Lercanidipine - A review of its use in hypertension

Lercanidipine is a vasoselective dihydropyridine calcium antagonist which c auses systemic vasodilation by blocking the influx of calcium ions through L-type calcium channels in cell membranes. It is a highly lipophilic drug a nd as such has a slower onset and longer duration of action than a number o f other calcium antagonists. Preclinical evidence suggests that lercanidipi ne has antiatherogenic potential and it may also protect against end-organ damage. In well controlled clinical studies, once daily administration of lercanidi pine 10 or 20mg effectively reduced blood pressure (BP) compared with place bo in patients with mild to moderate hypertension without affecting heart r ate. Response rate (percentage of patients with diastole BP less than or eq ual to 90mm Hg or reduced by greater than or equal to 10mm Hg from baseline ) ranged from 50 to 66% with lercanidipine 10 mg/day and up to 86% with ler canidipine 20 mg/day. The drug had a long duration of action: clinical meas urements for diastolic BP yielded a trough/peak ratio of >0.8 for both lerc anidipine dosages in 1 study. Comparative trials, either published in full or as abstracts, found lercanidipine 10mg once daily for greater than or eq ual to4 weeks to be at least as effective as atenolol 50mg once daily, cand esartan cilexetil 16 mg/day, captopril 25mg twice daily, enalapril 20 mg/da y, hydrochlorothiazide 12.5mg once daily, irbesartan 150 mg/day and slow re lease nifedipine 20mg twice daily in patients with mild to moderate hyperte nsion. In addition, lercanidipine 20 mg/day was as effective as amlodipine 10 mg/day. Lercanidipine is effective in the treatment of elderly patients (aged 60 to 85 years) with mild to moderate essential hypertension and in those with i solated systolic hypertension. In addition, monotherapy with lercanidipine 20 or 40 mg/day has shown efficacy in patients with severe hypertension, an d add-on therapy helped control BP in a large proportion of patients with s evere hypertension not responding sufficiently to beta -blockers, diuretics or ACE inhibitors. Unpublished data indicate that the drug reduces blood p ressure in patients with type 2 (non-insulin-dependent) diabetes mellitus, without adversely affecting glucose homeostasis. Lercanidipine was well tolerated in clinical trials, with most treatment-re lated adverse events typical of dihydropyridine calcium antagonists, namely headache, flushing, dizziness and ankle oedema. Conclusions: Lercanidipine is an effective and well tolerated once daily an tihypertensive agent in patients with mild to moderate hypertension. In add ition, the drug may reduce BP when used as monotherapy in patients with sev ere hypertension or when used adjunctively in patients with resistant hyper tension. Importantly, lercanidipine appears to be at least as effective and well tolerated as other commonly used antihypertensive agents. The drug th erefore represents a useful therapeutic option in the management of patient s with hypertension and will be particularly useful in patients not respond ing to, or intolerant of, antihypertensive agents from other drug classes.