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Gabapentin (Neurontin) is a pharmaceutical drug, specifically a GABA analog. It was originally developed to treat epilepsy, and currently is also used to relieve neuropathic pain.  NEURONTIN is a prescription medicine used to treat: Pain from damaged nerves (postherpetic pain) that follows healing of shingles (a painful rash that comes after a herpes zoster infection) in adults. Partial seizures when taken together with other medicines in adults and children 3 years of age and older with seizures.

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Gabapentin Action Mechanisms

The chemical structure of gabapentin (Neurontin) is derived by addition of a cyclohexyl group to the backbone of gamma-aminobutyric acid (GABA). Gabapentin prevents seizures in a wide variety of models in animals, including generalized tonic-clonic and partial seizures.

Gabapentin has no activity at GABAA or GABAB receptors of GABA uptake carriers of brain. Gabapentin interacts with a high-affinity binding site in brain membranes, which has recently been identified as an auxiliary subunit of voltage-sensitive Ca2+ channels. However, the functional correlate of gabapentin binding is unclear and remains under study.

Gabapentin crosses several lipid membrane barriers via system L amino acid transporters. In vitro, gabapentin modulates the action of the GABA synthetic enzyme, glutamic acid decarboxylase (GAD) and the glutamate synthesizing enzyme, branched-chain amino acid transaminase. Results with human and rat brain NMR spectroscopy indicate that gabapentin increases GABA synthesis. Gabapentin increases non-synaptic GABA responses from neuronal tissues in vitro.

In vitro, gabapentin reduces the release of several mono-amine neurotransmitters. Gabapentin prevents pain responses in several animal models of hyperalgesia and prevents neuronal death in vitro and in vivo with models of the neurodegenerative disease amyotrophic lateral sclerosis (ALS).

Gabapentin is also active in models that detect anxiolytic activity. Although gabapentin may have several different pharmacological actions, it appears that modulation of GABA synthesis and glutamate synthesis may be important.

What is Gabapentin ?

Gabapentin (Neurontin) is an anticonvulsant and analgesic drug. It was originally developed to treat epilepsy, and is currently also used to relieve neuropathic pain. It is recommended as a first line agent for the treatment of neuropathic pain arising from diabetic neuropathy, post-herpetic neuralgia, and central neuropathic pain.

Gabapentin capsules, tablets, and oral solution are used to help control certain types of seizures in people who have epilepsy. Gabapentin capsules, tablets, and oral solution are also used to relieve the pain of postherpetic neuralgia (PHN; the burning, stabbing pain or aches that may last for months or years after an attack of shingles).

Gabapentin extended-release tablets (Horizant) are used to treat restless legs syndrome (RLS; a condition that causes discomfort in the legs and a strong urge to move the legs, especially at night and when sitting or lying down).

Gabapentin is in a class of medications called anticonvulsants. Gabapentin treats seizures by decreasing abnormal excitement in the brain. Gabapentin relieves the pain of PHN by changing the way the body senses pain. It is not known exactly how gabapentin works to treat restless legs syndrome.

Gabapentin is used to help control partial seizures (convulsions) in the treatment of epilepsy. This medicine cannot cure epilepsy and will only work to control seizures for as long as you continue to take it.

Gabapentin is also used in adults to manage a condition called postherpetic neuralgia, which is pain that occurs after shingles.

Gabapentin works in the brain to prevent seizures and relieve pain for certain conditions in the nervous system. It is not used for routine pain caused by minor injuries or arthritis. Gabapentin is an anticonvulsant.

This medicine is available only with your doctor’s prescription.

On December 30, 1993, Gabapentin got final approval, which meant that it could be marketed in the United States. It is only marketed as an anticonvulsant. However, it has also been used for restless leg syndrome, pain issues, hot flashes, tremors, and a wide variety of psychiatric disorders.

 

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Gabapentin capsules, tablets, and oral solution are used to help control certain types of seizures in people who have epilepsy. Gabapentin capsules, tablets, and oral solution are also used to relieve the pain of postherpetic neuralgia (PHN; the burning, stabbing pain or aches that may last for months or years after an attack of shingles).

