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G.I. Drugs Flashcards

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1
Q

Esomeprazole

A

Proton Pump Inhibitor

Covalently modify the active site of H/K ATPase (IRREVERSIBLE)

Relies on slow turnover of ATPase at apical surface

First line treatment for hyperacidity (80-95% reduction)

Prodrug that requires acid activation to react with proton pump

Acid Labile

Must be absorbed into the blood and can only do so at higher pH so must be administered as:
- Gelatin Capsule

Lowers acid secretions by 90%

  • Used for GERD
  • Used for erosive esophagitis
  • Used for peptic ulcers
  • Zollinger- Ellison syndrome (secretion of gastrin from tumors in pancreas and intestine)
  • NSAID induced gastric ulcers
  • H. pylori treatment

NOT ALL Proton Pumps active at one time, so treatment requires 2-5 DAYS

Clearance through liver

Adverse Reaction

  • Hepatic Failure reduces clearance
  • Nausea, Abd pain, constipation, flatulence, diarrhea
  • Rare: Myopathy arthralgia, headache, skin rashes
  • Drug interactions through CYP activity
    • Increase serum warfarin concentration
    • Decrease activation of clopidogrel

Rebound hypergastrinemia and gastritis can occur (excessive gastrin secretion)

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2
Q

lansoprazole

A

Proton Pump Inhibitor

Covalently modify the active site of H/K ATPase (IRREVERSIBLE)

Relies on slow turnover of ATPase at apical surface

First line treatment for hyperacidity (80-95% reduction)

Prodrug that requires acid activation to react with proton pump

Acid Labile

Must be absorbed into the blood and can only do so at higher pH so must be administered as:
- Gelatin Capsule

Lowers acid secretions by 90%

  • Used for GERD
  • Used for erosive esophagitis
  • Used for peptic ulcers
  • Zollinger- Ellison syndrome (secretion of gastrin from tumors in pancreas and intestine)
  • NSAID induced gastric ulcers
  • H. pylori treatment

NOT ALL Proton Pumps active at one time, so treatment requires 2-5 DAYS

Clearance through liver

Adverse Reaction

  • Hepatic Failure reduces clearance
  • Nausea, Abd pain, constipation, flatulence, diarrhea
  • Rare: Myopathy arthralgia, headache, skin rashes
  • Drug interactions through CYP activity
    • Increase serum warfarin concentration
    • Decrease activation of clopidogrel

Rebound hypergastrinemia and gastritis can occur (excessive gastrin secretion)

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3
Q

Omeprazole

A

Proton Pump Inhibitor

Covalently modify the active site of H/K ATPase (IRREVERSIBLE)

Relies on slow turnover of ATPase at apical surface

First line treatment for hyperacidity (80-95% reduction)

Prodrug that requires acid activation to react with proton pump

Acid Labile

Must be absorbed into the blood and can only do so at higher pH so must be administered as:

  • Gelatin Capsule
  • Enteric coated capsule
  • Mixed with bicarbonate

Lowers acid secretions by 90%

  • Used for GERD
  • Used for erosive esophagitis
  • Used for peptic ulcers
  • Zollinger- Ellison syndrome (secretion of gastrin from tumors in pancreas and intestine)
  • NSAID induced gastric ulcers
  • H. pylori treatment

NOT ALL Proton Pumps active at one time, so treatment requires 2-5 DAYS

Clearance through liver

Adverse Reaction

  • Hepatic Failure reduces clearance
  • Nausea, Abd pain, constipation, flatulence, diarrhea
  • Rare: Myopathy arthralgia, headache, skin rashes
  • Drug interactions through CYP activity
    • Increase serum warfarin concentration
    • Decrease activation of clopidogrel

Rebound hypergastrinemia and gastritis can occur (excessive gastrin secretion)

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4
Q

cimetidine

A

H2 Receptor Antagonist

4-5hr duration

Adverse Reaction:

  • <3% incidence of effect overall
  • Minor effect: diarrhea, headache, drowsiness, fatigue, muscle pain
  • Parenteral administration in the elderly (hallucinations, delirium, confusion, slurred speech, and headaches)

Long term effect decrease testosterone binding to androgen receptor and hydroxylation

