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Pharmacology Final
Question | Answer |
---|---|
donepezil | Carbamate AChase inhibitor Used in tx of Alzheimer's dz |
Memantine | NMDA receptor antagonist Used in tx of Alzheimer's dz |
Carbachol | Direct agonist at cholinergic receptors. Metabolized more slowly than Ach "Can't Be Metabolized" Has effect at nicotinic/muscarinic receptors |
Bethanechol* | Direct agonist at cholinergic receptors. Metabolized more slowly than Ach "Can't Be Metabolized" Has effect only at muscarinic receptors Used to relieve urinary retention |
Methacholine | Direct agonist at cholinergic receptors. Metabolized more slowly than Ach "Can't Be Metabolized" Has effect only at muscarinic receptors Used for dx of asthma |
Pilocarpine | Muscarinic agonist Causes miosis, dec IOP, inc outflow of aqueous humor "pile on the sweat & tears" S/E if it gets into systemic circulation |
Nicotine | Tertiary amine, metabolized by liver Inc sympathetic activity, respiration & GI motility, cutaneous vasoconstriction, |
Physostigmine | Carbamate AChase inhibitor Tertiary |
Neostigmine | Carbamate AChase inhibitor, quartenary Tx of myasthenia gravis Used w/glycopyrrolate in reversal of NMB caused by non-depolarizing drugs |
Edrophonium | Carbamate AChase inhibitor, quaternary Dx of myasthenia gravis in pts being treated w/neostigmine |
Atropine | Muscarinic antagonist, tertiary Used to dec side effects of Ach agonists /AChase inhibitors "S.C.A.B" |
Malathion | Organophosphate AChase inhibitor, irreversible |
Parathion | Organophosphate AChase inhibitor, irreversible |
Isofluophate (DFP) | Organophosphate AChase inhibitor, irreversible |
Pralidoxime (2-PAM) | Given w/atropine for organophosphate poisoning. Regenerates phosphorylated AChase while atropine relieves symptoms |
Scopolamine | Muscarinic antagonist, tertiary. Prophylaxis of motion sickness. Antiemetic drug. "S.C.A.B" |
Cyclopentolate | Muscarinic antagonist, tertiary "S.C.A.B" |
Benztropine | Muscarinic antagonist, tertiary "S.C.A.B" |
N-methylatropine | Muscarinic antagonist, quaternary "N-methyl-PIG" |
Propantheline | Muscarinic antagonist, quaternary GI spasticity "N-methyl-PIG" |
Ipratropium* | Muscarinic antagonist, quaternary Prevent bronchoconstriction from air pollution/cold air "N-methyl-PIG" |
Glycopyrrolate* | Muscarinic antagonist, quaternary "N-methyl-PIG" |
Trimethaphan | Ganglionic blocking drug (N1 receptors) Blocks SNS & PSNS; block inc in plasma epi induced by hypoglycemia |
Hexamethonium | Ganglionic blocking drug (N1 receptors) Blocks SNS & PSNS; block inc in plasma epi induced by hypoglycemia |
Succinylcholine | Neuromuscular blocking drug (N2 receptors) depolarizing (non-competitive) |
Decamethonium | Neuromuscular blocking drug (N2 receptors) depolarizing (non-competitive) |
d-tubocurarine (curare) | Neuromuscular blocking drug (N2 receptors) non-depolarizing (competitive) |
pancuronium | Neuromuscular blocking drug (N2 receptors) non-depolarizing (competitive) |
Metyrosine | Inhibits tyrosine hydroxylae - rate-limiting enzyme in the synthesis of catecholamines |
Phenylephrine | alpha-1 agonist = Mydriasis w/o cycloplegia |
Ritodrine | B2-agonist = decreases uterine contraction in premature labor |
Isoproterenol | Non-selective B1 & B2 agonist = bronchodilation w/inc HR |
Albuterol | Selective B2 agonist = bronchodilation w/less inc in HR, for acute asthma |
Terbutaline | Selective B2 agonist = bronchodilation w/less inc in HR |
Clonidine | Centrally acting pre & post-synaptic alpha-2 adrenoceptor agonist. Antihypertensive drug. |
Reserpine | Dec NE release via depletion of neuronal NE stores, poisons NE storage vesicles |
Phenelzine | Non-selectively inhibit MAO-A and MAO-B. Used in tx depression. |
Tranylcypromine | Non-selectively inhibit MAO-A and MAO-B. Used in tx depression. |
Guanethidine | Inhibits Na-ATPase dependent pump = inhibits release of NE from the vesicle into cleft |
Cocaine | Indirect sympathomimetic. Inhibits reuptake of catecholamines from synaptic cleft |
