Progabide
pharmaceutical drug
Progabide, sold under the brand name Gabrene, is a GABA receptor agonist which is used in the treatment of epilepsy. It is an analogue of γ-aminobutyric acid (GABA) and acts both via a metabolite and as a prodrug of GABA, in turn behaving as an agonist of the GABA receptors.
Uses
Progabide was approved in France for either monotherapy or adjunctive use in the treatment of epilepsy—specifically, generalized tonic–clonic, myoclonic, partial, and Lennox-Gastaut syndrome seizures—in both children and adults... it was completely withdrawn in France in 1999 because of its high Hepatotoxicity
Side effects
Side effects of progabide include drowsiness, insomnia, and nausea. Less frequent side effects have been reported to include diaphoresis, malaise, gastralgia, somnolence, pruritus, urticaria, darkening of urine, and elevated liver enzymes. The drug has been associated with liver toxicity.
Pharmacology
Progabide acts as a non-selective GABA receptor agonist, including of both the GABAA and GABAB receptors. It is a GABA receptor agonist itself but also metabolizes into the more potent GABA receptor agonist progabide acid (SL-75.102). In addition, progabide and progabide acid are metabolized into gabamide and γ-aminobutyric acid (GABA), which act as GABA receptor agonists as well. Progabide crosses the blood–brain barrier, whereas gabamide and GABA do not, but progabide form gabamide and GABA within the brain.
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