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QuickView for gabapentin (compound)

Name: gabapentin
PubChem Compound ID: 3446
Molecular formula: C9H17NO2
Molecular weight: 171.237 g/mol
CAS-60142-96-3; Gabapentin; Prestwick1_000861; Gabapentinum [INN-Latin]; MLS000069358; Aclonium; D00332; Cyclohexaneacetic acid, 1-(aminomethyl)-; Go 3450; 60142-96-3.
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Name: gabapentin
Name (isomeric): DB00996
Drug Type: small molecule
Gabapentinum [INN-Latin]; Gabapetin; Gabapentin GR; Gabapentino [Spanish]; Gabapentino [INN-Spanish]; Gabapentine [INN-French]
Brand: Novo-Gabapentin, Aclonium, Neurontin
Category: Anti-anxiety Agents, Calcium Channel Blockers, Antiparkinson Agents, Analgesics, Antimanic Agents, Anticonvulsants, Excitatory Amino Acid Antagonists
CAS number: 60142-96-3
Indication: For the management of postherpetic neuralgia in adults and as adjunctive therapy in the treatment of partial seizures with and without secondary generalization in patients over 12 years of age with epilepsy.
Gabapentin, an analog of GABA, is used as an anticonvulsant to treat partial seizures, amyotrophic lateral sclerosis (ALS), and painful neuropathies. Potential uses include monotherapy of refractory partial seizure disorders, and treatment of spasticity in multiple sclerosis, tremor. mood disorders, and attenuation of disruptive behaviors in dement...
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Mechanism of Action:
Gabapentin interacts with cortical neurons at auxillary subunits of voltage-sensitive calcium channels. Gabapentin increases the synaptic concentration of GABA, enhances GABA responses at non-synaptic sites in neuronal tissues, and reduces the release of mono-amine neurotransmitters. One of the mechanisms implicated in this effect of gabapentin is ...
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Absorption: Rapid. Absorbed in part by the L-amino acid transport system, which is a carrier-mediated, saturable transport system; as the dose increases, bioavailability decreases. Bioavailability ranges from approximately 60% for a 900 mg dose per day to approximately 27% for a 4800 milligram dose per day. Food has a slight effect on the rate and extent of absorption of gabapentin (14% increase in AUC).
Protein binding: Less than 3% of gabapentin circulates bound to plasma protein.
Biotransformation: All pharmacological actions following gabapentin administration are due to the activity of the parent compound; gabapentin is not appreciably metabolized in humans.
Route of elimination: Gabapentin is eliminated from the systemic circulation by renal excretion as unchanged drug. Gabapentin is not appreciably metabolized in humans.
Half Life: 5-7 hours
Clearance: 190 mL/min
Toxicity: Symptoms of overdose include ataxia, labored breathing, ptosis, sedation, hypoactivity, and excitation.
Affected organisms: Humans and other mammals
Food interaction:
Avoid alcohol.
Take without regard to meals.
Drug interaction:
PhenytoinGabapentin may increase the therapeutic and adverse effects of phenytoin.
MephenytoinIncreases the effect of hydantoin
FosphenytoinGabapentin may increase the effect of fosphenytoin.
TriprolidineThe CNS depressants, Triprolidine and Gabapentin, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.
EthotoinIncreases the effect of hydantoin