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Anti-anginal drugs
Prepared By – UndhadTushar C.
Masters Of Pharmacy Sem – 1 (Pharmacology)
CONTENTS
• 1.Introduction
• 2.Type of angina
• 3.Risk factors
• 4.Pharmacology of antianginal drugs
• 5.Reference
Tushar Undhad antianginal drugs 2
1.Introduction
Angina pectoris is the chief
symptom of ischemic heart disease
(IHD) characterized by sudden,
severe, pain which may radiate to
the left shoulder and surface of the
left arm.
Tushar Undhad antianginal drugs 3
1.Introduction
• Myocardial oxygen
consumption depends
on preload afterload
and heart rate.
• When the oxygen
supply to the
myocardium is
insufficient for its
needs, myocardial
ischemia develops.
Tushar Undhad antianginal drugs 4
2.Type of angina
• 1.stable angina
• 2.unstable angina
• 3.variant angina
Tushar Undhad antianginal drugs 5
2.Type of angina
1. Classical angina
(stable angina):
• Pain is induced by
exercise or emotion,
both of which increase
myocardial oxygen
demand.
Tushar Undhad antianginal drugs 6
2.Type of angina
• In such patients there is
narrowing of the coronary
arteries due to atherosclerosis
and therefore the coronaries
cannot dilate to increase the
blood supply during exercise.
• Hence there is an imbalance
between oxygen supply and
demand.
Tushar Undhad antianginal drugs 7
2.Type of angina
2.Unstable angina:
• Unstable angina is classified between stable
angina and Myocardial infraction.
• What cause unstable angina- this atheroma
plague rapture and blood clot may form and
decrease blood flow in the artery.
Tushar Undhad antianginal drugs
8
2.Type of angina
• 3.Variant angina
• angina that occurs at rest
and is due to coronary
artery spasm.
• Symptoms are caused by
decreased blood flow to
the heart muscle from the
spasm of the coronary
artery.
Tushar Undhad antianginal drugs 9
3.Risk factors
• Hyperlipidaemia
• Hypertension
• Diabetes
• Smoking
Tushar Undhad antianginal drugs 10
4.Classification of antianginals drugs
Class of drugs Name of drugs
1. Nitrates Nitroglycerine, isosorbide
dinitrate, isosorbide mononitrate,
2. Calcium channel
blockers
Verapamil, diltiazem, amlodipine,
nifedipine, Nicardipin,
3.β-blockers Propranolol, atenolol, metoprolol,
4. Potassium channel
openers
Nicorandil, minoxidil, diazoxide,
5.Other antianginal Dipyridamole, aspirin,
trimetazidine
Tushar Undhad antianginal drugs 11
1. Nitrates
• Ex - Nitroglycerine, Isosorbide Dinitrate, Isosorbide
Mononitrate
• MOA:- Nitrates are vasodilators.
Tushar Undhad antianginal drugs 12
1. Nitrates
• They are converted to
nitric oxide.
• Activates vascular guanylyl
cyclase which increases
the synthesis of cGMP.
• This cGMP catalases the
phosphorylation of protein
kinases causing relaxation
of the smooth muscles.
Tushar Undhad antianginal drugs 13
1. Nitrates
• Pharmacokinetics :-
• Organic nitrates are lipid-soluble: well absorbed
from buccal mucosa. Action occur 5-7 min.
• Half life 2-5 hr.
Tushar Undhad antianginal drugs 14
1. Nitrates
• ADR:-
• Palpitation
• Fatigue, dizziness
• Postural hypotension
Tushar Undhad antianginal drugs 15
1. Nitrates
• USE:
• Angina pectoris
• Cardiac failure
• Myocardial infarction (Ml)
Tushar Undhad antianginal drugs 16
2.Calcium channel blockers
• Ex - Verapamil, Diltiazem, Amlodipine,
Nifedipine, Nicardipin.
• MOA:
• The intracellular concentration of calcium
plays an important role in maintaining the
tone of smooth muscle and in the
contraction of the myocardium.
Tushar Undhad antianginal drugs 17
2.Calcium channel blockers
• Calcium enters muscle cells through special
voltage sensitive calcium channels.
• This triggers release of calcium from the
sarcoplasmic reticulum and mitochondria, which
further increases the cytosolic level of calcium.
Tushar Undhad antianginal drugs 18
2.Calcium channel blockers
• Calcium channel blocker block L-type calcium
channels in the heart and in smooth muscle of
the coronary and peripheral arteriolar.
• This causes vascular smooth muscle to relax,
dilating mainly arterioles
Tushar Undhad antianginal drugs 19
2.Calcium channel blockers
• Pharmacokinetic action :
• Most of these agents have short half-lives (3 to 8
hours)
• Metabolized in liver
• Excreted in urine
Tushar Undhad antianginal drugs 20
2.Calcium channel blockers
• ADR:
• Dizziness, headache, and a feeling of fatigue
caused by a decrease in blood pressure
• Peripheral edema is another commonly reported
side effect of this class.
