Maynmar Product

Gabafast Capsule

Gabafast Capsule

Why you have been prescribed this medicine?

You have been prescribed this medicine if you have any of the following:

Epilepsy
Gabafast 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.
It is also indicated as monotherapy in the treatment of partial seizures with and without secondary generalization in adults and adolescents aged 12 years and above.

Treatment of peripheral neuropathic pain
Gabafast is indicated for the treatment of peripheral neuropathic pain such as painful diabetic neuropathy and post-herpetic neuralgia in adults..

When you should consult your doctor?

You should consult your doctor if you experience any of the following:

You should consult your doctor if you experience any of the following:
The adverse reactions observed during clinical studies conducted in epilepsy (adjunctive and monotherapy) and neuropathic pain have been provided in a single list below by class and frequency (very common (≥ 1/10); common (≥ 1/100 to< 1/10); uncommon (≥ 1/1000 to < 1/100); rare (≥ 1/10000 to < 1/1000); very rare (< 1/10000).
Infections and infestations
Very common:  Viral infection
Common: Pneumonia, respiratory infection, urinary tract infection, infection, otitis media
Blood and the lymphatic system disorders
Common: Leucopenia
Not known: Thrombocytopenia
Immune system disorders
Uncommon: Allergic reactions (e.g. urticaria)
Not known: Hypersensitivity syndrome, a systemic reaction with a variable presentation that can include fever, rash, hepatitis, lymphadenopathy, eosinophilia, and sometimes other signs and symptoms.
Metabolism and nutrition disorders
Common: Anorexia, increased appetite
Uncommon: Hyperglycemia (most often observed in patients with diabetes)
Rare: Hypoglycaemia (most often observed in patients with diabetes)
Not known: Hyponatraemia
Psychiatric disorders
Common: Hostility, confusion and emotional lability, depression, anxiety, nervousness, thinking abnormal.
Not known: HHallucinations
Nervous system disorders
Very common: Somnolence, dizziness, ataxia
Common: Convulsions, hyperkinesias, dysarthria, amnesia, tremor, insomnia, headache, sensations such as paresthesia, hypaesthesia, coordination abnormal, nystagmus, increased, decreased, or absent reflexes.
Uncommon: Hypokinesia, mental impairment
Rare: Loss of consciousness                              
Not known: Other movement disorders (e.g. choreoathetosis, dyskinesia, dystonia)
Eye disorders
Common: Visual disturbances such as amblyopia, diplopia
Ear and Labyrinth disorders
Common: Vertigo
Not known: Tinnitus
Cardiac disorders
Uncommon: Palpitations
Vascular disorders
Common: Hypertension, vasodilatation
Respiratory, thoracic and mediastinal disorders
Common:  Dyspnoea, bronchitis, pharyngitis, cough, rhinitis
Gastrointestinal disorders
Common: Vomiting, nausea, dental abnormalities, gingivitis, diarrhoea, abdominal pain, dyspepsia, constipation, dry mouth or throat, flatulence
Not known: Pancreatitis
Hepatobiliary disorders
Not known: Hepatitis, jaundice
Skin and subcutaneous tissue disorders
Common: Facial oedema, purpura most often described as bruises resulting from physical trauma, rash, pruritus, acne.
Not known: Stevens-Johnson syndrome, angioedema, erythema multiforme, alopecia, drug rash with eosinophilia and systemic symptoms.
Musculoskeletal and connective tissue disorders
Common: Arthralgia, myalgia, back pain, twitching
Uncommon: Rhabdomyolysis, myoclonus
Renal and urinary disorder
Not known: Acute renal failure, incontinence
Reproductive system and breast disorders
Common:  Impotence
Not known: Breast hypertrophy, gynaecomastia, sexual dysfunction (including changes in libido, ejaculation disorders and anorgasmia).
General disorders and administration site conditions
Very common: Fatigue, fever
Common: Peripheral oedema, abnormal gait, asthenia, pain, malaise, flu syndrome
Uncommon: Generalized oedema
Not known: Withdrawal reactions (mostly anxiety, insomnia, nausea, pains, sweating), chest pain. Sudden unexplained deaths have been reported where a causal relationship to treatment with gabapentin has not been established.
Investigations
Common: WBC (white blood cell count) decreased, weight gain
Uncommon: Elevated liver function tests SGOT (AST), SGPT (ALT) and bilirubin
Not known: Blood creatine phosphokinase increased
Injury and poisoning
Common: Accidental injury, fracture, abrasion
Uncommon: Fall

