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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
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.
3
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.
4
5
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
6
Symptoms
 Some more frequent
symptoms of coronary
heart disease include:
1. Angina (ischemic pain)
2. Myocardial Infarction
3. Shortness of breath
7
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
8
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
9
Coronary Artery O2 Supply
and Demand
10
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]
11
R/O MI Algorithm
Contemporary Diagnosis and Management of Unstable Angina
GUYS R. http://www.mayoclinicproceedings.com/inside.asp?AID=1529&UID=
12
Antianginal Pharmacologic
Agents
 Nitrates
 Beta blockers
 Calcium channel blockers
13
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)
14
Antianginal Agents:
Therapeutic Objectives
 Increase blood flow to ischemic heart muscle
and/or
 Decrease myocardial oxygen demand
15
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
16
Antianginal Agents:
1)Nitrates
Available forms:
Sublingual Ointments
Buccal Transdermal patches
Chewable tablets Inhalable sprays
Capsules Intravenous solutions
17
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
18
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
19
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
20
Antianginal Agents: Nitrates(5)
Side Effects
 Headache
 Usually diminish in intensity and frequency
with continued use
 Tachycardia, postural hypotension
 Tolerance may develop
21
Antianginal Agents:
2)Beta Blockers
 atenolol (Tenormin)
 metoprolol (Lopressor)
 propranolol (Inderal)
 nadolol (Corgard)
22
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
23
Antianginal Agents:
Beta Blockers(3)
Therapeutic Uses
 Antianginal
 Antihypertensive
 Cardioprotective effects, especially after MI
24
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
25
Antianginal Agents:
Beta Blockers(5)
Side Effects
Body System Effects
CNS dizziness, fatigue,
mental depression, lethargy,
drowsiness, unusual dreams
Other impotence
wheezing, dyspnea
26
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
27
Antianginal Agents:
Calcium Channel Blockers(2)
Mechanism of Action
 Cause peripheral arterial vasodilation
 Reduce myocardial contractility
(negative inotropic action)
 Result: decreased myocardial oxygen demand
28
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
29
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
30
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.
THE END
THANK YOU FOR YOUR ATTENTION

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IVMS-CV Pharmacology -Anti-Aniginal Agents

  • 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.
  • 3. 3 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.
  • 4. 4
  • 5. 5 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
  • 6. 6 Symptoms  Some more frequent symptoms of coronary heart disease include: 1. Angina (ischemic pain) 2. Myocardial Infarction 3. Shortness of breath
  • 7. 7 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
  • 8. 8 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
  • 9. 9 Coronary Artery O2 Supply and Demand
  • 10. 10 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]
  • 11. 11 R/O MI Algorithm Contemporary Diagnosis and Management of Unstable Angina GUYS R. http://www.mayoclinicproceedings.com/inside.asp?AID=1529&UID=
  • 12. 12 Antianginal Pharmacologic Agents  Nitrates  Beta blockers  Calcium channel blockers
  • 13. 13 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)
  • 14. 14 Antianginal Agents: Therapeutic Objectives  Increase blood flow to ischemic heart muscle and/or  Decrease myocardial oxygen demand
  • 15. 15 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
  • 16. 16 Antianginal Agents: 1)Nitrates Available forms: Sublingual Ointments Buccal Transdermal patches Chewable tablets Inhalable sprays Capsules Intravenous solutions
  • 17. 17 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
  • 18. 18 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
  • 19. 19 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
  • 20. 20 Antianginal Agents: Nitrates(5) Side Effects  Headache  Usually diminish in intensity and frequency with continued use  Tachycardia, postural hypotension  Tolerance may develop
  • 21. 21 Antianginal Agents: 2)Beta Blockers  atenolol (Tenormin)  metoprolol (Lopressor)  propranolol (Inderal)  nadolol (Corgard)
  • 22. 22 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
  • 23. 23 Antianginal Agents: Beta Blockers(3) Therapeutic Uses  Antianginal  Antihypertensive  Cardioprotective effects, especially after MI
  • 24. 24 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
  • 25. 25 Antianginal Agents: Beta Blockers(5) Side Effects Body System Effects CNS dizziness, fatigue, mental depression, lethargy, drowsiness, unusual dreams Other impotence wheezing, dyspnea
  • 26. 26 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
  • 27. 27 Antianginal Agents: Calcium Channel Blockers(2) Mechanism of Action  Cause peripheral arterial vasodilation  Reduce myocardial contractility (negative inotropic action)  Result: decreased myocardial oxygen demand
  • 28. 28 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
  • 29. 29 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
  • 30. 30 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. THE END THANK YOU FOR YOUR ATTENTION