Pharmacokinetics of fluconazole in normal volunteers

S Ripa, L Ferrante, M Prenna - Chemotherapy, 1993 - karger.com
S Ripa, L Ferrante, M Prenna
Chemotherapy, 1993karger.com
The pharmacokinetic profile of fluconazole, after 100 mg iv infusion or oral administration of
a single 50 mg or 150 mg dose, was investigated in 18 healthy volunteers. At a dose of 100
mg iv, the half-life (t½β) was 29.73±8.05 h. The mean residence time in the plasma was
27.56±5.98 h. The post-distributive volume Vp= 52.16±9.83 1, approximating that of total
body water. Renal excretion accounted for 61.64±8.80% of the drug elimination after 48 h,
with renal clearance Clr= 12.91±2.83 ml/min. Plasma clearance (Clp) was 21.03±5.07 …
Abstract
The pharmacokinetic profile of fluconazole, after 100 mg i.v. infusion or oral administration of a single 50 mg or 150 mg dose, was investigated in 18 healthy volunteers. At a dose of 100 mg i.v., the half-life (t½β) was 29.73 ± 8.05h. The mean residence time in the plasma was 27.56 ± 5.98 h. The post-distributive volume Vp = 52.16 ± 9.83 1, approximating that of total body water. Renal excretion accounted for 61.64 ± 8.80% of the drug elimination after 48 h, with renal clearance Clr = 12.91 ± 2.83 ml/min. Plasma clearance (Clp) was 21.03 ± 5.07 ml/min. At oral doses of 50 and 150 mg the distribution and elimination of fluconazole resembled that following i.v. infusion. The peak levels in plasma at 2.5 h were 0.93 ± 0.13 and 2.69 ± 0.43 μg/ml, respectively. The large distribution volume, the long half-life and mean residence times, combined with a rapid absorption after oral administration, suggest that fluconazole will be effective at a wide range of body sites.
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