Gabapentin
Prescription gabapentinoid; binds the α2δ-1 calcium channel subunit, used off-label for anxiety.
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Pharmacology
Contents
WHAT IS GABAPENTIN?
Detailed overview
Gabapentin (Neurontin) is a gabapentinoid originally developed as an anticonvulsant and now widely used for neuropathic pain, and off-label for anxiety and sleep. Despite its name and structural resemblance to GABA, it does not bind GABA receptors: instead it binds the α2δ-1 auxiliary subunit of presynaptic voltage-gated calcium channels, reducing their trafficking and dampening the release of excitatory neurotransmitters such as glutamate and substance P. Placebo-controlled trials show benefit in social anxiety disorder and in more severely ill panic-disorder patients, and it is often used for preoperative anxiety, though evidence for generalized anxiety is thinner. It is a prescription drug with real dependence and misuse potential, and it can cause dangerous respiratory depression when combined with opioids or other CNS depressants.
Mechanism
α2δ-1 calcium channel binder
Half-life
5-7 hours (renally cleared)
Legal status
Prescription (Rx), off-label for anxiety
Receptor profile
- α2δ-1 calcium channel subunitStrong
- Presynaptic voltage-gated calcium channelsStrong
- Excitatory neurotransmitter release (glutamate, substance P)Moderate
Safety
Side effects, stop signs, contraindications
Side effects · 6
- Drowsiness, sedation and fatigue, especially early in treatment
- Dizziness and coordination problems (ataxia), fall risk in the elderly
- Peripheral edema (limb swelling) and weight gain
- Withdrawal on abrupt cessation: anxiety, insomnia, sweating
- Life-threatening respiratory depression when combined with opioids or other CNS depressants
- Genuine misuse and dependence potential, especially with a history of substance use disorder
Contraindications · 5
- Renal impairment: the drug is cleared unchanged by the kidneys, dose adjustment required
- Concurrent opioids or CNS depressants: increased respiratory depression (FDA warning)
- History of substance use disorder: caution due to misuse risk
- Avoid abrupt discontinuation: gradual taper required
- Pregnancy and breastfeeding: only if benefit outweighs risk
Related Nootropics
Same therapeutic category
Studies
Related research and clinical findings
Treatment of social phobia with gabapentin: a placebo-controlled study
Pande AC, Davidson JR, Jefferson JW, et al.
Placebo-controlled study of gabapentin treatment of panic disorder
Pande AC, Pollack MH, Crockatt J, et al.
Gabapentin treatment for alcohol dependence: a randomized clinical trial
Mason BJ, Quello S, Goodell V, et al.
The Effect of Gabapentin on Postoperative Pain, Morphine Sparing Effect and Preoperative Anxiety in Patients Going for Sleeve Gastrectomy
Khan MU, Bamehriz FY, Aqil M, et al.
Antiepileptic drugs in the treatment of anxiety disorders: role in therapy
Van Ameringen M, Mancini C, Pipe B, et al.
FAQ
FAQ
Prescription gabapentinoid; binds the α2δ-1 calcium channel subunit, used off-label for anxiety.
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Structure & chemistry
The information here is strictly for educational and scientific purposes. It does not replace medical advice or clinical consultation, and it does not encourage illegal substance or pharmaceutical use. Data is sourced. When in doubt, consult your doctor.