Anti-anginal and anti-thrombotic drugs

Question 1

4 anti-platelets?

Answer 1

clopidogrel (plavix)
ticagrelor
prasugrel
aspirin

Question 2

MOA: irreversibly blocks P2Y component of ADP receptors on platelet surface, prevents activation of GPIIb/IIIa receptor complex & reduces platelet aggregation

Answer 2

clopidogrel, an anti-platelet

Question 3

distinguishing characteristics: Metabolized extensively hepatic via esterase-mediated hydrolysis to a carboxylic acid derivative (inactive) and via CYP450-mediated (CYP2C19, primarily) oxidation to a thiol metabolite (active)
predicted actions: onset is detected by 2nd day of tx, duration lasts for lifespan of platelet
uses: post NSTEMI, ACS, CVA, PCI, arterial occlusive dz to prevent clots
SEs: similar bleeding risk compared to aspirin, slight advantage w/GI bleeds

Answer 3

clopidogrel, an anti-platelet

Question 4

2 NO activating drugs? category?

Answer 4

nitroglycerine
isosorbide mononitrate
both nitrates

Question 5

MOA: relaxation of vascular MS & vasodilation

Answer 5

nitrates: nitroglycerine, isosorbide mononitrate

Question 6

distinguishing characteristics: various forms that change duration and onset, extensive 1st pass metabolism
predicted actions: Onset is 1-3min, 30min (patch), or 60min; duration 25min, 4-8hrs, or 10-12hrs; venous dilation leads to a reduced arterial pressure, reduced preload, reduced oxygen consumption; prefers coronary vessels over peripheral vessels
uses: angina (prophylactic & acute)
SEs: hypotension, H/A, flushing, light-headedness
avoid PDE-5 inhibitors

Answer 6

nitroglycerin

Question 7

distinguishing characteristics: onset is 30-45 mins, lasts >6 hrs, extensive 1st pass metabolism
uses: angina pectoris
SEs: hypotension, flushing, light-headedness

Answer 7

isosorbide mononitrate

Question 8

3 beta blockers?

Answer 8

part of class II drugs
metoprolol
atenolol
propranolol

Question 9

MOA: B1 receptor antagonist
distinguishing characteristics: cardioselective, metabolized through CYP2D6 & 2C19
predicted actions: onset 1 hours, duration 3-6 hrs or 24 hrs in ER form, blunts cardiac stimulation, prevents reflex tachycardia, decreased HR, contractility & BP
uses: MI, CHF, angina, THN
SEs: bradycardia, heart block, H/A, fatigue, eercise intolerance, hypotension, erectile dysfxn
no risk to diabetic or asthmatic pts

Answer 9

metoprolol

Question 10

MOA: B1 receptor antagonist
distinguishing characteristics: limited hepatic metabolism, higher mortality concern unless used w/a silent ischemia then better outcomes
predicted actions: onset <1 hr, duration 12-24 hrs
uses: MI, HTN, angina
SEs: bradycardia, heart block H/A, fatigue, exercise intolerance, hypotension, erectile dysfxn
don’t drink apple juice with!!

Answer 10

atenolol

Question 11

MOA: B1 & B2 receptor antagonist
distinguishing characteristics: very lipid soluble, significant 1st pass metabolism, highly variable plasma levels, metabolized through CYP1A2, 2C19, 2D6, 3A4, inhibits 1A2 & PgP
predicted actions: onset is 12 hrs, duration 6-12 or 24-27 hrs
uses: MI (tx & prevention), HTN, angina, migraine prophylaxis, SV arrhythmias
SEs: bradycardia, heart block, H/A, fatigue, exercise intolerance, hypotension, erectile dysfxn, C/I in diabetic & asthmatic pts

Answer 11

propranolol

Question 12

MOA: non-selective A1 adrenergic blockade

Answer 12

carvedilol
class II drug

Question 13

distinguishing characteristics: Metabolized through CYP1A4, 2C9, 2D6, 2E1, 3A4; inhibits PgP
predicted actions: onset <1 hr, duration 24 hrs
uses: MI, HTN, CHF, angina
avoid grapefruit juice since increases bioavailability

Answer 13

carvedilol

Question 14

3 CCBs?

Answer 14

amlodipine (dihydropyridine)
verapamil (diphenyl alkamine)
diltiazem (benzothiazepine)

Question 15

MOA: blocks Ca2+ influx leading to relaxation of SM, has more effect on peripheral tissues

Answer 15

amlodipine

Question 16

MOA: blocks Ca2+ influx leading to relaxation of cardiac SM, more selective of cardiac tissue compared to others other

