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GI Pharmacology

TermDefinition
Antacids to neutralize HCl in stomach. To decrease pepsin, can decrease absorption of other drugs
Al(OH)3 also causes constipation, SM – relaxation
Mg(OH)2 also cause diarrhea-osmotic.
CaCO3 also acts as a Ca supplement.
Sucralfate forms a protective barrier on the surface of ulcer. Side effect: constipation
Bismuth salts (Petpo-Bismol) coats ulcer, also bacteriostatic, also stimulates prostaglandin release. Side Effects: darkens tongue and stools.
Misoprostol (Cyclotec) PGE1 analog. Blocks pro-secretory effects of histamine. Increases HCO3-, mucus, blood flow. Side effects: diarrhea, cramping, *uterine contractions. **Also used off label for cervical ripening and labour induction.
Mucoprotectors Sucralfate, bismuth salts, misoprostol
Cimetidine ranitidine Famotidine achieve 70% acid suppression, exception safety record. Competitive inhibition of H2 receptor. 50% bioavailbility, GIT absorpation, 24 hour duration.
Cimetidine SIDE FX and USE anti-androgenic = gyno, low sperm count, affects CYP enzymes. Use: acid peptic disease, Zollinger –Ellison syndrome, GERD, erosive esophagitis.
Histamine- 2 Receptor Antagonists Cimetidine ranitidine Famotidine
Domperidone, metoclopramide doapminergic antagonists, increase low esophageal tone, stomach contractions, etc..
Metoclopramide SIDE FX and USE increased Ach activity in nigrostriatal pathway. Parkinson-like effects. USE: Anti-emetics, off label use: increase milk production in breast feeding moms.
Prokinetic Agents Domperidone, metoclopramide
Omeprazole (and esomeprazole) Lanzoprazole, pantoprazole, rabeprazole Accumulate in parietal cells, activation of PPI by protonation. Irreversible binding and inactivation of the H+/K+ ATPase. Side effects: diarrhea, headaches
Proton Pump Inhibitors Omeprazole (and esomeprazole) Lanzoprazole, pantoprazole, rabeprazole
Pirenzepine, atropine muscarinic Ach antagonist.
Methylnaltrexone opiod antagonist for constipation due to narcotics.
Docusate detergent like effect (Emollient) softens stool allows water penetration.
Scopolamine Muscarinic Antagonist
Lorazepam GABA antagonist
Loperamide Treats diarrhea from gastroentitis or IBD. Mu opiod receptor agonist.
Others Pirenzepine, atropine, Methylnaltrexone, Docusate, Scopolamine, Lorazepam, Loperamide
Created by: vbukorovic
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