Pharmacokinetics

Gabapentin has a favourable pharmacokinetic profile compared with other antiepileptic drugs. It is not metabolized by the liver and does not bind to plasma proteins, minimizing interactions with other drugs. Its chemical structure is similar to the amino acids leucine, valine, and phenylalanine. Thus, it is actively transported across the gut by an amino acid transporter. Its bioavailability is 60 per cent at therapeutic doses, but decreases with increasing dose of medication, owing to saturation of the transport mechanism.(29) Absorption is unaffected by food. Its plasma concentration peaks approximately 2 to 3 h after an oral dose. (29> Gabapentin is excreted unchanged in the urine. Its half-life is between 5 and 7 h, but this may increase with renal impairment, requiring dosage reduction. (30)

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