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Pharmacology-GI
| Question | Answer |
|---|---|
| cromolyn | inhibit mast cell degranulation by preventing release of Ca from SR & thus the inc in intracellular Ca concentration caused by IgE bridges. no de novo synth of bronchoconstrictors |
| olopatadine*** | inhibit mast cell degranulation by preventing release of Ca from SR & thus the inc in intracellular Ca concentration caused by IgE bridges. no de novo synth of bronchoconstrictors. also BLOCKS H1 RECEPTORS!! (given in eye) |
| brompheniramine | H1-receptor antagonists. |
| chlorphenirmaine | H1-receptor antagonists |
| diphenhydramine | H1-receptor antagonists; used to tx low BP in acute allergic rxns (immediate hypersensitivity), blocks CENTRAL muscarinic recp.-> sedation & antiemetic. topical causes local anesthesia (block Na chann in afferent sensory pain fibers), Tx of parkinson |
| dimenhydrinate*** | H1-receptor antagonists. also blocks CENTRAL muscarinic recep--> sedation & antiemetic **prophylaxis for motion sickness and for reduction of vertigo of vestibular origin (MENIERE'S dz) w/ meclizine |
| hydroxyzine | H1-receptor antagonists. also blocks CENTRAL muscarinic recep--> sedation & antiemetic |
| cyproheptadine | H1-receptor antagonists |
| promethazine*** | H1-receptor antagonists. also blocks CENTRAL muscarinic recep--> sedation & antiemetic. inhibits mast cell degranulation (slightly) ***Tx of motion sickness. never give i.v, |
| cetirizine | H1-receptor antagonist. 50% elim by kidney 50% by liver |
| fexofenadine | H1-receptor antagonists. inhibits mast cell degranulation(slightly). 95% eliminated by kidney |
| loratadine | H1-receptor antagonist. converted to active metabolite by hepatic first pass metab. toxic if liver failure |
| desloratadine | H1-receptor antagonist. active metab of loratadine. longer half life than loratadine. elim by kidney. |
| meclizine*** | H1-receptor antagonist. **prophylaxis for motion sickness & for reduction of vertigo of vestibular origin (MENIERE'S dz) w/ dimenhydrinate |
| olopatadine | H1-receptor antagonist |
| famotidine | H2-histamine receptor antagonist."tidine" inhib basal & nocturnal acid secretion. prvnts all gastric acid secretion. for ulcers, GERD, anaphylaxis, viral warts (skin lesions), tox: preg cat B, n/v, diarrhea, skin rashes |
| ranitidine | H2-histamine receptor antagonist."tidine" inhib basal & nocturnal acid secretion. prvnts all gastric acid secretion. for ulcers, GERD, anaphylaxis, viral warts (skin lesions), tox: preg cat B, n/v, diarrhea, skin rashes |
| cimetidine | H2-histamine recep antagonist."tidine" inhib basal & nocturnal acid secretion. prvnts all gastric acid secretion. for ulcers, GERD, anaphylaxis, viral warts (skin lesions), tox: preg cat B, inhib CYP450-> antiandrogenic, CNS effects, n/v, diarrhea, rash |
| sumatriptan**** | 5-HT 1B/1D recep agonist. MOA: cranial VC, **peripheral inhib of release of inflamm peptides from trigeminal n. by stim presyn recep, central inhib of 2nd order neurons in trigemino-cervical complex. can cause periph VC-> MI in CAD. tx of migraines, |
| metoclopramide*** | 5-HT3 & D2 recept ANTAGONIST and 5-HT4 recept AGONIST. GI stim inc ACh release, antiemetic, enhance cl of gastric acid, INC LES , accel gastric emptying, dec sml bowel transit time. empties stomach, prvnt n/v. S/E: sedation, fatigue, **dystonia |