Under treatment with gabapentin cases of acute pancreatitis were reported. Causality with gabapentin is unclear.
In patients on haemodialysis due to end-stage renal failure, myopathy with elevated creatine kinase levels has been reported.
Respiratory tract infections, otitis media, convulsions and bronchitis were reported only in clinical studies in children. Additionally, in clinical studies in children, aggressive behaviour and hyperkinesias were reported commonly.


What to do if you miss a dose?

If it is almost time for your next dose, skip the dose you missed and take your next dose when you are meant to. Otherwise take it as soon as you remember and then go back to taking it as you would normally.

Things you MUST NOT DO while on this medicine?

Discontinuation of gabapentin
In accordance with current clinical practice, if gabapentin has to be discontinued it is recommended this should be done gradually over a minimum of 1 week independent of the indication.
Interactions
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.

What to do if you accidentally take too much (overdose) of the medicine?

Acute, life-threatening toxicity has not been observed with gabapentin overdoses of up to    49 g. 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.

Is it safe in pregnancy and breast-feeding?

Risk related to gabapentin
There are no adequate data from the use of gabapentin in pregnant women.
Studies in animals have shown reproductive toxicity. The potential risk for humans is unknown. Gabapentin should not be used during pregnancy unless the potential benefit to the mother clearly outweighs the potential risk to the foetus.
No definite conclusion can be made as to whether gabapentin is associated with an increased risk of congenital malformations when taken during pregnancy, because of epilepsy itself and the presence of concomitant antiepileptic medicinal products during each reported pregnancy.

Breast-feeding
Gabapentin is excreted in human milk. Because the effect on the breast-fed infant is unknown, caution should be exercised when gabapentin is administered to a breast-feeding mother. Gabapentin should be used in breast-feeding mothers only if the benefits clearly outweigh the risks.

Storage Conditions:

Store below 30°C.
Keep all medicines out of reach of children.

Drug Description

Drug description
            General physico-chemical properties
Hard gelatin capsule of size “1” with red coloured cap & white coloured body containing white to off white powder.

Composition
Each hard gelatin capsule contains:
Gabapentin USP…………… 300 mg
Excipients: Mannitol SD 200, maize starch, magnesium stearate, purified talc, colloidal silicon dioxide, empty hard gelatin capsule shell size 1.

Indications and dosage.

INDICATIONS:
Epilepsy
Gabafast 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.
It is also indicated as monotherapy in the treatment of partial seizures with and without secondary generalization in adults and adolescents aged 12 years and above.

Treatment of peripheral neuropathic pain
Gabafast is indicated for the treatment of peripheral neuropathic pain such as painful diabetic neuropathy and post-herpetic neuralgia in adults.

DOSAGE AND MODE OF ADMINISTRATION
For all indications a titration scheme for the initiation of therapy is described in the dosing chart given below which is recommended for adults and adolescents aged 12 years and above. Dosing instructions for children under 12 years of age are provided under a separate sub-heading later in this section.

Dosing chart- initial titration
Day 1: 300 mg once a day
Day 2: 300 mg two times a day
Day 3: 300 mg three times a day

Discontinuation of gabapentin
In accordance with current clinical practice, 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 dosing chart 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.

Children 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 medicinal products.

