Pharmacokinetics of the antiviral agent beta-D-2',3'-didehydro-2',3'-dideoxy-5-fluorocytidine in rhesus monkeys.

Autor: Ma L; Department of Pediatrics, Emory University, USA., Hurwitz SJ, Shi J, Mcatee JJ, Liotta DC, McClure HM, Schinazi RF
Jazyk: angličtina
Zdroj: Antimicrobial agents and chemotherapy [Antimicrob Agents Chemother] 1999 Feb; Vol. 43 (2), pp. 381-4.
DOI: 10.1128/AAC.43.2.381
Abstrakt: The values of the pharmacokinetic parameters of the nucleoside antiretroviral agent beta-D-2',3'-didehydro-2',3'-dideoxy-5-fluorocytidine (D-D4FC) in rhesus monkeys were determined with a two-compartment model after the administration of a single dose. The average values for the terminal half-life, renal clearance, and total systemic clearance for the intravenous administration route were 3.6 h and 0.31 and 0.43 liter.kg-1.h-1, respectively. The oral bioavailability of D-D4FC averaged 41%. For the intravenous administration route, 76% of the compound was recovered intact in the urine within 8 h, indicating that D-D4FC was eliminated mainly by renal excretion. D-D4FC was detected in the cerebrospinal fluid (CSF) at similar concentrations after administration by both the intravenous and oral routes. D-D4FC levels in plasma and CSF were higher than the median effective concentration for human immunodeficiency virus type 1 in vitro.
Databáze: MEDLINE