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Buy Gabapentin (Neurontin) Cas 60142-96-3. Gabapentin, sold under the brand name Neurontin among others, is an anticonvulsant medication used to treat neuropathic pain and partial seizures of epilepsy.^[11]^[7] Gabapentin is a central nervous system (CNS) depressant and derivative of the inhibitory neurotransmitter GABA.^[7] It is used for the treatment of neuropathic pain caused by diabetic neuropathy, postherpetic neuralgia, and central pain.^[12] It is moderately effective: about 30–40% of those given gabapentin for diabetic neuropathy or postherpetic neuralgia have a meaningful benefit.^[13]

Gabapentin binds to α₂δ subunits to modulate calcium channel function and neurotransmitter release, weakly affects glutamate signaling pathways, and does not act on GABA receptors.^[14]^[15]^[16] Sleepiness and dizziness are the most common side effects. Serious side effects include extreme sedation, respiratory depression and allergic reactions.^[7] In December 2008, the US Food and Drug Administration issued a class-wide warning for gabapentinoids for an increased risk of suicide.^[7] Approximately two years after this pronouncement, a pharmacoepidemiologic study was conducted that showed there was no outstanding difference in suicide attempt rates between pre- and post-gabapentin prescription groups.^[17]

Gabapentin was first approved for use in the United Kingdom in 1993.^[18] It has been available as a generic medication in the United States since 2004.^[19] It is the first of several other drugs that are similar in structure and mechanism, called gabapentinoids. In 2023, it was the ninth most commonly prescribed medication in the United States, with more than 45 million prescriptions.^[20]^[21] During the 1990s, Parke-Davis, a subsidiary of Pfizer, used several illegal techniques to encourage physicians in the United States to prescribe gabapentin for unapproved uses.^[22] They have paid out millions of dollars to settle lawsuits regarding these activities.^[23]

Medical uses

In the US, gabapentin is indicated for the treatment of postherpetic neuralgia and as an adjunctive therapy in the treatment of partial-onset seizures without secondary generalization in people with epilepsy.^[7]

Gabapentin is recommended for use in focal seizures and neuropathic pain.^[7]^[11] Gabapentin is prescribed off-label in the US and the UK,^[24]^[25] for example, for the treatment of non-neuropathic pain,^[24] anxiety disorders, sleep problems and bipolar disorder.^[26] In recent years, gabapentin has seen increased use, particularly in the elderly.^[27] There is concern regarding gabapentin’s off-label use due to the lack of strong scientific evidence for its efficacy in multiple conditions, its proven side effects and its potential for misuse and physical/psychological dependency.^[28]^[29]^[3] Some harms, including nervous system harms, have been underreported in published trials of gabapentin, potentially resulting in the underestimation of harms in guidelines for the use of gabapentin.^[30]

Seizures

Gabapentin is approved for the treatment of focal seizures;^[31] however, it is not effective for generalized epilepsy.^[32]

Neuropathic pain

Gabapentin is recommended as a first-line treatment for chronic neuropathic pain by various medical authorities.^[11]^[12]^[33]^[34] This is a general recommendation applicable to all neuropathic pain syndromes except for trigeminal neuralgia, where it may be used as a second- or third-line agent.^[12]^[34]

Regarding the specific diagnoses, a systematic review has found evidence for gabapentin to provide pain relief for some people with postherpetic neuralgia and diabetic neuropathy.^[13] Gabapentin is approved for the former indication in the US.^[7] In addition to these two neuropathies, European Federation of Neurological Societies guideline notes gabapentin effectiveness for central pain.^[12] A combination of gabapentin with an opioid or nortriptyline may work better than either drug alone.^[12]^[34]

Evidence finds little or no benefit and significant risk in those with chronic low back pain or sciatica.^[35]^[36] Gabapentin is not effective in HIV-associated sensory neuropathy^[37] and neuropathic pain due to cancer.^[38]

Anxiety

There is a small amount of research on the use of gabapentin for the treatment of anxiety disorders.^[39]^[40]

Gabapentin is effective for the long-term treatment of social anxiety disorder and in reducing preoperative anxiety.^[28]^[29]

In a controlled trial of breast cancer survivors with anxiety,^[40] and a trial for social phobia,^[39] gabapentin significantly reduced anxiety levels.

For panic disorder, gabapentin has produced mixed results.^[40]^[39]^[29]

Sleep

Gabapentin is effective in treating sleep disorders such as insomnia and restless legs syndrome that are the result of an underlying illness, but comes with some risk of discontinuation and withdrawal symptoms after prolonged use at higher doses.^[41]

Gabapentin enhances slow-wave sleep in people with primary insomnia. It also improves sleep quality by elevating sleep efficiency and decreasing spontaneous arousal.^[42]

Drug dependence

Gabapentin is moderately effective in reducing the symptoms of alcohol withdrawal and associated craving.^[43]^[44]^[45] The evidence in favor of gabapentin is weak in the treatment of alcoholism: it does not contribute to the achievement of abstinence, and the data on the relapse of heavy drinking and percent of days abstinent do not robustly favor gabapentin; it only decreases the percent days of heavy drinking.^[46]

Gabapentin is ineffective in cocaine dependence and methamphetamine use,^[47] and it does not increase the rate of smoking cessation.^[48] While some studies indicate that gabapentin does not significantly reduce the symptoms of opiate withdrawal, there is increasing evidence that gabapentinoids are effective in controlling some of the symptoms during opiate detoxification. A clinical study in Iran, where heroin dependence is a significant social and public health problem, showed gabapentin produced positive results during an inpatient therapy program, particularly by reducing opioid-induced hyperalgesia and drug craving.^[49]^[47] There is insufficient evidence for its use in cannabis dependence.^[50]^{[needs update]}

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Sleepiness and dizziness are the most common side effects. Serious side effects include an increased risk of suicide, respiratory depression, and allergic reactions. Lower doses are recommended in those with kidney disease. Gabapentin acts by decreasing activity of a subset of calcium channels.

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Gabapentin was first approved for use in 1993. It has been available as a generic medication in the United States since 2004. In 2019, it was the tenth most commonly prescribed medication in the United States, with more than 47 million prescriptions. During the 1990s, Parke-Davis, a subsidiary of Pfizer, used a number of illegal techniques to encourage physicians in the United States to prescribe gabapentin for unapproved uses.

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They have paid out millions of dollars to settle lawsuits regarding these activities.

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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.^[51]^[52]^[53]

Gabapentin decreases the frequency of hot flashes in both menopausal women and people with breast cancer. However, antidepressants have similar efficacy, and treatment with estrogen more effectively prevents hot flashes.^[54]

Gabapentin reduces spasticity in multiple sclerosis and is prescribed as one of the first-line options.^[55] It is an established treatment of restless legs syndrome.^[56] Gabapentin alleviates itching in kidney failure (uremic pruritus)^[57]^[58] and itching of other causes.^[59] It may be an option in essential or orthostatic tremor.^[60]^[61]^[62]

Gabapentin does not appear to provide benefit for bipolar disorder,^[29]^[44]^[63] complex regional pain syndrome,^[64] post-surgical pain,^[65] or tinnitus,^[66] or prevent episodic migraine in adults.^[67]

Gabapentin is prescribed off-label as an anxiolytic or anti-anxiety medication, although not as effective as pregabalin in this regard, especially for generalized anxiety disorder