| ondansetron*** | 5-HT3 recept antagonist. blocks recp at vagal n. endings & CTZ to prvnt n/v. works better than metoclopramide & no dystonia/akathisia.**post op n/v. **"morning sickness" DOC for kids S/E: constipation |
| dolasetron | 5-HT3 recept antagonist |
| cyproheptadine*** | 5-HT1 and 5-HT2 recp antagonist. . for tx of ***carcinoid synd. also blocks H1&muscarinic->S/E: worse angle-closure glaucoma, BPH, GI obsrtuction, CNS depression, sedation, dry mouth, nose |
| ipecac | DOC for inducing emesis. stim CTZ & cause local irritation of stomach & upper duodenum. can use for antiemetic drug overdose. S/E: diarrhea, drowsiness, sedation, leargy, fever, diaphoresis, chronic use->cardiomyopathy |
| scopolamine | Antiemetic agent. blocks musc. recep in vestibular nuclei & reticular formation. S/E:xerosomia, sedation, inability to concentrate, amnesia, fatigue. prophylaxis for motion sickness |
| dimenhydrinate | Antiemetic. Antihistamine/anticholinergic. blocks muscarinic recep. prophylaxis for motion sickness & pregnancy "morning sickness"& tx of vestibular vertigo (Meniere's dz) |
| diphenhydramine | Antiemetic. Antihistamine/anticholinergic. blocks muscarinic recept |
| meclizine | Antiemetic. Antihistamine/anticholinergic. blocks muscarinic recept. prophylaxis for motion sickness &pregnancy "morning sickness" & tx of vestibular vertigo (Meniere's dz) |
| promethazine | Antiemetic. Antihistamine/anticholinergic. blocks muscarinic recept. tx for motion sickness |
| metoclopramide*** | Antiemetic. blocks 5-HT3 recep (vagal afferent fibers & CTZ) & D2 recep(CTZ). MOA: inc release of ACh by stim 5-HT4 recep on cholinergic fibers. increase: LES pres, gastric emptying, antegrade mvmt. clear stomach for procedures, tx:diabetic gastroparesis |
| prochlorperazine | Antiemetic. Dopamine recep antagonist |
| ondansetron | "setron" Antiemetic. 5-HT3 recep antagtonist. prophylaxis for pregnancy "morning sickness" |
| dexamethasone | Antiemetic. corticosteroid. MOA unknown. |
| dronabinol | Antiemetic. MOA unknown. used in cancer pts; chemotherapy |
| metoclopramide | Prokinetic agent. inc gastric emptying |
| methylcellulose | bulk laxative. attracts water, forms hydrogel w/feces in lrg bowel. inc bulk 30fold. distention activates strech recep->inc peristalsis. soften stool,inc water content, colonic transit rate &freq of defecation. no dependence.tx of constipation |
| psyllium | bulk laxative. hydrophilic mucilloid from indigestible seed coat. attracts water to form hydrogel w/feces in lrg bowel. inc bulk 30fold. no dependence. tx of constipation |
| calcium polycarbophil | laxative. hydrophilic resin. absbs 60x wt. draws water into bowel to expand bulk & activate local peristaltic reflex. no dependence.tx of constipation |
| lactulose | synthetic disacch. NOT absorbed in GI. bacteria in bwl degrade lactulose to lactic,acetic,organic acids->osmotic effect draws water into colon,inc peristalsis(local rflx) acidification of bwl->ammonia trapped in blood excr as ammonium ions. no dependence |
| docusate sodium | stool softener. laxative. "soap for poop" detergent lowers surface tension of feces, allows penetration of water.emulsifies poop. no laxative dependence. added to iron supp. to prvnt constipation |
| bisacodyl | laxative. .irritant action inc accumulation of water&electro in lumen of COLON &inc peristalsis via local rflx. soft stool 6-12hr purge effect 15-60 min.cathartic agent.can cause LAX DEPENDENCE -constipation, hypoK, mus weakness, abnml GI wall architec |
