1. CV Pharmacology
Anti-Anginal Agents
Prepared and presented:
Marc Imhotep Cray, M.D.
BMS and CK-CS Teacher
Reading:
Antianginal Drugs
Formative Assessment
Practice question
Clinical:
e-Medicine articles
Coronary Artery Disease
Risk Factors for CAD
Angina Pectoris

2. 2
Coronary heart disease (CHD)
Defined (Etiologic Dx)
 Coronary heart disease (CHD) is a
condition in which proper circulation of blood
and oxygen are not provided to heart and
surrounding tissue.
 Result is due to a narrowing of small blood
vessels, which normally supply heart with
blood and oxygen.
 Coronary heart disease, a type of
cardiovascular disease, is the leading
cause of death for both men and women
in the United States.

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Causes (Anatomic Dx)
 The typical cause of
coronary heart
disease is
atherosclerosis,
which takes place
with plaque and fatty
build up on the
artery walls,
narrowing the
vessels.

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CAD Risk Factors
 Certain conditions are considered to put an individual at greater
risk for coronary heart disease. The following are some risk
factors:
1. Age (particularly 40+)
2. Diabetes
3. Genetics (heredity)
4. High blood pressure
5. High bad cholesterol (LDL)
6. Increased levels of C-reactive protein, fibrinogen, or homocysteine
7. Lack of sufficient physical activity
8. Low good cholesterol (HDL)
9. Menopause
10. Obesity
11. Smoking

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Symptoms
 Some more frequent
symptoms of coronary
heart disease include:
1. Angina (ischemic pain)
2. Myocardial Infarction
3. Shortness of breath

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Diagnosis
 Diagnosis of coronary heart disease may be
accomplished by a variety of means:
1. Coronary angiography
2. Coronary arteriography
3. Coronary CT angiography
4. Echocardiogram
5. Electrocardiogram (ECG)
6. Electron-beam CT (EBCT)
7. Exercise stress test
8. Magnetic resonance angiography
9. Nuclear scan

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Treatment
 Coronary heart disease treatment methods
may include: (depends on the presenting
Physiologic Dx)
1. Angioplasty with stenting
2. Coronary artery bypass surgery
3. Medication
4. Minimally invasive heart surgery
5. Proper diet and exercise
6. Quitting smoking

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Coronary Artery O2 Supply
and Demand

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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 The myocardial supply:demand ratio--a critical
review. [Am J Cardiol. 1978]

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R/O MI Algorithm
Contemporary Diagnosis and Management of Unstable Angina
GUYS R. http://www.mayoclinicproceedings.com/inside.asp?AID=1529&UID=

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Antianginal Pharmacologic
Agents
 Nitrates
 Beta blockers
 Calcium channel blockers

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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)

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

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Antianginal Agents:
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

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Antianginal Agents:
1)Nitrates
Available forms:
Sublingual Ointments
Buccal Transdermal patches
Chewable tablets Inhalable sprays
Capsules Intravenous solutions

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Antianginal Agents: Nitrates(2)
 Cause vasodilation due to relaxation of
smooth muscles
 Potent dilating effect on coronary
arteries
 Used for prophylaxis and treatment
of angina

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Antianginal Agents: Nitrates(3)
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

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Antianginal Agents: Nitrates(4)
 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

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Antianginal Agents: Nitrates(5)
Side Effects
 Headache
 Usually diminish in intensity and frequency
with continued use
 Tachycardia, postural hypotension
 Tolerance may develop

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Antianginal Agents:
2)Beta Blockers
 atenolol (Tenormin)
 metoprolol (Lopressor)
 propranolol (Inderal)
 nadolol (Corgard)

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Antianginal Agents:
Beta Blockers(2)
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

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Antianginal Agents:
Beta Blockers(3)
Therapeutic Uses
 Antianginal
 Antihypertensive
 Cardioprotective effects, especially after MI

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Antianginal Agents: Beta
Blockers(4)
Side Effects
Body System Effects
Cardiovascular bradycardia, hypotension
second- or third-degree heart block
heart failure
Metabolic Altered glucose and lipid
metabolism

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Antianginal Agents:
Beta Blockers(5)
Side Effects
Body System Effects
CNS dizziness, fatigue,
mental depression, lethargy,
drowsiness, unusual dreams
Other impotence
wheezing, dyspnea

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Antianginal Agents:
3) Calcium Channel Blockers
Prototypical Agents
 Verapamil (Calan)
 diltiazem (Cardizem)
 nifedipine (Procardia)
•Dihydropyridines
•Amlodipine
(Norvasc),
Felodipine
(Plendil)
•Nimodipine
•Isradipine
•Nicardipine
•Nifedipine
•Non-Dihydropyridines
•Bepridil (Vascor)
•Diltiazem
(Cardiazem)
•Verapamil (Isoptin,
Calan)
Medicinal Chemistry Classes

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Antianginal Agents:
Calcium Channel Blockers(2)
Mechanism of Action
 Cause peripheral arterial vasodilation
 Reduce myocardial contractility
(negative inotropic action)
 Result: decreased myocardial oxygen demand

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Antianginal Agents:
Calcium Channel Blockers(2)
Therapeutic Uses
 First-line agents for treatment of angina,
hypertension, and supraventricular
tachycardia
 Short-term management of atrial fibrillation
and flutter
 Several other uses

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Antianginal Agents:
Calcium Channel Blockers(3)
Side Effects
 Very acceptable side effect and safety profile
 May cause hypotension, palpitations, tachycardia
or bradycardia, constipation, nausea, dyspnea

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Reference Resource
(Online Textbooks)
Principles of Pharmacology: The Pathophysiologic Basis of
Drug Therapy Cairo CW, Simon JB, Golan DE. (Eds.); LLW
2012 (Google Books Online).
Goodman and Gilman’s The Pharmacological Basis of
Therapeutics. Brunton LL, Chabner BA , Knollmann BC (Eds.);
M-H 12th ed. 2011.
Basic and Clinical Pharmacology, Katzung, Masters, Trevor; M-
H 12th ed.
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