Methylphenidate | tx ADHD/ADD |
Amphetamine | Indirect sympathomimetic. Releases stored catecholamines. |
Ephedrine | Indirect sympathomimetic at alpha receptors - no alpha after reserpine. Acts as direct at B1 and B2. |
Phentolamine | Competitive alpha blocker. Inc HR via baroreflex.Given to pts w/pheo tumor - dec BP. 3Ps |
Prazosin | Competitive alpha blocker. No effect on HR. 3Ps |
Phenoxybenzamine (PBZ) | Non-competitive alpha blocker. Inc HR via baroreflex. 3Ps |
Ergotamine | Partial alpha agonist - tx of migraine headaches |
Dihydroergotamine | Partial alpha agonist - tx of migraine headaches |
Tamsulosin | Blocks alpha-1A receptors in GU tract in pts w/BPH to enhance voiding |
atenolol | Competitive selective B1 blocker |
metoprolol | Selective B1 blocker |
Propranolol | Competitive non-selective B1 & B2 blocker. Causes local anesthesia of cornea. Tx of hyperthyroidism to control autonomic symptoms & block conversion of T4 to T3. Also tx for thyroid storm. |
Timolol | Non-selective B1 & B2 blocker. Tx of glaucoma by dec IOP w/o cycloplegia. Dec secretion of aqueous humor. "Tim is my ophthalmologist" |
TAP drugs | No effect after pretreatment w/reserpine Tyramine/amphetamine/phenylpropanolamine |
Selegiline | Selectively inhibits MAO-B to prevent DA breakdown in CNS. Used to tx depression. |
Tyramine | Releases NE to cause HT & tachycardia "cheese reaction" when MAO-A is inhibited in gut wall |
Alpha-methyldopa | Centrally acting pre & post-synaptic alpha-2 adrenoceptor agonist. Antihypertensive drug. |
Hydralazine | Arterial vasodilator. Dilate resistance vessels. Tx for HTN. S/E: lupus-like symptoms |
Minoxidil | Arterial vasodilator. Tx for HTN. S/E: hirsutism |
Diazoxide | Arterial vasodilator. Tx for HTN. S/E: inhibition of insulin release. |
Sodium nitroprusside (SNP) | Balanced vasodilation - dilates arteries & veins via release of NO. Used for HTN emergency. Thiocyanate toxicity in pts w/poor renal fxn. |
Labetalol | Used for HT emergency |
Nifedipine/amlodipine/felodipine | L-type calcium channel blocker. "pine" drugs mainly affect blood vessels & not the heart. Cause a greater dec in BP than VD drugs. |
Diltiazem | L-type calcium channel blocker. Primarily affect the heart. Dec AV conduction |
Verapamil | L-type calcium channel blocker. Primarily affect the heart. Dec AV conduction. Tx of AV nodal re-entry tachycardia. Prolongs state of inactivation of calcium channels. |
Disopyramide | Anti-arrhythmic that dec dp/dt (drugs that dec dp/dt: beta-blockers, calcium blockers, dii). Has antimuscarinic effects. |
Captopril | ACE inhibitors. Prevent conversion of Ang I to Ang II. Dec BP. S/E: cough |
Enalapril | ACE inhibitors. Prevent conversion of Ang I to Ang II. Dec BP. S/E: cough |
Losartan | ARB "-sartan." MOA in tx of CHF (inc CO by dec preload & afterload, reverse remodeling caused by angII). |
Acetazolamide | Diuretic. Inhibits carbonic anhydrase in PT & DT to prevent reabsorption of bicarb. Inc excretion of NA, K, HCO3. Urinary pH inc. Metabolic acidosis. |
Furosemide | Loop diuretic. Inhibit Na:K:2Cl symporter in ascending limb of loop of Henle. Also blocks Na transport in macula densa of DT = secondary hyperaldosteronism. Isotonic urine. Metabolic alkalosis. |
Ethacrynic acid | Loop diuretic. Inhibit Na:K:2Cl symporter in ascending limb of loop of Henle. Also blocks Na transport in macula densa of DT = secondary hyperaldosteronism. Isotonic urine. Metabolic alkalosis. |
Hydrochlorothiazide | Diuretic acts in distal tubule & dec GFR in all pts. Hypertonic urine. Tx of calcium stones & DOC for nephronegic DI. 2nd line tx for Li-induced DI. Metabolic alkalosis. |
Amiloride | K sparing diuretic. Block Na channels in principal cells of LDT/CD. Make urine alkaline. Tx for Lithium-induced DI. "TASK" |
Triamterene | K sparing diuretic. Block Na channels in principal cells of LDT/CD. Make urine alkaline. "TASK" |
