor antagonists

B - also safe in peds

737

Proton Pump Inhibitors- Prilosec / omeprazole, Prevacid / lansoprazole, Protonix / pantoprazole, Nexium/ esomeprazole
MOA?

Binds irreversibly to H+/ K+ exchanging ATPase pumps (proton pumps) in gastric parietal cells, decreasing both basal and stimulated gastric acid secretion

738

PPI's: pharmacokinetics/ dynamics

-PRODRUG: must survive the acidic environment of stomach to be absorbed into small bowel
-all have fairly good bioavailability, decreased with po intake
-metab in liver / inhibits CYP2C19
-excreted in stool; **dose-adjust for hepatic disease**
-little renal excretion

739

PPI's: adverse effects

H/A, diarrhea, constipation, nausea, increased risk C. diff infection, ⬇️Mg with prolonged use,
⬆️ risk osteoporosis-related fractures with prolonged use

740

PPI's: contraindications

Allergy

741

Types of laxatives:

1. Bulk (Metamucil, fibercon)
2. Osmotic laxatives ( milk of mag, lactulose, mg citrate, polyethylene glycol (miralax)

742

Osmotic laxatives MOA:

Causes water retention in stool; soluble but no absorbable compounds

743

Pharmacokinetics of osmotic laxatives

NO PO absorption/ excreted in stool unchanged

744

Adverse effects of osmotic laxatives:

Diarrhea
abdominal complaints

745

Contraindications of osmotic laxatives:

-Existing electrolyte abnormality
-Age under 2 yo

746

Osmotic laxatives: great option for long or short term relief?

No adverse effects shown up to 12 months of daily use

747

Bulk laxatives - MOA?
Pharmacokinetics

Absorb water and enlarge stools which stimulates propulsive movement through the lower GI tract
-no po absorption; excreted through stool as unchanged drug

748

Adverse effects of bulk laxatives:

N/V, abdominal fullness

749

Contraindications of bulk laxatives:

Bowel obstruction, under age of 6

750

Pregnancy Category bulk laxatives

B; safe in pregnancy and breastfeeding

751

Gastric motility agent (Metoclopramide/ Reglan) MOA

Binds to dopamine D2 receptors in CNS, as well as some 5-HT3 antagonism: gastric motility is caused by the D2 antagonism

752

Reglan: pharmacokinetics

Well-absorbed PO, 65-90% bioavailability
Metabolized via liver
Excreted via urine (decrease dose in renal insufficiency

753

Acid Reflux/ Gastritis:
prevalence, probable causes?

Very prevalent (10%) US pop
Several probable causes:
1. Transient lower esophageal sphincter relaxtion
2. Low resting lower esophageal sphincter
3. Poor esophageal acid clearance
4. Defects in esophagastric motility
5. Impaired mucosal resistance and over protective defenses

754

Descriptions and symptoms of gastritis

Burning sensation, nausea, chest pain, or globus (broad) sensation.
* can be very much like an MI ; differentiating SX - SOB, diaphoresis

755

Other contributing factors to gastritis?

Intake of acidic foods; treatment begins with removing these offenders / lifestyle modifications then mess

756

4 Types acid reflux/ gastritis meds

1. Antacids
2. Carafate
3. H2 receptor antagonists
4. PPI's

757

Antacids: sodium bicarbonate, calcium carbonate, magnesium hydroxide, aluminum hydroxide
MOA?

These are weak bases that fact with gastric acid to form a salt and water, therefore decreasing gastric acidity

758

Pharmokinetics/ dynamics of antacids

-Some po absorption; 25-35 % availability
-bicarbonate preps (bioavailability) improves with food bu hydroxide preparations poorly absorbed
-carbonate excreted via stool
-aluminum and mag excreted via urine

759

Pregnancy category of antacids

B, safe for breastfeeding as well

760

Antacids: adverse effects

N/V, constipation, dependence

761

Contraindications for taking antacids:

Renal Failure (for those with aluminum and magnesium) - ie, the re ally excreted ones

762

Carafate: MOA

Positively charged sucrose sulfate binds to negatively charged proteins in base of ulcers, forms an ADHERENT/ PROTECTIVE barrier from gastric acids and bile salts

763

Carafate: pharmacokinetics

-very little absorption, so not metabolized
-excreted in stool

764

Carafate: adverse effects

CONSTIPATION! Gotta love it!

765

Contraindications for use of Carafate-

Allergy; may use with caution with other meds... Can affect absorption

766

Carafate pregnancy category:

B ( off label for peds)

767

H2 receptor antagonists: Zantac, Pepcid, Tagamet
MOA?

Competitive inhibitors of H2 receptors in gastric parietal cells causing a decrease in gastric acid. No H1 or H3 efficacy (therefore not sedating).

768

H2 receptor antagonists: pharmacokinetics

-good po absorption
-metabolized via liver
-excreted in urine

769

H2 receptor antagonists
Adverse Effects

H/A, dizziness, confusion in elderly,
.....GYNECOMASTIA (for real!?!?!)

770

H2 receptor antagonists- contraindications

Potent P450 inhibitor!
Use Tagamet with caution in elderly

771

Pregnancy category for H2 receptor antagonists

B - also safe in peds

772

Proton Pump Inhibitors- Prilosec / omeprazole, Prevacid / lansoprazole, Protonix / pantoprazole, Nexium/ esomeprazole
MOA?

Binds irreversibly to H+/ K+ exchanging ATPase pumps (proton pumps) in gastric parietal cells, decreasing both basal and stimulated gastric acid secretion

773

PPI's: pharmacokinetics/ dynamics

-PRODRUG: must survive the acidic environment of stomach to be absorbed into small bowel
-all have fairly good bioavailability, decreased with po intake
-metab in liver / inhibits CYP2C19
-excreted in stool; **dose-adjust for hepatic disease**
-little renal excretion

774

PPI's: adverse effects

H/A, diarrhea, constipation, nausea, increased risk C. diff infection, ⬇️Mg with prolonged use,
⬆️ risk osteoporosis-related fractures with prolonged use

775

PPI's: contraindications

Allergy

776

Types of laxatives:

1. Bulk (Metamucil, fibercon)
2. Osmotic laxatives ( milk of mag, lactulose, mg citrate, polyethylene glycol (miralax)

777

Osmotic laxatives MOA:

Causes water retention in stool; soluble but no absorbable compounds

778

Pharmacokinetics of osmotic laxatives

NO PO absorption/ excreted in stool unchanged

779

Adverse effects of osmotic laxatives:

Diarrhea
abdominal complaints

780

Contraindications of osmotic laxatives:

-Existing electrolyte abnormality
-Age under 2 yo

781

Osmotic laxatives: great option for long or short term relief?

No adverse effects shown up to 12 months of daily use

782

Bulk laxatives - MOA?
Pharmacokinetics

Absorb water and enlarge stools which stimulates propulsive movement through the lower GI tract
-no po absorption; excreted through stool as unchanged drug

783

Adverse effects of bulk laxatives:

N/V, abdominal fullness

784

Contraindications of bulk laxatives:

Bowel obstruction, under age of 6

785

Pregnancy Category bulk laxatives

B; safe in pregnancy and breastfeeding

786

Gastric motility agent (Metoclopramide/ Reglan) MOA

Binds to dopamine D2 receptors in CNS, as well as some 5-HT3 antagonism: gastric motility is caused by the D2 antagonism

787

Reglan: pharmacokinetics

Well-absorbed PO, 65-90% bioavailability
Metabolized via liver
Excreted via urine (decrease dose in renal insufficiency

788

Acid Reflux/ Gastritis:
prevalence, probable causes?

