Gabapentin

Therapeutic Indications

Gabapentin is a prescription only medication available in both brand and generic versions. It is an anticonvulsant or anti-epileptic drug.  Gabapentin is manufactured as an oral capsule/tablet (both extended-release and immediate-release) as well as an oral solution. The drug is marketed under the brand name of Horizant and Neurontin.

Gabapentin is used by medical specialists to effectively treat epilepsy in adults and children. Gabapentin is prescribed to alleviate the following health problems:

• Partial seizures/epilepsy in adults and children
• Postherpetic neuralgia
• Numbness and tingling related to diabetes
• Hot flashes
• Restless legs syndrome (RLS)
• Chronic Anxiety Disorders

Do I need a Prescription?

Gabapentin is an anti-epileptic drug and needs to be consumed only on the advice of a qualified medical specialist. This is because the drug acts on the nerves and chemicals that trigger seizures. Hence, a prescription by a registered medical practitioner is mandatory due to the drug’s contraindications and side effects.

Dosage

The dosage for Gabapentin is fixed after evaluating key parameters pertaining to the medical condition, severity, the age of the patient, reaction to dosage and extent of relief.

• Gabapentin is manufactured, as a tablet, capsule and as a liquid. It is available in strengths of 100mg, 300mg, and 400 mg.
• Adult Dose for Postherpetic neuralgia typically begins at 300 milligrams (mg) and can increase up to 1,800 mg a day.
• Dosage for adults to treat epilepsy can be fixed from 900 to 1,800 mg a day.
• Child dosage (ages 12–17 years) for epilepsy may start at 300 mg three times daily spread over even intervals during the day. The dosage can be increased up to a maximum of 2,400–3,600 mg per day.
• Child dosage (ages 3–11 years) to treat epilepsy may begin with 10–15 mg/kg/day, split evenly into three doses in a day. Medical specialists may increase the dosage depending upon the response of the child to the initial dosage. The dosage cannot exceed 50 mg/kg/day.
• Safety of this drug to treat epilepsy for children below 3 years is yet to be established
• Senior dosage, for those 65 years and older will be much lower doses, to begin with. This is because of reduced kidney function associated with aging.

Important Guidelines

• Gabapentin oral capsules can be consumed with or without food, although the presence of food can reduce upset stomach.
• It is best to store Gabapentin at room temperature.
• Avoid damp areas to store this medication.
• Let the gap between doses not exceed 12 hours.
• Consume tablets without crushing, chewing or breaking them.

Chemical Composition

Gabapentin is also known by the chemical name, Aminomethyl cyclohexaneacetic acid. This chemical is the active ingredient in Neurontin

Ingredients of each Neurontin capsule contains Gabapentin of varying strengths -100 mg, 300 mg, or 400 mg. It also contains gelatin, cornstarch, lactose, talc, titanium dioxide, red iron oxide, and yellow iron oxide.

The chemical composition of each Neurontin tablet consists of 600 mg or 800 mg of Gabapentin along with magnesium stearate, talc, poloxamer 407, cornstarch,copovidone hydroxypropyl cellulose, and candelilla wax.

Neurontin oral solution has 250 mg of gabapentin per 5 mL and contains xylitol, glycerine, and purified water.

Mechanism of Action

• Gabapentin works well to prevent partial seizures.
• Gabapentinfunctions by transcending many lipid membrane barriers using L amino acid transporters to interact with a high-affinity binding site in brain membranes.
• Animal and human studies demonstrate that gabapentin improves GABA synthesis.
• Gabapentin increases non-synaptic GABA responses from neuronal tissues and reduces the release of several monoamine neurotransmitters.
• Gabapentin function effectively to prevent pain responses in animal studies of Hyperalgesia and offsets death of neurons as observed during studies conducted with models of amyotrophic lateral sclerosis (ALS).
• Most importantly, the role of Gabapentin in the modulation of GABA synthesis and glutamate synthesis assumes significance.
• Detailed research on the working of Gabapentin is needed to understand its functions.
• In victims of postherpetic neuralgia, gabapentin works by reducing sensitivity to pain.
• Gabapentin to treat seizures works by changing the effect of calcium on the brain. Low levels of calcium may trigger seizures.

