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Pharmacology > Mechanism of Action > Flashcards

Mechanism of Action Flashcards

0
Q

Activates muscarinic receptors in ciliary muscle

A

Pilocarpine

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1
Q

Used for the vasoocclusive crisis in sickle cell anemia with MOA of increasing HbF

A

Hydroxyurea

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2
Q

Activates nicotinic receptors

A

Nicotine, Varenicline

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3
Q

MOA: Betanechol

A

Activates muscarinic receptors

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4
Q

Inhibits acetylcholinesterase and amplifies endogenousy released acetylcholine

A

Edrophonium, Neostigmine, Pyridostigmine, Physostigmine, Rivastigmine

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5
Q

Competitively blocks all muscarinic receptors

A

Atropine, Homatropine, Cyclopentelate, Tropicamide

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6
Q

Binds phosphorus of organophosphate and breaks organophosphate bond with cholinesterase

A

Pralidoxime

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7
Q

Competitively blocks all muscarinic receptors restoring balance in the basal ganglia

A

Benztropine

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8
Q

Blocks muscarinic receptors in brochial smooth muscle preventing vagal-stimulated bronchoconstriction

A

Ipatropium, Tiotropium

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9
Q

Antagonizes histamine and serotonin

A

Scopolamine

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10
Q

Competitively blocks nicotinic Ach receptors

A

Hexamethonium, Trimethaptan

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11
Q

Activates alpha and beta receptors causing vasoconstriction, increased BP; increased HR, conduction and contractility; and bronchodilation

A

Epinephrine, Norepinephrine

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12
Q

Activates alpha, beta, and dopamine-1 receptors causing vasoconstriction, increased BP; increased HR, conduction and contractility; and vasodilation in sphlanchnic and renal vessels

A

Dopamine

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13
Q

Nonselectively activates beta adrenergic receptors

A

Isoproterenol

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14
Q

Selectively activates alpha-1 adrenergic receptors

A

Phenylephrine, Pseudoephedrine

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15
Q

Activates alpha-2 adrenergic receptors

A

Clonidine, Methyldopa, Apraclonidine

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16
Q

Activates beta-1 adrenergic receptors

A

Dobutamine

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17
Q

Activates beta-2 adrenergic receptors in bronchial smooth muscle causing bronchodilation

A

Albuterol, Salbutamol

Terbutaline, Ritodrine (uterine smooth muscles also)

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18
Q

Irreversibly blocks alpha adrenergic receptors (alpha1>alpha2)

A

Phenoxybenzamine

Nonselective alpha blocker

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19
Q

Reversibly blocks alpha adrenergic receptors (alpha1>alpha2)

A

Phenotolamine

Nonselective alpha blocker

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20
Q

Selectively blocks alpha-1 adrenergic receptors

A

Prazosin, Doxazosin, Terzosin, Tamsulosin, Sildosin

Selective alpha-1 blockers

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21
Q

Blocks beta-1 and beta-2 receptors. Blocks sympathetic effects on heart and BP reducing renin release

A

Propranolol, Pindolol, Timolol, Labetolol, Carvedilol, Nadolol
(Beta blockers)

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22
Q

Selectively blocks beta-1 receptors. Blocks sympathetic effects on heart and BP

A

Atenolol, Betaxolol, Esmolol, Acebutolol, Metoprolol

Selective beta-1 blockers

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23
Q

Drugs that causes decreased secretion of aqueous humor from the ciliary epithelium

A

Timolol (Beta blocker)
Mannitol (Osmotic diuretic)
Apraclonidine (Alpha-2 agonist)
Acetazolamide, Dorzolamide (Carbonic anhydrase inhibitors)

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24
Q

Alters intracellular Ca++ metabolism relaxing arteriolar smooth muscle causing vasodilation.

A

Hydralazine

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25
Q

Opens K+ channels in vascular smooth muscle causing hyperpolarization, muscle relaxation and vasodilation

A

Minoxidil

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26
Q

Blocks voltage gated L-type calcium channels (cardiac > vascular)

A

Verapamil, Diltiazem

Non-dihydopyridine calcium channel blockers

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27
Q

Blocks voltage gated L-type calcium channels (vascular > cardiac)

A

Nifedipine, Felodipine, Amlodipine, Nicardipine, Nisoldipine, Israpidine

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28
Q

Drugs that cause ciliary muscle contraction, opening of trabecular meshwork, increased outflow

A

Pilocarpine, Physostigmine

Cholinomimetics

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29
Q

Its MOA causes increased outflow through canal of Schlemm

A

Latanoprost

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30
Q

Increased outflow via uveoscleral veins

A

Epinephrine

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31
Q

Relaxes venous and arteriolar smooth muscle

A

Nitroprusside

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32
Q

Causes arteriolar vasodilation of the afferent and efferent arterioles increasing renal blood flow

A

Fenoldopam

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33
Q

Inhibits ACE and formation of Angiotensin II decreasing aldosterone secretion.

A

Captopril, Enalapril, Benazepril, Fosinopril, Lisinopril, Quinapril, Ramipril, Trandolapril

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34
Q

Blocks angiotension AT1 receptors in vascular smooth muscle and adrenal cortex decreasing aldosterone secretion.

