Medchem Exam 4 – Flashcards
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| Digoxin |
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| Lanoxin MOA: inhibits Na/K Pump -> Na gradient is inhibited -> Less Ca is pumped out -> increased Ca in cell -> increased contractility A: less than digitoxin D: PPB less than digitoxin M: kidney E: urine K t1/2: shorter than digitoxin |
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| Inamrinone |
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| Inocor IV MOA: inhibits PDE-3 -> longer CAMP residence -> increased Ca influx -> increased contractility M: directly phase II K t1/2: short |
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| Milrinone |
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| Primacor IV MOA: inhibits PDE-3 -> longer CAMP residence -> increased Ca influx -> increased contractility M: phase I -> phase II K t1/2: longer |
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| Digitoxin |
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| MOA: inhibits Na/K Pump -> Na gradient is inhibited -> Less Ca is pumped out -> increased Ca in cell -> increased contractility A: more than digoxin D: PPB more than digoxin M: liver E: bile -> recycled K t1/2: longer than digitoxin |
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| Dobutamine |
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| Dobutrex MOA: bind B1 stimulating contractility M: COMT & PhaseII |
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| Anti-Arrhythmic Drug Classes |
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| Class I: Phase 0: Na Channel Blockers Class II: Phase 2: Beta Blockers Class III: Phase 3: K Channel Blockers Class IV: CCBs |
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| Class IA Drugs |
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| Quinidine, Procainamide, Diisopyramide MOA: decrease upstroke height; slows rate of depol -> prolonged axn potential ADRs: anticholinergic effects |
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| Class IB Drugs |
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| Lidocaine, Tocainamide, Mexilitene, Phenytoin MOA: decrease upstroke height; increases rate of depol -> shortened axn potential ADRs: anticholingergic effects |
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| Quinidine |
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| Quinalan PO/IM Class IA Antiarrhythmic ADR: cinchonism M: O-demethylation |
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| Procainamide |
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| Pronestyl PO Class IA Antiarrhythmic M: amidases (benzaldehyde amide) long k t1/2, N-deethylation, PHASE II ACETYLATION* |
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| Diisopyramide |
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| Norpace PO Class IA Antiarrhythmic M: aromatic hydroxylation |
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| Lidocaine |
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| Xylocaine PO Class IB Antiarrhythmic M: amidases (anilino amide) short k t1/2 |
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| Tocainide |
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| Tonocard IV/PO Class IB Antiarrhythmic M: amidases (anilino amide) but sterically hindered long k t1/2 |
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| Mexilitene |
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| Mexitil IV/PO M: long k t1/2 No anticholinergic ADRs |
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| Phenytoin |
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| Dilantin IV/PO Class IB Antiarrhythmic *only acidic antiarrhythmic (imide) used in seizures M: aromatic hydroxylation |
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| Class IC Drugs |
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| Propaphenone, Moracizine, Fleicanide, Encainide MOA: decrease upstroke height; no effect on length of axn potential |
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| moracizine |
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| Ethmozine PO K Channel Affin: basic N heterocycle ADR: anticholindergic |
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| propaphenone |
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| Rhythmol PO K Channel Affin: aromatic ketone |
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| flecainide |
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| Tambocor PO K Channel Affin: aromatic ketone ADR: anticholinergic |
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| encainide |
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| Enkaid PO K Channel Affin: aromatic ketone |
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| Class II Drugs |
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| sotalol MOA: block autonomic NS stimulation @ B1 (phase 2) |
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| sotalol |
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| Betapace IV/PO Class II & Class III antiarrhythmic *also blocks Na *conatins methyl sulfonamino group for CIII |
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| Class III Drugs |
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| sotalol, ibutilide, dofetilide, amiodarone, dronedarone, bretylium tosylate MOA: inhibit K efflux (phase 3) -> longer axn potential |
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| ibutilide |
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| Corvert IV Class III antiarrhythmic *contains necessary methyl sulfonamino *also blocks Na |
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| dofetilide |
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| Tikosyn PO Class III antiarrhythmic *contains two methyl sulfonamino |
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| amiodarone |
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| Cordarone IV/PO Class III antiarrythmic *contains aromatic ketone for K channel affin ADR: decreased TH production (due to 2 iodine) |
