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GI Drugs Flashcards

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1
Q

Antacids moa

A

Weak bases that act locally in the stomach by neutralizing gastric acidity

Stimulates PG production

Binds bile salts

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2
Q

Antacid DOA
Fasting:
W/ meals:

A

Fasting: 30 mins

W/ meals: 2-3 hours

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3
Q

Antacid prescription

A

Given 1 and 3 hours after meals and at bedtime

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4
Q

Antacid preparations

Scam

A

Sodium bicarbonate
Calcium bicarbonate
Aluminum hydroxide
Magnesium hydroxide

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5
Q

NAHCO3 adverse effects

A

Fluid retention

Metabolic alkalosis

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6
Q

CaCO3 adverse effect

A

Hypercalcemia

Nephrolithiasis

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7
Q

Aluminum Hydroxide adverse fx

A

Osteoporosis

Hypophosphatemimilk-alkali syndrome(inc Ca, MA, RI)

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8
Q

MgOH adverse fx

A

Osmotic diarrhea

Hypermagnesemia

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9
Q

[PUD]

Drugs that reduce intragastric acidity (AHP)

A

Antacids
H2 receptor Atagonists
Proton pump inhibitors

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10
Q

Antacids drug interaction

A

It should be taken 2 hrs before or after taking other drugs

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11
Q

H2Receptor Antagonist Drugs

A

Cimetidine
Ranitidine
Famotidine
Nizatidine

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12
Q

H2RA Pk

A

Rapidly absorbed
Not affected by food
Cross bbb and placenta
First pass metab

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13
Q

Moa of H2RA

A

Competitive inhibitors of histamine at H2 receptors in parietal cells

Suppress basal and meal-induced acid secretion

Decrease volume of gastrin secretion and concentration of pepsin

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14
Q

H2RA clinical uses

A

GERD
PUD
NUD
Stress-related gastritis or bleeding

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15
Q

H2RA adverse fx in CNS

A

Altered mental status like headache hallucinations confusion delirium

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16
Q

Endocrine fx of H2RA
Cardiac
Pregnancy
Rare

A 
Men: gynecomastia and impotence
Women: galactorrhea
Bradycardia
No teratogenic fx
Blood dyscrasia
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17
Q

PPI DRUGS

A

Omeprazole

Esomeprarazole

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18
Q

PPI Pk (6)

A 
Highly protein bound
F decreased by 50 pc bc of food
Rapidly absorbed
Acid-labile
All are inactive prodrugs that require activation in an acid environment
Rapid first pass
Rebal clearance
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19
Q

PPI MOA

A

Inhibit fasting and meal-stimulated acid secretion

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20
Q

PPI CLINICAL USES

A 
GERD
PUD
NUD
stress-related gastric bleeding
Gastrinoma and other hypersecretory conditions
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21
Q

PPI ADVERSE FX

A 
Nausea
Abdominal pain
Constipation
Diarrhea
Skin rashes
No teratogenicity
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22
Q

Nutritional fx of ppi

A

Affect absorption of vit b12 and fe ca zinc esp in prolonged use

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23
Q

Respi and enteric infections of ppi

A

Increase in gastric bacterial concentration-> increase risk for HAP CAP and clostridium difficile

Inc gastrin levels- ECL hyperplasia
Gastric carcinoid tumors

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24
Q

[PUD]