A

Losartan, Candesartan, Valsartan, Irbesartan, Eprosartan, Telmisartan

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35
Q

Inhibits renin preventing conversion of angiotensinogen to angiotensin I

A

Aliskiren

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36
Q

Releases NO, increase cGMP and relaxes smooth muscle especially vascular

A 
Amyl nitrite (ultra short acting)
Nitroglycerin, Isosorbide dinitrate, Isosorbide mononitrate (short acting)
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37
Q

Inhibits Na/K-ATPase increasing intracellular Ca increasing cardiac contractility

A

Digoxin

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38
Q

Use- and state-dependent block of I-Na channels; some block of I-K channels. Slowed conduction velocityand pacemaker activity, prolonged AP duration and refractory period

A

Procainamide, Disopyramide, Quinidine

Class IA antiarrhythmic

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39
Q

Highly selective use- and state-dependent I-Na block; minimal effect on normal tissue, no effect on I-K

A

Lidocaine, Mexiletine, Tocainide, Phenytoin

Class IB antiarrhythmic

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40
Q

Selective use- and state-dependent I-Na block; slowed conduction velocity and pacemaker activity

A

Flecainide, Propafenone, Encainide, Moricizine

Class IC antiarrhythmic

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41
Q

Selective I-K block; prolonged AP and QT duration

A

Dofetilide

Class III antiarrhythmic

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42
Q

I-K block and beta-adrenoceptor block

A

Sotalol

Class III antiarrhythmic

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43
Q

Strong I-K block produces marked prolongation of AP and refractory period. Group 1 activity slows conduction velocity; groups 2 and 4 activity confer additional antiarrhythmic activity

A

Amiodarone, Dronedarone

Class III antiarrhythmic

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44
Q

Increase in diastolic I-K of AV node that causes marked hyperpolarization and conduction block; reduced I-Ca

A

Adenosine

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45
Q

Inhibits carbonic anhydrase

A

Acetazolamide, Dorzolamide, Brinzolamide, Dichlorphenamide, Methazolamide
(Carbonic anhydrase inhibitor)

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46
Q

Inhibit Na/K/2Cl transporter in thick ascending limb of LOH

A

Furosemide, Bumetanide, Toresamide, Ethacrynic acid

Loop diuretics

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47
Q

Inhibit Na/Cl transporter in DCT

A

Hydrochlorthiazide, Chlorthalidone, Indapamide, Metozalone

Thiazide diuretic

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48
Q

Steroid inhibitors of cytoplasmic aldosterone receptor in cortical CD reducing K excretion

A

Spironolactone, Eplerone

Aldosterone antagonist

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49
Q

Inhibitor of ENaC epithelial sodium channels in cortical CD, reducing Na reabsorption and K excretion

A

Amiloride, Triamterene

Na blocker, K sparing

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50
Q

Osmotically retains water in tubule by reducing reabsorption in PT, descending limb of LOH and CD

A

Mannitol, Glycerin, Isosorbide, Urea

Osmotic diuretic

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51
Q

Agonists at V1 and V2 receptos. Activate insertion of aquaporin water channels in CT

A

Desmopressin

Antidiuretic hormone

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52
Q

Antagonist at V1a, V2 receptors

A

Conivaptan, Tolvaptan, Lixivaptan, Demeclocycline, Lithium

ADH antagonist

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53
Q

Inhibits HMG-CoA reductase in the cholesterol biosynthesis

A

Simvastatin, Atorvastatin, Rosuvastatin, Fluvastatin, Pravastatin, Lovastatin, Pitavastatin

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54
Q

Binds bile acids preventing their reabsorption and increasing cholesterol utilization for replacement

A

Cholestyramine, Colesevelam, Colestipol

Bile acid-binding resin

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55
Q

Selective inhibitor of the NPC1L1 transporter, decreasing intestinal absorption of cholesterol and other phytosterols

A

Ezetimibe

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56
Q

Cholesterol analog, taking place of dietary and biliary cholesterol, decreasing intestinal absorption of cholesterol and other phytosterol

A

Sitosterol

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57
Q

Decreases VLDL synthesis and LDL cholesterol concentrations. Increases HDL concentration.

A

Niacin

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58
Q

Activates PPAR-alpha and increases expression of LPL and apolipoproteins. Lowers triglycerides. Increases HDL.

A

Gemfibrozil

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59
Q

Competitive pharmacologic block of peripheral and CNS H1 receptors plus alpha- and M-receptor block. Anti-motion sickness effect.

A

Diphenhydramine, Chlorpheniramine, Cyclizine, Meclizine, Promethazine

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60
Q

Competitive pharmacologic block of peripheral H1 receptors. No autonomic or anti-motion sickness effects.

A

Cetirizine, Loratadine, Fexofenadine, Desloratadine, Terfenadine, Astemizole

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61
Q

Competitive pharmacologic block of H2 receptors. Reduction of gastric acid secretion.

A

Cimetidine, Ranitidine, Famotidine, Nizatidine

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62
Q

5-HT1D agonist causing vasoconstriction. Modulates neurotransmitter release.

A

Sumatriptan, Almotriptan, Eletriptan, Frovatriptan, Naratriptan, Rizatriptan, Zolmitriptan

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63
Q

5-HT3 receptor antagonist

A

Ondansetron, Granisetron, Dolasetron, Palonosetron, Alosetron

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64
Q

Mixed partial agonist effects at 5HT2 and alpha-adrenoceptors causing marked smooth muscle contraction but blocks alpha-agonist vasoconstriction (vasoselective)

A

Ergotamine, Dihydroergotamine, Methysergide

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65
Q

Mixed partial agonist effects at 5HT2 and alpha-adrenoceptors causing marked smooth muscle contraction but blocks alpha-agonist vasoconstriction (uteroselective)

A

Ergonovine, Methyergonovine

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66
Q

Prostaglandin activating EP receptors causing increased HCO3 and mucus secretion in stomach.

