Ranolazine (Oral)

Ranolazine is a prescription drug used for the treatment of chronic angina.

Overview

Ranolazine is a cardiac drug used for the treatment of chronic angina. It is sold under the brand name Ranexa by Gilead Sciences, and was approved for use in 2006 in the U.S.

It can be used at the same time with beta blockers, calcium channel blockers, nitrates, antiplatelet therapy, ACE inhibitors, lipid-lowering therapy, and angiotensin receptor blockers.

Ranolazine works by inhibiting persistent or late inward sodium current in heart muscles. By doing so, it leads to reduced tension in the heart wall, which means that there are reduced oxygen requirements for the muscle. It also prevents calcium overload. These interactions improve blood flow to the heart, which makes the heart work more efficiently. The exact mechanism by which Ranolazine is not entirely known.

Ranexa is the most common brand name for Ranolazine, and is manufactured and sold by Gilead Sciences. It was originally developed by Syntex Inc 1985, and this company ran tests on the drug until 1994. After years of testing, a sustained-release formulation of Ranolazine was created, which was more effective.

Syntex was acquired by Roche in 1994 and, in 1996, a subsidiary of Roche licensed the North American and European rights to Ranolazine. In 2006, this same subsidiary acquired the remaining worldwide rights to Ranolazine. In 2009, Gilead Sciences acquired this subsidiary and now sells the product worldwide, expanding into Asia, in addition to North America and Europe. Today, Ranolazine is available through prescription in the U.S. The patent on brand name Ranexa in the U.S. expires in 2019, after which time other pharmaceutical companies will be able to produce and sell generic forms of the drug and sell it under their own brand names.

Conditions Treated

  • Chronic angina

Type of Medicine

  • Cardiac drug

Side Effects

The most common side effect of taking Ranolazine is dizziness. Though this is more common, you should still inform your doctor if you experience dizziness while taking Ranolazine, as it may mean that your dosage or this medication is not right for you.

Other more rare, but potentially serious side effects include:

  • Bloating or swelling of the face, arms, hands, lower legs, or feet
  • Ringing or buzzing in the ears
  • Difficult or labored breathing
  • Fast and/or irregular heartbeat and breath
  • Loss of hearing
  • Lightheadedness
  • Sudden and unusual weight gains or losses
  • Abnormal agitation
  • Blood in urine and difficulty urinating
  • Blurry vision and confusion
  • "Pins and needles" or tingling sensations
  • Abnormal chest pain, discomfort, or tightness in the chest
  • Chills or cold sweats
  • Depression
  • Dizziness or lightheadedness when standing up from a reclining position
  • Fainting spells
  • Headache
  • Irritability
  • Lethargy and unusual, extreme tiredness
  • Uncontrollable muscle twitching
  • Nausea
  • Seizures

If any of these symptoms occur, inform a medical professional immediately. In addition to this list, there may be other side effects. If you experience anything unusual when taking Ranolazine, inform your doctor immediately.

There are other well-known symptoms that may not require the attention of a doctor. However, if they are uncomfortable and seriously hinder your daily activity, you can talk to a doctor about whether another medication, dosage, or treatment option might be better for you. These less serious side effects include:

  • Difficulty having a bowel movement (stool)
  • Dry mouth
  • Stomach and abdominal pain
  • Loss of strength

Aside from these side effects, watch out for signs of an allergic reaction to Ranolazine. If you experience any signs of an allergic reaction, you should alert a medical professional immediately, as you may need to stop taking Ranolazine. Signs of an allergic reaction include:

  • Hives
  • Rashes
  • Difficulty breathing
  • Swelling of the face, tongue, throat, or lips

Side effects can occur differently when you first start taking Ranolazine, when you change your dosage, or as you age or have other changes in your life and habits. If any of these side effects become serious or worrisome, always tell a doctor.

Dosage

When you first start taking Ranolazine, the recommended dosage is 500 mg, taken twice per day. As you get accustomed to it, this dosage usually goes up to 1,000 mg, also twice per day. 1,000 mg twice per day is the maximum recommended daily dosage. Depending on whether you are taking other medications, your doctor may recommend staying with the lower dosage of 500 mg, twice daily, as Ranolazine can sometimes react with different drugs in a way that augments its effects. This is usually the case with patients who are also taking a class of drugs known as moderate CYP3A inhibitors, such as diltiazem, verapamil, erythromycin, fluconazole, and patients who consume grapefruit-containing products. In patients who are also also taking strong CYP3A inhibitors, Ranolazine is contraindicated.

Ranolazine usually comes in a tablet form, which is taken orally. Do not crush or chew the tablet. Ranolazine can be taken with or without food. These dosages should be taken around the same time every day. If you miss a dose, do not take a double dose, or a dose closer to your next dose. Simply wait until your next scheduled dosage and take it as normal.

If you experience negative side effects and wish to stop taking Ranolazine, you should consult with your doctor about other options or dosages. Do not suddenly stop taking Ranolazine without consulting your doctor, as this could cause adverse side effects. If you start or stop using a new medication, also tell your doctor, as this may effect your recommended dosage.

Interactions

Ranolazine interacts with other certain drugs, and it is important to speak to your doctor before taking Ranolazine or before taking a new medication while on Ranolazine for this reason.

Ranolazine should not be taken with strong CYP3A inhibitors, some of which include itraconazole, ketoconazole, clarithromycin, nelfinavir, nefazodone, indinavir, ritonavir, snd saquinavir.

Ranolazine should be carefully used in decreased dosages (usually this is 500 mg, taken twice daily) in patients who take moderate CYP3A inhibitors, some of which include verapamil, diltiazem, fluconazole, erythromycin, and foods or drinks that contain grapefruit products.