Spironolactone | K sparing diuretic. Aldosterone receptor antagonist. Partial agonist at androgen/pregesterone receptors. "TASK" |
Mannitol | Osmotic diuretic agent. Inhibits solute reabsorption in ascending limb of the loop of Henle |
Digoxin | Cardiac glycoside. Renal clearance. Inhibition of Na-K ATPase. Direct: Inc dp/dt. Indirect: inc vagal tone, dec HR, dec AV conduction. Tx for pts w/A fib. |
Digitoxin | Cardiac glycoside. Hepatic clearance. Inhibition of Na-K ATPase. |
Quinidine | Antidysrhythmic. Blocks Na channels in fast fibers. Delays ventricular repolarization via K channel block. Indirect effects (atropine-like) inc conduction while direct effect at AV node dec conduction. Tx of atrial & ventricular dysrhythmias. |
Procainamide | Antidysrhythmic. SLE & arthritis in slow acetylators. "SHIP" |
Amiodarone | Antidysrhythmic. Inc AP duration, refractory period in fast fibers by inhibiting K channels. Inc QT. Tx of recurrent ventricular tachycardia. S/E: pulm fibrosis, hypo-hyper-thyroidism. |
Lidocaine | Antidysrhythmic. Block Na channels in fast fibers. Given iv. Tx to prevent PVCs. S/E: Seizures |
Aspirin | Inhibits COX-1 to prevent synthesis of TXA2 |
Abciximab | Antiplatelet drug. Antagonist of platelet IIb/IIIa which uses fibrinogen to bind platelets together. Given iv only in hospital. |
Eptifibatide | Antiplatelet drug. Antagonist of platelet IIb/IIIa which uses fibrinogen to bind platelets together. Given iv only in hospital. |
Tirofiban | Antiplatelet drug. Antagonist of platelet IIb/IIIa which uses fibrinogen to bind platelets together. Given iv only in hospital. |
Ticlopidine | Antiplatelet drug. Antagonist of platelet purinergic (ADP) receptors preventing aggregation. Given if pt can't take aspirin. |
Clopidogrel | Antiplatelet drug. Antagonist of platelet purinergic (ADP) receptors preventing aggregation. Given if pt can't take aspirin. Irreversible w/fewer S/Es. |
Heparin | Antiplatelet drug. Accelerates binding of antithrombin III to activated clotting factors 2, 9-12. Inc aPTT. Cannot be given po. |
Protamine sulfate | Heparin antagonist. |
Ardeparin | LMW heparin. Bind to ATIII to primarily inhibit activated factor 10 (Xa). |
Dalteparin | LMW heparin. Bind to ATIII to primarily inhibit activated factor 10 (Xa). |
Enoxaparin | LMW heparin. Bind to ATIII to primarily inhibit activated factor 10 (Xa). |
Warfarin | Antiplatelet drug. Inhibits Vit K epoxide reductase. Inc PT. Only works in vivo. |
Dicumarol | Antiplatelet drug. Inhibits Vit K epoxide reductase. Inc PT. Only works in vivo. |
Phytonadion | Reduced vit K. Reverses anticoagulant action of warfarin. |
Urokinase | Thrombolytic (fibrinolytic) drug. Direct activation of plasminogen. |
tPA | Thrombolytic drug. Serine protease. Activates plasminogen when in close proximity to clot. Binds to fibrin lysine residue. |
Streptokinase | Thrombolytic drug. Produced by Beta-hemolytic Strep spp. Changes conformation of plasminogen to expose active protease site that hydrolyzes another plasminogen molecule to plasmin. |
Aminocaproic acid | Inhibitor of fibrinolysis. Lysine analog that binds to lysine-binding site of tPa, plasminogen, & plasmin. |
Statins | Antilipemic drug. Inhibit hepatic HMG CoA reductase. Lower Tc, LDL, TG. Slight inc in HDL. S/E: muscle weakness/damage leading to rhabdomyolysis. |
Ezetimibe | Antilipemic drug. Inhibition of cholesterol absorption from the GI tract. Lower Tc & LDL. Used in pts w/muscle weakness due to statin. |
Gemfibrozil | Antilipemic drug. Activates lipoprotein lipase to inc hydrolysis of VLDL. Lowers Tc, LDL, VLDL, & TGs. Slight inc in HDL. Used in tx of hypertriglyceridemia. S/E: rhabdomyolysis. |
Fenofibrate | Antilipemic drug. Activates lipoprotein lipase to inc hydrolysis of VLDL. Lowers Tc, LDL, VLDL, & TGs. Slight inc in HDL. Used in tx of hypertriglyceridemia. S/E: rhabdomyolysis. |
Niacin | Antilipemic drug. Used to inc HDL cholesterol. |
Beta-blockers | Antianginal drug. Dec HR, dp/dt, & afterload. Net effect is dec in cardiac oxygen demand. |
