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Gabapentin is a prescription drug, marketed as Neurontin and Horizant, that’s used to treat epilepsy. Doctors can prescribe gabapentin to treat epilepsy in people older than 12, and partial seizures in children ages 3 to 12.

Gabapentin may also be prescribed to treat restless legs syndrome (RLS), to relieve numberness and tingling related todiabetes, to prevent hot flashes, and to relieve pain that can accompany shingles (known as postherpetic neuralgia).

Studies have also found Gabapentin to have a substantial analgesic effects on diabetic neuropathy, postherpetic neuralgia, migraine, and other neuropathic pain conditions, as well as beneficial effect on sleep and restless legs syndrome. On the basis of these findings, some doctors also prescribe gabapentin to cure fibromyalgia pain. For more information, please click here.

Gabapentin is an effective prophylactic agent for patients with migraine. In addition, gabapentin appears generally well tolerated with mild to moderate somnolence and dizziness.

Pregabalin (Lyrica), a drug similar to gabapentin, was the first medication approved by the Food and Drug Administration (FDA) to treat fibromyalgia. While gabapentin hasn’t been approved by the FDA for the treatment of fibromyalgia, some doctors may prescribe it off-label for such use.

Anticonvulsant drugs, such as gabapentin, are becoming increasingly popular for migraine prevention.

Gabapentin has mush more usages, it can cure nerve pain, prevent migraines and headaches. It is also widely used to treat Insomnia, Fibromyalgia, and Restless Legs Syndrome Pain. For more information, please check What is Gabapentin and What It Is Used For ?

A study in the Canadian Journal of Anesthesia in 2013 revealed that gabapentin may help ease moderate to high levels of anxiety among people about to have surgery. The researchers noted that doctors are increasingly using the drug to treat pain after surgery as well as a variety of psychiatric diseases, such as chronic anxiety disorders.

Gabapentin Warnings

You should know that gabapentin may increase the risk for suicide.

Suicidal thoughts or behavior occurs in about one in 500 people taking medications like gabapentin. This risk may begin within a week of starting treatment.

Let your doctor know if you experience:

  • Thoughts of suicide
  • Symptoms of depression
  • Aggression
  • Irritability
  • Panic attacks
  • Extreme worry
  • Restlessness
  • Acting without thinking
  • Abnormal excitement

You should also let friends and family members know about these symptoms.

Gabapentin Mechanism Of Action

The precise mechanisms by which gabapentin produces its analgesic and antiepileptic actions are unknown. Gabapentin is structurally related to theneurotransmitter gamma-aminobutyric acid (GABA) but has no effect on GABA binding, uptake, or degradation. In vitro studies have shown that gabapentin binds with high-affinity to the α2δ subunit of voltage-activated calcium channels; however, the relationship of this binding to the therapeutic effects of gabapentin is unknown.

Do not stop taking NEURONTIN without first talking to your healthcare provider. Stopping NEURONTIN suddenly can cause serious problems.

Gabapentin Side effects

NEURONTIN can cause serious side effects including:

1. Suicidal Thoughts. Like other antiepileptic drugs, NEURONTIN may cause suicidal thoughts or actions in a very small number of people, about 1 in 500.

Call a healthcare provider right away if you have any of these symptoms, especially if they are new, worse, or worry you:

  • thoughts about suicide or dying
  • attempts to commit suicide
  • new or worse depression
  • new or worse anxiety
  • feeling agitated or restless
  • panic attacks
  • trouble sleeping (insomnia)
  • new or worse irritability
  • acting aggressive, being angry, or violent
  • acting on dangerous impulses
  • an extreme increase in activity and talking (mania)
  • other unusual changes in behavior or mood

How can I watch for early symptoms of suicidal thoughts and actions?

  • Pay attention to any changes, especially sudden changes, in mood, behaviors, thoughts, or feelings.
  • Keep all follow-up visits with your healthcare provider as scheduled.

Call your healthcare provider between visits as needed, especially if you are worried about symptoms.

Do not stop taking NEURONTIN without first talking to a healthcare provider.

  • Stopping NEURONTIN suddenly can cause serious problems. Stopping a seizure medicine suddenly in a patient who has epilepsy can cause seizures that will not stop (status epilepticus).
  • Suicidal thoughts or actions can be caused by things other than medicines. If you have suicidal thoughts or actions, your healthcare provider may check for other causes.

