PDA B2 Drugs & Terms Flashcards

Question

Aspirin / Acetylsalicylic Acid / ASA

Answer 1

Class: NSAID Action: Prodrug to Salicylic acid, Irreversible inhibitor of COX-2 via acetylation of Ser230 Use: Anti-inflammatory, Analgesia, Anti-pyretic; dose dept. uricosuric effects - compete with urate transporter @ high doses Route: Oral (IV available). Chewing increases absorption rate Other Preparations: Buffered (less pH alteration in stomach) and enteric (dissolves in intestines, bypassing potl. Stomach irritation) Elim: Renal S/E: GI irritation,

Answer 2

Class: 5-HT agonist Action: Rel. Nonspecific 5-HT2 receptor agonist. Potent hallucinogen

Answer 3

Class: 5-HT agonist Action: 5-HT1A receptor partial agonist Use: Antianxiety

Answer 4

AKA: Imitrex Class: 5-HT agonist Action: 5-HT1D receptors on cerebral blood vessels. Inhibit CGRP release, promote vasoconstriction. Use: Treatment of existing migraine headaches. S/E: GI effects, dizziness, flushing, angina Contra: Recent Mi

Answer 5

Class: Indirect 5-HT agonist Action: SSRI, increases 5-HT in synapse by preventing reuptake Use: Affective disorders, OCD, panic attacks S/E: Sexual dysfunction, nausea

Answer 6

Class: Indirect 5-HT agonist Action: inhibits MAO, blocking metabolism of 5-HT, NE, DA. Use: Affective disorders, narcolepsy (NE) S/E: Hypertensive crisis

Answer 7

Class: 5-HT Antagonist Action: 5-HT2 receptor antagonist AND histamine H1 antagonist Use: Allergies, pruritis, urticaria, carcinoid syndrome (5-HT producing tumor)

Answer 8

Class: 5-HT antagonist Action: 5-HT3 Use: Treats post-chemo nausea and vomiting via CNS and GI action

Answer 9

Class: 5-HT antagonist Action: 5-HT3 Use: Diarrhea - typically IBS in women S/E: Potential severe GI effects; prescribing is restricted

Answer 10

Class: Phenylalkylamine CCB Action: Binds deep within L-Type Ca2+ Channel (a1 subunit), use-dependent, slows SA firing and AV conduction with some coronal and periph. vasodilation Use: Supraventricular arrhythmias (incl. Supravent. Tachycardia) Route: Oral (high first pass effect) or IV S/E: Hypotension, headache, flushing, edema, CONSTIPATION, may exacerbate CHF or cause AV block Int: Other CCBs

Answer 11

Class: Benzothiazepine CCB Action: Binds deep within L-Type Ca2+ Channel (a1 subunit), use-dependent, slows SA firing and AV conduction with some coronal and periph. vasodilation Use: Supraventricular arrhythmias, angina, cardiac ischemia Route: Oral (low first pass effect) or IV S/E: Hypotension, headache, flushing, edema, may exacerbate CHF or cause AV block Int: Other CCBs

Answer 12

Class: 1,4-Dihydropyridine CCB Action: Binds SURFACE of L-Type Ca2+ Channel (a1 subunit) of ARTERIES (not veins), voltage-dependent, cause coronary and peripheral vasodilation Use: Hypertension, often with a beta blocker (propranolol) Route: Oral (low first pass effect) or IV S/E: Reflex tachycardia (treat w/ propranolol) Contra: tachyarrythmias Int: Other CCBs

Answer 13

Class: 1,4-Dihydropyridine CCB Action: Slow-acting, binds SURFACE of L-Type Ca2+ Channel (a1 subunit) of ARTERIES (not veins), voltage-dependent, cause coronary and peripheral vasodilation Use: Hypertension, often with a beta blocker (propranolol) Route: Oral (half-life compatible with 1x/day) S/E: Reflex tachycardia - slow acting, so less so than Nifedipine Contra: tachyarrythmias Int: Other CCBs

Answer 14

Class: Renal vasodilator (diuretic) Action: Increase RBF w/o changing GFR (decrease filtration fraction) and decrease prox. Tubule Na+ reabsorption, weak diuretics Use: Limited - Hypertensive crisis & shock Route: Some orally active

Answer 15

Class: Osmotic Diuretic Action: Act in tubular lumen as freely filtered, non-reabsorbable solute, osmotically increases excretion of Na, K, Cl, H2O, mannitol Use: Edema, Glaucoma, Acute renal failure Route: IV ONLY S/E: Hypokalemia (?)

