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107 Cards in this Set
- Front
- Back
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Cimetidine , Famotidine, Ranitidine, Nizatidine
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H2 receptor blockers,
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aluminum hdryoxide
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antaacid, weak base that reacts with HCl in stomach, raises intragastric pH, CONSTIPATION, affects bioavailaibitliy of TC, digoxin, antimuscarinics reduced.
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magnesium hydroxide
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antaacid, weak base that reacts with HCl in stomach, raises intragastric pH, DAIRRHEAn, affects bioavailaibitliy of TC, digoxin reduced.
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calcium carbonmate
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antaacid, weak base that reacts with HCl in stomach, raises intragastric pH, kindey stones, dense fecal matter
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histamine, Ach and gastrin
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imp stimuli for gastric acid secretion from pareital cell , activate K/KATPase pump
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Dycylomine
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blocks cholinergic receptor and reduces gastric acid secretion
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Cimetidine
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H2 antagonist, reduces gastric acid secretion , via GS(+cAMP), given orally, excreted in urine, short half life, increased renal failure, inhibits C450 and slows metab of warfarin, diazepam, pheytoin, quinidine, carbamazepine, theophylline, and imipramine , AE- gynecomastia, galactorea, reduced perm count
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misoprostol
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stimulates prostaglandin receptiron and reduces acid secretion , via Gi(-cAMP)
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omeprazole
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blocks proton pump
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Ranitidine , Famotidine, Nizatidine
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H2 antagonist, single dose reduces basal secretion og gastric acid, used for gastric and duodenal unclers and preventing recurrence, only paritally inhibits gastric acid secretion induced by acetylcholine or bethanechol , reoccurence of peptic ulcers wit htehse , AE- HA, diarrhea, muscular pain, CNS( confusion, hallucinations) , reduces ketonacoazole reabsotion(needs gastric acid medium)
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ranitidine
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10 times more potent than cimetidine, no antiandrogenic and protein stimaution effects, does not inhibit mixed function oxygenase in liver
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Famotidine
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40-50X more potent than comeitine
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nizatidine
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no first pass metab, 100% bioavailability, elimiated by kidney, no IV
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Omeprazole, esomeprazole
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proton pump inhibitrs, binds to H/K ATPase, proton pump of parietal cell, supresses secretion of H ions into gastric lumen , approved for GERD, reduce risk of bleeding with NSAIDs, used for hemoragic ulcers, eradicate PPIs, AE- increased gastric carcinoid tumors, inhibits metabolism of warfarin, phenytoin, diazepam, cyclosporine, prolonged use of PPI and H2 blockers may decrease B12 bioavailability, calcium carbonate- requires low gastric pH, give calcium citrate, small increase inGI infections, rarely pancreatitis, hepatotoxicity, and intersitital nephritis
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sucralfate
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cytoprotentic(mucosal protective) agent, compel of AlOH and sulfated sucrose, bind to protiens forming complex gels with epithelial cells, sucralfate creates physical barrier againt HCl and prevents degradation of mucus by pepsin and acid , stimulates prostaglandin release as well as mucus and bicarb output, requires acidic pH for polymeriazation, dont give with H2 atnaogins
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prostaglandins
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PGE2 produced by gastric mucosa inhibits HCl secretion and stimulates secretion of mucus and bicar(cytoprotective effect), defieciency of PGs invovled in pathogenesis of peptic ulcers
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misoprostol
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analog of porstiglaidin E, approved for presenvtion of gastric ulcers induced by NSAIDs , less effective than H2 antagonists and PPIs for acute treatment of peptic ulcers
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regimens for H pylori
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1) PPI+claryothromycin+amoxillin2)PPI+clarithromycin+metronidazole3) bismuth subsalicyclate+metronidazole+tetracyline+ranitidine or PPI
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rofecoxib and vioxx , celebrex
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coxibs are superior gastro AE profile over conventiornal NSAIDs, taken off market in 2004 due to MI(bioxx),
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pirenzipine
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Anticholinergic, msucarinic antagonis, supresses acid secretion via M3, poor penetration through BBB low CNS toxicity, used for petic ulcer in regractory cases
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dycyclomine
