What class is gabapentin
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Gabapentin: Classification and Mechanisms
Gabapentin as an Antiepileptic Agent
Gabapentin, marketed under the brand name Neurontin, is primarily classified as an antiepileptic agent. It is used as an adjunctive therapy for the treatment of partial seizures in humans, particularly when standard antiseizure drugs are not effective1 5. Gabapentin works by binding to the α2δ subunit of voltage-dependent calcium channels, which distinguishes it from other antiepileptic drugs1 7.
Gabapentin as an Antihyperalgesic Agent
In addition to its antiepileptic properties, gabapentin is recognized as a novel class of antihyperalgesic agents. It has been shown to effectively inhibit the late phase of nociceptive responses in inflammatory pain models, such as the formalin and carrageenan-induced pain tests in rats1. This antihyperalgesic action is dose-dependent and does not lead to tolerance, unlike traditional opioids like morphine1.
Gabapentin and Pregabalin: Controlled Substances
Due to the rising misuse and associated mortality, gabapentin, along with pregabalin, has been reclassified as a class C controlled substance in the United Kingdom. This reclassification aims to curb the misuse and reduce the number of deaths linked to these drugs2 3 4 6. The reclassification requires a physical prescriber signature for each prescription, highlighting the need for stricter control measures2.
Mechanisms of Action
Gabapentin and pregabalin are structurally and mechanistically distinct from other analgesics. They are not GABAergic, despite being chemically related to the inhibitory neurotransmitter gamma-aminobutyric acid (GABA). Instead, they reduce the stimulated release of neurotransmitters by binding to calcium channel alpha2-delta (CaVα2-δ) proteins7. This binding reduces neuronal excitability and provides analgesic effects, making them effective for chronic pain management7.
Veterinary Use and Performance Enhancement
Gabapentin is also used in veterinary medicine, particularly in performance horses. It is listed as a class 3 performance-enhancing substance by the Association of Racing Commissioners International, indicating its potential to influence race outcomes. Accurate quantification methods have been developed to monitor its use in equine biological fluids5.
Conclusion
Gabapentin is a multifaceted drug classified primarily as an antiepileptic agent but also recognized for its antihyperalgesic properties. Its reclassification as a controlled substance underscores the need for careful monitoring due to its potential for misuse and associated mortality. Understanding its mechanisms of action and applications in both human and veterinary medicine highlights its significance in various therapeutic contexts.
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Most relevant research papers on this topic
Gabapentin (neurontin) and S‐(+)‐3‐isobutylgaba represent a novel class of selective antihyperalgesic agents
Gabapentin and S-(+)-3-isobutylgaba effectively reduce late-phase nociceptive responses in inflammatory pain models, while the R-()-enantiomer shows minimal effect.
Non-RCT
Animal Study
Highly CitedNeed for international classification of gabapentin as a controlled substance
International classification of gabapentin as a controlled substance is needed to address the increased risk of death associated with its misuse.
Rigorous JournalUK government to reclassify pregabalin and gabapentin after rise in deaths
Pregabalin and gabapentin could be reclassified as class C controlled substances after an increase in deaths linked to their use, following safety warnings and concerns about misuse and addiction.
Very Rigorous JournalPregabalin and gabapentin become controlled drugs to cut deaths from misuse
Pregabalin and gabapentin will become controlled drugs in the UK from next April to reduce deaths from their misuse, the government said.
Rigorous JournalGabapentin in horses: validation of an analytical method for gabapentin quantitation.
This study developed a sensitive GC-MS method for accurately quantifying gabapentin in equine biological fluids, enabling its use in pharmacokinetic and forensic studies.
Misuse and Mortality Related to Gabapentin and Pregabalin are Being Under-Estimated: A Two-Year Post-Mortem Population Study.
GBP and PGL are significantly under-reported in fatalities, with their prevalence significantly higher in heroin users compared to non-heroin users.
Observational StudyMechanisms of analgesia by gabapentin and pregabalin – Calcium channel α2-δ [Cavα2-δ] ligands
Gabapentin and pregabalin reduce chronic pain by binding to calcium channel alpha2-delta proteins, not GABAergic, and reducing stimulated transmitter release.
Very Rigorous JournalHighly CitedFormulation and In-Vitro Evaluation of Gabapentin Loaded Transferosomal Gel
The optimized formulation Gf6 of Gabapentin transferosomes shows high entrapment efficiency, drug content, and in-vitro drug release, overcoming convectional drug delivery issues.
Gabapentin misuse, abuse and diversion: a systematic review.
Gabapentin misuse is prevalent globally, with substance abuse populations at a higher risk for misuse/abuse, primarily for recreational purposes and self-medication.
Systematic ReviewRigorous JournalHighly CitedGabapentin for chronic neuropathic pain in adults.
Gabapentin at 1200 mg daily or greater provides moderate to substantial pain relief for adults with chronic neuropathic pain conditions like postherpetic neuralgia and painful diabetic neuropathy.
Systematic ReviewVery Rigorous JournalHighly Cited