2024年10月15日星期二

Antianginal Drugs for Angina Pectoris_ A Comprehensive Overview


Antianginal Drugs for Angina Pectoris: A Comprehensive Overview

Angina pectoris, commonly referred to as angina, is a symptom of coronary artery disease characterized by chest pain or discomfort due to insufficient blood flow to the heart muscle. Antianginal drugs play a crucial role in managing this condition by improving the balance between myocardial oxygen supply and demand. This article provides an in-depth look at the various classes of antianginal medications used to treat angina pectoris.

Nitrates are one of the oldest and most widely used antianginal drugs. They work by releasing nitric oxide, which causes vasodilation of both coronary and peripheral blood vessels. This action reduces preload and afterload on the heart, thereby decreasing myocardial oxygen demand. Short-acting nitrates, such as sublingual nitroglycerin tablets or sprays, provide rapid relief for acute anginal episodes. Long-acting nitrates, like isosorbide mononitrate and isosorbide dinitrate, are used for chronic angina management. However, tolerance can develop with continuous use, necessitating a nitrate-free interval in dosing regimens.

Beta-blockers form another cornerstone of angina treatment. These drugs reduce heart rate, blood pressure, and myocardial contractility, effectively lowering oxygen demand. They are particularly beneficial in patients with concurrent hypertension or a history of myocardial infarction. Commonly prescribed beta-blockers include metoprolol, atenolol, and carvedilol. Some newer beta-blockers, like nebivolol, also have vasodilatory properties, offering additional benefits in angina management.

Calcium channel blockers (CCBs) are the third major class of antianginal drugs. They reduce myocardial oxygen demand by decreasing afterload through peripheral vasodilation and, in some cases, by reducing heart rate and contractility. CCBs are categorized into dihydropyridines (e.g., amlodipine, nifedipine) and non-dihydropyridines (e.g., verapamil, diltiazem). Dihydropyridines primarily cause peripheral vasodilation, while non-dihydropyridines also significantly affect heart rate and contractility.

Ranolazine, a newer antianginal agent, works as a late sodium current inhibitor. It reduces intracellular calcium overload in ischemic myocardium, improving diastolic function without affecting heart rate or blood pressure. Ranolazine is particularly useful in patients with diabetes or those who cannot tolerate heart rate-lowering medications.

Ivabradine, a selective inhibitor of the If current in the sinoatrial node, reduces heart rate without affecting blood pressure or myocardial contractility. It is beneficial in patients with chronic stable angina who have a contraindication to beta-blockers or in combination with beta-blockers when optimal heart rate control is not achieved.

Trimetazidine, a metabolic modulator, enhances glucose oxidation and reduces fatty acid oxidation in the myocardium, improving cardiac efficiency without hemodynamic effects. While widely used in Europe and Asia, it is not approved for use in the United States.

The choice of antianginal therapy depends on various factors, including the patient's comorbidities, contraindications, and individual response to treatment. Often, a combination of drugs from different classes is necessary to achieve optimal symptom control. Regular follow-up and dose adjustments are essential to ensure efficacy and minimize side effects.

In addition to pharmacological interventions, lifestyle modifications play a crucial role in managing angina pectoris. These include smoking cessation, regular exercise, weight management, and stress reduction. Patients are also often prescribed antiplatelet agents like aspirin to reduce the risk of thrombotic events associated with coronary artery disease. 

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