Anti-anginal drugs Prepared By – Undhad Tushar 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. 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
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
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
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
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
5.References: Essentials Of Medical Pharmacology 8th Edition 2018 By KD Tripathi 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, 11 th -Edition 2006 Rang & Dale’s Pharmacology, Eighth edition Tushar Undhad antianginal drugs 32