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231 Cards in this Set
- Front
- Back
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Question
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Answer
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Cyclosporine
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Binds to cyclophilins. Complex blocks differentiation and activation of T-cells by inhibiting calcineurin, thus preventing production of IL-2 and its receptor
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Tacrolimus (FK506)
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Like cyclosporine; binds to FK binding protein, inhibiting secretion of IL-2 and other cytokines
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Azathioprine
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Antimetabolite precursor of 6-mercaptopurine that interferes with the metabolism and synthesis of nucleic acids
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Muromonab-CD3 (OKT3)
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Monoclonal Antibody that binds to CD3 on T-cell surface. Blocks cellular interaction with CD3 protein responsible for T-cell signal transduction
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Sirolimus
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Binds to mTOR. Inhibits T-cell proliferation in response to IL-2
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Mycophenolate motefil
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inhibits de novo guanine synthesis; block lymphocyte proliferation
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daclizumab
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mAb with high affinity for IL-2R on activated T-cells
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Heparin
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cofactor for activation of antithrombin III. Decreases thrombin and Xa. Short half-life
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LMW heparin
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acts more on Xa, longer half-life
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Lepirudin bivalirudin agrotroban
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directly inhibit thrombin
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Warfarin
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interferes with gamma carboxylation and synthesis of vitamin K dependent clotting factors 2,7,9,10 and anticoagulation factors Protein C, S. Metabolized by cytoP450. Long half life
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Streptokinase Urokinase tPA(alteplase) anistreplase
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Aid conversion of plasminogen to plasmin, which cleaves thrombin and fibrin clots. Increases PT, PTT, no change in platelet count
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Aspirin
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Acetylates and irreversibly inhibits COX to prevent conversion of AA to TXA2 . Increases BT. No effect on PT, PTT.
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Clopidogrel Ticlopidine
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inhibit platelet aggregation by irreversibly blocking ADP receptors. Inhibit fibrinogen binding by preventing Glycoprotein 2b/3a expression.
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Abciximab
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mAb that binds to gp2b/3a receptor on activated platelets, preventing aggregation
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Methotrexate
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Folic acid analog. Inhibits dihydrofolate reductase. Decreases dTMP, DNA, protein synthesis
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5-Flurouracil (5-FU)
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Pyrimidine analog. Activated to 5F-dUMP, which covalently complexes folic acid. This complex inhibits thymidylate synthase leading to decreased dTMP, DNA, and protein synthesis
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6-Mercaptopurine (6-MP)
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Purine analog. Decrease de novo purine synthesis. Activated by HGPRTase
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6-thioguanine (6-TG)
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Same as 6-MP
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Cytarabine
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Pyrimidine antagonist. Inhibition of DNA polymerase
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Dactinomycin (Actinomycin D)
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intercalates in DNA
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doxorubicin (adriamycin) daunorubicin
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generates free radicals. Noncovalently intercalates in DNA and causes DNA breaks and decreased replication
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Bleomycin
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G2 phase specific. Induces free radicals which cause breaks in DNA strands
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Etoposide Teniposide
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Late S to G2 phase specific. Inhibits DNA topo 2 leading to increased DNA degradation
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Cyclophosphamide ifosphamide
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Covalently X-link DNA at guaning N-7. Require bioactivation by liver.
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Nitrosoureas - Carmustine Lomustine Semustine Streptozocin
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Require bioactivation. Cross BBB into CNS
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Busulfan
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Alkylates DNA
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Vincristine Vinblastine
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bind to tubulin in M phase and block polymerization of microtubules so that the mitotic spindle can't form.
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Paclitaxel
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hyperstabilize polymerized microtubules in M phase so that mitotic spindle cannot break down (preventing anaphase).
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Cisplatin Carboplatin
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Cross links DNA
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Hydroxyurea
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Inhibits Ribonucleotide Reductase - decreases DNA synthesis. S-phase specific
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Tamoxifen Raloxifene
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SERM - receptor antagonist in breast, agonists in bone; block binding of estrogen to ER+ cells
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Trastuzumab (Herceptin)
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mAb against HER-2 (erb-B2). Kills breast cancer that overexpress HER-2, possibly through antibody dependent cytotoxicity
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Imatinib (Gleevec)
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Philadelphia chromosome bcr-abl tyrosine kinase inhibitor
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Bethanecol
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Muscarinic Agonist. Activates Bowel and Bladder smooth muscle
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Carbachol
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Muscarinic Agonist
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Pilocarpine
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Muscarinic Agonist. Potent stimulator of sweat, tears, and saliva
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Methacholine
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Muscarinic agonist
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Neostigmine
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increases endogenous Ach; no CNS penetration.
