Clinical pharmacokinetics of pregabalin in healthy volunteers.
Author(s): Bockbrader HN, Radulovic LL, Posvar EL, Strand JC, Alvey CW, Busch JA, Randinitis
EJ, Corrigan BW, Haig GM, Boyd RA, Wesche DL.
Affiliation(s): Pfizer Global Research & Development, 50 Pequot Ave, New London, CT 06320, USA.
Publication date & source: 2010, J Clin Pharmacol. , 50(8):941-50
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.