Multiple-dose pharmacokinetics of nilvadipine in healthy volunteers.
Nilvadipine, a new antihypertensive and antianginal drug, was studied in six healthy male volunteers to evaluate its steady-state pharmacokinetics after oral dosing. The subjects were given a single dose of 4 mg, followed by 4 mg every 12 hours for six days after a washout period of more than 3 days. The pharmacokinetics of nilvadipine were well described by a linear model of triexponential equation with zero-order absorption. The steady state was reached by the fourth day of multiple dosing, with a twofold accumulation of trough plasma concentration and no accumulation of peak concentration. The mean plasma concentration at steady state was 1.0 ng/mL. The optical enantiomers of nilvadipine were also determined in the plasma. The plasma concentration of (+)-nilvadipine was about two and a half times higher than that of (-)-nilvadipine, and this ratio was unaffected by multiple dosing.
Terakawa
M
M
Department of Clinical Research, Fujisawa Pharmaceutical Co., Ltd., Osaka, Japan.
Tokuma
Y
Y
Kuwahara
N
N
Shishido
A
A
Noguchi
H
H
D000284:Administration, Oral; D000328:Adult; D006801:Humans; D008297:Male; D009543:Nifedipine / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000097:blood / Q000493:pharmacokinetics; D013237:Stereoisomerism; D013997:Time Factors
C035100:nilvadipine; D009543:Nifedipine