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32 Cards in this Set
- Front
- Back
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esomeprazole, omeprazole, lansoprazole, pantoprazole, rabeprazole
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proton pump inhibitors
tx secretory disorders inhibit gastric acid secretion benzimidazole compounds irreversibly inhibit the parietal cell proton pump, H+/K+ ATPase are prodrugs that are inactive at neutral pH most effective drugs for suppressing gastric acid secretion b/c gastric response to ALL stimuli is inhibited single daily dose inhibits gastric acid secretion by 95-100% w/o affecting pepsin secretion or gastric motility irreversibly inhibits proton pump well tolerated adverse effects: GI effects (nausea/colic/flatulence/constipation/diarrhea), CNS effects (HA, dizziness, somnolence), skin rashes, w/ prolonged use, diarrhea b/c of GIT bacterial overgrowth from removal of natural acid barrier, hypergastrinemia hepatic metabolism w/ negligible renal clearance intestinal absorption is rapid, but bioavailability depends on activation at gastric acid pH promotes peptic ulcer healing, prevents ulcer recurrence effective in pts unresponsive to H2 antagonists more effective than H2 antagonists for GERD or NSAID-induced peptic ulcers |
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cimetidine, famotidine, nizatidine, and ranitidine
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H2 receptor antagonists to tx secretory disorders
reduces gastrin secretion blocks histamine-induced increase in cAMP and proton pump activation (gastric acid secretion) histamine (via H2 receptor) enhances parietal cell affinity for both gastrin and acetylcholine all are OTC preps that inhibit acid secretion for < 6 hrs prescription doses inhibit 60-70% of the total 24-hr acid secretion all are equally effective, rapidly and well absorbed orally, and generally well tolerated with few side effects selectively reduce gastric acid and pepsin secretion especially effective against nocturnal secretion which is largely due to histamine relative potency varies oer a 50-fold range: famotidine>nizatidine = ranitidine>cimetidine are extremely safe with minor and infrequent adverse effects should not be given to pregnant or nursing women as they cross the placenta and are secreted into breast milk most common side effects: diarrhea, HA, fatigue myalgias constipation and bradycardia mental changes like confusion, hallucinations, and agitation may occur with IV administration in patietns who are elderly or have renal or hepatic dysfunction cimetidine: longest on the market gynecomastia or imporence in men and galactorrhea in women, these endocrine effects occur because cimetidine inhibits binding of dihydrotestosterone to androgen receptors, inhibits estradiol metabolism and increases serum prolactin interferes with cytochrome P450 pathways for hepatic metabolism of many drugs all equally effective for healing and preventing recurrence of PUD given once daily at bedtime to suppress nocturnal acid secretion will produce ulcer healing rates of >80-90% after 6-8 weeks of tx their use declined markedly following the discovery of PPIs and role of H. pylori in PUD 20% failure in ulcer patients who smoke and in the elderly should not be used in combo with PPIs b/c reduce the efficacy of PPIs by reducing acid activation combined w/ antibiotics and bismuth for tx of patietns w/ H. pylori infection |
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aluminum hydroxide
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antacid to tx secretory disorders
seldome used, but act by reducing gastric acidity, inactivating pepsin, are weak bases that neutralize gastric HCl to form salt and water, and may interfere with absorption of other drugs may also provide mucosal protection by stimulating PG synthesis most adverse effects: diarrhea for magnesium and constipation for AL, cation absorption and systemic alkalosis in renal patients vary widely in neutralizing capacity, taste, and price antacid tablets are generally weak, needed in large numbers, and not recommended for tx of active peptic ulcers used as needed to relieve pain in esophagitis, peptic ulcer, and GERD |
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calcium carbonate
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antacid to tx secretory disorders
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combo aluminum hydroxide and magnesium hydroxide
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antacid to tx secretory disorder
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sucralfate
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mucosal protective agents, used to tx secretory disorders
binds selectively to necrotic ulcer tissue and acts as a barrier - polymerizes to produce a viscous, sticky gel that adheres strongly to epithelial cells and ulcer craters in acid environment effective in healing duodenal ulcers most common side-effect is consipation poorly absorbed systemically and has few adverse effects requires acid pH for activationa nd should not be given together with antacids, H2 antagonists, or PPIs |
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misoprostol
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mucosal protective, used to tx secretory disorders
the methyl analog of PGE1 binds to PG receptors on parietal cells to inhibit acid secretion ecause NSAIDs inhibit PG, used to prevent NSAID-induced ulcers exact mech uncertain but may be cytoprotective or by inhibiting histamine-stimulated gastric secretion adverse effect: diarrhea, abdominal pain, may cause abortion |
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bismuth subsalicylate
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mucosal protective agents, used to tx secretory disorders
protective coating of ulcers antibacterial against H. pylori OTC with estimated use by 60% of american households for tx dyspepsia and acute diarrhea adverse effects: minimal, darken tongue,stools |
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clarithromycin, amoxicillin, PPI
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antimicrobial drugs, used to tx secretory disorders
effective against H. pylori infection 10-14 day tx using "triple therapy" |
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saline laxatives
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osmotically active laxatives, used to tx osmotically active laxatives
nonabsorbable salts containing magnesium cations or phasphat anions act by osmotic force to hold water inside the intestines --> distended intestines --> stimulate peristalsis have an intensely bitter taste that is masked by adding citrus usu well tolerated, but should be avoided in pts with renal insuff, heart disease, electrolyte imbalance, diuretic drug cotx |
