What are anti-anginal (antianginal) medications?

From the Guidelines

First-line treatment for angina symptoms should include beta-blockers and/or calcium channel blockers (CCBs) to control heart rate and symptoms, as recommended by the 2019 ESC guidelines 1. The main classes of antianginal medications include nitrates, beta-blockers, and calcium channel blockers.

• Nitrates like nitroglycerin provide immediate relief by dilating blood vessels, reducing cardiac workload, and are recommended for immediate relief of effort angina 1.
• Beta-blockers like metoprolol or atenolol reduce heart rate and contractility, decreasing oxygen demand.
• Calcium channel blockers such as amlodipine or diltiazem relax arterial smooth muscle, improving blood flow and reducing cardiac workload. For stable angina, a combination approach is often used, starting with a beta-blocker or calcium channel blocker plus nitrates as needed for acute episodes.
• If angina symptoms are not successfully controlled on a beta-blocker or a CCB, the combination of a beta-blocker with a dihydropyridine calcium channel blocker (DHP-CCB) should be considered, as per the 2019 ESC guidelines 1.
• Long-acting nitrates should be considered as a second-line treatment option when initial therapy with a beta-blocker and/or a non-DHP-CCB is contraindicated, poorly tolerated, or inadequate to control angina symptoms 1.
• Nicorandil, ranolazine, ivabradine, or trimetazidine should be considered as a second-line treatment to reduce angina frequency and improve exercise tolerance in subjects who cannot tolerate, have contraindications to, or whose symptoms are not adequately controlled by beta-blockers, CCBs, and long-acting nitrates 1. It's essential to address underlying coronary artery disease through lifestyle modifications, antiplatelet therapy, statins, and blood pressure control, and patients should be educated about proper medication use, especially sublingual nitroglycerin, and instructed to seek emergency care if chest pain persists after three doses taken 5 minutes apart.

From the FDA Drug Label

Ranolazine Extended-Release Tablets is an antianginal indicated for the treatment of chronic angina. DOSAGE AND ADMINISTRATION 500 mg twice daily and increase to 1000 mg twice daily, based on clinical symptoms The primary use of ranolazine is as an antianginal medication for the treatment of chronic angina.

• The recommended dosage is 500 mg twice daily, which can be increased to 1000 mg twice daily based on clinical symptoms 2 2.

From the Research

Antianginal Medications

• Nitrates are highly effective in terminating acute attacks of angina pectoris and in the prophylaxis of symptomatic and asymptomatic myocardial ischemia 3
• Preload reduction by venodilatation is the prevailing mechanism of nitrates in patients with chronic stable angina, distinguishing them from beta and calcium-channel blockers 3
• Nitrates dilate coronary arteries not only in pre- and poststenotic vessels, but also in eccentric lesions, and seem to be the physiological substitute for endothelium-derived relaxing factor in patients with endothelial dysfunction 3

Nitrate Tolerance

• Nitrate tolerance is a clinically relevant loss of the anti-ischemic effects of nitrates, which can occur with repetitive, continuous use 3, 4
• Intermittent therapy with once-daily ingestion of high-dose sustained-release isosorbide dinitrate or isosorbide-5-mononitrate can prevent the development of tolerance 3
• A daily low-nitrate interval is required to prevent tolerance development, with a 12-h patch-free interval recommended to prevent tolerance in most patients 3

Treatment of Angina

• Angina pectoris is defined as substernal chest pain, pressure, or discomfort that is typically exacerbated by exertion and/or emotional stress, and is relieved by rest and nitroglycerin 5
• Pharmacologic therapy for angina includes β-blockers, nitrates, calcium channel blockers, and ranolazine, with additional agents used in other countries 5
• Revascularization is indicated in certain high-risk individuals, and can improve angina, but a substantial percentage of patients may return with recurrent or continued angina 5

Management of Stable Angina

• Management of stable angina pectoris includes antianginal medications, medications to prevent progression of atherosclerosis, and aggressive treatment of causative risk factors 6
• Antianginal medications commonly used include nitrates, beta-blockers, calcium channel blockers, and ranolazine, with antiplatelet agents, statins, and angiotensin-converting enzyme inhibitors used to prevent progression of atherosclerosis 6
• Aggressive risk factor control with diet, exercise, treatment of diabetes, hypertension, and dyslipidemia, and strategies to stop smoking and reduce weight should be part of the treatment strategy in all patients 6