Antianginal

Question 1

Isosorbide Mononitrate

Answer 1

CLASS:Organic Nitrates

MOA:Mimic the action of endogenous NO

Rapid reduction in myocardial O2 demand [via systemic
vasodilation] and relief of
symptoms

Nitrates activate guanylyl 
cyclase
Functions of NO:
Vasodilation
Anti-thrombotic
Anti-inflammatory

USES:Indicated for ALL anginas, Oral prophylaxis of angina

AE:HA→ cerebral vasodilation
Postural hypotension
Flushing
Reflex tachycardia

Desensitization/overcome
tolerance → “nitrate free
interval” of 10-12 hours needed

Contraindicated in pts taking
Sildenafil!Inhibits PDE5
which breaks down
cGMP leading to an even greater increase in cGMP

Question 2

Isosorbide Dinitrate

Answer 2

CLASS:Organic Nitrates

MOA:Mimic the action of endogenous NO

Rapid reduction in myocardial O2 demand [via systemic
vasodilation] and relief of
symptoms

Nitrates activate guanylyl 
cyclase
Functions of NO:
Vasodilation
Anti-thrombotic
Anti-inflammatory

USES:Indicated for ALL anginas, Ongoing Attack

AE:HA→ cerebral vasodilation
Postural hypotension
Flushing
Reflex tachycardia

Desensitization/overcome
tolerance → “nitrate free
interval” of 10-12 hours needed

Contraindicated in pts taking
Sildenafil!Inhibits PDE5
which breaks down
cGMP leading to an even greater increase in cGMP

Question 3

Nitroglycerin

Answer 3

CLASS:Organic Nitrates

MOA:Mimic the action of endogenous NO

Rapid reduction in myocardial O2 demand [via systemic
vasodilation] and relief of
symptoms

Nitrates activate guanylyl 
cyclase
Functions of NO:
Vasodilation
Anti-thrombotic
Anti-inflammatory

USES:Indicated for ALL anginas IV→ unstable angina and
acute HF
Sublingual→ 1st line
treatment of acute SXS

AE:HA→ cerebral vasodilation
Postural hypotension
Flushing
Reflex tachycardia

Desensitization/overcome
tolerance → “nitrate free
interval” of 10-12 hours needed

Contraindicated in pts taking
Sildenafil!Inhibits PDE5
which breaks down
cGMP leading to an even greater increase in cGMP

Question 4

Sodium

Nitroprusside

Answer 4

CLASS:Organic Nitrates

MOA:Mimic the action of endogenous NO

Rapid reduction in myocardial O2 demand [via systemic
vasodilation] and relief of
symptoms

Nitrates activate guanylyl 
cyclase
Functions of NO:
Vasodilation
Anti-thrombotic
Anti-inflammatory

USES:Indicated for ALL anginas,Direct NO donor→ HTNemergencies & severe HF in
emergency settings

AE: Severe, nausea, vomiting, HA, cyanide poisoning

Question 5

Acebutolol

Answer 5

CLASS: B-blocker

MOA:↓ heart rate and contractility
↓ O2 demand
↓ frequency and severity of stable/unstable
angina attacks [RAAS not as important here
as in HTN]

USES:Recommended in ‘all’ pts with stable angina who have LV dysfunction

AE:Rebound HTN or angina if drug is discontinued abruptly [upregulate receptors]

Contraindicated in asthma, COPD, Diabetes, PVD
Sinus bradycardia/partial AV block & Prinzmetal angina

Question 6

Atenolol

Answer 6

CLASS: B-blocker, B1 cardioselective

MOA: ↓ heart rate and contractility
↓ O2 demand
↓ frequency and severity of stable/unstable
angina attacks [RAAS not as important here
as in HTN]

USES:Recommended in ‘all’ pts with stable angina who have LV dysfunction

AE:Rebound HTN or angina if drug is discontinued abruptly [upregulate receptors]

Contraindicated in asthma, COPD, Diabetes, PVD
Sinus bradycardia/partial AV block & Prinzmetal angina

