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Antianginal agents
Anti-anginal agents
WriteMOAofanti-anginalagentsandclassifyitwithoneexamplefromeach class. 10M
Classify antianginal agents. Write a structure and MOA of any two drugs belonging
to different class.
3M
Explain the chemistry and MOA of organic nitrates as antianginal agents. 4M
 Angina pectoris – commonly known as angina – It occurs due to insufficient
oxygen supply to the myocardium i.e the sensation of chest pain
 The term derives from the Latin angina ("infection of the throat") from
the Greek ἀγχόνη ankhonē ("strangling"), and the Latin pectus ("chest"), and
can, therefore, be translated as "a strangling feeling in the chest".
 Angina pectoris is chronic disease affecting the coronary arteries which
supply oxygenated blood from the left ventricle to all heart tissues.
 Angina is the primary symptom of oxygen deficient heart disease &
characteristic by the sudden pain originating in the chest , often regarding to
the left shoulder and down of left arm
 There can be severe pain with little or no risk of a myocardial
infarction {commonly known as a heart attack}, and a heart attack can
occur without pain)
 Based on electrophysiological changes observed during the attack
 angina is result of advanced state of food, exercise, emotional factor.
 Typical angina characterized by low ST
 Angina results when there is an imbalance between the heart's oxygen
demand and supply. This imbalance can result from an increase in
demand (e.g., during exercise) without a proportional increase in supply
(e.g., due to obstruction or atherosclerosis of the coronary arteries).
 However, the path physiology of angina in females varies significantly as
compared to males.[
 Non-obstructive coronary disease is more common in females
2. Major risk factors
Age (≥ 55 for men, ≥ 65 for
women)
 Cigarette smoking
 Diabetes mellitus (DM)
 Family History
 Hypertension (HTN)
 Kidney disease
 Obesity
 Physical inactivity
 Medications
 Types of Angina
Typical Angina ( Classical Angina )
 pain is commonly induced by exercise,
excitement or a heavy meal
 secondary to advanced atherosclerosis of
the coronary vessels
 associated with ST-segment depression
on ECG
Variant Angina ( Prinzmetal Angina)
 pain is induced while at rest
 associated with ST-segment elevation on
ECG
 secondary to vasospasm of the coronary
vessels
Unstable angina
 may involve coronary spasm and may also
have the component of atherosclerosis
 the duration of manifestation is longer than
the first two and has the manifestation of
Myocardial infarction.
* Myocardial ischemia which produces angina results from
imbalances in myocardial oxygen supply & demand relationship
such as decreased oxygen supply and/or increased oxygen
demand.
Etiology
1. Decrease oxygen supply
2. Increase demand for oxygen
Treatment Plan/Approach to develop antianginal drugs include
A. decrease the risk factor like atherosclerosis, hypertension, smoking
B. increase oxygen supply
C. decrease oxygen demand
D- to decrease workload on heart
E- to prevent or inhibit vasospasm
Antianginal Agents
 Nitrates
 Beta blockers
 Calcium channel blockers
I. AGENTS WHICH ↓ O2 DEMAND & ↑ O2 SUPPLY
A. NITRATES
B. CALCIUM CHANNEL BLOCKERS
II. AGENTS WHICH ↓ O2 DEMAND
C. BETA BLOCKERS
Classification of Antianginal Drugs
 For the treatment of angina pectoris include
 1- nitrates and nitrites
 2- Xanthines
 3 – nicotinic acid and derivative
 4 – papavarine
 5- B- Adrenergic Blockers
 6- MAO inhibitors
 7- miscellaneous
2) Xanthine 3)Nicotinic acid
4) Papavarine
1st mechanism of action
Coronary artery dilatation
Decrease coronary bed
resistance
(Relieved coronary
vasospasm)
Increase coronary blood flow
Increase oxygen supply
 2nd mechanism of action
Reduction on peripheral resistance
(Secondary to dilatation of
aorta)
Decrease blood pressure
Decrease after load
Decrease workload
Decrease oxygen consumption
3rd mechanism of action
Reduced venous return
(Due to dilatation of the veins)
Decrease left ventricular volume
Decrease preload
Decrease workload
Decrease oxygen consumption
 Antianginal drug

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Antianginal drug