Very prevalent (10%) US pop
Several probable causes:
1. Transient lower esophageal sphincter relaxtion
2. Low resting lower esophageal sphincter
3. Poor esophageal acid clearance
4. Defects in esophagastric motility
5. Impaired mucosal resistance and over protective defenses

789

Descriptions and symptoms of gastritis

Burning sensation, nausea, chest pain, or globus (broad) sensation.
* can be very much like an MI ; differentiating SX - SOB, diaphoresis

790

Other contributing factors to gastritis?

Intake of acidic foods; treatment begins with removing these offenders / lifestyle modifications then mess

791

4 Types acid reflux/ gastritis meds

1. Antacids
2. Carafate
3. H2 receptor antagonists
4. PPI's

792

Antacids: sodium bicarbonate, calcium carbonate, magnesium hydroxide, aluminum hydroxide
MOA?

These are weak bases that fact with gastric acid to form a salt and water, therefore decreasing gastric acidity

793

Pharmokinetics/ dynamics of antacids

-Some po absorption; 25-35 % availability
-bicarbonate preps (bioavailability) improves with food bu hydroxide preparations poorly absorbed
-carbonate excreted via stool
-aluminum and mag excreted via urine

794

Pregnancy category of antacids

B, safe for breastfeeding as well

795

Antacids: adverse effects

N/V, constipation, dependence

796

Contraindications for taking antacids:

Renal Failure (for those with aluminum and magnesium) - ie, the re ally excreted ones

797

Carafate: MOA

Positively charged sucrose sulfate binds to negatively charged proteins in base of ulcers, forms an ADHERENT/ PROTECTIVE barrier from gastric acids and bile salts

798

Carafate: pharmacokinetics

-very little absorption, so not metabolized
-excreted in stool

799

Carafate: adverse effects

CONSTIPATION! Gotta love it!

800

Contraindications for use of Carafate-

Allergy; may use with caution with other meds... Can affect absorption

801

Carafate pregnancy category:

B ( off label for peds)

802

H2 receptor antagonists: Zantac, Pepcid, Tagamet
MOA?

Competitive inhibitors of H2 receptors in gastric parietal cells causing a decrease in gastric acid. No H1 or H3 efficacy (therefore not sedating).

803

H2 receptor antagonists: pharmacokinetics

-good po absorption
-metabolized via liver
-excreted in urine

804

H2 receptor antagonists
Adverse Effects

H/A, dizziness, confusion in elderly,
.....GYNECOMASTIA (for real!?!?!)

805

H2 receptor antagonists- contraindications

Potent P450 inhibitor!
Use Tagamet with caution in elderly

806

Pregnancy category for H2 receptor antagonists

B - also safe in peds

807

Proton Pump Inhibitors- Prilosec / omeprazole, Prevacid / lansoprazole, Protonix / pantoprazole, Nexium/ esomeprazole
MOA?

Binds irreversibly to H+/ K+ exchanging ATPase pumps (proton pumps) in gastric parietal cells, decreasing both basal and stimulated gastric acid secretion

808

PPI's: pharmacokinetics/ dynamics

-PRODRUG: must survive the acidic environment of stomach to be absorbed into small bowel
-all have fairly good bioavailability, decreased with po intake
-metab in liver / inhibits CYP2C19
-excreted in stool; **dose-adjust for hepatic disease**
-little renal excretion

809

PPI's: adverse effects

H/A, diarrhea, constipation, nausea, increased risk C. diff infection, ⬇️Mg with prolonged use,
⬆️ risk osteoporosis-related fractures with prolonged use

810

PPI's: contraindications

Allergy

811

Types of laxatives:

1. Bulk (Metamucil, fibercon)
2. Osmotic laxatives ( milk of mag, lactulose, mg citrate, polyethylene glycol (miralax)

812

Osmotic laxatives MOA:

Causes water retention in stool; soluble but no absorbable compounds

813

Pharmacokinetics of osmotic laxatives

NO PO absorption/ excreted in stool unchanged

814

Adverse effects of osmotic laxatives:

Diarrhea
abdominal complaints

815

Contraindications of osmotic laxatives:

-Existing electrolyte abnormality
-Age under 2 yo

816

Osmotic laxatives: great option for long or short term relief?

No adverse effects shown up to 12 months of daily use

817

Bulk laxatives - MOA?
Pharmacokinetics

Absorb water and enlarge stools which stimulates propulsive movement through the lower GI tract
-no po absorption; excreted through stool as unchanged drug

818

Adverse effects of bulk laxatives:

N/V, abdominal fullness

819

Contraindications of bulk laxatives:

Bowel obstruction, under age of 6

820

Pregnancy Category bulk laxatives

B; safe in pregnancy and breastfeeding

821

Gastric motility agent (Metoclopramide/ Reglan) MOA

Binds to dopamine D2 receptors in CNS, as well as some 5-HT3 antagonism: gastric motility is caused by the D2 antagonism

822

Reglan: pharmacokinetics

Well-absorbed PO, 65-90% bioavailability
Metabolized via liver
Excreted via urine (decrease dose in renal insufficiency

823

Acid Reflux/ Gastritis:
prevalence, probable causes?

Very prevalent (10%) US pop
Several probable causes:
1. Transient lower esophageal sphincter relaxtion
2. Low resting lower esophageal sphincter
3. Poor esophageal acid clearance
4. Defects in esophagastric motility
5. Impaired mucosal resistance and over protective defenses

824

Descriptions and symptoms of gastritis

Burning sensation, nausea, chest pain, or globus (broad) sensation.
* can be very much like an MI ; differentiating SX - SOB, diaphoresis

825

Other contributing factors to gastritis?

Intake of acidic foods; treatment begins with removing these offenders / lifestyle modifications then mess

826

4 Types acid reflux/ gastritis meds

1. Antacids
2. Carafate
3. H2 receptor antagonists
4. PPI's

827

Antacids: sodium bicarbonate, calcium carbonate, magnesium hydroxide, aluminum hydroxide
MOA?

These are weak bases that fact with gastric acid to form a salt and water, therefore decreasing gastric acidity

828

Pharmokinetics/ dynamics of antacids

-Some po absorption; 25-35 % availability
-bicarbonate preps (bioavailability) improves with food bu hydroxide preparations poorly absorbed
-carbonate excreted via stool
-aluminum and mag excreted via urine

829

Pregnancy category of antacids

B, safe for breastfeeding as well

830

Antacids: adverse effects

N/V, constipation, dependence

831

Contraindications for taking antacids:

Renal Failure (for those with aluminum and magnesium) - ie, the re ally excreted ones

832

Carafate: MOA

Positively charged sucrose sulfate binds to negatively charged proteins in base of ulcers, forms an ADHERENT/ PROTECTIVE barrier from gastric acids and bile salts

833

Carafate: pharmacokinetics

-very little absorption, so not metabolized
-excreted in stool

834

Carafate: adverse effects

CONSTIPATION! Gotta love it!

