Composition:

Each Neuroglopentin capsule contains 100 mg, 300 mg, or 400 mg of gabapentin.

Pharmacodynamics:

Neuroglopentin, gabapentin, is an oral antiepileptic drug (AED).

It is structurally related to the neurotransmitter GABA (gamma-aminobutyric acid) but it does not interact with GABA receptors, it is not converted metabolically into GABA or a GABA agonist, and it is not an inhibitor of GABA uptake or degradation.

Its main site of action appears to be on T-type calcium channel function, by binding to a particular channel subunit (α2δ), & it inhibits the release of various neurotransmitters & modulators.

Pharmacokinetics:

Absorption:

Gabapentin is absorbed from the gastrointestinal tract by means of a saturable mechanism. 

Following multiple dosing, peak plasma concentrations are usually achieved within 2 hours of administration and steady state achieved within 1 to 2 days.

 Distribution:

Less than 3% of gabapentin circulates bound to plasma protein.

It is widely distributed throughout the body and is distributed into breast milk.

 Metabolism:

It is not extensively metabolized and most of the dose is excreted unchanged in the urine with the remainder appearing in the feces.

Elimination:

The elimination half-life has been reported to be about 5 to 7 hours.

In elderly patients, and in patients with impaired renal function, gabapentin plasma clearance is reduced. 

It can be removed from plasma by hemodialysis.

Therapeutic Indications:

For the treatment of neuropathic pain in adults.

Post-herpetic Neuralgia:

Neuroglopentin is indicated for the management of post-herpetic neuralgia in adults.

Epilepsy:

Neuroglopentin is indicated as adjunctive therapy in the treatment of partial seizures with and without secondary generalization in patients over 12 years of age with epilepsy. 

It is also indicated as adjunctive therapy in the treatment of partial seizures in pediatric patients age 3 – 12 years.

Dosage and Administration:

Adult with Neuropathic pain, Post-herpetic Neuralgia:

Neuroglopentin therapy may be initiated as a single 300-mg dose on Day 1, followed by 600 mg/day on Day 2 in divided doses, (twice daily), and 900 mg/day on Day 3 in divided doses, (three times daily).

The dose can subsequently be titrated up as needed for pain relief to a daily dose of 1800 mg in divided doses, three times daily.

Epilepsy:

Neuroglopentin is recommended for add-on therapy in patients 3 years of age and older.

Patients >12 years of age:

The effective dose of Neuroglopentin is 900 to 1800 mg/day and given in divided doses (three times a day) using 300 or 400 mg capsules, The starting dose is 300 mg three times a day.

If necessary, the dose may be increased using 300 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.

 Pediatric patients age 3-12 years:

The starting dose should range from 10-15 mg/kg/day in 3 divided doses, and the effective dose reached by upward titration over a period of approximately 3 days.

The effective dose of Neuroglopentin in patients 5 years of age and older is 25-35 mg/kg/day and given in divided doses (three times a day).

The effective dose in pediatric patients aged 3 and 4 years is 40 mg/kg/day and given in divided doses (three times a day).

Drug–Drug Interactions:

Gabapentin is not appreciably metabolized nor does it interfere with the metabolism of commonly co-administered antiepileptic drugs such as: phenytoin, carbamazepine, valproic acid, phenobarbital.

Naproxen: Co-administration of naproxen sodium with gabapentin appears to increase the amount of gabapentin absorbed by 12% to 15%. Gabapentin had no effect on naproxen pharmacokinetic parameters.  

Antacids: Antacids may reduce the bioavailability of gabapentin. It is recommended that gabapentin should be taken at least 2 hours following antacid administration.

Precautions:

Patients should be advised neither to drive a car nor to operate other complex machinery until they have gained sufficient experience on gabapentin.

Patients who require concomitant treatment with morphine may experience increases in gabapentin concentrations, therefore the dose of gabapentin or morphine should be reduced.

Patients should be carefully observed for signs of CNS depression, such as somnolence.

Antiepileptic drugs should not be abruptly discontinued because of the possibility of increasing seizure frequency.

Contraindications:

Gabapentin is contraindicated in patients who have demonstrated hypersensitivity to the drug or any of its ingredients.

 Pregnancy:

Gabapentin should not be used during pregnancy.

Lactation:

Gabapentin should not be used in women who are nursing.

Pediatric:

Effectiveness in pediatric patients below the age of 3 years has not been established.

Adverse Reactions:

The most commonly reported adverse effects associated with gabapentin are somnolence, dizziness, ataxia, and fatigue.

Nystagmus, tremor, diplopia, amblyopia, pharyngitis, dysarthria, weight gain, dyspepsia, amnesia, weakness, paresthesia, arthralgia, purpura, leucopenia, anxiety, and urinary-tract infection may less frequently to occur.

Rarely, pancreatitis, altered liver function tests, erythema multiforme, Stevens-Johnson syndrome, rhinitis, nervousness, myalgia, headache, edema, nausea and vomiting. Blood glucose fluctuations in diabetics have been reported.

Rare CNS effects include confusion, depression, hallucinations, and psychoses.

Presentation & Storage:

Neuroglopentin 100 mg is supplied in boxes of 30 capsules each.

Neuroglopentin 300 mg is supplied in boxes of 30 capsules each.

Neuroglopentin 400 mg is supplied in boxes of 30 capsules each.

Store at a temperature not exceeding 30C, in a dry place.

Patient Instructions:

Follow the recommendations from the doctor; do not exceed the recommended dose.

Avoid driving or operating machinery use as it may cause drowsiness.