INDICATIONS     CONTRA-INDICATIONS     DOSAGE     SIDE-EFFECTS     PREGNANCY     OVERDOSE     IDENTIFICATION     PATIENT INFORMATION

Logo EPLEPTIN 100 mg (capsules)
EPLEPTIN 300 mg (capsules)
EPLEPTIN 400 mg (capsules)

SCHEDULING STATUS:
S3

PROPRIETARY NAME
(and dosage form):

EPLEPTIN 100 mg (capsules)
EPLEPTIN 300 mg (capsules)
EPLEPTIN 400 mg (capsules)

COMPOSITION:
EPLEPTIN 100 mg: Each capsule contains 100 mg
gabapentin.
EPLEPTIN 300 mg: Each capsule contains 300 mg gabapentin.
EPLEPTIN 400 mg: Each capsule contains 400 mg gabapentin.

PHARMACOLOGICAL CLASSIFICATION
A 2.5 Central nervous system depressants. Anticonvulsants, including anti-epileptics.

PHARMACOLOGICAL ACTION
Pharmacodynamics
Gabapentin is an analogue of the neurotransmitter GABA (gamma-aminobutyric acid). It is neither a GABA agonist nor antagonist and its mechanism of action, as an anti-epileptic drug remains unclear.

Pharmacokinetics
Gabapentin is rapidly absorbed after oral administration in part by the L-amino acid transport system, which is a carrier-mediated, saturable transport system. As the dose increases,
bioavailability decreases.
Peak plasma concentrations are reached within 2 to 3 hours after administration. Absorption is unaffected by food and plasma protein binding is very low.
Absolute bioavailability of 300 mg and 400 mg gabapentin capsules is approximately 55%. Gabapentin elimination parameters are independent of dose.
Gabapentin has an apparent volume of distribution of approximately 50 to 60 L. Gabapentin penetrates the blood-brain barrier, yielding cerebrospinal fluid (CSF) concentrations in the range of 7 to 35% of corresponding steady-state plasma trough concentrations in patients with epilepsy.
Gabapentin is not metabolized and is eliminated solely by renal excretion. Gabapentin does not induce hepatic mixed-function oxidase enzymes responsible for drug metabolism.
In elderly patients with decrease in renal function, plasma clearance is decreased and elimination half-life is increased. Gabapentin elimination-rate constant, plasma clearance, and renal clearance are directly proportional to creatinine clearance.
Gabapentin is removed from plasma by haemodialysis.

INDICATIONS
EPLEPTIN is indicated:
as an adjunct to other standard anticonvulsant medications in patients who have not achieved adequate seizure control with these agents used alone or in combination.
in controlling both simple and complex partial seizures with or without secondarily generalized tonic clonic seizures.

CONTRA-INDICATIONS
Hypersensitivity to gabapentin or the product’s excipients.
Safety and efficacy in children under 12 years has not been established.
Safety and efficacy in pregnancy and lactation has not been established.

WARNINGS
Patients should be warned that EPLEPTIN may affect their alertness and that caution should be exercised when driving a vehicle, operating machinery or performing hazardous tasks. The concomitant use of alcohol will intensity these effects.

INTERACTIONS
There is no interaction between EPLEPTIN, phenobarbitone, phenytoin, valproic acid, carbamazepine or carbamazepine-10,11-epoxide.
Co-administration of EPLEPTIN with oral contraceptives, containing norethindrone and/or ethinyl estradiol, does not influence the steady-state plasma concentrations of either component.
Concomitant use of EPLEPTIN with a magnesium- and aluminium-containing antacid reduces gabapentin bioavailability by approximately 20%. It is recommended that gabapentin be taken about two hours following antacid administration.
Concurrent use of EPLEPTIN with alcohol and other CNS depressants may increase the CNS depressant effects.
False positive tests for proteinuria may occur with Ames Multistix-SG.

PREGNANCY AND LACTATION
Safety in pregnancy and lactation has not been established.

DOSAGE AND DIRECTIONS FOR USE
Adults and children over 12 years
Initially 300 mg three times a day. The dosage may be gradually increased based on the clinical response. Dosages of 900 to 1800 mg per day taken in three divided doses with not more than 12 hours between doses are effective for most patients. Dosages of up to 3600 mg in divided doses three times a day for short periods have been well tolerated.
Since titration to an effective dose can progress rapidly, this may be accomplished in as few as three days using one of the following approaches:
900 mg/day
Day 1: 1 x 100 mg, three times a day
        or 1 x 300 mg, once a day.
Day 2: 2 x 100 mg, three times a day
        or 1 x 300 mg twice a day.
Day 3: 1 x 300 mg, three times a day
        or 1 x 300 mg, three times a day.
1200 mg/day
Day 1: 2 x 100 mg, three times a day
  or 1 x 400 mg, once a day.
Day 2: 3 x 100 mg, three times a day
  or 1 x 400 mg twice a day.
Day 3: 1 x 400 mg, three times a day
  or 1 x 400 mg, three times a day.

Children under 12 years
Safety and effectiveness in children under 12 years have not been established.

Elderly patients
Elderly patients may require dosage adjustment because of decrease in renal function with age. Dosage adjustment may be made on clinical response.

