Name: | gabapentin |
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PubChem Compound ID: | 3446 |
Molecular formula: | C9H17NO2 |
Molecular weight: | 171.237 g/mol |
Synonyms: |
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 |
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Name (isomeric): | DB00996 |
Drug Type: | small molecule |
Synonyms: |
Gabapentinum [INN-Latin]; Gabapetin; Gabapentin GR; Gabapentino [Spanish]; Gabapentino [INN-Spanish]; Gabapentine [INN-French]
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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. |
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Pharmacology: |
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: |
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Drug interaction: |
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