Nilvadipine in hypertension with renal dysfunction.
The pharmacokinetics and pharmacodynamics of nilvadipine, a new dihydropyridine calcium antagonist, were examined in 16 patients divided into two different population groups. The first group of eight patients had arterial hypertension with limited renal function (creatinine clearance of 15-50 ml/min). The second group of eight patients had arterial hypertension with no concomitant renal dysfunction (creatinine clearance over 80 ml/min). Following a 1-week placebo washout period, all patients were given 8 mg of nilvadipine once daily for 10 days. The diastolic blood pressure (24-h postdose) fell in group I from a mean of 100.5 to 91.5 mm Hg and in group II from a mean of 106.7 to 88.2 mm Hg, which was significant in comparison to the placebo period. In neither group was there a significant change in heart rate, renin and aldosterone plasma levels, serum electrolytes, or sodium and potassium excretion. The pharmacokinetics of the unchanged nilvadipine were not significantly different between group I and group II. Neither group showed unchanged nilvadipine in urine. There was a slight increase in plasma levels of the inactive main metabolites M3 and M7; there was correspondingly less M3 found in the urine of group I patients. Nilvadipine appears to be an effective hypotensive agent at single daily doses of 8 mg. This dosage was well tolerated. The findings of this study did not suggest that lower doses need to be given to patients with limited renal function, at least not those with a creatinine clearance between 15 and 50 ml/min.
D000328:Adult; D000368:Aged; D000450:Aldosterone / Q000097:blood; D000959:Antihypertensive Agents / Q000493:pharmacokinetics* / Q000494:pharmacology; D001794:Blood Pressure / Q000187:drug effects; D003404:Creatinine / Q000652:urine; D005260:Female; D006339:Heart Rate / Q000187:drug effects; D006801:Humans; D006973:Hypertension / Q000378:metabolism*; D007674:Kidney Diseases / Q000378:metabolism*; D007677:Kidney Function Tests; D008297:Male; D008875:Middle Aged; D009543:Nifedipine / Q000031:analogs & derivatives* / Q000493:pharmacokinetics / Q000494:pharmacology; D012083:Renin / Q000097:blood
D000959:Antihypertensive Agents; C035100:nilvadipine; D000450:Aldosterone; D003404:Creatinine; D012083:Renin; D009543:Nifedipine