Agents that promote mucosal protection

A

Sucralfate
Prostaglandin analogs
Colloidal Bismuth Conpounds

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25
MOA SUCRALFATE
Polymerization and selective binding to necrotic ulcer tissue to act as a barrier against pepsin gastrin and bile for up to six hrs after a single doe
26
AE OF SUCRALFATE
Nausea and constipation
27
Colloidal Bismuth Compounds MOA
Selectively binds to ulcer coating it and protecting it from gastin and pepsin Other: inhibit pepsjn activity, stimulate mucus production and increase prostaglandin secretion
28
Prostaglandin analogs
Misoprostol and rebamipide
29
Misoprostol moa
Both acid inhibitory and mucosal protective properties
30
Rebamipide moa
PG synthesis and scavenging ros
31
Pg analog fx
Reduce incidence of nsaid-induced ulcer and ulcer complication Stimulate uterine contractions
32
Agents used to eradicate H. Pylori | Clinical use
Ppi in triple therapy (with antibiotics) | To prevent ulcer recurrence
33
Prokinetic agents moa
Selectively stimulate gut motor function
34
Prokinetic agents
Cholinomimetic agents Dopamine receptor antagonist Macrolides 5-HT4 agonist
35
Cholinomimetic agents
Bethanecol | Neostigmine
36
Bethanecol Moa Clinical use
Stimulate M3 receptors | gerd
37
Neostigmine Moa Clinical uses
Acetylcholinesterase inhibitor Enhance gastric, si, and colonic emptying Ogilvie's syndrome
38
Cholinomimetic agents effects
Excessive salivation, nausea, vomiting diarrhea bradycardia
39
Dopamine receptor antagonists
Domperidone | Metoclopromide
40
DRA MOA
Blocks the inhibitory effect of dopamine receptors-> increase esophageal peristaltic amplitude, increase LES pressure, enhance gastric emptying, no fx on si and colonic motility
41
DRA MOA
Also block D2 receptors in the chemoteceptor trigger zone of tbe medulla -> antinausea and antiemetic action
42
DRA CLINICAL USES
``` GERD postsurgical and diabetic gastroparesis Prevention and treatment for vomiting NUD Promote postpartum lactation (domperidone) ```
43
Metoclopromide CNS AE | Extrapyramidal effects
Insomnia, anxiety, agitation Dystonias akathisia parkinsonian features Tardive diskinesia
44
Metoclopromide and domperidone | AE
``` Prolactenemia Galactorrhea Gynecomastia Impotence Menstrual disorders ```
45
Macrolides moa | Exaple and use
Stimulate motilin receptors on GI smooth muscle and promote MMC Erythromycin: gastroparesis
46
Laxatives classification
Stimulants or irritants Luminally active agents Prokinetic agents
47
Bulk forming agents examples | AE
Bran, psylliumbloating flatus
48
Osmotic laxatives moa | Clinical use
Soluble but nonabsorbable cmpds-> increase stool liquidity due to an obligate increase in fecal fluid Use: treatment of acute constipation or prevention of chronic constipation
49
Osmotic laxatives Example Subexample with AE
Nonabsorbable sugars or salts: lead to intravascular volume depletion and intravascular volume depletion - milk of magnesia: hypermagnesemia - mg citrate and na phosphate: - Sorbitol and lactulose: severe flatulose and cramps - Polyethylene glycol
50
Stool softeners Examples Use
Mineral oil and docusate glycerin supository | Prevent constipation and prevent straining
51
Stimulant lacatives moa
Induce bowel movement thru direct stimulation of ens and colonic electrolyte and fluid secretion
52
Stinulant laxatives examples
Anthraquinones- cascara and aloe::melanosis coli Diphenylmethane derivatives- bisacodyl Castor oil
53
Chloride channel activator moa
Stimulation kf chloride channel openjng in the SI increases Cl- rich fluid secretion into the intestine and shortens intestinal transit time
54
Cl channel activator uses | Example
Chronic constipaion and IBS-C Lubiprostone Linaclotide
55
Opioid receptor antagonist Moa Example and uses Ae
Inhibit peripheral mu-opioid receptors Methylnaltrexone- treatment of opioid induced constipation Alvimopan- postoperative ileus Cardiovascular toxicity
56
``` Serotonin 5-HT4 receptor agonist Moa Example Use AE ```
Stimulates second order enteric neurons to promote peristaltic reflex Chronic constipation and IBS constipation Cardiovascular due to QT prolongation of tegaserod Tegaserod and prucalopride
57
Antidiarrheal agents
Fluid and electrolyte therapy Antidiarrheal agents Treat the underlying cause
58
Fluid and electrolyte therapy
Oral rehydration solution | Parenteral ivf
59
Antidiarrheal agents | Examples
Opioid agonists Bile salt binding resin Somatistatin/octreotide
60
Opioid agonist | Effect
