Product Information
Registration Status: ActiveNEURONTIN CAPSULE 300mg is approved to be sold in Singapore with effective from 1995-08-25. It is marketed by PFIZER PTE LTD, with the registration number of SIN08303P.
This product contains Gabapentin 300mg in the form of CAPSULE. It is approved for ORAL use.
This product is manufactured by Pfizer Manufacturing Deutschland GmbH in PUERTO RICO, andPFIZER PHARMACEUTICALS LLC in GERMANY.
It is a Prescription Only Medicine that can only be obtained from a doctor or a dentist, or a pharmacist with a prescription from a Singapore-registered doctor or dentist.
Description
Gabapentin (brand name Neurontin) is a medication originally developed for the treatment of epilepsy. Presently, gabapentin is widely used to relieve pain, especially neuropathic pain. Gabapentin is well tolerated in most patients, has a relatively mild side-effect profile, and passes through the body unmetabolized.
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.
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 the reduction of the axon excitability measured as an amplitude change of the presynaptic fibre volley (FV) in the CA1 area of the hippocampus. This is mediated through its binding to presynaptic NMDA receptors. Other studies have shown that the antihyperalgesic and antiallodynic effects of gabapentin are mediated by the descending noradrenergic system, resulting in the activation of spinal alpha2-adrenergic receptors. Gabapentin has also been shown to bind and activate the adenosine A1 receptor.
Pharmacokinetics
- 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).
- Distribution
- * 58±6 L
- Metabolism
- All pharmacological actions following gabapentin administration are due to the activity of the parent compound; gabapentin is not appreciably metabolized in humans.
- Elimination
Clearance
* 190 mL/min
Toxicity
Symptoms of overdose include ataxia, labored breathing, ptosis, sedation, hypoactivity, and excitation.
Active Ingredient/Synonyms
1-(Aminomethyl)cyclohexaneacetic acid | Gabapentin GR | Gabapentina | Gabapentine | Gabapentino | Gabapentinum | Gabapetin | Gabapentin |
Source of information: Drugbank (External Link). Last updated on: 3rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.