Gabatin 300 mg capsule is a white to off-white powder encapsulated in capsule size #1 with orange cap and white body.
Gabatin 100 mg capsule is a white to off-white powder encapsulated in capsule size #3 with white cap and white body.
Each capsule contains: Gabapentin, USP 100 mg & 300 mg.
Antiepileptic.
Pharmacology: Pharmacodynamics: Gabapentin is structurally related to the inhibitory neurotransmitter gamma-aminobutyric acid (GABA). It has sufficient lipid solubility to cross the blood-brain barrier. Despite its structural relationship to GABA and demonstrate antiepileptic activity, gabapentin's precise mechanism of action remains unknown. It does not modify GABAA or GABAB. It is not converted metabolically into GABA or a GABA agonist, and it is not an inhibitor of GABA uptake or degradation.
Gabapentin also has no affinity for binding sites on common neuroreceptors such as benzodiazepine, glutamate, N-methyl-D-aspartate (NMDA), quisqualate, kainite, strychnine-insensitive or strychnine-sensitive glycine, alpha1, alpha2, or beta adrenergic, adenoside A1 or A2, cholinergic muscarinic or nicotinic, dopamine D1 or D2, histamine H1, serotonin S1 or S2, delta, or kappa, cannabinoid 1, voltage-sensitive calcium channel sites labeled with nitrendipine or diltiazem, or at voltage-sensitive sodium channel sites labeled with batrachotoxinin A20-alpha-benzoate. Furthermore, gabapentin does not alter the cellular uptake of dopamine, noradrenaline or serotonin. The mechanism of gabapentin's anticonvulsant action is unknown. Gabapentin exhibits antiseizure activity in mice and rats in both the maximal electroshock and pentylenentetrazole seizure models and other preclinical models (e.g., strains with genetic epilepsy, etc.). The mechanism of gabapentin's analgesic action is unknown. In animal models, gabapentin prevents allodynia (pain-related behavior in response to a normally innocuous stimulus) and hyperalgesia (exaggerated response to painful stimuli). It prevents pain-related responses in neuropathic pain models and decreases pain-related responses after peripheral inflammation in rats or mice.
Pharmacokinetics: Gabapentin is absorbed from the gastrointestinal tract by means of a saturable mechanism. Following multiple dosing peak plasma concentrations are usually achieved within 2 to 3 hours of administration and steady state achieved within 1 to 2 days. Gabapentin is not appreciably metabolized and most of a dose is excreted unchanged in the urine with the remainder appearing in faeces. Gabapentin is widely distributed throughout the body but binding to plasma proteins is minimal. The elimination half-life has been reported to be about 5 to 7 hours. Gabapentin is distributed into breast milk.
For the treatment of epilepsy.
The initial adult dose of Gabapentin for the treatment of epilepsy is 300 mg by mouth on the first day of treatment, 300 mg twice daily on the second day and 300 mg three times daily on the third day: thereafter the dose may be increased in increments of 300 mg daily until effective antiepileptic control is achieved which is usually within the range of 0.9 to 1.2 g daily. Higher doses up to a maximum of 2.4 g daily may be required in some patients. The total daily dose should be taken in three equally divided doses and the maximum dosage intervals should not exceed 12 hours or as prescribed by the physician.
The initial dose for children 6 to 12 years of age for the treatment of epilepsy is 10 mg per kg body-weight on the first day of treatment, 20 mg per kg on the second day, and 25 to 35 mg per kg on the third day. Recommended maintenance doses are 900 mg daily for children weighing 26 to 36 kg and 1200 mg daily for those weighing 37 to 50 kg. In the treatment of neuropathic pain in adults, doses should be titrated to a maximum of 1.8 g daily in three divided dose, in a similar manner to that recommended for the treatment of epilepsy in adults given as previously mentioned. Or as prescribed by the physician.
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, loss of consciousness, lethargy, and mild diarrhea. 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, minimize toxicity from overdoses. Although gabapentin can be removed by hemodialysis, based on prior experience. It is usually not required. However, in patients with severe renal impairment, hemodialysis 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, labored breathing, ptosis, hypoactivity, or excitation.
Gabapentin is contraindicated in patients who are hypersensitive to gabapentin.
Gabapentin should be used with caution in patients with a history of psychotic illness. It should also be used with caution in renal impairment; the manufacturer recommends dosage reduction in patients with reduced renal function or those undergoing haemodialysis. False positive readings have been reported with some urinary protein test in patients taking Gabapentin.
Pregnancy: Pregnancy Category C: Gabapentin has been shown to be fetotoxic in rodents, causing delayed ossification of several bones in the skull, vertebrae, forelimbs, and hindlimbs. These effects occurred when pregnant mice received oral doses of 1000 mg or 3000 mg/kg/day during the period of orgagenesis, or approximately 1 to 4 times that maximum dose of 3600 mg/day given to epileptic patients on mg/m2 basis. The no-effect level was 500 mg/kg/day or approximately ½ of the human dose on a mg/m2 basis. There are no adequate and well-controlled studies in pregnant women. This drug should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Lactation: Gabapentin is excreted in human milk. Because the effect on the nursing infant is unknown, caution should be exercised when gabapentin is administered to a nursing mother. Gabapentin should be used in nursing mothers only if the benefits clearly outweigh the risks.
The most commonly reported adverse effects associated with Gabapentin are somnolence, dizziness, ataxia, and fatigue. Nystagmus, tremor, diplopia, amblyopia, pharyngitis, dysarthria, weight gain, dyspepsia, amnesia, weakness, paraesthesia, arthralgia, purpura leucopenia, anxiety, and urinary-tract infection may occur less frequently. Rarely pancreatitis, altered liver function tests, erythema multiforme, Stevens-Johnson Syndrome, rhinitis, nervousness, myalgia, headache, nausea and vomiting, and blood glucose fluctuations in diabetics have been reported.
The absorption of Gabapentin from the gastrointestinal tract is reduced by antacids and concomitant administration is therefore not recommended. Cimetidine has been reported to reduce the renal clearance of Gabapentin but the manufacturers do not consider this to be of clinical importance.
Store at temperatures not exceeding 30°C.
N02BF01 - gabapentin ; Belongs to the class of gabapentinoids. Used to relieve pain and other conditions.
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