Anti-anginal (Unit:- 2)

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Anti-anginal (Med Chem: 2) Notes Download

Keywords: Download PDF, Notes, PPT, Anti-anginal Drugs, Angina Pectoris, Vasodilators, Calcium Channel Blockers, Potassium Channel Openers, β-Adrenoceptor Antagonists, Metabolic Modifiers, Organic Nitrates, Structure-Activity Relationship

This document provides detailed notes on anti-anginal drugs, including their classification, mechanisms of action, therapeutic uses, and structure-activity relationships.

Anti-anginal (Med Chem: 2) Notes

Introduction

Angina pectoris, commonly referred to as angina, is characterized by severe chest pain caused by ischemia (lack of blood and oxygen supply) of the heart muscle. This ischemia results from obstruction or spasm of the coronary arteries, which supply blood to the heart. The primary cause of angina is coronary artery disease, often due to atherosclerosis of the cardiac arteries.

Unstable angina, often grouped with acute coronary syndrome, may present with symptoms such as worsening angina attacks, sudden onset of angina at rest, or angina lasting more than 15 minutes. These conditions can lead to myocardial infarction (heart attack) and require urgent medical attention.

Anti-anginal Drug Therapy

Anti-anginal drug therapy aims to restore the balance between oxygen supply and demand in the ischemic area of the myocardium. The drugs are classified as follows:

1. Vasodilators (Organic Nitrites and Nitrates): Amyl nitrite, Sodium nitrite, Nitroprusside sodium, Isosorbide dinitrate, Isosorbide mononitrate, Erythrityl tetranitrate, and Nitroglycerine.
2. Calcium Channel Blockers:
   • Arylalkylamines: Bencyclane, Bepridil hydrochloride, Caroverine, Cetiedil citrate, Diltiazem hydrochloride, Doprenilamine, Etafenone, Fendiline, Mecinarone, Prenylamine, Proadifen, and Terodiline.
   • Phenyldihydropyridine Derivatives: Amlodipine, Darodipine, Felodipine, Flordipine, Isrodipine, Mesudipine, Nicardipine, Nifedipine, Niludipine, Nilvadipine, Nimodipine, Nisoldipine, Nitrendipine, Oxodipine, and Riodipine.
   • Piperazine Derivatives: Cinnarizine, Flunarizine, and Lidoflazine.
   • Verapamil and Related Drugs: Anipamil, Dagapamil, Devapamil, Emopamil, Falipamil, Gallopamil, Methoxyverapamil, Ronipamil, Tiapamil, and Verapamil hydrochloride.
   • Miscellaneous Agents: Flutonidine, Fostedil, Perhexiline, and Piprofurol.
3. Potassium Channel Opener: Nicorandil.
4. β-Adrenoceptor Antagonists (β-Blockers): Atenolol, Metoprolol, Nadolol, and Propranolol.
5. Metabolic Modifiers: Ranolazine and Trimetazidine.

Therapeutic Uses

Different classes of anti-anginal drugs have the following therapeutic uses:

• Organic Nitrates: Used to treat ischemic symptoms of angina and congestive heart failure by acting through nitric oxide (NO) replacement therapy.
• Calcium Channel Blockers: Used to treat both stable and variant angina. They reduce afterload and oxygen demand in stable angina and relieve coronary artery spasm in variant angina.
• Potassium Channel Openers: Used in symptomatic patients awaiting surgery or angioplasty.
• β-Adrenergic Blockers: Used in combination with nitrates for angina treatment and as prophylactic treatment for chronic angina and post-myocardial infarction.

Structure-Activity Relationship

The structure-activity relationship (SAR) of anti-anginal drugs is influenced by lipophilicity, steric factors, and electronic interactions. Key SAR features include:

• β-Blockers: The O-CH2 group, aromatic ring, and secondary amine nitrogen are critical for activity. Substituents like isopropyl and tertiary butyl groups enhance activity.
• Calcium Channel Blockers: The dihydropyridine ring, secondary nitrogen, and bulky substituents like phenyl are essential for activity.

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