Redline Drugs Flashcards
Omeprazole
Antisecretory/Cytoprotective Agent
Proton Pump Inhibitor
Available OTC
Administered as prodrug, absorbed into circulation, then diffuses into parietal cells where it irreversible inactivates the enzyme
Once daily dosing (18 hours are required for new enzyme synthesis)
Ranitidine
Antisecretory/Cytoprotective Agent
H2 receptor antagonist
Reversible, competitive block at parietal cell H2 receptors on basolateral membrane. Less efficacious than PPIs.
Better at blocking nocturnal acid secretion rather than meal-stimulated acid
Used in GERD, PUD and stress-related gastritis
Cimetidine
Antisecretory/Cytoprotective Agent
H2 receptor antagonist
Reversible, competitive block at parietal cell H2 receptors on basolateral membrane. Less efficacious than PPIs.
Better at blocking nocturnal acid secretion rather than meal-stimulated acid
Used in GERD, PUD and stress-related gastritis
- *Inhibits cytochrome P450 oxidative metabolism**
- *Also headache, confusion, man-boobies and decreased libido in men**
CaCO3 (Tums)
Antisecretory/Cytoprotective Agent
Antacid (raises pH of stomach to 4-5)
Used as pain relief due to peptic ulcers and actute gastritis
- Can see rebound secretion due to Ca2+ effect on gastrin release
- Safe, but should not be used long-term
- Constipation can occur, sometimes hypercalcemia
Mg (OH)2
Antisecretory/Cytoprotective Agent
Antacid (raises pH of stomach to 4-5)
Used as pain relief due to peptic ulcers and actute gastritis
- Major side effect is osmotic diarrhea, often added to antacid preparations to counteract Al or Ca-induced constipation
- Avoid use if renal disease is present
Al (OH)3
Antisecretory/Cytoprotective Agent
Antacid (raises pH of stomach to 4-5)
Used as pain relief due to peptic ulcers and actute gastritis
- Very widely used, binds phosphate in gut
- Main side effect is constipation
- Chronic intake may lead to CNS toxicity
Metoclopramide
Antiemetic Agent, Prokinetic Agent
Dopamine receptor antagonist
Pro-motility; increase agonist activity at smooth muscle M3-receptors
Antagonist at presynaptic dopamine receptors that inhibit the release of ACh
Relieves n/v by block of dopamine receptors in chemorecptor trigger zone
oral-IV-IM
May cause somnolence, dystonic reaction, and tardive dyskinesia
Can be used in morning sickness, no significant increase in birth defects
Psyllium Seed (metamucil)
Laxative
Bulk-forming/fiber
Safe to use every day
Effective in 12-24 hours to 3 days, always need to take with 8oz of fluids
Polyethylene glycol
Laxative
Saline (osmotically-active) cathartic
High-volume: Widely used for bowel cleansing prior to radiologic, surgical, or endoscopic procedures
Smaller-volume: Now used to treat difficult constipation.
Prolonged use can lead to electrolyte depletion
Bisacodyl
Laxative
Stimulant/irritant
Try if fiber/saline treatments fail
Acts via increase in peristaltic activity by inducing low-grade inflammation in bowel to promote accumulation of water and electrolytes and stimulation of intestinal motility (activation of prostaglandin-cAMP and NO-cGMP pathways)
Potentially dangerous side effects of electrolyte/fluid deficiencies or severe cramping. Most widely abused class
Docusate
Laxative
Wetting agents, Surfactant
Acts as stool softener. Role is primarily prevention.
Used in pts with cardiovascular disease/hernia/postpartum pts. Often used in combo with stimulant laxatives with initiating opioid therapy
Mineral oil
Laxative
Wetting agent
Coats fecal contents preventing colonic absorption of fecal water. used with caution in very young/elderly due to potential aspiration into lungs
Loperamide (Imodium)
Antidiarrheals
Opioid
Effective against travelers diarrhea, alone or in combination with antimicrobrial agents. Should be discontinued if no improvement after 48 hours.
Los addiction liability. Can cause CNS depression in overdose. May worsen Shigella infections
Anti-secretory activity against cholera toxin
Polycarbophil
Antidiarrheal
Opioid
Useful in diarrhea by absorbing 60x weight in H20
Useful in constipation by preventing fecal desiccation
Bismuth subsalicylate
Antidiarrheal
Absorbent agent
Absorbs “toxins” that cause irritation. Can also absorb drugs, nutrients, digestive enzymes.
*Avoid use in children under 12 due to risk of Reye’s syndrome