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28 Cards in this Set

  • Front
  • Back
omeprazole
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
Cimetidine (tagamet)
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
Ranitidine (zantac)
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
Misoprostol
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)
Sucralfate
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
Mylanta/Maalox
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
Bethanecol
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
Neostigmine
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)
Metoclopramide
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
Domperidone
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
Erythromycin
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
Tergaserod
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
Cisapride
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.
Alosetrone
Serotonin Modulator
Mechanism:*Selective 5-HT3 antagonist --> ↓GI contractility, ↓motility, ↓visceral pain

Adverse Reaction:*ischemic colitis --> drug withdrawn

Clinical Use:*diarrhea predominant IBS
Odansetron
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
Psyllium (metamucil)
Fiber/Bulk Laxatives
Mechanism:*Non-absorbable polysaccharide --> ↑ bulk and water content of stool

Adverse Reaction:*gas and bloating

Clinical Use:*constipation
Methylcellulose
Fiber/Bulk Laxatives
Mechanism:*Non-absorbable polysaccharide --> ↑ bulk and water content of stool

Adverse Reaction:*gas and bloating *excessive bowel activity

Clinical Use:*constipation
Docusate Sodium
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
Senna
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
Biscotyl
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
Magnesium Hydroxide (milk of magnesia)
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
Magnesium citrate
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
Polyethylene glycol
Osmotic laxatives
Mechanism:*↑ stool osmolality and H20 content *inert non-absorbed

Adverse Reaction:*abdominal distension *flatulence

Clinical Use:*colon preparation for surgery *constipation
Loperamide
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
Kaopectate (peptobismal)
Anti-diarrheal
Mechanism:*salicylate --> ↓ secretion
*bismuth --> antimicrobial

Adverse Reaction:*gray/black stool or tongue *tinnitus

Clinical Use:*diarrhea *upset stomach *indigestion
Dipheynoxylate
Antidiarrheal
Mechanism:*Gut wall opioid receptor agonist --> ↓ peristalsis *subtherapeutic atropine --> discourage overdose

Adverse Reaction:*respiratory depression *ileus *pancreatitis *toxic megacolon *angioedema

Clinical Use:*diarrhea
Mesalamine
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
Ursodiol
Anti-biliary
Mechanism:*↓cholesterol synthesis secretion and absorption *alters bile cholesterol composition

Adverse Reaction:*leucopenia

Clinical Use:*gallstone prevention *gallstone dissolution