ALL THE DRUGS Flashcards
Cyclosporine
Binds to cyclophilins. Complex blocks differentiation and activation of T-cells by inhibiting calcineurin, thus preventing production of IL-2 and its receptor
Tacrolimus (FK506)
Like cyclosporine; binds to FK binding protein, inhibiting secretion of IL-2 and other cytokines
Azathioprine
Antimetabolite precursor of 6-mercaptopurine that interferes with the metabolism and synthesis of nucleic acids
Muromonab-CD3 (OKT3)
Monoclonal Antibody that binds to CD3 on T-cell surface. Blocks cellular interaction with CD3 protein responsible for T-cell signal transduction
Sirolimus
Binds to mTOR. Inhibits T-cell proliferation in response to IL-2
Mycophenolate motefil
inhibits de novo guanine synthesis; block lymphocyte proliferation
daclizumab
mAb with high affinity for IL-2R on activated T-cells
Heparin
cofactor for activation of antithrombin III. Decreases thrombin and Xa. Short half-life
LMW heparin
acts more on Xa, longer half-life
Lepirudin bivalirudin agrotroban
directly inhibit thrombin
Warfarin
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
Streptokinase Urokinase tPA(alteplase) anistreplase
Aid conversion of plasminogen to plasmin, which cleaves thrombin and fibrin clots. Increases PT, PTT, no change in platelet count
Aspirin
Acetylates and irreversibly inhibits COX to prevent conversion of AA to TXA2 . Increases BT. No effect on PT, PTT.
Clopidogrel Ticlopidine
inhibit platelet aggregation by irreversibly blocking ADP receptors. Inhibit fibrinogen binding by preventing Glycoprotein 2b/3a expression.
Abciximab
mAb that binds to gp2b/3a receptor on activated platelets, preventing aggregation
Methotrexate
Folic acid analog. Inhibits dihydrofolate reductase. Decreases dTMP, DNA, protein synthesis
5-Flurouracil (5-FU)
Pyrimidine analog. Activated to 5F-dUMP, which covalently complexes folic acid. This complex inhibits thymidylate synthase leading to decreased dTMP, DNA, and protein synthesis
6-Mercaptopurine (6-MP)
Purine analog. Decrease de novo purine synthesis. Activated by HGPRTase
6-thioguanine (6-TG)
Same as 6-MP
Cytarabine
Pyrimidine antagonist. Inhibition of DNA polymerase
Dactinomycin (Actinomycin D)
intercalates in DNA
doxorubicin (adriamycin) daunorubicin
generates free radicals. Noncovalently intercalates in DNA and causes DNA breaks and decreased replication
Bleomycin
G2 phase specific. Induces free radicals which cause breaks in DNA strands
Etoposide Teniposide
Late S to G2 phase specific. Inhibits DNA topo 2 leading to increased DNA degradation
Cyclophosphamide ifosphamide
Covalently X-link DNA at guaning N-7. Require bioactivation by liver.
Nitrosoureas - Carmustine Lomustine Semustine Streptozocin
Require bioactivation. Cross BBB into CNS
Busulfan
Alkylates DNA
Vincristine Vinblastine
bind to tubulin in M phase and block polymerization of microtubules so that the mitotic spindle can’t form.
Paclitaxel
hyperstabilize polymerized microtubules in M phase so that mitotic spindle cannot break down (preventing anaphase).
Cisplatin Carboplatin
Cross links DNA
Hydroxyurea
Inhibits Ribonucleotide Reductase - decreases DNA synthesis. S-phase specific
Tamoxifen Raloxifene
SERM - receptor antagonist in breast, agonists in bone; block binding of estrogen to ER+ cells
Trastuzumab (Herceptin)
mAb against HER-2 (erb-B2). Kills breast cancer that overexpress HER-2, possibly through antibody dependent cytotoxicity
Imatinib (Gleevec)
Philadelphia chromosome bcr-abl tyrosine kinase inhibitor
Bethanecol
Muscarinic Agonist. Activates Bowel and Bladder smooth muscle
Carbachol
Muscarinic Agonist
Pilocarpine
Muscarinic Agonist. Potent stimulator of sweat, tears, and saliva
Methacholine
Muscarinic agonist
Neostigmine
increases endogenous Ach; no CNS penetration.
