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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. There are, however, concerns regarding the quality of the trials conducted for a number of conditions

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.

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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.

We have added Gabapentin as the substitutes of tramadol, please you can try to buy Gabapentin.  Gabapentin is said better better Analgesic than Tramadol because gabapentin has no addictive problems. But Gabapentin is not used for children under age 6.   Gabapentin is an anti-epileptic medication, also called an anticonvulsant. It affects chemicals and nerves in the body that are involved in the cause of seizures and some types of pain. Gabapentin is used in adults to treat nerve pain caused by herpes virus or shingles (herpes zoster). The Horizant brand Gabapentin is also used to treat restless legs syndrome (RLS). The Neurontin brand is also used to treat seizures in adults and children who are at least 6 years old.

Neurontin is FDA-approved for partial seizure (adjunct) in children age 3 to 12 and in adults. It is also FDA-approved for postherpetic neuralgia in adults. Neurontin is used primarily to treat epilepsy. More specifically it treats elementary partial seizures (brief, without loss of consciousness) and complex partial seizures (consciousness impaired), with and without secondary generalization (grand mal epilepsy with loss of consciousness). Usually it must be taken for two to three weeks to determine if it decreases the frequency or severity of seizures. Neurontin can only treat epilepsy; it is not a cure. Neurontin is also used to treat: Anxiety, Insomnia, and Chronic pain (not FDA approved for this use) Neurontin has been used as a mood stabilizer, but some studies show that it is no more effective than a placebo in treating bipolar disorder.

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), fibromyalgia, 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.

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Gabapentin Warnings and Precautions

Neurontin has been tested in children and adolescents from 3 to 18 years old, and its effects have been found to be the same as those in adults, when dosage is appropriately adjusted.  Neurontin may impair the ability to drive or operate heavy machinery.

Neurontin should not be discontinued suddenly – sudden withdrawal may cause seizures to return or occur more frequently. Dosage should be gradually tapered over at least 7 days when Neurontin is discontinued. For Pregnant or Nursing Mothers: Neurontin has not been studied in pregnant women, but other antiepileptic drugs have been known to cause birth defects. Studies in animals indicate that very high doses of Neurontin can cause bone and kidney problems. It is not known whether Neurontin passes into breast milk, and nursing mothers should be cautious about using Neurontin.

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How  Gabapentin is typically packaged?

Capsule: 100, 300, 400mg Tablet: 100, 300, 400, 600, 800mg Oral solution (brand-name only): 250mg/5mL

Normal Dosage Of Gabapentin

USAGE FOR EPILEPSY: The usual starting dose is 300mg for adults and children over 12 years of age. This dose is taken on the evening of the first day. Your doctor may then increase the dose on the second day to 300mg in the morning, and 300mg in the evening. On the third day you may be increased to 300mg three times per day. The maximum dosage is 3600mg per day. Gabapentin is not recommended for children under 12 years.

USAGE FOR DIABETIC NERVE PAIN: The dosage follows the rules for epilepsy, and may be continued for up to 5 months. If you suffer from any kidney problems, the doctor may issue a lower dosage.

USAGE AS A NERVE BLOCK:  Gabapentin is not marketed for use as a nerve block, but is commonly used as such following successful applications. The dosage follows the same rules as for epilepsy patients, with a maximum dosage of 3600mg. For chronic pain conditions, Gabapentin may need

