Comprehensive Overview of Anti-Anginal Drugs and Their Therapeutic Uses in Cardiovascular Care

Comprehensive Overview of Anti-Anginal Drugs and Their Therapeutic Uses in Cardiovascular Care

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  PREPARED BY Prof. ASHISHN. UMALE M. PHARM IN PHARMACOLOGY ASSISTANT PROFESSOR SHRADDHA INSTITUTE OF PHARMACY, WASHIM- 444505 PHARMACOLOGY-II
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  Introduction Angina pectoris isa clinical syndrome characterized by transient episodes of chest pain or discomfort caused by myocardial ischemia. It occurs when the oxygen demand of the heart exceeds the oxygen supply due to reduced coronary blood flow. The primary aim of anti-anginal therapy is to restore the balance between myocardial oxygen supply and demand, thereby relieving chest pain, improving exercise tolerance, and preventing cardiovascular complications. Definition Anti-anginal drugs are medications used to relieve or prevent anginal attacks by increasing coronary blood flow, reducing myocardial oxygen demand, or both. These drugs improve the oxygen supply-demand balance of the myocardium and reduce the frequency and severity of anginal episodes. ANTI-ANGINAL DRUGS
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  Goals of Anti-anginalTherapy The objectives of anti-anginal therapy include: Relief of chest pain Prevention of anginal attacks Improvement of exercise capacity Reduction of myocardial oxygen demand Improvement of coronary blood flow Prevention of myocardial infarction Reduction of cardiovascular mortality Type of Angina Cause Characteristics Stable / Classical(Typical) Fixed atherosclerotic narrowing Predictable pain on exertion Unstable (Crescendo) Plaque rupture with thrombus Pain at rest, increasing severity Variant (Prinzmetal's) Coronary vasospasm Pain at rest, usually at night
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  Organic Nitrates ↓ Converted toNitric Oxide (NO) ↓ Activation of Guanylate Cyclase ↓ ↑ cGMP Formation ↓ Relaxation of Vascular Smooth Muscle ↓ Predominant Venodilation ↓ ↓ Venous Return (Preload) ↓ ↓ Left Ventricular Wall Tension ↓ ↓ Myocardial Oxygen Demand ↓ Relief of Anginal Pain 1. ORGANIC NITRATES / VASODILATERS
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  Therapeutic Effects Organic nitratesrapidly relieve chest pain by reducing myocardial oxygen demand. They also dilate coronary arteries and improve coronary blood flow.  Clinical Uses:- Organic nitrates are used in stable angina, unstable angina, variant (Prinzmetal) angina, acute myocardial infarction, acute heart failure, and hypertensive emergencies.  Adverse Effects:- headache, flushing, dizziness, postural hypotension, reflex tachycardia, and nitrate tolerance during prolonged therapy.  Contraindications:- severe hypotension, shock, raised intracranial pressure, hypertrophic obstructive cardiomyopathy, and in patients receiving phosphodiesterase-5 inhibitors such as sildenafil
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  β-Blockers ↓ Block β1 AdrenergicReceptors ↓ ↓ Heart Rate ↓ Myocardial Contractility ↓ ↓ Cardiac Output ↓ ↓ Myocardial Oxygen Consumption ↓ Prevention of Anginal Attacks 2. BETA-ADRENERGIC BLOCKERS
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  Therapeutic Effects Beta blockersdecrease myocardial oxygen demand and improve exercise tolerance. They reduce the frequency of anginal attacks and decrease mortality after myocardial infarction.  Clinical Uses: chronic stable angina, hypertension, myocardial infarction, heart failure, and cardiac arrhythmias.  Adverse Effects: Bradycardia, fatigue, bronchospasm, depression, erectile dysfunction, and cold extremities.  Contraindications: Bronchial asthma, severe bradycardia, cardiogenic shock, second- or third-degree heart block.
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  Calcium Channel Blockers ↓ BlockL-Type Calcium Channels (Electrical) ↓ ↓ Calcium Entry into Cardiac & Vascular Smooth Muscle ↓ Coronary Vasodilation ↓ ↓ Peripheral Vascular Resistance ↓ ↓ Afterload + Verapamil & Diltiazem ↓ ↓ Heart Rate & ↓ Contractility ↓ ↓ Myocardial Oxygen Demand ↓ Relief of Angina 3. CALCIUM CHANNEL BLOCKERS
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  Therapeutic Effects: Calciumchannel blockers increase coronary blood flow & decrease myocardial oxygen demand. Clinical Uses: stable angina, variant angina, hypertension, supraventricular tachyarrhythmias, and Raynaud's phenomenon. Adverse Effects: Peripheral edema, flushing, constipation (especially with verapamil), headache, dizziness, bradycardia, and hypotension. Contraindications: Severe heart failure, sick sinus syndrome, severe hypotension, and second- or third-degree heart block.
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  Nicorandil ↓ Opens ATP-Sensitive K+Channels ↓ Hyperpolarization of Smooth Muscle(outflow) ↓ Arterial Vasodilation + Releases Nitric Oxide ↓ Venodilation ↓ ↓ Preload + ↓ Afterload ↓ ↓ Myocardial Oxygen Demand ↓ Relief of Angina 4. POTASSIUM CHANNEL OPENER
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  Therapeutic Effects: Nicorandilreduces both preload and afterload while improving coronary blood flow. Clinical Uses: Used in chronic stable angina not adequately controlled by conventional therapy. Adverse Effects: Headache, flushing, hypotension, dizziness, and oral ulcers. Contraindications: Severe hypotension, cardiogenic shock, and concomitant use with phosphodiesterase-5 inhibitors.
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  Ivabradine ↓ Blocks Funny (If)Channels in SA Node ↓ ↓ Pacemaker Current ↓ ↓ Heart Rate ↓ ↑ Diastolic Filling Time ↓ ↑ Coronary Blood Flow ↓ ↓ Myocardial Oxygen Demand ↓ Relief of Angina 5. IF CHANNEL INHIBITOR
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  Therapeutic Effects Ivabradine lowersheart rate without reducing myocardial contractility or blood pressure. Clinical Uses: Used in chronic stable angina and chronic heart failure in patients with sinus rhythm. Adverse Effects: Bradycardia, luminous phenomena (phosphenes), atrial fibrillation, and headache. Contraindications: Acute myocardial infarction, severe hypotension, severe bradycardia, sick sinus syndrome, and severe hepatic impairment.
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  Ranolazine / Trimetazidine ↓ ImproveMyocardial Energy Metabolism ↓ ↓ Fatty Acid Oxidation ↓ ↑ Glucose Oxidation ↓ Efficient ATP Production ↓ ↓ Myocardial Ischemia ↓ Relief of Anginal Symptoms 6. METABOLIC MODULATORS
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  Therapeutic Effects: Thesedrugs improve myocardial efficiency and reduce ischemic symptoms without significantly affecting heart rate or blood pressure. Clinical Uses: Used as add-on therapy in chronic stable angina inadequately controlled by first-line drugs. Adverse Effects Ranolazine may cause constipation, nausea, dizziness, headache, and QT interval prolongation. Trimetazidine may cause gastrointestinal disturbances, dizziness, and rarely extrapyramidal symptoms. Contraindications Ranolazine is contraindicated in severe hepatic impairment and pre-existing QT prolongation. Trimetazidine should be avoided in patients with Parkinson's disease and severe renal impairment.