Gabapentin extended-release tablets (Horizant) are used to treat restless legs syndrome (RLS; a condition that causes discomfort in the legs and a strong urge to move the legs, especially at night and when sitting or lying down). Gabapentin is in a class of medications called anticonvulsants. Gabapentin treats seizures by decreasing abnormal excitement in the brain. Gabapentin relieves the pain of PHN by changing the way the body senses pain. It is not known exactly how gabapentin works to treat restless legs syndrome.

Gabapentin is also commonly prescribed for many off-label uses, such as treatment of restless leg syndrome, anxiety disorders, insomnia, and bipolar disorder. There are, however, concerns regarding the quality of the trials conducted and evidence for some such uses, especially in the case of its use as a mood stabilizer in bipolar disorder.

Gabapentin interacts with voltage-sensitive calcium channels in cortical neurons.  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 alpha-2 adrenergic receptors.  Gabapentin has also been shown to bind and activate the adenosine A1 receptor.

Before taking Gabapentin

You should not use this medication if you are allergic to gabapentin.

To make sure this medicine is safe for you, tell your doctor if you have:

  • kidney disease;
  • liver disease;
  • heart disease; or
  • (for patients with RLS) if you are a day sleeper or work a night shift.

Some people have thoughts about suicide while taking this medicine. Your doctor will need to check your progress at regular visits while you are using gabapentin. Your family or other caregivers should also be alert to changes in your mood or symptoms.

FDA pregnancy category C. It is not known whether gabapentin will harm an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant while using this medication.

Gabapentin, or Neurontin, is an anticonvulsant with analgesic properties that is available in capsule, tablet and oral solution. It has a wide range of intended uses, including controlling specific types of seizures in patients with epilepsy, treating postherpetic neuralgia (PHN) and restless leg syndrome.

In the treatment of seizures, gabapentin decreases abnormal activity in the brain, specifically excitement. When treating PHN, which is the lingering pain after suffering shingles, gabapentin changes the way the body senses pain, lowering the burning, aching and stabbing pain that can last up to years after a diagnosis. However, it is unknown exactly how it works in the treatment of restless legs syndrome.

Gabapentin can also be used to as a pain reliever for those suffering from diabetic neuropathy, which is numbness or pain due to diabetes and subsequent nerve damage. For menopausal women or women being treated for breast cancer, gabapentin can relieve hot flashes. It has also proven as an effective treatment for those suffering from alcohol dependency. In a recent study, patients who received high doses of gabapentin were four times more likely to stop drinking altogether, and twice as likely to refrain from heavy drinking. It is the only medication to have shown to help the alcohol dependent sleep better and improve their moods.

How should Gabapentin be used?

Gabapentin comes as a capsule, a tablet, an extended-release (long-acting) tablet, and an oral solution (liquid) to take by mouth. Gabapentin capsules, tablets, and oral solution are usually taken with a full glass of water (8 ounces [240 milliliters]), with or without food, three times a day.

These medications should be taken at evenly spaced times throughout the day and night; no more than 12 hours should pass between doses. The extended-release tablet (Horizant) is taken with food once daily at about 5 PM. Follow the directions on your prescription label carefully, and ask your doctor or pharmacist to explain any part you do not understand. Take gabapentin exactly as directed. Do not take more or less of it or take it more often than prescribed by your doctor.

Gabapentin extended-release tablets cannot be substituted for another type of gabapentin product. Be sure that you receive only the type of gabapentin that was prescribed by your doctor. Ask your pharmacist if you have any questions about the type of gabapentin you were given.

Swallow the extended-release tablets whole; do not cut, chew, or crush them.

If your doctor tells you to take one-half of a regular tablet as part of your dose, carefully split the tablet along the score mark. Use the other half-tablet as part of your next dose. Properly throw away any half-tablets that you have not used within several days of breaking them.

If you are taking gabapentin to control seizures or PHN, your doctor will probably start you on a low dose of gabapentin and gradually increase your dose as needed to treat your condition. If you are taking gabapentin to treat PHN, tell your doctor if your symptoms do not improve during your treatment.

Gabapentin may help to control your condition but will not cure it. Continue to take gabapentin even if you feel well. Do not stop taking gabapentin without talking to your doctor, even if you experience side effects such as unusual changes in behavior or mood. If you suddenly stop taking gabapentin tablets, capsules, or oral solution, you may experience withdrawal symptoms such as anxiety, difficulty falling asleep or staying asleep, nausea, pain, and sweating. If you are taking gabapentin to treat seizures and you suddenly stop taking the medication, you may experience seizures more often. Your doctor may decrease your dose gradually over at least a week.

