Galepsi

Composition ;

Each capsule GALEPSI® contains Gabapentin 300 mg

 

Pharmacology :

Gabapentin is structurally binds to the neurotransmitter GABA (gamma – aminobutyric acid) but its mechanism is different from the drugs – other drugs that interact with GABA synapses including valproate, barbiturates, benzodiazepines, GABA transaminase inhibitors, GABA uptake inhibitors, GABA-agonist and prodrug GABA. In vitro Study using Gabapentin radiolabeled shows the presence of a bonding site in mouse brain tissue that includes neocortex and hippocampus that may be associated with anticonvulsant activity of gabapentin and its derivativ. Gabapentin at clinical concentrations does not bind to certain other drug or neurotransmitter receptors of the brain including GABAA, GABAB, benzodiazepine, glutamate, glycine, or receptor N – methyl – d – aspartate.

Gabapentin does not interact with Na channels and this is very different from phenytoin and carbamazepine. Gabapentin partially reduces responses glutamate agonist N – methyl – d – aspartate (NMDA) in some tests in vitro, but only at concentrations greater than 100 M, which was not achieved in vivo. Gabapentin slightly reduces the release of monoamine neurotransmitters in vitro. Giving Gabapentin in rats increases GABA turnover in some parts of the brain in the same way as sodium valproate but in different parts of the brain. The linkage between Gabapentin’s diverse work and its anticonvulsant effects continues to be developed. In animal experiments, Gabapentin immediately enters the brain tissue and prevents attacks from maximal electroshock, from chemical convulsant including synthetic GABA inhibitors and in genetically-acquired attacks.

 

Indication :

  • Epilepsy:

Gabapentin is indicated as adjunctive therapy in the treatment of partial attacks with or without secondary generalization in adults and children aged 3 years and over. The safety and effectiveness of additional therapy in pediatric patients under 3 years can not be determined

  • Neuropathic pain:
  • Gabapentin is indicated for the treatment of neuropathic pain in adults over 18 years of age. Safety and effectiveness in patients under 18 years can not be determine

 

Dosage :

Gabapentin is given orally with or without food.

If the doctor suggests dose reduction, discontinuation or replacement with other drugs, this should be done gradually for at least one week.

  • Epilepsy

Adult and over than 12 years old:

Effective dose range: 900 – 1800 mg / day. Treatment should be initiated by administering 300 mg (TID) on day 1 or with a titration dose such as:

 

Level Dose-Initial titration
Dosage Day 1 Day 2 Day 3
900 mg 300 mg QDa 300 mg BIDb 300 mg TIDc

QDa : once daily (at night)

BIDb : twice daily (in the morning and evening)

TIDc : three time daily (in the morning, afternoon, and evening)

 

After that the dosage can be increased to a maximum dose of 2400 mg / day divided into 3 doses. The dosing time should not exceed 12 hours to prevent a sudden attack.

 

Children 3 – 12 years old:

The initial dose should be within the range of 10 – 15 mg / kg / day administered in divided doses (three times daily) and the effective dose is achieved by increasing the dose within three days.

The effective dose of Gabapentin in pediatric patients> 5 years is 25 – 35 mg / kg / day administered in divided doses (three times daily).

Effective dose in pediatric patients 3 – 5 years is 40 mg / kg / day given in divided doses (three times a day), interval time may not exceed 12 hour.

 

  • Neurophatic pain:

Adult:

300 mg once daily on the first day, 300 mg twice daily on the second day and 300 mg three times daily on the third day. After that the dosage can be increased by adding 300 mg per day given in three divided doses up to a maximum dose of 1800 mg per day.

In patients with impaired renal function and hemodialysis, dose regulation is necessary. Treatment of doses in patient with impaired renal function with neuropathy or epilepsy:

 

Treatment doses of gabapentin in adult patients with impaired renal function
Creatinine Clearance (mL/minte) Total doses per day

Normal dosage
≥ 80 900 1200 2400
50-79 600 600 1200
30-49 300 300 600
15-29 150** 300 300
< 15 150** 150** 300

 

*Total doses daily should be given as a TID regimen. Dosage is applied for healing patients with normal renal function (creatinine clearance > 80 ml / minute), range between 900-2400 mg/day. Dose reduction was performed on patient with impaired renalfunction (creatinine clearance <79 ml / min).

** To be given 300 mg daily the next day.

 

  • Dose adjustment in patient undergoing hemodiálisis

In patients currently on treatment with Gabapentin, the recommended initial dose is 300-400 mg, followed by a dose of 200-300 mg of Gabapentin every 4 hours after hemodiálisis. On the day the patient does not undergo diálysis not allowed to undergo treatment with Gabapentin. If treatment with Gabapentin is discontinued and or undergo additional treatment with other anticonvulsant, this should be done gradually for at least 1 week.

  • How and when to give

Gabapentin capsules should be drunk with drinking water to taste. Giving can be done during or between meals, On giving three times a day, the interval of dosing between 2 doses can not be more than 12 hours. In the case of doses of Gabapentine (more than 12 hours after the last administration), Gabapentin dosage should be added after or without the Doctor’s guidance. In concomitant treatment with antacids containing magnesium or aluminum, Gabapentin should be administered at least 2 hours after administration of antacids. It aims to prevent the decline in Gabapentin bioavailability. Half time depends on clinical requirements. In the treatment of epilepsy, it is usually necessary long-term therapy. If therapy with oral gabapentin should be discontinued, dose reduced, or replaced with other drugs, should be done gradually at least 1 week, although there is no evidence of repetition of the incidence of attacks (an increase in the incidence of epilepsy abruptly after treatment is stopped). In the treatment of neuropari pain, efficacy and safety have not been tested in clinical trials for a treatment period longer than 5 months.

 

Presentation and Registration Number :

GALEPSI® Box, 3 strips @ 10 capsules; DKL0808014801A1

 

ON MEDICAL PRESCRIPTION ONLY

 

 

 

 

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