Antianginal Agents

د.شامل هاشم ألنعيمي م\3\موصل 25\2\2018
عدد الاوراق ( 3 ) ادوية lec:13
Antianginal Agents
Nitrates
Beta blockers
Calcium channel blockers

Angina Pectoris (Chest Pain)

When the supply of oxygen and nutrients in the blood is insufficient to meet the demands of the heart, the heart muscle aches.
The heart demands a large supply of oxygen to meet the demands placed on it.

Types of Angina

Chronic stable angina (also called classic or effort angina)
Unstable angina(also called preinfarction or crescendo angina)
Vasospastic angina(also called Prinzmetal’s or variant angina)

Angina Drug Therapy

Antianginal Agents:
Therapeutic Objectives
Increase blood flow to ischemic heart muscle
and/or
Decrease myocardial oxygen demand

Therapeutic Objectives

Minimize the frequency of attacks and decrease the duration and intensity of anginal pain
Improve the patient’s functional capacity with as few side effects as possible
Prevent or delay the worst possible outcome, MI

Antianginal Agents: Nitrates

Available forms:
Sublingual Ointments
Buccal Transdermal patches
Chewable tablets Inhalable sprays
Capsules Intravenous solutions

Antianginal Agents: Nitrates

Cause vasodilation due to relaxation of smooth muscles
Potent dilating effect on coronary arteries
Used for prophylaxis and treatment of angina


Antianginal Agents: Nitrates
Nitroglycerin
Prototypical nitrate
Large first-pass effect with PO forms
Used for symptomatic treatment of ischemic heart conditions (angina)
IV form used for BP control in perioperative hypertension, treatment of CHF, ischemic pain, and pulmonary edema associated with acute MI
Antianginal Agents: Nitrates
isosorbide dinitrate (Isordil, Sorbitrate, Dilatrate SR)
isosorbide mononitrate (Imdur, Monoket, ISMO)

Used for:

Acute relief of angina
Prophylaxis in situations that may provoke angina
Long-term prophylaxis of angina

Antianginal Agents: Nitrates

Side Effects
Headache
Usually diminish in intensity and frequency with continued use
Tachycardia, postural hypotension
Tolerance may develop


Interactions
An important footnote to the use of nitrate has been the marked potentiation of their vasodilator effects observed in patients taking phosphodiesterase (PDE) inhibitors, such as sildenafil and tadalafil .

Antianginal Agents: Beta Blockers

atenolol (Tenormin)
metoprolol (Lopressor)
propranolol (Inderal)
nadolol (Corgard)

Antianginal Agents: Beta Blockers

Mechanism of Action
Decrease the HR, resulting in decreased myocardial oxygen demand and increased oxygen delivery to the heart
Decrease myocardial contractility, helping to conserve energy or decrease demand

Antianginal Agents: Beta Blockers

Therapeutic Uses
Antianginal
Antihypertensive
Cardioprotective effects, especially after MI

Antianginal Agents: Beta Blockers

Side Effects
Body System Effects
Cardiovascular bradycardia, hypotension second- or third-degree heart block heart failure
Metabolic Altered glucose and lipid metabolism


Antianginal Agents: Beta Blockers
Side Effects
Body System Effects
CNS dizziness, fatigue, mental depression, lethargy, drowsiness, unusual dreams
Other impotence wheezing, dyspnea

Antianginal Agents: Calcium Channel Blockers

verapamil (Calan)
diltiazem (Cardizem)
nifedipine (Procardia)

Antianginal Agents: Calcium Channel Blockers

Mechanism of Action
Cause peripheral arterial vasodilation
Reduce myocardial contractility (negative inotropic action)
Result: decreased myocardial oxygen demand

Antianginal Agents: Calcium Channel Blockers

Therapeutic Uses
First-line agents for treatment of angina, hypertension, and supraventricular tachycardia
Short-term management of atrial fibrillation and flutter
Several other uses
Antianginal Agents: Calcium Channel Blockers
Side Effects
Very acceptable side effect and safety profile
May cause hypotension, palpitations, tachycardia or bradycardia, constipation, nausea, dyspnea