What is the classification of gabapentin (anticonvulsant)?

Gabapentin Drug Classification

Gabapentin is classified as an anticonvulsant (antiepileptic drug) that is structurally related to the neurotransmitter GABA but does not function as a GABA mimetic. 1

Pharmacological Classification

• Primary drug class: Anticonvulsant/Antiepileptic Drug (AED) 2, 3
• Structural classification: GABA analog (gamma-aminobutyric acid structural analog) 1, 3
• Functional classification: Gabapentinoid 4

Mechanism of Action

• Gabapentin binds with high affinity to the α2δ subunit of voltage-activated calcium channels, though the precise relationship of this binding to therapeutic effects remains unknown 1
• Despite being structurally related to GABA, gabapentin has no effect on GABA binding, uptake, or degradation and does not act as a GABA mimetic 1, 3
• The drug modulates calcium channel activity and neurotransmitter release, which likely accounts for its pharmacological actions 5
• Gabapentin is a substrate for the large neutral amino acid (L-system) transporter, which allows CNS penetration 1, 5

Clinical Classification Context

• Therapeutic use classification: Gabapentin is used as an adjuvant analgesic, particularly for neuropathic pain management 4
• The National Comprehensive Cancer Network and American Geriatrics Society classify gabapentin among the "gabapentinoids" alongside pregabalin when discussing pain management 4
• Both the FDA and clinical guidelines recognize gabapentin primarily as an anticonvulsant that has been repurposed for pain management 1, 2

Important Distinction

• Gabapentin is not metabolized in humans—all pharmacological actions are due to the parent compound 1
• The drug is eliminated unchanged by renal excretion, which distinguishes it from many other anticonvulsants 1, 3