Answer 16

verapamil & diltiazem

Question 17

distinguishing characteristics: Metabolized through CYP1A2, 2B6, 2C9, 2E1, 3A4, and PgP; inhibits 1A2, 2C9, 3A4, and PgP
predicted actions: Onset is 1-2hrs; duration 6-8hrs or 24hrs
uses: HTN, chronic stable angina, variant angina, angina in general, SVT, a. fib, a. flutter
SEs: tachycardia, edema, H/A, fatigue, exercise intolerance, hypotension
avoid in pts w/EF <35% in combo w/BB, hypotension, AV block, sick-sinus syndrome, certain arrhythmias

Answer 17

verapamil

Question 18

distinguishing characteristics: Metabolized through CYP2C9, 2D6, 3A4, and PgP; inhibits CYP2C9, 2D6, 3A4
predicted actions: Onset is 15-60min; duration 6hrs or 24hrs
uses: atrial arrhythmia, HTN, SVT, angina
SEs: tachy, edema, H/A, fatigue, exercise intolerance, hypotension
Avoid with patients with an ejection fraction <35% (heart failure), in combination with BB (dec. HR), hypotension, AV block, sick-sinus syndrome, and certain arrhythmias; same interactions as amlodipine

Answer 18

diltiazem

Question 19

MOA: non-selective, irreversible COX inhibitor (acetylation)

Answer 19

aspirin, NSAID

Question 20

distinguishing characteristics: metabolized to salicylate by esterase in the GI mucosa, RBC, synovial fluid & blood, metabolized quickly via hepatic conjugation
uses: MI
SEs: increased GI bleeding, disruption of renal perfusion

Answer 20

aspirin, NSAID

Question 21

MOA: Reversibly blocks the P2Y component of ADP receptors on platelets surface; prevents activation of the GPIIb/IIIa receptor complex and reduces platelet aggregation
distinguishing characteristics: metabolized through CYP3A4
uses: prophylactic use for post ACS, MI or PCI
SEs: increased risk of bleeding, increased uric acid levels
reduced efficacy when used w/aspirin doses >100 mg/d

Answer 21

ticagrelor

Question 22

MOA: Irreversibly blocks the P2Y component of ADP receptors on platelet surface; prevents activation of the GPIIb/IIIa receptor complex and reduces platelet aggregation
distinguishing characteristics: Prodrug that is metabolized to an active metabolite; metabilized rapidly by the intestinal/serum metabolism via esterase-mediated hydrolysis to an inactive intermediate - which is then converted via CYP3A4 and 2B6 to an active metabolite

Answer 22

prasugrel

Question 23

uses: prophylactic use for post ACS, MI or PCI
SEs: avoid in pts who have had a prior TIA or stroke, increased risk for bleeding w/body wt <60 kg

Answer 23

prasugrel

Question 24

5 anticoagulants?

Answer 24

warfarin
rivaroxaban
apixaban
low molecular weight fractionated heparin
dabigatran

Question 25

vitamin K inhibitor
MOA: inhibits vit K oxide reductase
distinguishing characteristics: metabolized through CYP1A2, 2C19, 2C9, 3A4
predicted actions: onset 2-5 d, duration 20-60 hrs
use: decrease clotting risk
interactions w/tons of foods high in vit K

Answer 25

warfarin

Question 26

MOA: direct, reversible inhibition of factor Xa & prevents activation of thrombin
distinguishing characteristics: Metabolized through CYP3A4/5 and 2J2
use: decrease clotting risk
SEs: risk of clotting and INRs can’t be routinely completed

Answer 26

rivaroxaban (xarelto)

Question 27

factor Xa inhibitor
MOA: direct, reversible inhibition of factor Xa & prevents activation of thrombin
distinguishing characteristics: Metabolized through CYP3A4/5 and 1A2, 2C8, 2C9, 2C19, and 2J2; substrate of PgP and BCRP
use: decrease clotting risk
SEs: renal fxn should be monitored, more favorable safety/efficacy profile to warfarin

Answer 27

apixaban (eliquis)

Question 28

MOA: enhances inhibition rate of clotting proteases by antithrombin III, impairing normal homeostasis & inhibition of factor Xa
used as a bridging tx

Answer 28

LMWH

Question 29

factor IIa inhibitor
MOA: direct thrombin inhibitor
distinguishing characteristics: metabolized primarily through renal, pro-drug hydrolyzed to active form hepatically
use: decrease clotting risk
SEs: similar safety/efficacy compared to warfarin, concern for GI bleed, MI

Answer 29

dabigatran