View information on Ranexa's safety profile below, including information on contraindications, warnings and precautions, adverse reactions, dosage and administration, and drug interactions.
Contraindications
- Ranexa is contraindicated in paitients:
- Taking strong inhibitors of CYP3A (eg, ketoconazole, itraconazole, clarithromycin, nefazodone, nelfinavir, ritonavir, indinavir, and saqinavir).
- Taking inducres of CYP3A (eg, rifampin, rifabutin, rifapentin, phenobarbital, phenytoin, carbamazepine, and St. John's wort).
- With liver cirrhosis.
Warnings and precautions
- Ranexa blocks IKr and prolongs the QTc interval in a dose-related manner.
- Clinical experience did not show an increased risk of proarrhythmia or sudden death.
- There is little experience with high doses (> 1000 mg twice daily) or exposure, other QT-prolonging drugs, with potassium channel variants resulting in a long QT interval, in patients with family history of (or congenital) long QT syndrome, or in patients with known acquired QT interval prolongation.
Adverse Reactions
The most common adverse reactions (> 4% and more common that with placebo) during treatment with Ranexa were dizziness, headache, constipation, and nausea.
Dosage and Administration
- Begin treatment with 500 mg twice daily and increase to the maximum recommended dose of 1000 mg twice daily, based on clinical symptoms. Swallow tablets whole; do no crush,
break or chew.
- Limit the dose of Ranexa to 500 mg twice daily in patients on moderate CYP3A inhibitors(eg, diltiazem, verapamil, erythromycin, fluconazole, and grapefruit juice or grapefruit-containing products).
Drug interactions
- Inducers and strong inhibitors of CYP3A: Do not use Ranexa (see Contraindications).
- Moderate CYP3A inhibitors: Limit Ranexa to 500 mg twice daily (see Dosage and Administration).
- P-gp inhibitors(eg, cyclosprine): Ranexa exposure increased; titrate Ranexa based on clinical response.
- CYP3A substrates: Limit simvastatin to 20 mg when used with Ranexa. Doses of other sensitive CYP3A substrates (eg, lovastatin) and CYP3A substrate with narrow therapeutic range (eg, cyclosporine, tacrolimus, sirolimus) may need to be reduced with Ranexa.
- Drugs transported by P-gp (eg, digoxin) or metabolized by CYP2D6 (eg, tricyclic antidepressants and antipsychotics): Doses of these drugs may need to be reduced.
