Gabapentin is an anti-epileptic that is used as an adjuvant therapy in patients with refractory partial epilepsy. At present, doses up to 3600 mg per day are used. The relatively mild side-effects and the non-occurrence of interactions up to now are the plus points of this drug.
More randomized clinical trials are needed to clarify the position as monotherapy and the position relative to the other new anti-epileptics.
Gabapentin is an antiepileptic that is used in doses up to 3600 mg/day as an adjunctive treatment for refractory partial epilepsy. Its relatively mild side effects and lack of interactions are advantages; however, more randomized clinical studies are needed to clarify the place of gabapentin as monotherapy and with regard to other new antiepileptic.
Gabapentin (1-(aminomethyl) cyclohexane acetate) is structurally related to gamma-aminobutyric acid (GABA). The mechanism of action differs from other drugs that interact with GABA-negative synapses, such as valproic acid. Gabapentin is not a GABA (ant) agonist or inhibitor of GABA uptake or breakdown. Radiolabeled gabapentin was recovered at sites in the central nervous system that are involved in an epileptic seizure. The exact mechanism of action is not known.
After oral administration, the maximum plasma concentration is reached within two to three hours. Food intake has no effect on the absorption of gabapentin. Bioavailability is 60%. The transport mechanism for recording is saturable; it smooths at a dose above 1800 mg and it is saturated at a dose of 3600 mg.
Gabapentin is not bound to plasma protein. In epilepsy patients, the gabapentin concentration in the cerebrospinal fluid is approximately 20% of the corresponding steady-state plasma concentration. The steady-state concentrations in plasma are not predictive of the efficacy and safety of the product.
The clearance is completely renal. Gabapentin is not metabolized in humans. The average elimination half-life is five to seven hours. The elimination rate, plasma clearance, and renal clearance are related to creatinine clearance. It is necessary to adjust the dosage in elderly patients and patients with renal impairment. Gabapentin can be eliminated by hemodialysis.
Gabapentin has a large therapeutic breadth. If intervention is necessary, hemodialysis is indicated in severe renal impairment.
Gabapentin is contraindicated in patients with hypersensitivity to gabapentin or to any of the excipients. The capsules contain lactose, cornstarch, and talc. The capsule shell contains gelatin, titanium dioxide (E171) or titanium dioxide with iron oxide (E172).
Gabapentin can affect the reaction and concentration ability.
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