CV: DRUGS FOR ANGINA PECTORISDRUG ADMINITRATION INDICATION MOA ADVERSE EFFECT

1. Nitratesa. Nitroglycerin SL, spray, transdermal patch, oral

(BA: 10-20%), IV infusion SL

Avoid 1st pass Achieve therapeutic blood

level rapidly Onset: 2 min

Cornerstone of angina therapy, most commonly used

All forms of angina

Must be taken at the onset of anginal pain or prior to Px anginal episodes

converted to nitric oxide (NO) à inc. cGMP à smooth muscle relaxation à vasodilation

orthostatic hypotension, tachycardia and throbbing headache

Tolerance ↓ tissue SH ↑ oxygen free radicals Tx: “nitrate-free peroid”: ≥ 8

hours bet. dosesb. Amyl nitrite Inhalation Relieve Sx of acute anginac. Isosorbide dinitrate,

mononitrate SL, oral Px of angina

NOT for acute attack1. Calcium Channel Blockers

Nifedipine, Amlodipine, Nicardipine,

Diltiazem, Verapamil

- DOC for Prinzmetal’s angina relieve and Px the primary cause

of variant angina—focal coronary artery spasm

cardiac arrest, bradycardia, AV block and HF (↑↑ Ca2+ influx)

2. β Blockers Propranolol, Metoprolol,

Atenolol, Nadolol, Timolol, Acebutolol,

Betaxolol, Bisoprolol, Pindolol, LabetALOL,

Penbutolol

DOC stable angina For improved exercise tolerance

↓ HR, contractionà ↓ CO à ↓ O2

demand ↑ in diastolic volume and ejection

time

3. Sodium Channel Blocker Ranolazine

Alone or in combination Tx chronic angina Tx refractory angina

Inhibits late phase Na+ current à ↑ O2 supply à ↓ intracellular Na and Ca à improved diastolic fx