What's all the "GABA" 'bout?

Author: Courtney Kominek

Gabapentin and pregabalin are nonopioid analgesics used for various pain conditions and are collectively and commonly referred to as gabapentinoids. While structurally related to gamma-aminobutyric acid (gaba), gabapentin and pregabalin do not alter the uptake or breakdown of gaba, convert to gaba, or bind to gabaa or gabaB receptors.1-3 The proposed mechanism of both gabapentin and pregabalin is through binding at the ?2-? subunit of the voltage-gated calcium channel, which reduces the calcium-dependent release of pro-nociceptive neurotransmitters (such as glutamate, norepinephrine, and substance P).1,4 In recent years, there has been a growing prevalence of misuse and abuse associated with gabapentinoids, possibly related to the changes in chronic pain management focusing on nonopioid pharmacotherapy and push to reduce opioid doses for chronic nonmalignant pain. This article reviews the misuse and abuse of gabapentin and pregabalin, as presented at PAINWeek 2017.


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