Gabapentin Mechanism of action

The mechanism of the anticonvulsant action of gabapentin has not been fully described. Several possible mechanisms for pain improvement have been discussed. Though similar in structure to the endogenous neurotransmitter GABA, gabapentin has not been shown to bind to GABA receptors at concentrations at or below 1 mM.  Gabapentin modulates the action of glutamate decarboxylase (GAD) and branched chain aminotransferase (BCAT), two enzymes involved in GABA biosynthesis. In human and rat studies, gabapentin was found to increase GABA biosynthesis, and to increase non-synaptic GABA neurotransmission in vitro. Gabapentin readily enters the brain and prevents seizures in a number of animal models of epilepsy. Gabapentin does not possess affinity for either GABAA or GABAB receptor nor does it alter the metabolism of GABA. It does not bind to other neurotransmitter receptors of the brain and does not interact with sodium channels. Gabapentin binds with high affinity to the α2δ (alpha-2-delta) subunit of voltage-gated calcium channels and it is proposed that binding to the α2δ subunit may be involved in gabapentin’s anti-seizure effects in animals. Broad panel screening does not suggest any other drug targets other than α2δ. Evidence from several preclinical models inform that the pharmacological activity of gabapentin may be mediated via binding to α2δ through a reduction in release of excitatory neurotransmitters in regions of the central nervous system. Such activity may underlie gabapentin’s anti-seizure activity. The relevance of these actions of gabapentin to the anticonvulsant effects in humans remains to be established Gabapentin also displays efficacy in several preclinical animal pain models. Specific binding of gabapentin to the α2δ subunit is proposed to result in several different actions that may be responsible for analgesic activity in animal models. The analgesic activities of gabapentin may occur in the spinal cord as well as at higher brain centers through interactions with descending pain inhibitory pathways. The relevance of these preclinical properties to clinical action in humans is unknown.

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.

Gabapentin has been shown to bind to the α2δ-1 subunit of voltage gated calcium ion channels, which contributes to its pain attenuation effects in diabetic neuropathy and post-herpetic neuralgia. Other neurophysiological findings indicate that gabapentin also interacts with NMDA receptors, protein kinase C, and inflammatory cytokines.

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. 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.

Gabapentin Warnings

Side effects reported in children age 3 to 12 include: Aggressive behaviors / behavior problems,Anxiety, fidgeting or restlessness, Difficulty concentrating or change in school performance, Crying, False sense of well-being, Hyperactivity, Depression, Emotionally overreacting, mood swings.

Side effects in adults: Drowsiness,Dizziness, Fatigue, Clumsiness, Tremor, Nystagmus (rapid involuntary movements of the eyes), Ataxia (shaky movements and unsteady gait), Rhinitis (excessively runny nose and eyes), Nausea, Weight gain, Skin rash, Changes in vision, Vomiting, Low blood pressure, Constipation, Impotence, Lowered white blood cell count, Sleepiness, Mood swings, Hostile behavior, Disordered thinking, Hyperactive behavior

Rarely Gabapentin Side Effects: Severe skin rash (Stevens-Johnson syndrome, rare), Seizure

Gabapentin Interactions with Drugs and Other Substances

Drugs or substances that may interact with Neurontin include:

• • • Antacids (within 2 hours) – taking Neurontin with antacids may reduce Neurontin’s effects.
    • Alcohol – frequent use of alcohol may seriously reduce the effectiveness of Neurontin.
    • Tagamet (cimetidine) – may increase blood levels of Neurontin.
    • Dilantin (phenytoin) – taking Neurontin with Dilantin may lead to phenytoin toxicity.
    • Central nervous system (CNS) depressants, including cold medicines – these medications may add to the sedative effects of Neurontin.

Gabapentin For Migraine Prevention

International and domestic studies that have evaluated Neurontin for migraine prevention suggest that it is effective. In a study of 63 patients with migraine (with or without aura), gabapentin significantly reduced migraine frequency and intensity among 30 patients who received it. In this study, adverse events were mild to moderate in severity.

Similarly, in a large study, 143 people with migraine received daily doses of Neurontin or placebo for 12 weeks. At the end of 12 weeks, the migraine rate had declined from 4.2 migraines before treatment to 2.7 migraines after treatment in those who received this drug. This decrease was significantly greater than the decrease from 4.1 migraines to 3.5 migraines among those who received placebo. Of the 56 gabapentin recipients, 46% had at least a 50% reduction in the four-week migraine rate. Drug-related adverse events (sleepiness and dizziness) led to drug withdrawal in 13% of patients in the gabapentin group compared with 7% in the placebo group. The researchers concluded that this medication is an effective and well-tolerated preventive for migraine.

However, the American Academy of Neurology (AAN), the organization that provides guidance for the use of drugs to prevent migraines, has stated that there is not enough evidence at this time to support the use of gabapentin for migraine prevention. Healthcare professionals can choose to prescribe gabapentin when other prevention therapies have not worked, however.

