Ranolazine

Generic name: ranolazine
Brand name: Ranexa
Dosage form: oral tablet, extended release (1000 mg; 500 mg)
Drug class: Antianginal agents

Medically reviewed by A Ras MD.

What is ranolazine used for?

Ranolazine is a prescription medicine that is used to treat a type of long-term chest pain (stable angina) in some people.

Description

Ranexa (ranolazine) is available as a film-coated, non-scored, extended-release tablet for oral administration.

Ranolazine is a racemic mixture, chemically described as 1-piperazineacetamide, N-(2,6-dimethylphenyl)-4-[2-hydroxy-3-(2-methoxyphenoxy)propyl]-, (±)-. It has an empirical formula of C24H33N3O4, a molecular weight of 427.54 g/mole, and the following structural formula:

Ranolazine is a white to off-white solid. Ranolazine is soluble in dichloromethane and methanol; sparingly soluble in tetrahydrofuran, ethanol, acetonitrile, and acetone; slightly soluble in ethyl acetate, isopropanol, toluene, and ethyl ether; and very slightly soluble in water.

Ranexa tablets contain 500 mg or 1000 mg of ranolazine and the following inactive ingredients: carnauba wax, hypromellose, magnesium stearate, methacrylic acid copolymer (Type C), microcrystalline cellulose, polyethylene glycol, sodium hydroxide, and titanium dioxide. Additional inactive ingredients for the 500 mg tablet include polysorbate 80 and FD&C Yellow No. 6 Lake; additional inactive ingredients for the 1000 mg tablet include lactose monohydrate, triacetin, and Iron Oxide Yellow.

Mechanism of Action

The mechanism of action of ranolazine’s antianginal effects has not been determined. Ranolazine has anti-ischemic and antianginal effects that do not depend upon reductions in heart rate or blood pressure. It does not affect the rate-pressure product, a measure of myocardial work, at maximal exercise. Ranolazine at therapeutic levels can inhibit the cardiac late sodium current (INa). However, the relationship of this inhibition to angina symptoms is uncertain.

The QT prolongation effect of ranolazine on the surface electrocardiogram is the result of inhibition of IKr, which prolongs the ventricular action potential.

Before taking ranolazine, tell your doctor:

If you are allergic to ranolazine; any part of this medicine; or any other drugs, foods, or substances. Tell your doctor about the allergy and what signs you had.
If you have liver disease.
If you take any drugs (prescription or OTC, natural products, vitamins) that must not be taken with ranolazine, like certain drugs that are used for HIV, infections, or seizures. There are many drugs that must not be taken with ranolazine.

This is not a list of all drugs or health problems that interact with ranolazine.

Tell your doctor and pharmacist about all of your drugs (prescription or OTC, natural products, vitamins) and health problems. You must check to make sure that it is safe for you to take ranolazine with all of your drugs and health problems. Do not start, stop, or change the dose of any drug without checking with your doctor.

What are some things I need to know or do while I take ranolazine?

Tell all of your health care providers that you take ranolazine. This includes your doctors, nurses, pharmacists, and dentists.
Avoid driving and doing other tasks or actions that call for you to be alert until you see how ranolazine affects you.
To lower the chance of feeling dizzy or passing out, rise slowly if you have been sitting or lying down. Be careful going up and down stairs.
If you drink grapefruit juice or eat grapefruit often, talk with your doctor.
Do not use ranolazine to treat sudden chest pain. It will not help. Talk with your doctor.
Kidney failure has happened with ranolazine in people who already had kidney problems. Talk with the doctor.
If you are 75 or older, use ranolazine with care. You could have more side effects.
Tell your doctor if you are pregnant, plan on getting pregnant, or are breast-feeding. You will need to talk about the benefits and risks to you and the baby.

How is ranolazine best taken?

Use ranolazine as ordered by your doctor. Read all information given to you. Follow all instructions closely.

Take with or without food.
Swallow whole. Do not chew, break, or crush.
Keep taking ranolazine as you have been told by your doctor or other health care provider, even if you feel well.

What do I do if I miss a dose?

Skip the missed dose and go back to your normal time.
Do not take 2 doses at the same time or extra doses.

What are the side effects of ranolazine that I need to call my doctor about immediately?

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.
Signs of kidney problems like unable to pass urine, change in how much urine is passed, blood in the urine, or a big weight gain.
Chest pain that is new or worse.
A type of abnormal heartbeat (prolonged QT interval) can happen with ranolazine. Call your doctor right away if you have a fast heartbeat, a heartbeat that does not feel normal, or if you pass out.

What are some other side effects of ranolazine?

All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:

Dizziness or headache.
Constipation.
Upset stomach.

These are not all of the side effects that may occur. If you have questions about side effects, call your doctor. Call your doctor for medical advice about side effects.

You may report side effects to the FDA at 1-800-332-1088. You may also report side effects at https://www.fda.gov/medwatch.

If overdose is suspected:

If you think there has been an overdose, call your poison control center or get medical care right away. Be ready to tell or show what was taken, how much, and when it happened.

How do I store and/or throw out ranolazine?

Store at room temperature in a dry place. Do not store in a bathroom.
Keep all drugs in a safe place. Keep all drugs out of the reach of children and pets.
Throw away unused or expired drugs. Do not flush down a toilet or pour down a drain unless you are told to do so. Check with your pharmacist if you have questions about the best way to throw out drugs. There may be drug take-back programs in your area.