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Anticholinergic, msucarinic antagonis, ihinits acid secretion by binding to mAchR in parietal cels, not as effective as H2 or PPI, use- IBS, AE- dryness of mouth, blurred vision, urinary retention, arrythmias and constipation at higher doses
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cisapride
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not avail in US, release Ach in myenteric plexus, increases muscle tone in esophageal sphicnter, GERD, increases gastric emptying in people with diabetic gastroparesis, treat bowel constipation , AE- long QT syndrome, predispoises to arrhythnmias with erythromycin, ketoconazole, diarrhea
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senna
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stimulant laxative, orally, 8-10 hrs, water and electrolute secretion into bowel, used in combo with docusate, to treat cases of opioid induced constipation
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bisacodyl
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suppositories and enteric coated tablets, potent stimulator of colon, AE- abd cramps and potential atonic colon with prolonged use, don’t take with antacids, could lead to stomac rirrilation and pain
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castor oil
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broken down in small intestine to ricinoleic acid- irritates gut, increases peristalisis, avoid in pregnant pts, stimuates uterine contractions
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methycellulose(citrulcel), psylium seed(metamucil), bran
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bulk laxative, hydrophilic substances(from indigestible parts of fruit and veggies), forms gen in LI causing water retention and intestinal distention, increases peristalitc acitlbity, use with caution in bed bound pts, can cause intestinal obstruction
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bismuth salts
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do not neutralize stomach acids
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Mg citrate, Mg sulfate, Mg phsphate, Mg hydroxide
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nonabsorbale salts that hold water by osmosis and distends bowel by causing stimulation follwoed by defecation
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lactulose
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ostomatic laxative, semysynthetic disacchraide sugar, large doseases- degreaded by colonic bacteria and form lactic, formicand acetic acid which increases osmotic effect, treating hepatoencephalopathy- helps draw out ammonia prevents hyperammonia
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PEG(polyethyl glycol)
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colonic lavage for endoscopic and radiological procedures
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mineral oilds and glycerin suppositories
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lubicrant laxatives, lubicatns aid easy passage of stools
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docusate sodium, docusate calcdium, docusate potassium
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stool softener, surface active agents emulsified with stools to make softer and eaiser passage
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odansteron, graniststron
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antiemetic, 5HT3 receptor blockers in periphery, long duration of action, administer prior to chemotherapy , prolongation of QT wave
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prochorplerazine
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D2 blockers, phenothiazine, low or moderately ematogenic chemotherapy, AE- hypotension, restlessness, dose limiting, extrapyrimidal sympotms and sedation
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metoclorpamide
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D2 antagonist, mixed HT3/HT4 antagonist. antiemetic action due to antagonistic activity at D2 in CTZ resubstituted benzamides with antiemetic acitivity, effective agaisnt cisplatin, AE- antidopinergic side efffects- sedation, diarrhea, extrapyrimidal symtpms, limits its use in high dose , precausitons- inhibitionsaction of DA, should be used with caution in parkinds, uses- diabetic gastroparesis, antiemetic, GERD , high doseases- 5HT3- antiemetic
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lorazapam and alprazolam
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low antiemetic potenticy, benzediapenies, sedative, anxiolytic and amnesic efect, useful for anticipatory vomiting
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droperidol and haloperidok
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antiemetic, butyrophenones that act by blcoksngi D2, doleperiodl- prolongs QT interval, reserved for refractory cases
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dexamethasone and methyprednisolone
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antiemetic, mildly to moderaltey emetogenic chemotherapy, may be due to blockage of prostaglandins AE- insomnia, hyperglycemia- DM
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aprepitant
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blocks neurokinin-1/substance P in brain, administered orally with dexamethasone and palonestron, CYP3A4 metabolism, it can affect the metabolism of other drugs metabolized by this enzyme, can also induce enzyme and affect response with warfarin, shorten half life of the anticoag, AE- constipation and fatigue
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apomorphine and syrup ipecac
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emetics, act by stimualtions CTZ, gastric mucosal irritation and used for accidental poisonings
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diphenoxylate, loperamide
