GASTROINTESTINAL-Pharmacology Flashcards by Armando Monroy

H2 blockers

Cimetidine, ranitidine, famotidine, nizatidine

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Mechanism of action for H2 blockers

Reversible block of histamine H2 receptors → ↓ H+ secretion by parietal cells

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Clinical use for H2 blockers

Peptic ulcer, gastritis, mild esophageal reflux

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Toxic effects of Cimetidine

Potent inhibitor of cytochrome P-450 (multiple drug interactions); antiandrogenic effects; can cross blood brain barrier and placenta

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Which antiandrogenic efects does cimetidine has?

Prolactin release, gynecomastia, impotence, ↓ libido in males

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Which common toxic effect does cimetidine and ranitide have?

↓ renal excretion of creatinine

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Proton pump inhibitors

Omeprazole, lansoprazole, esomeprazole, pantoprazole, dexlansoprazole

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Proton pump inhibitors mechanism of action

Irreversibly inhibit H+/K+ ATPase in stomach in parietal cells

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Clinical use for proton pump inhibitors

Peptic ulcer, gastritis, esophageal refluxm Zollinger Ellison syndorme

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Toxic effects of Proton pump inhibitors

Increased risf of C. difficile infection, pneumonia. Hip fracture, ↓ serum Mg2+ with long term use

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Mechanism of action of Bismuth and sucralfate

Binds to ulcer base, providing physical protection and allowing HCO3- secretion to reestablish pH gradient in the mucous layer

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Clinical use for Bismuth and sucralfate

↑ ulcer healing, travelers’ diarrhea

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What family is Misoprostol?

A PGE1 analog

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Mechanism of action of Misoprostol

Increases production and secretion of gastric mucous barrier, ↓ acid production

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Clinical use for Misoprostol

Prevention of NSAID- induced peptic ulcers
Maintenance of a Patent Ductus arteriosus
Also used to induce labor (ripens cervix)

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How does misoprostol prevents NSAID- induced peptic ulcers?

NSAIDs block PGE1 production

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Secondary effects of Misoprostol

Diarrhea

Contraindicated in women of childbearing potential (abortifacent)

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How does Ocreotide works?

Long acting somatostatin analog

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Clinical use for Ocreotide

Acute variceal bleeds, acromegaly, VIPoma, and carcinoid tumors

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Toxic effecs Ocreotide

Nause, cramps, steatorrhea

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Antacid examples

Aluminum hydroxide
Calcium carbonate
Magnesium hydroxide

Side effects of Antacid use

Can affect absorption, bioavailability, or urinary excretion of other drugs
All can cause hypokalemia

How does antacids affect affect absorption, bioavailability, or urinary excretion of other drugs?

By altering gastric and urinary pH or by delaying gastric emptying

Toxic effects of Aluminum hydroxide

Constipation and hypophosphatemia: proximal weakness, osteodystrophy, seizures

Calcium carbonate side effects

Hypercalcemia, rebound acid increased

Which drugs are mainly affected by calcium carbonate?

Can chelate and ↓ effectiveness of other drugs (eg. tetracycline)

Side effects of Magnesium hydroxide?

Diarrhea, hyporeflexia, hypotension, cardiac arrest

Side effects of Magnesium hydroxide?

Diarrhea, hyporeflexia, hypotension, cardiac arrest

Osmotic laxatives

Magnesium hydroxide, magnesium citrate, polyethilene glycol, lactulose

Mechanism of action of Osmotic laxatives

Provide osmotic load to draw water out

Which other benefit does lactulose has?

Also treats hepatic encephalopathy

How does lactulose treat hepatic encephalopathy?

Since gut flora degrade it into metabolites (lactic acid and acetic acid) that promote nitrogen excretion as NH4+

Clinical use foe Osmotic laxative

Constipation

Toxic effects of Osmotic laxative

Diarrhea, dehydrarion; may be abused by bulimics

What is Infliximab?

Monoclonal antibody to TNF-α

Clinical use for Infliximab

Crohn disease, ulcerative colitis, rheumatoid arthritis, ankylosing spondylitis, psoriasis

Toxic effects caused by Infliximab

Infection (including reactivation of latent TB), fever, hypotension

How is Sulfazalasine composed?

Combination of sulfapyridine (antibacterial) and 5 aminoslicylic acid (anti- inflammatory)

What activates Sulfasalazine?

Colonic bacteria

Clinical use for Sulfasalazine

Ulcerative Colitis, Crohn disease

Secondary effects of Sulfasalazine

Malaise, nauseam sulfonamide toxicity, reversible oligospermia

Mechanism of action of Ondansetron

5 HT3 antagonist; ↓ vagal stimulation

How is Ondansetron consider?

Powerful central acting antiemetic

Clinical use for Ondansetron

Control vomiting postoperatively and in patients undergoing cencer chemotherapy

Side effects of Ondansetron

Headache, constipation

D2 receptor antagonist

Metoclopramide

Mechanism of action of Metoclopramide

↑ resting tone, contractility, LES tone, motility

Does Metoclopramide influence colon transport time?

Clinical use for Metoclopramide

Diabetic and post surgery gastroparesis, antiemetic

Toxic effects of Metoclopramide

↑ parkinsonian effects. | Restlessness, drowsiness, fatigue, depression, nauseam diarrhea

Which drugs interact with Metoclopramide?

Drug interaction with digoxin and diabetic agents

When is Metoclopramide contraindicated?

In patients with small bowel obstruction or Parkinson disease (D1 receptor blockade)