Gabapentin EU

Gabapentin: A Widely Studied Agent for Neuropathic Pain, Epilepsy, and Beyond

🔎 What is Gabapentin?

Gabapentin is a structural analog of GABA (gamma-aminobutyric acid), primarily prescribed as an anticonvulsant and analgesic. Despite its structural similarity to GABA, it does not act on GABA receptors. Instead, it targets the α2δ subunit of voltage-gated calcium channels, modulating neuronal excitability and reducing the release of excitatory neurotransmitters such as glutamate.

Developed in the 1990s, gabapentin has since become a cornerstone of treatment for neuropathic pain, partial seizures, and is widely used off-label for anxiety disorders, insomnia, and fibromyalgia.

⚙️ Mechanism of Action

Gabapentin binds to the α2δ-1 and α2δ-2 auxiliary subunits of presynaptic voltage-gated calcium channels. By inhibiting calcium influx, it reduces neuronal excitability and neurotransmitter release, particularly in pain pathways and seizure-prone circuits.

• Not GABAergic: It doesn’t directly affect GABA levels or receptors.

• No activity at benzodiazepine, opioid, or glutamate receptors.

• Indirect inhibition of excitatory neurotransmission.

💊 Common Uses

✅ Approved Indications

• Adjunctive treatment for partial (focal) seizures

• Postherpetic neuralgia

🧪 Off-Label and Research Uses

• Generalized anxiety disorder

• Fibromyalgia

• Restless legs syndrome

• Alcohol withdrawal

• Chronic migraine

• Bipolar depression

Gabapentin’s flexibility comes from its wide CNS distribution and favorable safety profile.

📦 Dosage Guidelines