Antianginal drugs

Apr 3, 20201 like1,640 views

S.R.L.T institution of pharmaceutical science & technology

This document summarizes a presentation on antianginal drugs. It introduces angina pectoris as chest pain caused by coronary heart disease and myocardial ischemia from an imbalance of blood supply and oxygen demand to the heart. The document classifies common antianginal drugs as nitrates, beta-blockers, calcium channel blockers, and potassium channel openers. It provides examples of drugs in each class and describes their mechanisms of action in treating angina by relaxing smooth muscles or reducing heart rate and oxygen demand.

A presentation on antianginal drugs
Presented by –
Mandakini porwal
B.Pharm ,sem-6th ,3rd year
(S.R.L.T institute of pharmaceutical science & technology)

Content-
 Introduction of antianginal drugs
 Introduction of angina pectoris
 Types of angina
 Classification of antianginal drugs
 Mode of action of antianginal drugs
 Synthesis of antianginal drugs
 S.A.R of antianginal drugs
 Uses & recent advances of anti angina drugs

Antianginal are those drugs who prevent or terminate
attacks of angina pectoris
 Angina pectoris is the medical term for chest pain due to
coronary heart disease
 Angina pectoris is the result of myocardial ischemia
caused by an imbalance between myocardial blood supply
and oxygen demand
 It occur when arteries that carry blood to heart become
narrowed due to atherosclerosis or blood clot.

Classification of antianginal drugs
Nitrates ,B-blockers ,calcium channel blockers and potassium channel
Openers agents are used in the treatment of angina pectoris as a
Antianginal agents.

Nitrates
 Organic nitrates are rapidly denitrates in the smooth muscle cells to
release reactive free radical nitric oxide ,dilate veins
 Which cause peripheral pooling of blood
Examples-

B-blockers
 B- blockers act by reducing work and oxygen consumption and decrease heart rate
 All B-blockers are effective in decreasing frequency and severity of attakes
Examples-
1. Atenolol
2. Metoprolol
3. Propranolol and others

Calcium channel blockers
 These agents inhibits action potential of calcium ion channel in cardiac muscle
 Via trigger release of more calcium ions from intracellular stores and releax
cardiac muscles
 Calcium channel bockers cause depolarisation of smooth muscles by inward
moment of calcium ions through voltage sensitive channels.
Examples-

Mechanism of action of antianginal drugs
Organic nitrates are enzymatically denitrated in the smooth muscles cell to release
reactive free radical nitric oxide which activates cytosolic guanylyl cyclase
Increased cGMP which cause dephosphorylation of MLCK
MLCK fails to activate myosin
It fails to cause action of contraction
Consequently relaxation occurs
Intracellular cGmp may also reduce calcium ions entry –contribute to relaxation.

S.A.R OF ANTIANGINAL DRUGS
 The potency of organic nitrate for guanylate cyclase activation is mainly
determined by the number of nitrate groups.
 So potency of compound is increased with increasing the number of nitrate group.
 Due to esterification of free OH group in isosorbide mononitrate increased in
lipophilicity , had no major influence on guanylate cyclase activation.

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Antianginal drugs

1. A presentation on antianginal drugs Presented by – Mandakini porwal B.Pharm ,sem-6th ,3rd year (S.R.L.T institute of pharmaceutical science & technology)

2. Content-  Introduction of antianginal drugs  Introduction of angina pectoris  Types of angina  Classification of antianginal drugs  Mode of action of antianginal drugs  Synthesis of antianginal drugs  S.A.R of antianginal drugs  Uses & recent advances of anti angina drugs

3. Antianginal are those drugs who prevent or terminate attacks of angina pectoris  Angina pectoris is the medical term for chest pain due to coronary heart disease  Angina pectoris is the result of myocardial ischemia caused by an imbalance between myocardial blood supply and oxygen demand  It occur when arteries that carry blood to heart become narrowed due to atherosclerosis or blood clot.

4. Types of angina -

5. Classification of antianginal drugs Nitrates ,B-blockers ,calcium channel blockers and potassium channel Openers agents are used in the treatment of angina pectoris as a Antianginal agents.

6. Nitrates  Organic nitrates are rapidly denitrates in the smooth muscle cells to release reactive free radical nitric oxide ,dilate veins  Which cause peripheral pooling of blood Examples-

7. B-blockers  B- blockers act by reducing work and oxygen consumption and decrease heart rate  All B-blockers are effective in decreasing frequency and severity of attakes Examples- 1. Atenolol 2. Metoprolol 3. Propranolol and others

8. Calcium channel blockers  These agents inhibits action potential of calcium ion channel in cardiac muscle  Via trigger release of more calcium ions from intracellular stores and releax cardiac muscles  Calcium channel bockers cause depolarisation of smooth muscles by inward moment of calcium ions through voltage sensitive channels. Examples-

9. Mechanism of action of antianginal drugs Organic nitrates are enzymatically denitrated in the smooth muscles cell to release reactive free radical nitric oxide which activates cytosolic guanylyl cyclase Increased cGMP which cause dephosphorylation of MLCK MLCK fails to activate myosin It fails to cause action of contraction Consequently relaxation occurs Intracellular cGmp may also reduce calcium ions entry –contribute to relaxation.

10. Synthesis of isosorbide dinitrate-

11. S.A.R OF ANTIANGINAL DRUGS  The potency of organic nitrate for guanylate cyclase activation is mainly determined by the number of nitrate groups.  So potency of compound is increased with increasing the number of nitrate group.  Due to esterification of free OH group in isosorbide mononitrate increased in lipophilicity , had no major influence on guanylate cyclase activation.

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Antianginal drugs

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Antianginal drugs