Contraindications

Before starting on Gabapentin, it is important to inform your healthcare professional about all the medications being consumed. This includes medicine supplements, over the counter medications, recreational drugs and herbs.

Drug interactions with Gabapentin

The following types of drugs could trigger interactions

• Medications prescribed for heartburn
• Opiate pain medications
• Naproxen

Gabapentin and Alcohol

• Medical experts advice either total abstinence from alcohol or permit its use in extremely limited quantities.
• This is because Gabapentin interacts with alcohol and can trigger deleterious side effects
• Gabapentin may also be prescribed by experts as a treatment for alcohol dependence.
• Gabapentin was found to reduce symptoms associated with relapse.

Other Interactions

• Avoid driving or operating risky machinery till patient completely understands the side effects of Gabapentin
• Gabapentin could challenge patients’ ability to make judgments, as it induces sleep
• Urine tests to gauge protein levels may not be accurate under the effect of Gabapentin

Precautions/warning

• Never discontinue Gabapentin suddenly. It can trigger long seizures in epileptics
• The side effects of Gabapentin for children between 3-12 years can manifest as behavioral problems. Children can portray hyperactivity and restlessness.
• Victims suffering from kidney issues need to exercise caution before starting this drug. Since the drug is processed slowly in the body, there are chances that it remains in the body for longer hours.
• Pregnant women must know that Gabapentin during pregnancy can cause adverse effects on the fetus. It should be prescribed to the expectant mother only if the benefits far exceed the potential side effects of the drug on the growing fetus.
• Breastfeeding women should consult specialists about the continuation of the drug. Gabapentin can likely be conveyed to the child through the breast milk which can lead to serious side effects.
• Gabapentin for children below 3 years to treat seizures is not recommended.
• Seniors may also process Gabapentin much slower than younger people. Therefore, a reduced dose may be good to begin. This offsets the unhealthy accumulation of the drug in the body.

Side Effects of Gabapentin

Common side effects:

• Dizziness
• Sleepiness
• Awkward gait
• Fatigue
• Alterations in vision or even double vision
• Nervousness
• Swelling of hands or feet
• Weight gain
• Memory loss
• Tremor
• Runny nose
• Dry mouth
• Indigestion
• Headache
• Weird thoughts
• Muscle ache
• Fever
• Diarrhea or constipation
• Itchy eyes

Serious side effects: Need for emergency medical assistance

• Breathing difficulty
• Seizure
• Severe rash
• Suicidal thoughts
• Self-harm tendencies
• Inflammation of lymph nodes
• Swelling of the face, lips, or tongue
• Difficulty Swallowing

What to Do if You Skip a Dose

If you happen to skip a dose, take it as soon as you remember. In case, this is close to the timing of the next dose, take only one dose. Never take doses together as this could prove highly dangerous.

Overdose

• Overdosing on Gabapentin means deleterious levels of the drug in the system, this could manifest as slurred speech, fatigue, double vision, and diarrhea.
• Contact the medical emergency case of Gabapentin overdose

Generic Brand Names of Gabapentin

• FusePaq Fanatrex
• Gabarone
• Gralise
• Neurontin

Different Brands and Manufacturing Companies of the Drug

Nearly 37 companies manufacture Gabapentin with different brand names. Few names are indicated below:

• Dobin Drukst Biotech
• Encentin East West Pharma
• Gaba Hanburys Health Care Pvt. Ltd.
• Gabacent Crescent Therapeutics Ltd
• Gabaciz Invision Medi Sciences Pvt. Ltd.
• Gabalept Micro Labs Ltd.
• Gabantin Sun Pharmaceuticals Industries Ltd.
• Gabator Torrent Pharmaceuticals Ltd.
• Neurontin Parke Davis (India) Limited

Substitutes for the Drug

Drug alternatives for Gabapentin are indicated below:

• Cymbalta (duloxetine)
• Lyrica (pregabalin)
• Depakote (divalproex)
• Elavil (amitriptyline)
• Norpramin
• Pamelor
• Lidoderm

References

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