Single-Dose and Steady-State Pharmacokinetic and Pharmacodynamic Profiles of Nisoldipine Coat-Core Tablets in Healthy Young, Healthy Elderly, and Elderly Hypertensive Volunteers

Abstract

The single-dose and steady-state pharmacokinetic and pharmacodynamic profiles of the nisoldipine coat-core tablet were determined in an open multiple dose nonrandomised study. 20 healthy young male volunteers, 21 healthy elderly volunteers, and 11 elderly hypertensive volunteers completed the study. One nisoldipine coat-core tablet (20mg) was administered as a single daily dose on days 1, 3, 4, 5, 6 and 7. Days 1 and 2 (after a single dose) and days 7 and 8 (after multiple doses) were pharmacokinetic and pharmacodynamic profile days. After both single and multiple doses, the plasma nisoldipine concentrations in the healthy elderly and elderly hypertensive volunteers were higher than in healthy young male volunteers. There was no accumulation of nisoldipine in the young males, but there was accumulation in the elderly. The degree of accumulation was similar for the healthy elderly and the elderly hypertensive volunteers. After multiple dose administration of nisoldipine (5 days), the supine diastolic blood pressure in the healthy young males remained unchanged, but a moderate decrease in the healthy elderly volunteers and a significant decrease in the elderly hypertensive volunteers could be seen. Substantial decreases in supine systolic blood pressure for both the healthy elderly volunteers and the elderly hypertensive volunteers were recorded. A small decrease in supine systolic blood pressure was recorded in the healthy young male volunteers. The results of this study indicate that once-daily administration of nisoldipine 20mg coat-core tablets is both safe and effective in elderly hypertensive volunteers.