A

Misoprostol, Gemeprost

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67
Q

Activates EP receptors causing vascular smooth muscle and relaxation

A

Alprostadil

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68
Q

Prostaglandin E2 analog that in low concentrations contract and high concentrations relax uterine and cervical smooth muscle

A

Dinoprostine, Sulprostone

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69
Q

Activates FP receptors

A

Carboprost, Bimaprost, Travoprost, Unoprostone

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70
Q

Activates IP receptors causing vasodilation and reducing platelet aggregation

A

Epoprostenol, Beraprost, Iloprost, Trepostinil

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71
Q

Anti-asthma drug that inhibits phosphodiesterase antagonizing adeonosine receptors causing bronchodilation

A

Theophylline, Aminophylline, Pentoxyfylline

Methylxanthines

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72
Q

Anti-asthma drug that prevents Ca influx and stabilizes mast cells, preventing degranulation and release of histamine, leukotrienes and other mediators

A

Cromolyn, Nedodromil, Lodoxamide

Mast cell stabilizer

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73
Q

Anti-asthma drug that inhibits phospholipase A2 reducing expression of cyclooxygenase

A

Fluticasone, Beclomethasone, Budesonide, Ciclesonide, Flunisolide, Momethasone, Triamcinoline
(Corticosteroid)

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74
Q

Anti-asthma drug that inhibits 5-lipooxygenase reducing synthesis of leukotrienes preventing airway inflammation and bronchoconstriction

A

Zileuton

Leukotriene synthesis inhibitor

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75
Q

Anti-asthma drug that blocks cysteinyl leukotriene-1 receptor for leukotrienes C4, D4, E4 preventing airway inflammation and bronchoconstriction

A

Montelukast, Zafirlukast, Pranlukast

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76
Q

Anti-asthma that binds IgE antibodies on mast cells reducing reaction to inhaled

A

Omalizumab

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77
Q

Cofactor required for essential enzymatic reactions that form tetrahydrofolate, convert homocysteine to methione and metabolize methymalonyl-CoA

A

Cyanocobalamin, Hydroxycobalamin

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78
Q

Precursor of an essential donor of methyl groups used for synthesis of amino acids, purines, and deoxynucleotide

A

Folic acid, Folacin, Folinic acid

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79
Q

Agonist of erythropoeitin receptors expressed by red cell progenitors

A

Epoetin alfa, Darbepoetin alfa, Methoxy polyethylene, Glycolepoetin beta

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80
Q

Binds receptors on myeloid progenitors and stimulates cell maturation and proliferation; accelerates neutrophil recovery and reduces incidence of infection

A

Filgrastim, Sargramostim, Pegfilgrastim

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81
Q

Recombinant form of an endogenous cytokine, activating IL-11 receptors

A

Oprelvekin

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82
Q

Nonselective, irreversible COX 1&2 inhibitor reducing platelet production of thromboxane A2, a potent stimulator of platelet aggregation

A

Aspirin

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83
Q

Inhibits platelet aggregation by interfering with GPIIb/IIIa binding to fibrinogen and other ligands
What disease does it resemble?

A

Abciximab, Eptifibatide, Tirofiban
(Glycoprotein IIb-IIIa inhibitors)
Glanzmann’s Thrombasthenia

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84
Q

Irreversibly inhibits binding of ADP to platelet receptors reducing platelet aggregation

A

Clopidogrel, Ticlopidine, Prasugrel

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85
Q

Inhibits phosphodiesterase III and increase cAMP in platelets and blood vessels inhibiting platelet aggregation and causes vasodilation

A

Dipyridamole, Cilostazol

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86
Q

Activates antithrombin III by inactivating thrombin or factor IIa, factor IXa & factor Xa by forming stable complexes with them

A

Heparin

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87
Q

Binds and potentiates effect of antithrombin III on factor Xa more selective

A

Enoxaparin, Daltaparin, Tinzaparin, Danaparoid, Fondaparinux

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88
Q

Binds to thrombin’s active site and inhibits its enzymatic action

A

Lepuridin, Desidurin, Bivalirudin, Argatroban

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89
Q

Inhibits vitamin K epoxide reductase responsible for gamma-carboxylation of the vitamin K-dependent clotting factors

A

Warfarin, Dicumarol

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90
Q

Chemical antagonist of heparin

A

Protamine sulfate

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91
Q

Tissue plasminogen activator analog converting plasminogen to plasmin which degrades the fibrin and fibrinogen causing thrombolysis

A

Alteplase, Anistreplase, Reteplase, Streptokinase, Tenecteplase, Urokinase

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92
Q

Competitively inhibits plasminogen activation

A

Aminocaproic acid, Tranexamic acid

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93
Q

Increases supply of reduced vitamin K which is required for synthesis of functional vitamin K-dependent clotting and anticlotting factors

A 
Vitamin K1 (Phytonadione)
Vitamin K2 (Menaquinone)
Vitamin K3 (Menadione)
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94
Q

Selective COX2 inhibitor, inhibiting prostaglandin synthesis

A

Celecoxib, Etroricoxib, Parecoxib, Rofecoxib, Valdecoxib

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95
Q

Inhibits AICAR transformylase and thymidylate synthetase with secondary effects on polymorphonuclear chemotaxis