835

Contraindications for use of Carafate-

Allergy; may use with caution with other meds... Can affect absorption

836

Carafate pregnancy category:

B ( off label for peds)

837

H2 receptor antagonists: Zantac, Pepcid, Tagamet
MOA?

Competitive inhibitors of H2 receptors in gastric parietal cells causing a decrease in gastric acid. No H1 or H3 efficacy (therefore not sedating).

838

H2 receptor antagonists: pharmacokinetics

-good po absorption
-metabolized via liver
-excreted in urine

839

H2 receptor antagonists
Adverse Effects

H/A, dizziness, confusion in elderly,
.....GYNECOMASTIA (for real!?!?!)

840

H2 receptor antagonists- contraindications

Potent P450 inhibitor!
Use Tagamet with caution in elderly

841

Pregnancy category for H2 receptor antagonists

B - also safe in peds

842

Proton Pump Inhibitors- Prilosec / omeprazole, Prevacid / lansoprazole, Protonix / pantoprazole, Nexium/ esomeprazole
MOA?

Binds irreversibly to H+/ K+ exchanging ATPase pumps (proton pumps) in gastric parietal cells, decreasing both basal and stimulated gastric acid secretion

843

PPI's: pharmacokinetics/ dynamics

-PRODRUG: must survive the acidic environment of stomach to be absorbed into small bowel
-all have fairly good bioavailability, decreased with po intake
-metab in liver / inhibits CYP2C19
-excreted in stool; **dose-adjust for hepatic disease**
-little renal excretion

844

PPI's: adverse effects

H/A, diarrhea, constipation, nausea, increased risk C. diff infection, ⬇️Mg with prolonged use,
⬆️ risk osteoporosis-related fractures with prolonged use

845

PPI's: contraindications

Allergy

846

Types of laxatives:

1. Bulk (Metamucil, fibercon)
2. Osmotic laxatives ( milk of mag, lactulose, mg citrate, polyethylene glycol (miralax)

847

Osmotic laxatives MOA:

Causes water retention in stool; soluble but no absorbable compounds

848

Pharmacokinetics of osmotic laxatives

NO PO absorption/ excreted in stool unchanged

849

Adverse effects of osmotic laxatives:

Diarrhea
abdominal complaints

850

Contraindications of osmotic laxatives:

-Existing electrolyte abnormality
-Age under 2 yo

851

Osmotic laxatives: great option for long or short term relief?

No adverse effects shown up to 12 months of daily use

852

Bulk laxatives - MOA?
Pharmacokinetics

Absorb water and enlarge stools which stimulates propulsive movement through the lower GI tract
-no po absorption; excreted through stool as unchanged drug

853

Adverse effects of bulk laxatives:

N/V, abdominal fullness

854

Contraindications of bulk laxatives:

Bowel obstruction, under age of 6

855

Pregnancy Category bulk laxatives

B; safe in pregnancy and breastfeeding

856

Gastric motility agent (Metoclopramide/ Reglan) MOA

Binds to dopamine D2 receptors in CNS, as well as some 5-HT3 antagonism: gastric motility is caused by the D2 antagonism

857

Reglan: pharmacokinetics

Well-absorbed PO, 65-90% bioavailability
Metabolized via liver
Excreted via urine (decrease dose in renal insufficiency

858

Acid Reflux/ Gastritis:
prevalence, probable causes?

Very prevalent (10%) US pop
Several probable causes:
1. Transient lower esophageal sphincter relaxtion
2. Low resting lower esophageal sphincter
3. Poor esophageal acid clearance
4. Defects in esophagastric motility
5. Impaired mucosal resistance and over protective defenses

859

Descriptions and symptoms of gastritis

Burning sensation, nausea, chest pain, or globus (broad) sensation.
* can be very much like an MI ; differentiating SX - SOB, diaphoresis

860

Other contributing factors to gastritis?

Intake of acidic foods; treatment begins with removing these offenders / lifestyle modifications then mess

861

4 Types acid reflux/ gastritis meds

1. Antacids
2. Carafate
3. H2 receptor antagonists
4. PPI's

862

Antacids: sodium bicarbonate, calcium carbonate, magnesium hydroxide, aluminum hydroxide
MOA?

These are weak bases that fact with gastric acid to form a salt and water, therefore decreasing gastric acidity

863

Pharmokinetics/ dynamics of antacids

-Some po absorption; 25-35 % availability
-bicarbonate preps (bioavailability) improves with food bu hydroxide preparations poorly absorbed
-carbonate excreted via stool
-aluminum and mag excreted via urine

864

Pregnancy category of antacids

B, safe for breastfeeding as well

865

Antacids: adverse effects

N/V, constipation, dependence

866

Contraindications for taking antacids:

Renal Failure (for those with aluminum and magnesium) - ie, the re ally excreted ones

867

Carafate: MOA

Positively charged sucrose sulfate binds to negatively charged proteins in base of ulcers, forms an ADHERENT/ PROTECTIVE barrier from gastric acids and bile salts

868

Carafate: pharmacokinetics

-very little absorption, so not metabolized
-excreted in stool

869

Carafate: adverse effects

CONSTIPATION! Gotta love it!

870

Contraindications for use of Carafate-

Allergy; may use with caution with other meds... Can affect absorption

871

Carafate pregnancy category:

B ( off label for peds)

872

H2 receptor antagonists: Zantac, Pepcid, Tagamet
MOA?

Competitive inhibitors of H2 receptors in gastric parietal cells causing a decrease in gastric acid. No H1 or H3 efficacy (therefore not sedating).

873

H2 receptor antagonists: pharmacokinetics

-good po absorption
-metabolized via liver
-excreted in urine

874

H2 receptor antagonists
Adverse Effects

H/A, dizziness, confusion in elderly,
.....GYNECOMASTIA (for real!?!?!)

875

H2 receptor antagonists- contraindications

Potent P450 inhibitor!
Use Tagamet with caution in elderly

876

Pregnancy category for H2 receptor antagonists

B - also safe in peds

877

Proton Pump Inhibitors- Prilosec / omeprazole, Prevacid / lansoprazole, Protonix / pantoprazole, Nexium/ esomeprazole
MOA?

Binds irreversibly to H+/ K+ exchanging ATPase pumps (proton pumps) in gastric parietal cells, decreasing both basal and stimulated gastric acid secretion

878

PPI's: pharmacokinetics/ dynamics

-PRODRUG: must survive the acidic environment of stomach to be absorbed into small bowel
-all have fairly good bioavailability, decreased with po intake
-metab in liver / inhibits CYP2C19
-excreted in stool; **dose-adjust for hepatic disease**
-little renal excretion

879

PPI's: adverse effects

H/A, diarrhea, constipation, nausea, increased risk C. diff infection, ⬇️Mg with prolonged use,
⬆️ risk osteoporosis-related fractures with prolonged use

880

PPI's: contraindications

Allergy

881

Types of laxatives:

1. Bulk (Metamucil, fibercon)
2. Osmotic laxatives ( milk of mag, lactulose, mg citrate, polyethylene glycol (miralax)

882

Osmotic laxatives MOA:

Causes water retention in stool; soluble but no absorbable compounds

883

Pharmacokinetics of osmotic laxatives

NO PO absorption/ excreted in stool unchanged

884

Adverse effects of osmotic laxatives:

Diarrhea
abdominal complaints

885

Contraindications of osmotic laxatives:

-Existing electrolyte abnormality
-Age under 2 yo

886

Osmotic laxatives: great option for long or short term relief?