| magnesium hydroxide | laxative. can cause LAX DEPENDENCE, GI colic, dehyd, electro imbal. osmotic(saline). hypertonic osmotic force draws water into LRG bowel.GI disten activ stretch recep->inc peristalsis via local rflx. cathartic agent. S/E: diarrhea |
| polyethyleneglycol | laxative. can cause LAX DEPENDENCE, GI colic, dehyd, electro imbal. osmotic(saline). hypertonic osmotic force draws water into LRG bowel.GI disten activ stretch recep->inc peristalsis via local rflx |
| Irritable bowel syndrome*** | bulk laxitives. (methylcellulose, psyllium, polycarbophil). expand lrg bowel &prvnt alternating segmental contractions of smth muscle. restore antegrade peristalsis |
| Irritable bowel syndrome | dicyclomine. muscarinic recep antagonist that may prvnt bowel spams ass w/ Irritable bowel syndrome |
| Tx of portal-systemic encephalopathy of hepatic disease | lactulose. (acidifies colonic contents -> ammonia trapping in bowel to be excreted. dec plasma ammonium . improves mental state |
| diphenoxylate | Antidiarrheal. opiate. slows colonic transit rate by direct/indirect inhib of GI motility (dec motility but inc tone) bowel stasis |
| loperamide*** | Antidiarrheal. opiate. slows colonic transit rate by direct/indirect inhib of GI motility (dec motility but inc tone) bowel stasis. tx of DIARRHEA |
| kaopectate | Antidiarrheal. absorbent powder. large suface area of finely powdered clay(w/neg charge) absorbs bacterial toxins. pectin is hydrated &forms viscous solution that consolidates stool |
| calcium polycarbophil*** | Antidiarrheal. resin that aborbs excessive water in bowel to form gel which helps consolidate stool. only drug used for tx of BOTH CONSITPATION & DIARRHEA |
| bismuth subsalicylate | ANTIDIARREAL:coating agent.incredible antibacterial:bind -SH groups, prvnt binding by dec adhesiveness. ANTIULCER:protects irritated mucosa,coats mucosa,inc PG synth &alkali secretion, antiproteolytic.S/E:salicylate tox, dec abs tetracyclines,stool dark |
| octreotide | Antidiarrheal. somatostatin agonist. stim somat recep in GI.tx of carcinoid synd (inhib release of serotonin from tumor cells)& VIPomas, stop bleeding-esoph varices(fewerS/E than AVP no angina/MI),constrict splanchnic arterioles dec portal press |
| clarithromycin*** | Antibiotic triple therapy "say CAiO to ulcers" |
| amoxicillin*** | Antibiotic triple therapy "say CAiO to ulcers" |
| omeprazole*** | Antibiotic triple therapy "say CAiO to ulcers" |
| Aluminum hydroxide | anti-ulcer. antacids. S/E: constipation; contraindicated when using doxycycline |
| Mg hydroxide | anti-ulcer. antacids. S/E: diarrhea; contraindicated when using doxycycline |
| cimetidine | anti-ulcer. blocks H2 recep in gastric parietal cells. dec basal & nocturnal acid secr. block acid secr elicited by histamine,food,coffee,insulin,&inc vagal act. S/E:inhib CYP450(inc 1/2life other drugs, antiadrogenic,CNS effects |
| ranitidine | anti-ulcer. H2 recep antagonist. blocks H2 recep in gastric parietal cells. dec basal & nocturnal acid secretion. block acid secretion elicited by histamine,food,coffee,insulin,&inc vagal act. NO CNS EFFECTS, NO INHIB DRUG METAB, NO ANTIANDROGENIC EFFECT |
| famotidine | anti-ulcer. H2 recep antagonist. blocks H2 recep in gastric parietal cells. dec basal & nocturnal acid secretion. block acid secretion elicited by histamine,food,coffee,insulin,&inc vagal act. NO CNS EFFECTS, NO INHIB DRUG METAB, NO ANTIANDROGENIC EFFECT |