2. Changes in behavior and thinking –Using NEURONTIN in children 3 to 12 years of age can cause emotional changes, aggressive behavior, problems with concentration, restlessness, changes in school performance, and hyperactivity.

3. NEURONTIN may cause serious or life-threatening allergic reactions that may affectyour skin or other parts of your body such as your liver or blood cells. This may cause you to be hospitalized or to stop NEURONTIN. You may or may not have a rash with an allergic reaction caused by NEURONTIN. Call a healthcare provider right away if you have any of the following symptoms:

  • skin rash
  • hives
  • difficulty breathing
  • fever
  • swollen glands that do not go away
  • swelling of your face, lips, throat, or tongue
  • yellowing of your skin or of the whites of the eyes
  • unusual bruising or bleeding
  • severe fatigue or weakness
  • unexpected muscle pain
  • frequent infections

These symptoms may be the first signs of a serious reaction. A healthcare provider should examine you to decide if you should continue taking NEURONTIN.

The most common side effects of gabapentin in adult patients include dizziness, fatigue, drowsiness, weight gain, and peripheral edema (swelling of extremities).[40] Gabapentin may also produce sexual dysfunctionin some patients, symptoms of which may include loss of libido, inability to reach orgasm, and erectile dysfunction. Gabapentin should be used carefully in patients with renal impairment due to possible accumulation and toxicity. What side effects can Gabapentin cause?

Gabapentin Dosage

A typical adult dose for postherpetic neuralgia usually starts at 300 milligrams (mg), and your doctor may increase the dose to up to 1,800 mg a day.

A typical adult dose for epilepsy may range from 900 to 1,800 mg a day.

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Usual Adult Dose for Postherpetic Neuralgia:

Initial dose: 300 mg orally on day one, 300 mg orally twice a day on day two, then 300 mg orally 3 times a day on day three.

The dose may be titrated up as needed for pain relief to a daily dose of 1800 mg.
Maintenance dose: 900 to 1800 mg orally in 3 divided doses.

Efficacy was demonstrated in clinical studies over a range of 1800 mg/day to 3600 mg/day. However, no additional benefit was demonstrated from the use of doses over 1800 mg/day.

Gabapentin available under the trade name Gralise (R):

Maintenance dose: Gralise (R) should be titrated to 1800 mg orally once daily with the evening meal.

Recommended titration schedule:
Day 1: 300 mg orally with the evening meal
Day 2: 600 mg orally with the evening meal
Days 3 through 6: 900 mg orally with the evening meal
Days 7 through 10: 1200 mg orally with the evening meal
Days 11 through 14: 1500 mg orally with the evening meal
Day 15: 1800 mg orally with the evening meal

Gralise (R) is not interchangeable with other gabapentin products because of differing pharmacokinetic profiles that affect the frequency of administration.

Gabapentin enacarbil extended release tablets available under the trade name Horizant (R):

The recommended dosage is 600 mg orally twice daily. Therapy should be initiated at a dose of 600 mg orally in the morning for 3 days of therapy, then increased to 600 mg twice daily (1,200 mg/day) on day four.

Gabapentin enacarbil extended release tablets available under the trade name Horizant (R) and gabapentin are not interchangeable.

Usual Adult Dose for Restless Legs Syndrome:

Gabapentin enacarbil available under the trade name Horizant (R):
600 mg orally once daily with food at about 5 PM

Usual Pediatric Dose for Epilepsy:

Less than 3 years: Effectiveness has not been established.

Greater than or equal to 3 and less than 12 years:
Starting Dose: ranges from 10 to 15 mg/kg/day in 3 divided doses.
Effective Dose: reached by upward titration over a period of approximately 3 days. The effective dose of gabapentin in patients 5 years of age and older is 25 to 35 mg/kg/day and given in divided doses (three times a day). The effective dose in pediatric patients ages 3 and 4 years is 40 mg/kg/day and given in divided doses (three times a day). Gabapentin may be administered as the oral solution, capsule, or tablet, or using combinations of these formulations. Dosages up to 50 mg/kg/day have been well tolerated in a long term clinical study. The maximum time interval between doses should not exceed 12 hours.

