Gabapentin

Gabapentin is an oral anticonvulsant. Gabapentin was developed as a gamma-aminobutyric acid (GABA) agonist and is an analog of GABA. Gabapentin possesses high lipid solubility, is not metabolized by the liver, has no protein binding, and is devoid of the usual drug interactions (e.g., enzyme induction). Gabapentin is used as adjunct therapy in the treatment of partial seizures with or without secondary generalized tonic-clonic seizures. More recently, gabapentin has been shown to treat painful neuropathies. Investigational uses include monotherapy of refractory partial seizure disorders, treatment of spasticity in multiple sclerosis, and tremor. In addition, gabapentin appears to reduce hot flashes in menopausal women or women with breast cancer.

Gabapentin’s innovator is Pfizer-Global and is known world-wide by the brand names: Gabarone and Neurontin.

The exact mechanism by which gabapentin exerts its anticonvulsant activity is not known, but it does not appear to be related to its development as a GABA analog. Animal studies have shown that gabapentin binds with high affinity in the brain but does not act at GABA receptors, and does not inhibit sustained repetitive firing of sodium action potentials. Gabapentin does appear to interact with cortical neurons at auxillary subunits of voltage-sensitive calcium channels, but the relationship of this action to functional activity is unclear. Gabapentin crosses brain cell lipid membranes via L-system amino acid transporters. In vitro actions include the modulation of GABA synthetic enzyme, glutamate synthesizing enzyme, glutamic acid decarboxylase, and branched-chain amino acid transaminase. In animals, gabapentin increases GABA responses at non-synaptic sites in neuronal tissues, and reduces the release of mono-amine neurotransmitters. In humans, NMR spectroscopy has indicated that gabapentin increases GABA synthesis. In animal models, gabapentin is most effective in inhibiting seizures produced by maximal electroshock. Gabapentin reduces pain responses in several animal models of hyperalgesia, and prevents neuron death in models of amyotrophic lateral sclerosis (ALS). Animal models have also demonstrated anxiolytic activities of gabapentin.

Gabapentin appears in the following formulation and dosage:
Oral - 100 mg/day to 3600 mg/day

General data on Gabapentin Active Pharmaceutical Ingredient

CAS Registry: 60142-96-3
ATC: N03AX12
Molecular Formula: C9H17NO2
Molecular Weight: 171.2
Pharmacopoeias: In US.

USP 30: Gabapentin is a white to off-white, crystalline solid. Gabapentin is freely soluble in water and in alkaline and acidic solutions. A 2% solution in water has a pH of 6.5 to 8.0.

TAPI's Gabapentin Pharmaceutical Ingredient

TAPI's Gabapentin Active Pharmaceutical Ingredient is produced in Assia Chemical Industries Limited - Teva Tech site in Beer Sheva, Israel.

Gabapentin is produced by TAPI by Organic synthesis and considered to be high volume Active Pharmaceutical Ingredient.

2008 Available DMF: U.S. DMF, EU CTD, Turkey DMF and Other DMF.

TAPI provide full service on Gabapentin and other APIs in our portfolio. Our local sales offices provide full information on our product, regulatory compliance and documentation on Gabapentin. Contact us today for further inquiries and samples and kilograms availability information for TAPI's Gabapentin.

Another product, in the group of ANTIEPILEPTIC - Gaba analouges available on TAPI's portfolio is Pregabalin. Contact us today for information on these products.

Legal Note

Product exploitation, including development, sales and offer for sale are performed where permissible by patent law. This presentation is not and should not constitute an offer for sale in territories where it is not permitted by law. In USA Products  that  Currently on Patent are available for R&D Use in Accordance with 35 USC §271 (e) (1).

*TAPI stands for Teva's Active Pharmaceutical Ingredients