title: Plasma pharmacokinetics and urinary excretion of thalidomide after oral dosing in healthy male volunteers.
abstract: The plasma pharmacokinetics and urinary excretion of thalidomide have been evaluated in eight healthy male volunteers receiving a single oral dose of 200 mg. Concentrations of thalidomide were determined by a new HPLC assay. Plasma concentration vs. time data were well fit by a one-compartment model. The mean (+/- SD) peak concentration, 1.15 +/- 0.2 microgram/ml, was achieved at 4.39 +/- 1.27 hr. Absorption and elimination half-lives were 1.70 +/- 1.05 hr and 8.70 +/- 4.11 hr, respectively, with a lag time of 0.41 +/- 0.17 hr observed in six subjects. The apparent volume of distribution and total body clearance rate, based on assumed complete bioavailability, were 120.69 +/- 45.36 liters and 10.41 +/- 2.04 liters/hr. The urinary excretion of thalidomide accounted for only 0.6 +/- 0.22% of the total dose administered over 24 hr, and the renal clearance rate was 0.08 +/- 0.03 liter/hr. This suggests that the major route of elimination of thalidomide is nonrenal.
authors.affiliation: Oncology Center, Johns Hopkins University, Baltimore, MD 21205.
authors.forename: T L
authors.initials: TL
authors.lastname: Chen
authors.forename: G B
authors.initials: GB
authors.lastname: Vogelsang
authors.forename: B G
authors.initials: BG
authors.lastname: Petty
authors.forename: R B
authors.initials: RB
authors.lastname: Brundrett
authors.forename: D A
authors.initials: DA
authors.lastname: Noe
authors.forename: G W
authors.initials: GW
authors.lastname: Santos
authors.forename: O M
authors.initials: OM
authors.lastname: Colvin
mesh_terms: D000284:Administration, Oral; D000328:Adult; D002851:Chromatography, High Pressure Liquid; D006207:Half-Life; D006801:Humans; D008297:Male; D013792:Thalidomide / Q000008:administration & dosage / Q000493:pharmacokinetics* / Q000652:urine
chemical_list: D013792:Thalidomide