Question 7

Metoprolol

Answer 7

CLASS: B-blocker, B1 cardioselective

MOA:↓ heart rate and contractility
↓ O2 demand
↓ frequency and severity of stable/unstable
angina attacks [RAAS not as important here
as in HTN]

USES:Recommended in ‘all’ pts with stable angina who have LV dysfunction

AE:Rebound HTN or angina if drug is discontinued abruptly [upregulate receptors]

Contraindicated in asthma, COPD, Diabetes, PVD
Sinus bradycardia/partial AV block & Prinzmetal angina

Question 8

Propranolol

Answer 8

CLASS: B-blocker, NOT Cardioselective

MOA:↓ heart rate and contractility
↓ O2 demand
↓ frequency and severity of stable/unstable
angina attacks [RAAS not as important here
as in HTN]

USES:Recommended in ‘all’ pts with stable angina who have LV dysfunction

AE:Rebound HTN or angina if drug is discontinued abruptly [upregulate receptors]

Contraindicated in asthma, COPD, Diabetes, PVD
Sinus bradycardia/partial AV block & Prinzmetal angina

Question 9

Amlodipine

Answer 9

CLASS: calcium channel blocker, cardioselective

MOA:Entry of Ca2+ via L-type channel blocked→ ↓smooth muscle tone & PVR→
arteriolar vasodilation→ ↓BP
-used in combo with B-blockers when B-blockers are not successful or is
contraindicated

USES: DOC for Variant Angina

AE:Flushing, Reflex tachycardia, HA,
Hypotension, Peripheral edema, Constipation, Bradycardia, AV
block, anorexia, constipation,
edema

Question 10

Felodipine

Answer 10

CLASS: calcium channel blocker, cardioselective

MOA:Entry of Ca2+ via L-type channel blocked→ ↓smooth muscle tone & PVR→
arteriolar vasodilation→ ↓BP
-used in combo with B-blockers when B-blockers are not successful or is
contraindicated

USES: DOC for Variant Angina

AE:Flushing, Reflex tachycardia, HA,
Hypotension, Peripheral edema, Constipation, Bradycardia, AV
block, anorexia, constipation,
edema

Question 11

Nifedipine

Answer 11

CLASS: calcium channel blocker, cardioselective

MOA:Entry of Ca2+ via L-type channel blocked→ ↓smooth muscle tone & PVR→
arteriolar vasodilation→ ↓BP
-used in combo with B-blockers when B-blockers are not successful or is
contraindicated

USES: DOC for Variant Angina,

AE:Flushing, Reflex tachycardia, HA,
Hypotension, Peripheral edema, Constipation, Bradycardia, AV
block, anorexia, constipation,
edema

Should always be used with B-blockers to avoid reflex tachycardia

Question 12

Verapamil

Answer 12

CLASS: calcium channel blocker, cardioselective

MOA:Slows AV conduction directly→ ↓HR, contractility, BP, O2 demand
-cardioselective!greatest depressant effect on heart

USES: DOC for Variant Angina

AE:Verapamil/Diltiazem:
Contraindicated in pts w/
preexisting depressed cardiac
function or AV conduction
abnormalities
Use with caution in pts taking
digoxin

Question 13

Diltiazem

Answer 13

CLASS: calcium channel blocker, cardioselective

MOA:Slows AV conduction directly→ ↓HR, contractility, BP, O2 demand
-cardioselective!greatest depressant effect on heart

USES: Slows AV conduction similar to Verapamil, but decreases HR to a lesser extent

AE:Verapamil/Diltiazem:
Contraindicated in pts w/
preexisting depressed cardiac
function or AV conduction
abnormalities
Use with caution in pts taking
digoxin

Question 14

Ranolazine

Answer 14

CLASS: Na Channel Blocker

MOA:↓ contractility
↓ O2 demand
May modify fatty acid oxidation

Metabolized by CYP3A4

USES:Prophylaxis for pts in which all other antianginal
therapies have failed

AE:QT prolongation
Nausea, constipation
Dizziness

Contraindicated in pts with
prolonged QT! torsade’s de
pointes and ventricular
tachyarrhythmia