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Neurontin (Gabapentin)
Gabapentin binds with high-affinity to α2δ subunit of voltage-activated calcium channels; precise mechanism unknown.
Gabapentin is an antiepileptic and analgesic agent indicated for postherpetic neuralgia and adjunctive seizure management in adults and pediatric patients 3 years and older. It binds to α2δ subunits of voltage-activated calcium channels with high affinity, though the precise mechanism of therapeutic action remains unknown. Significant risk of respiratory depression and death exists with concurrent opioid use, requiring careful monitoring and potential dose adjustment. The drug is renally eliminated unchanged with a 5-7 hour half-life and shows non-dose-proportional bioavailability, necessitating individualized dosing particularly in elderly and renal-impaired patients.
At a glance
| Generic name | Gabapentin |
|---|---|
| Sponsor | Pfizer Inc. |
| Drug class | Antiepileptic/Analgesic |
| Target | α2δ subunit of voltage-activated calcium channels |
| Modality | Small molecule |
| Therapeutic area | Oncology |
| Phase | FDA-approved |
Mechanism of action
Gabapentin is structurally related to the neurotransmitter gamma-aminobutyric acid (GABA) but has no effect on GABA binding, uptake, or degradation. In vitro studies have shown that gabapentin binds with high-affinity to the α2δ subunit of voltage-activated calcium channels; however, the relationship of this binding to the therapeutic effects of gabapentin is unknown. The precise mechanisms by which gabapentin produces its analgesic and antiepileptic actions remain unknown.
Approved indications
- Postherpetic neuralgia
- Partial seizures
- Seizures associated with amyotrophic lateral sclerosis (ALS)
- Neuropathic pain associated with spinal cord injury
- Phantom limb pain
- Hot flashes associated with breast cancer
- Chronic low back pain
- Pain associated with fibromyalgia
Common side effects
- Somnolence
- Dizziness
- Ataxia
- Fatigue
- Nystagmus
- Tremor
- Dyspepsia
- Dry mouth or throat
- Constipation
- Dysarthria
- Dental abnormalities
- Increased weight
Drug interactions
- Morphine
- Hydrocodone
- Oxycodone
- Buprenorphine
- Maalox (aluminum hydroxide, magnesium hydroxide)
- Other Antiepileptic Drugs
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- Neurontin CI brief — competitive landscape report
- Neurontin updates RSS · CI watch RSS
- Pfizer Inc. portfolio CI