| omeprazole | anti-ulcer. PPI."prazole"inhib H-K ATPase. acid secr blocked 24-72hr.inhib basal &nocturnal&other stimuli secretion. gastric pH rises to 4-5. no LES,motility effect. does NOT inhib release of IF,rise in pH part.inhib B12 absorb but NO megabls anemia |
| esomeprazole | anti-ulcer. PPI."prazole"inhib H-K ATPase. acid secr blocked 24-72hr.inhib basal &nocturnal&other stimuli secretion. gastric pH rises to 4-5. no LES,motility effect. does NOT inhib release of IF,rise in pH part.inhib B12 absorb but NO megabls anemia |
| misoprostol | anti-ulcer. PGE analog. stim of PGE1 recep on gastric parietal cells inhib acid secr. no effect on basal acid secr but blocks secr caused by stimuli, protects mucosa, S/E:diarrhea,NOT FOR WOMEN OF CHILD BEARING AGE. potent abortifacient |
| sucralfate | anti-ulcer. protective coating agent.forms gel in ACIDIC envir binds ulcerated mucosa &can help tx GERD. NO CHANGE stomach pH or inhib acid secr. better on DUOD ulcers. prvnts relapse. DON'T USE W/H2 blocker,omeprazole,antacids. S/E:Al tox, hyperPHOS |
| methylprednisone | inflammatory bowel disease (IBD). corticosteroid. inhib PG and LT synth. locally alt immune fxn. |
| mesalamine | inflammatory bowel disease (IBD). NSAID. 5-ASA. |
| olsalazine | inflammatory bowel disease (IBD). NSAID. two 5-ASA |
| ursodiol | dissolves gallstones.undergoes enterohepatic recirculation. incr ratio of bile salt acids & phospholipids to CHO by dec CHO synth (inhib HMG CoA), reduce GI absorp of CHO, dec biliary secr of CHO. inc solub of CHO. NOT for severe colicky/cholecystitis |
| ursodiol | Tx of primary biliary cirrhosis. (slows progression) |
| psyllium | Tx of hyperlipoproteinemia. (lowers total CHO & LDL). MOA: binds to bile acids & incr their fecal excr. loss of bile dec intrahepatic concent of sterol pool-> upreg hepatic LDL recep-> dec plasma LDL cholesterol |
| S/E of sumatriptan | rebound headaches, atypical sensations (tingling etc), dizziness, vertigo, severe coronary vasospams in pts w/CAD or MI, inc SBP/DBP, do not use w/ergot-type drug |
| S/E of metoclopramide | sedation & fatigue, altered GI absopt of other drugs, dystonia, mvmt d/o (parkinsons), increasd plasma prolactin->galactorrhea, amenorrh, gynecmastia, |
| tx of Diarrhea | DIPHENOXYLATE/ LOPERAMIDE(invasive like shigella); kaopectate abs excess fluid &toxins inc consistency; bismuth subsal antibacterial &abs toxins; loperamide/ diphenoxylate bowel stasis w/o opiate addiction; promethazine for n/v |
| tx of Gastric Ulcers | H2 blocker (CIMETIDINE); antibiotics: clarithromycin, omeprazole,amoxacillin; PGE agonist: (MISOPROSTOL); PPI:omeprazole; sucralfate, antacid (Al &/ Mg hydroxides) |
| prophylaxis of NSAID-induced gastropathy | MISOPROSTOL (prvnt GI ulcer&bleed, does NOT affect NSAID action, use only in high risk pts 60+,smokers,prorHx of ulcers) SUCRALFATE (dec heartburn, epigas pain, does not change stomach pH) |
| preferred drug in ventilated pt w/stress ulcer | SUCRALFATE (does not increase stomach pH so no incr risk of nosocomial pneumonia that would have been prnted by gastric acid |
| prophylaxis of corticosteroid induced gastropathy | MISOPROSTOL |
| Tx of heartburn | OTC antacids, H2 blocker (cimetidine, famotidine) |
| Tx of GERD | inhib gastric secretion: OMEPRAZOLE (PPI), CIMETIDINE or FAMOTIDINE (H2 blocker), SUCRALFATE, antacids, CISAPRIDE (inc LES), TEGASEROD |