Antianginals: Uses, common brands, and safety info

In 1867, amyl nitrate was recognized as the first effective treatment for acute angina, a painful heart condition caused by a narrowing of the arteries of the heart. In 1879, nitroglycerin was discovered to be similarly effective for treating coronary artery disease. In the 1960s the first beta blocker (Inderal, generic name propranolol), was introduced and provided for long-term management for patients with stable angina. Following the discovery of Inderal, and with a better understanding of the causes of angina, new pharmacological therapies began to emerge with different mechanisms of action that could be tailored to the underlying causes of the heart disease.

The following table lists the antianginal medications approved for use by the U.S. Food and Drug Administration (FDA), followed by information on how they work, what conditions they treat, safety, and cost.

Other antianginals

• Procardia XL (nifedipine ER)

• Sular (nisoldipine)

• Nitroglycerin

• GoNitro (nitroglycerin)

• Nitrolingual (nitroglycerin)

• Nitromist (nitroglycerin)

• Nitrostat (nitroglycerin)

• Nitro-bid (nitroglycerin topical)

• Pindolol

• Propranolol HCl

• Propranolol HCl ER

• Inderal LA (propranolol HCl ER)

• Ranolazine ER

• Ranexa (ranolazine ER)

• Timolol maleate

• Verapamil HCl

• Verapamil HCl ER

• Calan SR (verapamil HCL ER)

What are antianginals?

Antianginal is a term used to describe a wide variety of oral medicines used to prevent or provide relief from stable angina, also known as angina pectoris, a condition caused by reduced coronary blood flow to the heart causing chest pain. Unstable angina is a more serious vascular disease and should be treated as an emergency requiring medical treatment.

How do antianginals work?

Drug treatment for angina focuses on two pharmacological actions: 1) improve oxygen delivery to the heart from the coronary artery and 2) decrease the oxygen demand of the heart. The different antianginal agents have different mechanisms of action to achieve these goals: 

• Nitrates (e.g., nitroglycerin, isosorbide dinitrate, and isosorbide mononitrate) act as a vasodilator by relaxing the smooth muscles within the blood vessels, widening them and making it easier for blood and oxygen to reach the heart.

• Beta blockers (e.g., propranolol, atenolol, pindolol, and metoprolol), considered first-line therapies for angina along with calcium channel blockers,  block the effects of adrenaline, which slows the heart, reducing how hard it has to work and its need for oxygen. Beta blockers also help dilate blood vessels to the heart. 

• Calcium channel blockers, also known as calcium antagonists (e.g., diltiazem, nifedipine, nimodipine, and verapamil), prevent calcium from transferring into cells lining the blood vessels allowing them to relax and open resulting in an increase in blood and oxygen reaching the heart. Calcium channel blockers, along with beta blockers, are considered first-line therapies for angina.

• Ranolazine is relatively new and the exact mechanism of action is unknown. It is thought ranolazine makes the heart muscles work more efficiently by improving their metabolism resulting in reduced angina symptoms. 

What are antianginals used for?

Antianginal medicines differ in their approved uses based on their mechanisms of action.

• Short-acting nitrates are absorbed quickly and are used for immediate relief of symptoms of angina attacks.

• Long-acting nitrates are intended to help with long-term prevention of angina symptoms.

• Beta blockers are used over the long term to reduce or prevent angina symptoms. Beta blockers are also prescribed to treat high blood pressure (hypertension), atrial fibrillation (irregular heartbeat), congestive heart failure, myocardial infarction (heart attack), and even such varied conditions as migraine headaches and tremors.

• Calcium channel blockers channel blockers are used for the long-term management of chronic stable angina as well as for other cardiovascular diseases such as hypertension and arrhythmias. Calcium channel blockers may also be combined with statins to treat angina.

• The piperazine derivative ranolazine is indicated for the long-term treatment of chronic angina and is often used in combination with nitrates, beta blockers, and calcium channel blockers.