No adverse effects shown up to 12 months of daily use

887

Bulk laxatives - MOA?
Pharmacokinetics

Absorb water and enlarge stools which stimulates propulsive movement through the lower GI tract
-no po absorption; excreted through stool as unchanged drug

888

Adverse effects of bulk laxatives:

N/V, abdominal fullness

889

Contraindications of bulk laxatives:

Bowel obstruction, under age of 6

890

Pregnancy Category bulk laxatives

B; safe in pregnancy and breastfeeding

891

Gastric motility agent (Metoclopramide/ Reglan) MOA

Binds to dopamine D2 receptors in CNS, as well as some 5-HT3 antagonism: gastric motility is caused by the D2 antagonism

892

Reglan: pharmacokinetics

Well-absorbed PO, 65-90% bioavailability
Metabolized via liver
Excreted via urine (decrease dose in renal insufficiency

893

Acid Reflux/ Gastritis:
prevalence, probable causes?

Very prevalent (10%) US pop
Several probable causes:
1. Transient lower esophageal sphincter relaxtion
2. Low resting lower esophageal sphincter
3. Poor esophageal acid clearance
4. Defects in esophagastric motility
5. Impaired mucosal resistance and over protective defenses

894

Descriptions and symptoms of gastritis

Burning sensation, nausea, chest pain, or globus (broad) sensation.
* can be very much like an MI ; differentiating SX - SOB, diaphoresis

895

Other contributing factors to gastritis?

Intake of acidic foods; treatment begins with removing these offenders / lifestyle modifications then mess

896

4 Types acid reflux/ gastritis meds

1. Antacids
2. Carafate
3. H2 receptor antagonists
4. PPI's

897

Antacids: sodium bicarbonate, calcium carbonate, magnesium hydroxide, aluminum hydroxide
MOA?

These are weak bases that fact with gastric acid to form a salt and water, therefore decreasing gastric acidity

898

Pharmokinetics/ dynamics of antacids

-Some po absorption; 25-35 % availability
-bicarbonate preps (bioavailability) improves with food bu hydroxide preparations poorly absorbed
-carbonate excreted via stool
-aluminum and mag excreted via urine

899

Pregnancy category of antacids

B, safe for breastfeeding as well

900

Antacids: adverse effects

N/V, constipation, dependence

901

Contraindications for taking antacids:

Renal Failure (for those with aluminum and magnesium) - ie, the re ally excreted ones

902

Carafate: MOA

Positively charged sucrose sulfate binds to negatively charged proteins in base of ulcers, forms an ADHERENT/ PROTECTIVE barrier from gastric acids and bile salts

903

Carafate: pharmacokinetics

-very little absorption, so not metabolized
-excreted in stool

904

Carafate: adverse effects

CONSTIPATION! Gotta love it!

905

Contraindications for use of Carafate-

Allergy; may use with caution with other meds... Can affect absorption

906

Carafate pregnancy category:

B ( off label for peds)

907

H2 receptor antagonists: Zantac, Pepcid, Tagamet
MOA?

Competitive inhibitors of H2 receptors in gastric parietal cells causing a decrease in gastric acid. No H1 or H3 efficacy (therefore not sedating).

908

H2 receptor antagonists: pharmacokinetics

-good po absorption
-metabolized via liver
-excreted in urine

909

H2 receptor antagonists
Adverse Effects

H/A, dizziness, confusion in elderly,
.....GYNECOMASTIA (for real!?!?!)

910

H2 receptor antagonists- contraindications

Potent P450 inhibitor!
Use Tagamet with caution in elderly

911

Pregnancy category for H2 receptor antagonists

B - also safe in peds

912

Proton Pump Inhibitors- Prilosec / omeprazole, Prevacid / lansoprazole, Protonix / pantoprazole, Nexium/ esomeprazole
MOA?

Binds irreversibly to H+/ K+ exchanging ATPase pumps (proton pumps) in gastric parietal cells, decreasing both basal and stimulated gastric acid secretion

913

PPI's: pharmacokinetics/ dynamics

-PRODRUG: must survive the acidic environment of stomach to be absorbed into small bowel
-all have fairly good bioavailability, decreased with po intake
-metab in liver / inhibits CYP2C19
-excreted in stool; **dose-adjust for hepatic disease**
-little renal excretion

914

PPI's: adverse effects

H/A, diarrhea, constipation, nausea, increased risk C. diff infection, ⬇️Mg with prolonged use,
⬆️ risk osteoporosis-related fractures with prolonged use

915

PPI's: contraindications

Allergy

916

Types of laxatives:

1. Bulk (Metamucil, fibercon)
2. Osmotic laxatives ( milk of mag, lactulose, mg citrate, polyethylene glycol (miralax)

917

Osmotic laxatives MOA:

Causes water retention in stool; soluble but no absorbable compounds

918

Pharmacokinetics of osmotic laxatives

NO PO absorption/ excreted in stool unchanged

919

Adverse effects of osmotic laxatives:

Diarrhea
abdominal complaints

920

Contraindications of osmotic laxatives:

-Existing electrolyte abnormality
-Age under 2 yo

921

Osmotic laxatives: great option for long or short term relief?

No adverse effects shown up to 12 months of daily use

922

Bulk laxatives - MOA?
Pharmacokinetics

Absorb water and enlarge stools which stimulates propulsive movement through the lower GI tract
-no po absorption; excreted through stool as unchanged drug

923

Adverse effects of bulk laxatives:

N/V, abdominal fullness

924

Contraindications of bulk laxatives:

Bowel obstruction, under age of 6

925

Pregnancy Category bulk laxatives

B; safe in pregnancy and breastfeeding

926

Gastric motility agent (Metoclopramide/ Reglan) MOA

Binds to dopamine D2 receptors in CNS, as well as some 5-HT3 antagonism: gastric motility is caused by the D2 antagonism

927

Reglan: pharmacokinetics

Well-absorbed PO, 65-90% bioavailability
Metabolized via liver
Excreted via urine (decrease dose in renal insufficiency

928

Acid Reflux/ Gastritis:
prevalence, probable causes?

Very prevalent (10%) US pop
Several probable causes:
1. Transient lower esophageal sphincter relaxtion
2. Low resting lower esophageal sphincter
3. Poor esophageal acid clearance
4. Defects in esophagastric motility
5. Impaired mucosal resistance and over protective defenses

929

Descriptions and symptoms of gastritis

Burning sensation, nausea, chest pain, or globus (broad) sensation.
* can be very much like an MI ; differentiating SX - SOB, diaphoresis

930

Other contributing factors to gastritis?

Intake of acidic foods; treatment begins with removing these offenders / lifestyle modifications then mess

931

4 Types acid reflux/ gastritis meds

1. Antacids
2. Carafate
3. H2 receptor antagonists
4. PPI's

932

Antacids: sodium bicarbonate, calcium carbonate, magnesium hydroxide, aluminum hydroxide
MOA?