Greater than 12 years:
Initial dose: 300 mg orally on day one, 300 mg orally twice a day on day two, then 300 mg orally 3 times a day on day three.
Maintenance dose: 900 to 1800 mg orally in 3 divided doses. If necessary, the dose may be increased using 300 mg or 400 mg capsules three times a day up to 1800 mg/day. Dosages up to 2400 mg/day have been well tolerated in long term clinical studies. Doses of 3600 mg/day have also been administered to a small number of patients for a relatively short duration, and have been well tolerated. The maximum time between doses in the three times a day schedule should not exceed 12 hours.

Your doctor will usually start you at a low dose of gabapentin and then increase the dose gradually until you get to a level that works best for you. For More information, please check   How should Gabapentin be used?

Gabapentin Overdose

A lethal dose of gabapentin was not identified in mice and rats receiving single oral doses as high as 8000 mg/kg. Signs of acute toxicity in animals included ataxia, labored breathing, ptosis, sedation, hypoactivity, or excitation.

Acute oral overdoses of NEURONTIN up to 49 grams have been reported. In these cases, double vision, slurred speech, drowsiness, lethargy, and diarrhea were observed. All patients recovered with supportive care. Coma, resolving with dialysis, has been reported in patients with chronic renal failure who were treated with NEURONTIN.

Gabapentin can be removed by hemodialysis. Although hemodialysis has not been performed in the few overdose cases reported, it may be indicated by the patient’s clinical state or in patients with significant renal impairment.

Online Gabapentin Brand Names

In the U.S.

  • FusePaq Fanatrex
  • Gabarone
  • Gralise
  • Neurontin

Available Dosage Forms:

  • Tablet
  • Capsule
  • Suspension
  • Solution

Therapeutic Class: Anticonvulsant

Chemical Class: Gamma Aminobutyric Acid (class)

The off-lable use of Gabapentin for migraine

Gabapentin is as an anti-epileptic drug and as an analgesic, particularly for pain of the neuropathic or neurogenic type.  When used for controlling epilepsy, it is usually used in conjunction with another anti-epileptic drug.  But Gabapentin is widely used  to treat nerve pain or neuropathic pain than it is to treat epilepsy.  It is also widely used to treat Anxiety and Migraine prevention.

Gabapentin Off-Label Usage

One of Gabapentin “off-label” usage is for migraine prevention and treatment, including migraines with or without aura, vestibular migraines. It can reduce the frequency of headaches, pain intensity, and the use of symptomatic medications. Gabapentin is a good preventive therapy for migraines refractory to standard medications.

The chemical structure of gabapentin is related that of gamma-aminobutyric acid (GABA) which is a neurotransmitter in the brain. The exact mechanism as to how gabapentin controls epilepsy and relieves pain is unknown, but it probably acts like the neurotransmitter GABA.

The effective dose of gabapentin varies greatly. Some persons need only 200-300 mg a day whereas others may need 3000 mg or more a day. It may take several weeks to become effective, so it is important to stay on it for an adequate length of time.

The Efficacy of gabapentin in migraine prophylaxis experiment shows  gabapentin is an effective prophylactic agent for patients with migraine.

In the Clinical trials143 patients evaluated gabapentin for migraine prophylaxis.  After 3 months the patients taking gabapentin had a reduction of the migraine frequency by 1.5 migraines per month (or by 35.7%) compared with a reduction of 0.6 migraines per month for the placebo group. Also, gabapentin reduced the headache frequency by 50% or greater in 45% patients compared with only 16% patients on placebo. The most frequently reported adverse events  were asthenia, dizziness, somnolence, and infection.

Gabapentin for Migrain patient Reviews

In Famous medical websites, migraine patients also review the gabapentin as the migraine prevention medicine. They rate Gabapentin 8.1 stars out of ten stars. It is a high mark and means Gabapentin is a very effective medicine for migraine prevention.

I haven’t been taking this medication for long but it’s helped so much. Neuro started me off on 300mg at night and now I’m at 600mg at night. It doesn’t make me sleepy or drowsy. Before starting gabapentin, I was having migraines just about every day. I started having aphasia and vision changes with my migraines, so I decided to take action. I’ve only been on it for almost 2 weeks but I’ve been migraine free and my triggers are no longer triggers at this point, which is fantastic. I should note it has reduced my appetite but this is not a negative thing.” –  Crystaldreams July 25, 2017

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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 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 Adverse Reactions

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

Migraine

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