Decrease pepsin and intrinsic factor output

Tolerance can develop in 3 days

Rebound is a problem if discontinued suddenly

Block base level of acid secretion from ECL cells

Useful for nocturnal acid secretion, important for duodenal ulcers (4-8wk)

Use for Zollinger-Ellison syndrome (excessive gastrin secretion)

Not as effective as proton pump inhibitor but decreases acid secretion by 70% for 24 hours with daily dosing

Excretion is renal via organic cation system

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5
Q

famotidine

A

H2 Receptor Antagonist

10-12hr duration

Adverse Reaction:

  • <3% incidence of effect overall
  • Minor effect: diarrhea, headache, drowsiness, fatigue, muscle pain
  • Parenteral administration in the elderly (hallucinations, delirium, confusion, slurred speech, and headaches)

Long term effect decrease testosterone binding to androgen receptor and hydroxylation

Decrease pepsin and intrinsic factor output

Tolerance can develop in 3 days

Rebound is a problem if discontinued suddenly

Block base level of acid secretion from ECL cells

Useful for nocturnal acid secretion, important for duodenal ulcers (4-8wk)

Use for Zollinger-Ellison syndrome (excessive gastrin secretion)

Not as effective as proton pump inhibitor but decreases acid secretion by 70% for 24 hours with daily dosing

Excretion is renal via organic cation system

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6
Q

ranitidine

A

H2 Receptor Antagonist

6-8hr duration

Adverse Reaction:

  • <3% incidence of effect overall
  • Minor effect: diarrhea, headache, drowsiness, fatigue, muscle pain
  • Parenteral administration in the elderly (hallucinations, delirium, confusion, slurred speech, and headaches)

Long term effect decrease testosterone binding to androgen receptor and hydroxylation

Decrease pepsin and intrinsic factor output

Tolerance can develop in 3 days

Rebound is a problem if discontinued suddenly

Block base level of acid secretion from ECL cells

Useful for nocturnal acid secretion, important for duodenal ulcers (4-8wk)

Use for Zollinger-Ellison syndrome (excessive gastrin secretion)

Not as effective as proton pump inhibitor but decreases acid secretion by 70% for 24 hours with daily dosing

Excretion is renal via organic cation system

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7
Q

sucralfate

A

Misc. Drug

Octasulfate of sucrose with Al(OH)3

Forms sticky neutral pH polymer coating that swells and covers the epithelium

Used for STRESS ULCERS (sticks better to duodenal)

Acid activated, take before food and avoid antacids/PPIs

Common Side Effect is constipation (2%)

Block absorption of other drugs through the stomach

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8
Q

aluminum hydroxide

A

Neutralizing Antacids

Neutralizes pH of gastric contents

Largely supplanted by proton pump inhibitors

Used over the counter

Al is slower than Mg

Adverse effect:

  • Rebound acid secretion
  • AlOH- Constipation, nausea, possible phosphate loss, binds tetracyclines

Use in combo for H. Pylori Treatment

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9
Q

calcium carbonate

A

Neutralizing Antacids

Neutralize pH of gastric contents

Largely supplanted by PPIs

Widely used over the counter

Largely supplanted by proton pump inhibitors

Used over the counter

Adverse effect:
- Rebound acid secretion

Use in combo for H. Pylori Treatment

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10
Q

magnesium hydroxide

A

Antacids

Neutralize pH of gastric contents

Fast Acting

Stimulates gastric emptying and motility while

Largely supplanted by PPIs

Widely used over the counter

Largely supplanted by proton pump inhibitors

Used over the counter

Adverse effect:
- Rebound acid secretion

Use in combo for H. Pylori Treatment

ALSO A LAXATIVE

  • Mg stimulates CCK receptors and increases motility
  • Avoid in individuals with
  • Cardiac Disease
  • Renal Insufficiency
  • Diuretic Use
  • Electrolyte abnormalities
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11
Q

magnesium trisilicate

A

Antacids

Neutralize pH of gastric contents

Fast Acting

Stimulates gastric emptying and motility while

Largely supplanted by PPIs

Widely used over the counter

Largely supplanted by proton pump inhibitors

Used over the counter

Adverse effect:
- Rebound acid secretion

Use in combo for H. Pylori Treatment

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12
Q

misoprostol

A

Prostaglandin Analogs

Synthetic analogue of PGE1

Reduce 80-90% of basal or food-induced acid production

Short acting, up to 3 hr

Used to prevent NSAID-induced injury (but PPIs and H2-antagonists more commonly used for this purpose)

