21 Facts About Gabapentin

Gabapentin, sold under the brand name Neurontin among others, is an anticonvulsant medication primarily used to treat partial seizures and neuropathic pain.

Gabapentin is recommended for use in focal seizures and neuropathic pain.

Gabapentin is widely prescribed off-label in the US and UK, for example, for the treatment of non-neuropathic pain, anxiety disorders and bipolar disorder.

Gabapentin is approved for the treatment of focal seizures; however, it is not effective for generalized epilepsy.

Gabapentin is recommended as a first-line treatment for chronic neuropathic pain by various medical authorities.

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Gabapentin is not effective in HIV-associated sensory neuropathy and neuropathic pain due to cancer.

Gabapentin is effective in treating sleep disorders such as insomnia and restless legs syndrome.

Gabapentin is moderately effective in reducing the symptoms of alcohol withdrawal and associated craving.

Gabapentin is ineffective in cocaine dependence and methamphetamine use, and it does not increase the rate of smoking cessation.

Gabapentin is recommended as a first-line treatment of the acquired pendular nystagmus, torsional nystagmus, and infantile nystagmus; however, it does not work in periodic alternating nystagmus.

Gabapentin reduces spasticity in multiple sclerosis and is prescribed as one of the first-line options.

Gabapentin should be used carefully and at lower doses in people with kidney problems due to possible accumulation and toxicity.

Gabapentin label contains a warning of an increased risk of suicidal thoughts and behaviors.

Gabapentin is a ligand of the a2d calcium channel subunit.

Gabapentin is not a direct channel blocker: it exerts its actions by disrupting the regulatory function of a2d and its interactions with other proteins.

Gabapentin prevents delivery of the calcium channels to the cell membrane, reduces the activation of the channels by the a2d subunit, decreases signaling leading to neurotransmitters release, and disrupts interactions of a2d with NMDA receptors, neurexins, and thrombospondins.

Gabapentin is a potent activator of voltage-gated potassium channels KCNQ3 and KCNQ5, even at low nanomolar concentrations.

Gabapentin is absorbed from the intestines by an active transport process mediated via an amino acid transporter, presumably, LAT2.

Gabapentin was designed by researchers at Parke-Davis to be an analogue of the neurotransmitter GABA that could more easily cross the blood–brain barrier and was first described in 1975 by Satzinger and Hartenstein.

Gabapentin was scheduled V drug in other states such as West Virginia, Tennessee, Alabama.

Gabapentin when taken in excess can induce euphoria, a sense of calm, a marijuana-like high, improved sociability, and reduced alcohol or cocaine cravings.