Ranolazine

What is Ranolazine?

• Ranolazine (Ranexa) is an antianginal used to treat heart related chest pain.

Ranolazine

What are the uses of this medicine?

• Ranolazine (Ranexa) is a prescription medicine used to treat angina that keeps coming back (chronic angina).
• RANEXA may be used with other medicines that are used for heart problems and blood pressure control.

How does this medicine work?

• Ranolazine (ra nol' a zeen) is a piperazine derivative which has unique activity against symptoms of angina pectoris.
• Its mechanism of action is unclear, but is believed to involve inhibition of fatty acid oxidation and blockage of the inward sodium currents in cardiomyocytes which reduces intracellular calcium accumulation and improves left ventricular function.
• Unlike other antiangina agents, ranolazine does not decrease heart rate, blood pressure or vascular resistance.
• In multiple clinical trials, extended release formulations of ranolazine were shown to reduce angina attacks and prolong exercise tolerance in patients with coronary artery disease.
• It also appears to have some degree of antiarrhythmia activity.

Who Should Not Use this medicine ?

This medicine cannot be used in patients who: take any of the following medicines:

• for fungus infection: ketoconazole (Nizoral®), itraconazole (Sporanox®, Onmel™)
• for infection: clarithromycin (Biaxin®)
• for depression: nefazodone
• for HIV: nelfinavir (Viracept®), ritonavir (Norvir®), lopinavir and ritonavir (Kaletra®), indinavir (Crixivan®), saquinavir (Invirase®)
• for tuberculosis (TB): rifampin (Rifadin®), rifabutin (Mycobutin®), rifapentine (Priftin®)
• for seizures: phenobarbital, phenytoin (Phenytek®, Dilantin®, Dilantin-125®), carbamazepine (Tegretol®)
• St. John's wort (Hypericum perforatum)

• have scarring (cirrhosis) of your liver.

What drug interactions can this medicine cause?

RANEXA may affect the way other medicines work and other medicines may affect how RANEXA works.

Tell your doctor if you take medicines:

• for your heart
• for cholesterol
• for diabetes
• for infection
• for fungus
• for transplant
• for nausea and vomiting because of cancer treatments
• for mental problems

Is this medicine FDA approved?

• Ranolazine was approved for use in the United States in 2006 and current indications are for chronic angina, either alone or in combination with other angina medications (such as beta blockers or calcium channel blockers).

How should this medicine be used?

Recommended dosage:

• 500 mg twice daily and increase to 1000 mg twice daily, based on clinical symptoms.

Administration:

• Take RANEXA exactly as your doctor tells you.
• Your doctor will tell you how much RANEXA to take and when to take it.
• Do not change your dose unless your doctor tells you to.
• Tell your doctor if you still have symptoms of angina after starting RANEXA.
• Take RANEXA by mouth, with or without food.
• Swallow the RANEXA tablets whole. Do not crush, break, or chew RANEXA tablets before swallowing.
• If you miss a dose of RANEXA, wait to take the next dose of RANEXA at your regular time. Do not make up for the missed dose. Do not take more than 1 dose at a time.
• If you take too much RANEXA, call your doctor, or go to the nearest emergency room right away.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Extended-release tablets: 500 mg, 1000 mg

This medicine is available in fallowing brand namesː

• RANEXA

What side effects can this medication cause?

The most common side effects of this medicine include:

• dizziness
• headache
• constipation
• nausea

RANEXA may cause serious side effects, including:

• changes in the electrical activity of your heart called QT prolongation.
• kidney failure in people who already have severe kidney problems.

What special precautions should I follow?

• Ranolazine blocks IKr and prolongs the QTc interval in a dose-related manner. Little data available on high doses, long exposure, use with QT interval-prolonging drugs, potassium channel variants causing prolonged QT interval, in patients with a family history of (or congenital) long QT syndrome, or in patients with known acquired QT interval prolongation.
• Acute renal failure has been observed in some patients with severe renal impairment (creatinine clearance [CrCL] < 30 mL/min) while taking RANEXA. Monitor renal function after initiation and periodically in patients with moderate to severe renal impairment (CrCL<60 mL/min). If acute renal failure develops, discontinue RANEXA.
• Chronic ranolazine therapy has not been associated with serum enzyme elevations, but has been linked to rare cases of mild, clinically apparent liver injury.

What to do in case of emergency/overdose?

Symptoms of overdosage may include:

• Hypotension
• QT prolongation
• bradycardia
• myoclonic activity
• severe tremor
• unsteady gait/incoordination
• dizziness
• nausea
• vomiting
• dysphasia
• hallucinations
• diplopia
• paresthesia
• confusion
• syncope

Treatment of overdosage:

• In addition to general supportive measures, continuous ECG monitoring may be warranted in the event of overdose.
• Since ranolazine is about 62% bound to plasma proteins, hemodialysis is unlikely to be effective in clearing ranolazine.

Can this medicine be used in pregnancy?

• There are no available data on RANEXA use in pregnant women to inform any drug-associated risks.

Can this medicine be used in children?

• Safety and effectiveness have not been established in pediatric patients.

What are the active and inactive ingredients in this medicine?

Active ingredient: ranolazine

Inactive ingredients:

• 500 mg tablet: carnauba wax, hypromellose, magnesium stearate, methacrylic acid copolymer (Type C), microcrystalline cellulose, polyethylene glycol, sodium hydroxide, titanium dioxide, polyvinyl alcohol, talc, Iron Oxide Yellow, and Iron Oxide Red.
• 1000 mg tablet: carnauba wax, hypromellose, magnesium stearate, methacrylic acid copolymer (Type C), microcrystalline cellulose, polyethylene glycol, sodium hydroxide, titanium dioxide, lactose monohydrate, triacetin, and Iron Oxide Yellow.

Who manufactures and distributes this medicine?

Manufactured for:

• Gilead Sciences, Inc.
• Foster City, CA

What should I know about storage and disposal of this medication?

• Store RANEXA tablets at room temperature between 59° to 86°F (15° to 30°C).

• Dailymed label info on Ranolazine
• FDA Ranolazine