Peripheral neuropathic pain
Adults
The therapy may be initiated by titrating the dose as described in the dosing chart above. Alternatively, the starting dose is 900 mg/day given as three equally divided doses. 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.
In the treatment of peripheral neuropathic pain such as painful diabetic neuropathy and post-herpetic neuralgia, efficacy and safety have not been examined in clinical studies for treatment periods longer than 5 months. If a patient requires dosing longer than 5 months for the treatment of peripheral neuropathic pain, the treating physician should assess the patient's clinical status and determine the need for additional therapy.

Instruction for all areas of indication
In patients with poor general health, i.e., low body weight, after organ transplantation etc., the dose should be titrated more slowly, either by using smaller dosage strengths or longer intervals between dosage increases.

Use in elderly patients (over 65 years of age)
Elderly patients may require dosage adjustment because of declining renal function with age (shown below in dosage of gabapentin in adults based on renal function). Somnolence, peripheral oedema and asthenia may be more frequent in elderly patients.

Use in patients with renal impairment
Dosage adjustment is recommended in patients with compromised renal function described in dosage of gabapentin in adults based on renal function or those undergoing haemodialysis. Gabapentin 100 mg capsules can be used to follow dosing recommendations for patients with renal insufficiency.

Dosage of gabapentin in adults based on renal function
Creatinine Clearance (ml/min): ≥ 80
Total Daily Dosea (mg/day): 900-3600

Creatinine Clearance (ml/min): 50-79
Total Daily Dosea (mg/day): 600-1800

Creatinine Clearance (ml/min): 30- 49
Total Daily Dosea (mg/day): 300-900

Creatinine Clearance (ml/min): 15- 29
Total Daily Dosea (mg/day): 150b- 600

Creatinine Clearance (ml/min): < 15c
Total Daily Dosea (mg/day): 150b- 300

a Total daily dose should be administered as three divided doses. Reduced dosages are for patients with renal impairment (creatinine clearance < 79 ml/min).
b To be administered as 300 mg every other day.
c For patients with creatinine clearance <15 ml/min, the daily dose should be reduced in proportion to creatinine clearance (e.g., patients with a creatinine clearance of 7.5 ml/min should receive one-half the daily dose that patients with a creatinine clearance of 15 ml/min receive).

Use in patients undergoing haemodialysis
For anuric 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, is recommended. On dialysis-free days, there should be no treatment with gabapentin.
For renally impaired patients undergoing haemodialysis, the maintenance dose of gabapentin should be based on the dosing recommendations provided above in dosage of gabapentin in adults based on renal function. In addition to the maintenance dose, an additional 200 to 300 mg dose following each 4-hour haemodialysis treatment is recommended.

Method of administration:oral
Gabafast can be given with or without food and should be swallowed whole with sufficient fluid- intake (e.g. a glass of water).

Side effects and drug interactions.