Adverse Effect:

  • Diarrhea (30%)
  • Exacerbate inflammatory bowel disease
  • Increase Uterine Contractions during Pregnancy
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13
Q

pirenzepine

A

Muscarinic Antagonist

Selective for M1 receptor

Blocks neurotransmission in Intramural Ganglia resulting in less stimulation of parietal cells and ECL cells

Reduce basal acid (40-50%)

Significant anticholinergic side effects

Rarely Used

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14
Q

bethanechol

A

Prokinetic Agent

Activating M receptors do not activate coordinated motility

Selectively activate M2 and M3 receptors

Side Effects:

  • Bradycardia
  • Flushing
  • Diarrhea
  • Cramps
  • Salivation
  • Blurred vision
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15
Q

cisapride

A

Prokinetic Agent

5-HT4 receptor agonist and adenylate cyclase stimulant

Used for GERD

Stimulate intrinsic sensory neurons

Adverse reaction:
- Fatal Cardiac arrythmia

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16
Q

erythromycin

A

Imitates Motilin

Increases motility

Macrolide Antibiotic

Cause gastric dumping, moves bezoars and improves gastric emptying with ILEUS, SCLERODERMA, and PSEUDOOBSTRUCTIONS

Fast dumps can be painful so not recommended for chronic use

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17
Q

metoclopramide

A

Prokinetic Agent

Dopamine receptor antagonist
- DA decreases ACh release so drugs enhance normal ACh response

Long used, increases lower esophageal sphincter tone and upper GI motility

Relieves GERD symptoms but does not promote healing

Used for nausea and vomiting in dysmotility syndromes

Used as AntiEMETIC also
- PREFERRED AGENT IN CHEMOTHERAPY INDUCED NAUSEA

Also a laxative

Adverse effect:
- Extrapyramidal side effects, dystonias, Parkinson’s like symptoms, Tardive dyskenesia with chronic use

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18
Q

neostigmine

A

Prokinetic Agent

AChE inhibitor (not insecticide)
- Commonly used to counter ILEUS
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19
Q

Tegaserod

A

Prokinetic Agent

Partial 5-HT agonist in gut for FEMALES with Irritable bowel syndrome

Can improve lower bowel motility in cases with chronic constipation and bloating

Adverse Reaction:
- Fatal Cardiac Arrhythmias

USED FOR CONSTIPATION PREDOMINANT IBS

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20
Q

magnesium citrate

A

Laxative

Osmotic Laxative

  • Non absorbable agent
  • Cause water retention

Techically a cathartic causing bowel emptying with watery stool, but act as laxative at lower dosages

Mg Stimulates CCK receptors and Increases motility

Avoid in individuals with renal insufficiency
Cardiac Disease
Electrolyte abnormalities
Diuretic Use

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21
Q

magnesium sulfate

A

Laxative

Osmotic Laxative

  • Non absorbable agent
  • Cause water retention

Techically a cathartic causing bowel emptying with watery stool, but act as laxative at lower dosages

Mg Stimulates CCK receptors and Increases motility

Avoid in individuals with renal insufficiency
Cardiac Disease
Electrolyte abnormalities
Diuretic Use

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22
Q

polyethylene glycol

A

Laxative

Osmotic Laxative

Non-absorbable agent

Cause water retention

Cathartics that cause bowel emptying with watery stool, but act as laxatives at lower dosages

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23
Q

lactulose

A

Laxative

Osmotic Laxative

Sugar

Used for constipation associated with opioid use and vincristine

Bacterial fermentation of lactulose also drops luminal pH and traps NH4 (increased in colons of patients suffering from hepatic disease)

