Progabide

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Progabide is a medication once used to treat epilepsy, sold under brand names such as Gabrene and Gabren. It is a GABA receptor agonist and works as a prodrug of GABA, meaning it is transformed inside the brain into active forms that boost GABA activity.

How it works
Progabide acts on GABA receptors and is metabolized into progabide acid, gabamide, and GABA, all of which also stimulate GABA receptors. Progabide can cross the blood–brain barrier, while gabamide and GABA mostly act inside the brain.

How it is used
It was approved in France for epilepsy, used either as the main treatment or as an add-on. It covered several seizure types, including generalized tonic–clonic, myoclonic, partial, and Lennox-Gastaut syndrome, in both adults and children. It was not widely approved outside France.

Side effects and safety
Common side effects include drowsiness, trouble sleeping, and nausea. Other possible effects are sweating, feeling unwell, stomach pain, itching, hives, dark urine, and raised liver enzymes. Liver toxicity has been a concern with progabide.

Pharmacokinetics
Progabide is taken by mouth. It usually reaches peak levels in 2–3 hours, with a typical elimination half-life of 10–12 hours. Steady-state levels are reached after about 2–4 days of regular use. The drug is heavily metabolized, and only trace amounts are recovered in urine.

History and status
Progabide was first described in 1979 and was marketed in France around 1985 by Dausse-Synthelabo. It was studied in other countries but never gained wide international use. Research explored its effects on Parkinson’s disease, schizophrenia, depression, anxiety, and spasticity, but concerns about liver toxicity and limited effectiveness limited its adoption. A 2004 Cochrane review concluded that any potential benefits were probably outweighed by adverse effects.