Types of antianginals

Nitrates

• Short-acting nitrates

  • GoNitro (nitroglycerin)

  • Nitrolingual (nitroglycerin)

  • NitroMist (nitroglycerin)

  • Nitrostat (nitroglycerin)

• Long-acting nitrates

  • Isosorbide dinitrate

  • Isosorbide mononitrate

Beta blockers

• Tenormin (atenolol)

• Corgard (nadolol) 

• Pindolol 

• Inderal (propranolol)

• Lopressor (metoprolol)

• Kapspargo Sprinkle (metoprolol)

• Timolol 

Calcium channel blockers 

• Norvasc (amlodipine)

• Cardizem, Cartia XT, Matzim LA, Taztia XT, Tiazac ER (

  diltiazem) 

• Felodipine ER

• Cardene SR (nicardipine)

• Procardia, Procardia XL (nifedipine)

• Sular (nisoldipine)

• Calan, Calan SR, Verelan, Verelan PM (verapamil)

Piperazine derivative

• Ranexa (ranolazine) 

Who can take antianginals?

Adults

In double-blind controlled trials, the safety and effectiveness of antianginal agents have been established in adults and the drugs are well tolerated and rarely cause serious side effects. 

Children and adolescents

Because angina is a rare condition in younger people, there have been no cardiology clinical trials conducted on children or adolescents and therefore the safety and effectiveness of antianginal medicines have not been established nor are they recommended.

Seniors

In general, randomized clinical trials of antianginal agents did not include sufficient numbers of patients 65 and older to determine if they responded differently from younger patients. Dose selection for elderly patients should be done cautiously, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased liver, kidney, or cardiac function, and due to the likelihood of other disease states or other drug therapies.

Women who are pregnant or breastfeeding 

There are no well-controlled clinical studies in pregnant women and the use of antianginal medicines. They should only be used if the potential benefit justifies the potential risk to the fetus.

Because many of the antianginal drugs are excreted in human milk, caution should be exercised when considering antianginal medicine use in a nursing woman.

A woman’s healthcare provider is the best source of information when considering the use of antianginal medicines while pregnant or breastfeeding.

Are antianginals safe?

Antianginal medicines are considered safe and generally well tolerated. Because there are several classes of medications approved for the treatment of angina and each has the potential for adverse effects, selection of the initial drug or adjustment of therapy is based on each individual patient’s health status (e.g., resting heart rate, blood pressure ranges, cardiac status, other medications being taken, and other disease states present.)

Recalls

There are no current recalls as of October 2021.

Contraindications

You should not take antianginal medicine if you are allergic to any of the active or inactive ingredients. Use caution when considering specific antianginal therapy if you have any of the following conditions:

• Patients should not use nitrates if they are taking PDE5 inhibitors, such as Viagra (sildenafil), Cialis (tadalafil), or Levitra (vardenafil), as the combined use can cause severe hypotension (abnormally low blood pressure), syncope (fainting), or myocardial ischemia (reduced blood flow to the heart).

• Beta blockers should not be used in patients experiencing cardiogenic shock (damage to the heart so that it no longer pumps blood effectively), sinus bradycardia (a type of slow heartbeat), or bronchial asthma.

• Calcium channel blockers should not be used in patients with either sick sinus syndrome (the inability of the heart’s natural pacemaker to generate normal heartbeats) or second- or third-degree AV block except in patients with a ventricular pacemaker, patients with hypotension (less than 90 mm Hg systolic), or patients experiencing cardiogenic shock.

• Ranexa should not be used by patients with cirrhosis of the liver or taking medicines that inhibit or activate an enzyme in the body called CYP3A4; these drugs include clarithromycin, erythromycin, diltiazem, itraconazole, ketoconazole, ritonavir, verapamil, phenobarbital, phenytoin, rifampicin, and glucocorticoids as well as supplements such as goldenseal and St. John’s Wort and grapefruit juice.

Are antianginals controlled substances?

No, antianginals are not controlled substances.

Common antianginal side effects

The following are potential common side effects when taking antianginal medicines, although each individual class may have different adverse event profiles. This is not an exhaustive list and you should always talk to your healthcare professional and seek medical advice about what adverse reactions to expect and how to address them.

• Headache 

• Vertigo (sensation of feeling off-balance)

• Dizziness

• Weakness

• Palpitation (rapid, strong, or irregular heartbeat)

• Hypotension (low blood pressure)

• Bradycardia (slow heart rate)

How much do antianginals cost?

Antianginal medicines have a wide price range depending on the specific drug, quantity, dosage, and dosing regimen. Medicare and most insurance plans cover antianginal medicines. Since most antianginals are available in generic formulations, they are much less expensive than their brand-name counterparts. A SingleCare discount card could reduce prescription costs up to 80% at participating pharmacies.