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| dronaderone |
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| Multaq PO Class III antiarrhythmic very selective: contains aromatic ketone & methyl sulfonamido |
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| bretylium tosylate |
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| IV ADR: severe hypotension |
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| Class IV Drugs |
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| Diltiazem, Verapamil |
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| Coagulation Cascade |
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| Injury Epithelium releases thromboplastin *synthesis of prothrombin is coupled with oxidation of reduced vitamin K Prothrombin -> thrombin Fibrinogen -> fibrin Fibrin binds GPIIb&IIIa Conformation Change -> P2Y12 receptor available ADP Binds P2Y12 -> platelet becomes sticky Termination: AT3 binds thrombin to inactivate; accelerated by heparin binding |
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| 8 Anticoagulant Drug Classes |
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| Heparin & d/dx Vit K Reductase Inhibs Thrombin Antags Ab for Platelets Fibrinogen Antags PDEis Proteolytic Enz Inhibs Prostaglandins |
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| Heparin |
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| IV MOA: increase deactivation of thrombin via binding AT3 & thrombin -> decrease fibrin OOA: Fast acting Chem: gluconic acid & glucosamine repeating units antidote: protamine sulfate |
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| Vitamin K Reductase Inhibitors |
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| PO MOA: blocks reduction of oxidized Vitamin K -> prothrombin not made OOA: slow acting A: lipophilic -> good D: strong PPB M: aromatic hydroxylase (cyp) antidote: vitamin K (slow acting) |
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| Warfarin |
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| Coumadin Vit K Reductase Inhib |
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| acenocoumarol |
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| Sintrom Vit K Reductase Inhib |
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| phenprocoumon |
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| Marcumar Vit K Reductase Inhib |
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| bishydroxycoumarin |
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| Vit K Reductase Inhib |
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| dicoumarol |
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| Vit K Reductase Inhib dimer |
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| Thrombin Inhibitors |
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| IV "Rudins" MOA: bind & inhibit thrombin (resemble AT3 structure) |
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| Antibody Against Platelets |
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| MOA: Antibody against GPIIb/IIIa; antagonist to fibrinogen |
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| Abciximab |
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| Repopro IV Antibody against platelets |
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| Fibrinogen Antagonists |
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| 1)Polypeptides IV MOA: similar to fibrinogen; defebrutide 2)Nonpeptides PO a)MOA: bind GPIIb/IIIa directly b)MOA: bind purinergic P2Y12 receptor (inhibit ADP) |
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| Aspirin/ASA |
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| Advil, Motrin PO Nonpeptide fibrinogen antagonist MOA: acetylates GPIIb/IIIa irreversibly |
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| tirofiban |
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| Aggrostat IV Nonpeptide fibrinogen antagonist MOA: binds GPIIb/IIIa receptor contains tryptophan |
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| clopridogrel |
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| Plavix PO P2Y12 fibrinogen antagonist k t1/2: shorter than ticlopidine b t1/2: longer than ticlopidine (active metabolites) |
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| ticlopidine |
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| Ticlid PO P2Y12 fibrinogen antagonist k t1/2: longer than clopridogrel b t1/2: shorter than clopridogrel |
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| Proteolytic Enzyme Inhibitors |
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| MOA: Inhibits thrombin's cleavage of fibrinogen (-> fibrin) |
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| Defibrotide |
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| Peptide Fibrinogen Antagonist |
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| Nafamostat |
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| HCl Salt IV Proteolytic Enz Inhib Uses: during hemodialysis M: Esterases (must be continuously infused) |
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| Prostaglandin (PG) Synth |
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| Arachidonic Acid (20C w/4pi bonds) cleaved from PL memb via phospholipase -> enters cytosol -> COX -> 5-memb ring + 2 pi bonds (PGE2, PGF2) |
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| PGE2 Uses |
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| *smooth muscle dilation anti-HTN for PAH anti-ulcer -> mucin secretion induce labor -> relax circular cervix muscle induce menstruation induce abortion (RU486) anti-asthma nasal spray |
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| PGF2 Uses |
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| *smooth muscle contraction post-partum bleeding -> vasoconstriction induce labor -> contract uterus & contract radial cervix |