  Adverse reactions:
The adverse reactions observed during clinical studies conducted in epilepsy (adjunctive and monotherapy) and neuropathic pain have been provided in a single list below by class and frequency (very common (≥ 1/10); common (≥ 1/100 to< 1/10); uncommon (≥ 1/1000 to < 1/100); rare (≥ 1/10000 to < 1/1000); very rare (< 1/10000).
Infections and infestations
Very common:  Viral infection
Common: Pneumonia, respiratory infection, urinary tract infection, infection, otitis media
Blood and the lymphatic system disorders
Common: Leucopenia
Not known: Thrombocytopenia
Immune system disorders
Uncommon: Allergic reactions (e.g. urticaria)
Not known: Hypersensitivity syndrome, a systemic reaction with a variable presentation that can include fever, rash, hepatitis, lymphadenopathy, eosinophilia, and sometimes other signs and symptoms.
Metabolism and nutrition disorders
Common: Anorexia, increased appetite
Uncommon: Hyperglycemia (most often observed in patients with diabetes)
Rare: Hypoglycaemia (most often observed in patients with diabetes)
Not known: Hyponatraemia
Psychiatric disorders
Common: Hostility, confusion and emotional lability, depression, anxiety, nervousness, thinking abnormal.
Not known: HHallucinations
Nervous system disorders
Very common: Somnolence, dizziness, ataxia
Common: Convulsions, hyperkinesias, dysarthria, amnesia, tremor, insomnia, headache, sensations such as paresthesia, hypaesthesia, coordination abnormal, nystagmus, increased, decreased, or absent reflexes.
Uncommon: Hypokinesia, mental impairment
Rare: Loss of consciousness                              
Not known: Other movement disorders (e.g. choreoathetosis, dyskinesia, dystonia)
Eye disorders
Common: Visual disturbances such as amblyopia, diplopia
Ear and Labyrinth disorders
Common: Vertigo
Not known: Tinnitus
Cardiac disorders
Uncommon: Palpitations
Vascular disorders
Common: Hypertension, vasodilatation
Respiratory, thoracic and mediastinal disorders
Common:  Dyspnoea, bronchitis, pharyngitis, cough, rhinitis
Gastrointestinal disorders
Common: Vomiting, nausea, dental abnormalities, gingivitis, diarrhoea, abdominal pain, dyspepsia, constipation, dry mouth or throat, flatulence
Not known: Pancreatitis
Hepatobiliary disorders
Not known: Hepatitis, jaundice
Skin and subcutaneous tissue disorders
Common: Facial oedema, purpura most often described as bruises resulting from physical trauma, rash, pruritus, acne.
Not known: Stevens-Johnson syndrome, angioedema, erythema multiforme, alopecia, drug rash with eosinophilia and systemic symptoms.
Musculoskeletal and connective tissue disorders
Common: Arthralgia, myalgia, back pain, twitching
Uncommon: Rhabdomyolysis, myoclonus
Renal and urinary disorder
Not known: Acute renal failure, incontinence
Reproductive system and breast disorders
Common:  Impotence
Not known: Breast hypertrophy, gynaecomastia, sexual dysfunction (including changes in libido, ejaculation disorders and anorgasmia).
General disorders and administration site conditions
Very common: Fatigue, fever
Common: Peripheral oedema, abnormal gait, asthenia, pain, malaise, flu syndrome
Uncommon: Generalized oedema
Not known: Withdrawal reactions (mostly anxiety, insomnia, nausea, pains, sweating), chest pain. Sudden unexplained deaths have been reported where a causal relationship to treatment with gabapentin has not been established.
Investigations
Common: WBC (white blood cell count) decreased, weight gain
Uncommon: Elevated liver function tests SGOT (AST), SGPT (ALT) and bilirubin
Not known: Blood creatine phosphokinase increased
Injury and poisoning
Common: Accidental injury, fracture, abrasion
Uncommon: Fall

Under treatment with gabapentin cases of acute pancreatitis were reported. Causality with gabapentin is unclear.
In patients on haemodialysis due to end-stage renal failure, myopathy with elevated creatine kinase levels has been reported.
Respiratory tract infections, otitis media, convulsions and bronchitis were reported only in clinical studies in children. Additionally, in clinical studies in children, aggressive behaviour and hyperkinesias were reported commonly.

           Drug interactions
There are spontaneous and literature case reports of respiratory depression and/or sedation associated with gabapentin and opioid use. In some of these reports, the authors considered this a particular concern with the combination of gabapentin and opioids, especially in elderly patients.
Patients who require concomitant treatment with opioids should be carefully observed for signs of CNS depression, such as somnolence, sedation and respiratory depression and the dose of gabapentin or opioid should be reduced appropriately.
No interaction between gabapentin and phenobarbital, phenytoin, valproic acid or carbamazepine has been observed.
Gabapentin steady-state pharmacokinetics is similar for healthy subjects and patients with epilepsy receiving these antiepileptic 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.