Tushar Undhad antianginal drugs 21
2.Calcium channel blockers
• Therapeutic uses:
• Hypertension
• Treatment of angina
• Arrhythmias
Tushar Undhad antianginal drugs 22
3.β-blockers
• Ex- Propranolol, Atenolol, Metoprolol.
• MOA:
• Blockade of cardiac β1 receptors results in
decreased myocardial contractility and cardiac
output.
• They reduce the BP due to a fall in the cardiac
output.
• They also lower plasma renin activity and have
an additional central antihypertensive action.
Tushar Undhad antianginal drugs 23
3.β-blockers
Tushar Undhad antianginal drugs 24
Mechanism of action:
3.β-blockers
• Pharmacokinetic action :
• β-blockers are orally active
• Metabolised in the liver
• t½ is 3-7 hrs.
Tushar Undhad antianginal drugs 25
3.β-blockers
• ADR:
• Bradycardia
• Fatigue
• Insomnia
• Sexual dysfunction
• Hypotension
Tushar Undhad antianginal drugs 26
3.β-blockers
• Therapeutic uses:
• Previous myocardial infarction,
• Angina pectoris
• Chronic heart failure
• Hypertension
Tushar Undhad antianginal drugs 27
4. Potassium channel openers
• MOA:
• Opening these channels
hyperpolarizes the smooth
muscle, which closes voltage-
gated calcium channels and
decreases intracellular calcium.
• This leads to relaxation and
vasodilation.
Tushar Undhad antianginal drugs 28
Ex - Nicorandil, Minoxidil, Minoxidil, Diazoxide
4. Potassium channel openers
Tushar Undhad antianginal drugs 29
4. Potassium channel openers
• ADR:
• Headaches, flushing
• Reflex tachycardia
• Fluid and salt retention
Tushar Undhad antianginal drugs 30
4. Potassium channel openers
• Therapeutic uses:
• Hypertension
• Smooth muscle relaxing activity
• Vasodilator to treat angina
Tushar Undhad antianginal drugs 31
5.References:
• Essentials Of Medical Pharmacology 8th Edition
2018 By KDTripathi
• Lippincott's pharmacology
• Padmaja Uday Kumar Professor and Head
Department of Pharmacology Fr. Muller Medical
College, Mangalore Karnataka India
• Goodman and Gilman’s The Pharmacological Basis of
Therapeutics, 11th -Edition 2006
• Rang & Dale’s Pharmacology, Eighth edition
Tushar Undhad antianginal drugs 32
Tushar Undhad antianginal drugs 33

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Antianginal drugs.pptx

  • 1. Anti-anginal drugs Prepared By – UndhadTushar C. Masters Of Pharmacy Sem – 1 (Pharmacology)
  • 2. CONTENTS • 1.Introduction • 2.Type of angina • 3.Risk factors • 4.Pharmacology of antianginal drugs • 5.Reference Tushar Undhad antianginal drugs 2
  • 3. 1.Introduction Angina pectoris is the chief symptom of ischemic heart disease (IHD) characterized by sudden, severe, pain which may radiate to the left shoulder and surface of the left arm. Tushar Undhad antianginal drugs 3
  • 4. 1.Introduction • Myocardial oxygen consumption depends on preload afterload and heart rate. • When the oxygen supply to the myocardium is insufficient for its needs, myocardial ischemia develops. Tushar Undhad antianginal drugs 4
  • 5. 2.Type of angina • 1.stable angina • 2.unstable angina • 3.variant angina Tushar Undhad antianginal drugs 5
  • 6. 2.Type of angina 1. Classical angina (stable angina): • Pain is induced by exercise or emotion, both of which increase myocardial oxygen demand. Tushar Undhad antianginal drugs 6
  • 7. 2.Type of angina • In such patients there is narrowing of the coronary arteries due to atherosclerosis and therefore the coronaries cannot dilate to increase the blood supply during exercise. • Hence there is an imbalance between oxygen supply and demand. Tushar Undhad antianginal drugs 7
  • 8. 2.Type of angina 2.Unstable angina: • Unstable angina is classified between stable angina and Myocardial infraction. • What cause unstable angina- this atheroma plague rapture and blood clot may form and decrease blood flow in the artery. Tushar Undhad antianginal drugs 8
  • 9. 2.Type of angina • 3.Variant angina • angina that occurs at rest and is due to coronary artery spasm. • Symptoms are caused by decreased blood flow to the heart muscle from the spasm of the coronary artery. Tushar Undhad antianginal drugs 9
  • 10. 3.Risk factors • Hyperlipidaemia • Hypertension • Diabetes • Smoking Tushar Undhad antianginal drugs 10
  • 11. 4.Classification of antianginals drugs Class of drugs Name of drugs 1. Nitrates Nitroglycerine, isosorbide dinitrate, isosorbide mononitrate, 2. Calcium channel blockers Verapamil, diltiazem, amlodipine, nifedipine, Nicardipin, 3.β-blockers Propranolol, atenolol, metoprolol, 4. Potassium channel openers Nicorandil, minoxidil, diazoxide, 5.Other antianginal Dipyridamole, aspirin, trimetazidine Tushar Undhad antianginal drugs 11