Nitrates (nitroglycerin/glyceryl trinitrate/isosorbide mono-&dinitrate) | Antianginal drug. NO donors that preferentially dilate veins. Dec venous return which dec preload = dec cardiac oxygen demand. |
Calcium Channel blockers | Antianginal drug. Dec cardiac oxygen demand and inc oxygen supply. |
Niclosamide | DOC for cestodes (tapeworms). Uncouples oxidative metabolism. |
Praziquantal | DOC for Trematodes (flukes). DOC for unknown tapeworms. Opens calcium channels to cause muscular tetany, spastic paralysis, causes tegmental damage which activates host immune system. |
Albendazole | DOC for mixed infections caused by roundworms & tapeworms. Inhibits synthesis of microtubules needed for glucose uptake = dec glycogen & ATP = death. DOC for neurocysticercosis. Not used for pinworms |
Ivermectin | DOC for threadworm, onchocerciasis, & ectoparasites. Releases GABA = facilitates opening of chloride channels in NM jxn = flaccid muscle paralysis. Tonic paralysis of musculature of nematodes via glutamate-gated Cl channels found only in invertebrates. |
Thiabendazole | Used in tx of threadworm & trichinosis. Inhibits mitochondrial fumurate reductase. |
Diethylcarbamazine | DOC for Wucheria bancrofti. Immobilizes microfilariae via dec muscular activity. Also alters surface membranes to make organism more susceptible to host immune defenses. |
Pyrantel pamoate | Kills round/pin/hook worms. Ganglionic nicotinic cholinergic agonists = muscular tetany. |
Mebendazole | Kills round & tape worms. Inhibits synthesis of microtubules needed for glucose uptake = dec glycogen & ATP = death. |
Levamisole | Worm drug. Ganglionic nicotinic cholinergic agonists = muscular tetany. |
Metronidazole | Antiprotozoal drug. Active against anaerobic protozoa & bacteria. Reactive nitro radicals inhibits DNA replication. S/E: disulfiram-like rxn w/EtOH |
Pentamidine isethionate | Second choice for tx of PCP in AIDS pt. |
Trimethoprim-sulfamethoxazole | Bactericidal. DOC for tx of PCP in pts w/AIDS. Sulfa - Inhibits dihydropteroate synthase. Trim - Inhibits DHF reductase & can cause megaloblastic anemia. Sulf can cause kernicterus in neonates (so can Ceftriaxone & aspirin)! |
Primaquine | Antimalarial. Only drug that kills the hepatic form of P. vivax & ovale. Causes hemolytic anemia in pts w/genetic deficiency of glucose-6-phosphate dehydrogenase. |
Chloroquine | Antimalarial. Kills RBC stage only. Blocks DNA/RNA synthesis. Resistance developing. S/E: tinnitus, headache |
Mefloquine | Antimalarial. DOC for prophylaxis for areas w/chloroquine-resistant strains. |
Sulfadoxine-Pyrimethamine | Antimalarial. DOC for tx of chloroquine-resistant malaria. Sulfa - Inhibits dihydropteroate synthase. Pyri - Inhibits DHF reductase & can cause megaloblastic anemia. |
Acyclovir | Antiviral. Tx of herpes simplex & varicella-zoster virus. Inhibits viral DNA polymerase. |
Valacyclovir | Antiviral. Tx of herpes simplex & varicella-zoster virus. Inhibits viral DNA polymerase. |
Ganciclovir | Antiviral. Tx of CMV. Inhibits viral DNA polymerase. |
Idoxuridine | Antiviral. Thymidine derivative. Tx of HSV keratitis. Triphosphate inhibits viral DNA polymerase. |
Amantadine (not likely to be on final) | Antiviral. Blocks uncoating of viral RNA inside human cell by interfering w/fxn of viral M2 protein. Prophylaxis to prevent infection w/Influenza A. |
Zanamivir (not likely to be on final) | Antiviral. Blocks release of new viral particles from infected cells via inhibition of viral neuraminidase. Tx of influenza A & B. |
Interferons (not likely to be on final) | Antiviral. Causes protein synthesis to interfere w/viral penetration, uncoating, assembly, release, viral mRNA synthesis & translation. |
Cidofovir | Antiviral. Tx CMV retinitis. Converted to active diphosphate by host cell enzymes. Used for resistant strains of HSV. |
Foscarnet | Antiviral. Used to treat HSV which are resistant to acyclovir. Directly inhibits viral DNA polymerase. |