Loperamide- dies not cross bbb not analgesic no ptential for addiction Diphenoxylate Increase colonic transit time and fecal water absorption Decrease mass colonic movement and gastrocolic reflex
61
Bile salt binding resins Example Ae
Cholestyramine and colestipol- decrease diarrhea caused by excess fecal bile acids Bloating flatulence
62
Somatostatin/Octreotide effects
Somatostatin- inhibit secretion of hormones, reduce intestinal fluid secretion and pancreatic secretion, slows gi motility (kulang) Octreo same
63
S/O uses
Gi neuroendocrine tumors pancreatic fistula, GI bleeding
64
S/O ae
Bradycardia, steatorrhea, hypothyroidism
65
Treat the underlying cause
Antimicrobials | Dietary modif
66
Drugs for IBS
Serotonin 5-HT3 receptor antagonists Antispasmodics Clrode channel activator
67
Antispasmodics Ex Moa Ae
Dicyclomine & hyocyamine Inhibit muscariniv cholinergic receptors jn the enteric plexus and on sm: for abdominal pakn and disconfort Dry mouth visual disturbancesconstipation
68
Prokinetic agents moa
Selectively stimulate gut motor function
69
Prokinetic agents
Cholinomimetic agents Dopamine receptor antagonist Macrolides 5-HT4 agonist
70
Cholinomimetic agents
Bethanecol | Neostigmine
71
Bethanecol Moa Clinical use
Stimulate M3 receptors | gerd
72
Neostigmine Moa Clinical uses
Acetylcholinesterase inhibitor Enhance gastric, si, and colonic emptying Ogilvie's syndrome
73
Antispasmodics Ex Moa Ae
Dicyclomine & hyocyamine Inhibit muscariniv cholinergic receptors jn the enteric plexus and on sm: for abdominal pakn and disconfort Dry mouth visual disturbancesconstipation
74
Drugs for IBS
Serotonin 5-HT3 receptor antagonists Antispasmodics Clrode channel activator
75
Treat the underlying cause
Antimicrobials | Dietary modif
76
S/O ae
Bradycardia, steatorrhea, hypothyroidism
77
S/O uses
Gi neuroendocrine tumors pancreatic fistula, GI bleeding
78
Somatostatin/Octreotide effects
Somatostatin- inhibit secretion of hormones, reduce intestinal fluid secretion and pancreatic secretion, slows gi motility (kulang) Octreo same
79
Bile salt binding resins Example Ae
Cholestyramine and colestipol- decrease diarrhea caused by excess fecal bile acids Bloating flatulence
80
Opioid agonist | Effect
Loperamide- dies not cross bbb not analgesic no ptential for addiction Diphenoxylate Increase colonic transit time and fecal water absorption Decrease mass colonic movement and gastrocolic reflex
81
Antidiarrheal agents | Examples
Opioid agonists Bile salt binding resin Somatistatin/octreotide
82
Fluid and electrolyte therapy
Oral rehydration solution | Parenteral ivf
83
Antidiarrheal agents
Fluid and electrolyte therapy Antidiarrheal agents Treat the underlying cause
84
``` Serotonin 5-HT4 receptor agonist Moa Example Use AE ```
Stimulates second order enteric neurons to promote peristaltic reflex Chronic constipation and IBS constipation Cardiovascular due to QT prolongation of tegaserod Tegaserod and prucalopride
85
Opioid receptor antagonist Moa Example and uses Ae
Inhibit peripheral mu-opioid receptors Methylnaltrexone- treatment of opioid induced constipation Alvimopan- postoperative ileus Cardiovascular toxicity
86
Cl channel activator uses | Example
Chronic constipaion and IBS-C Lubiprostone Linaclotide
87
Chloride channel activator moa
Stimulation kf chloride channel openjng in the SI increases Cl- rich fluid secretion into the intestine and shortens intestinal transit time
88
Stinulant laxatives examples
Anthraquinones- cascara and aloe::melanosis coli Diphenylmethane derivatives- bisacodyl Castor oil
89
Stimulant lacatives moa
Induce bowel movement thru direct stimulation of ens and colonic electrolyte and fluid secretion
90
Stool softeners Examples Use
Mineral oil and docusate glycerin supository | Prevent constipation and prevent straining
91
Osmotic laxatives Example Subexample with AE
Nonabsorbable sugars or salts: lead to intravascular volume depletion and intravascular volume depletion - milk of magnesia: hypermagnesemia - mg citrate and na phosphate: - Sorbitol and lactulose: severe flatulose and cramps - Polyethylene glycol
92
Osmotic laxatives moa | Clinical use
Soluble but nonabsorbable cmpds-> increase stool liquidity due to an obligate increase in fecal fluid Use: treatment of acute constipation or prevention of chronic constipation
93
Bulk forming agents examples | AE
Bran, psylliumbloating flatus
94
Laxatives classification
Stimulants or irritants Luminally active agents Prokinetic agents
95
Macrolides moa | Exaple and use
