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What is Gabapentin and How to take Gabapentin ?

Gabapentin is used with other medications to prevent and control seizures. It is also used to relieve nerve pain following shingles (a painful rash due to herpes zoster infection) in adults. Gabapentin is known as an anticonvulsant or antiepileptic drug.

OTHER USES: This section contains uses of this drug that are not listed in the approved professional labeling for the drug but that may be prescribed by yourhealth care professional. Use this drug for a condition that is listed in this section only if it has been so prescribed by your health care professional.

Gabapentin may also be used to treat other nerve pain conditions (such as diabetic neuropathy, peripheral neuropathy, trigeminal neuralgia) and restless legs syndrome.

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.

The Neurontin brand is also used to treat seizures in adults and children who are at least 3 years old.

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.

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

Once a medicine has been approved for marketing for a certain use, experience may show that it is also useful for other medical problems. Although this use is not included in product labeling, gabapentin is used in certain patients with the following medical condition:

Diabetic peripheral neuropathy.

This product is available in the following dosage forms:

Tablet, Capsule, Suspension, Solution.

US Brand Name

  1. FusePaq Fanatrex
  2. Gabarone
  3. Gralise
  4. Neurontin

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.

How should Gabapentin be used ?

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 special precautions should I follow?

Before taking gabapentin,

  • 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.

    Gabapentin
    Gabapentin

  • 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.

 

Mechanism of action of Gabapentin

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.

Gabapentin is best known under the brand name Neurontin manufactured by Pfizer subsidiary Parke-Davis. A Pfizer subsidiary named Greenstone markets generic gabapentin.

In December 2004 the FDA granted final approval to a generic equivalent to Neurontin made by the Israeli firm Teva.

Neurontin began as one of Pfizer’s best selling drugs; however, Pfizer has been criticized and under litigation for its marketing of the drug. They face allegations that Parke-Davis marketed the drug for at least a dozen supposed uses that the FDA had not approved. Today it is a mainstay drug for migraines, even though it was not approved for such use in 2004.

Fioricet Side Effects

Drowsiness, dizziness, loss of coordination, tiredness, blurred/double vision, unusualeye movements, or shaking (tremor) may occur. If any of these effects persist or worsen, tell your doctor or pharmacist promptly.

Remember that your doctor has prescribed this medication because he or she has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.

Tell your doctor right away if any of these unlikely but serious side effects occur: swelling of the hands/ankles/feet, signs of infection (such as fever, cough, persistentsore throat).

A small number of people who take anticonvulsants for any condition (such as seizures, bipolar disorder, pain) may experience depression, suicidalthoughts/attempts, or other mental/mood problems. Tell your doctor immediately if you or your family/caregiver notice any unusual/sudden changes in your mood, thoughts, or behavior including signs of depression, suicidal thoughts/attempts, thoughts about harming yourself.

Get medical help right away if you have any serious side effects, including: unusual fever, swollen glands, yellowing skin/eyes, unusual tiredness, dark urine, change in the amount of urine, chest pain.

A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash,itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.

This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.

In the US –

Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

In Canada – Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.

Gabapentin Interactions

Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor’s approval.

Tell your doctor or pharmacist if you are taking other products that cause drowsiness including alcohol, antihistamines (such as cetirizine, diphenhydramine), drugs forsleep or anxiety (such as alprazolam, diazepam, zolpidem), muscle relaxants, and narcotic pain relievers (such as codeine, morphine).

Check the labels on all your medicines (such as allergy or cough-and-cold products) because they may contain ingredients that cause drowsiness. Ask your pharmacist about using those products safely.

Do not use this medication with other medications that contain gabapentin (including gabapentin enacarbil).

This medication may interfere with certain laboratory tests for urine protein. Make sure laboratory personnel and all your doctors know you use this drug.

Overdose

If 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.

Notes

Do not share this medication with others.

Missed Dose

If you miss a dose, take it as soon as you remember. If it is near the time of the next dose, skip the missed dose and resume your usual dosing schedule. Do not double the dose to catch up. If you take gabapentin 3 times a day to control seizures, do not let more than 12 hours pass between doses because your seizures may increase. Consult your doctor right away if this occurs.

Storage

Store at room temperature away from light and moisture. Do not store in the bathroom. Keep all medications away from children and pets.

Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.

MEDICAL ALERT: Your condition can cause complications in a medical emergency. For information about enrolling in MedicAlert, call 1-888-633-4298 (US) or 1-800-668-1507 (Canada).

Information last revised December 2013. Copyright(c) 2013 First Databank, Inc.

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