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41 Cards in this Set
- Front
- Back
2 physiological agents that induce secretion of acid
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gastrin, histamine
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makin pathway that regulate acid production?
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meal/anticipation of meal --> releases gastrin from gastrin containing cells --> induces release of histamine from enterochromaffin like cells (ECL) --> histamine diffuses to parietal cell and acts on H2 receptors on parietal cells to produce cAMP and activate proton pump -> secrete H+
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minor pathway that regulates acid production
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activation of M1 receptors on ECL cells cause histamine release; activation of M3 receptors on parietal cells cause Ca+ mediated acid release; activation of gastrin receptors on parietal cells cause Ca+ med acid release; activation of EP receptors on parietal cells activated by prostaglandin inhibit acid secretion
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what does proton pump do
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membrane bound H+ K+ ATPase protein that pumps H+ into lumen across conc gradient
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for disease causally linked to Helicobacter pylori, what is the main risk factor?
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infected family membors; gastric/ duodenal uclcer
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in gastric/duodenal ulcers, what is secreted by causative agent that neutralizes gastric acid
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h. pylori secretes urease
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what is the therapy for gastric/duodenal ulcers?
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antibacterial plus agent that decreases acid
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5 ways to diagnostically test for h. pylori
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serology; non-endoscopic urease test (urease breath test, measure expired CO2); fecal antigen test, culture, endoscopy
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first line for GERD, major dyspepsia, acid disorders?
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proton pump inhibitors
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MOA of PPIs?
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suicide inhibitor of HKATPase - covalent binds, prodrug activates in acidic environment and becomes protonated and trapped on acidic parietal cell
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admin and form of PPI?
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delayed release, gelatin coated capsules, or enteric coated granules or tablets, or powdered drug with sodium bicarbonate; absorbed rapidly, better absorb before meal
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half life and absorption of PPI?
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absorb rapidly, bound to plasma portein, cleared by hepatic metabolism, metabolites excreted in urine.
t1/2 of 30-90 min |
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which PPI is least metabolized by CYP2D19
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rabeprazole
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for peptic ulcers, which is better: H2 antagonists or omeprazole
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omeprazole
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what other syndrome is PPI used for?
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zollinger-ellison
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what should you worry about for long term, high dose PPI therapy in elderly?
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increased incidence of hip fracture
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first line therapy for eradicating H pylori infxn
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PPI + amoxicillin + clarithromycin
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if you have a resistant H pylori infxn what can you give them
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PPI + bismuth subsalicylate + tetracycline + metronidazole
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what is the mechanism of action for the non-ulcer dyspepsia tx that has an anti-androgenic side effect?
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h2 receptor antagonist (cimetidine); acts via histamine H2 receptors on parietal cells; inhibits acid secretion stim by gastrin and muscarinic agonists; inhbits gastric HCl secretion
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what does H2 receptor antagonists decrease and block?
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volume of gastric juice, pepsin production, intrinsic factor production
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what is a potential complication of h2 receptor antagonists?
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vit deficiency
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3 mucosal protective agents
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colloidal bismuth compound, misoprostol (cytotec), sucralfate (carafate)
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what should you never use in pregnant women bc its side effect of uterine contraction?
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misoprosol, a mucosal protective agent
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how does subsalicylate work?
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increases mucosal secretion, coats ulcer, detachment of h pylori from gastric epithelium and bacteria lysis; no acid-neutralizing activity
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what is the MOA of a rapidly absorbed mucosal prot agent that is approved only for NSAID induced gastric ulcers?
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synthetic analog of PGE1, decrease gastric acid secretion, increases mucus and bicarb secretion
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what is triple therapy?
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multi drug therapy
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what mechanism is responsible for lengthy duration of action in ppis
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covalent binding to HKATPase, new synth of enzyme must be made
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which h2 antagonist may be admin IV?
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?
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how does sucralfate and misoprostol differ in moa?
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sucralfate- complex Al-sucrose sulfate; thought to coat ulcer, acid/pepsin barrier, may stim pge synth
misoprostol - synth analog of pge, increases mucus, bicarb, decreases acid secretion |
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list major antacids?
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sodium bicarb, calcium carbonate, magnesium salts, aluminum compounds, antacid mixtures
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role of colloidal bismuth compound in triple therapy?
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used with PPI and tetaracycline and metronidazole for resistant h pylori
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what are the side effects/toxicity of a drug in which bases present react to neutralize stomach acid, decrease heartburn/pain sx, heal ulcer?
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alkaluria and kidney stones, high sodium content dangerous for hypertensive or CHF pts
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what exacerbates GERD and is not recommended for peptic ulcer tx, GERD, hypertensives, most others?
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sodium bicarbonate
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which antacid is recommended for women, esp pregnant women?
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calcium carbonate, tums
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what antacid that produces belching also causes transient metabolic alkalosis
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sodium bicarbonate
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which antacids are cathartics, osmotic effects, and stim intestinal motility?
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magnesium salts, milk of magnesia
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what is one diff between sodium bicarb and magnesium salts
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mg salts have longer duration of action
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which constipating antacid binds to phosphate preventing absorption and shouldn't be given with tetracycline?
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aluminum compounds
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what happens to aluminum compounds on storage
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lose potency
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which two antacids are usually used together to overcome constipating and cathartic side effects?
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aluminum and magnesium
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what are all the uses of ppis?
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gerd, peptic ulcer, major dyspepsia, nsaid induced ulcer, lifetime therapy, zollinger ellison syndrome
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