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Ranolazine

Ranolazine

Introduction

Coronary heart disease (CHD) remains the major cause of death throughout European and other developed countries. While death rates have been consistently falling, rates in the UK remain relatively high compared to some Western European countries. The commonest clinical presentation of CHD is angina pectoris. Angina incidence rates generally increase with age and are highest in the 65−74 years age group in both men and women. The prevalence of angina is estimated to be 5% in men and 4% in women in the UK, giving a total of nearly 2.1 million (>1.2 million <75 years of age) with the condition.1 It is therefore a common disease, which carries a prognosis similar to patients who have had a myocardial infarction (MI) or who have been revascularised.2 Many patients experience anginal attacks despite revascularisation and pharmacological antianginal treatments. In the Clinical Outcomes Utilization Revascularization and Aggressive Drug Evaluation (COURAGE) trial,3 for example, over 25% of patients experienced angina up to five years post-percutaneous coronary intervention (PCI) with optimal medical treatment (OMT). Such findings suggest that we need better strategies to improve both symptoms and prognosis in patients with chronic stable angina.

DOSAGE & INDICATIONS

For the treatment of chronic angina.

NOTE: The concomitant use of ranolazine and CYP3A inducers or strong CYP3A inhibitors is contraindicated.

NOTE: The effects of ranolazine on angina frequency and exercise tolerance are considerably smaller in women than in men.

Oral dosage

Adults

500 mg PO twice daily. Based on clinical symptoms, the dose may be increased up to the maximum dose of 1,000 mg PO twice daily if needed. The ERICA trial utilized this dosing schedule, escalating to the higher dose after 1 week. Closely monitor clinical response. The concomitant use of ranolazine with other commonly administered cardiovascular medications that are not contraindicated (amlodipine, beta-blockers, nitrates, anti-hypertensive agents) is well-tolerated. The first placebo controlled trial (MARISA), which showed beneficial antianginal effects of ranolazine monotherapy, utilized a broader dosage range (500 to 1,500 mg PO twice daily).. However, doses higher than 1,000 mg PO twice daily are not currently recommended due to the risk of QT prolongation and potential for proarrhythmic effects. The subsequent ERICA trial showed statistically significant reductions in angina frequency and nitroglycerin use in patients treated with ranolazine 500 to 1,000 mg twice daily as add-on therapy for chronic angina patients refractory to amlodipine 10 mg once daily. The efficacy of ranolazine is primarily based on the CARISA trial which showed a significant improvement in exercise duration and angina symptoms with added ranolazine (vs. placebo) in patients already taking antianginal therapy. The CARISA trial randomized patients to receive placebo or fixed doses of 750 or 1,000 mg PO twice daily as add-on therapy to traditional antianginal agents. The patients were allowed to receive 1 prior antianginal therapy (i.e., atenolol, diltiazem, or amlodipine) concurrently to assess safety and efficacy.

Adult patients taking diltiazem, verapamil, aprepitant, erythromycin, or fluconazole

Limit the dose to 500 mg PO twice daily. The dose modification may apply to other drugs that moderately inhibit CYP3A4.

Geriatric

See adult dosage. Initiate therapy at the lower end of the adult dosage range.

For the treatment of acute coronary syndromes in patients with acute myocardial infarction, NSTEMI†.

Intravenous† and Oral dosage

NOTE: The IV formulation is not available in the US.

Adults

Dosage not established. Within 48 hours of ischemic symptoms, patients were randomized to ranolazine 200 mg IV bolus over 1 hour then 80 mg/hour IV infusion for 12 to 96 hours followed by 1,000 mg PO twice daily or placebo. There was no significant difference in the primary efficacy endpoint of composite cardiovascular death, myocardial infarction, or recurrent ischemia.

For the treatment of acute coronary syndromes in patients with unstable angina†.

Intravenous† and Oral dosage

NOTE: The IV formulation is not available in the US.

Adults

Dosage not established. Within 48 hours of ischemic symptoms, patients were randomized to ranolazine 200 mg IV bolus over 1 hour then 80 mg/hour IV infusion for 12 to 96 hours followed by 1,000 mg PO twice daily or placebo. There was no significant difference in the primary efficacy endpoint of composite cardiovascular death, myocardial infarction, or recurrent ischemia.

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