Clinical pharmacokinetics of pregabalin in healthy volunteers.

Autor: Bockbrader HN; Pfizer Global Research & Development, 50 Pequot Ave, New London, CT 06320, USA. Howard.Bockbrader@pfizer.com, Radulovic LL, Posvar EL, Strand JC, Alvey CW, Busch JA, Randinitis EJ, Corrigan BW, Haig GM, Boyd RA, Wesche DL
Jazyk: angličtina
Zdroj: Journal of clinical pharmacology [J Clin Pharmacol] 2010 Aug; Vol. 50 (8), pp. 941-50. Date of Electronic Publication: 2010 Feb 10.
DOI: 10.1177/0091270009352087
Abstrakt: Pregabalin has shown clinical efficacy for treatment of neuropathic pain syndromes, partial seizures, and anxiety disorders. Five studies in healthy volunteers are performed to investigate single- and multiple-dose pharmacokinetics of pregabalin. Pregabalin is rapidly absorbed following oral administration, with peak plasma concentrations occurring between 0.7 and 1.3 hours. Pregabalin oral bioavailability is approximately 90% and is independent of dose and frequency of administration. Food reduces the rate of pregabalin absorption, resulting in lower and delayed maximum plasma concentrations, yet the extent of drug absorption is unaffected, suggesting that pregabalin may be administered without regard to meals. Pregabalin elimination half-life is approximately 6 hours and steady state is achieved within 1 to 2 days of repeated administration. Corrected for oral bioavailability, pregabalin plasma clearance is essentially equivalent to renal clearance, indicating that pregabalin undergoes negligible nonrenal elimination. Pregabalin demonstrates desirable, predictable pharmacokinetic properties that suggest ease of use. Because pregabalin is eliminated renally, renal function affects its pharmacokinetics.
Databáze: MEDLINE