A

Methotrexate

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96
Q

Binds to TNF-alpha preventing it from TNF-alpha receptor

A

Infliximab, Adalimumab, Etanercept

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97
Q

Forms 6-Thioguanine, suppressing inosinic acid synthesis, B-cell and T-cell function, immunoglobulin production and interleukin-2 secretion

A

Azathioprine

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98
Q

Suppression of T-lymphocyte responses to mitogens decreasing leukocyte chemotaxis, stabilization of lysosomal enzymes, inhibition of DNA and RNA synthesis, trapping of free radicals

A

Chloroquine, Hydroxychloroquine

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99
Q

Forms phosphoramide mustard which cross-links DNA to prevent cell replication suppresses T-cell and B-cell activation

A

Cyclophospamide

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100
Q

Inhibits interleukin-1 and interleukin-2 receptor production and secondarily inhibits macrophage T-cell interaction and T-cell rsponsiveness

A

Cyclosporine

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101
Q

Its active product inhibits inosine monophosphate dehydrogenase and inhibits T-cell lymphocyte proliferation

A

Mycophenolate mofetil

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102
Q

Active metabolite inhibits the release of inflammatory cytokines

A

Sulfasalazine

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103
Q

Antigout drug that inhibits microtuble assembly, decreasing macrophage migration and synthesis

A

Colchicine

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104
Q

Competes with uric acid for reabsorption in the proximal tubules increasing uric acid excretion

A

Probenecid

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105
Q

Active metabolite, alloxanthine irreversibly inhibits xanthine oxidase and lowers production of uric acid

A

Allopurinol

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106
Q

Nonpurine reversible inhibitor of xanthine oxidase more selective than allopurinol lowering production of uric acid

A

Febuxostat

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107
Q

Bind to GABA-A receptor subunits to increasing frequency of Cl channel opening hyperpolarizing membrane

A

Benzodiazepenes
Midazolam, Brotizolam, Triazolam, Oxazepam, Etizolam (short-acting)
Lorazepam, Alprazolam, Estazolam, Clonazepam,Lormetrazepam, Nitrazepam, Temazepam (intermediate-acting)
Diazepam, Chlorazepate, Chlordiazepoxide, Flurazepam, Quezepam, Flunitrazepam (long-acting)

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108
Q

Antagonist at benzodiazepene sites on GABA-A receptor

A

Flumazenil

109
Q

Bind to GABA-A receptor sites by increasing duration of Cl channel opening

A

Barbiturates
Thiopental, Methohexital, Thiamylal (ultrashort)
Pentobarbital, Secobarbital, Amobarbital, Butalbital, Butabarbital, Talbultal, Aprobarbital (short and intermediate)
Phenobarbital, Mephobarbital, Primidone
(long)

110
Q

Bind selectively to a subgroup of GABA-A receptors, acting like benzodiazepenes to enhance membrane hyperpolarization

A

Zolpidem, Zaleplon, Eszopiclone

111
Q

Anxiolytic that partial antagonist at 5-HT1 receptors and possibly D2 receptors

A

Buspirone

112
Q

Anti-seizure drug that blocks voltage gated channels

A

Phenytoin, Fosyphenytoin, Mephenytoin, Ethotoin

113
Q

Anti-seizure drug that blocks voltage gated channels and decrease glutamate release

A

Carbamazepine

114
Q

Anticonvulsant that blocks high frequency firing of neurons modifies amino acid metabolism

A

Valproic acid

115
Q

Anticonvulsant that decreases Ca++ currents in thalamus

A

Ethosuximide

116
Q

Anticonvulsant that blocks Ca++ channels inhibiting neuronal discharge from seizure foci

A

Gabapentin, Pregabalin

117
Q

Anticonvulsant that blocks Na and Ca channels decreasing glutamate

A

Lamotrigine

118
Q

Anticonvulsant that selectively binds synaptic vesicular protein SV2A modifyng synaptic release of glutamate and GABA

A

Levetiracetam

119
Q

Anticonvulsant with multiple actions on synaptic function via actions on phosphorylation

A

Topiramate

120
Q

Facilitates GABA-mediated inhibition blocking brain NMDA and ACh-N receptors

A

Inhalational anesthetics

121
Q

Intravenous anesthetic that blocks excitation by glutamate at NMDA receptors

A

Ketamine

122
Q

Intravenous anesthetic that modulates GABAa receptors containing beta-3 subunits

A

Etomidate

123
Q

Intravenous anesthetic that potentiates GABA-A receptors and blocks Na channels

A

Propofol

124
Q

Blockade of Na channels slows then prevents axon potential propagation

A

Ester local anesthetics (1i) - Procaine, Benzocaine, Butamben, Cocaine, Tetracaine
Amide local anesthtics (2is) - Lidocaine, Prilocaine, Bupivacaine, Ropivacaine

125
Q

Competitive antagonists at skeletal muscle nicotinic acetylcholine receptors

A

Tubocurarine, Mivacurium, Atracurium, Vecuronium, Rocuronium, Pancuronium

126
Q

Agonist at ACh-N receptors causing initial twitch then persistent depolarization

A

Succinylcholine

127
Q

Inhibits peripheral metabolism of Levodopa via dopa decarboxylase

A

Carbidopa

128
Q

Antiparkinsonism drug that partially antagonizes dopamine D2 receptors in brain

A

Bromocriptine, Pergolide

129
Q

Antiparkinsonism drug that partially agonizes dopamine D3 receptors in brain

A

Pramipexole, Ropinirole

130
Q

Antiparkinsonism drug that partially agonizes dopamine D3 receptors and antagonizes at 5-HT and alpha-adrenoceptors

