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28 Cards in this Set
- Front
- Back
omeprazole
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Proton Pump Inhibitor
Mechanism:*Inactive acid labile prodrug --> converted to active produg in bile duct cannulicular --> binds sulfhydral group in H/K ATPase --> irreversibly inactivates proton pump *active prodrug only binds actively secreting pumps --> give 30 minutes before meals Adverse reaction:*very safe *serious side effects rare *slight ↑ in bacteria --> pneumonia, traveler’s diarrhea, clostridium difficile in hospitalized patients *osteoporosis w/ long term use Clinical use:*healing and maintenance of Erosive esophagitis *healing of Gastric and duodenal ulcer *prevention of acute rebleeding ulcers *Prevention of NSAID ulcer *treatment of zollinger-ellison syndrome *GERD |
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Cimetidine (tagamet)
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H2 Blocker
Mechanism:*Inhibits parietal cell H2 receptor --> ↓basal > ↓postprandial acid secretion Adverse reaction:*avoid use requires frequent dosing, side effects, drug interactions.*CNS side effects with confusion esp. elderly *Endocrine side effects *gynecomastia *↓sperm production Clinical use:*Duodenal ulcer active and maintenance *gastric ulcer active * GERD *Zollinger-Ellison syndrome |
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Ranitidine (zantac)
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H-2 blocker
Mechanism:*Inhibits parietal cell H2 receptor --> ↓basal > ↓postprandial acid secretion Adverse reaction:*well tolerated *non-specific sideffects Clinical use:*Duodenal ulcer active and maintenance *gastric ulcer active * GERD *Zollinger-Ellison syndrome |
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Misoprostol
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Mucosal defense
Mechanism: *Analog of PGE1 --> binds PG receptor on parietal cell --> ↓ histamine-stimulated cAMP -->↓ acid *Also stimulates HCO3 and mucous secretion, enhances mucosal blood flow Adverse reaction: *Diarrhea and abdominal pain (limits use) Contraindication:*pregnancy --> stimulates uterine contractions Clinical use: *Prevention of NSAID ulceration (rarely used due to side effects) |
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Sucralfate
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Mucosal Defense
Mechanism:*consists of salt sucrose w/ sulfated aluminum that in acid environment extensive crosslinking produces viscous polymer that bind to ulcer craters and damaged epithelium --> prevents further damage *may stimulate local production of prostaglandins and epidermal growth factor Adverser Reaction:*constipation (aluminum) Contra indication:*renal failure (aluminum) Clinical Use:*mucositis *Bile acid gastropathy |
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Mylanta/Maalox
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Antacids
Mechanism:*AlOH and MgOH neutralize HCL --> rapid heartburn relief Adverse Reaction:AlOH --> constipation MgOH --> diarrhea Clinical Use:*fastest relief for heartburn but symptom relief is short |
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Bethanecol
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Cholinergic Agent
Mechanism:*produces uncoordinated contraction --> minimal prokinetic effect Adverse Reaction:*poorly tolerated --> broad muscarinic effects *bradycardia *diarrhea *cramps *salivation *blurred vision Clinical Use: *GERD *Gastroparesis |
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Neostigmine
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Cholinergic Agent
Mechanism:*Inhibits Ach degradation --> acclimation andmuscarine activation Adverse Reaction:*Cholinergic effects Contraindication:*Cardiac conduction problems *bronchospasm *bowel obstruction Clinical Use: *Olgives syndrome (intestinal pseudobstruction) |
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Metoclopramide
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Dopamine antagonist
Mechanism:*Substituted benzamide *Blocks D2 receptor --> ↑ACH release --> ↑intestinal motility, ↑ esophageal sphincter pressure *5Ht4 agonism also mediates effects *blocks medullary D2 receptor --> antiemetic effects Adverse Reaction:*Parkinsonian type dystonias (high doses) *tardive diskanesisa (long term use) *Restlessness, anxiety, agitation, drowsiness (10-20%) Clinical Use: *Promotility of Upper GI (no effect on lower GI) *Gastroparesis |
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Domperidone
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Dopamine antagonist
Mechanism:*D2 receptor blocker (does not cross CNS) *Blocks D2 receptor --> ↑ACH release --> ↑intestinal motility, ↑ esophageal sphincter pressure *5Ht4 agonism also mediates effects Adverse Reaction:*galactoria (blocks inhibitory effect of dopamine on prolactin as this part of CNS lacks BBB --> milk production) Clinical Use: *Gastroparesis |
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Erythromycin
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Motility agonist
Mechanism:*promotility agent *mimic action of motilin hormone --> activate motiline receptor on smooth muscle cells and enteric nerves --> ↑amplitude of migrating motor complexes Adverse Reaction:*Abdominal pain *tachyphylaxis Clinical Use:*gastroparesis *dysmotility (constipation) in scleroderma and bacterial overgrowth |
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Tergaserod
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Serotonin Modulator