Answer 16

Class: Carbonic Anhydrase Inhibitor Action: Filtered & secreted by organic acid transporter (OAT) into lumen, inhib, CA in prox. And dist. Tubule, increase excretion of Na, K, bicarb, and H2O Use: Glaucoma, alkalinize urine (dec. drug toxicity), altitude sickness, anticonvulsant - acidosis inhibits effects Route: Oral S/E: Metab. Acidosis, Hypokalemia

Answer 17

Class: Loop Diuretics Action: Filtered/secreted by OAT, inhibits Na-K-2Cl symporter, increase excretion of Na, K, Cl, H2O in medullary and cortical parts of ascending loop of Henle; rapid, powerful (20-30% Na), and short-acting Use: cardiac, renal, hepatic, or pulmonary edema; hypertension Route: Oral and IV S/E: Hypokalemia, Alkalosis, Hypovolemia, Hyperuricemia, Hyperglycemia (furosemide only), Ototoxicity

Answer 18

Class: Thiazide-like Diuretics Action: Excreted/secreted by OAT, Inhibits Na-Cl symporter, cortical segment of dist. Tubule, incr. excretion of Na, K, Cl, H2O, long acting and moderate excretion (8-10% Na) - hypertonic urine, unable to dilute Use: Edema from CHF, hypertension, hypercalciuria Route: Oral S/E: Hypokalemia, Alkalosis, Hyperuricemia, Hyperglycemia, Decrease GFR

Answer 19

Class: Aldosterone Antagonist / K+ Sparing Diuretic Action: Block aldosterone's effect on collecting duct, incr. Na excretion (2-3% of load) along with Cl and H2O, but WITHOUT K Use: Edema, Hypertension, Improve survival in CHF, Used in combination with a more potent diuretic Route: Oral S/E: Hyperkalemia, Gynecomastia (mostly spironolactone)

Answer 20

Class: Na+ Channel Inhib. / K+ Sparing Diuretic Action: Block Na entra into principal cells of collecting duct, increase Na (2-3% of load), Cl, and H2O excretion w/o K loss Use: Edema, Hypertension, often used in combination with a more potent diuretic Route: Oral S/E: Hyperkalemia, Mild azotemia, Triamterene reduces RBF and GFR at high doses

Answer 21

Class: Anti-coagulant Action: Mix of sulfated polysaccharides, neg. charged. Increases rate of antithrombin 1000x by making active site more accessible to coagulation factors. Prevents clots, DOES NOT degrade clots. Use: Acute venous thromboembolism, Cardiopulmonary bypass, prophylaxis against venous thrombosis Route: IV or SQ S/E: Bleeding, THROMBOCYTOPENIA (1-5%) Contra: Bleeding, Uncontrolled HTN, Recent surgery of eye, brain, spinal cord Note: does not cross placenta; useable during pregnancy

Answer 22

AKA: Low-MW heparins Class: Anticoagulants Action: Poorly inhibits Thrombin via AT, but still significantly inhibits factor Xa via AT Use: Acute & Prophylaxis for AVT, Acute unstable angina / MI, hip replacement surgery Route: Parenteral S/E: Bleed and thrombocytopenia risk lower than heparin Contra: Bleeding, Uncontrolled HTN, Eye/Brain/Spinal Cord surgery, Renal impairment (metabolism)

Answer 23

Class: Anticoagulants Action: Direct inhibition of thrombin - blocks substrate binding site Route: IV Use: Same as other anticoagulants; heparin replacement for pts who have had thrombocytopenia S/E: Bleeding Contra: Same as other anticoagulants; Renal impairment (metabolism)

Answer 24

Class: Anticoagulant Action: Directly inhibits Factor Xa Use: DVT prevention during surgery, acute PE, acute DVT w/o PE Route: SQ S/E: Same as other anticoagulants Contra: Same as others; renal impairment (excreted)