Trifluridine (aka trifluorothymidine) | Antiviral. Thymidine derivative. Tx herpes keratitis. Converted to active triphosphate by host cell enzymes. |
Zidovudine (AZT) | NRTI. Nucleoside converted to active triphosphate & inhibits HIV reverse transcriptase & incorporated into DNA to stop chain elongation. S/E: bone marrow depression & anemia |
Saquinavir | HIV protease inhibitor preventing the conversion of viral polyproteins into functional subunits needed for assembly of new viruses |
Amphotericin B | Antifungal. Binds to ergosterol in cell membrane to form pores. Does not cross BBB. S/E: nephrotoxicity. |
Fluconazole | Antifungal. DOC for Coccidioides immitis. DOC for cryptococcal meningitis in AIDS pts. Prevent ergosterol synthesis by inhibiting fungal CYP450. |
Voriconazole | Antifungal. DOC for Asperigillis spp. |
Ketoconazole | Antifungal. Prevent ergosterol (cell wall) synthesis by inhibiting fungal CYP450. Suppresses plasma cortisol in pt w/nl pituitary fxn by blocking CYP450scc. |
Flucytosine | Antifungal. Converted to fluorouracil which inhibits thymidylate synthesis & thus inhibits DNA synthesis. Not converted in humans. S/E: bone marrow suppression. Synergistic w/Ampho B |
Griseofulvin | Antifungal. DOC for ring worm. Tx of dermatophyts w/hypae. Disrupts mitotic spindle by interacting w/polymerized microtubules to inhibit fungal mitosis. |
Miconazole | Antifungal. Tx of athlete's foot. Prevent ergosterol synthesis by inhibiting fungal CYP450. |
Penicillin | Bind to active site of PBP to inhibit transpeptidation & cell wall synthesis. |
Probenecid | Increases half-life of penicillin by inhibiting its renal secretion |
Methcillin/oxacillin/nafcillin | Penicillins. Acid labile (given iv). Kills resistant (Beta-lactamase-producing) staph aureus |
cloxacillin/dicloxacillin | Penicillins. Acid stable (given po). Kills resistant (Beta-lactamase-producing) staph aureus |
Clavulanate/sulbactam/tazobactam | Inhibitors of Beta-lactamases. Protects susceptible PCN's from inactivation. |
Imipenam | Carbapenem - same MAO as PCN. Resistant to B-lactamase. Metabolized by renal dihydropeptidases (DHP). |
Cilastatin | DHP inhibitor. Given in combination w/imipenam to dec its renal clearance & inc its half-life. |
Clindamycin or trim-sulfa or doxycycline | tx of MRSA (outpatient) |
Vancomycin | Bacteriocidal. Covalently binds to D-ala-D-ala terminus of peptide side chains inhibiting cell wall synthesis. DOC for severe MRSA infections. p.o. used to treat C. difficile infection. |
Tetracycline | Bacteriostatic. Binds to 30S ribosome subunit to block binding of t-RNA. Tx of Rickettsiae, mycoplasma, chlamydia & amebas. Chelates cations. Do not use in pregnant women & children. |
Erythromycin/clarithromycin/azithromycin | Macrolides. Bacteriostatic. DOC for community-acquired pneumonia. Erythr causes stomach cramping. |
Clindamycin | Lincosamide. Binds to 50S ribosome subunit & blocks translocation of peptide chain. Historically linked w/C. difficle infection. |
Fluoroquinolones | Bactericidal. Drugs that end in "floxacin". Inhibit DNA gyrase. |
Nalidixic acid | Inhibit DNA gyrase. |
Aminoglycosides (gentamicin, tobramycin, amikacin) | Bactericidal. Bind 30S ribosome subunit to block initiation of peptide synthesis, cause misread mRNA codons, & prevent translation. Tx of penicillin-resistant gonorrhea. Gentamycin dec sensitivity to ADH. S/E: ototoxicity, nephrotoxicity |
Spectinomycin | Bacteriostatic. Binds to 30S ribosome subunit. Used to treat penicillin-resistant gonorrhea. |
Chloramphenicol | Bacteriostatic. Binds to 50S ribosome subunit. |
Isoniazid (INH) | Tx of TB "RIPE". Causes peripheral neuropathy & hepatotoxicity. Give pyridoxine (Vit B6) to reverse neuropathy. Slow acetylator "SHIP" |
Rifampin | Tx of TB "RIPE". Induces CYP450. Turns skin & fluids orange. |
Pyrazinamide | Tx of TB "RIPE". |
Ethambutol | Tx of TB "RIPE". |
Cromolyn sodium | Antihistamine. Inhibit mast cell degranulation by preventing inc in intracellular Ca caused by IgE bridging. Prophylaxis. |
