Ranolazine

Trade Names:
Ranexa
- Tablets, extended release 500 mg

Pharmacology

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Mechanism of action unknown. Ranolazine has antianginal and anti-ischemic effects that do not depend upon reductions in heart rate or BP.

Pharmacokinetics

Absorption

Mean steady state C _max is 2,569 ng/mL (range, 420 to 6,080 ng/mL); usually attained within 3 days of twice daily dosing. Bioavailability from oral solution about 76%.

Distribution

Protein binding is approximately 62%.

Metabolism

Extensively metabolized in gut and liver with less than 5% excreted unchanged. Primarily metabolized by CYP3A and to a lesser extent by CYP2D6.

Elimination

Apparent terminal t _½ is 7 h. Approximately 75% excreted in urine and 25% in feces.

Peak

Achieved between 2 and 5 h after oral dosing.

Special Populations

Plasma levels increase about 50%.

Increased plasma levels in patients with mild and moderate hepatic impairment.

No effect on pharmacokinetics of ranolazine.

Has not been evaluated.

Indications and Usage

Treatment of chronic angina.

Contraindications

Preexisting QT prolongation; hepatic impairment; QT prolonging drugs; moderately potent and potent CYP3A inhibitors (including diltiazem).

Dosage and Administration

PO 500 mg twice daily. May increase to 1,000 mg twice daily based on symptoms (max, 2,000 mg/day).

General Advice

• Can be used in combination with amlodipine, beta-blockers, nitrates, or antihypertensives.
• Administer without regard to meals. Administer with food if GI upset occurs.
• Advise patient to swallow tablet whole and not to crush, chew, or break.

Storage/Stability

Store tablets at controlled room temperature (59° to 86°F).

Drug Interactions

Plasma levels of these agents may be elevated, increasing the risk of side effects.

Avoid coadministration.

Use with caution.

Ranolazine plasma levels may be elevated, increasing the risk of side effects.

Ranolazine plasma levels may be elevated; do not coadminister.

Coadministration is contraindicated

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Palpitations (less than 2%).

CNS

Dizziness, headache (6%).

EENT

Tinnitus, vertigo (less than 2%).

GI

Constipation, nausea (4%); abdominal pain, dry mouth, vomiting (less than 2%).

Respiratory

Dyspnea (less than 2%).

Miscellaneous

Peripheral edema (less than 2%).

Precautions

Pregnancy

Category C .

Lactation

Undetermined.

Children

Safety and efficacy not established.

Elderly

Dose selection should be cautious, usually starting at the lower end of the dosing range, reflecting the greater frequency of decreased hepatic and renal function, and comorbidity.

Renal Function

May increase BP 10 to 15 mm Hg in patients with severe renal function impairment. Avoid in severe renal function impairment.

Hepatic Function

Contraindicated in patients with mild, moderate, or severe liver disease because of increased QTc-prolonging effect.

QT prolongation

Ranolazine can prolong the QTc interval in a dose related manner. Do not use doses greater than 1,000 mg twice daily, or in patients with known QT prolongation, history of ventricular tachycardia, or receiving drugs that prolong the QTc interval.

Tumor promotion

Ranolazine has been reported to promote tumor formation and progression to malignancy in mice.

Overdosage

Symptoms

No cases reported; expected symptoms include confusion, diplopia, dizziness, nausea, paresthesia, prolonged loss of consciousness, QT interval prolongation, syncope, vomiting.

Patient Information

• Ensure that patient understands that ranolazine is taken daily to reduce the frequency of angina attacks and is not to be used as needed to try to treat an acute angina episode.
• Advise patient to review the Patient Information leaflet carefully before starting therapy and to read and check for new information each time the medication is refilled.
• Advise patient that ranolazine is used in combination with at least 1 other antianginal medication and to continue to take other antianginal medications as prescribed by health care provider.
• Caution patient to take exactly as prescribed and not to change the dose or stop taking unless advised by health care provider.
• Caution patient that max daily dose is 2 tablets twice daily and to never exceed that amount because of risk of serious toxicity.
• Advise patient to take each dose without regard to meals, but to take with food if stomach upset occurs.
• Caution patient to swallow tablets whole and not to crush, chew, or break.
• Caution patient to avoid grapefruit juice and grapefruit-containing products while taking ranolazine.
• Review with patient and family the signs and symptoms of angina (eg, acute onset of pressure-like chest pain that may radiate down the left arm and/or into the neck or jaw, often associated with sweating and shortness of breath or difficulty breathing).
• Ensure that patient has SL nitroglycerin available at all times, knows when and how to use SL nitroglycerin, and what to do if angina pain worsens or fails to respond to SL nitroglycerin.
• Advise patient to notify health care provider if angina symptoms increase in frequency or severity, or if there is a sudden increase in the frequency of use of SL nitroglycerin.
• Caution patient that medication may cause dizziness or light-headedness, and to use caution driving or performing other tasks requiring alertness or coordination until tolerance is determined.
• Advise patient to discontinue therapy and contact health care provider immediately if any of the following occur: difficulty breathing, fainting, hives, itching, palpitations, skin rash, or unexplained shortness of breath.

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