  • 2. Anti-anginal agents WriteMOAofanti-anginalagentsandclassifyitwithoneexamplefromeach class. 10M Classify antianginal agents. Write a structure and MOA of any two drugs belonging to different class. 3M Explain the chemistry and MOA of organic nitrates as antianginal agents. 4M
  • 3.  Angina pectoris – commonly known as angina – It occurs due to insufficient oxygen supply to the myocardium i.e the sensation of chest pain  The term derives from the Latin angina ("infection of the throat") from the Greek ἀγχόνη ankhonē ("strangling"), and the Latin pectus ("chest"), and can, therefore, be translated as "a strangling feeling in the chest".  Angina pectoris is chronic disease affecting the coronary arteries which supply oxygenated blood from the left ventricle to all heart tissues.  Angina is the primary symptom of oxygen deficient heart disease & characteristic by the sudden pain originating in the chest , often regarding to the left shoulder and down of left arm
  • 4.  There can be severe pain with little or no risk of a myocardial infarction {commonly known as a heart attack}, and a heart attack can occur without pain)  Based on electrophysiological changes observed during the attack  angina is result of advanced state of food, exercise, emotional factor.  Typical angina characterized by low ST  Angina results when there is an imbalance between the heart's oxygen demand and supply. This imbalance can result from an increase in demand (e.g., during exercise) without a proportional increase in supply (e.g., due to obstruction or atherosclerosis of the coronary arteries).  However, the path physiology of angina in females varies significantly as compared to males.[  Non-obstructive coronary disease is more common in females
  • 5. 2. Major risk factors Age (≥ 55 for men, ≥ 65 for women)  Cigarette smoking  Diabetes mellitus (DM)  Family History  Hypertension (HTN)  Kidney disease  Obesity  Physical inactivity  Medications  Types of Angina Typical Angina ( Classical Angina )  pain is commonly induced by exercise, excitement or a heavy meal  secondary to advanced atherosclerosis of the coronary vessels  associated with ST-segment depression on ECG Variant Angina ( Prinzmetal Angina)  pain is induced while at rest  associated with ST-segment elevation on ECG  secondary to vasospasm of the coronary vessels Unstable angina  may involve coronary spasm and may also have the component of atherosclerosis  the duration of manifestation is longer than the first two and has the manifestation of Myocardial infarction.
  • 6. * Myocardial ischemia which produces angina results from imbalances in myocardial oxygen supply & demand relationship such as decreased oxygen supply and/or increased oxygen demand. Etiology 1. Decrease oxygen supply 2. Increase demand for oxygen Treatment Plan/Approach to develop antianginal drugs include A. decrease the risk factor like atherosclerosis, hypertension, smoking B. increase oxygen supply C. decrease oxygen demand D- to decrease workload on heart E- to prevent or inhibit vasospasm
  • 7. Antianginal Agents  Nitrates  Beta blockers  Calcium channel blockers I. AGENTS WHICH ↓ O2 DEMAND & ↑ O2 SUPPLY A. NITRATES B. CALCIUM CHANNEL BLOCKERS II. AGENTS WHICH ↓ O2 DEMAND C. BETA BLOCKERS
  • 8. Classification of Antianginal Drugs  For the treatment of angina pectoris include  1- nitrates and nitrites  2- Xanthines  3 – nicotinic acid and derivative  4 – papavarine  5- B- Adrenergic Blockers  6- MAO inhibitors  7- miscellaneous
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  • 10. 2) Xanthine 3)Nicotinic acid 4) Papavarine
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  • 13. 1st mechanism of action Coronary artery dilatation Decrease coronary bed resistance (Relieved coronary vasospasm) Increase coronary blood flow Increase oxygen supply  2nd mechanism of action Reduction on peripheral resistance (Secondary to dilatation of aorta) Decrease blood pressure Decrease after load Decrease workload Decrease oxygen consumption
  • 14. 3rd mechanism of action Reduced venous return (Due to dilatation of the veins) Decrease left ventricular volume Decrease preload Decrease workload Decrease oxygen consumption