Neuran

Neuran

gabapentin

Manufacturer:

Hovid

Distributor:

DCH Auriga - Healthcare
/
Four Star
Full Prescribing Info
Contents
Gabapentin.
Action
Pharmacology: The mechanism of action is unknown. Gabapentin does not react with GABA receptors, is not metabolized to a GABA agonist or to GABA, and does not inhibit GABA uptake or degradation. In rats, gabapentin interacts with a novel binding site on cortical neurons that may be associated with the L-system amino acid transporter of brain cell membranes.
Pharmacokinetics: Absorption: Rapid. Gabapentin is absorbed in part by the L-amino acid transport system, which is a carrier-mediated, saturable transport system; as the dose increases, bioavailability decreases. Bioavailability ranges from approximately 60% for a 300 mg dose to approximately 35% for a 1600 mg dose. Absorption is unaffected by food.
Distribution: Volume of distribution (VolD) is approximately 50 to 60 L. Gabapentin penetrates the blood-brain barrier, yielding cerebrospinal fluid (CSF) concentrations approximately equal to 20% of corresponding steady-state plasma through concentrations in patients with epilepsy. Brain tissue concentrations in one patient undergoing temporal lobectomy were approximately 80% of corresponding plasma concentrations.
Protein Binding: Very low (<5%).
Biotransformation: Gabapentin is not metabolized.
Elimination: Renal- Entire absorbed dose, as unchanged drug. Gabapentin clearance is directly proportional to creatinine clearance.
In dialysis- Gabapentin can be removed from plasma by hemodialysis. The elimination half-life of Gabapentin is independent of dose and averages 5 to 7 hours.
Indications/Uses
Epilepsy: Gabapentin is indicated as adjunctive therapy in the treatment of partial seizures with and without secondary generalization in adults and children aged 6 years and above. Gabapentin is indicated as monotherapy in the treatment of partial seizures with and without secondary generalization in adults and adolescents aged 12 years and above.
Peripheral Neuropathic Pain: Gabapentin is indicated for the treatment of peripheral neuropathic pain which includes painful diabetic neuropathy and post-herpetic neuralgia in adults.
Dosage/Direction for Use
For oral use. Gabapentin can be given with or without food.
If gabapentin has to be discontinued it is recommended this should be done gradually over a minimum of 1 week independent of the indication.
Epilepsy: Epilepsy typically requires long-term therapy. Dosage is determined by the treating physician according to individual tolerance and efficacy.
Adults and Adolescents: In clinical trials, the effective dosing range was 900 to 3600 mg/day. Therapy may be initiated by titrating the dose as described in Table 1 or by administering 300 mg three times a day (TID) on Day 1. Thereafter, based on individual patient response and tolerability, the dose can be further increased in 300 mg/day increments every 2-3 days up to a maximum dose of 3600 mg/day. Slower titration of gabapentin dosage may be appropriate for individual patients. The minimum time to reach a dose of 1800 mg/day is one week, to reach 2400 mg/day is a total of 2 weeks, and to reach 3600 mg/day is a total of 3 weeks. Dosages up to 4800 mg/day have been well tolerated in long-term open-label clinical studies. The total daily dose should be divided in three single doses, the maximum time interval between the doses should not exceed 12 hours to prevent breakthrough convulsions. (See Table 1.)

Click on icon to see table/diagram/image

Pediatric Patients Aged 6 years and above: The starting dose should range from 10 to 15 mg/kg/day and the effective dose is reached by upward titration over a period of approximately three days. The effective dose of gabapentin in children aged 6 years and older is 25 to 35 mg/kg/day. Dosages up to 50 mg/kg/day have been well tolerated in a long-term clinical study. The total daily dose should be divided in three single doses, the maximum time interval between doses should not exceed 12 hours. It is not necessary to monitor gabapentin plasma concentrations to optimize gabapentin therapy. Further, gabapentin may be used in combination with other antiepileptic medicinal products without concern for alteration of the plasma concentrations of gabapentin or serum concentrations of other antiepileptic.
Neuropathic Pain in Adults: The starting dose is 900 mg/day given as three equally divided doses and increased, if necessary, based on response, up to  maximum dose of 3600 mg/day. Therapy should be initiated by titrating the dose as described in Table 1.
Dosage Adjustment in Impaired Renal Function for Patients with Neuropathic Pain or Epilepsy: Dosage adjustment is recommended in patients with compromised renal function as described in Table 2 and/or those undergoing hemodialysis. (See Table 2.)

