Classifications: antianginal agent; Therapeutic:antianginal; partial fatty acid oxidation (pfox) inhibitor
Pregnancy Category: C
500 mg extended release tablets
Complete mechanism of action is unknown. Ranolazine is a partial fatty-acid oxidation inhibitor that shifts myocardial metabolism
away from fatty acids to glucose. This shift in fuel source requires less oxygen for oxidation and results in decreased
oxygen demand by the myocardium.
Ranolazine improves exercise tolerance and angina symptoms. It has no effect on heart rate or hemodynamic action of the
Treatment of chronic stable angina in patients who are unresponsive or cannot tolerate other antianginal agents. Used in
combination with amlodipine, beta-blockers, or nitrates.
Mild, moderate, or severe hepatic impairment; severe renal impairment, renal failure, hypokalemia, hypomagnesemia; preexisting
QT prolongation, history of torsades de pointes, ventricular tachycardia, ventricular arrhythmias, significant bradycardia,
acute MI, cardiac arrhythmia; concurrent use with QT prolongation drugs; grapefruit juice; concurrent use of potent or moderately
potent CYP3A inhibitors; pregnancy (category C); lactation. Safety and efficacy in children have not been established.
History of QT prolongation; older adult.
Route & Dosage
|Chronic Stable Angina
Adult: PO 5001000 mg b.i.d.
- Must be swallowed whole. Should not be crushed, broken, or chewed.
- Store at 15°30° C (59°86° F).
Adverse Effects (≥1%)Body as a Whole:
Peripheral edema. CNS: Dizziness,
Abdominal pain, constipation,
dry mouth, nausea, vomiting. Respiratory: Dyspnea
. Special Senses:
Diagnostic Test Interference
Ranolazine is not known to interfere with any diagnostic laboratory test.
Inhibitors of P-glycoprotein (e.g., ritonavir, cyclosporine
) may increase ranolazine absorption. Ranolazine increases the plasma
concentrations of digoxin
Inhibitors of CYP3A4 [e.g., diltiazem, grapefruit juice, hiv protease inhibitors
, ketoconazole, macrolide antibiotics
] can increase plasma
levels and QTc
a CYP2D6 inhibitor, increases the plasma
levels of ranolazine. class i
or iii antiarrhythmics
(e.g., quinidine, dofetilide, sotalol
can cause additive increases in QTc
73% of PO dose absorbed. Peak:
25 h. Distribution:
62% protein bound. Metabolism:
Extensive hepatic metabolism
75% in urine; 25% in feces. Half-Life:
Assessment & Drug Effects
- Monitor ECG at baseline and periodically for prolongation of the QTc interval.
- Lab tests: Baseline and periodic LFTs.
- Monitor blood levels of digoxin with concurrent therapy.
- When coadministered with simvastatin, monitor for and report unexplained muscle weakness or pain.
Patient & Family Education