These are weak bases that fact with gastric acid to form a salt and water, therefore decreasing gastric acidity

933

Pharmokinetics/ dynamics of antacids

-Some po absorption; 25-35 % availability
-bicarbonate preps (bioavailability) improves with food bu hydroxide preparations poorly absorbed
-carbonate excreted via stool
-aluminum and mag excreted via urine

934

Pregnancy category of antacids

B, safe for breastfeeding as well

935

Antacids: adverse effects

N/V, constipation, dependence

936

Contraindications for taking antacids:

Renal Failure (for those with aluminum and magnesium) - ie, the re ally excreted ones

937

Carafate: MOA

Positively charged sucrose sulfate binds to negatively charged proteins in base of ulcers, forms an ADHERENT/ PROTECTIVE barrier from gastric acids and bile salts

938

Carafate: pharmacokinetics

-very little absorption, so not metabolized
-excreted in stool

939

Carafate: adverse effects

CONSTIPATION! Gotta love it!

940

Contraindications for use of Carafate-

Allergy; may use with caution with other meds... Can affect absorption

941

Carafate pregnancy category:

B ( off label for peds)

942

H2 receptor antagonists: Zantac, Pepcid, Tagamet
MOA?

Competitive inhibitors of H2 receptors in gastric parietal cells causing a decrease in gastric acid. No H1 or H3 efficacy (therefore not sedating).

943

H2 receptor antagonists: pharmacokinetics

-good po absorption
-metabolized via liver
-excreted in urine

944

H2 receptor antagonists
Adverse Effects

H/A, dizziness, confusion in elderly,
.....GYNECOMASTIA (for real!?!?!)

945

H2 receptor antagonists- contraindications

Potent P450 inhibitor!
Use Tagamet with caution in elderly

946

Pregnancy category for H2 receptor antagonists

B - also safe in peds

947

Proton Pump Inhibitors- Prilosec / omeprazole, Prevacid / lansoprazole, Protonix / pantoprazole, Nexium/ esomeprazole
MOA?

Binds irreversibly to H+/ K+ exchanging ATPase pumps (proton pumps) in gastric parietal cells, decreasing both basal and stimulated gastric acid secretion

948

PPI's: pharmacokinetics/ dynamics

-PRODRUG: must survive the acidic environment of stomach to be absorbed into small bowel
-all have fairly good bioavailability, decreased with po intake
-metab in liver / inhibits CYP2C19
-excreted in stool; **dose-adjust for hepatic disease**
-little renal excretion

949

PPI's: adverse effects

H/A, diarrhea, constipation, nausea, increased risk C. diff infection, ⬇️Mg with prolonged use,
⬆️ risk osteoporosis-related fractures with prolonged use

950

PPI's: contraindications

Allergy

951

Types of laxatives:

1. Bulk (Metamucil, fibercon)
2. Osmotic laxatives ( milk of mag, lactulose, mg citrate, polyethylene glycol (miralax)

952

Osmotic laxatives MOA:

Causes water retention in stool; soluble but no absorbable compounds

953

Pharmacokinetics of osmotic laxatives

NO PO absorption/ excreted in stool unchanged

954

Adverse effects of osmotic laxatives:

Diarrhea
abdominal complaints

955

Contraindications of osmotic laxatives:

-Existing electrolyte abnormality
-Age under 2 yo

956

Osmotic laxatives: great option for long or short term relief?

No adverse effects shown up to 12 months of daily use

957

Bulk laxatives - MOA?
Pharmacokinetics

Absorb water and enlarge stools which stimulates propulsive movement through the lower GI tract
-no po absorption; excreted through stool as unchanged drug

958

Adverse effects of bulk laxatives:

N/V, abdominal fullness

959

Contraindications of bulk laxatives:

Bowel obstruction, under age of 6

960

Pregnancy Category bulk laxatives

B; safe in pregnancy and breastfeeding

961

Gastric motility agent (Metoclopramide/ Reglan) MOA

Binds to dopamine D2 receptors in CNS, as well as some 5-HT3 antagonism: gastric motility is caused by the D2 antagonism

962

Reglan: pharmacokinetics

Well-absorbed PO, 65-90% bioavailability
Metabolized via liver
Excreted via urine (decrease dose in renal insufficiency

963

Acid Reflux/ Gastritis:
prevalence, probable causes?

Very prevalent (10%) US pop
Several probable causes:
1. Transient lower esophageal sphincter relaxtion
2. Low resting lower esophageal sphincter
3. Poor esophageal acid clearance
4. Defects in esophagastric motility
5. Impaired mucosal resistance and over protective defenses

964

Descriptions and symptoms of gastritis

Burning sensation, nausea, chest pain, or globus (broad) sensation.
* can be very much like an MI ; differentiating SX - SOB, diaphoresis

965

Other contributing factors to gastritis?

Intake of acidic foods; treatment begins with removing these offenders / lifestyle modifications then mess

966

4 Types acid reflux/ gastritis meds

1. Antacids
2. Carafate
3. H2 receptor antagonists
4. PPI's

967

Antacids: sodium bicarbonate, calcium carbonate, magnesium hydroxide, aluminum hydroxide
MOA?

These are weak bases that fact with gastric acid to form a salt and water, therefore decreasing gastric acidity

968

Pharmokinetics/ dynamics of antacids

-Some po absorption; 25-35 % availability
-bicarbonate preps (bioavailability) improves with food bu hydroxide preparations poorly absorbed
-carbonate excreted via stool
-aluminum and mag excreted via urine

969

Pregnancy category of antacids

B, safe for breastfeeding as well

970

Antacids: adverse effects

N/V, constipation, dependence

971

Contraindications for taking antacids:

Renal Failure (for those with aluminum and magnesium) - ie, the re ally excreted ones

972

Carafate: MOA

Positively charged sucrose sulfate binds to negatively charged proteins in base of ulcers, forms an ADHERENT/ PROTECTIVE barrier from gastric acids and bile salts

973

Carafate: pharmacokinetics

-very little absorption, so not metabolized
-excreted in stool

974

Carafate: adverse effects

CONSTIPATION! Gotta love it!

975

Contraindications for use of Carafate-

Allergy; may use with caution with other meds... Can affect absorption

976

Carafate pregnancy category:

B ( off label for peds)

977

H2 receptor antagonists: Zantac, Pepcid, Tagamet
MOA?

Competitive inhibitors of H2 receptors in gastric parietal cells causing a decrease in gastric acid. No H1 or H3 efficacy (therefore not sedating).

978

H2 receptor antagonists: pharmacokinetics

-good po absorption
-metabolized via liver
-excreted in urine

979

H2 receptor antagonists
Adverse Effects

H/A, dizziness, confusion in elderly,
.....GYNECOMASTIA (for real!?!?!)

980

H2 receptor antagonists- contraindications

Potent P450 inhibitor!
Use Tagamet with caution in elderly

981

Pregnancy category for H2 receptor antagonists

B - also safe in peds

982

Proton Pump Inhibitors- Prilosec / omeprazole, Prevacid / lansoprazole, Protonix / pantoprazole, Nexium/ esomeprazole
MOA?

