Gabix

Main information

  • Trade name:
  • Gabix 100mg Capsule
  • Dosage:
  • 100mg
  • Pharmaceutical form:
  • Capsule
  • Units in package:
  • Blister pack x 10's in a box
  • Medicine domain:
  • Humans
  • Medicine type:
  • Allopathic drug
  • Manufactured by:
  • Getz Pharma Pvt Ltd

Documents

Localization

  • Available in:
  • Gabix 100mg Capsule
    Philippines
  • Language:
  • English

Therapeutic information

  • Therapeutic area:
  • Anti-Convulsant
  • Therapeutic indications:
  • Various types of neuropathic pain in adults: Postherpetic neuralgia (PHN). Painful diabetic neuropathy. Trigeminal neuralgia. Central pain. Complex regional pain syndrome. Epilepsy: As adjunctive therapy in the treatment of partial seizures with and without secondary generalization in adults and children aged 6 years and above. As monotherapy in the treatment of partial seizures with and without secondary generalization in adults and adolescents aged 12 years and above.

Status

  • Source:
  • FDA - Food And Drug Administration - Philippines
  • Authorization number:
  • DR-XY34011
  • Authorization date:
  • 27-11-2017
  • Last update:
  • 26-01-2017

Summary of Product characteristics: dosage, interactions, side effects

DESCRIPTION

Gabapentin (GABIX

) is a new antiepileptic drug that is structurally similar

to the neurotransmitter gamma aminobutyric acid (GABA) and the

endogenous amino acid L-leucine. Chemically gabapentin is 1-(aminomethyl)

cyclohexaneacetic acid. Its molecular formula is C

The structural

formula is:

FORMULATION

Gabapentin (GABIX

) is available for oral administration as:

Gabapentin (GABIX

) Capsules 100mg

Each capsule contains:

Gabapentin …100mg

Gabapentin (GABIX

) Capsules 300mg

Each capsule contains:

Gabapentin …300mg

CLINICAL PHARMACOLOGY

Mechanism of Action

Gabapentin has proven affinity for special site in brain tissues such as

neocortex and hippocampus. Though exact mechanism of its CNS

depressant and anticonvulsant activity is not fully understood, it is thought

to be activated through peptide binding sites (receptor).

Pharmacokinetics

Absorption

Gabapentin is absorbed from the gastrointestinal tract by means of saturable

mechanism. Gabapentin bioavailability is not dose proportional i.e., as

dose is increased bioavailability is decreased. Absolute bioavailability of

300mg oral dose is approximately 60%. At doses of 300mg and 400mg,

gabapentin bioavailability was unchanged following multiple-dose

administration. Food has no effect on the rate and extent of absorption.

Distribution

Gabapentin circulates largely unbound (<3%) to plasma proteins. Gabapentin

is distributed into breast milk.

Metabolism and Elimination

Gabapentin is not appreciably metabolised and is eliminated from the

systemic circulation by renal excretion as unchanged drug. Elimination

half-life (t

) ranges from 5 to 7 hours and is unaltered by dose or following

multiple dosing. Gabapentin elimination rate constant, plasma clearance

and renal clearance are directly proportional to creatinine clearance.

Special Populations

Renal Insufficiency

The mean gabapentin half-life ranged from about 6.5 hours (patients with

creatinine clearance (CL

) >60mL/min) to 52 hours (CL

<30mL/min) and

gabapentin renal clearance ranged from 90mL/min (CL

>60mL/min) to

about 10mL/min (CL

<30mL/min). Gabapentin dosage should be adjusted

in patients with compromised renal function.

Patients on Hemodialysis

In anuric patients, the elimination half-life of gabapentin on a nondialysis

day was about 132 hours; during dialysis the apparent half-life was reduced

to 3.8 hours. Thus hemodialysis has a significant effect on gabapentin

elimination in anuric patients.

Gabapentin dosage should be adjusted in patients undergoing

hemodialysis.

Elderly Patients

The apparent oral clearance (CL/F) of gabapentin decreased as age

increased, from about 225mL/min in those under 30 years of age to about

125mL/min in those over 70 years of age. Reduction of gabapentin dose

may be required in patients who have age related compromised renal

function.

Drug-Drug Interactions

Naproxen: Co-administration of naproxen sodium (250mg) with gabapentin

(125mg) appears to increase the amount of gabapentin absorbed by 12%

to 15%. These doses are lower than the therapeutic doses for both drugs.