Mechanism:*partial 5HT4 agonist --> ↑adynyl cyclase -->*stimulates GI motility in stomach, small bowel and colon *↓abdominal pain and bloating in IBS *stimulates chloride secretion Adverse Reaction:*diarrhea *adverse cardiovascular event --> drug withdrawn Contraindication:*Hx of Cardiovascular disease Clinical Use:*Constipation predominant IBS in women *chronic constipation in men and women |
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Cisapride
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Serotonin Modulator
Mechanism:*5HT4 agonist --> ↑ adenylyl cyclase activity in neurons *Weak 5-HT3 agonist Adverse Reaction:*Blocks HERG K+ channel --> QT prolongation --> ventricular arrythmias Clinical Use:*Severe dysmotility (constipation) who fail all other agents. |
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Alosetrone
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Serotonin Modulator
Mechanism:*Selective 5-HT3 antagonist --> ↓GI contractility, ↓motility, ↓visceral pain Adverse Reaction:*ischemic colitis --> drug withdrawn Clinical Use:*diarrhea predominant IBS |
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Odansetron
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Serotonin Modulator
Mechanism:*5HT3 antagonist in solitary nucleus of vagus, area postrema, chemoreceptor zone in brain stem, peripheral vagals afferent Clinical Use:*Nausea (chemotherapy or noxious GI stimulation) *Not for motion sicknes |
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Psyllium (metamucil)
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Fiber/Bulk Laxatives
Mechanism:*Non-absorbable polysaccharide --> ↑ bulk and water content of stool Adverse Reaction:*gas and bloating Clinical Use:*constipation |
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Methylcellulose
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Fiber/Bulk Laxatives
Mechanism:*Non-absorbable polysaccharide --> ↑ bulk and water content of stool Adverse Reaction:*gas and bloating *excessive bowel activity Clinical Use:*constipation |
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Docusate Sodium
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Stool Softner
Mechanism:*surfactant laxative --> ↓surface tension --> allows mixing of water with stool --> soften stool but no ↑ in frequency Adverse Reaction:*cramping *excessive bowel activity Clinical Use:*constipation |
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Senna
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Stimulant Laxatives
Mechanism:*Increase intestinal secretion and motor activity Adverse Reaction:*abuse potential *melanosis coli (brown benign pigmentation of colon – lipofusin in macrophages) *excessive diarrhea, cramping Clinical Use:*constipation |
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Biscotyl
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Stimulant Laxatives
Mechanism:*Increase intestinal secretion and motor activity Adverse Reaction:*abuse potential *melanosis coli (brown benign pigmentation of colon – lipofusin in macrophages) *excessive diarrhea, cramping Clinical Use:*constipation |
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Magnesium Hydroxide (milk of magnesia)
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Osmotic laxatives
Mechanism:*↑ stool osmolality and H20 content Adverse Reaction:*effective and safe for long term use Contraindication:*avoid long term use in renal failure Clinical Use:*constipation |
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Magnesium citrate
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Osmotic laxatives
Mechanism:*↑ stool osmolality and H20 content Adverse Reaction:*effective and safe for long term use Contraindication:*avoid long term use in renal failure Clinical Use:*constipation |
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Polyethylene glycol
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Osmotic laxatives
Mechanism:*↑ stool osmolality and H20 content *inert non-absorbed Adverse Reaction:*abdominal distension *flatulence Clinical Use:*colon preparation for surgery *constipation |
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Loperamide
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Anti-diarrheal
Mechanism:*Gut wall opioid receptor agonists --> ↓ peristalsis and ↑anal sphincter tone Adverse Reaction:*toxic megacolon *paralytic ileus *angioedema *steven-johnson syndrome *toxic epidermal necrolysis Clinical Use:*acute and chronic diarrhea |
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Kaopectate (peptobismal)
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Anti-diarrheal
Mechanism:*salicylate --> ↓ secretion *bismuth --> antimicrobial Adverse Reaction:*gray/black stool or tongue *tinnitus Clinical Use:*diarrhea *upset stomach *indigestion |
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Dipheynoxylate
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Antidiarrheal
Mechanism:*Gut wall opioid receptor agonist --> ↓ peristalsis *subtherapeutic atropine --> discourage overdose Adverse Reaction:*respiratory depression *ileus *pancreatitis *toxic megacolon *angioedema Clinical Use:*diarrhea |
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Mesalamine
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Anti-inflammatory
Mechanism:*exact mechanism unknown * blocks cyclooxygenase -->↓ prostaglandin production in colon --> anti-inflammatory effects Adverse reaction:*ulcerative colitis exacerbation *acute intolerance syndrome *Reye’s syndrome *aplastic anemia *renal failure *pericarditis *myocarditis *hepatotoxicity Clinical use:*chron’s disease *ulcerative colitis |
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Ursodiol
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Anti-biliary
Mechanism:*↓cholesterol synthesis secretion and absorption *alters bile cholesterol composition Adverse Reaction:*leucopenia Clinical Use:*gallstone prevention *gallstone dissolution |