Pharmacokinetics and Pharmacodynamics of Gabapentin: Clinical and Forensic Features of Abuse

Abstract

Gabapentin (1-(aminomethyl)cyclohexaneacetic acid) is an antiepileptic drug commonly prescribed for epilepsy, restless legs syndrome, and neuropathic pain (such as post-herpetic neuralgia and diabetic neuropathy). It is also used off-label for the treatment of migraines, mood and anxiety disorders, and substance abuse. In fact, gabapentin is a widely prescribed drug due to its pharmacokinetic properties and, subsequently, good safety profile. Nevertheless, recent reports of gabapentin misuse have been documented, particularly in the context of polypharmacy abuse. Indeed, in many countries, there has been a discussion regarding the reclassification of gabapentin as a controlled substance. Therefore, to further comprehend these clinical and forensic phenomena, a literature review was conducted on gabapentin's pharmacokinetic and pharmacodynamic profiles.