The magnitude of interaction within the recommended dose is not known.

Hydrocodone: Co-administration of gabapentin decreases hydrocodone

and AUC values in a dose-dependent manner relative to administration of

hydrocodone alone. Hydrocodone increases gabapentin AUC values by 14%.

Morphine: When 60mg of morphine administered 2 hours prior to 600mg

of gabapentin, the mean gabapentin AUC increased by 44% compared to

gabapentin administered without morphine.

THERAPEUTIC INDICATIONS

Gabapentin (GABIX

) is indicated:

For various types of neuropathic pain in adults:

Postherpetic neuralgia (PHN)

Peripheral diabetic neuropathies.

Trigeminal neuralgia.

As adjunctive therapy in the treatment of partial seizures with and

without secondary generalization in patients over 12 years of age with

epilepsy. Gabapentin (GABIX

) is also indicated as adjunctive therapy

in the treatment of partial seizures in pediatric patients age 6 – 12

years.

DOSAGE & ADMINISTRATION

Gabapentin (GABIX

) is given in titrations that lead to an effective dose.

Treatment progresses rapidly and can be accomplished over a few days.

The total dose should be divided into three doses given at intervals not

exceeding 12 hours. Gabapentin (GABIX

) may be given orally with or

without food.

Neuropathic Pain (Adults-over the age of 18)

The initial daily dose of Gabapentin (GABIX

) can be titrated as given in

the table below. Thereafter the dose maybe increased in increments of

300mg daily up to a maximum of 3600mg/day in three divided doses. It

is not necessary to divide the doses equally when titrating Gabapentin

(GABIX

Effectiveness as an adjunct therapy of neuropathic pain in pediatric

patients has not been established.

Epilepsy

Adults and children over 12 years of age:

Therapy may be initiated by administering 300mg three times a day on

day 1 or by titrating the dose as described in the following table.

Thereafter the dose maybe increased in increments of 300mg daily until

effective epileptic control is achieved, which is usually within the range of

900-1200mg daily. Higher doses up to a maximum of 2400mg daily may

be required in some patients.

Children aged 6 to 12 years:

The initial recommended dose of Gabapentin (GABIX

) is 25-35mg/kg/day

given in divided doses (3 times a day). Titration to an effective dose can

take place over 3 days by giving 10mg/kg/day on day 1, 20mg/kg/day on

day 2, and 25-35mg/kg/day on day 3.

The following table shows the recommended maintenance doses according

to the respective weight.

Special Populations

Renal Impaired Patients

A dosage adjustment is recommended in renally impaired patients with

neuropathic pain or epilepsy.

G a b a p e n t i n

Weight Range (Kg)

Daily Dose (mg/day)

26-36

37-50

1200

300mg

Once a day

300mg

Two times a day

300mg

Three times a day.

Day 1

Day 2

Day 3

300mg

Once a day

300mg

Two times a day

300mg

Three times a day.

Day 1

Day 2

Day 3

100mg and 300mg Capsule

Neuropathic Pain/

Anti-Convulsant

GABAPENTIN

a

Total daily dose should be administered as a tid regimen. Doses

used to treat patients with normal renal function (creatinine clearance

>80mL/min) range from 900 to 3600mg/day. Reduced dosages are

for patients with renal impairment (creatinine clearance <79mL/min)

b

To be administered on every other day.

Patients undergoing Hemodialysis

The recommended loading dose of Gabapentin (GABIX

) is 300-400mg

then 200-300mg following each 4 hours of hemodialysis.

ADVERSE REACTIONS

Neuropathic Pain

Common: Dizziness, somnolence.

Less Common: Diarrhea, dry mouth, peripheral oedema, weight gain,

abnormal gait, amnesia, ataxia, abnormal thinking, rash and amblyopia.

Rare: Accidental injury, asthenia, back pain, constipation, flatulence,

nausea, confusion, hypesthesia, vertigo, dyspnea and pharyngitis.

Epilepsy (Adults)

Common: Dizziness, somnolence.

Less Common: Ataxia, fatigue, nystagmus, tremor, diplopia, amblyopia,

abnormal vision, dysarthria, amnesia, asthenia, paraesthesia, arthralgia,

purpura, dyspepsia, anxiety, weight increase, urinary tract infection and

pharyngitis.

Uncommon: Leucopenia, nervousness, rhinitis and male sexual dysfunction

(impotence).