A

Apomorphine

131
Q

Selective inhibitors of MAO type B leading to decreased degradation of dopamine and increasing response to levodopa/carbidopa

A

Selegiline, Rasagiline

132
Q

Antiparkinsonism drug that block L-dopa metabolism by inhibiting catechol-O-methytransferase in periphery or CNS prolonging response to levodopa

A

Entacapone, Tolcapone

133
Q

Antiparkinsonism drug that potentiates dopaminergic function by influencing the synthesis, release or reuptake of dopamine antagonizing the effects of adenosine at adenosine A2 receptors

A

Amantadine

134
Q

Antiparkinsonism drug that decreases the excitatory actions of cholinergic neurons on cells in the striatum by blocking muscarinic receptors

A

Benztropine, Biperiden, Trihexyphenidyl, Orphenadrine

135
Q

Block of D2 receptors&raquo_space; 5-HT2 receptors

A

Typical antipsychotics

Chlorpromazine, Thioridazine, Haloperidol, Droperidol

136
Q

Block of 5-HT2 receptors&raquo_space; D2 receptors

A

Atypical antipsychotics

Clozapine, Olanzapine, Quetiapine, Risperidone, Ziprasidone, Aripriprazole

137
Q

Mood stabilizer that decreases cAMP inhibiting inosotol-1-phosphatase causing depleting of inositol and inositol triphosphate

A

Lithium

138
Q

Blocks NE and 5-HT transporters

A

Imipramine, Clomipramine, Desipramine, Amitryptyline, Nortryptiline
(Tricyclic antidepressant)

139
Q

Inhibits neuronal reuptake of serotonin

A

Fluoxetine, Parozetine, Citalopram, Escitalopram, Sertraline, Fluvoxamine
(Selective serotonin reuptake inhibitor)

140
Q

Inhibits neuronal reuptake of serotonin and norepinephrine

A

Venlafaxine, Duloxetine, Desvenlafaxine

Serotonin-norepinephrine reuptake inhibitor

141
Q

Blocks 5-HT2 receptors

A

Trazadone, Nefazodone

serotonin antagonist

142
Q

Strong norepinephrine reuptake inhibitor and weak serotonin reuptake inhibitor; blocks dopamine D2 receptors

A

Amoxapine

143
Q

Increases amine release from nerve endings by antagonism of presynaptic alpha-2 adrenoceptors; blocks serotonin 5-HT2 receptors

A

Mirtazipine

144
Q

Inhibits neuronal reuptake of dopamine and norepinephrine increasing their activities

A

Bupropion

145
Q

Inhibits MAO types A and B increasing CNS levels of NE and serotonin

A

Phenelzine, Tranylcypromine, Selegeline

146
Q

Strong agonist at mu receptors

A

Morphine, Fentanyl, Sufentanil, Alfentanil, Remifentanil, Ohmefentanyl, Methadone

147
Q

Strong agonist at mu and kappa receptors

A

Meperidine, Hydroxycodone, Oxycodone

148
Q

Decreases sensitivity of cough receptors depressing the medullary cough center through sigma receptor stimulation

A

Dextrometorpham, Codeine

149
Q

Weak agonist at mu receptors

A

Propoxyphene, Levopropoxyphene, Dextropropo, Tramadol, Tapentadol

150
Q

Strong agonist at kappa receptors, weak antagonist activity at mu receptors

A

Nalbuphine, Buprenorphine, Butorphanol, Pentazocine

151
Q

Competitively blocks mu, delta and kappa receptors

A

Naloxone, Naltrexone, Nalmefene

152
Q

Increases release of IGF-1 in the liver and cartilage

A

Somatropin

153
Q

Suppression secretion of GH, IGF-1, serotonin and GI peptides

A

Octreotide, Lanreotide

154
Q

Activates FSH receptos mimicking effects of endogenous FSH

A

Follitropin alfa, Menotropins, Urofollitropin, Follitropin beta

155
Q

Activates LH receptos mimicking effects of endogenous LH

A

Choriogonadotropin alfa, Human chorionic gonadotropin, Lutropin

156
Q

Increased LH and FSH secretion with intermittent administration and reduced LH and FSH secretion with prolonged continuous administration

A

Leuprolide, Gonadorelin, Goserelin, Histrelin, Nafarelin, Triptorelin

157
Q

Blocks GnRH receptors reducing production of LH and FSH

A

Ganirelix, Cetrorelix, Abarelix, Degarelix

158
Q

Inhibits thyroid peroxidase reactions; blocks iodine organification; inhibits peripheral conversion of T4 into T3

A

Propylthiouracil

159
Q

Inhibits thyroid peroxidase reactions; blocks iodine organification

A

Methimazole

160
Q

Emits beta rays causing destruction of thyroid parenchyma

A

Radioactive iodine

161
Q

Inhibits iodine organification and hormone release reducing size and vascularity of thyroid gland

A

Potassium iodide

Lugol’s solution

162
Q

Activates glucocorticoid receptors, leading to altered gene transcription suppressing inflammation

A

Hydrocortisone
Desonide (low potency)
Fluticasone, Mometasone (medium potency)
Desoximethasone, Clobetasol (high potency)

163
Q

Strong agonist of mineralocorticoid receptors and moderate activation of glucocorticoid receptors

A

Fludrocortison, Deoxycorticosterone

164
Q

Inhibits desmolase blocking conversion of cholesterol to pregnenolone reducing synthesis of all hormonally active steroids

A

Aminogluthethimide

165
Q

Inhibits cholesterol side-chain cleavage, cytochrome P450 enzymes blocking ergosterol synthesis

A

Ketoconazole, Fluconazole, Itraconazole

166
Q

Inhibits cholesterol side-chain cleavage, cytochrome P450 enzymes blocking ergosterol synthesis

A

Ketoconazole, Fluconazole, Itraconazole

Clotrimazole

167
Q

Estrogen antagonistic actions in breast tissue and CNS. Estrogen agonist effects in uterus, liver, and bone.