  • 12. 1. Nitrates • Ex - Nitroglycerine, Isosorbide Dinitrate, Isosorbide Mononitrate • MOA:- Nitrates are vasodilators. Tushar Undhad antianginal drugs 12
  • 13. 1. Nitrates • They are converted to nitric oxide. • Activates vascular guanylyl cyclase which increases the synthesis of cGMP. • This cGMP catalases the phosphorylation of protein kinases causing relaxation of the smooth muscles. Tushar Undhad antianginal drugs 13
  • 14. 1. Nitrates • Pharmacokinetics :- • Organic nitrates are lipid-soluble: well absorbed from buccal mucosa. Action occur 5-7 min. • Half life 2-5 hr. Tushar Undhad antianginal drugs 14
  • 15. 1. Nitrates • ADR:- • Palpitation • Fatigue, dizziness • Postural hypotension Tushar Undhad antianginal drugs 15
  • 16. 1. Nitrates • USE: • Angina pectoris • Cardiac failure • Myocardial infarction (Ml) Tushar Undhad antianginal drugs 16
  • 17. 2.Calcium channel blockers • Ex - Verapamil, Diltiazem, Amlodipine, Nifedipine, Nicardipin. • MOA: • The intracellular concentration of calcium plays an important role in maintaining the tone of smooth muscle and in the contraction of the myocardium. Tushar Undhad antianginal drugs 17
  • 18. 2.Calcium channel blockers • Calcium enters muscle cells through special voltage sensitive calcium channels. • This triggers release of calcium from the sarcoplasmic reticulum and mitochondria, which further increases the cytosolic level of calcium. Tushar Undhad antianginal drugs 18
  • 19. 2.Calcium channel blockers • Calcium channel blocker block L-type calcium channels in the heart and in smooth muscle of the coronary and peripheral arteriolar. • This causes vascular smooth muscle to relax, dilating mainly arterioles Tushar Undhad antianginal drugs 19
  • 20. 2.Calcium channel blockers • Pharmacokinetic action : • Most of these agents have short half-lives (3 to 8 hours) • Metabolized in liver • Excreted in urine Tushar Undhad antianginal drugs 20
  • 21. 2.Calcium channel blockers • ADR: • Dizziness, headache, and a feeling of fatigue caused by a decrease in blood pressure • Peripheral edema is another commonly reported side effect of this class. Tushar Undhad antianginal drugs 21
  • 22. 2.Calcium channel blockers • Therapeutic uses: • Hypertension • Treatment of angina • Arrhythmias Tushar Undhad antianginal drugs 22
  • 23. 3.β-blockers • Ex- Propranolol, Atenolol, Metoprolol. • MOA: • Blockade of cardiac β1 receptors results in decreased myocardial contractility and cardiac output. • They reduce the BP due to a fall in the cardiac output. • They also lower plasma renin activity and have an additional central antihypertensive action. Tushar Undhad antianginal drugs 23
  • 24. 3.β-blockers Tushar Undhad antianginal drugs 24 Mechanism of action:
  • 25. 3.β-blockers • Pharmacokinetic action : • β-blockers are orally active • Metabolised in the liver • t½ is 3-7 hrs. Tushar Undhad antianginal drugs 25
  • 26. 3.β-blockers • ADR: • Bradycardia • Fatigue • Insomnia • Sexual dysfunction • Hypotension Tushar Undhad antianginal drugs 26
  • 27. 3.β-blockers • Therapeutic uses: • Previous myocardial infarction, • Angina pectoris • Chronic heart failure • Hypertension Tushar Undhad antianginal drugs 27
  • 28. 4. Potassium channel openers • MOA: • Opening these channels hyperpolarizes the smooth muscle, which closes voltage- gated calcium channels and decreases intracellular calcium. • This leads to relaxation and vasodilation. Tushar Undhad antianginal drugs 28 Ex - Nicorandil, Minoxidil, Minoxidil, Diazoxide
  • 29. 4. Potassium channel openers Tushar Undhad antianginal drugs 29
  • 30. 4. Potassium channel openers • ADR: • Headaches, flushing • Reflex tachycardia • Fluid and salt retention Tushar Undhad antianginal drugs 30
  • 31. 4. Potassium channel openers • Therapeutic uses: • Hypertension • Smooth muscle relaxing activity • Vasodilator to treat angina Tushar Undhad antianginal drugs 31
  • 32. 5.References: • Essentials Of Medical Pharmacology 8th Edition 2018 By KDTripathi • Lippincott's pharmacology • Padmaja Uday Kumar Professor and Head Department of Pharmacology Fr. Muller Medical College, Mangalore Karnataka India • Goodman and Gilman’s The Pharmacological Basis of Therapeutics, 11th -Edition 2006 • Rang & Dale’s Pharmacology, Eighth edition Tushar Undhad antianginal drugs 32