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GI Disorders

Med Chem

DrugClinically relevant PK/PDADMETInactivationPharmacophoreStimuliMoeityAnalogs
Omeprazole OBA decreases with food; take ≥30 min before meals Metabolism: CYP2C19, CYP3A4; counsel calcium if long-term use. enteric-coated to avoid pre-systemic acid inactivation 2-pyridylmethylsulfinylbenzimidazole Acid secretion is stimulated by gastrin, acetylcholine, histamine (context for target). Substituted benzimidazole resemble imidazoles that bind CYP heme iron R enantiomer has greater AUC
Esomeprazole OBA decreases with food; take ≥30 min before meals Metabolism: CYP2C19, CYP3A4; counsel calcium if long-term use. enteric-coated to avoid pre-systemic acid inactivation 2-pyridylmethylsulfinylbenzimidazole Acid secretion is stimulated by gastrin, acetylcholine, histamine (context for target). Substituted benzimidazole resemble imidazoles that bind CYP heme iron S (-) enantiomer
Lansoprazole OBA decreases with food; take ≥30 min before meals Metabolism: CYP2C19, CYP3A4; counsel calcium if long-term use. enteric-coated to avoid pre-systemic acid inactivation 2-pyridylmethylsulfinylbenzimidazole Acid secretion is stimulated by gastrin, acetylcholine, histamine (context for target). Substituted benzimidazole resemble imidazoles that bind CYP heme iron Class analogs listed together
Dexlansoprazole OBA decreases with food; take ≥30 min before meals Metabolism: CYP2C19, CYP3A4; counsel calcium if long-term use. enteric-coated to avoid pre-systemic acid inactivation 2-pyridylmethylsulfinylbenzimidazole Acid secretion is stimulated by gastrin, acetylcholine, histamine (context for target). Substituted benzimidazole resemble imidazoles that bind CYP heme iron R (+) enantiomer, greater AUC
Pantoprazole OBA decreases with food; take ≥30 min before meals Metabolism: CYP2C19, CYP3A4; counsel calcium if long-term use. enteric-coated to avoid pre-systemic acid inactivation 2-pyridylmethylsulfinylbenzimidazole Acid secretion is stimulated by gastrin, acetylcholine, histamine (context for target). Substituted benzimidazole resemble imidazoles that bind CYP heme iron Class analogs listed together
Rabeprazole OBA decreases with food; take ≥30 min before meals Metabolism: CYP2C19, CYP3A4; counsel calcium if long-term use. enteric-coated to avoid pre-systemic acid inactivation 2-pyridylmethylsulfinylbenzimidazole Acid secretion is stimulated by gastrin, acetylcholine, histamine (context for target). Substituted benzimidazole resemble imidazoles that bind CYP heme iron Class analogs listed together
Vonoprazan dose-dependent ionic binding to H+ Acid secretion is stimulated by gastrin, acetylcholine, histamine
Cimetidine Oral BA ~50%; mainly excreted renal+hepatic Minimal metabolic transformation; largely unchanged with minor inactive metabolites; renal+hepatic excretion. Substituted aromatic ring separated from a polar, non-ionizable group by an ethylthiomethyl chain Histamine is the stimulus for H2-mediated acid secretion Imidazole ring
Famotidine Oral BA ~50%; mainly excreted renal+hepatic Substituted aromatic ring separated from a polar, non-ionizable group by an ethylthiomethyl chain Histamine is the stimulus for H2-mediated acid secretion Imidazole ring
Ranitidine NDMA impurity concerns; NDMA is hepatotoxic/carcinogenic; withdrawal in April 2020; later references to reformulation in lecture. Substituted aromatic ring separated from a polar, non-ionizable group by an ethylthiomethyl chain Histamine is the stimulus for H2-mediated acid secretion Imidazole ring
Misoprostol Orally active; inhibits acid secretion; stimulates mucus and bicarbonate. Rapid metabolic inactivation avoided by structural changes at C-16; Abortifacient warning. mimics PGE, PGI2 Prostaglandins act as inhibitors of acid secretion
Sucralfate Reacts with gastric HCl to form viscous, paste-like barrier; binds albumin/fibrinogen on ulcers; prevents back-diffusion of H+; adsorbs pepsin and bile acids. Aluminum salt of sulfated sucrose
Bismuth subsalicylate Rapid dissociation in stomach; salicylate absorbed bismuth eliminated in feces Bismuth salt
Aluminum hydroxide OH- neutralizes gastric H+; Al3+ contributes to protective coating Often combined with Mg(OH)2 (Maalox®, Gelusil®, Mylanta®)
Magnesium hydroxide OH- neutralizes gastric H+; Mg2+ contributes to protective coating Often combined with Al(OH)3
Calcium carbonate carbonate may stimulate gastrin → possible acid rebound
Sodium bicarbonate
Metoclopramide dopamine
Palonosetron Less effect on QTc; longer half-life (40 hrs), effective for delayed CINV IV; long duration Serotonin (enterochromaffin cells) Ondansetron, granisetron, dolasetron
Aprepitant t1/2 ~9 h; requires redosing on subsequent days for highly emetogenic chemo Oral; CNS penetration Morpholine-containing (class) Substance P Fosaprepitant (IV prodrug)
Rolapitant Very long t1/2 ~7 days → dose once per cycle Oral; IV formulation withdrawn in US due to anaphylaxis risk — Substance P Aprepitant
Netupitant Moderate CYP3A4 inhibitor; used with palonosetron Oral (combo Akynzeo) — Substance P Fosnetupitant (IV prodrug)
Droperidol Rapid onset; short procedures; strong antiemetic potency Requires EKG monitoring Butyrophenone core Dopamine Haloperidol
Olanzapine Sedation prominent first days; useful for breakthrough NV Oral; crosses BBB Thienobenzodiazepine Dopamine/serotonin mediated —
Created by: CaristW
 

 



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