Pfizer Global Research & Development, 50 Pequot Ave, New London, CT 06320, USA.
J Clin Pharmacol. 2010 Aug;50(8):941-50. doi: 10.1177/0091270009352087. Epub 2010 Feb 10.
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.
普瑞巴林在治疗神经性疼痛综合征、部分癫痫发作和焦虑症方面显示出临床疗效。在健康志愿者中进行了五项研究，以调查普瑞巴林的单剂量和多剂量药代动力学。普瑞巴林口服后吸收迅速，血浆峰浓度在 0.7 至 1.3 小时之间出现。普瑞巴林的口服生物利用度约为 90%，且与剂量和给药频率无关。食物可降低普瑞巴林的吸收速度，导致较低和延迟的最大血浆浓度，但药物吸收的程度不受影响，这表明普瑞巴林可以不受进餐影响而给药。普瑞巴林的消除半衰期约为 6 小时，重复给药 1 至 2 天后达到稳态。经口服生物利用度校正后，普瑞巴林的血浆清除率与肾清除率基本相当，表明普瑞巴林几乎没有非肾清除。普瑞巴林表现出理想的、可预测的药代动力学特性，表明其易于使用。由于普瑞巴林经肾脏消除，因此肾功能会影响其药代动力学。
