Description
How Supply:
Each Capsule Contains 300 mg Gabapentin,10 Capsule per blister pack,10 blister with a leaflet in a box.
Category
Anticonvulsant,Antineuralgic
Mechanism of Action
The chemical structure of gabapentin (Neurontin) is derived by addition of a cyclohexyl group to the backbone of gamma-aminobutyric acid (GABA). Gabapentin has no activity at GABAA or GABAB receptors of GABA uptake carriers of brain. Gabapentin interacts with a high-affinity binding site in brain membranes, which has recently been identified as an auxiliary subunit of voltage-sensitive Ca2+ channels. Gabapentin crosses several lipid membrane barriers via system L amino acid transporters. it increases non-synaptic GABA responses from neuronal tissues in vitro.Gabapentin is also active in models that detect anxiolytic activity.
Pharmacokinetics
- Absorption:Rapid,Gabapentin bioavailability (fraction of dose absorbed) tends to decrease with increasing dose. Absolute bioavailability of a 300mg capsule is approximately 60%.
- Distribution:volume of distribution is approximately 50 to 60 lit.
- 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.
- Half-Life:Elimination-Normal renal function 5 to 7 hours;Impaired renal function:52
Pregnancy and breast feeding
FDA pregnancy category C ,Gabapentin capsules should not be taken during pregnancy, unless advised by your doctor and it is distributed into human breast milk.
Precautions
- Importance of regular visit to physician to check progress therapy.
- Discussing Alcohol use or use of other CNS depressants with physicians
- Possible blured or double vision,dizziness,drowsiness,impairment of thinking or motor skill,caution when driving or doing job requiring alartness.
- Not discontinuing gabapentin abruptly,consulting physician about gradually reducing dose
Drug interactions
Inform your doctor if you are taking any of the following medicine:Alcohol ,CNS depression producing medication,Antacids especially aluminium and magnesium containing,Hydrocodone,Morphine,naproxen
Dosage and Administration
Usual and adolescent dose:
- Anticonvulsant:oral,initially 300mg three times a day. Dosage 900 to 1800 mg per day are effective for most patientshowever dosage as high as 2400 to 3600 mg per day have been well tolerated.
- Postherpetic neuralgia: oral,initial single dose of 300mg on day1, 600 mg per day(divide d two times a day) on day 2, 900 mg per day(divided three times a day) on day 3, dose may be titrated up to 1800 mg(divided three times a day)
- Diabetic peripheral neuropathic pain: oral,initially 900 mg per day titrated to a maximum of 3600 mg per day.
Usual adult and adolescent prescribing limit:3600 mg per day
Usual pediatric Dose:
- Anticonvulsant:
- Children 3 year to 18 years: the starting dose should range from 10 to 15 mg/kg of body weight per day,divided into three dose,the effective dose should be reached over a oweriod of approximately 3 days.
- Age 5 years and older:the effective dose is 25 to35 mg per kg of body weight per day three times a day.
- Age 3 years and 4 years: the effective dose is 40 mg per kg of body weight per day three times a day.
Side effects
Those indicating need for medical attention: Ataxia,nystagmus,neuropsychiatric problems including emotional lability,hostility,hyperkinesias and thought disorder,amnesia depression,irritability or other mood or mental changes,fracture,leukopenia
Those indicating need for medical attention only if they continue or are bothersome:Abnormal thinking,asthenia,diarrhea,dizziness,fatigue,fever,infection,myalgia,peripheral edema,somnolence,tremor,viral infection,vision abnormalities including blurred vision and diplopia
Storage
Store below 30˚c. Protect from Light and moisture .
keep out of reach of children .
Manufactured by Pursina Pharmaceutical Co Tehran-Iran