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| PGI2 (Prostacyclin) Uses |
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| Open heart surgery -> inhibit blood clotting & dilate vessels |
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| TXA Uses |
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| after surgery -> induce platelet aggregation to stop bleeding |
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| PGE2 Structure |
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| cyclopentane w/ketone + 7C A chain (pi@5,6) + 8C B chain (pi@13,14) |
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| PGF2 Structure |
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| cyclopentane w/chiral OH + 7C A chain (same direction as OH) (pi@5,6) + 8C B Chain (pi@13,14) |
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| PGI2 Structure |
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| cyclopentane+furan + 5C A chain (pi@5,6) + 8C B chain (pi@13,14) |
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| TXA2 Structure |
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| Pyran Backbone + 7C A chain (pi@5,6) + 8C B chain (pi@13,14) |
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| Montelukast |
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| Singulair PO Leukotriene Antagonist Bronchodilation |
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| Antipyretic Analgesic Drug Classes |
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| Salicylates & Anilines |
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| aspirin |
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| Salicylate Antipyretic Analgesic |
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| diflunisal |
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| Dolobid Salicylate Antipyretic Analgesic |
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| methylsalicylate |
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| Bengay Salicylate Antipyretic Analgesic |
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| acetaminophen |
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| Tylenol Aniline Antipyretic Analgesic M: oxidized to NAPQI -> reactive with any -SH (glutathione) -> toxicity Antidote: Mesna releases glutathiones |
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| NSAID structure |
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| similar to arachidonic acid: lipophilic tail + acidic head |
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| NSAID Drug Classes |
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| fenamates, acetic acid d/dx, propionic acid d/dx, enoic acid d/dx, misc :) |
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| mefenamic acid |
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| Ponstel fenamate NSAID |
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| meclofenamic acid |
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| Meclomen fenamate NSAID |
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| indometacin |
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| Indocin acetic acid NSAID ADR: serious HA/dizzy due to CNS affinity |
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| sulindac |
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| Clinoril -- PRODRUG acetic acid NSAID contains sulfoxide (too polar) -> sulfide (lipo) long t 1/2 |
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| zomeprac |
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| Zomax acetic acid NSAID |
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| etodolac |
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| Lodine acetic acid NSAID |
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| NSAID ADME & ADR |
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| A: good oral absorption D: high PPB M: Phase 1 -> inactive metabolite (too polar to bind COX) E: Phase II glucoronide in urine ADR: ulcerogenic bc acid & mucin inhibition |
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| ibuprofen |
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| Motrin, Advil Propionic acid NSAID |
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| naproxen |
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| Naprosyn/Aleve propionic acid NSAID long t 1/2 |
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| peroxicam |
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| Feldene enoic acid NSAID *contains sulfonamide -> directly Phase II *longest t 1/2 :) |
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| nabumetone |
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| Relafen -- PRODRUG miscellaneous NSAID ketone -> acid *avoids stomach irritation :) |
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| celecoxib |
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| Celebrex miscellaneous NSAID -- Cox2 Selective *minimized ulcer risk *contains sulfonamide -> longest t 1/2 |
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| Anti-Gout Drug Classes |
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| Inhibitors of WBC Maturation; Xanthine Oxidase Inhibitors; Uricosuric Agents |
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| cochicine |
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| Colcrys WBC Maturation Inhibitor |
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| allopurinol |
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| Zyloprim XO Inhibitor Nitrogens are simply closer together |
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| probenacid |
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| Probalan Uricosuric MOA: prevent proximal tubule reabsorp of uric acid *contains sulfonamide -> goes directly to SOA |
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| sulfinpyrazone |
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| Anturane Uricosuric MOA: prevent proximal tubule reabsorp of uric acid |
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