Stimulate motilin receptors on GI smooth muscle and promote MMC Erythromycin: gastroparesis
96
Metoclopromide and domperidone | AE
``` Prolactenemia Galactorrhea Gynecomastia Impotence Menstrual disorders ```
97
Metoclopromide CNS AE | Extrapyramidal effects
Insomnia, anxiety, agitation Dystonias akathisia parkinsonian features Tardive diskinesia
98
Serotonin 5-HT3 receptor antagonist Moa Ex use Ae
Inhibit colonic motility esp in left colon inc total colonic transit time Alosetron- IBS with diarrhea Constipation
99
Antiemetics
``` Serotonin 5-HT3 antagonists Corticosteroids Neurokinin receptor antagonists Phenothiazined and butyrophenones Substituted benzamides H1 antihistamines and anticholinergics Benzodiazepines Cannabinoids ```
100
``` [antiemetics] Serotonin 5-HT3 antagonists Moa Examples Ae ```
Block receptors in the vomiting center and CTZ and peripheral receptors kn extrinsic intestinal vagal anf soinal sfferent nerves Ondansetron Headachedizzines constipation prolong qt interval
101
Corticosteroids Ex Moa
Dexamethadone and methylprednisolone | Enhance efficacy of 5-HT3 receptor antagonists for prevention of comit due to chemo
102
Neurokinin receptor antagonist Moa Ex- characteristics
Central blockage in the area postrema | Aprepitant- highly selective NK1 receptor antagonist crosses bbb
103
Phenothiazines Moa Ex
Inhibit dopamine and muscarinic receptors | Prochlorperazine
104
Butyrophenones
Central dopaminergic blockade
105
Substituted benzamines Ex Moa Ae
Metoclopromide Dopamine receptor blockade Extrapyramidal effect: restlessness parkinsonian symptoms
106
H1 antihistamines and anticholinergics Ae Use Ex- use
Treatment of motion sickness Dizziness sedation Diphenhydramine- sedating Meclizine- less sedation; motion sickness and vertigo due to labyrinth dys Huoscine(scopolamine)- muscarinic receptor antagonist; motion sickness
107
Benzodiazepines
Lorazepam or diazepam- used prior to chemo to reduce vomiting/ vomiting due to anciety
108
Cannabinoids Ex- use Ae
Drinabinol-as appetite stimulant and antiemetic - euphoria sedation hallucination Nabiline- thc analog
109
Drugs used tn treat inflammatory bowel disease
Azo cmpds- sulfasalazine | Mesalamine cmpds- rowasa
110
[IBD] | Immunosuppressive agents
``` Glucocorticoids Purjne analogs Methotrexate AntiTNF therapy Anti-integrin therapy ```
111
[IBD] Immunosuppressive agents GLUCOCORTICOIDS EX Mode
Prednisone prednisolone | Rectal
112
``` [IBD] Immunosuppressive agents PURJNE ANALOGS Ex Use Ae ```
Azathioprine and 6- mercaptopurine For jnduction and maintenance of remission of ulcrrative colitis and Chron's disease Nausea vomiting
113
``` [IBD] Immunosuppressive agents Methotrexate Moa Use Ae ```
Inhibit dihydrofolate reductase; interfere with inflamm action of Il-1 Induce and maintain remission in Chron's Bone mattoe duppression alopecia
114
AntitNF therapy Ex Use Ae
Infliximab adalimimab golimumab certolizumab Acute and chronic treatment of Uc and Cron's Infection lymphoma
115
Bile acid therapy for gall stones Moa Use
Ursodiol Expands bile acid pool Dec cholesterol content of bile bunreducing hepatic cholesterol secretion
116
Drugs used for upper Gi bleeding Ex Moa Use
Somatostatin/Octreotide Reduce portal bf and varice pressures Initial hemostasid from bleeding esophageal varices
117
Drugs used for upper Gi bleeding Ex Moa Use
Vasopressin ang terlipressin Causes splanchnic arterial vasoconstriction leading yo reduced splanchnic perfusion and loerred portal venous pressure Ae: MI HPN
118
Drugs used for upper Gi bleeding Ex Moa Use
Beta receptor blocking agents Reduce portal venous pressure via a decrease in portal venous pressure via a decrease ib portal venous inflow due to decrease in CO (B1 blovkade) and splanchnic vasoconstriction (B2 blockade) To reduce incidence of initial bleeding anf reduce rate of recurrent bleeding
119
DRA CLINICAL USES
``` GERD postsurgical and diabetic gastroparesis Prevention and treatment for vomiting NUD Promote postpartum lactation (domperidone) ```
120
DRA MOA
Also block D2 receptors in the chemoteceptor trigger zone of tbe medulla -> antinausea and antiemetic action
121
DRA MOA
Blocks the inhibitory effect of dopamine receptors-> increase esophageal peristaltic amplitude, increase LES pressure, enhance gastric emptying, no fx on si and colonic motility
122
Dopamine receptor antagonists
Domperidone | Metoclopromide
123
Cholinomimetic agents effects
Excessive salivation, nausea, vomiting diarrhea bradycardia

Pharmacology (2 decks)

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