A

Tamoxifen, Toremifene

168
Q

Estrogen antagonistic actions in breast tissue, uterus and CNS. Estrogen agonist effects in liver, and bone.

A

Raloxifene

169
Q

Partial agonist of estrogen receptors in pituitary; reduces negative feedback by estradiol; increases FH and LSH output

A

Clomiphene

170
Q

Estrogen synthesis inhibitor

A

Anastrazole, Letrozole, Exemestane

171
Q

Partial agonist of progestin and androgen receptors

A

Danazol

172
Q

Pharmacologic antagonist of glucocorticoid and progesterone receptors

A

Mifeprestone

173
Q

Competitive antagonist at androgen receptor

A

Flutamide, Bicalmutamide, Nilutamide

174
Q

Inhibits 5alpha-reductase enzyme that converts testosterone to dihydrotestosterone

A

Finasteride, Dutasteride

175
Q

Increases insulin secretion from panceratic beta cells by closing ATP-sensitive K+ channels

A

Insulin secretagogues
Chlorpropamide, Tolbutamide, Tolazamide (1st gen)
Glipizide, Glimepiride, Glyburide, Glibenclamide, Gliclazide (2nd gen)
Repaglinide, Nateglinide, Mitiglinide

176
Q

Activates AMP-stimulated protein kinase leading to inhibition of hepatic and renal gluconeogenesis

A

Metformin

177
Q

Regulates gene expression by binding to PPAR-gamma

A

Pioglitazone, Rosiglitazone, Troglitazone

178
Q

Inhibits intestinal alpha-glucosidase

A

Acarbose

179
Q

Activates amylin receptors suppressing glucagon release; delays gastric emptying; stimulates CNS to reduce appetite

A

Pramlintide

180
Q

Activates GLP-1 receptors augmenting stimulated insulin release from pancreatic B cells; inhibits glucagon secretion; produces satiety

A

Exanatide

Incretin modulator

181
Q

Inhibts dipeptidyl peptidase-4 that degrades GLP-1 and other incretins

A

Sitagliptin, Linagliptin

182
Q

Inhibits GI and pancreatic lipases reducing absoprtion of fats

A

Orlistat

183
Q

Antiobesity drug that inhibits NE and serotonin reuptake in the CNS

A

Sibutramine

184
Q

Antiobesity drug that selectively blocks cannabinoid receptors

A

Rimonabant

185
Q

Acts through PTH receptors to produce a net increase in bone formation

A

Teriparatide

186
Q

Suppresses the activity of osteoclasts inhibiting bone resorption

A

Alendronate, Etidronate, Ibandronate, Pamidronate, Risedronate, Tiludronate, Zoledronic acid

187
Q

Binds to dietary phosphate and prevents its absorption

A

Sevelamer

188
Q

Binds to proteins inhibiting transpeptidation in bacterial cell walls

A

Penicillins

189
Q

Inhibits inactivation of penicillins by bacterial beta-lactamase

A

Clavulanic acid, Sulbactam, Tazobactam

190
Q

Inhibits cell wall synthesis by binding to the D-ala-D-ala terminus of nascent polypeptidoglycan

A

Vancomycin, Teicoplanin

191
Q

Interferes with a late stage in cell wall synthesis in gram positive organisms

A

Bacitracin

192
Q

Blocks incorporation of D-ala into the pentapeptide side chain of the peptidoglycan

A

Cycloserine

193
Q

Bacterial protein synthesis inhibitors

A 
buy AT 30, CELLS at 50
A = Aminoglycosides
T = Tetracyclines
C = Chloramphenicol
E = Erythromycin
L = Lincosamides
L = Linezolid
S = Streptogranins
194
Q

Bacterial protein synthesis inhibitor that binds to 30s ribosomal subunit by blocking formation of the initiation complex, causing misreading of the code on the mRNA template and inhibiting translocation

A

Aminoglycosides

Gentamicin, Amikacin, Streptomycin, Neomycin, Spectinomycin

195
Q

Binds to 30s subunit by inhibiting binding of tRNA to A side

A

Tetracycline, Doxycycline, Minocycline, Tigecycline, Demeclocycline

196
Q

Binds to 50s subunit by inhibiting transpeptidation

A

Chloramphenicol

197
Q

Binds to 50s subunit by inhibiting translocation

A

Macrolides and Lincosamides
Macrolide - Erythromycin, Azithromycin, Clarithromycin, Telithromycin
Lincosamide - Clindamycin, Lincomycin

198
Q

Inhibits dihydropteroate synthase

A

Silver sulfadiazine, Mafenide acetate, Sulfamethoxazole

199
Q

Sequential blockade of dihydropteroate synthase and dihydrofolate reductase

A

Co-trimoxazole (Sulfamethoxazole-Trimethprim)

200
Q

Inhibits DNA replication by binding to DNA gyrase and topoisomerase IV

A

Fluoroquinolones
Ciprofloxacin, Ofloxacin, Norfloxacin (2nd gen)
Levofloxacin, Sparfloxacin, Grepafloxacin (3rd gen)
Moxifloxacin, Trovafloxacin, Gemifloxacin, Gatifloxacin (4th gen)
Nadilixic acid, Cinaxacin, Rosoxacin (1st gen - obsolete)

