Drug intelligence / Profile preview

barbexaclone

Development stage
Discontinued
Modality
Implantable Devices → Device-based Delivery → Drug Delivery Systems, Small Molecules, Transdermal Patches → Device-based Delivery → Drug Delivery Systems, Inhalation Devices → Device-based Delivery → Drug Delivery Systems
Administration
Oral
01

Overview

Barbexaclone is a pharmaceutical salt compound consisting of phenobarbital (a barbiturate anticonvulsant) and propylhexedrine (a sympathomimetic stimulant), typically in a ratio of 60% phenobarbital to 40% propylhexedrine by weight. It was introduced in the 1960s as an antiepileptic drug, with the intent that the stimulant properties of propylhexedrine would counteract the sedative effects of phenobarbital. Barbexaclone has been reported to be as effective as phenobarbital for seizure control, but with improved tolerability and reduced sedation. Its mechanism of action reflects those of its components: phenobarbital acts primarily by enhancing GABAergic inhibition via GABA receptors in the central nervous system, while propylhexedrine acts as a TAAR1 agonist and adrenergic agonist, providing mild psychostimulant effects. Barbexaclone was used mainly for epilepsy treatment but was discontinued from markets such as Turkey in 2009 due to lack of large controlled trials confirming its benefits over standard therapy[1][2][3][6].

Brand names
Maliasin
Other names
barbexaclone [INN]
02

Targets

GABRR (GABA-A receptor subunit rho)TAAR1 (Trace amine-associated receptor 1)AR (Adrenergic receptors)

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