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control diarrhea, opoid like function in gut, activate presynpatic opioid receptros to inhibit Ach release and peristalisis, atropine added to discourage abuse, AE- drowsiness, abd crampls, dizziness, toxic megacolon young children or in pts with severe colitis
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bismuth subsalycylate
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antimcrobial, inhibits acitiiy of pepsin, increases mucus and interacts with glucorptiens in necrotic mucosal tissue to coat and protect ulcer crater antidirrheal, coats intestinal epithelium and decrease GI irritation
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octreotide
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somatostatin derivative, control diarrheas associated with met carcinoid tumors and vasoactive intestinal peptide tumors
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steroids
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ulcerative coilitis and crohns disease , acute cases and to control flares
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sulfasalazine
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sufolonamide derivative, antiinflammatory effect used in UC and CD, prodrug converted into sulfapyridine and 5-ASA in GI , inhibits PGs and LTs
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hyoscyamine, dicylomine
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antispasmodic that helps with cramps or diarrhea
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ursodiol
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aka ursodeoxylic acud(UDCA), secondary bile acid, used for gall stones where risk of surgery is too high, dissolves gallstoes in bile ducks
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celecoxib
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COX 2 selective inhbits, sulfonamide, may caus hypersensitivty(rashes),
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warfarin
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increase bleeding when used with NSAIDs
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NSAID CI
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pregnancy , cat 3 in 1 and 2 trimester, D in trim 3
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aspirin
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irreverible COX inhibitor
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NSAIDS AE
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epigastric distress, prolonged bleeding time, hypersnesitivty , hepatic injury with high doses of salicylcates
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coxibs
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cox 2 inhibitos, analgesic, antipyertic, antiinfl, fewwer GI effects, not cardioprotective, renal toxicity , linked to cardiovascualr thrombotic events , rofecoxib, valdecoxib, etoricoxib not available in US , colexocib only one avail in US
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mexolicam
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not as selective forCox 2 as coxibs
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acetaminophen
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analgesic and antipyertic, mild to moderate pain, DOC for OA, fever and flulike symptoms, short term fever and minor pain in opreg, RA use with other drugs, AE- liver impairment in high dosees , DOC for antipyerisis in children and teens , use acetylcysteine to tx overdose
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methotrexate
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DOC for treatment of RA, lower than for chemo doses, inhibits aminoimidazolecaboxamide ribonucleotide(AICAR) transformylase, AICAR transforlymlase catalyzed the final steps of de novo purine syntehsis-->IMPthymidylate synthase pathway may be invovled, inhibition of AICAR-->acumulation of adenosinde which is an antiinf mediator -->acts of A2b receptor and supresses NFkB indcued by TNF
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cyclophosphamide
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alkylating agents cross link DNA, preventing cell replication, AE0 bone marrow supresion, infertivility, hemoragic cystitis, long term use increases risk of infeciton nad malignancy
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azathioprine
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cytotxic agent-purine antimetabolite, converted to 6-mercaptopurine, inhibits de no vo purine syntehsis, leads to B and T cell supression, and decreased IL2 secretion , AE- xanthine oxidase splits active material to 6- thioruic acid prior to excretion in urine, pts receiving allopurinol for control of hyperuriciemia should have the dose of azathioprine reduced, AE- bone marrow suprression,GI disturbances, infections and malignancies
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cyclosporine
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immunophilin ligand, antifinammatory, forms complex with cyclophilin and immunophilin, complex inhibits calcineurin, which is needed to activate NFAT which induces cytokine, AE- nephrotxicity
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Hydroxychoroquine
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antiinfl, mechanism unknown, antimalarial, used in combo with other drugs, AE- serious effects rare, hemolysis in G6PD pts, retinal damange is rare, opthalmologic exam recomented for those that are high risk(over 60, liver disease, retinal disease), low risk- examine every 5 yrs
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sulfasalazine
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metablized by bacteria in colon, 5-ASA imp for RA, not imp in UC, AE- rash, nausea, vomting, dizziness, HA, leukopenia
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gold sodium thiomalate
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IM, rare due to toxicity
