Pharmacology of Anti-aniginal Agents

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CV Pharmacology

Anti-Anginal Agents Reading: Antianginal Drugs Formative Assessment Practice question Clinical: e-Medicine articles Coronary Artery Disease Risk Factors for CAD Angina Pectoris

Prepared and presented: Marc Imhotep Cray, M.D. BMS and CK-CS Teacher


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. 2


Causes (Anatomic Dx) ď Ž

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. 3


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CAD Risk Factors ď Ž

1. 2. 3. 4. 5. 6. 7. 8. 9. 10. 11.

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


Symptoms ď Ž

1. 2. 3.

Some more frequent symptoms of coronary heart disease include: Angina (ischemic pain) Myocardial Infarction Shortness of breath

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Diagnosis ď Ž

1. 2. 3. 4. 5. 6. 7. 8. 9.

Diagnosis of coronary heart disease may be accomplished by a variety of means: Coronary angiography Coronary arteriography Coronary CT angiography Echocardiogram Electrocardiogram (ECG) Electron-beam CT (EBCT) Exercise stress test Magnetic resonance angiography Nuclear scan 7


Treatment ď Ž

1. 2. 3. 4. 5. 6.

Coronary heart disease treatment methods may include: (depends on the presenting Physiologic Dx) Angioplasty with stenting Coronary artery bypass surgery Medication Minimally invasive heart surgery Proper diet and exercise Quitting smoking 8


Coronary Artery O2 Supply and Demand

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Angina Pectoris (Chest Pain) ď Ž

ď Ž

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] 10


R/O MI Algorithm

Contemporary Diagnosis and Management of Unstable Angina

GUYS R. http://www.mayoclinicproceedings.com/inside.asp?AID=1529&UID= 11


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 Buccal Chewable tablets Capsules

Ointments Transdermal patches Inhalable sprays 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 19


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 ď Ž

ď Ž

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

Metabolic

bradycardia, hypotension second- or third-degree heart block heart failure Altered glucose and lipid metabolism

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Antianginal Agents: Beta Blockers(5) Side Effects Body System Effects CNS

Other

dizziness, fatigue, mental depression, lethargy, drowsiness, unusual dreams impotence wheezing, dyspnea

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

(Cardiazem) •Verapamil (Isoptin, Calan)

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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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THE END

THANK YOU FOR YOUR ATTENTION

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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