Lercanidipine is a vasoselective
dihydropyridine calcium antagonist which causes systemic vasodilation by blocking the influx of
calcium ions through
L-type calcium channels in cell membranes. It is a highly lipophilic
drug and as such has a slower onset and longer duration of action than a number of other
calcium antagonists. Preclinical evidence suggests that
lercanidipine has antiatherogenic potential and it may also protect against end-organ damage. In well controlled clinical studies, once daily administration of
lercanidipine 10 or 20mg effectively reduced blood pressure (BP) compared with placebo in patients with mild to moderate
hypertension without affecting heart rate. Response rate (percentage of patients with diastolic BP < or =90mm Hg or reduced by > or =10mm Hg from baseline) ranged from 50 to 66% with
lercanidipine 10 mg/day and up to 86% with
lercanidipine 20 mg/day. The
drug had a long duration of action: clinical measurements for diastolic BP yielded a trough/peak ratio of >0.8 for both
lercanidipine dosages in 1 study. Comparative trials, either published in full or as abstracts, found
lercanidipine 10mg once daily for > or =4 weeks to be at least as effective as
atenolol 50mg once daily,
candesartan cilexetil 16 mg/day,
captopril 25mg twice daily,
enalapril 20 mg/day,
hydrochlorothiazide 12.5mg once daily,
irbesartan 150 mg/day and slow release
nifedipine 20mg twice daily in patients with mild to moderate
hypertension. 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
isolated systolic hypertension. In addition, monotherapy with
lercanidipine 20 or 40 mg/day has shown efficacy in patients with severe
hypertension, and add-on
therapy helped control BP in a large proportion of patients with severe
hypertension not responding sufficiently to beta-blockers,
diuretics or
ACE inhibitors. Unpublished data indicate that the
drug reduces blood pressure 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-related adverse events typical of
dihydropyridine calcium antagonists, namely
headache,
flushing,
dizziness and ankle oedema.
CONCLUSIONS: