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What is gabapentin?

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 of gabapentin is also used to treat restless legs syndrome (RLS). The Neurontin brand of gabapentin is also used to treat seizures in adults and children who are at least 3 years old.  Gabapentin is also used to cure migraine. Gabapentin is effective in insomnia. Gabapentin is effective in alleviating itching in renal failure (uremic pruritus) and itching of other etiologies.

Use only the brand and form of gabapentin that your doctor has prescribed. Check your medicine each time you get a refill at the pharmacy, to make sure you have received the correct form of this medication.

Gabapentin was first approved for use in 1993. In the United States it has been available as a generic medication since 2004.

Gabapentin may be useful in the treatment of comorbid anxiety in bipolar patients, (however not the bipolar state itself).  Gabapentin may be effective in acquired pendular nystagmus and infantile nystagmus, (but not periodic alternating nystagmus). It is effective in hot flashes. It may be effective in reducing pain and spasticity in multiple sclerosis. Gabapentin may reduce symptoms of alcohol withdrawal (but it does not prevent the associated seizures). Use for smoking cessationhas had mixed results.

Suicide

In 2009 the U.S. Food and Drug Administration issued a warning of an increased risk of depression and suicidal thoughts and behaviors in patients taking gabapentin, along with other anticonvulsant drugs.  modifying the packaging insert to reflect this.  A 2010 meta analysis confirmed the increased risk of suicide associated with gabapentin use.

Gabapentin Mechanism of action

The mechanism of the anticonvulsant action of gabapentin has not been fully described. 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-mechanism

Gabapentin has been shown to bind to the α2δ-1 subunit of voltage gated calcium ion channels which attributes 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

HOW TO USE Gabapentin

Neurontin 800 mgRead the Medication Guide and, if available, the Patient Information Leaflet provided by your pharmacist before you start taking gabapentin and each time you get a refill. If you have any questions, ask your doctor or pharmacist.

Take this medication by mouth with or without food as directed by your doctor. Dosage is based on your medical condition and response to treatment. For children, the dosage is also based on weight.

If you are taking the tablets and your doctor directs you to split the tablet in half, take the other half-tablet at your next scheduled dose. Discard half tablets if not used within several days of splitting them. If you are taking the capsules, swallow them whole with plenty of water.

It is very important to follow your doctor’s dosing instructions exactly. During the first few days of treatment, your doctor may gradually increase your dose so your body can adjust to the medication. To minimize side effects, take the very first dose at bedtime.

Take this medication regularly to get the most benefit from it. This drug works best when the amount of medicine in your body is kept at a constant level. Therefore, take gabapentin at evenly spaced intervals at the same time(s) each day. If you are taking this medication 3 times a day to control seizures, do not let more than 12 hours pass between doses because your seizures may increase.

Do not take this medication more often or increase your dose without consulting your doctor. Your condition will not improve any faster and the risk of serious side effects may increase.

Do not stop taking this medication without consulting your doctor. Some conditions may become worse when the drug is suddenly stopped. Your dose may need to be gradually decreased.

Antacids containing aluminum or magnesium may interfere with the absorption of this medication. Therefore, if you are also taking an antacid, it is best to take gabapentin at least 2 hours after taking the antacid.

Different forms of gabapentin (such as immediate-release, sustained-release, enacarbil sustained-release) are absorbed in the body differently. Do not switch from one form to the other without consulting your doctor.

Tell your doctor if your condition does not improve or if it worsens.

What Diseases can Gabapentin be treated ?

By Drugs.com, Gabapentin Can be used for a lot of Nerve Pain related health conditions.
including Cough, Hot Flashes, Alcohol Withdrawal, Anxiety 161 reviews, Bipolar Disorder, Trigeminal Neuralgia, Postherpetic Neuralgia, Migraine, Insomnia， Occipital Neuralgia， Peripheral Neuropathy，Vulvodynia, Benign Essential Tremor, Epilepsy, Fibromyalgia, Pain Relief, Diabetic Peripheral Neuropathy , Neuropathic Pain，Reflex Sympathetic Dystrophy Syndrome，Periodic Limb Movement Disorder， Spondylolisthesis， Burning Mouth Syndrome，Pudendal Neuralgia， Small Fiber Neuropathy.

A lot of Patients use Gabapentin (Neurontin) to treat Hot Flashes, Anxiety, Bipolar Disorder, Migraine, Insomnia, Restless Legs Syndrome, Peripheral Neuropathy, Fibromyalgia, Neuropathic Pain. Fe patients use gabapentin to treat Pruritus, Cough, Occipital Neuralgia, Benign Essential Tremor, ement Disorder, Spondylolisthesis, Burning Mouth Syndrome, Pudendal Neuralgia, Small Fiber Neuropathy.

What you must know before you take Gabapentin 

Before taking gabapentin, tell your doctor or pharmacist if you are allergic to it; or to gabapentin enacarbil; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.

Before using this medication, tell your doctor or pharmacist your medical history, especially of: kidney disease, mental/mood problems (such as depression, thoughts of suicide), use/abuse of drugs/alcohol.

This drug may make you dizzy or drowsy or cause blurred vision. Do not drive, use machinery, or do any activity that requires alertness or clear vision until you are sure you can perform such activities safely. Limit alcoholic beverages.

Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).

Older adults may be more sensitive to the side effects of this drug, especially swelling of the hands/ankles/feet, dizziness, or loss of coordination. Dizziness and loss of coordination can increase the risk of falling.

Children may be more sensitive to the side effects of this drug, especially mental/mood/behavior changes (such as hostility, problems concentrating, restlessness).

During pregnancy, this medication should be used only when clearly needed. Discuss the risks and benefits with your doctor.

Gabapentin passes into breast milk. Consult your doctor before breast-feeding.

What kind of patients are not allowed to buy Gabapentin Online

Gabapentin

You can not buy gabapentin online if you have following health conditions:

1. kidney disease (or if you are on dialysis);
2. liver disease;
3. heart disease; or
4. (for patients with RLS) if you are a day sleeper or work a night shift.
5. being pregnant, it is not known whether this medicine will harm an unborn baby, but you need talk to a local Doctor;
6. breast-feeding a baby, Gabapentin can pass into breast milk and may harm a nursing baby;
7. Having suicide thoughts.
8. epilepsy or other seizure disorder;
9. diabetes;
10. a history of depression, mood disorder, drug abuse;
11. You have sent fraud check and not a reliable patient.

It does not mean you cannot take gabapentin. If you have above health conditions, you must go to your local street doctor and let the doctor have your health checked.

What is the most important information I should know about gabapentin (Neurontin)?

Gabapentin

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

Before taking gabapentin, tell your doctor if you have kidney, liver, or heart disease.

You may have thoughts about suicide while taking gabapentin. Your doctor will need to check you at regular visits. Do not miss any scheduled appointments.

Report any new or worsening symptoms to your doctor, such as: mood or behavior changes, anxiety, depression, or if you feel agitated, hostile, restless, hyperactive (mentally or physically), or have thoughts about suicide or hurting yourself.

Do not stop taking gabapentin for seizures without first talking to your doctor, even if you feel fine. You may have increased seizures if you stop using gabapentin suddenly. You may need to use less and less before you stop the medication completely.

Contact your doctor if your seizures get worse or you have them more often while taking gabapentin.

Wear a medical alert tag or carry an ID card stating that you take gabapentin. Any doctor, dentist, or emergency medical care provider who treats you should know that you take seizure medication.

Gabapentin dosing information

Gabapentin

Gabapentin comes as:

gabapentin300mg2

  • 100 mg, 300 mg, and 400 mg capsules
  • 300 mg, 600 mg, and 800 mg tablets
  • a 250 mg/5 mL oral (by mouth) solution.

gabapentin800mgtab

Inactive ingredients in the capsules include lactose, cornstarch, and talc.

  • The 100-mg capsule shell also contains: gelatin and titanium dioxide.
  • The 300-mg capsule shell also contains: gelatin, titanium dioxide, and yellow iron oxide.
  • The 400-mg capsule shell also contains: gelatin, red iron oxide, titanium dioxide, and yellow iron oxide. The imprinting ink contains FD&C Blue No. 2 and titanium dioxide.

Inactive ingredients in the tablets include poloxamer 407, copolyvidonum, cornstarch, magnesium stearate, hydroxypropyl cellulose, talc, candelilla wax, and purified water.

Inactive ingredients in the oral solution include glycerin, xylitol, purified water, and artificial flavor

Usual Adult Dose for Epilepsy:

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.

The safety and effectiveness of gabapentin available under the trade name Gralise (R) or Horizant (R) in patients with epilepsy has not been studied.

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.

Dose Adjustments

Because elderly patients are more likely to have decreased renal function, the dose of this drug should be adjusted based on CrCl values.

GRALISE (R):
-If the dose of this drug under the trade name Gralise (R) is reduced, discontinued, or substituted with an alternative medication, this should be done gradually over a minimum of 1 week or longer or as directed by the physician.

HORIZANT (R):
-If the dose of this drug available under the trade name Horizant (R) is discontinued, patients with RLS receiving 600 mg or less once daily can discontinue the drug without tapering. If the recommended dose is exceeded, the dose should be reduced to 600 mg daily for 1 week prior to discontinuation to minimize the potential of withdrawal seizure.
-Patients with PHN receiving Horizant (R) twice daily should reduce the dose to once daily for 1 week prior to discontinuation to minimize the potential for withdrawal seizure.

Precautions

-Safety and efficacy have not been established in patients younger than 18 years in the management of postherpetic neuralgia.
-Safety and efficacy have not been established in patients younger than 3 years in the adjunctive treatment of partial seizures.
-Safety and efficacy have not been established in patients younger than 18 years for gabapentin available under the trade names Gralise (R) or Horizant (R).

Consult WARNINGS section for additional precautions.

NEURONTIN (Gabapentin) Overdose

Gabapentin

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.

f overdose is suspected, contact a poison control center or emergency room immediately. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center. Symptoms of overdose may include: severe drowsiness, slurred speech, weakness.