Answer 25

Class: Heparin antagonist Action: Positively charged - binds and inactivates heparin 1:1 Use: Heparin OD w/ severe bleeding, reverse heparin after bypass surgery S/E: Anaphylaxis (fish products, some insulin preps), severe pulmonary HTN, weak anticoagulant itself at high doses or alone

Answer 26

Class: Anticoagulant Action: Vitamin K analogue - inhibition of VKORC1 prevents gamma-carboxylation (requires Vit K reduced) of prothrombin, factors VII, IX, X, Proteins C and S, impairing their functions. Affects synthesis, so takes up to days to be therapeutic. Use: thromboembolism prophylaxis (Afib, prosthetic heart valves, dilated cardiomyopathy), venous TE treatment Route: Oral Metab: Liver CYP2C9 (*2 and *3 less active; drug/food interactions!), highly plasma protein bound S/E: Bleeding, Purple Toe Syndrome, skin necrosis / gangrene (protein C deficiency) Contra: Heparin contras, but also: CYP2C9 polymorph, VKORC1 variations, pregnancy (teratogen), liver/kidney diseases, Vit K deficiency

Answer 27

Class: Anticoagulant (Etexilate is given prodrug, via hydrolysis by esterase) Action: Binds active site of both free AND fibrin-bound thrombin. Shorter T1/2 than warfarin Use: Nonvalvular Afib w/ risk of stroke or embolism; prophylaxis in knee/hip replacement pts Route: Oral Monitoring: NONE S/E: Bleeding (less than warfarin, but NO antidote), GI upset Contra: Renal disease (Metab), liver disease (baseline coagulation impaired), PROSTHETIC HEART VALVES Drug Int: Drugs that induce (rifampin) or inhibit (verapamil, quinidine, others) P-glycoprotein

Answer 28

Class: Anticoagulant Action: Directly binds and inhibits free and complexed/clot-bound Factor Xa (Pockets S1 and S4) to inhibit more thrombin activation - does not affect existing thrombin. Rapid onset and long duration. Use: Same as dabigatran Route: Oral S/E: Bleeding Monitoring: If needed (high risk), PT time Metab: Hepatic CYP3A4/5, 2J2; Kidney AS WELL Int: P-gp-affecting drugs

Answer 29

AKA: Recombinant Tissue Plasminogen Activator (t-PA) Class: Thrombolytic Action: Activates plasminogen to plasmin in order to lyse fibrin at a thrombus Use: Acute MI, PE, DVT, Stroke Route: IV (very short T1/2) S/E: Bleeding (lyse thrombi; systemic lytic state). Greater risk in long term treatment. Contra: Bleeding, Hx of cerebrovascular trouble, uncontrolled HTN, recent spinal cord surgery or trauma, brain tumor

Answer 30

Class: Procoagulant: Plasminogen Inhibitor Action: Binds Lys-binding sites on plasmin(ogen) to inhibit plasmin binding to fibrin Use: Reverse acute bleeding effects of excessive fibrinolysis; conc. in urine so useful in stopping urinary tract bleeding

Answer 31

Class: Anti-platelet Action: Inhibits PDE3/5 to increase cAMP in platelets, inhibiting their aggregation. Also a vasodilator. Use: prophylaxis of thromboemboli in pts with prosthetic heart valves S/E: Headache, GI upset; secondary prevention of MI or TIA

Answer 32

Class: Anti-platelet Action: via P2Y1/12 receptors, inhibit ADP-induced platelet aggregation. All irrev. EXCEPT Ticagrelor. Prasugrel: prodrug activated by esterase and then CYP3A4 & 2B6. Clopidogrel and Ticlopidine are prodrugs activated by CYP2C19. Use: Angina, NSTEMI, STEMI, MI, Stroke, Periph. Vascular disease, manage pts during surgery Route: Oral SE: Bleeding; Ticagrelor - dyspnea; Ticlopidine - neutropenia (not used often) Int: CYP metabolized drugs!!! See: Clopidogrel + aspirin + omeprazole

Answer 33

Class: antihistamine Action: stabilizes mast cell membranes to prevent histamine release Use: chronic control of asthma, bronchospasm prophylaxis, not for acute attack Route: inhalation (also oral - mastocytosis, nasal - allergies, opthalmic - conjunctivitis) S/E: Few

