Ranexa may be used with the most common cardiovascular agents

Ranexa is indicated for the treatment of chronic angina. Ranexa may be used with:

  • Beta-blockers
  • Calcium channel blockers
  • Nitrates
  • ACE inhibitors
  • Anti-platelet therapy
  • Angiotensin receptor blockers
  • Lipid-lowering therapy

Ranexa is taken twice daily

  • Initiate Ranexa at 500 mg twice daily and increase to 1000 mg twice daily as needed, based on clinical symptoms.
  • Limit dose of Ranexa to 500 mg twice daily when used with moderate CYP3A inhibitors, such as diltiazem, verapamil, aprepitant, erythromycin, fluconazole, and grapefruit juice or grapefruit-containing products.
  • When used with P-gp inhibitors (eg, cyclosporine), the dose of Ranexa may need to be lowered based on clinical response.
  • Doses of drugs transported by P-gp (eg, digoxin) or metabolized by CYP2D6 (eg, tricyclic antidepressants and antipsychotics) may need to be reduced.
  • Ranexa may be taken with or without meals.
  • The maximum recommended dose of Ranexa is 1000 mg twice daily.
  • Swallow Ranexa tablets whole; do not crush, break, or chew.
  • If a dose of Ranexa is missed, patients should take the prescribed dose at the next scheduled time.

Ranexa does not require dose adjustment in chronic angina patients with heart failure or diabetes

  • In patients with chronic angina, Ranexa pharmacokinetics are not affected by heart failure or diabetes.

Contraindications

  • Do not use with strong CYP3A inhibitors (eg, ketoconazole, itraconazole, clarithromycin, nefazodone, nelfinavir, ritonavir, indinavir, and saquinavir).
  • Do not use with CYP3A inducers (eg, rifampin, rifabutin, rifapentin, phenobarbital, phenytoin, carbamazepine, and St. John's wort).
  • Do not use in patients with significant hepatic impairment.

Hemodynamically neutral: Ranexa works independently of reductions in heart rate or blood pressure

  • The anti-ischemic and antianginal effects of Ranexa do not depend upon reductions in heart rate or blood pressure. In controlled clinical trials Ranexa had minimal changes in mean heart rate (< 2 bpm) and systolic blood pressure (< 3 mm Hg).
    • Ranexa does not affect the rate-pressure product, a measure of myocardial work, at maximal exercise.
  • The mechanism of action of ranolazine's antianginal effects has not been determined.
    • Ranexa at therapeutic levels can inhibit the cardiac late sodium current.
    • The relationship of this inhibition to angina symptoms is uncertain.

Ranexa is not associated with tolerance or rebound after 12 weeks of therapy.

  • Rebound increases in angina, as measured by exercise duration, have not been observed following abrupt discontinuation of Ranexa.

Safety Profile in Special Populations

Clinical trials of Ranexa included patients with chronic angina including elderly patients and chronic angina patients with diabetes, heart failure, and renal impairment.

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