Gabapentin
Originally developed as an anticonvulsant, gabapentin found its widest use in treating nerve pain. It binds the alpha-2-delta subunit of voltage-gated calcium channels, reducing calcium entry at nerve terminals and thereby dampening the release of excitatory signals that carry abnormal or painful impulses. This action underlies its use in epilepsy, postherpetic neuralgia, and a range of other neuropathic pain conditions. A small molecule (C9H17NO2) structurally related to the neurotransmitter GABA, though it does not act directly on GABA receptors, it has a half-life of about 5 to 7 hours and is eliminated unchanged by the kidneys. Its renal clearance shapes dosing in people with reduced kidney function. Gabapentin is an approved medicine spanning seizure control and chronic pain.
This medication was originally developed as an anticonvulsant but is also widely used to treat nerve pain by modulating calcium channels in nerve cells to reduce abnormal electrical activity. It is prescribed for epilepsy, postherpetic neuralgia, and various other neuropathic pain conditions.
Molecular Weight
171.2370 g/mol
LogP
-1.10
TPSA
63.30 Ų
Lipinski RO5
Pass
Therapeutic Areas
Drug Classes
Mechanism of Action
Binds alpha-2-delta subunit of voltage-gated calcium channels.
Pharmacokinetics (PK)
Pharmacodynamics (PD)
Binds alpha-2-delta subunit of voltage-gated calcium channels.
2D Structure
Cite this structure
Embed this structure
SMILES
NCC1(CC(=O)O)CCCCC1
InChI
InChI=1S/C9H17NO2/c10-7-9(6-8(11)12)4-2-1-3-5-9/h1-7,10H2,(H,11,12)
Molecular Formula
C9H17NO2
HBD / HBA
2 / 3
Rotatable Bonds
3
Heavy Atoms
12
Gabapentin and oxycodone together produce enhanced CNS and respiratory depression beyond what either drug causes alone, with risk of fatal overdose.
Gabapentin significantly potentiates the CNS and respiratory depressant effects of morphine, increasing overdose risk.
Gabapentin and valproic acid have a minor pharmacokinetic interaction; valproate may slightly increase gabapentin renal clearance.
Hydrochlorothiazide-induced sodium and fluid loss can increase the risk of dizziness and orthostatic hypotension when combined with gabapentin, which also causes dizziness and impairs balance.
Gabapentin adds to zolpidem's CNS depressant effects, increasing the risk of excessive sedation, falls, and next-morning psychomotor impairment.
Combining gabapentin and pregabalin, two alpha-2-delta ligands with similar mechanisms, produces additive CNS depression and dose-dependent adverse effects including respiratory depression, dizziness, and somnolence.
Alprazolam and gabapentin produce additive CNS depression, increasing the risk of sedation, dizziness, and psychomotor impairment.
No side effects recorded
Side effect data is not yet available for this drug.
Frequently Asked Questions
This medication was originally developed as an anticonvulsant but is also widely used to treat nerve pain by modulating calcium channels in nerve cells to reduce abnormal electrical activity. It is prescribed for epilepsy, postherpetic neuralgia, and various other neuropathic pain conditions.
Binds alpha-2-delta subunit of voltage-gated calcium channels.
Key pharmacokinetic parameters for Gabapentin: Half-life: 5-7 hours.
Yes, Gabapentin is an approved drug. It has reached clinical phase 4. It is classified as a Small molecule.
Related Drugs
Same Drug Class
References & Data Sources
- ChEMBL — European Bioinformatics Institute (EBI). CHEMBL940. Open-access bioactivity database.
- PubChem — National Center for Biotechnology Information (NCBI). CID 3446. Chemical information database.
Data aggregated from publicly available pharmacological databases. Last updated 2026-03-04.
Embed This Widget
Add the script tag and a data attribute to embed this widget.
<script src="https://cdn.jsdelivr.net/npm/drugfyi-embed@1/dist/embed.min.js" defer></script>
<div data-drugfyi="drug" data-slug="gabapentin"></div>Embed via iframe for maximum compatibility.
<iframe src="https://drugfyi.com/iframe/drug/gabapentin/" width="420" height="400" frameborder="0" style="border:0;border-radius:10px;max-width:100%" loading="lazy"></iframe>Paste this URL in WordPress, Medium, or any oEmbed-compatible platform.
https://drugfyi.com/drug/gabapentin/Add a dynamic SVG badge to your README or docs.
[](https://drugfyi.com/drug/gabapentin/)Use the native HTML custom element.
<script src="https://cdn.jsdelivr.net/npm/drugfyi-embed@1/dist/embed.min.js" defer></script>
<drugfyi-drug slug="gabapentin"></drugfyi-drug>