201
Q

Reactive reduction by ferredoxin forming free radicals that disrupt electron transport chain

A

Metronidazole, Tinidazole

202
Q

Forms multiple ractive intermediates when acted upon by bacterial nitrofuran reductase

A

Nitrofurantoin

203
Q

Antimycobacterial that inhibits mycolic acid synthesis

A

Isoniazid

204
Q

Antimycobacterial that inhibits DNA-dependent RNA polymerase

A

Rifampicin, Rifabutin, Rifapentine

205
Q

Antimycobacterial that inhibits arabinosyl transferases involved in the synthesis of arabinogalactan in mycobacterial cell wall

A

Ethambutol

206
Q

Antimycobacterial that inhibits folic acid synthesis

A

Dapsone

207
Q

Antimycobacterial that binds to guanine in bacterial DNA

A

Clofazimine

208
Q

Antifungal that binds to ergosterol in fungal cell membranes forming artificial pores

A

Amphotericin B

Nystatin

209
Q

Accumulated by fungal cells by the action of permease and converted by cytosine deaminase to 5-FU which inhibits thimidylate synthase

A

Flucytosine

210
Q

Inhibits beta-glucan sythase decreasing fungal cell wall synthesis

A

Caspofungin, Anidulafungin, Micafungin

211
Q

Antifungal that interferes with microtubule function inhibiting synthesis and polymerization of nucleic acids

A

Griseofulvin

212
Q

Interferes with ergosterol synthesis by inhibiting fungal squalene oxidase

A

Terbinafene

213
Q

Activated by viral thymidine kinase to forms that inhibit viral DNA polymerase

A

Acyclovir, Valacyclovir, Penciclovir, Famciclovir, Docosanol

214
Q

Inhibits viral DNA polymerase causing chain termination

A

Ganciclovir, Valganciclovir

Cifodovir

215
Q

Inhibits viral RNA polymerase, DNA polymerase and HIV reverse transcriptase and binds to pyrophosphate binding site

A

Foscarnet

216
Q

Inhibit HIV reverse transcriptase after phosphorylation by cellular enzymes

A

Zidovudine, Abacavir, Didonasine, Emtricitabine, Lamivudine, Stavudine, Tenofovir, Zalcitabine
(Nucleoside reverse transcriptase inhibitors)

217
Q

Inhibit HIV reverse transcriptase but no phosphorylation

A

Delavirdine, Efavirenz, Etravirine, Nevirapine (Non-nucleoside reverse transcriptase inhibitors)

218
Q

Inhibit viral protein processing

A

Indinavir, Amprenavir, Atazanavir, Darunavir, Indinavir, Lopinavir, Nelfinavir, Ritonavir, Saquinavir, Tipranavir
(Protease inhibitor)

219
Q

Binds to gp41 subunit of viral envelope glycoprotein preventing fusion of viral and cellular membranes

A

Enfuvirtide

Fusion inhibitor

220
Q

Blocks viral attachment via transmembrane chemokine receptor CCR5

A

Maraviroc

221
Q

Inhibit early step replication and prevent uncoating by binding to M2 proton channels

A

Amantadine, Rimantadine

222
Q

Inhibits neuramidase decreasing releasing of progeny virus

A

Oseltamivir, Zanamivir

223
Q

Degrades viral RNA via activation of host cell RNAase

A

Interferon-alpha

224
Q

Inhibits HBV DNA polymerase

A

Lamivudine, Adefovir dipivoxil, Entacavir, Telbivudine, Tenofovir

225
Q

Inhibits GTP formation, prevents capping of viral mRNA and blocks RNA-dependent RNA polymerase

A

Ribavirin

226
Q

Antimalarial drug that prevents polymerization of heme into hemozoin

A

Chloroquine, Hydroxychloroquine

227
Q

Antimalarial drug that complexes with DNA to prevent strand separation, blocks DNA replication and transcription

A

Quinine, Quinidine

228
Q

Antimalarial drug that forms electron-transfering redox compounds that act as cellular oxidants; tissue schizonticide

A

Primaquine

229
Q

Antimalarial drug that disrupts mitochondrial electron transport and inhibits folate synthesis

A

Atovaquone-Proguanil

230
Q

Antimalarial drug with sequential blockade of folic acid synthesis

A

Sulfadoxone-Pyrimethamine

231
Q

Antimalarial drug that impairs progeny of malarial apicoplast genes resulting in abnormal cell division

A

Doxycycline

232
Q

Antimalarial drug that forms free radicals in malarial food vacuole

A

Artemisin, Artesunate, Artemether, Dihydroartemisinin

233
Q

Antiprotozoal drug that inhibits protein synthesis and blocks ribosomal movement along messenger RNA

A

Emetine, Dehydroemetine

234
Q

Antiprotozoal drug that inhibits protein synthesis and binds to 16s ribosomal subunit

A

Paromomycin

235
Q

Antiprotozoal drug that reduces ferredoxin forming free radicals that disrupt electron transport chain

A

Nitazoxanide

236
Q

Antiprotozoal drug that is suicide inhibitor of ornithine decarboxylase

A

Eflornithine

237
Q

Antiprotozoal drug that is a organic arsenical and inhibits enzyme sulfahydryl groups in trypanosomes

