Activity of Lercanidipine Administered in Single and Repeated Doses Once Daily as Monitored Over 24 Hours in Patients with Mild to Moderate Essential Hypertension

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Abstract
Two ambulatory blood pressure monitoring (ABPM) studies were performed to define the antihypertensive activity and the tolerability of lercanidipine. a new longacting dihydropyridine calcium antagonist, in patients with mild to moderate essential hypertension. Two different pharmaceutical preparations, a regular tablet and a Sherer capsule, were employed in studies 1 and 2, respectively. The Sherer capsule (a soft gelatine capsule that contains the active ingredient dissloved) gives a similar amount but a faster rate of absorption of the drug as compared with the tablet (Tmax 1 h vs. 1.5 h). In the first study, three parallel groups of eight patients each were treated with a single daily dose of 5-, 10-, or 20-mg lercanidipine tablets for 4 weeks after a 3-week placebo run-in period. ABPM was carried out with a Spacelab 90207 device at the end of the placebo period and at the end of the 4-week treatment period. Compared to basal BP values, lercanidipine produced a highly significant reduction in both systolic and diastolic BP in the 10- and 20-mg but not in the 5-mg q.d. groups. At doses of 10 and 20 mg/day. BP values were equally well controlled over 24 h. No significant changes were observed in HR. ECG. and laboratory parameters. In the second study. 20 patients were enrolled in a cross-over design and were treated with single doses of 10 and 20 mg lercanidipine Sherer capsules. Each active treatment day was preceded and followed by 3 and 2 weeks of placebo, respectively. All treatments were administered at 8 a.m. ABPM was carried out during the placebo period and during the active treatment day. The results showed that a single 20-mg dose of lercanidipine significantly decreased BP for 24 h, whereas a single 10-mg dose reduced BP only during the day. With either dose, the peak fall in BP occurred between the second and the third hour and was accompanied by an insignificant increase in heart rate. However, the tachycardic response faded out within 6-7 h with both the 10- and the 20-mg dose. Analyzed together, data from the two studies indicate that lercanidipine is an effective, long-acting, and well-tolerated antihypertensive drug devoid of the potential inconveniences of older calcium antagonists in terms of reflex cardiostimulation and short duration of action. The 10-mg dose is likely to provide effective and sustained blood pressure control in the majority of patients with mild to moderate essential hypertension.