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Pyridostigmine
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increases endogenous Ach; increases strength; no CNS penetration; long-acting
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Edrophonium
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increases endogenous Ach; extremely short-acting
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Physostigmine
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increases endogenous Ach; Crosses BBB
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Echothiophate
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increases endogenous Ach
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Atropine
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muscarinic antagonist
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homatropine tropicamide
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muscarinic antagonist
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benztropine
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muscarinic antagonist
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scopolamine
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muscarinic antagonist
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ipratropium
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muscarinic antagonist
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oxybutynin glycopyrrolate
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muscarinic antagonist
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metscopolamine pirenzepine propanetheline
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muscarinic antagonist
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Hexamethonium
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nicotinic antagonist (ganglionic blocker)
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Epinephrine
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a1, a2, B1, B2 agonists. Low doses selective for B1
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Norepinephrine
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a1, a2 > B1 agonists.
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Isoproterenol
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B1 = B2 agonist
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Dopamine
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D1 = D2 > B > a
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Dobutamine
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B1 > B2
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Phenylephrine
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a1 > a2
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Metaproterenol albuterol salmeterol terbutaline
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B2 > B1
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Ritrodine
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B2
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Amphetamine
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releases stored catecholamines
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Ephedrine
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releases stored catecholamines
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cocaine
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catecholamine uptake inhibitor
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Clonidine alpha-methyldopa
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centrally acting a2 agonist
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Phenoxybenzamine (irreversible); Phentolamine (reversible)
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nonselective alpha blockers
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Prazosin Terazosin Doxazosin
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a1 blockers
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Mirtazapine
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a2 blocker
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Propranolol Timolol Nadolol Pindolol
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nonselective beta blockers (pindolol is partial B Ag at high levels)
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Acebutolol Betaxolol Esmolol Atenolol Metoprolol
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B1 > B2 blocker; (acetbutolol is a partial B Ag, esmolol is short-acting)
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Carvedilol Labetalol
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nonselective alpha and beta blockers
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Hydralazine
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increases cGMP which leads to smooth muscle relaxation
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Minoxidil
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potassium channel opener - hyperpolarizes and relaxes vascular smooth muscle
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Nifedipine Verapamil Diltiazem
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Block voltage-gated L-type potassium channels of cardiac and smooth muscle and thereby reduce muscle contractility
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Nitroglycerin, Isosorbide dinitrate
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Vasodilate by releasing NO in smooth muscle, causing increased cGMP and smooth muscle relaxation. Dilate veins>>arteries. Decrease preload.
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Nitroprusside
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Short acting. Increase cGMP via direct release of NO. Can cause cyanide toxicity
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Fenoldopam
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Dopamine D1 receptor agonist-relaxes renal vascular smooth muscle
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Diazoxide
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Potassuim Channel Opener-hyperpolarizes and relaxes vascular smooth muscle
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Nitrates, B-Blockers, Calcium Channel Blockers
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Nitrates and Nifedipine decrease preload. B-Blockers and Verapamil decrease afterload.
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Digoxin
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Direct inhibition of Na/K ATPase leads to indirect inhibition of Na/Ca exchanger antiport. Increases intracellular calcium leading to positive inotropy. Stimulates vagus nerve
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Quinidine Procainamide Disopyramide
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Na channel blocker. Increases ERP and QT interval.
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Lidocaine Mexilitine Tocainide Phenytoin
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Na channel blocker. Decrease AP duration. Preferentially affect ishemic or depolarized Purkinje and ventricular tissue.
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Flecainide Encainide Propafenone
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Na channel blocker. No effect on AP duration.