Warnings and precautions

• Suicidal ideation and behaviour
Suicidal ideation and behaviour have been reported in patients treated with antiepileptic agents in several indications. A meta-analysis of randomized placebo controlled trials of antiepileptic 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.

• Acute pancreatitis
If a patient develops acute pancreatitis under treatment with gabapentin, discontinuation of gabapentin should be considered.

• Seizures
Although there is no evidence of rebound seizures with gabapentin, abrupt withdrawal of anticonvulsants in epileptic patients may precipitate status epilepticus.
As with other antiepileptic medicinal products, some patients may experience an increase in seizure frequency or the onset of new types of seizures with gabapentin.
As with other antiepileptics, attempts to withdraw concomitant antiepileptics in treatment refractive patients on more than one antiepileptic, in order to reach gabapentin monotherapy have a low success rate.
Gabapentin is not considered effective against primary generalized seizures such as absences and may aggravate these seizures in some patients. Therefore, gabapentin should be used with caution in patients with mixed seizures including absences.
Gabapentin treatment has been associated with dizziness and somnolence, which could increase the occurrence of accidental injury (fall). There have also been postmarketing reports of confusion, loss of consciousness and mental impairment. Therefore, patients should be advised to exercise caution until they are familiar with the potential effects of the medication.

• Concomitant use with opioids
Patients who require concomitant treatment with opioids should be carefully observed for signs of central nervous system (CNS) depression, such as somnolence, sedation and respiratory depression. Patients who use gabapentin and morphine concomitantly may experience increases in gabapentin concentrations. The dose of gabapentin or opioids should be reduced appropriately.

• Use in elderly patients (over 65 years of age)
No systematic studies in patients 65 years or older have been conducted with gabapentin. In one double blind study in patients with neuropathic pain, somnolence, peripheral oedema and asthenia occurred in a somewhat higher percentage in patients aged 65 years or above, than in younger patients. Apart from these findings, clinical investigations in this age group do not indicate an adverse event profile different from that observed in younger patients.

• Paediatric population
The effects of long-term (greater than 36 weeks) gabapentin therapy on learning, intelligence, and development in children and adolescents have not been adequately studied. The benefits of prolonged therapy must therefore be weighed against the potential risks of such therapy.

• Abuse and Dependence
Cases of abuse and dependence have been reported in the post-marketing database. Carefully evaluate patients for a history of drug abuse and observe them for possible signs of gabapentin abuse e.g. drug-seeking behaviour, dose escalation, development of tolerance.

• Drug Rash with Eosinophilia and Systemic Symptoms (DRESS)
Severe, life-threatening, systemic hypersensitivity reactions such as Drug rash with eosinophilia and systemic symptoms (DRESS) have been reported in patients taking antiepileptic drugs including gabapentin.
It is important to note that early manifestations of hypersensitivity, such as fever or lymphadenopathy, may be present even though rash is not evident. If such signs or symptoms are present, the patient should be evaluated immediately. Gabapentin should be discontinued if an alternative etiology for the signs or symptoms cannot be established.

• Laboratory tests
False positive readings may be obtained in the semi-quantitative determination of total urine protein by dipstick tests. It is therefore recommended to verify such a positive dipstick test result by methods based on a different analytical principle such as the Biuret method, turbidimetric or dye-binding methods, or to use these alternative methods from the beginning.


Overdosage and Contraindications

Overdosage:
Acute, life-threatening toxicity has not been observed with gabapentin overdoses of up to    49 g. 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
Hypersensitivity to gabapentin or any of the other ingredients.

 

Clinical pharmacology.