Answer 34

``` Class: antihistamine Action: IgG mAb that binds circulating IgE (Fc region) to prevent mast cell activation Use: asthma? Route: SQ S/E: injection site rxn, anaphylaxis ```

Answer 35

Aka: Benadryl Class: Antihistamine (ethanolamine, 1st gen) Action: H1 receptor blocker / inverse agonist. Inhibits capillary permeability but not BP or bronchoconstriction. CNS anticholinergic effects. Use: allergies (rhinitis, uritcaria, conjunctivitis), non-prescription sleep aid, early stage Parkinson's Route: oral, nasal, opthalmic S/E: profound sedation, paradoxical stimulation in children / overdose, atropine-like effects

Answer 36

Aka: Dramamine Class: Antihistamine (ethanolamine, 1st gen) Action: H1 receptor blocker / inverse agonist. CNS anticholinergic effects. Use: Motion sickness, vestibular disorders Route: oral, IV S/E: sedation, paradoxical stimulation in children / overdose, atropine-like effects

Answer 37

Class: Antihistamine (alkylamine, 1st gen) Action: H1 receptor blocker / inverse agonist. Inhibits capillary permeability but not BP or bronchoconstriction. CNS anticholinergic effects. Use: allergies (rhinitis, uritcaria, conjunctivitis) - among most potent, with less drowsiness than diphenhydramine Route: Oral, IV, IM, SQ S/E: sedation, paradoxical stimulation in children / overdose, atropine-like effects

Answer 38

Class: Antihistamine (phenothiazine, 1st gen) Action: H1 receptor blocker / inverse agonist, ALSO Dopamine2 blocker. CNS anticholinergic effects. Use: motion sickness, chemo-induced nausea/emesis Route: oral, IV, topical, IM, rectal S/E: profound sedation, paradoxical stimulation in children / overdose, atropine-like effects

Answer 39

AKA: Allegra Class: antihistamine (piperidine, 2nd gen) Action: Terfenadine is the prodrug. H1 receptor inverse agonist Use: Allergies (rhinitis, urticaria, conjunctivitis) Route: Oral S/E: Unlike 1st gens, little anticholinergic or sedative effects in brain (little crosses BBB)

Answer 40

Aka: Claritin / Clarinex (Des- form) Class: antihistamine (piperidine, 2nd gen) Action: Prodrug of the active Desloratidine. H1 receptor inverse agonist Use: Allergies (rhinitis, urticaria, conjunctivitis) Route: Oral S/E: Unlike 1st gens, little anticholinergic or sedative effects in brain (little crosses BBB) Metab: into ACTIVE form by liver CYP3A4/2D6

Answer 41

Aka: Zyrtec Class: antihistamine (piperazine, 2nd gen) Action: hydroxyzine is the prodrug. H1 receptor inverse agonist Use: Allergies (rhinitis, urticaria, conjunctivitis) Route: Oral S/E: Unlike 1st gens, little anticholinergic effect in brain (little crosses BBB). Cetirizine causes most sedation of 2nd gen antihistamines.

Answer 42

Class: Antihistamine (H2) Action: H2 receptor blocker Use: Relief of gastric upset / peptic ulcer disease / GERD via inhibition of gastric acid release by parietal cells. Historic use: Zollinger-Ellison syndrome (now treated with PPI). Least potent of H2 blockers. Route: oral or IV S/E: usually minor. Diarrhea, headache, drowsiness. Rare: confusion, delirium, slurred speech. Long term use in men can causes Gynecomastia, impotence via decrease of T binding and estradiol metab Int: Inhibits CYP enyzymes, prolonging half lives of CYP-metabolized drugs

Answer 43

Class: Antihistamine (H2) Action: H2 receptor blocker Use: Relief of gastric upset / peptic ulcer disease / GERD via inhibition of gastric acid release by parietal cells. Moderate potency among H2 blockers. Route: Oral or IV S/E: usually minor. Diarrhea, headache, drowsiness. Rare: confusion, delirium, slurred speech. Int: Minor inhibition of CYP enzymes (10% of cimetidine), prolonging half lives of CYP-metabolized drugs

Answer 44

Class: Antihistamine (H2) Action: H2 receptor blocker Use: Relief of gastric upset / peptic ulcer disease / GERD via inhibition of gastric acid release by parietal cells. High potency among H2 blockers. Route: Oral or IV S/E: usually minor. Diarrhea, headache, drowsiness. Rare: confusion, delirium, slurred speech.