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Propranolol Esmolol Metoprolol Atenolol Timolol
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B-Blockers. Decrease cAMP, decrease Ca currents. Supress abnormal pacemakers by decreased slope of phase 4. AV node particularly sensitive - increases PR interval. Esmolol is very short acting
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Sotalol Ibutilide Bretylium Dofetilide Amiodarone
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Block K channels. Increase AP duration, increase ERP. Increases QT interval. Amiodarone has class I, II, III, and IV effects because it alters the lipid membrane.
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Verapamil Diltiazem
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Ca-channel blocker. Primarily affect AV nodal cells. Decreases conduction velocity, increases ERP, increases PR interval
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Adenosine
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Causes K efflux from cell, hyperpolarizing the cell and decreasing intracellular Ca. Very short acting.
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Potassium
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Depresses ectopic pacemakers in hypokalemia
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Magnesium
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Lovastatin Pravastatin Simvastatin Atorvastatin Rosuvastatin
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Inhibits cholesterol precursor, mevalonate. HMG CoA reductase inhibitors
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Niacin
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inhibits lipolysis in adipose tissue; reduces hepatic VLDL secretion into cirulation
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Cholestyramine Colestipol Colesevelam
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Bile acid resins. Prevents intestinal reabsorption of bile acids; liver must use cholesterol to make more
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Ezetimibe
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Cholesterol absorption blocker. Prevents cholesterol reabsorption at small intestine brush border
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Gemfibrozil Clofibrate Bezafibrate Fenofibrate
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Upregulate Lipoprotein Lipase, increasing TAG clearance
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Cimetidine Ranitidine Famotidine Nizatidine
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Reversible block of histamine H2 receptors leading to decreased H+ (proton) secretion by parietal cells
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Omeprazole Lansoprazole
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Proton pump inhibitors. Irreversibly inhibit H/K ATPase in stomach parietal cells
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Bismuth Sucralafate
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Bind to ulcer base, providing physical protection and allowing bicarb secretion to reestablish pH gradient in the mucous layer
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Misoprostol
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PGE1 analog. Increase production of gastric mucous barrier, decreases acid production
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Pirenzepine Proprantheline
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Muscarinic Antagonists. Block M1 receptors on ECL cells (decrease histamine secretion) and M3 receptors on parietal cells (decrease H+ secretion)
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Aluminum OH
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Antacid. Affects absorption, bioavailability of other drugs by altering gastric pH or by delaying gastric emptying
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Magnesium OH
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Antacid. Affects absorption, bioavailability of other drugs by altering gastric pH or by delaying gastric emptying
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Calcium Carbonate
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Antacid. Affects absorption, bioavailability of other drugs by altering gastric pH or by delaying gastric emptying
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Infliximab
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mAb to TNF
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Sulfasalazine
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combination of slufapyridine (antibacterial) and 5-aminosalicylic acid (anti-inflammatory). Activated by colonic bacteria
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Ondasetron
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5-HT3 antagonist. Powerful central-acting antiemetic
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Metoclopramide
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D2 receptor antagonist. Increase resting tone, contractility, LES tone, motility. Does not influence colon transport time
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Lispro (SA) Aspart (SA) Regular (SA) NPH (IA) Glargine (LA) Detemir (LA)
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Bind insulin receptor. Liver: increase glucose stored as glycogen. Muscle: increases glycogen and protein synthesis, and potassium uptake. Fat: aids TAG storage
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Tolbutamide Chlorpropamide
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1st gen sulfonylureas. Close K channel in B-islet cell membrane, depolarizing cell and triggering insulin release via increased Ca influx
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Glyburide Glimepiride Glipizide
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2nd gen sulfonylureas. Close K channel in B-islet cell membrane, depolarizing cell and triggering insulin release via increased Ca influx
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Metformin
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Biguanide. Possibly decreases gluconeogenesis, increases glycolysis, decreases serum glucose levels. Insulin sensitizer
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Pioglitazone Rosiglitazone
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increase insulin sensitivity in peripheral tissue
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Acarbose Miglitol
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Inhibit intestinal brush border alpha-glucosidases. Delayed sugar hydrolysis and glucose absorption leads to decreased postprandial hyperglycemia
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Pramlintide
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decreases glucagon
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Exenatide
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GLP-1 mimetic: increases insulin and decreases glucagon release
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Orlistat
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alters fat metabolism by inhibiting pancreating lipases
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Sibutramine
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Sypmathomimetic serotonin and norepinephrine reuptake inhibitor
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Propylthiouracil
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inhibit organification of iodide and coupling of thyroid hormone synthesis. Also decreases peripheral conversion of T4 to T3
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Methimazole
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inhibit organification of iodide and coupling of thyroid hormone synthesis
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Levothyroxine Triiodothyronine
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thyroxine replacement
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Demeclocycline
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ADH antagonist
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Hydrocortisone Prednisone Triamcinolone Dexamethasone Beclomethasone
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Glucocorticoids. Decreases the production of leukotrienes and prostaglandins by inhibiting phospholipase A2 and expression of COX-2
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Aspirin
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Irreversibly inhibits COX by covalent bonding, which decreases synthesis of both thromboxane and prostaglandins
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Ibuprofen Naproxen Indomethacin Ketorolac
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NSAIDs. Reversibly inhibit COX. Blocks prostaglandin synthesis.