Pyridostigmine
increases endogenous Ach; increases strength; no CNS penetration; long-acting
Edrophonium
increases endogenous Ach; extremely short-acting
Physostigmine
increases endogenous Ach; Crosses BBB
Echothiophate
increases endogenous Ach
Atropine
muscarinic antagonist
homatropine tropicamide
muscarinic antagonist
benztropine
muscarinic antagonist
scopolamine
muscarinic antagonist
ipratropium
muscarinic antagonist
oxybutynin glycopyrrolate
muscarinic antagonist
metscopolamine pirenzepine propanetheline
muscarinic antagonist
Hexamethonium
nicotinic antagonist (ganglionic blocker)
Epinephrine
a1, a2, B1, B2 agonists. Low doses selective for B1
Norepinephrine
a1, a2 > B1 agonists.
Isoproterenol
B1 = B2 agonist
Dopamine
D1 = D2 > B > a
Dobutamine
B1 > B2
Phenylephrine
a1 > a2
Metaproterenol albuterol salmeterol terbutaline
B2 > B1
Ritrodine
B2
Amphetamine
releases stored catecholamines
Ephedrine
releases stored catecholamines
cocaine
catecholamine uptake inhibitor
Clonidine alpha-methyldopa
centrally acting a2 agonist
Phenoxybenzamine (irreversible); Phentolamine (reversible)
nonselective alpha blockers
Prazosin Terazosin Doxazosin
a1 blockers
Mirtazapine
a2 blocker
Propranolol Timolol Nadolol Pindolol
nonselective beta blockers (pindolol is partial B Ag at high levels)
Acebutolol Betaxolol Esmolol Atenolol Metoprolol
B1 > B2 blocker; (acetbutolol is a partial B Ag, esmolol is short-acting)
Carvedilol Labetalol
nonselective alpha and beta blockers
Hydralazine
increases cGMP which leads to smooth muscle relaxation
Minoxidil
potassium channel opener - hyperpolarizes and relaxes vascular smooth muscle
Nifedipine Verapamil Diltiazem
Block voltage-gated L-type potassium channels of cardiac and smooth muscle and thereby reduce muscle contractility
Nitroglycerin, Isosorbide dinitrate
Vasodilate by releasing NO in smooth muscle, causing increased cGMP and smooth muscle relaxation. Dilate veins»arteries. Decrease preload.
Nitroprusside
Short acting. Increase cGMP via direct release of NO. Can cause cyanide toxicity
Fenoldopam
Dopamine D1 receptor agonist-relaxes renal vascular smooth muscle
Diazoxide
Potassuim Channel Opener-hyperpolarizes and relaxes vascular smooth muscle
Nitrates, B-Blockers, Calcium Channel Blockers
Nitrates and Nifedipine decrease preload. B-Blockers and Verapamil decrease afterload.
Digoxin
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
Quinidine Procainamide Disopyramide
Na channel blocker. Increases ERP and QT interval.
Lidocaine Mexilitine Tocainide Phenytoin
Na channel blocker. Decrease AP duration. Preferentially affect ishemic or depolarized Purkinje and ventricular tissue.
Flecainide Encainide Propafenone
Na channel blocker. No effect on AP duration.
Propranolol Esmolol Metoprolol Atenolol Timolol
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
Sotalol Ibutilide Bretylium Dofetilide Amiodarone
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.
Verapamil Diltiazem
Ca-channel blocker. Primarily affect AV nodal cells. Decreases conduction velocity, increases ERP, increases PR interval
Adenosine
Causes K efflux from cell, hyperpolarizing the cell and decreasing intracellular Ca. Very short acting.
Potassium
Depresses ectopic pacemakers in hypokalemia
Lovastatin Pravastatin Simvastatin Atorvastatin Rosuvastatin
Inhibits cholesterol precursor, mevalonate. HMG CoA reductase inhibitors
Niacin
inhibits lipolysis in adipose tissue; reduces hepatic VLDL secretion into cirulation
Cholestyramine Colestipol Colesevelam
Bile acid resins. Prevents intestinal reabsorption of bile acids; liver must use cholesterol to make more
Ezetimibe
Cholesterol absorption blocker. Prevents cholesterol reabsorption at small intestine brush border