PHARMACOLOGICAL PROPERTIES
Pharmacodynamic properties
Pharmacotherapeutic Group: Other antiepileptics
ATC code: N03AX12

Gabapentin readily enters the brain and prevents seizures in a number of animal models of epilepsy. Gabapentin does not possess affinity for either GABAA or GABAB receptor nor does it alter the metabolism of GABA. It does not bind to other neurotransmitter receptors of the brain and does not interact with sodium channels. Gabapentin binds with high affinity to the α2δ (alpha-2-delta) subunit of voltage-gated calcium channels and it is proposed that binding to the α2δ subunit may be involved in gabapentin's anti-seizure effects in animals. Broad panel screening does not suggest any other drug target other than α2δ.
Evidence from several pre-clinical models informs that the pharmacological activity of gabapentin may be mediated via binding to α2δ through a reduction in release of excitatory neurotransmitters in regions of the central nervous system. Such activity may underlie gabapentin's anti-seizure activity. The relevance of these actions of gabapentin to the anticonvulsant effects in humans remains to be established.
Gabapentin also displays efficacy in several pre-clinical animal pain models. Specific binding of gabapentin to the α2δ subunit is proposed to result in several different actions that may be responsible for analgesic activity in animal models. The analgesic activities of gabapentin may occur in the spinal cord as well as at higher brain centers through interactions with descending pain inhibitory pathways. The relevance of these pre-clinical properties to clinical action in humans is unknown.

Pharmacokinetic properties
Absorption
Following oral administration, peak plasma gabapentin concentrations are observed within 2 to 3 hours. Gabapentin bioavailability (fraction of dose absorbed) tends to decrease with increasing dose. Absolute bioavailability of a 300 mg capsule is approximately 60%. Food, including a high-fat diet, has no clinically significant effect on gabapentin pharmacokinetics.
Gabapentin pharmacokinetics is not affected by repeated administration. Although plasma gabapentin concentrations were generally between 2 μg/mL and 20 μg/mL in clinical studies, such concentrations were not predictive of safety or efficacy.

Distribution
Gabapentin is not bound to plasma proteins and has a volume of distribution equal to 57.7 liters. In patients with epilepsy, gabapentin concentrations in cerebrospinal fluid (CSF) are approximately 20% of corresponding steady-state trough plasma concentrations. Gabapentin is present in the breast milk of breast-feeding women.

Biotransformation
There is no evidence of gabapentin metabolism in humans. Gabapentin does not induce hepatic mixed function oxidase enzymes responsible for drug metabolism.

Elimination
Gabapentin is eliminated unchanged solely by renal excretion. The elimination half-life of gabapentin is independent of dose and averages 5 to 7 hours.
In elderly patients, and in patients with impaired renal function, gabapentin plasma clearance is reduced. Gabapentin elimination-rate constant, plasma clearance, and renal clearance are directly proportional to creatinine clearance.
Gabapentin is removed from plasma by haemodialysis. Dosage adjustment in patients with compromised renal function or undergoing haemodialysis is recommended.
Gabapentin pharmacokinetics in children was determined in 50 healthy subjects between the ages of 1 month and 12 years. In general, plasma gabapentin concentrations in children > 5 years of age are similar to those in adults when dosed on a mg/kg basis.
In a pharmacokinetic study in 24 healthy paediatric subjects aged between 1 month and 48 months, an approximately 30% lower exposure (AUC), lower Cmax and higher clearance per body weight have been observed in comparison to available reported data in children older than 5 years.

STORAGE CONDITION
Store below30°C.
Keep all medicines out of reach of children.

DOSAGE FORM AND PACKING AVAILABLE
PVC/PVDC/Alu blister pack of 10 hard gelatin capsules, 3 or 10 blisters are packed in a carton.

SHELF- LIFE
24 months

NAME AND ADDRESS OF MANUFACTURER
Kusum Healthcare Pvt. Ltd.
SP 289 (A), RIICO, Indl. Area,
Chopanki, Bhiwadi (Rajasthan), India

CERTIFICATES

KEEP IN TOUCH

Kusum Healthcare
D-158A, OKHLA,INDUSTRIAL AREA,
PHASE-I, NEW DELHI,
Pin 110020
INDIA
Tel: 011-41005147, 011-40514919
Fax: +91-11-40527575