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auranofin
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oral, gold salts taken up by macropahges and supress phagocysosi and lysosomal enxyme, toxicity high, used infreunqcyly
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adalimumab
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anti TNF drug, fully human IgG1 anti-TNF monoclonal antibody, binds to soluble TNF alpha and prevents its interaction with TNF receptors, results in down regulation of macrophage and T cell function. AE- cytopenia(monitor CBC), serious infections, don’t give in pts with active infection, screen for latent TF before, and during tx with this drug
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entanercept
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anti TNF drug, recombinant fusion of two TNF receptors linked to Fc portion of human IgG-1, binds to hyuman TNF alpha , AE- cytopenia(monitor CBC), serious infections, don’t give in pts with active infection, screen for latent TF before, and during tx with this drug
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Inflimiximab
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anti TNF drug, chimeric monochomnal anti TNF alpha anbivoy, binds to hyuman TNF alpha , , AE- cytopenia(monitor CBC), serious infections, don’t give in pts with active infection, screen for latent TF before, and during tx with this drug
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anakinra
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IL-1 receptor antagoinst
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glucocorticoids
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prompt and dramatic but controvversical, use short course before you begin other drug, AE- lots, osteoporosoisi, wt gain , fluid retension, cataracts, poor wound healing, gastric ulcers, GI bleeding, hyperglycemia, hypertension, adrenal supresion, increase risk of infections
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Leflunomide
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cytotoxic agent, combo with methotrexates increases risk of hepaoxitcity, undergo rapid conversion to its active metabolize A77-1726 which inhibits dihydroratate dehydrogenase, leading to lower levels of UMP, arrest in G1 phase, inhibits autoimmune T cell proliferation and production of autoantiboeis by B cells,
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NSAIDS
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first line of treatment for acute gout , but aspirin CI because it comptees with uric acid for organic acid secretion mechanism in proximal tubule
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cholchicine
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binds to tubulin, inhibits its polymerization and prevents formation of microtubues, disrupts granulocytes decreasing migration into affected area, blocks cell fivision by disrupti g mitoic simple, inhibits synthesis and release of lekuotrienes, AE- nausea, vmting, abd pain, diarrhea, myopahty, neutropenia, aplastic anemia, alopecia
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glucocorticoids
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antiinflammantory and immunosuppresive, could be used for acute attack of gout, depot preperatiosn can be injected in site
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allopurinal
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decreases uric acid syn, used for gout, MOA- purine analong, inhibits xanthine oxidase, facilitates dissolution of tophi by lowering uric acid plasma concentration , NSAID or cholichocine given in first 4-6 mo to reduce chance of acute attack of gout AE- hypersnesitivty skin reactions, steven johnson syndrome, drug interactions- with anticanger drug mercaptorine and immunospreasant azathoprine which are also metabolzied by xanthine oxidase, toxic levels of these drugs with coadmin, dose reduction of other drugs
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probenecid and sulfinpyrazone
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enhance uric acid excretion, urate is filtehred,secreted and reabsorbed by kidneys, mediated by specific transporter, transporter exhcnages urate for anion, comptes with urate for transporter and inhibts reabsortion
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probenecid
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do not use with pts with kidney stones or overproduction of uric acid, given with cholcinine or NSAID to prevent acute attac kf gout, AE- mid GI irrtnat, hypersneticit reaction, lots of fluids to avoid kindey stones
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sufinyarzone
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AE- gi irritant, jhypersensity(rash with fever), depression of hemaptoeptisis, don’t use with underlying blood dysciraiss, risk of kidney stoens so take lots of fluids, inhibits warfarn metabolism
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rasburicase
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agents that enhance uric acid metabolsim, oxidizes uric acid to allatoin, a soulbule compound excreted by kineys, in chemo can cause increase in plkasma urate levels due to rapid lysis of tumor cellsand can lead to massive renal injury, exogenous uricase can reduce plasma urate levels and prevent renal damage, can use allupruinor to prevent tumor lysis sytem, a recomb version of aspergillus urincase avail in US
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acetaminophen
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NSAIDs
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use for mild to moderate pain, in inflammatory conditions like arhtiritis and gout
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codeine, hydrocodone, oxycodone, meperidine, propoxyphene, tramadol
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opioids for mild-moderate pain
