ARX-LERCANIDIPINE

What it is

ARX-LERCANIDIPINE is available as 10 mg and 20 mg film coated tablets containing lercanidipine hydrochloride as the active ingredient. Lercanidipine is a calcium antagonist of the dihydropyridine group that selectively inhibits the transmembrane influx of calcium into cardiac and vascular smooth muscle, with a greater effect on vascular smooth muscle than on cardiac smooth muscle.

Approved indications

— Treatment of hypertension.

Dosing overview

The recommended dose is 10 mg once daily, taken at least 15 minutes before a meal. The dose may be increased to 20 mg once daily depending on individual response. Dose titration should be gradual, as it may take about 2 weeks for the maximal antihypertensive effect to be apparent. Doses above 20 mg are not recommended. Some individuals not adequately controlled on a single antihypertensive agent may benefit from the addition of lercanidipine at the same doses used in monotherapy to the existing regimen with a beta-blocker, a diuretic or an ACE-inhibitor.

Key safety warnings

Some short-acting dihydropyridines may be associated with increased cardiovascular risk in patients with ischaemic heart disease. Although lercanidipine is long-acting, caution should be required in such patients. Lercanidipine has been associated with the development of cloudy peritoneal effluent in patients on peritoneal dialysis, due to an increased triglyceride concentration in the peritoneal effluent. The turbidity tends to resolve soon after withdrawal of lercanidipine. This association is important to recognise as cloudy peritoneal effluent can be mistaken for infective peritonitis with consequential unnecessary hospitalisation and empiric antibiotic administration. Inducers of CYP3A4 like anticonvulsants (for example phenytoin, carbamazepine) and rifampicin may reduce lercanidipine plasma levels and therefore the efficacy of lercanidipine may be less than expected.

Contraindications

ARX-LERCANIDIPINE is contraindicated in hypersensitivity to any dihydropyridine or any ingredient; left ventricular outflow tract obstruction; untreated congestive cardiac failure; unstable angina pectoris or recent (within 1 month) myocardial infarction; severe hepatic impairment; severe renal impairment (GFR less than 30 mL/min), including patients undergoing dialysis; and coadministration with strong inhibitors of CYP3A4, ciclosporin, or grapefruit or grapefruit juice.

Regulatory history

ARX-LERCANIDIPINE 10 mg and 20 mg tablet blister packs were first listed on the Australian Register of Therapeutic Goods on 14 July 2011.