Diflucan

[Fluconazole]

Pharmacokinetics in Children

In children, the following pharmacokinetic data {Mean(% cv)} have been reported:
Age Studied Dose (mg/ kg) Clearance (mL/ min/ kg) Half-life (Hours) Cmax ( g/ mL) Vdss (L/ kg)
9 Months-13 years Single-Oral 2 mg/ kg 0.40 (38%) N= 14 25.0 2.9 (22%) N= 16 ___
9 Months-13 years Single-Oral 8 mg/ kg 0.51 (60%) N= 15 19.5 9.8 (20%) N= 15 ___
5-15 years Multiple IV 2 mg/ kg 0.49 (40%) N= 4 17.4 5.5 (25%) N= 5 0.722 (36%) N= 4
5-15 years Multiple IV 4 mg/ kg 0.59 (64%) N= 5 15.2 11.4 (44%) N= 6 0.729 (33%) N= 5
5-15 years Multiple IV 8 mg/ kg 0.66 (31%) N= 7 17.6 14.1 (22%) N= 8 1.069 (37%) N= 7

Clearance corrected for body weight was not affected by age in these studies. Mean body clearance in adults is reported to be 0.23 (17%) mL/ min/ kg.

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In premature newborns (gestational age 26 to 29 weeks), the mean (% cv) clearance within 36 hours of birth was 0.180 (35%, N= 7) mL/ min/ kg, which increased with time to a mean of 0.218 (31%, N= 9) mL/ min/ kg six days later and 0. 333 (56%, N= 4) mL/ min/ kg 12 days later. Similarly, the half-life was 73.6 hours, which decreased with time to a mean of 53.2 hours six days later and 46.6 hours 12 days later.

Drug Interaction Studies Oral contraceptives

Oral contraceptives were administered as a single dose both before and after the oral administration of DIFLUCAN 50 mg once daily for 10 days in 10 healthy women. There was no significant difference in ethinyl estradiol or levonorgestrel AUC after the administration of 50 mg of DIFLUCAN. The mean increase in ethinyl estradiol AUC was 6% (range: –47 to 108%) and levonorgestrel AUC increased 17% (range: –33 to 141%).

In a second study, twenty-five normal females received daily doses of both 200 mg DIFLUCAN tablets or placebo for two, ten-day periods. The treatment cycles were one month apart with all subjects receiving DIFLUCAN during one cycle and placebo during the other. The order of study treatment was random. Single doses of an oral contraceptive tablet containing levonorgestrel and ethinyl estradiol were administered on the final treatment day (day 10) of both cycles. Following administration of 200 mg of DIFLUCAN, the mean percentage increase of AUC for levonorgestrel compared to placebo was 25% (range: -12 to 82%) and the mean percentage increase for ethinyl estradiol compared to placebo was 38% (range: -11 to 101%). Both of these increases were statistically significantly different from placebo.

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