Linear pharmacokinetics of penciclovir following administration of single oral doses of famciclovir 125, 250, 500 and 750 mg to healthy volunteers.

Autor: Pue MA; SmithKline Beecham Pharmaceuticals, Welwyn, Herts, UK., Pratt SK, Fairless AJ, Fowles S, Laroche J, Georgiou P, Prince W
Jazyk: angličtina
Zdroj: The Journal of antimicrobial chemotherapy [J Antimicrob Chemother] 1994 Jan; Vol. 33 (1), pp. 119-27.
DOI: 10.1093/jac/33.1.119
Abstrakt: Twenty healthy male volunteers received single oral doses of famciclovir (125-750 mg), in a randomized, single-blind, crossover study. Plasma and urine concentrations of penciclovir and its 6-deoxy precursor, BRL 42359, were determined and penciclovir plasma concentration-time data submitted to model-independent pharmacokinetic analysis. Peak plasma concentrations of penciclovir were obtained at median times of 0.5-0.75 h after dosing. The areas under the concentration versus time curves (AUC) and the peak penciclovir concentration (Cmax) increased linearly with dose of famciclovir. Time to Cmax, elimination half-life, urinary recovery and renal clearance of penciclovir did not change with increasing dose. Famciclovir was excreted via the kidneys as penciclovir (60%) and BRL 42359 (5%), respectively. Famciclovir was well tolerated by all subjects with a low incidence of adverse effects. In conclusion, penciclovir thus displays linear pharmacokinetics in the anticipated therapeutic dose range of famciclovir.
Databáze: MEDLINE