ANTIANGINAL DRUGS

Angina pectoris is a characteristic sudden severe, pressing chest pain radiating to the neck, jaw, back
and arms.
- Caused by coronary blood flow that is insufficient to meet the oxygen demand of the
myocardium, leading to ischemia
- Inadequate blood flow results from occlusion of coronary arteries or coronary artery spasm
Antianginals treat angina pectoris by:
- Increasing oxygen supply
- Decreasing oxygen demand of the heart

Types of Angina:
A. Stable Angina – triggered by stress and exertion and is relieved by rest
B. Unstable Angina – progresses in severity and is not relieved by rest; often a sign of an impending
heart attack
C. Prinzmetal’s or variant or vasospastic angina – occurs at rest because of vasospasm
D. Mixed forms of Angina

Antianginal Drugs
A. Organic Nitrates
1. Isosorbide dinitrate
2. Isosorbide mononitrate
3. Nitroglycerin
B. Β-Blockers
1. Acebutol
2. Atenolol
3. Metoprolol
4. Propranolol
C. Ca2+ Channel Blockers
1. Amlodipine
2. Diltiazem
3. Felodipine
4. Nicardipine
5. Nifedipine
6. Verapamil

Organic Nitrates
A. Mechanism of Action
o Nitrates decrease coronary vasoconstriction or spasm and increase perfusion of the
myocardium by relaxing coronary arteries.
o They relax veins, decreasing preload and myocardial oxygen consumption.
B. Effect on the Cardiovascular system
o All agents differ in their onset of action and rate of elimination
o Drug of choice for prompt relief of ongoing attack of angina precipitated by exercise and
emotional stress – Nitroglycerin, sublingual of spray form
o Major effects of Nitroglycerin at therapeutic doses
 Causes dilation of large veins, resulting in pooling of blood in the veins; this
diminishes preload and reduces the work of the heart.
  Dilates the coronary vasculature, providing an increased blood supply to the
heart
C. Pharmacokinetics
o Onset of action: Nitroglycerin = 1 minute
o Isosorbide mononitrate = more than 1 hour
o Metabolism: liver
D. Adverse effects
o Most common for Nitroglycerin: Headache
o Postural hypotension, facial flushing, tachycardia
o Action of Nitrates potentiated by Sildenafil (Viagra); this combination is contraindicated
E. Tolerance
o Develops rapidly
o Can be overcome by providing a daily “nitrate-free interval” of 10 to 12 hours usually at
night

β-Adrenergic Blockers
- Decrease the oxygen demands of the myocardium by lowering both the rate and the force of
contraction of the heart.
- Suppress the activation of the heart by blocking β 1 receptors, and they reduce the work of the
heart by decreasing heart rate, contractility, cardiac output and blood pressure.
- Demand for oxygen by the myocardium is reduced both during exercise and at rest
- Prototype: Propranolol, but it is not cardioselective
- Preferred agents: Metoprolol, Atenolol
- Contraindicated in patients with asthma, diabetes, severe bradycardia, peripheral vascular, or
chronic obstructive
- Must not be discontinued abruptly, must be gradually tapered off over 5 to 10 days to avoid
rebound angina or hypertension

Calcium-Channel Blockers
- Protect the tissue by inhibiting the entrance of calcium into cardiac and smooth muscle cells of
the coronary and systemic arterial beds.
- Arteriolar vasodilators that cause a decrease in smooth muscle tone and vascular resistance
A. Nifedipine
o An arteriolar vasodilator
o Has minimal effect on cardiac conduction or heart rate
o Side effects: Can cause flushing, headache, hypotension and peripheral edema;
constipation, reflex tachycardia
B. Verapamil
o Slows cardiac AV conduction directly, and decreases heart rate, contractility, blood
pressure and oxygen demand
o Metabolized in the liver; must be adjusted in patients with liver dysfunction
o Contraindicated in patients with pre-existing depressed cardiac function or AV
conduction abnormalities.
o Can cause constipation
o Caution when taken with Digoxin
C. Diltiazem
o Similar to Verapamil in its CV effects
Other options for treatment of Angina:
1. Angioplasty
2. Coronary Artery Bypass Graft (CABG)

Special Concerns in Rehabilitation Patients with Angina Pectoris

1. Therapists must make sure that the drug is always nearby during therapy sessions.
Increase in myocardial oxygen demand during therapy sessions (exercise, functional training, etc) may cause
occurrence of angina attacks.

2. Therapists must still be aware, however, that many rehabilitation activities may disturb the balance between
myocardial oxygen supply and demand, particularly by increasing oxygen demand beyond the ability of the
coronary arteries to increase oxygen supply to the heart.

3. Consequently, therapists must be aware of the cardiac limitations in their patients with angina and use
caution in not overtaxing the heart to the extent that the antianginal drugs are ineffective.

4. Another important consideration in rehabilitation is the effect of antianginal drugs on the

response to an exercise bout. Some patients taking these drugs may experience an increase in
exercise tolerance because the patient is not as limited by symptoms of angina.

Sources:
1. Lippincott’s Illustrated Reviews: Pharmacology (4 th Edition, 2009)
2. Pharmacology in Rehabilitation

Summary:

DRUG GROUP Variant Angina Stable Angina

Nitrates Relaxation of coronary arteries Dilation of veins, which
which decreases vasospasms decreases preload and
and increases oxygen supply decreases oxygen demands

Beta-Blockers Not effective Decreases heart rate and

contractility, which decreases
oxygen demand

Calcium channel blockers Relaxation of coronary arteries, Dilation of arterioles, which

which decreases vasospasms
and increases oxygen supply
decreases afterload and
decreases oxygen demand.
Verapamil and diltiazem
decrease heart rate and
contractility

V2016