A

Melarsoprol

238
Q

Antiprotozoal drug that inhibits trypanothione reductase

A

Nifurtimox

239
Q

Antihelminthic drug that inhibits microtubule synthesis and glucose uptake in nematodes

A

Mebendazole

240
Q

Antihelminthic drug that inhibits microtubule synthesis that is ovicidal and larvicidal

A

Albendazole

241
Q

Antihelminthic drug that intensifies GABA-mediated neurotransmission in nematodes

A

Ivermectin

242
Q

Antihelminthic drug that stimulates nicotinic receptors at NMJ of nematodes causing depolarization-induced paralysis

A

Pyrantel pamoate

243
Q

Antihelminthic drug that inhibits microtubule synthesis and glucose reuptake in nematodes; inhibits fumarate reductase

A

Thiabendazole

244
Q

Antihelminthic drug that increases membrane permeability to calcium causing muscle paralysis, vacuolization and death

A

Praziquantel

245
Q

Antihelminthic drug that uncouples oxidative phosphorylation or activates ATPases

A

Niclosamide

246
Q

Alkalyting agents that form DNA cross-links resulting in inhibition of DNA synthesis and function

A

Cyclophosphamide, Chlorambucil, Cisplatin, Carboplatin, Oxaliptin, Bisulfan

247
Q

Alkalyting agent that forms hydrogen peroxide which generates free radicals that cause DNA strand scission

A

Procarbazine, Dacarbazine

248
Q

Antimetabolite chemotherapeutic drugs that inhibit de novo purine nucleotide synthesis

A

6-Mercaptopurine, 6-Thioguanine, Fludarabine, Cladribine

249
Q

Antimetabolite chemotherapeutic drug that inhibits thymidilate synthesis causing thymineless death

A

5-Flurouracil

250
Q

Antimetabolite chemotherapeutic drugs that inhibit DNA synthesis and repair; inhibit ribonucleotide reductase with reduced formation of dNTPs

A

Cytarabine, Gemcitabine

251
Q

Chemotherapeutic drug that prevents microtubule assembly causing cell arrest at metaphase

A

Vincristine, Vinblastine

252
Q

Chemotherapeutic drug that inhibits DNA topoisomerase II (DNA gyrase) and inhibits mitochondrial electron transport

A

Etoposide, Teniposide

253
Q

Chemotherapeutic drug that inhibits DNA topoisomerase I (DNA swivelase)

A

Topotecan, Irinotecan

254
Q

Chemotherapeutic drug that interferes with mitotic spindle and prevents microtubule disassembly into tubulin monomers

A

Paclitaxel, Docetaxel

255
Q

Antitumor antibiotic that intercalates between base pairs, inhibits topoisomerase II and generates free radicals

A

Doxorubicin, Daunorubicin, Idarubicin, Epirubicin, Mitoxantrone

256
Q

Antitumor antibiotic that generates free radical which cause DNA strand breaks and intercalates with DNA

A

Bleomycin

257
Q

Antitumor antibiotic that binds to double-stranded DNA and inhibits DNA-dependent RNA synthesis

A

Actinomycin D

258
Q

Anticancer drug that inhibits tyrosine kinase activity of the protein product of bcl-abl oncogene in CML and c-kit tyrosine kinase in GIST

A

Imatinib, Dasatinib, Nilotinib

259
Q

Anticancer drug that acts against breast cancer cells that over-express the HER-2/neu receptor for epidermal growth factor (EGF)

A

Trastuzumab

260
Q

Anticancer drug that inhibits binding of VEGF to VEGFR leading to inhibition of VEGF signaling; inhibits tumor vascular permeability but enhances tumor blood flow and drug delivery

A

Bevacizumab

261
Q

Anticancer drug that binds to a surface protein in NHL cells inducing complement-mediated lysis, direct cytotoxicity and induction of apoptosis

A

Rituximab

262
Q

Anticancer drug that depletes serum asparagine

A

Asparaginase

263
Q

Anticancer drug that allows DNA transcription and differentiation of immature leukemic promyelocytes into mature granulocytes

A

All-trans retinoic acid

264
Q

Neutralize stomach acid by reacting with protons in the lumen of the gut

A

Magnesium-aluminum hydroxide

265
Q

Irreversible blockade of H/K/ATPase in active gastric parietal cells causing long-lastng reduction of meal-stimulated and nocturnal acid secretion

A

Omeprazole, Lansoprazole, Rabeprazole, Pantoprazole, Esomeprazole

266
Q

Binds to injured tissue and forms a protective covering over ulcer beds accelerating healing of peptic ulcers and reduces recurrence rate

A

Sucralfate

267
Q

Forms a protective coating on ulcerated tissue; stimulates mucosal protective mechanisms, direct antimicrobial effects and sequestration of enterotoxins

A

Bismuth salicylate

268
Q

Soften stool material permitting water and lipids to penetrate

A

Docusate, Glycerine, Mineral oil

269
Q

Indigestible, hydrophillic colloids that absorb water forming a bulky, emollient gel that distends the colon and promotes peristalsis

A

Psyllium, Methylcellulose, Polycarbophil

270
Q

Soluble but nonabsorbable compounds that result in increased stool liquidity due to an obligate increase in fecal fluid

A

Lactulose, Magnesium oxide, Sorbitol, Magnesium citrate, Sodium phosphate, Polyethylene glycol

271
Q

Chemo drugs that bind and inhibit EGF receptors

A

Transtuzumab (breast)
Cetuximab (colon)
Bevaxizumab (head and neck)

Pharmacology (4 decks)

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