Some people can prevent migraines by avoiding triggers. Others have prevented migraines successfully through relaxation techniques, acupuncture, or exercise. However, these therapies alone don’t work for everyone. Some people also need treatment with medication to reduce the number of migraines they have. The drugs used to prevent migraines are different from drugs that to treat migraines once a migraine starts. Drugs that prevent migraines, such as gabapentin, must be taken daily.

For more information about Gabapentin, please check Gabapentin information in drugs.com or Gabapentin information in Webmd.com

Gabapentin is FDA-approved for:

• Partial seizures (adjunctive therapy)

• Postherpetic neuralgia (PHN)

However, gabapentin is widely prescribed off-label for a range of conditions due to its effects on nerve excitability and modulation of pain signals. Below is a detailed breakdown of off-label uses of gabapentin, categorized by medical domains, along with supporting rationale and available evidence where relevant.

? Neurology / Psychiatry

1. Generalized Anxiety Disorder (GAD)

• Rationale: Modulates GABAergic activity and reduces excitatory neurotransmission.

• Evidence: Small studies and case reports support its anxiolytic effects.

• Clinical Use: Often considered when SSRIs/SNRIs are contraindicated or not tolerated.

2. Bipolar Disorder (esp. Bipolar II or rapid cycling)

• Rationale: Mood stabilization through calcium channel modulation.

• Evidence: Limited; some benefit reported in adjunctive therapy, but not robust compared to mood stabilizers like lithium or valproate.

3. Insomnia (especially with comorbid anxiety or pain)

• Rationale: Sedative effects and reduced sleep latency.

• Use Case: In patients with fibromyalgia, anxiety, or chronic pain.

4. Alcohol Withdrawal and Cravings

• Rationale: Enhances GABA, decreases glutamate (similar to benzodiazepines).

• Evidence: Clinical trials support reduced withdrawal symptoms and relapse rates.

• Dose: Often 900–1800 mg/day in divided doses.

5. Restless Legs Syndrome (RLS)

• Rationale: Modulates dopamine and glutamate pathways.

• Evidence: Gabapentin enacarbil is FDA-approved for RLS; gabapentin is used off-label similarly.

? Pain Management (Non-FDA Approved Neuropathic Pain)

6. Diabetic Neuropathy

• Rationale: Modulates α2δ subunit of voltage-gated calcium channels, reducing neuropathic pain signals.

• Evidence: Strong; included in many guidelines for diabetic peripheral neuropathy.

7. Fibromyalgia

• Rationale: Reduces central sensitization.

• Evidence: Gabapentin can improve sleep and reduce pain; FDA-approved alternative is pregabalin.

8. Chronic Migraine or Tension-Type Headache (Prophylaxis)

• Rationale: Inhibits cortical spreading depression, stabilizes nerve activity.

• Evidence: Modest benefit; used when traditional preventives fail.

9. Postoperative Pain / Perioperative Pain Reduction

• Rationale: Reduces central sensitization post-surgery.

• Use: Common in multimodal pain management protocols.

10. Trigeminal Neuralgia

• Rationale: Reduces paroxysmal pain episodes.

• Evidence: Especially helpful when carbamazepine is not tolerated.

?‍♀️Women’s Health

11. Hot Flashes (Menopausal or Hormone-Suppression-Induced)

• Rationale: Thought to stabilize thermoregulatory centers.

• Evidence: Moderate; used in breast cancer patients where hormone therapy is contraindicated.

• Typical Dose: 900 mg/day, divided.

? Other Neurological / Cognitive Disorders

12. Essential Tremor

• Rationale: May reduce abnormal cerebellar output.

• Evidence: Mild efficacy, used second-line to propranolol or primidone.

13. Spinal Cord Injury–Related Spasticity and Pain

• Rationale: Reduces hyperexcitability in the spinal cord.

• Clinical Use: Often used in combination with baclofen or tizanidine.

? Off-label Psychiatric / Addiction Uses (Experimental or Case-Based)

14. Cocaine and Methamphetamine Dependence

• Rationale: Reduces withdrawal symptoms, possibly via GABA modulation.

• Evidence: Mixed; some positive trials but not FDA-approved.

15. PTSD (Post-Traumatic Stress Disorder)

• Rationale: May reduce nightmares, anxiety, and hyperarousal.