Olopatadine | Antihistamine. Inhibit mast cell degranulation AND blocks H1-histamine receptors in the eye. Tx: Conjunctivitis assoc. w/seasonal allergy |
Diphenhydramine | Sedating H1-receptor antagonist. |
Meclizine | Sedating H1-receptor antagonist. Prophylaxis of motion sickness by blocking central muscarinic receptors. DOC for tx of Meniere's dz. |
Terfenadine | Non-sedating H1-receptor antagonist. |
Fexofenadine | Non-sedating H1-recepter antagonist. |
Clemastine | Non-sedating H1-receptor antagonist. |
Dimenhydrinate | Sedating H1-receptor antagonist. Prophylaxis of motion sickness by blocking central muscarinic receptors. |
Cimetidine | H2-receptor blocker. Blocks gastric acid secretion & allergic responses in skin. Inhibits CYP450 |
Famotidine | H2-receptor blocker. Blocks gastric acid secretion & allergic responses in skin. |
Ranitidine | H2-receptor blocker. Blocks gastric acid secretion & allergic responses in skin. |
Buspirone | Partial agonist at 5-HT1A receptors in CNS. Opens K channels to hyperpolarize neurons. Tx anxiety. Slow onset of action. No drug dependence. |
Octreotide | Somatostatin analog. Tx of carcinoid syndrome by inhibiting release of serotonin from tumor cells. Suppress GH secretion in pt w/acromegaly. |
Cyproheptadine | Blocks 5-HT1 & 5-HT2 receptors. Tx of carcinoid syndrome. |
Metoclopramide | Blocks D2-receptors, Blocks 5-HT3 receptors, Stimulates 5-HT4 receptors. Causes antiemetic effects & GI stimulation. Tx: GERD & empty stomach prior to emergency surgery. |
Odansetron | Antagonist at 5-HT3 receptor at both the CTZ and at vagal afferent fibers. Antiemetic drug. |
Cisapride | Agonist at 5-HT4 receptor on prejxnal cholinergic neurons. Enhances Ach release: inc LES tone, tx: GERD, empty stomach prior to emergency surgery. |
Sumatriptan | Agonist at 5-HT1B/1D receptors to inhibit the release of inflammatory peptides from trigeminal nerves. Tx: migraine & cluster headaches. |
Ipecac | DOC for emesis. Stimulates CTZ & irritates stomach & upper portion of duodenum. |
Apomorphine | Stimulates D2-receptors in CTZ to induce emesis. |
Lactulose | Synthetic disaccharide. Slow acting laxative converted to organic acids in bowel exerting an osmotic effect to slowly draw water into feces. Tx: Hepatic portal encephalopathy. |
Docusate sodium | Stool softener. An anionic surfactant: detergent action allows water to enter feces, softens stool w/o increasing its bulk. |
Loperamide | Antidiarrheal drug. Stimulate mu opiate receptor to increase GI muscle tone but decrease GI motility. |
Diphenoxylate | Antidiarrheal drug. Stimulate mu opiate receptor to increase GI muscle tone but decrease GI motility. |
Sulcralfate | Antiulcer drug. Mixture of AlOH & sucrose which forms a viscous gel at acidic pH; getl coats ulcerated tissue. |
Clarithromycin/Amoxacillin/Omeprazole | Antiulcer drug. Antibiotic triple therapy for eradication of H. pylori from GI tract |
Al/Mg hydroxide | Antiulcer drug. Antacids. Weak bases that neutralize acid in treatment of gastric & duodenal ulcers. Al - constipation. Mg - diarrhea (laxative). |
Omeprazole | Antiulcer drug. Proton pump inhibitor. Inhibit gastric H-K ATPase blocking acid secretion for 24-72 hrs. |
Misoprostol | Antiulcer drug. Structural PGE1 analog. Stimulation of PGE1 receptors on gastric parietal cells inhibit acid secretion. |
Sulfasalazine | Conjugation of sulfapyridine & 5-aminosalicyclic acid. 5-ASA blocks PG's & LT's synthesis. Tx of IBD. Sulfapyridein, esp in slow acetylators, can cause hepatic damage & bone marrow depression. |
Bisacodyl | Laxative. MOA: Irriant action inc accumulation of water & electrolytes in lumen of colon & enhances colonic peristalsis by activation of local factors. |
Glucocorticoids | Decrease number of B & T lymphocytes, monocytes, eosinophils, & basophils. Increase release of neutrophils. |
Cyclosporine | Immunosuppressant. Inhibits calcineurin to prevent production of IL-2 by helper T-cells. |
