Antianginals and Antiplatelets

Question 1

nitroglycerin

Answer 1

minitran/nitrostat/nitro-dur is a venodilator used to treat angina, hf and htn

Question 2

venodilator moa

Answer 2

forms NO increases cGMP causing smooth muscle relaxation producing a vasodilation effect with primary effect on veins

Question 3

venodilator contraindications

Answer 3

use with phosphodiesterase inhibitors (ex: sildenafil, tadalafil)

Question 4

venodilator adr

Answer 4

ha, dizziness, syncope
nitrates also risk reflex tachycardia and increase in contractility

Question 5

venodilator notes

Answer 5

low oral bioavailability due to first pass metabolism- needs formulations to bypass
available as SL tablet, spray, ointment, etc.
SL/spray- sit before taking medication, dissolve one tab under tongue or spray every 5 minutes for up to 3 doses

Question 6

SL/spray nitroglycerin

Answer 6

instant acting (1-3 minute onset), lasts only 10-30 minutes

Question 7

nitrogylcerin ointment

Answer 7

onset of 15-30 minutes, lasts 3-6 hrs

Question 8

PK/PD of nitrates

Answer 8

all nitrate develop tolerance (tachyphylaxis)- worse with long acting preparations, beneficial effects do not last longer than 8-10 hrs
tolerance is due to diminished release of NO and systemic compensation

Question 9

Nitroglycerin storage

Answer 9

SL nitroglycerin is volatile and can adsorb to plastic surfaces- should be kept in tightly closed glass container

Question 10

wait time for dosing of avanafil (stendra) and nitroglycerin

Answer 10

12 hrs

Question 11

wait time for dosing of sildenafil (Viagra, revatio) and nitroglycerin

Answer 11

24 hrs

Question 12

wait time for dosing of vardenafil (levitra, staxyn) and nitroglycerin

Answer 12

24 hrs

Question 13

wait time for dosing of tadalafil (adcirca, cialis) and nitroglycerin

Answer 13

48 hrs

Question 14

DHP CCB

Answer 14

amlodipine (norvasc), nifedipine (procardia), may cause reflex sympathetic activation/tachycardia, amlodipine might take a full week to take effect, major CYP3A4 substrate

Question 15

NON-DHP CCB

Answer 15

diltiazem (cardizem), verapamil (calan), additional AV nodal blockage, do not use with 2nd or 3rd degree heart block, verapamil has greatest depressant effects on SNS, diltiazem has modest effects, major CYP3A4 substrates, moderate CYP3A4 inhibitors, DDI worse with verapamil

Question 16

beta blockers

Answer 16

metoprolol (lopressor, toprol XL), may cause severe bradycardia, receptor selectivity, additive AV nodal blockage with NONDHP CCB, avoid abrupt withdrawal, may mask feelings of hypoglycemia, fatigue will abate over time

Question 17

ranolazine

Answer 17

ranexa is a antianginal used to treat angina

Question 18

antianginal moa

Answer 18

inhibits late phase of inward Na, reducing intracellular Na concentration and Ca influx, decreasing contractility of the heart and O2 requirement

Question 19

antianginal contraindications

Answer 19

hepatic cirrhosis, concurrent use of strong CYP3A4 inhibitors or inducers

Question 20

antianginal adr

Answer 20

constipation, nausea, qt prolongation

Question 21

antianginal ddi

Answer 21

weak inhibitor of cyp3a4 and cyp2d6

Question 22

antianginal notes

Answer 22

little to no impact on blood pressure and heart rate, mainly decreases myocardial contractile force

Question 23

aspirin

Answer 23

antiplatelet used to treat IHD and stroke

Question 24

aspirin moa

Answer 24

inhibits COX 1 and 2, irreversibly inhibits formation of thromboxane A2 needed for platelet aggregation

Question 25

aspirin contraindications

Answer 25

n/a

Question 26

aspirin adr

Answer 26

bleeding

Question 27

aspirin notes

Answer 27

onset for non-enteric coded: <1hr, onset for enteric: 3-4 hrs, onset for chewed: 20 minutes. Irreversible inhibitor- needs to create new platelets for them to work again

Question 28

aspirin ddi

Answer 28

increased bleed risk with other antiplatelets, anticoagulants and NSAIDs

Question 29

clopidogrel

Answer 29

plavix is a P2Y12 inhibitor used for CAD, ischemic stroke, and PAD- irreversibly binds, variable effect based on CYP2C19 activity

Question 30

prasugrel

Answer 30

effient is a P2Y12 inhibitor used for CAD, ischemic stroke, and PAD. Irreversibly binds
contraindicated with history of TIA or stroke

Question 31

ticagrelor

Answer 31

Brilinta is a P2Y12 inhibitor used to treat CAD, ischemic stroke, and PAD, reversible, allosteric binder
contraindicated with history of intracranial hemorrhage, sever liver disease
max aspirin daily dose: 100mg

Question 32

P2Y12 contraindications

Answer 32

active bleeding (all)

Question 33

P2Y12 adrenaline

Answer 33

minor and major bleeding including intracranial hemorrhage, thrombotic thrombocytopenic purpura

Question 34

P2Y12 DDI

Answer 34

increased risk of bleeding with other antiplatelets, anticoagulants, and NSAIDs

Question 35

P2Y12 notes

Answer 35

severe bleeding can occur- rare- contact doctor for bleeding that wont stop- may experience easy bruising or bleeding, avoid taking with NSAIDs

Question 36

Clopidogrel PK/PD

Answer 36

irreversible binding to ADP receptor site, prodrug, onset of 2-6 hrs, peak 300mg load at 6hrs, peak 600 mg load at 2 hrs, converted by a 2 step process involving CYP2C19

Question 37

prasugrel PK/PD

Answer 37

irreversible binding to ADP receptor site, prodrug, onset of 30min, 60 mg load peak in 1 hr, 90-70% platelet inhibition

Question 38

ticagrelor PK/PD

Answer 38

reversible allosteric binder, not a prodrug, onset of 30 minutes, 180mg load peak <1hr, CYP3A4 metabolism, 60-70% platelet inhibition