Lacidipine (Caldine®, Lacimen®, Lacipil®, Midotens®, Motens®) is a once-daily, orally-administered, lipophilic dihydropyridine calcium antagonist with an intrinsically slow onset of activity, resulting in a lack of reflex tachycardia. It has a long duration of action and a high degree of vascular selectivity. In addition to calcium channel-modulated vasodilation, lacidipine displays antioxidant activity greater than that of other dihydropyridine calcium antagonists.

In randomised, well-controlled trials, lacidipine 2–6mg orally once daily had antihypertensive efficacy similar to that of other long-acting dihydropyridine calcium antagonists, thiazide diuretics, atenolol (a β-blocker) and enalapril (an ACE inhibitor). Lacidipine was effective in elderly patients (including those with isolated systolic hypertension), African Nigerian patients and patients with concurrent type 2 diabetes mellitus.

During long-term treatment for 4 or 5 years in patients with isolated systolic hypertension or essential hypertension, the incidence of cardiovascular events and mortality with lacidipine was similar to that with chlorthalidone or atenolol.

The European Lacidipine Study on Atherosclerosis (ELSA), in which 2334 patients with hypertension were randomised to 4 years of therapy with lacidipine 4–6 mg/day or the β-blocker atenolol 50–100 mg/day, demonstrated significantly lower atherosclerotic progression and plaque formation with lacidipine compared with atenolol in patients completing the full 4 years of the study. Between-group differences in favour of lacidipine for the primary efficacy variable (mean change in carotid artery intima-media thickness) did not reach statistical significance in the intent-to-treat population.

The tolerability profile of lacidipine (headache, flushing, pedal oedema, dizziness and palpitations) is similar to that of other dihydropyridine calcium antagonists, but with a lower incidence of peripheral oedema. Data from the ELSA study suggest that the incidence of serious adverse events during long-term lacidipine therapy is similar to that with atenolol.

Conclusion: Lacidipine is an effective, well tolerated, once-daily, oral antihypertensive agent that can be used in a wide variety of patients. As with other members of its class, lacidipine has shown potentially beneficial antiatherosclerotic effects, although definitive data with respect to possible superiority over other drug classes are still required. Therefore, lacidipine is an attractive therapy for the long-term management of essential hypertension.

Lacidipine is a once-daily, orally-administered lipophilic 1,4-dihydropyridine calcium antagonist with an intrinsically slow onset of activity and long duration of action. The lipophilic nature of the drug results in the accumulation of lacidipine in membrane lipid bilayers from which it is slowly and continuously released. Lacidipine blocks voltage-dependent L-type calcium channels, producing vasodilation, and thereby reduces total peripheral vascular resistance, resulting in a reduction in blood pressure (BP). In addition, lacidipine has antioxidant activity that is considered to play a role in reducing endothelial dysfunction induced by oxidative stress. The antioxidant activity of lacidipine is greater than that of other dihydropyridine calcium antagonists.

The onset of the antihypertensive effect occurs 0.5–1.0 hours post-dose, and is maintained throughout a 24-hour period during multiple dosing. Lacidipine administration once daily in the morning reduces BP over 24 hours as demonstrated by ambulatory BP monitoring, although …