Binds irreversibly to H+/ K+ exchanging ATPase pumps (proton pumps) in gastric parietal cells, decreasing both basal and stimulated gastric acid secretion

983

PPI's: pharmacokinetics/ dynamics

-PRODRUG: must survive the acidic environment of stomach to be absorbed into small bowel
-all have fairly good bioavailability, decreased with po intake
-metab in liver / inhibits CYP2C19
-excreted in stool; **dose-adjust for hepatic disease**
-little renal excretion

984

PPI's: adverse effects

H/A, diarrhea, constipation, nausea, increased risk C. diff infection, ⬇️Mg with prolonged use,
⬆️ risk osteoporosis-related fractures with prolonged use

985

PPI's: contraindications

Allergy

986

Types of laxatives:

1. Bulk (Metamucil, fibercon)
2. Osmotic laxatives ( milk of mag, lactulose, mg citrate, polyethylene glycol (miralax)

987

Osmotic laxatives MOA:

Causes water retention in stool; soluble but no absorbable compounds

988

Pharmacokinetics of osmotic laxatives

NO PO absorption/ excreted in stool unchanged

989

Adverse effects of osmotic laxatives:

Diarrhea
abdominal complaints

990

Contraindications of osmotic laxatives:

-Existing electrolyte abnormality
-Age under 2 yo

991

Osmotic laxatives: great option for long or short term relief?

No adverse effects shown up to 12 months of daily use

992

Bulk laxatives - MOA?
Pharmacokinetics

Absorb water and enlarge stools which stimulates propulsive movement through the lower GI tract
-no po absorption; excreted through stool as unchanged drug

993

Adverse effects of bulk laxatives:

N/V, abdominal fullness

994

Contraindications of bulk laxatives:

Bowel obstruction, under age of 6

995

Pregnancy Category bulk laxatives

B; safe in pregnancy and breastfeeding

996

Gastric motility agent (Metoclopramide/ Reglan) MOA

Binds to dopamine D2 receptors in CNS, as well as some 5-HT3 antagonism: gastric motility is caused by the D2 antagonism

997

Reglan: pharmacokinetics

Well-absorbed PO, 65-90% bioavailability
Metabolized via liver
Excreted via urine (decrease dose in renal insufficiency

998

Acid Reflux/ Gastritis:
prevalence, probable causes?

Very prevalent (10%) US pop
Several probable causes:
1. Transient lower esophageal sphincter relaxtion
2. Low resting lower esophageal sphincter
3. Poor esophageal acid clearance
4. Defects in esophagastric motility
5. Impaired mucosal resistance and over protective defenses

999

Descriptions and symptoms of gastritis

Burning sensation, nausea, chest pain, or globus (broad) sensation.
* can be very much like an MI ; differentiating SX - SOB, diaphoresis

1000

Other contributing factors to gastritis?

Intake of acidic foods; treatment begins with removing these offenders / lifestyle modifications then mess

1001

4 Types acid reflux/ gastritis meds

1. Antacids
2. Carafate
3. H2 receptor antagonists
4. PPI's

1002

Antacids: sodium bicarbonate, calcium carbonate, magnesium hydroxide, aluminum hydroxide
MOA?

These are weak bases that fact with gastric acid to form a salt and water, therefore decreasing gastric acidity

1003

Pharmokinetics/ dynamics of antacids

-Some po absorption; 25-35 % availability
-bicarbonate preps (bioavailability) improves with food bu hydroxide preparations poorly absorbed
-carbonate excreted via stool
-aluminum and mag excreted via urine

1004

Pregnancy category of antacids

B, safe for breastfeeding as well

1005

Antacids: adverse effects

N/V, constipation, dependence

1006

Contraindications for taking antacids:

Renal Failure (for those with aluminum and magnesium) - ie, the re ally excreted ones

1007

Carafate: MOA

Positively charged sucrose sulfate binds to negatively charged proteins in base of ulcers, forms an ADHERENT/ PROTECTIVE barrier from gastric acids and bile salts

1008

Carafate: pharmacokinetics

-very little absorption, so not metabolized
-excreted in stool

1009

Carafate: adverse effects

CONSTIPATION! Gotta love it!

1010

Contraindications for use of Carafate-

Allergy; may use with caution with other meds... Can affect absorption

1011

Carafate pregnancy category:

B ( off label for peds)

1012

H2 receptor antagonists: Zantac, Pepcid, Tagamet
MOA?

Competitive inhibitors of H2 receptors in gastric parietal cells causing a decrease in gastric acid. No H1 or H3 efficacy (therefore not sedating).

1013

H2 receptor antagonists: pharmacokinetics

-good po absorption
-metabolized via liver
-excreted in urine

1014

H2 receptor antagonists
Adverse Effects

H/A, dizziness, confusion in elderly,
.....GYNECOMASTIA (for real!?!?!)

1015

H2 receptor antagonists- contraindications

Potent P450 inhibitor!
Use Tagamet with caution in elderly

1016

Pregnancy category for H2 receptor antagonists

B - also safe in peds

1017

Proton Pump Inhibitors- Prilosec / omeprazole, Prevacid / lansoprazole, Protonix / pantoprazole, Nexium/ esomeprazole
MOA?

Binds irreversibly to H+/ K+ exchanging ATPase pumps (proton pumps) in gastric parietal cells, decreasing both basal and stimulated gastric acid secretion

1018

PPI's: pharmacokinetics/ dynamics

-PRODRUG: must survive the acidic environment of stomach to be absorbed into small bowel
-all have fairly good bioavailability, decreased with po intake
-metab in liver / inhibits CYP2C19
-excreted in stool; **dose-adjust for hepatic disease**
-little renal excretion

1019

PPI's: adverse effects

H/A, diarrhea, constipation, nausea, increased risk C. diff infection, ⬇️Mg with prolonged use,
⬆️ risk osteoporosis-related fractures with prolonged use

1020

PPI's: contraindications

Allergy

1021

Types of laxatives:

1. Bulk (Metamucil, fibercon)
2. Osmotic laxatives ( milk of mag, lactulose, mg citrate, polyethylene glycol (miralax)

1022

Osmotic laxatives MOA:

Causes water retention in stool; soluble but no absorbable compounds

1023

Pharmacokinetics of osmotic laxatives

NO PO absorption/ excreted in stool unchanged

1024

Adverse effects of osmotic laxatives:

Diarrhea
abdominal complaints

1025

Contraindications of osmotic laxatives:

-Existing electrolyte abnormality
-Age under 2 yo

1026

Osmotic laxatives: great option for long or short term relief?

No adverse effects shown up to 12 months of daily use

1027

Bulk laxatives - MOA?
Pharmacokinetics

Absorb water and enlarge stools which stimulates propulsive movement through the lower GI tract
-no po absorption; excreted through stool as unchanged drug

1028

Adverse effects of bulk laxatives:

N/V, abdominal fullness

1029

Contraindications of bulk laxatives:

Bowel obstruction, under age of 6

1030

Pregnancy Category bulk laxatives

B; safe in pregnancy and breastfeeding

1031

Gastric motility agent (Metoclopramide/ Reglan) MOA

Binds to dopamine D2 receptors in CNS, as well as some 5-HT3 antagonism: gastric motility is caused by the D2 antagonism

1032

Reglan: pharmacokinetics

Well-absorbed PO, 65-90% bioavailability
Metabolized via liver
Excreted via urine (decrease dose in renal insufficiency

1033

Acid Reflux/ Gastritis:
prevalence, probable causes?

