Gabapentin
From Free net encyclopedia
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Image:Gabapentin.png | |
| 1-(aminomethyl)-cyclohexaneacetic acid | |
| CAS number 60142-96-3 | ATC code N03AX12 |
| Chemical formula | C9H17NO2 |
| Molecular weight | 171.238 |
| Bioavailability | Highly variable |
| Metabolism | ? |
| Elimination half-life | 6hrs |
| Excretion | Kidneys |
| Pregnancy category | Not recommended, however a worldwide registry exists for pregnant epileptic women with seizure disorder severe enough to justify the drug risk for the infant being less than the risk to the infant if the mother has uncontrolled seizures during her pregnancy. A great deal of information regarding the safety of Anti Epilepsy Drugs during pregnancy will soon be available. |
| Legal status | PoM (UK) |
| Routes of administration | Oral tablets & capsules |
Gabapentin (brand name: Neurontin®) is an anticonvulsant medication indicated in the treatment of epilepsy and neuropathic pain. Gabapentin is known for having a relatively mild side-effect profile, and passes through the body unmetabolized.
Gabapentin is similar in structure to the neurotransmitter GABA but is not believed to act on the same brain receptors. Its exact mechanism of action is unknown, but its therapeutic action on neuropathic pain is thought to involve voltage-gated calcium ion channels.
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Clinical uses
Gabapentin has also been used in the treatment of bipolar disorder. However, its off-label use for this purpose is increasingly controversial. Some claim gabapentin acts as a mood stabilizer and has the advantage of having fewer side-effects than more conventional bipolar drugs such as lithium and valproic acid. Some small, non-controlled studies in the 1990s, most sponsored by gabapentin's manufacturer, suggested that gabapentin treatment for bipolar disorder may be promising. However, more recently, several larger, controlled, and double-blind studies have found that gabapentin was no more effective than (and in one study, slightly less effective than) placebo, and the manufacturer has even halted its own studies regarding gabapentin and bipolar disorder. Despite this scientific evidence against the efficacy of gabapentin in the treatment of bipolar disorder, many psychiatrists continue to prescribe it for this purpose.
Gabapentin has also been used off label in the treatment of anxiety disorders such as social anxiety disorder and obsessive-compulsive disorder, in treatment-resistant depression, and for insomnia. Gabapentin may be effective in reducing pain and spasticity in multiple sclerosis.
In addition to its use in mood disorders, gabapentin was approved by the FDA for treating postherpetic neuralgia (neuropathic pain following shingles).
Marketing of gabapentin
Gabapentin is best known under the brand name Neurontin manufactured by Pfizer . In October 2004, FDA approved a generic equivalent to Neurontin made by Israeli firm Teva. Neurontin is one of Pfizer’s best selling drugs, and was one of the 50 most prescribed drugs in the United States in 2003. However, in recent years Pfizer has come under heavy criticism for its marketing of Neurontin, facing allegations that behind the scenes Pfizer marketed the drug for at least a dozen supposed uses for which the drug had not been FDA approved. By some estimates, so-called off-label prescriptions account for roughly 90% of Neurontin sales. While off-label prescriptions are common for a number of drugs and are perfectly legal (if not always appropriate), marketing for off-label uses of a drug is strictly illegal. In 2004, Pfizer agreed to pay a $430 million settlement for the illegal marketing of Neurontin for off-label purposes, and further legal action is pending.
Pfizer has developed a successor to gabapentin, called pregabalin (being marketed as Lyrica®). Structurally related to gabapentin, Pregabalin is effective for neuropathy pain associated with diabetes and shingles, and for the treatment of epilepsy and seizures.
Side effects
Gabapentin's main side effect is drowsiness. In most cases, however, the drowsiness subsides after a few days, but the therapeutic effects persist.