Mycophenolate | Inhibits "inosine monophosphate dehydrogenase" which prevents the de novo synthesis of purines by T & B lymphocytes. |
Azathioprine | Cytotoxic immunosuppressant. Converted to 6-mercaptopurine which interferes w/nucleic acid synthesis needed for proliferation of T & B cells. |
Cyclophosphamide | Cytotoxic immunosuppressant. Alkylates DNA thus inhibiting replication & translation leading to cell death. S/E: hemorrhagic cystitis. |
Dexamethasone | Glucocorticoid. Used to differentiate bilateral adrenal hyperplasia from adrenal carcinoma. |
Metyrapone | Blocks 11-beta-hydroxylase, the final step in cortisol synthesis. Lack of cortisol feedback to pituitary causes increased release of ACTH leading to increased synthesis of testosterone. Does not work in adrenal carcinoma. |
Aminogluthethimide | Causes medical adrenalectomy by blocking all adrenal & extra-adrenal steroid synthesis. Prevents the conversion of cholesterol to pregnenolone. Tx: cushing's syndrome |
Glucagon | Increases hepatic CAMP to activate the breakdown of glycogen & to activate enzymes of gluconeogenesis. No effect on skeletal muscle glycogen stores. Inc dt/dt & HR via inc in CAMP. tx: hypoglycemia, poisoning w/b-blockers, dx of DM1. |
Aspirin | NSAID. Inhibits platelet aggregation by irreversibly inhibiting COX-1 to prevent synthesis of TXA2. Inc bleeding time. tx: chest pn in unstable angina |
Dipyridamole | Inhibits PDEase in platelets preventing the breakdown of CAMP maintaining the inhibition platelet aggregation. |
Ibuprofen | NSAID. DOC for primary dysmenorrhea (menstrual cramps) |
Indomethacin | NSAID. Given iv to preterm infants to close patent ductus arteriosus. 2nd line tx for nephrogenic DI. |
Alprostadil | PGE1 analog dilates ductus arteriosus to keep it open prior to surgery. |
Acetaminophen | Antipyretic & analgesic but not anti-inflammatory. Does not cause "aspirin hypersensitivity". S/E: overdose increases AST/ALT. |
n-acetylcysteine | Tx of acetaminophen overdose. Precursor of glutathione. Replenishes glutathione stores to combine w/toxic metabolite of acetaminophen. |
Colchicine | Tx of gout. Binds to tubulin to inhibit polymerization into microtubles. Inhibits leukocyte migration & phagocytosis. Tx of pn of acute attacks. |
Allopurinol | Tx of gout. Inhibit xanthine oxidase to block synthesis of uric acid from purines. |
Probenecid & large doses of aspirin | Uricosuric drugs. Enhance renal clearance of urate. |
Epinephrine | Sympathomimetic drug. Produces bronchodilation via direct stimulation of B2-receptors. |
Zafirulkast | Competitive leukotriene receptor antagonist. Decreases late bronchoconstriction caused by allergens. |
Theophylline/Aminophylline | Inhibit PDEase intracellularly to prevent bronchoconstriction. |
Ferrous iron | Tx of Fe-deficiency anemia. Vitamin C enhances GI absorption of ferrous iron. |
p.o. folate/i.m. folate | Tx of folate deficiency. Use i.m. for those who can't absorb folate from GI tract. |
i.m. cyanocobalamin or hydroxocobalamin | Tx of vitamin B12 deficiency. Must be continued for life. |
Leucovorin | Reverse megaloblastic anemia in pt taking methotrexate. |
Erythropoetin (EPO)/epoetin alfa/darbepoetin | Increase RBC production in order to increase hematocrit |
Clomiphene | SERM. Blocks estrogen receptors in hypothalamus interrupting feedback inhibition. Leads to increase LH/FSH which stimulate estrogen to produce ovulation (multiple can occur). |
Tamoxifen | SERM. Blocks estrogen recepotrs in breast tissue (dec risk of breast CA). Agonist at liver, uterus, bone & lipid. |
Raloxifene | SERM. Antagonist at breast tissue & uterus (no endometrial hyperplasia). Agonist at liver, bone, & lipid. |
Mifepristone (RU-486) | Progesterone receptor antagonist leading to fetal abortion. |
Alendronate/risedronate/ibandronate | Bisphosphates. Inhibit resorption of bone by inhibiting the ability of osteoclasts to dissolve hydroxyapatite crystals. tx: cortisol-induced osteoporosis, w/calcitonin to treat Paget's dx, post-menopausal women who can't take estrogen |