Very prevalent (10%) US pop
Several probable causes:
1. Transient lower esophageal sphincter relaxtion
2. Low resting lower esophageal sphincter
3. Poor esophageal acid clearance
4. Defects in esophagastric motility
5. Impaired mucosal resistance and over protective defenses

1034

Descriptions and symptoms of gastritis

Burning sensation, nausea, chest pain, or globus (broad) sensation.
* can be very much like an MI ; differentiating SX - SOB, diaphoresis

1035

Other contributing factors to gastritis?

Intake of acidic foods; treatment begins with removing these offenders / lifestyle modifications then mess

1036

4 Types acid reflux/ gastritis meds

1. Antacids
2. Carafate
3. H2 receptor antagonists
4. PPI's

1037

Antacids: sodium bicarbonate, calcium carbonate, magnesium hydroxide, aluminum hydroxide
MOA?

These are weak bases that fact with gastric acid to form a salt and water, therefore decreasing gastric acidity

1038

Pharmokinetics/ dynamics of antacids

-Some po absorption; 25-35 % availability
-bicarbonate preps (bioavailability) improves with food bu hydroxide preparations poorly absorbed
-carbonate excreted via stool
-aluminum and mag excreted via urine

1039

Pregnancy category of antacids

B, safe for breastfeeding as well

1040

Antacids: adverse effects

N/V, constipation, dependence

1041

Contraindications for taking antacids:

Renal Failure (for those with aluminum and magnesium) - ie, the re ally excreted ones

1042

Carafate: MOA

Positively charged sucrose sulfate binds to negatively charged proteins in base of ulcers, forms an ADHERENT/ PROTECTIVE barrier from gastric acids and bile salts

1043

Carafate: pharmacokinetics

-very little absorption, so not metabolized
-excreted in stool

1044

Carafate: adverse effects

CONSTIPATION! Gotta love it!

1045

Contraindications for use of Carafate-

Allergy; may use with caution with other meds... Can affect absorption

1046

Carafate pregnancy category:

B ( off label for peds)

1047

H2 receptor antagonists: Zantac, Pepcid, Tagamet
MOA?

Competitive inhibitors of H2 receptors in gastric parietal cells causing a decrease in gastric acid. No H1 or H3 efficacy (therefore not sedating).

1048

H2 receptor antagonists: pharmacokinetics

-good po absorption
-metabolized via liver
-excreted in urine

1049

H2 receptor antagonists
Adverse Effects

H/A, dizziness, confusion in elderly,
.....GYNECOMASTIA (for real!?!?!)

1050

H2 receptor antagonists- contraindications

Potent P450 inhibitor!
Use Tagamet with caution in elderly

1051

Pregnancy category for H2 receptor antagonists

B - also safe in peds

1052

Proton Pump Inhibitors- Prilosec / omeprazole, Prevacid / lansoprazole, Protonix / pantoprazole, Nexium/ esomeprazole
MOA?

Binds irreversibly to H+/ K+ exchanging ATPase pumps (proton pumps) in gastric parietal cells, decreasing both basal and stimulated gastric acid secretion

1053

PPI's: pharmacokinetics/ dynamics

-PRODRUG: must survive the acidic environment of stomach to be absorbed into small bowel
-all have fairly good bioavailability, decreased with po intake
-metab in liver / inhibits CYP2C19
-excreted in stool; **dose-adjust for hepatic disease**
-little renal excretion

1054

PPI's: adverse effects

H/A, diarrhea, constipation, nausea, increased risk C. diff infection, ⬇️Mg with prolonged use,
⬆️ risk osteoporosis-related fractures with prolonged use

1055

PPI's: contraindications

Allergy

1056

Types of laxatives:

1. Bulk (Metamucil, fibercon)
2. Osmotic laxatives ( milk of mag, lactulose, mg citrate, polyethylene glycol (miralax)

1057

Osmotic laxatives MOA:

Causes water retention in stool; soluble but no absorbable compounds

1058

Pharmacokinetics of osmotic laxatives

NO PO absorption/ excreted in stool unchanged

1059

Adverse effects of osmotic laxatives:

Diarrhea
abdominal complaints

1060

Contraindications of osmotic laxatives:

-Existing electrolyte abnormality
-Age under 2 yo

1061

Osmotic laxatives: great option for long or short term relief?

No adverse effects shown up to 12 months of daily use

1062

Bulk laxatives - MOA?
Pharmacokinetics

Absorb water and enlarge stools which stimulates propulsive movement through the lower GI tract
-no po absorption; excreted through stool as unchanged drug

1063

Adverse effects of bulk laxatives:

N/V, abdominal fullness

1064

Contraindications of bulk laxatives:

Bowel obstruction, under age of 6

1065

Pregnancy Category bulk laxatives

B; safe in pregnancy and breastfeeding

1066

Gastric motility agent (Metoclopramide/ Reglan) MOA

Binds to dopamine D2 receptors in CNS, as well as some 5-HT3 antagonism: gastric motility is caused by the D2 antagonism

1067

Reglan: pharmacokinetics

Well-absorbed PO, 65-90% bioavailability
Metabolized via liver
Excreted via urine (decrease dose in renal insufficiency

1068

Acid Reflux/ Gastritis:
prevalence, probable causes?

Very prevalent (10%) US pop
Several probable causes:
1. Transient lower esophageal sphincter relaxtion
2. Low resting lower esophageal sphincter
3. Poor esophageal acid clearance
4. Defects in esophagastric motility
5. Impaired mucosal resistance and over protective defenses

1069

Descriptions and symptoms of gastritis

Burning sensation, nausea, chest pain, or globus (broad) sensation.
* can be very much like an MI ; differentiating SX - SOB, diaphoresis

1070

Other contributing factors to gastritis?

Intake of acidic foods; treatment begins with removing these offenders / lifestyle modifications then mess

1071

4 Types acid reflux/ gastritis meds

1. Antacids
2. Carafate
3. H2 receptor antagonists
4. PPI's

1072

Antacids: sodium bicarbonate, calcium carbonate, magnesium hydroxide, aluminum hydroxide
MOA?

These are weak bases that fact with gastric acid to form a salt and water, therefore decreasing gastric acidity

1073

Pharmokinetics/ dynamics of antacids

-Some po absorption; 25-35 % availability
-bicarbonate preps (bioavailability) improves with food bu hydroxide preparations poorly absorbed
-carbonate excreted via stool
-aluminum and mag excreted via urine

1074

Pregnancy category of antacids

B, safe for breastfeeding as well

1075

Antacids: adverse effects

N/V, constipation, dependence

1076

Contraindications for taking antacids:

Renal Failure (for those with aluminum and magnesium) - ie, the re ally excreted ones

1077

Carafate: MOA

Positively charged sucrose sulfate binds to negatively charged proteins in base of ulcers, forms an ADHERENT/ PROTECTIVE barrier from gastric acids and bile salts

1078

Carafate: pharmacokinetics

-very little absorption, so not metabolized
-excreted in stool

1079

Carafate: adverse effects

CONSTIPATION! Gotta love it!