Answer 45

Class: Direct renin inhibitor Action: active-site, non-peptide inhibitor. Renin only - no inhibition of other aspartic proteases. Decreases plasma angiotensin II and aldosterone levels Use: Hypertension, typically with another drug Route: Oral, 1x/day (T1/2 ~ 24hrs) S/E: Minor / similar to placebo: fatigue, headache, GI symptoms

Answer 46

Class: AT1 receptor blocker Action: competitive angiotensin receptor 1 antagonist. No effect on AT2 receptors. Use: Essential hypertension, heart failure (lowers afterload), cardiac fibrosis/hypertrophy (lowers preload). Does not cause hyperkalemia. Route: oral S/E: dizziness, cough, angioedema, hypotension (esp. w/ diuretics) Contra: Pregnancy

Answer 47

Class: ACE inhibitors Action: inhibit angiotensin I converting enzyme, blocking ATII and bradykinin degradation Use: Essential hypertension (lower BP w/o increasing HR), heart failure (reduces afterload), cardiac fibrosis/hypertrophy (reduces preload). Increases CO. Route: Oral S/E: cough, angioedema. Captopril: rash, proteinuria, neutropenia. Lowers aldosterone release to hyperkalemia may occur (can use to offset diuretic-caused hypokalemia) Metab: Enalapril and Lisinopril are prodrugs of the active enaprilate and lisinoprilate, respectively.

Answer 48

Class: anticoagulant Action: Fab fragment of mAb that binds platelet GP IIb/IIIa receptor to NON-COMPETITIVELY inhibit fibrinogen binding and cross-linking Use: prevent thrombosis in coronary angioplasty & stent placement (w/ aspirin and heparin) Route: IV S/E: bleeding, thrombocytopenia, hypotension, bradycardia

Answer 49

Class: anticoagulant Action: binds platelet GP IIb/IIIa receptor to COMPETITIVELY, REVERSIBLY inhibit fibrinogen binding and cross-linking ( novel KGD aa sequence, from rattlesnake venom) Use: prevent coronary thrombosis in unstable angina & MI (w/ LMWH), or during coronary angioplasty / stent placement Route: IV S/E: bleeding, thrombocytopenia, hypotension, bradycardia Contra: renal disease (renal clearance)

Answer 50

Class: nitrates Action: relaxation of arterial and venous (dominant) SM via donation of NO Use: heart failure Route: oral, IV, sublingual, topical/transdermal S/E: hypotension

Answer 51

Class: nitrates Action: relaxation of arterial and venous SM via donation of NO Use: heart failure, hypertensive emergencies Route: IV S/E: hypotension

Answer 52

Class: direct vasodilators Action: dilates ARTERIAL SM by binding and activating K+ channels, causing K+ efflux that hyperpolarizes the cells. Increases cGMP. Use: heart failure, hypertensive emergencies Route: oral, IV S/E: hypotension, headache, tachycardia

Answer 53

``` Aka: Rogaine Class: direct vasodilators Action: K+/ATP channel opener, hyperpolarizes arterial SM; hair growth Use: severe HTN; alopecia Route: oral; topical S/E: fluid retention - use with diuretic ```

Answer 54

``` Class: antihypertensive Action: causes K+ efflux to hyperpolarize SM cells; inhibits insulin secretion Use: HTN emergencies, hypoglycemia Route: oral, IV S/E: ```

Answer 55

``` Class: phosphodiesterase inhibitors Action: inhibit PDE3 to increase cAMP levels in cardiac myocytes, increasing contractility. Also vasodilator effects. Use: heart failure Route: IV, Cilostazol oral S/E: ```

Answer 56

``` Class: phosphodiesterase inhibitors Action: inhibit PDE5 to increase cGMP levels and cause vasodilation of SM Use: Erectile dysfunction Route: oral S/E: ```

Answer 57

Action: b2 adrenergic agonists - promote bronchodilation via cAMP/PKA increase Use: acute asthma attacks, COPD Route: inhalation S/E: tachycardia

Answer 58

``` Class: bronchodilators Action: adenosine receptor antagonists & PDE inhibitors to increase cAMP and cause bronchodilation Use: asthma and COPD Route: oral, IV S/E: ```