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24
Q

mannitol

A

Osmotic Laxative

Sugar

Used for constipation associated with opioid use and vincristine

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25
sorbitol
Osmotic Laxative Sugar Used for constipation associated with opioid use and vincristine
26
docusate
Stool wetting agent Surfactants that allow mixing of fatty substances and water in stool. Effective as stool softeners Do not increase frequency of defecation
27
bisacodyl
Irritant laxative Used orally or rectally Generally safe but overdose causes catharsis Warn patients not to chew tablets or mix with milk or antacids to ensure that the tablet reaches the site of action in the small intestine and avoid gastric irritation
28
castor oil
Irritant laxative Smooth muscle stimulant Used as cathartic - laxative - induce labor - Purge - Neolid Made from castor bean 4 ml will produce laxative effect in 4 hours 16 ml for cathartic effect
29
glycerin
Irritant glycerin Suppository that acts as hydroscopic agent and lubricant Increased water retention Stimulates peristalsis and produces an evacuation reflex Rectal admin can produce a bowel movement in a hour
30
methylcellulose
Bulk-forming laxative Fiber based Great for regular soft stools May exacerbate intestinal obstructions May absorb other drugs
31
polycarbophil
ulk-forming laxative Fiber based Great for regular soft stools May exacerbate intestinal obstructions May absorb other drugs
32
Psyllium
ulk-forming laxative Fiber based Great for regular soft stools May exacerbate intestinal obstructions May absorb other drugs
33
bismuth subsalicylate
Antidiarrheal Also used in H. pylori treatment Suspended in magnesium aluminum silicate and oil of wintergreen Naturally pink Salicylate is released in stomach and absorbed systemically
34
diphenoxylate
Antidiarrheal Opioid Piperidine derivative Can have CNS effects Packaged with atropine to discourage abuse
35
loperamide
Antidiarrheal Opioid mu opioid receptor agonist that stops bowel motility 40-50X more potent than morphine Does not enter CNS
36
octreotide
Antidiarrheal Agent Same as Somatostatin Parenteral octapeptide Used to combat secretory diarrhea of hormone secreting tumors Used for post-surgical gastric dumping syndrome Diarrhea associated with chemotherapy Used to rest the pancreas in pancreatitis Adverse reactions: - Nausea - Bloating - injection site pain Long term therapy may result in gallstones
37
chlorpromazine
Antiemetic Agent Dopamine Receptor Antagonist Phenothiazines Originally used as antipsychotics Preferred use is anti-nauseants and anti-emetic Mechanism targets D2 receptors in CTZ and H1 receptors Good for motion sickness Can be useful in chemotherapy induced nausea
38
cyclizine
Antiemetic Antihistamine Also has anticholinergic effects used in patients with abdominal cancer H1 receptor antagonist Used for post-operative emesis Act primarily on brainstem and vestibular apparatus
39
diphenhydramine
Antiemetic Antihistamine Also has anticholinergic effects used in patients with abdominal cancer H1 receptor antagonist Used for post-operative emesis Act primarily on brainstem and vestibular apparatus
40
dimenhydrinate
Antiemetic Antihistamine Dosed from of diphenhydramine Also has anticholinergic effects used in patients with abdominal cancer H1 receptor antagonist Used for post-operative emesis Act primarily on brainstem and vestibular apparatus
41
dolasetron
Antiemetic 5-HT3 antagonist Used in chemotherapy and antiemesis Oral or parenteral Excretion through liver
42
hydroxyzine
Antiemetic Antihistamine Also has anticholinergic effects used in patients with abdominal cancer H1 receptor antagonist Used for post-operative emesis Act primarily on brainstem and vestibular apparatus
43
granisetron
Antiemetic agent
44
metoclopramide
Prokinetic agent Also a Antiemetic agent and Laxative Dopamine receptor antagonist Increases forward motility Stops emesis, promotes defecation Preferred agent for chemotherapy induced nausea
45
ondansetron
Antiemetic 5HT3 antagonis 5HT3 promotes gut motility Act centrally at the CTZ and the STN Act peripherally in small intestine Most widely used for chemotherapy induced emesis and nausea 3.9 hours
46
palonosetron
Antiemetic Given parenterally only 5HT3 antagonis 5HT3 promotes gut motility Act centrally at the CTZ and the STN Act peripherally in small intestine Most widely used for chemotherapy induced emesis and nausea Excretion via kidney 40 hours