L-thyroxine | Tx of hypothyroidism. |
Propylthiouracil (PTU) | Tx of hyperthyroidism. Prevents organification, coupling of MIT & DIT, and conversion of T4 to T3. DOC in pregnant women. |
Desmopressin | Tx of central DI. Long acting synthetic analog of AVP |
Demeclocycline | DOC for SIADH. Inhibits action of ADH in CD. |
Fluoxymesterone | Androgen used for its anabolic effects. Prevent catabolic action of cortisol. Stimulate protein synthesis & erythropoiesis. |
Nandrolone | Androgen used for its anabolic effects. Prevent catabolic action of cortisol. Stimulate protein synthesis & erythropoiesis. |
Flutamide/Bicalutamide | Androgen receptor antagonists |
Leuprolide/Goserelin/Nafarelin | GnRH receptor agonists. Tx: prostatic cancer, endometriosis, leiomyomas, & in-vitro synchronous follicular development. |
Finasteride | Block synthesis of DHT by inhibiting 5-alpha-reductase. Tx of BPH & hair loss. |
Growth hormone | Increases the production of insulin-like growth factor. Enlarges organs. Causes arthralgia, fluid retention, & hyperglycemia. |
Bromocriptine | Suppress the secretion of GH hormone in pt w/acromegaly. |
Plicamycin (mithramycin) | Cytotoxic antibiotic drug that inhibits bone resorption. Tx for vit D toxicity. |
1,25 diOH vitamin D | Tx for pt w/renal failure who has low plama calcium |
Calcitonin | tx of Paget's dz. Inhibits bone resorption & dec reabsorption of calcium & phosphate by kidneys. |
Tolbutamide/Chlorpropamide/Glyburide/Glipizide | Sulfonylureas. Block K channels in B-islet cells to release insulin. Tx DM2. S/E: hypoglycemia |
Metformin | Tx DM2. Enhances sensitivity of peripheral & hepatic tissues to actions of insulin. S/E: lactic acidosis |
Rosiglitazone/pioglitaozone | Tx DM2. Enhances sensitivity of peripheral tissues to actions of insulin. S/E: lactic acidosis |
Deferoxamine | Tx of Fe overdose. Chelating agent used to remove excess iron from body. |
Phenytoin | Antiepileptic drug that prolongs state of Na channel inactivation. DOC for generalized tonic-clonic seizures. S/E: gingival hyperplasia, osteomalacia. |
Diazepam | Antiepileptic drug. Benzodiazepine. DOC for status epilepticus. Give i.v. |
Fosphenytoin | Antiepileptic drug. Tx of status epilepticus if Diazepam is ineffective. |
Carbamazepine | Antiepileptic drug that prolongs state of Na channel inactivation. DOC for trigeminal neuralgia. |
Primidone | Antiepileptic drug. Metabolized to phenobarbital. |
Ethosuximide | Antiepileptic drug. Blocks T-type Ca channels in thalamus. DOC for absence seizurs. 3Hz spike wave rhythms. |
Baclofen | Skeletal muscle relaxant. Enhances K conductance by interacting w/GABA-B receptors to prevent release of glutamate & dec efferent excitation of spastic skeletal muscle. tx: spasticity from spinal cord injury, CP, MS. |
Dantrolene Na | Skeletal muscle relaxant. Inhibits release of Ca from SR in skeletal muscle. tx: spasticity from spinal cord injury, malignant hyperthermia, neuroleptic malignant syndrome. |
Desipramine | Antidepressant. Secondary amine TCA selectively blocks reuptake of NE. |
Fluoxetine | Antidepressant. SSRI. Selectively blocks reuptake of 5-HT. Tx of OCD. |
Paroxetine | Antidepressant. SSRI. Selectively blocks reuptake of 5-HT. Tx of OCD. |
Citalopram | Antidepressant. SSRI. Selectively blocks reuptake of 5-HT. Tx of OCD. |
Fluvoxamine | Antidepressant. SSRI. Selectively blocks reuptake of 5-HT. Tx of OCD, |
Imipramine | Antidepressant. Tertiary amine TCA that non-selectively blocks reuptake of Ne & 5-HT. Converted to desipramine. |
Cloimipramine | Antidepressant. TCA that non-selectively blocks reuptake of Ne & 5-HT. Tx of OCD. |
Venlafaxine | Antidepressant. Blocks 5-HT uptake (low doses), nonselectively blocks 5-HT & NE uptake (hihg doses). |
Phenelzine | Antidepressant. Irreversibly inhibits MAOA & B. Tyramine-containing foods contraindicate due to "HTN crisis". |
Tranylcypromine | Antidepressant. Irreversibly inhibits MAOA & B. Tyramine-containing foods contraindicate due to "HTN crisis". |