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Celecoxib
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Selective COX-2 inhibitor. Reversibly inhibits COX-2, which is found in inflammatory cells and vascular endothelium and mediates inflammation and pain. Spares COX-1 which helps maintain the gastric mucosa.
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Acetaminophen
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Reversibly inhibits COX, mostly in CNS. Inactivated peripherally
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Etidronate Pamidronate Alendronate Risedronate
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Bisphosphonates. Inhibits osteoclastic activity; reduces both formation and resorption of hydroxyapatite
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Colchicine
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Binds and stabilizes tubulin to inhibit polymerization, impairing leukocyte chemotaxis and degranulation.
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Probenecid
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Inhibits reabsorption of uric acid in PCT (also inhibits secretion of penicillin)
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Allopurinol
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Inhibits xanthine oxidase. Decreases conversion of xanthine to uric acid.
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Etanercept
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Recombinant form of human TNF receptor that binds TNF
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Infliximab
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Anti-TNF antibody
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Adalimumab
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Directly binds TNF-a receptor sites
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Epinephrine
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alpha agonist. Decreases aqueous humor due to vasoconstiction
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Brimonidine
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alpha agonist. Decreases aqueous humor synthesis
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Timolol Betaxolol Carteolol
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beta blockers. Decreases aqueous humor secretion
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acetazolamide
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decreases aqueous humor secretion due to decreased bicard via inhibition of carbonic anhydrase
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Pilocarpine Carbachol
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Direct cholinomimetics. Contract ciliary muscle and open trabecular meshwork
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Physostigmine Echothophate
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Indirect cholinomimetics. Contract ciliary muscle and open trabecular meshwork
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Latanoprost
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PGF-2a. Increases outflow of aqueous humor
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Morphine Fentanyl Codeine Heroin Methadone Meperidine
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Acts as agonists at opioid receptors to modulate synaptic transmission. Opens K channels and closes Ca channels leading to decreased synaptic transmission. Inhibit release of Ach, NE, 5-HT, glutamate, and substance P.
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Dextromorphan
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Opioid agonist
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Loperamide Diphenoxylate
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Opioid agonist
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Butorphanol
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Agonist at kappa receptors. Partial Agonist at mu receptors
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Tramadol
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Weak opioid agonist. Inhibits serotonin and NE reuptake
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Phenytoin
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Use-dependent blockade of Na channels; Increases refractory period; inhibits glutamate release from excitatory presynaptic neuron
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Carbamazepine
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Increases Na channel inactivation (similar to phenytoin
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Lamotrigine
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Blocks voltage gated Na channels
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Gabapentin
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GABA analog, but primarily works by inhibiting HVA calcium channels
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Topiramate
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Blocks Na channels, increases GABA action
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Phenobarbital Pentobarbital Thiopental Secobarbital
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Barbituates. Facilitate GABAa action by increasing duration of Cl channel opening, thus decreasing neuron firing
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Diazepam Lorazepam Chlordiazepoxide Midazolam Alprazolam Triazolam Temezepam Oxazepam
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Benzodiazepines. Facilitate GABAa action by increasing frequency of Cl channel opening. Decreases REM sleep.