1080

Contraindications for use of Carafate-

Allergy; may use with caution with other meds... Can affect absorption

1081

Carafate pregnancy category:

B ( off label for peds)

1082

H2 receptor antagonists: Zantac, Pepcid, Tagamet
MOA?

Competitive inhibitors of H2 receptors in gastric parietal cells causing a decrease in gastric acid. No H1 or H3 efficacy (therefore not sedating).

1083

H2 receptor antagonists: pharmacokinetics

-good po absorption
-metabolized via liver
-excreted in urine

1084

H2 receptor antagonists
Adverse Effects

H/A, dizziness, confusion in elderly,
.....GYNECOMASTIA (for real!?!?!)

1085

H2 receptor antagonists- contraindications

Potent P450 inhibitor!
Use Tagamet with caution in elderly

1086

Pregnancy category for H2 receptor antagonists

B - also safe in peds

1087

Proton Pump Inhibitors- Prilosec / omeprazole, Prevacid / lansoprazole, Protonix / pantoprazole, Nexium/ esomeprazole
MOA?

Binds irreversibly to H+/ K+ exchanging ATPase pumps (proton pumps) in gastric parietal cells, decreasing both basal and stimulated gastric acid secretion

1088

PPI's: pharmacokinetics/ dynamics

-PRODRUG: must survive the acidic environment of stomach to be absorbed into small bowel
-all have fairly good bioavailability, decreased with po intake
-metab in liver / inhibits CYP2C19
-excreted in stool; **dose-adjust for hepatic disease**
-little renal excretion

1089

PPI's: adverse effects

H/A, diarrhea, constipation, nausea, increased risk C. diff infection, ⬇️Mg with prolonged use,
⬆️ risk osteoporosis-related fractures with prolonged use

1090

PPI's: contraindications

Allergy

1091

Types of laxatives:

1. Bulk (Metamucil, fibercon)
2. Osmotic laxatives ( milk of mag, lactulose, mg citrate, polyethylene glycol (miralax)

1092

Osmotic laxatives MOA:

Causes water retention in stool; soluble but no absorbable compounds

1093

Pharmacokinetics of osmotic laxatives

NO PO absorption/ excreted in stool unchanged

1094

Adverse effects of osmotic laxatives:

Diarrhea
abdominal complaints

1095

Contraindications of osmotic laxatives:

-Existing electrolyte abnormality
-Age under 2 yo

1096

Osmotic laxatives: great option for long or short term relief?

No adverse effects shown up to 12 months of daily use

1097

Bulk laxatives - MOA?
Pharmacokinetics

Absorb water and enlarge stools which stimulates propulsive movement through the lower GI tract
-no po absorption; excreted through stool as unchanged drug

1098

Adverse effects of bulk laxatives:

N/V, abdominal fullness

1099

Contraindications of bulk laxatives:

Bowel obstruction, under age of 6

1100

Pregnancy Category bulk laxatives

B; safe in pregnancy and breastfeeding

1101

Gastric motility agent (Metoclopramide/ Reglan) MOA

Binds to dopamine D2 receptors in CNS, as well as some 5-HT3 antagonism: gastric motility is caused by the D2 antagonism

1102

Reglan: pharmacokinetics

Well-absorbed PO, 65-90% bioavailability
Metabolized via liver
Excreted via urine (decrease dose in renal insufficiency

1103

Acid Reflux/ Gastritis:
prevalence, probable causes?

Very prevalent (10%) US pop
Several probable causes:
1. Transient lower esophageal sphincter relaxtion
2. Low resting lower esophageal sphincter
3. Poor esophageal acid clearance
4. Defects in esophagastric motility
5. Impaired mucosal resistance and over protective defenses

1104

Descriptions and symptoms of gastritis

Burning sensation, nausea, chest pain, or globus (broad) sensation.
* can be very much like an MI ; differentiating SX - SOB, diaphoresis

1105

Other contributing factors to gastritis?

Intake of acidic foods; treatment begins with removing these offenders / lifestyle modifications then mess

1106

4 Types acid reflux/ gastritis meds

1. Antacids
2. Carafate
3. H2 receptor antagonists
4. PPI's

1107

Antacids: sodium bicarbonate, calcium carbonate, magnesium hydroxide, aluminum hydroxide
MOA?

These are weak bases that fact with gastric acid to form a salt and water, therefore decreasing gastric acidity

1108

Pharmokinetics/ dynamics of antacids

-Some po absorption; 25-35 % availability
-bicarbonate preps (bioavailability) improves with food bu hydroxide preparations poorly absorbed
-carbonate excreted via stool
-aluminum and mag excreted via urine

1109

Pregnancy category of antacids

B, safe for breastfeeding as well

1110

Antacids: adverse effects

N/V, constipation, dependence

1111

Contraindications for taking antacids:

Renal Failure (for those with aluminum and magnesium) - ie, the re ally excreted ones

1112

Carafate: MOA

Positively charged sucrose sulfate binds to negatively charged proteins in base of ulcers, forms an ADHERENT/ PROTECTIVE barrier from gastric acids and bile salts

1113

Carafate: pharmacokinetics

-very little absorption, so not metabolized
-excreted in stool

1114

Carafate: adverse effects

CONSTIPATION! Gotta love it!

1115

Contraindications for use of Carafate-

Allergy; may use with caution with other meds... Can affect absorption

1116

Carafate pregnancy category:

B ( off label for peds)

1117

H2 receptor antagonists: Zantac, Pepcid, Tagamet
MOA?

Competitive inhibitors of H2 receptors in gastric parietal cells causing a decrease in gastric acid. No H1 or H3 efficacy (therefore not sedating).

1118

H2 receptor antagonists: pharmacokinetics

-good po absorption
-metabolized via liver
-excreted in urine

1119

H2 receptor antagonists
Adverse Effects

H/A, dizziness, confusion in elderly,
.....GYNECOMASTIA (for real!?!?!)

1120

H2 receptor antagonists- contraindications

Potent P450 inhibitor!
Use Tagamet with caution in elderly

1121

Pregnancy category for H2 receptor antagonists

B - also safe in peds

1122

Proton Pump Inhibitors- Prilosec / omeprazole, Prevacid / lansoprazole, Protonix / pantoprazole, Nexium/ esomeprazole
MOA?

Binds irreversibly to H+/ K+ exchanging ATPase pumps (proton pumps) in gastric parietal cells, decreasing both basal and stimulated gastric acid secretion

1123

PPI's: pharmacokinetics/ dynamics

-PRODRUG: must survive the acidic environment of stomach to be absorbed into small bowel
-all have fairly good bioavailability, decreased with po intake
-metab in liver / inhibits CYP2C19
-excreted in stool; **dose-adjust for hepatic disease**
-little renal excretion

1124

PPI's: adverse effects

H/A, diarrhea, constipation, nausea, increased risk C. diff infection, ⬇️Mg with prolonged use,
⬆️ risk osteoporosis-related fractures with prolonged use

1125

PPI's: contraindications

Allergy

1126

Types of laxatives:

1. Bulk (Metamucil, fibercon)
2. Osmotic laxatives ( milk of mag, lactulose, mg citrate, polyethylene glycol (miralax)

1127

Osmotic laxatives MOA:

Causes water retention in stool; soluble but no absorbable compounds

1128

Pharmacokinetics of osmotic laxatives