Rare: Urinary incontinence, pancreatitis, elevated liver function tests,

erythema multiforme and Stevens Johnson Syndrome, confusion,

depression, emotional lability, hostility, abnormal thinking and

psychoses/hallucinations, blood glucose fluctuations in patients with

diabetes, myalgia, headache, nausea and/or vomiting.

Epilepsy (Children 3-12 years)

Common: Emotional lability, nervousness and thinking abnormally. All

reports of these events were rated as mild or moderate and discontinuation

or dose reduction was infrequent.

Uncommon: Somnolence, fatigue, weight increase, hostility, emotional

lability, dizziness, hyperkinesia, nausea/vomiting, viral infection, fever,

bronchitis, respiratory infection.

Adverse events associated with both epilepsy and neuropathic pain include:

acute kidney failure, allergic reaction including urticaria, alopecia,

angioedema, chest pain, hepatitis, jaundice, movement disorders such as

choreoathetosis, dyskinesia and dystonia, palpitation, thrombocytopenia,

and tinnitus.

Adverse events following the abrupt discontinuation of gabapentin have

also been reported. The most frequently reported events are anxiety,

insomnia, nausea, pain and sweating.

CONTRAINDICATIONS

Gabapentin is contraindicated in patients with known hypersensitivity to

gabapentin or any of the components of the product.

PRECAUTIONS

Gabapentin should not be abruptly discontinued because of the

possibility of increasing seizure frequency.

Caution is recommended in patients with a history of psychotic illness.

Gabapentin should not be considered a treatment of absence seizures

and may exacerbate these seizures in some patients. Consequently,

gabapentin should be used with caution in patients who have mixed

seizure disorders that include absence seizures.

Patients should be advised neither to drive a car nor to operate

complex machinery until they have gained sufficient experience on

gabapentin.

Pregnancy

There are no adequate and well-controlled studies in pregnant women.

Gabapentin should be used during pregnancy only if the potential benefit

justifies the potential risk to the fetus.

Nursing Mothers

Gabapentin is secreted into breast milk following oral administration. The

effect on the nursing infant is unknown. Therefore, gabapentin should be

used in nursing women only if the potential benefits clearly out weigh the

risks.

Drug Interactions

Phenytoin, Valproic acid, Carbamazepine or Phenobarbitone: There is no

interaction during the concomitant administration of gabapentin with these

drugs. Gabapentin steady-state pharmacokinetics is similar for healthy

subjects and patients with epilepsy receiving anti-epileptic agents.

Morphine: 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.

Antacid: Gabapentin’s bioavailability was reduced by up to 24% when co-

administered at the same time with an aluminum and magnesium containing

antacid. It is recommended that gabapentin be taken about two hours

following any such antacid administration.

STORAGE CONDITIONS

Store at temperatures not exceeding 30°C.

Protect from sunlight and moisture.

The expiration date refers to the product correctly stored at the required

conditions.

Keep out of reach of children.

AVAILABILITY

Gabapentin (GABIX

) 100mg capsules are available in blister pack of 10’s.

Gabapentin (GABIX

) 300mg capsules are available in blister pack of 10’s.

CAUTION

Foods, Drugs, Devices and Cosmetics Act prohibits dispensing without

prescription.

For suspected adverse drug reaction, report to FDA: www.fda.gov.ph

REGISTRATION NUMBER:

Gabix Capsule 100mg: DR-XY34011

Gabix Capsule 300mg: DR-XY34012

DATE OF FIRST AUTHORIZATION / RENEWAL OF AUTHORIZATION

Gabix Capsule 100mg:

Initial: 27 November, 2007

Renewal: 05 December, 2012

Gabix Capsule 300mg:

Initial: 27 November, 2007

Renewal: 06 December, 2012

DATE OF REVISION OF PACKAGING INSERT 02 October, 2017.

Please read the contents carefully before use.

This package insert is continually updated from time to time.

Manufactured by: Getz Pharma (Pvt.) Ltd., 29-30/27, K.I.A., Karachi - 74900, Pakistan.

Imported by: Getz Pharma (Phils.) Inc., 2/F Tower 1, The Rockwell Business Center,

Ortigas Ave., Pasig City, Philippines.

PH-200010020

> 80

900-3600

50-79

600-1800

30-49

300-900

15-29

-600

< 15

Creatinine Clearance (mL/min)

Total Daily Dose

(mg/day)