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Valproic Acid
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Increases Na channel inactivation, increases GABA concentration
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Ethosuximide
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Blocks thalamic T-type Ca channels
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Tiagabine
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Inhibits GABA reuptake
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Vigabatrin
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Irreversibly inhibits GABA transaminase, increasing GABA
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Levetiracetam
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unknown. May modulate GABA and glutamate release
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Halothane Enflurane Isoflurane Sevoflurane Methoxyflurane Nitrous Oxide
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Mechanism unknown.
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Thiopental
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Barb. High potency, high lipid solubility. Effect terminated by rapid redistribution into tissue and fat.
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Midazolam
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Benzo.
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Ketamine
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PCP analog. Blocks NMDA receptors.
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Morphine Fentanyl
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opiates
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Propofol
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Potentiates GABAa.
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Procaine Cocaine Tetracaine Lidocaine Mepivacaine Bupivacaine
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Block Na channels by binding to specific receptors on inner portion of channel. Preferentially bind to activated Na channels, so most effective in rapidly firing neurons
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Succinylcholine
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Depolarizing neuromuscular blocker. Selective for motor nicotinic receptor.
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Tubocurarine Atracurium Mivacurium Pancuronium Vecuronium Rocuronium
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Nondepolarizing neuromuscular blocker. Competes with Ach for receptors
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Dantrolene
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Prevents the release of Ca from sarcoplasmic reticulum of skeletal muscle
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Bromocriptine Pergolide Pramiprexole Ropinirole
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Agonize dopamine receptors. Pergolide is an ergot and a partial agonist. Ropinirole in a non-ergot. Non-ergots are preferred
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Amantadine
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Increases Dopamine release
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L-dopa/carbidopa
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Increases dopamine in CNS. L-dopa can cross BBB and is converted by dopa decarboxylase in the CNS to dopamine.
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Selegiline
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Selective MAO type B inhibitor, which preferentially metabolizes Dopamine over NE and 5-HT. Prevents pre-synaptic dopamine breakdown
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Entacapone Tolcapone
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COMT inhibitors. Prevents post-synaptic L-dopa degradation, thereby increasing dopamine availability
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Benztropine
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Antimuscarinic. Curbs excess cholinergic activity
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Memantine
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NDMA receptor antagonist; helps prevent excitotoxicity (mediated by Ca)
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Donepozil Galantamine Rivastigmine
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Acetylcholinesterase inhibitors
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Reserpine Terbenazine
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Amine depletors
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Haloperidol
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dopamine receptor antagonist
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Sumatriptan
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5-HT 1B/1D agonist. Causes vasoconstriction, inhibition of trigeminal activation and vasoactive peptide release.
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Methylphenidate (Ritalin)
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increase presynaptic NE vesicular release (similar to amphetamines)
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Haloperidol Trifluoperazine Fluphenazine Thioridazine Chlorpromazine
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Typical antipsychotics. Block D2 receptors. Increase cAMP.
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Olanzapine Clozapine Quetiapine Risperidone Aripiprazole Ziprasidone
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Atypical antipsychotics. Block 5-HT2, alpha, H1, and dopamine receptors.
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Lithium
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possibly inhibits phosphoinositol cascade
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Buspirone
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Stimulates 5-HT-1a receptors
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Imipramine Amitriptyline Despiramine Nortriptyline Clomimpramine Doxepin Amoxapine
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Tricyclic Antidepressants. Block reuptake of NE AND serotonin.
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Fluoxetine Paroxetine Sertraline Citalopram
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SSRI.
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Venlafaxine Duloxetine
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Inhibit serotonin and NE reuptake
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Phenelzine Tranylcypromine Isocarboxazid Selegiline (selective for MAO-B)
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inhibits MAO leading to increased levels of amine neurotransmitters
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Bupropion
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Atypical antidepressant. Increases NE and dopamine via unknown mechanism.
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Mirtazapine
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a2 antagonist increases NE and serotonin release. Potent 5-HT2 and 5-HT3 antagonist
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Maprotiline
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Blocks NE reuptake
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Trazodone
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Primarily inhibits serotonin reuptake.