Ranolazine should not be taken with CYP3A inducers. CYP3A inducers include rifabutin, rifampin, rifapentine, phenytoin, phenobarbital, St. John's wort and carbamazepine. Let your doctor know if you take any of these medications.

Warnings

Ranolazine has not been tested in patients under 18 years of age, and should thus not be used by children. If you have a child who suffers from chronic angina, speak to your doctor about what options might be best for your child. They may be able to recommend a different medication or dosage. Ranolazine may not be effective or could have adverse effects in patients over the age of 75. Patients over 75 who take Ranolazine should check with their doctor first, and be aware of any occurring side effects. There may be other options if Ranolazine is not right for you.

Because Ranolazine is known to cause headaches and dizziness, as well as some less common side effects, it is important that you understand how Ranolazine will effect you. Do not drive or operate heavy machinery when you start Ranolazine until you know how you respond to it. Do not drive or operate heavy machinery when you change dosages of Ranolazine, as this may have a similar effect.

Ranolazine is used for the treatment of chronic angina, and should not be used to treat acute angina episodes. It will not be effective.

Do not take Ranolazine if you have cirrhosis of the liver. Tell a doctor if you have a liver disease, kidney disease, or heart rhythm disorder before starting Ranolazine.

It is possible to overdose on Ranolazine. Overdose of Ranolazine can cause increased dizziness, nausea, and vomiting and can cause serious harm. That is why it is important that you never take more than your recommended dosage, and never take a double dose because you have missed one. If you believe that you or someone you know has overdosed on Ranolazine, consult emergency medical services immediately.

Signs of an overdose include:

  • Nausea (worse than usual)
  • Vomiting
  • Dizziness
  • Double vision
  • Fainting
  • Uncontrollable shaking in any part of your body
  • Difficulty speaking
  • Hallucinations

Patients who are pregnant or planning to become pregnant should consult their doctor when taking Ranolazine. You should also alert your doctor if you become pregnant while taking Ranolazine. Also tell your doctor if you are breastfeeding, as the effects of breastfeeding while taking Ranolazine are not known. Effects of taking Ranolazine while pregnant are not entirely known, and a doctor can help you determine what is best for you and your baby.

Always tell your doctor if you stop or start using any other medications, vitamins, dietary supplements, or minerals.

Storage

Ranolazine should be stored at 25°C, if possible. In cases where this is not possible, you can store it in a safe place between 15°C and 30°C. Do not store Ranolazine in extreme cold or heat or where it could get wet.

Like all medications, Ranolazine should be stored in a safe and secure place, out of the reach of children. Be sure that all lids and child safety locks are securely in place when storing. It is best to store medications in dry places, out of direct sunlight. Bathrooms may be too damp for some medications.

If your prescription of Ranolazine expires or you have expired Ranolazine in storage, be sure to dispose of it safely. The best way to dispose of expired or unneeded medications is through a medicine take-back program. You can talk to your local pharmacist about where and when these take-back programs take place. If your local community does not have these take-back programs, you should refer to the FDA's Safe Disposal of Medicines guidance. Never flush prescription medicines down the toilet or in the trash. Before throwing out empty prescription bottles of Ranolazine, scratch any personal details off of the bottle for your own security.

Summary

Ranolazine is a cardiac drug used for the treatment of chronic angina. It is most commonly sold under the brand name Ranexa by Gilead Sciences.

Ranolazine is taken orally, and comes in the form of an extended-release tablet. It is usually taken in doses of 500 mg or 1,000 mg, taken twice per day at around the same time every day. 1,000 mg twice per day is the maximum recommended daily dosage. Always tell your doctor about your side effects and other medications you are taking, as these could change the recommended dosage you should be taking.

Ranolazine works by inhibiting persistent or late inward sodium current in heart muscles. By doing so, it leads to reduced tension in the heart wall, which means that there are reduced oxygen requirements for the muscle. It also prevents calcium overload.

There are many observed side effects to Ranolazine, with dizziness being the most common. You should review all side effects when taking Ranolazine, as some side effects are more serious, and some may require the attention of a medical professional.

Ranolazine interacts with other certain drugs, and it is important to speak to your doctor before taking Ranolazine or before taking a new medication while on Ranolazine for this reason. Ranolazine should not be taken with strong CYP3A inhibitors, and when taken with moderate CYP3A inhibitors, the recommended dosage is often lowered to 500 mg, taken twice daily.

Ranolazine has not been tested in patients under 18 years of age, and should thus not be used by children. Ranolazine may not be effective or could have adverse effects in patients over the age of 75. Patients over 75 who take Ranolazine should check with their doctor first, and be aware of any occurring side effects.

Ranolazine is used for the treatment of chronic angina, and should not be used to treat acute angina episodes. It will not be effective.

It is possible to overdose on Ranolazine and overdose can cause increased dizziness, nausea, and vomiting and can cause serious harm. If you believe that you or someone you know has overdosed on Ranolazine, consult emergency medical services immediately or call the U.S. Poison Help line at 1-800-222-1222.

Patients who are pregnant or planning to become pregnant should consult their doctor when taking Ranolazine.

Ranolazine should be stored in a safe, dry place at 25°C, if possible. In cases where this is not possible, you can store it in a safe place between 15°C and 30°C. Keep Ranolazine stored securely out of the reach of children and dispose of it safely.

If your prescription of Ranolazine expires or you have expired Ranolazine in storage, be sure to dispose of it safely. The best way to dispose of expired or unneeded medications is through a medicine take-back program. You can talk to your local pharmacist about where and when these take-back programs take place. If your local community does not have these take-back programs, you should refer to the FDA's Safe Disposal of Medicines guidance. Never flush prescription medicines down the toilet or in the trash.

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Last Reviewed:
February 01, 2018
Last Updated:
January 27, 2018