Clinical Pharmacokinetics of Lofexidine, the α 2-Adrenergic Receptor Agonist, in Opiate Addicts Plasma Using a Highly Sensitive Liquid Chromatography Tandem Mass Spectrometric Analysis

Elmer Yu University of Pennsylvania and Philadelphia Veterans Affairs Medical Center, Philadelphia, Pennsylvania, USA

Karen Miotto University of California at Los Angeles and Long Beach Veterans Affairs Medical Center, Los Angeles, California, USA

Evaristo Akerele Columbia University College of Physicians and Surgeons and New York State Psychiatric Institute, New York, New York, USA

Charles P. O'Brien University of Pennsylvania and Philadelphia Veterans Affairs Medical Center, Philadelphia, Pennsylvania, USA

Walter Ling University of California at Los Angeles and Long Beach Veterans Affairs Medical Center, Los Angeles, California, USA

Herbert Kleber Columbia University College of Physicians and Surgeons and New York State Psychiatric Institute, New York, New York, USA

Marian W. Fischman Columbia University College of Physicians and Surgeons and New York State Psychiatric Institute, New York, New York, USA

Ahmed Elkashef Division of Pharmacotherapeutics and Medical Consequences of Drug Abuse (PMC), National Institute on Drug Abuse (NIDA), National Institute of Health (NIH), Bethesda, Maryland, USA

Barbara H. Herman Division of Pharmacotherapeutics and Medical Consequences of Drug Abuse (PMC), National Institute on Drug Abuse (NIDA), National Institute of Health (NIH), Bethesda, Maryland, USA

Abeer M. Al-Ghananeem Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, Lexington, Kentucky, USA

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Abstract

Objectives: The objective of this investigation was to characterize the pharmacokinetic profile of lofexidine. Lofexidine is an orally bioavailable α 2-adrenergic receptor agonist analogue of clonidine that acts centrally to suppress opiate withdrawal symptoms. Methods: During the detoxification period of a phase 3 placebo-controlled, randomized, double-blind trial, six subjects were entered in this preliminary pharmacokinetic study. Results: Pharmacokinetic analysis of plasma samples collected during study day 7 indicated that C_max was 3242 ± 917 ng/L. The mean trough levels between the study days were not significantly different (p >. 05), suggesting that the subjects were at steady-state. Conclusions: Although preliminary due to the limited number of subjects, these findings are the first to document lofexidine clinical pharmacokinetics in opiate addicts using a highly sensitive liquid chromatography tandem mass spectrometric analysis.

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Clinical Pharmacokinetics of Lofexidine, the α 2-Adrenergic Receptor Agonist, in Opiate Addicts Plasma Using a Highly Sensitive Liquid Chromatography Tandem Mass Spectrometric Analysis

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Clinical Pharmacokinetics of Lofexidine, the α 2-Adrenergic Receptor Agonist, in Opiate Addicts Plasma Using a Highly Sensitive Liquid Chromatography Tandem Mass Spectrometric Analysis

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