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Mannitol
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Osmotic diuretic. Increases tubular fluid osmolarity, producing increased renal flow
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Acetazolamide
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Carbon anhydrase inhibitor. Causes self-limited NaHCO3 diuresis and reduction in total-body HCO3 stores
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Furosemide
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Sulfonamide loop diuretic. Inhibits Na/K/2Cl cotransporter of thick ascending limb. Abolishes hypertonicity of medulla, preventing concentration of urine
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Ethacrynic acid
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phenoxyacetic acid derivative (not a sulfonamide). Essentially same action as furosemide
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Hydrochlorothiazide
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Thiazide diuretic. Inhibits NaCl reabsorption in early distal tubule, reducing diluting capacity of the nephron. Decreases Ca excretion
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Spironolactone Eplerenone
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Potassium Sparing Diuretics. Competetive aldosterone receptor antagonist in the cortical collecting tubule
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Triamterene Amiloride
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Potassium Sparing Diuretic. Block Na channels in the cortical collecting tubule
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Captopril Enalapril Lisinopril
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ACE inhibitors. Reduce levels of angiotensin II and prevent inactivation of bradykinin, a potent vasodilator. Increases renin release
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Leuprolide
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GnRH analog with agonist properties when used in pulsatile fashion; antagonist when used in continuos fashion.
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Testosterone
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Agonist at androgen receptors
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Finasteride
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Antiandrogen. 5-alpha reductase inhibitor, decreasing conversion of testosterone to DHT.
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Flutamide
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Antiandrogen. Nonsteroidal competitive inhibitor of androgens at the testosterone receptor.
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Ketoconazole
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Antiandrogen. Inhibits desmolase, inhibiting steroid synthesis
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Spironolactone
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Antiandrogen. Inhibits steroid binding
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Ethinyl estradiol DES Mestranol
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Bind estrogen receptors
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Clomiphene
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SERM. Partial agonis at estrogen receptors in hypothalamus. Prevents normal feedback inhibition and increases release of LH an FSH from pitiutary, which stimulates ovulation.
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Tamoxifen
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SERM. Antagonist in breast tissue
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Raloxifene
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SERM. Agonist on bone. Reduces resorption of bone
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Estrogen Progesterone
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Hormone replacement therapy
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Anastrozole Exemestane
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Aromatase inhibitors
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Progestins
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Bind progesterone receptors, reduce growth and increase vascularization of endometrium
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mifepristone (RU-486)
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competitive inhibitor of progestins at progesterone receptors
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Dinoprostone
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PGE2 analog; causes cervical dilation and uterine contraction
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Ritodrine Terbutaline
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B2 agonists that relax the uterus;
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Tamsulosin
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a1 antagonist; inhibits smooth muscle contration. Selective for a1A,D receptors in prostate
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Sildenafil Vardenafil
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inhibit cGMP phosphodiesterase, causing increased cGMP, smooth muscle relaxation in corpus cavernosum, increased blood flow, and penile erection
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Diphenhydramine Dimenhydrinate Chlorpheniramine
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1st gen antihistamine. Reversible inhibitors of H1 histamine receptors
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Loratidine Fexofenadine Desloratadine Cetirizine
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2nd gen antihistamines. Reversible inhibitors of H1 histamine receptors
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Guaifenesin
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expectorant.
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N-acetylcysteine
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expectorant. Mucolytic - reduces intermolecular disulfide bridges
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Bosentan
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Competitively antagonizes endothelin-1 receptors, decreasing pulmonary vascular resistance
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Isoproterenol
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nonspecific B-agonist. Relaxes bronchial smooth muscle (B2).
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Albuterol
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B2 agonist. Relaxes bronchial smooth muscle (B2).
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Salmeterol
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B2 agonist. Relaxes bronchial smooth muscle (B2).
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Theophylline
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Methylxanthine. Causes bronchodilation by inhibiting phosphodiesterase, thereby reducing cAMP hydrolysis
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Ipratropium
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Muscarinic antagonist. Competitively blocks muscarinic receptors, preventing bronchoconstriction
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Cromolyn
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Prevents release of mediators from mast cells.
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Beclosmethasone Prednisone
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corticosteroids. Inhibits the synthesis of virtually all cytokines. Inactivates NF-kB, the transcription factor that induces the production of TNF-a, among other inflammatory agents.
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Zileuton
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Antileukotriene. A 5-LOX pathway inhibitor. Blocks conversion of arachidonic acid to leukotrienes
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Montelukast Zafirlukast
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Antileukotriene. Blocks leukotriene receptors.
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