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nondigestible sugars and alcohols
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glycerin, lactulose, sorbitol, and mannitol
glycerin - trihydroxy alcohol that when given rectally acts as a lubricant and hygroscopic agent --> water retention --> stimulate peristalsis lactulose, sorbitol, and mannitol are nonabsorbable sugars --> hydrolyzed to organic acids --> acidify luminal contents --> draw water into lumen --> increase colonic propulsive motility |
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polyethylene glycol (PEG) - electrolyte solutions
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osmotically active laxatives used to tx motility disorders
PEG is poorly absorbed and retains added water by high osmotic pressure |
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anthraquinones, ricinoleic acid
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stimulant or irritant laxatives, used to tx motility disorders
in general: act directly on enterocytes, enteric neurons, and muscle --> induce low-grade intestinal inflammation --> water and electrolytes accumulate --> increase intestinal motility specifically for anthraquinones: poorly absorbed in small intestine, require activatino in colon, laxative effect 6-12 hrs later, long term use --> melanomic pigmentation of colon mucosa and colon becomes dilated and ahaustral ricinoleic acid, specifically: (castor oil) - local irritant that increases intestinal secretion and motility, seldom used b/c of unpleasant taste and toxic potential |
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methylcellulose, lactulose, and polycarbophil
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bulk-forming laxatives, used to tx motility disorders
add bulk, hold water to intestinal contents |
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mineral oil, glycerin suppositories, and docusate
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stool softener, used to tx motility disorders
soften stools, facilitate expulsion given orally or rectally docusate - prescribed to prevent straining in hospitalized pts |
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loperamide, difenoxin, diphenoxylate
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antidiarrheal
act on intestinal opioid receptors --> inhibit ACh release --> decrease GIT motility (peristalsis) loperamide, specifically: 40-50x more effective than morphine for diarrhea - does not cross BBB acts quickly on oral administration with peak levels at 305 hrs --> relief of acute, nonspecific diarrhea effective agaisnt traveler's diarrhea, should be discontinued if clinical improvement doesnt occur w/in 48 hrs few adverse effects, more effective than diphenoxylate |
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bismuth subsalicylate
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antidiarrheal
inhibits intestinal secretions --> management of infectious diarrhea |
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kaolin/pectin
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antidiarrheal
acts by absorbind compounds and presumably binding potential intestinal toxins |
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dimenhydrinate, diphenydramine, cyclizine, meclizine
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histamine H1 antagonists, antiemetic
many 1st generation H1 blockers --> sedation, antimuscarinic activity which prevents motion sickness |
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metoclopramide, trimethobenzamide
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D2 antagonists, antiemetic
unclear mech of antiemetic action |
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ondansetron, granisetron, dolasetron
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HT3 antagonists, anti-emetic
currently used for nausea/vomiting during cancer chemo |
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chlorpromazine, prochlorperazine
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phenothiazines, antiemetic
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lorazepam, alprazolam
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benzodiazepine, anti-emetic
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tetrahydrocannabinol, dronabinol
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marijuana derivatives, anti-emetic
underlying mech not known dronabinol - used as prophylacic in pts receiving cancer chemo adverse effects: central sympathomimetic activity - "marijuana highs" - mood changes, laughing, paranoid reactions, thinking abnormalities |
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amitriptyline, desipramine
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tx IBS, tricyclic antidepressant
tx abdominal pain |
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dicyclomine, hyoscyamine
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anticholinergic, antispasmodic
used to tx IBS |
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tegaserod
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5-HT4 partial agonist
emergency tx only - IBS with constipation - where no alternative exists serious CV events can occur |
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alosetron
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5-HT3 antagonist
used when conventional therapy fails, diarrhea-predominant IBS |
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orlistat
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anti-obesity drugs
targets the gut, GI lipase inhibitor reduces absorption of fats side effects: flatulence, steatorrhea, fecal incontinence |
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sibutramine
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anti-obesity drug
target organ - CNS target molecule - SERT and NET inhibitor reduces appetite adverse effects: cardiovascular - tachycardia, hypertension |
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rimonabant
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anti-obesity drug
target organ: CNS (peripheral?) target molecule - C1 receptor antagonist reduces appetite adverse effects: CNS - depression, anxiety, nausea |
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diphenylmethane derivatives: bisacodyl, phenolphthaleine
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stimulant or irritant laxatives
bisacodyl - available as enteric coated tablets taken at bedtime to take effect the next morning to avoid activation in stomach, tablets should be swallowed w/o chewing or crushing phenolphthalein - withdrawn due to potential carcinogenicity |