Click on icon to see table/diagram/image

Dosage Adjustments in Patients Undergoing Haemodialysis: For patients undergoing haemodialysis who have never received gabapentin, a loading dose of 300 to 400 mg, then 200 to 300 mg of gabapentin following each 4 hours of haemodialysis.
Overdosage
Acute, life-threatening toxicity has not been observed with gabapentin overdoses of up to 49 grams. Symptoms of the overdoses included dizziness, double vision, slurred speech, drowsiness, lethargy and mild diarrhoea. All patients recovered fully with supportive care. Reduced absorption of gabapentin at higher doses may limit drug absorption at the time of overdosing and, hence, minimise toxicity from overdoses. Overdoses of gabapentin, particularly in combination with other CNS depressant medications, may result in coma.
Although gabapentin can be removed by haemodialysis, based on prior experience it is not usually required. However, in patients with severe renal impairment, haemodialysis may be indicated.
An oral lethal dose of gabapentin was not identified in mice and rats given doses as high as 8000 mg/kg. Signs of acute toxicity in animals included ataxia, laboured breathing, ptosis, hypoactivity, or excitation.
Contraindications
Gabapentin is contraindicated in patients who are hypersensitive to gabapentin.
Special Precautions
General: Although there is no evidence of rebound seizures with gabapentin abrupt withdrawal of anticonvulsants in epileptic patients may precipitate status epilepticus.
Gabapentin is not generally considered effective in the treatment of absence seizures.
Patients who require concomitant treatment with morphine may experience increases in gabapentin concentrations. Patients should be carefully observed for signs of CNS depression, such as somnolence, and the dose of gabapentin or morphine should be reduced appropriately.
Gabapentin may impair ability to drive a car or operate potentially dangerous machinery. Until it is known that this medication does not affect the ability to engage in these activities, do not drive a car or operate potentially dangerous machinery.
Suicidal ideation and behaviour have been reported in patients treated with anti-epileptic agents in several indications. A meta-analysis of randomised placebo controlled trials of anti-epileptic drugs has also shown a small increased risk of suicidal ideation and behaviour. The mechanism of this risk is not known and the available data do not exclude the possibility of an increased risk for gabapentin.
Therefore patients should be monitored for signs of suicidal ideation and behaviours and appropriate treatment should be considered. Patients (and caregivers of patients) should be advised to seek medical advice should signs of suicidal ideation or behaviour emerge.
Use In Pregnancy & Lactation
Use During Pregnancy: There are no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, this drug should be used during pregnancy only if the potential benefit to the patient justifies the potential risk to the fetus.
Use During Lactation: Gabapentin is excreted in human milk. Because the effect on the nursing infant is unknown, caution should be exercised when gabapentin is administered to a nursing mother. Inform the physician if the patient is breast feeding an infant.
Gapabentin should be used in nursing mothers only if the benefits clearly outweigh the risks.
Adverse Reactions
Adverse effects from gabapentin therapy are generally mild to moderate in severity, and tend to diminish with continued use.
Those indicating need for medical attention: Incidence more frequent: Ataxia (Clumsiness and unsteadiness) - may be dose-related; nystagmus (continuous, uncontrolled, back-and-forth and/or rolling eye movements).
Incidence less frequent: Amnesia (loss of memory); depression, irritability, or other mood or mental changes.
Incidence rare: Leukopenia (usually asymptomatic; rarely, fever or chills; cough or hoarseness; lower back or side pain; painful or difficult urination).
Those indicating need for medical attention only if they continue or are bothersome: Incidence more frequent: Dizziness; fatigue (unusual tiredness or weakness); myalgia (muscle ache or pain); peripheral edema (swelling of hands, feet, or lower legs); somnolence (drowsiness) - may be dose-related; tremor (trembling or shaking); vision abnormalities, including blurred vision and diplopia (double vision).
Incidence less frequent or rare: Asthenia (weakness or loss of strength); back pain; dryness of mouth or throat; dysarthria (slurred speech); frequent urination; gastrointestinal effects, including constipation, diarrhea, dyspepsia (indigestion); nausea, and vomiting; headache; hypotension (low blood pressure); impotence (decrease in sexual desire or ability); insomnia (trouble in sleeping); rhinitis (runny nose); tinnitus (noise in ears); trouble in thinking; twitching; weight gain.
Drug Interactions
No interaction between gabapentin and phenobarbital, phenytoin, valproic acid, or carbamazepine has been observed.
Gabapentin steady-state pharmacokinetics are similar for healthy subjects and patients with epilepsy receiving these anti-epileptic agents.
Coadministration of gabapentin with oral contraceptives containing norethindrone and/or ethinyl estradiol, does not influence the steady-state pharmacokinetics of either component.
Coadministration of gabapentin with antacids containing aluminium and magnesium, reduces gabapentin bioavailability up to 24%. It is recommended that gabapentin be taken at the earliest two hours following antacid administration.
Renal excretion of gabapentin is unaltered by probenecid.
A slight decrease in renal excretion of gabapentin that is observed when it is coadministered with cimetidine is not expected to be of clinical importance.
Storage
Store below 25°C. Protect from moisture.
ATC Classification
N03AX12 - gabapentin ; Belongs to the class of other antiepileptics.
Presentation/Packing
Cap 300 mg (light yellow opaque with 'GP300' printed on one end and 'hovid' on the other end of the size 1 capsule filled with white to off-white powder) x 100's.
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