Influence of Renal Function on the Pharmacokinetics and Cardiovascular Effects of Nisoldipine After Single and Multiple Dosing

Abstract

The pharmacokinetics and cardiovascular effects of the calcium entry blocker nisoldipine (10 mg twice daily) were studied in 6 patients with renal failure (creatinine clearance 23 +/- 9 ml/min) and 6 healthy control subjects after a single dose and 1 week of oral administration. No significant differences in elimination half-life, area under the concentration/time curve, peak plasma drug concentration and time to reach that peak were observed between renal patients and control subjects, and between single-dose and short term administration. The decrease in systolic blood pressure and increase in heart rate were similar in both groups, but the decrease in diastolic blood pressure was more pronounced in the patients. This can be explained by increased haemodynamic sensitivity for nisoldipine. Adverse effects were mainly restricted to the first day of administration.

Pharmacokinetics of Newer Drugs in Patients with Renal Impairment (Part II)

“…Thus, the pharmacokinetics of these new calcium antagonists in renal failure did not differ from those obtained in subjects with normal renal function, as already reported for nifedipine (Kleinbloesem et al 1985;Martre et al 1985), nicardipine (Clair et al 1985;Lee et al 1986), felodipine (Edgar et al 1989), isradipine (Chandler et al 1988;Schran et al 1988), nisoldipine (Boelaert et al 1988Van Harten et al 1989), amlodipine (Doyle et al 1989) and nitrendipine (Ankermann et al 1989;Aronoff & Sloan 1985;Bortel et al 1989).…”