For patients with impaired renal function or those undergoing haemodialysis the following maintenance dosage regimen are recommended:
Renal Function Total Daily Dose Regimen
Creatinine Clearance Dose (mg)
(ml per minute) (mg/day)  
>60 1200 400 three times a day
30-60 600 300 two times a day
15-30 300 300 once a day
<15 150 300 once every other day
Haemodialysis a - 200 to 300 b

a Loading dose of 300 to 400 mg
b Maintenance dose of 200 to 300 mg gabapentin
Following each 4 hours of haemodialysis

Gabapentin plasma concentrations need not to be monitored to optimize EPLEPTIN therapy.
EPLEPTIN may be used as adjunct with phenobarbital, phenytoin, valproic acid and carbamazepine without any alteration of the plasma concentrations or serum concentrations of gabapentin or the other anti-epileptic agents.
Withdrawal of EPLEPTIN therapy or the addition of another medication to the treatment should be done gradually over a minimum of one week.

SIDE EFFECTS AND SPECIAL PRECAUTIONS
Side-effects
Nervous system disorders
Frequent: Fatigue, somnolence, dizziness, ataxia, tremor, vertigo.
Less frequent: Headache, dysarthria, amnesia, confusion, insomnia, twitching, abnormal co-ordination, paraesthesia, nervousness.
Gastro-intestinal disorders
Less frequent: Nausea and vomiting, dyspepsia, abdominal pain, dryness of mouth or throat, constipation, dental abnormalities, diarrhoea.
Eye disorders
Frequent: Diplopia, amblyopia, nystagmus.
Respiratory system
Less frequent: Rhinitis, pharyngitis, coughing, respiratory tract infection.
Skin and subcutaneous tissue disorders
Less frequent: Rash, pruritus, abrasion, acne, maculopapular rash.
Psychiatric disorders
Frequent: Depression, emotional lability.
Less frequent: Thinking abnormal.
Reproductive system disorders
Less frequent: Impotence.
Musculoskeletal and bone disorders
Frequent: Myalgia.
Less frequent: Back pain, fracture.
Vascular disorders
Frequent: Peripheral oedema.
Less frequent: Vasodilation.
Blood and lymphatic system disorders
Less frequent: Leucopenia, purpura, white blood cells decreased.
Infections and infestations
Less frequent: Viral infection.
Metabolism and nutrition disorders
Less frequent: Increased appetite resulting in weight gain.
General disorders
Less frequent: Fever.

Special precautions
EPLEPTIN should be used with caution in patients with a history of psychotic illness. It should also be used with caution in renal impairment. See table for dosage guidelines in renal impairment and haemodialysis.
Abrupt withdrawal of EPLEPTIN in epileptic patients may precipitate status epilepticus. Should it be required to reduce the dosage, discontinue the treatment or substitute with another anticonvulsant medicine, it should be done gradually over a minimum of one week.

KNOWN SYMPTOMS OF OVERDOSAGE AND PARTICULARS OF ITS TREATMENT
Symptoms of overdose include dizziness, double vision, slurred speech, drowsiness, lethargy and mild diarrhoea. See “SIDE-EFFECTS AND SPECIAL PRECAUTIONS”. Treatment is symptomatic and supportive. Haemodialysis has been shown to be effective in eliminating EPLEPTIN and may be indicated in patients with renal impairment.
Reduced absorption of EPLEPTIN at higher doses may limit drug absorption and hence minimize toxicity at the time of overdosing.

IDENTIFICATION
EPLEPTIN 100 mg: Hard gelatine capsules size ‘3’white cap and white body with “137” imprinted in black on cap and body, containing white crystalline powder.
EPLEPTIN 300 mg: Hard gelatine capsules size ‘1’yellow cap and yellow body with “138”imprinted in black on cap and body, containing white crystalline powder.
EPLEPTIN 400 mg: Hard gelatine capsules size ‘0’orange cap and orange body with “139”imprinted in black on cap and body, containing white crystalline powder.

PRESENTATION
EPLEPTIN 100 mg are packed into 75 cc white round HDPE bottles with 33 mm polypropylene white ribbed caps. 100 capsules per bottle.
EPLEPTIN 300 mg are packed into 150 cc white round HDPE bottles with 38 mm polypropylene white ribbed caps. 100 capsules per bottle.
EPLEPTIN 400 mg are packed into 150 cc white round HDPE bottles with 38 mm polypropylene white ribbed caps. 100 capsules per bottle.

STORAGE INSTRUCTIONS
Store in a cool (below 25°C) dry place.
KEEP OUT OF REACH OF CHILDREN.

REGISTRATION NUMBER
EPLEPTIN 100 mg (capsules): A40/2.5/0158
EPLEPTIN 300 mg (capsules): A40/2.5/0159
EPLEPTIN 400 mg (capsules): A40/2.5/0160

NAME AND BUSINESS ADDRESS OF THE HOLDER OF THE CERTIFICATE OF REGISTRATION
Pharmaplan (Pty) Ltd.
106 16th Road
Midrand

DATE OF PUBLICATION OF THE PACKAGE INSERT
4 October 2005

New addition to this site: December 2006
Source: Pharmaceutical Industry

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