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morphine, hydromirphine, oxymorphine, levorphanol, fentanyl, sufentanil, methadone
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opidiods for moderate to severe pain
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mepridine
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u receptor agonist, metabolic toxicity, half life of 3h, its metabolite normeperidine has no analgesic properities, has half life of 15-20 hr, AE- tremulousness, dysphoria, myoclonus and seizures , convulsion, refelxes, serotonin syndrome(deilrium, hyperthermia, head ache, hyper or hypotension, rigidity, convulsions, coma, death
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propxyphene
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administered doses that produce little analgesia, dose escalation could lead to norpropoxyphene, renal dysfucntion eledery at risk
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pentazocine, butorphanol, nalbuphine
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mixed opioid agonist-antagonist . Pentacozine and butorphanol can cause psychomimetic effects
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antideperransatns, anticonvulsants, corticosteroids, hydroxyzine, clonidine, lidocaine, capsaicin, caffeine
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analgesic adjunctive agents
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SSRIs
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less effective for enuropathic pain
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TCAs
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can releive neuropathic pain including diabetic neuropathy and postherpetic neuralgia
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carbamazepine
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DOC for trigem neuralgia , anticonvulsant
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gabapentin
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postherpetic neuralagia and diabetic neuropathy, anticonvulsant
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pregabalin
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anticonvulsant ,postherpetic neuralgia, diabetic neuropathy, fibromyalgia
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valproate and topiramate
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anticonvulsant , migraine prophylaxis
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dexamethasone
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DOC out analgesic adjunctive agents
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methadone
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less euphoria and longer duration of action, u receptor agonist, NMDA antagonist, serotonin and NE reuptake inhibitors, detoxification and for maintaince of chronic relapsing heroid addict, AE- QT prolongation, torsades, death
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levomethadyl acetate
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longer half life than methadone, approved for detox clinics
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codeine, oxycodone, and hydrocodone
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less efficanous than morphine, used in combo, CYP2D6
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Dextropropoxyphene
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u agonist, weaker analgesic than codeine, propoxyphe has increased risk of seixures and cardiac conduction abdnomlarities and should be avoided in elderly , mild to moderate agonist
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propoxyphene
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mold to moderate agonsit, half life is 30 hrs, accumulation canlead to toxicity, don’t give routinely, cardiotoxicity, no logner used in US
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tramadol
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mold to moderate agonist, weak u afonist and NE and serootonin reuptake inhibitor, useful for neuropathic pain, increased risk of seizires in pts pts with seizure disorder and those taking medication for lower seizure threshold, serotonin syndrome
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pentazocine butorphanol, nalbuphine, buprenorphine
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mixed agonist antagonist, mixed opiod- agonist-antagonist potent analgesic in opiod naïve pts, precpipate withardwa in people who are physciall depedent on opioid , useful for mild to mod pain, ceiling effect, AE- psychomemtiectic effects with petazocine, butorphanol, nalbuphine
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pentazocine , butorphanol
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k agonist and a u antagonist or partial agonist
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nalbuphine
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k agonist and a u antagonist
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buprenorpihine
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partial u agonsit and k antagonist , approved for mamangement of opioid addiction
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naloxone and naltrexone
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naloxone- tx acute opioid overdose , Naltrexone- opoinoid addition, decreased craving for alcohol in chornic alcoholics
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dextrometoprhan and codine
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antitussives, most effective supression of cough, differ from other opinoids
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diphenoxylate, loperamide
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anitmotility agents, used to tx diarrhea, act by different mechanisms by mu or delta receptros on enetic nerves, epitheial cells and muscle
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