metharbital

Metharbital is a barbiturate anticonvulsant and central nervous system depressant used primarily for the treatment of epilepsy and short-term insomnia. It was first patented in 1905 by Emil Fischer at Merck and later marketed as Gemonil by Abbott Laboratories. Metharbital acts similarly to phenobarbital, inducing drowsiness and relieving tension or nervousness but confers little analgesia. Its mechanism of action involves binding to a distinct site on the GABA A receptor chloride ion channel complex, increasing the duration that the Cl⁻ ionopore remains open. This potentiates inhibitory GABAergic tone in the central nervous system, particularly prolonging post-synaptic inhibition in the thalamus. Additionally, barbiturates like metharbital can directly inhibit excitatory AMPA-type glutamate receptors, further suppressing glutamatergic neurotransmission[1][3][4][8]. Metharbital has been withdrawn from many markets.

Brand names

Gemonil

Other names

Endiemalmetharbitonemethobarbitone