• Evidence: Limited; used as adjunctive treatment.

? Musculoskeletal and Miscellaneous Conditions

16. Chronic Low Back Pain (esp. with radiculopathy)

• Rationale: Targets neuropathic pain elements.

• Evidence: Useful when there is nerve compression or sciatica.

17. Irritable Bowel Syndrome (IBS) – Pain-Predominant Subtype

• Rationale: Calms visceral hypersensitivity through central mechanisms.

• Evidence: Experimental; not first-line.

? Summary Table

What Special Precautions Should I Follow?

• tell your doctor and pharmacist if you are allergic to gabapentin, any other medications, or any of the inactive ingredients in the type of gabapentin you plan to take. Ask your pharmacist for a list of the inactive ingredients.
• you should know that gabapentin is available in different forms that may be prescribed for different uses. Ask your doctor to be sure that you are not taking more than one product that contains gabapentin.
• tell your doctor and pharmacist what prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take. Be sure to mention any of the following: hydrocodone (in Hydrocet, in Vicodin, others), medications that make you feel dizzy or drowsy, morphine (Avinza, Kadian, MSIR, others), and naproxen (Aleve, Anaprox, Naprosyn, others). Your doctor may need to change the doses of your medications or monitor you carefully for side effects.
• if you are taking antacids such as Maalox or Mylanta, take them at least 2 hours before you take gabapentin tablets, capsules, or solution.
• tell your doctor if you have or have ever had kidney disease. If you will be taking the extended-release tablets, also tell your doctor if you need to sleep during the day and stay awake at night.
• tell your doctor if you are pregnant, plan to become pregnant, or are breast-feeding. If you become pregnant while taking gabapentin, call your doctor.
• if you are having surgery, including dental surgery, tell the doctor or dentist that you are taking gabapentin.
• you should know that this medication may make you drowsy or dizzy, may slow your thinking, and may cause loss of coordination. Do not drive a car or operate machinery until you know how this medication affects you, and your doctor agrees that it is safe for you to begin these activities.
• if you are giving gabapentin to your child, you should know that your child’s behavior and mental abilities may change while he or she is taking gabapentin. Your child may have sudden changes in mood, become hostile or hyperactive, have difficulty concentrating or paying attention, or be drowsy or clumsy. Have your child avoid activities that could be dangerous, such as riding a bicycle, until you know how gabapentin affects him or her.
• remember that alcohol can add to the drowsiness caused by this medication.
• you should know that your mental health may change in unexpected ways and you may become suicidal (thinking about harming or killing yourself or planning or trying to do so) while you are taking gabapentin for the treatment of epilepsy, mental illness, or other conditions. A small number of adults and children 5 years of age and older (about 1 in 500 people) who took anticonvulsants such as gabapentin to treat various conditions during clinical studies became suicidal during their treatment. Some of these people developed suicidal thoughts and behavior as early as one week after they started taking the medication. There is a risk that you may experience changes in your mental health if you take an anticonvulsant medication such as gabapentin, but there may also be a risk that you will experience changes in your mental health if your condition is not treated. You and your doctor will decide whether the risks of taking an anticonvulsant medication are greater than the risks of not taking the medication. You, your family, or your caregiver should call your doctor right away if you experience any of the following symptoms: panic attacks; agitation or restlessness; new or worsening irritability, anxiety, or depression; acting on dangerous impulses; difficulty falling or staying asleep; aggressive, angry, or violent behavior; mania (frenzied, abnormally excited mood); talking or thinking about wanting to hurt yourself or end your life; withdrawing from friends and family; preoccupation with death and dying; giving away prized possessions; or any other unusual changes in behavior or mood. Be sure that your family or caregiver knows which symptoms may be serious so they can call the doctor if you are unable to seek treatment on your own.

• • • 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.

If you experience a serious side effect, you or your doctor may send a report to the Food and Drug Administration’s (FDA) MedWatch Adverse Event Reporting program online [at http://www.fda.gov/Safety/MedWatch] or by phone [1-800-332-1088].

Symptoms of overdose may include the following:

• double vision
• slurred speech
• drowsiness
• diarrhea