Your doctor or pharmacist will give you the manufacturer’s patient information sheet (Medication Guide) when you begin treatment with gabapentin and each time you refill your prescription. Read the information carefully and ask your doctor or pharmacist if you have any questions. You can also visit the Food and Drug Administration (FDA) website (http://www.fda.gov/Drugs) or the manufacturer’s website to obtain the Medication Guide.

What side effects can Gabapentin cause?

The most common adverse reactions with NEURONTIN in combination with other antiepileptic drugs in patients >12 years of age, not seen at an equivalent frequency among placebo-treated patients, were somnolence, dizziness, ataxia, fatigue, and nystagmus.

The most common adverse reactions with NEURONTIN in combination with other antiepileptic drugs in pediatric patients 3 to 12 years of age, not seen at an equal frequency among placebo-treated patients, were viral infection, fever, nausea and/or vomiting, somnolence, and hostility .

Gabapentin may cause side effects. Tell your doctor if any of these symptoms are severe or do not go away:

  • drowsiness
  • tiredness or weakness
  • dizziness
  • headache
  • uncontrollable shaking of a part of your body
  • double or blurred vision
  • unsteadiness
  • anxiety
  • memory problems
  • strange or unusual thoughts
  • unwanted eye movements
  • nausea
  • vomiting
  • heartburn
  • diarrhea
  • dry mouth
  • constipation
  • increased appetite
  • weight gain
  • swelling of the hands, feet, ankles, or lower legs
  • back or joint pain
  • fever
  • runny nose, sneezing, cough, sore throat, or flu-like symptoms
  • ear pain
  • red, itchy eyes (sometimes with swelling or discharge)

Some side effects may be serious. If you experience any of the following symptoms, call your doctor immediately:

  • rash
  • itching
  • swelling of the face, throat, tongue, lips, or eyes
  • hoarseness
  • difficulty swallowing or breathing
  • seizures

Gabapentin may cause other side effects. Call your doctor if you have any unusual problems while taking this medication.

In case of overdose, call your local poison control center at 1-800-222-1222. If the victim has collapsed or is not breathing, call local emergency services at 911.

Symptoms of overdose may include the following:

  • double vision
  • slurred speech
  • drowsiness
  • diarrhea

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There are only a few interaction issues that are known. Antacids have been known to decrease absorption of the drug, as well as lower the blood level by 20%. Gabapentin could also increase the level of concentration of some oral contraceptives by up to 13%. However, these two interaction possibilities are not clinically significant in any way.

By usahealthstore.com, gabapentin can be used for preventing migraine, treat nerve pain, restless legs syndrome, and Fibromyalgia.  Actually Gabapentin relieves the pain of PHN by changing the way the body senses pain. You can buy Gabapentin to treat attention deficit hyperactivity disorder (ADHD), alcohol withdrawal, chronic neuropathic pain, cocaine addiction, diabetic peripheral neuropathy,generalized anxiety disorder (GAD), menopause, migraine prevention, panic disorder, post-traumatic stress disorder (PTSD), social phobia, trigeminal neuralgia.

Gabapentin can also be used for more than 30 off-label health conditions such as: Benign Essential Tremor,,Bipolar Disorder,,Burning Mouth , yndrome, Cluster-Tic Syndrome, Cough, Diabetic Peripheral Neuropathy, Epilepsy, Erythromelalgia, Fibromyalgia, Hiccups, Hot Flashes,  Hyperhidrosis,  Insomnia,  Lhermitte’s Sign,  Migraine, Nausea/Vomiting, Chemotherapy Induced, Neuropathic Pain, Occipital Neuralgia, Pain, Periodic Limb Movement Disorder, Peripheral Neuropathy, Postherpetic Neuralgia,  Postmenopausal Symptoms,Pruritus,,Pudendal Neuralgia,,Reflex Sympathetic Dystrophy Syndrome,  Restless Legs Syndrome, Small Fiber Neuropathy, Spondylolisthesis, Syringomyelia, Transverse Myelitis, Trigeminal Neuralgia, Vulvodynia.  For more information, please check drug.com Gabapentin page.