47
prochlorperazine
Antiemetic Agent Dopamine Receptor Antagonist Phenothiazines Originally used as antipsychotics Preferred use is anti-nauseants and anti-emetic Mechanism targets D2 receptors in CTZ and H1 receptors Good for motion sickness Can be useful in chemotherapy induced nausea
48
promethazine
Antiemetic Antihistamine Also has anticholinergic effects used in patients with abdominal cancer H1 receptor antagonist Used for post-operative emesis Act primarily on brainstem and vestibular apparatus
49
scopolamine
Antiemetic Anticholinergic Muscarinc ACh receptor antagonist Used parenterally but most commonly used as trans-dermal patch Effective for short or long-term prevention of motion sickness Used for post-operative emesis Acts on vestibular apparatus Not effective for chemotherapy induced nausea, minimal CTZ effects Adverse effects: - Blurred Vision - Outburst of uncontrolled behavior when used in presence of pain or anxiety
50
apomorphine
Emetic Acts on CTZ Given Sub-Q Largely superceded by activated charcoal
51
ipecac
Emetic Acts on CTZ Given Sub-Q Largely superceded by activated charcoal
52
6-mercaptopurine
Irritable bowel disease therapy Thiopurine Derivative of chemotherapy Prodrug Converted to 6-thioguanine to inhibit DNA synthesis Rapidly proliferating immune cells targetd Used to maintain remission in both UC and Crohns disease May help treat fistulas Effective in 66% of patients but may require weeks/months Adverse reactions: - Pancreatitis - Fever - Rash - Arthralgia - N/V are common
53
adalimumab
IBD immune modulation Fully human antibody used to maintain remission May gain use in acute UC must be given parenterally Used for both Crohn's and UC Adverse effects: - Increased respiratory infections - Lack of effective response to TB
54
alosetron
IBS treatment Used for diarrheal predominant IBS Focuses on motility of gut
55
azathioprine
IBD treatment Thiopurine Protypical drug Converted to 6-mercaptopurine which is converted to 6-thioguanine Inhibits DNA synthesis Rapidly proliferating immune cells targeted Maintain remission in UC and Crohn's disease May help treat fistulas in Crohns disease Effective in 66% of patients but may require weeks/months for clinical response Adverse effects: - Pancreatitis - Fever - Rash - Arthralgias Nausea and vomiting are common Bone marrow suppression
56
budesonide
IBD treatment Glucocorticoids Target immune and inflammatory response Indicated for acute exacerbations and severe disease 200 more potent that hydrocortisone but is only 10% bioavailable and most of that is removed in hepatic first pass Topical treatment inside the bowel (enema) Adverse reaction: - Immunosuppresion - Endocrine disruption - Steroid psychoses - Other effects typical of steroid treatments
57
infliximab
IBD treatment Anti-TNF antibody Humanized mouse antibody to TNF-a, interferes with inflammatory response Used in maintaining remission May gaine use in UC. Must be used parenterally Used for both Crohn's and UC Adverse effect: - Increased respiratory infections - Lack of effective response to TB
58
mesalamine
IBD treatment 5-ASA based therapy 5-aminosilicyclic acid DO not act through COX inhibition Act though inhibition of TNF-a Delivered as pro-drug or as enteric coated tablet Delayed release in the jejunum UC: treatment for acute flare-ups Crohns: useful for flare-ups, must select dosage to target part of colon involved
59
olsalazine
IBD treatment 5-ASA based therapy 5-aminosilicyclic acid DO not act through COX inhibition Act though inhibition of TNF-a Delivered as pro-drug or as enteric coated tablet Activated in the colon UC: treatment for acute flare-ups Crohns: useful for flare-ups, must select dosage to target part of colon involved
60
prednisone
IBD glucocorticoid Oral is prototype Target immune and inflammatory response Indicated for acute exacerbations and severe disease
61
sulfasalazine
IBD treatment 5-ASA based therapy 5-aminosilicyclic acid DO not act through COX inhibition Act though inhibition of TNF-a Delivered as pro-drug or as enteric coated tablet Activated in the colon UC: treatment for acute flare-ups Crohns: useful for flare-ups, must select dosage to target part of colon involved Has most side effect due to sulfa group ``` Headache Nausea Fatigue Allergic reactions Contraindicated in pregnancy ```

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