Population pharmacokinetic/pharmacodynamic analysis of nociceptive pain models following an oral pregabalin dose administration to healthy subjects

Michiel J van Esdonk, Ian Lindeman, Pieter Okkerse, Marieke L de Kam, Geert J Groeneveld, Jasper Stevens

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    A battery of pain models can be used in clinical trials to investigate the efficacy and to establish the concentration-effect relationship of novel analgesics. This study quantified the pharmacokinetics (PK) of pregabalin after a single oral dose of 300 mg and the pharmacodynamics (PD) on the pain tolerance threshold (PTT) of the cold pressor, electrical stimulation and the pressure pain model and on the pain detection threshold of a contact heat pain model. The PK were best described using a 1-compartment model with lag time, linear absorption and linear elimination. The PTT of the cold pressor showed a negative linear decrease over time without pregabalin. A linear drug effect was identified on the PTT of the cold pressor test and an on/off effect for the electrical stimulation PTT. No PK/PD relationship could be identified on the pressure pain and heat pain test. This article is protected by copyright. All rights reserved.

    Original languageEnglish
    Pages (from-to)573-580
    Number of pages8
    JournalCPT: Pharmacometrics & Systems Pharmacology
    Issue number9
    Early online date24-Jul-2018
    Publication statusPublished - Sep-2018



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