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SPEARS GI EXAM 1
| CLASS | DRUGS | MOA | ADRS | NOTES |
|---|---|---|---|---|
| Two major causes of PUD | Helicobacter (H.) pylori-induced and NSAID-induced | |||
| H2-histamine receptor blockers (PUD/GERD) | cimetidine, famotidine, nizaridine, ranitidine | Selective, reversible competitive inhibitors at parietal cells, cAMP dependent | CNS-hallucinations cimetidine: Endocrine/metabolic: decreases libido, impotence, gynecomastia, galactorrhea, breast soreness | decrease basal and meal acid secrection |
| Proton pump inhibitors (PUD/GERD) | Dexlansoprazole (dexilant), Esomeprazole (nexium), Lansoprazole (prevacid), Omeprazole (prilosec), Pantoprazole (prontonix), Rabeprazole (aciphex) | Block (ATP pump) H/K ATPase at parietal cells | generally safe, common harmless ADRs, can cause B12 def, reduced mineral absorption and increased bone fracture risk | more effective than histamine blockers, take on empty stomach, irreversibly inactivates pump |
| Antacids (PUD/GERD) | Calcium carbonate (tums), sodium bicarbonate, aluminum, hydrozide | Weak bases that neutralize (H), results in higher pH (less acid) | endocrine/metabolic, and GI effects (Mg diarrhea),(Al/Ca constipation) | low dose antacids - high dose laxative |
| Potassium-competitive acid blocker (PUD/GERD) | Vonoprazan (voquenza) | K competitive acid blocker (P-CAB) - reversibly competes with K to bind to H/K ATPase | Fracture risk | |
| Coating agents (PUD/GERD) | Bismuth subsalicylate (pepto-bismol), bismuth subcitrate potassium | inhibits growth of H. pylori AND salts combine with mucus glycoproteins forming a layer that coats erosions/ulcers | avoid in renal insufficiency, may cause constipation, salicylate toxicity (Reye's syndrome) with prolonged use/high dose - avoid in pediatric and pregnant patients | |
| Coating agent (PUD/GERD) | sucralfate (carafate) | sucrose sulfate + Al (OH)3, physical barrier at ulcer/erosion site to restrict damage, binds positively charged proteins of epithelial cells | ||
| Prokinetic agents (GERD) | Metoclopramide (reglan) | Dopamine 2 receptor antagonist, works to reduce reflux of gastirc contents and increase emptying rate Prokinetic action (peripherally acting): increase emptying rate Atcs centrally to prevent nausea at dopamine receptor at high doses | BW: tardive dyskinesia (facials ticks) CNS restlessness, drowsiness, insomnia, anxiety, depression, parkinson-like syndromes | |
| Dopamine 2 receptor antagonists | Amisulpride Metoclopramide (at higher doses) Antipsychotics (prochlorperazine, droperidol, haloperidol, olanzapine) | all work to block D2 receptor in chemoreceptor trigger zone (CTZ) | sedations | used for chemo induced vomiting and postoperative nausea and vomiting (PONV) |
| 5HT3 receptor antagonists | Ondansetron, granisetron, dolasetron, palonosetron | Blocks 5HT3 in peripheral system (intestinal nerves) and targets CTZ | serotonin syndrome with SS/SNRIS, QT prolongation | used for chemo induced vomiting and postoperative nausea and vomiting (PONV) |
| Neurokinin NK1 receptor antagonists | Aprepitant, rolapitant, netupitat and palonosetron | cross BBB, block NK1 | fatigue, dizziness, diarrhea, combined with steroids or 5HT3's | prevent acute and delayed emesis from chemotherapy or surgery |
| Corticosteroids | Dexamethasone, methylprednisone | larger dose usually required for antemetic effect, unknown MOA enhances efficacy of 5HT3's | PONV/CINV | |
| Antihistamines | Cyclizine * Diphenhydramine* Dimenhydrinate* Hydroxyzine Meclizine* Promethazine* Scopolamine (Hyoscine)* Doxylamine | competitive, reversible H1 antagonism | dizziness, sedation, confusion | motion sickness, nausea with pregnancy weak CYP2D6 inhibitor |
| Cannabinoid receptor agonists | Dronabinol (CB1 and Cb2 receptor) Nabilone (synthetic delta 9) (CB1 receptor agonist) Marijuana | Agonists at CB1 or CB2, antiemetic effects via 5HT1a mechanism | cannabinoid induced hyperemesis syndrome (get nausea when you smoke) | for chemo-induced nausea/vomiting, interacts with CNS depressants CB1 receptors are located in the CNS |