03/02/2026
Medication Monday: Gabapentin
Brand Names:
Neurontin. Gralise. Horizant.
Mechanism
Gabapentin has a similar structure to GABA, but it does not influence the synthesis of GABA nor does it bind to GABA receptors. Instead, Gabapentin freely passes the blood-brain barrier and works by binding to the α2δ-1 and especially the α2δ-2 subunits of voltage-gated calcium channels in the brain. Binding to these sites inhibits the release of excitatory neurotransmitters in the presynaptic area that participate in epileptogenesis. This mechanism also normalizes neurotransmitter release, including excitatory glutamate, aiding in the management of restless legs syndrome and other excitatory conditions.
Indications
FDA-Approved Uses:
- Post-herpetic neuralgia
- Adjunctive therapy for managing partial seizures
- Moderate-to-severe restless legs syndrome
Common Off-Label Uses:
- Fibromyalgia
- Bipolar disorder
- Anxiety disorders
- Resistant depressants
- Mood disorders
- Irritable bowel syndrome
- Alcohol withdrawal
- Post-operative analgesia
- Migraine prophylaxis
- Interstitial cystitis
- Painful diabetic neuropathy
- Social phobia
- Generalized tonic-clonic seizures
- Pruritus
- Insomnia
- Post-traumatic stress disorder
- Refractory chronic couch
- Post-menopausal vasomotor symptoms
- Essential tremors
Contraindications
- Hypersensitivity
Use With Caution:
- When opioids are given concurrently as this can lead to an increased risk of respiratory depression
- With pediatric patients
Routes
- Oral
Source
https://www.ncbi.nlm.nih.gov/books/NBK493228/
