WITH SOLUTIONS GRADED A+
✔✔Describe antisecretory agents. - ✔✔Histamine 2-Antagonists & Proton Pump
Inhibitors
H2RA - ranitidine, cimetidine, famotidine, nizatidine
THINK: histamINE = drugs end in -dINE
PPI - omeprazole, esomeprazole, lansoprazole, pantoprazole, rabeprazole
THINK: prOton pump inhibitors = end in -zOle
✔✔List indications for H2RAs. - ✔✔duodenal ulcer treatment and maintenance
gastric ulcer treatment
GERD
pathologic hypersecretory conditions
✔✔List indications for PPIs. - ✔✔gastric and duodenal ulcers
GERD
pathologic hypersecretory conditions
H. pylori
✔✔Describe H2RAs. - ✔✔MOA: acts selectively on H2Rs in stomach, blood vessels,
and other sites; blocks binding of histamine (less effective than PPIs for stimulated
secretion)
Clinical Use: inhibit gastric acid secretion, better for basal secretion (at night and when
fasting)
Dosing: early evening is optimal time
ADEs: very safe; <3% of pts will have diarrhea, HA, fatigue, myalgias, and constipation
do NOT use for NSAID-induced ulcers or active ulcers (use PPIs instead)
Interactions: may interfere with drugs that require acidic medium for absorption (e.g.
ketoconazole, iron)
,✔✔Describe some precautions to consider when using cimetidine. - ✔✔inhibits CYP450
system and can slow metabolism of other drugs (warfarin, diazepam, phenytoin,
quinidine, carbamazepine, theophylline and imipramine)
can have endocrine effects - antiandrogen (gynecomastia, galactorrhea, reduced sperm
count)
✔✔Describe PPIs: - ✔✔MOA: inhibits the H+/K+-ATPase proton pump, suppresses
secretion of hydrogen ions into the gastric lumen and thus gastric acid secretion
all PPIs are enteric coated "pro-drugs" and need to be converted into the active form
once in the alkaline duodenum
Clinical Use: inhibits both basal and stimulated gastric acid secretion; used to treat
GERD, PUD, H. pylori ulcers (w/ ABX), NSAID ulcers, stress ulcer prophylaxis, erosive
esophagitis, gastrinoma, non-ulcer dyspepsia, and other hypersecretory conditions
Dosing: should be taken 30 min before largest meal, typically works within 1-2 hours of
first dose, powder form (Zegrid - omeprazole + NaHCO3) for faster absorption is
available, H2RAs should be taken well after PPI
ADEs: generally well tolerated; commonly causes diarrhea, HA, abd pain in 1-5% of pts;
FDA mantated warning about increased risk of fx with osteoporosis (risk for incomplete
calcium absorption and lifetreatening hypoMg w/ hypoCa)
Concerns regarding LT safety - possible increased acute interstitial nephritis and CKD
risk, increased gastric bacterial concentration (pneumonia risk), risk of low vitamin B12
absorption, and 203x increased risk of acquired C. diff
Interactions: may alter absorption of drugs, omeprazole inhibits metabolism of certain
drugs (warfarin, phenytoin, diazepam, and cyclosporine), FDA warning on reduced
efficacy of clopidogrel (Plavix) with omeprazole
✔✔Describe ABX treatments for H. pylori. - ✔✔Must use combination of drugs (Tx with
a single ABX is less effective, results in antimicrobial resistance, and is NOT
recommended)
Clarithromycin quadruple therapy x 14 days: PPI, clarithromycin, amoxicillin, and
metronidazole
Bismuth quadruple therapy x 10-14 days: PPI, bismuth subsalicylate, tetracycline, and
metronidazole
✔✔Describe antidiarrheal agents. - ✔✔antimotility agents (opiates and opioid
derivatives)(paregoric, lomotil, imodium)
, absorbents (Kaopectate)
antisecretory agents (bismuth subsalicylate)
others: probiotics, eluxadoline (Viberzi)(Rx opioid agonist for IBS-D; do NOT use with
pancreatitis, ETHO, or sphincter of Oddi disease)
***do NOT use with bloody diarrhea, high fever, or systemic toxicity***
✔✔List indications for antidiarrheals. - ✔✔acute nonspecific diarrhea
chronic diarrhea (IBS or IBD)
treatment of acute traveler's diarrhea
mild to moderate diarrhea
✔✔Bismuth Subsalicylate (Pepto-Bismol) - ✔✔antisecretory medication for diarrhea
bismuth may have antimicrobial effects, salicylate provides antisecretory effect, and
generally binds toxins
✔✔Kaopectate - ✔✔absorbent for diarrhea, kaolin + pectin
absorbs bacterial toxins and fluid in infectious diarrhea, decreases stool liquidity and
intestinal motility
reduces bioavailability of co-administered drugs
✔✔Diphenoxylate + Atropine (Lomotil) - ✔✔opioid derivative used to control diarrhea by
slowing peristalsis
formulated with atropine to decrease abuse potential
no analgesic effect @ antimotility doses, but higher doses can affect CNS
✔✔Loperamide (Imodium) - ✔✔opioid derivative used for diarrhea, decreases
peristalsis
no analgesic properties or addiction potential, but FDA warning that high doses can
induce euphoria and cardiac arrhythmias
ADEs: drowsiness, abd cramps, dizziness
can contribute to toxic megacolon, avoid in children or those with severe colitis