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Benzodiazepines are a class of anxiolytic drugs known for their rapid efficacy and high therapeutic-to-lethal dose ratio, but with a potential risk of drug dependence. These drugs are lipophilic, allowing for rapid absorption after oral administration, eventually reaching the central nervous system (CNS). Once in the CNS, benzodiazepines bind to the allosteric site of the GABAA receptor. This binding enhances the inhibitory effects of the neurotransmitter GABA. By doing so, they prevent...
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The elimination half-life and drug clearance of drugs following nonlinear kinetics can vary with dosage. The Michaelis-Menten parameters and drug concentration influence these factors. As the dose increases, the elimination half-life tends to lengthen, resulting in a reduction in clearance and a disproportionately larger area under the curve. The total clearance can be derived from the Michaelis-Menten equation for drugs following a one-compartment model.
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High-throughput and Comprehensive Drug Surveillance Using Multisegment Injection-Capillary Electrophoresis-Mass Spectrometry
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Pregabalin serum levels in apprehended drivers.

Pirkko Kriikku1, Lars Wilhelm2, Janne Rintatalo3

  • 1Vita Laboratory, Vita Health Care Services Ltd., Helsinki, Finland; Department of Forensic Medicine, Hjelt Institute, University of Helsinki, Helsinki, Finland.

Forensic Science International
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This study found high serum pregabalin levels in drivers suspected of drug impairment, with nearly half exceeding therapeutic ranges. Many drivers abused pregabalin recreationally alongside other psychoactive substances.

Keywords:
DUIDDrivingDrugs of abusePregabalin

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Area of Science:

  • Pharmacology
  • Forensic Toxicology
  • Drug Abuse Research

Background:

  • Pregabalin, used for epilepsy and neuropathic pain, has known abuse potential.
  • Recent reports highlight illegal pregabalin use, necessitating further investigation.

Purpose of the Study:

  • To assess the extent and nature of pregabalin abuse.
  • To analyze serum pregabalin levels in drivers apprehended for driving under the influence of drugs (DUID) in Finland.

Main Methods:

  • Serum samples from DUID drivers in Finland (2012) were analyzed using LC-MS/MS.
  • Pregabalin levels were compared to therapeutic ranges, considering driver demographics.

Main Results:

  • Pregabalin was detected in 206 samples, with a median serum concentration of 6.2 mg/L.
  • Nearly 50% of cases showed pregabalin levels above the typical therapeutic range.
  • Most drivers (80%) had used pregabalin with a mean of four other drugs, indicating polydrug abuse.

Conclusions:

  • Pregabalin is frequently used at high, likely recreational, doses.
  • The majority of pregabalin-positive drivers are probable drug abusers using it with other psychoactive substances.
  • Pregabalin likely contributes to driving impairment, though the exact extent requires further study.