Drug intelligence / Profile preview

phenprobamate

Development stage
Unknown
Modality
Small Molecules
Administration
Oral
01

Overview

Phenprobamate is a centrally acting skeletal muscle relaxant with additional sedative and anticonvulsant effects. It is used primarily for the treatment of pain caused by muscle spasms, as well as for muscle cramps, spasticity, and occasionally as an anxiolytic or adjunct in general anesthesia. Its mechanism of action is believed to be similar to that of meprobamate—likely involving positive modulation of the GABA A receptor—though the precise molecular target has not been definitively established. Phenprobamate has been largely replaced by newer agents but remains available over-the-counter in some European countries and has also been marketed as a nootropic. The drug is metabolized via oxidative degradation of its carbamate group and ortho-hydroxylation of its benzene ring; it is eliminated renally with an elimination half-life of 5–8 hours[1][2][7].

Brand names
GamaquilIsotonilActozine
Other names
3-phenylpropylcarbamate
02

Targets

GABRR (GABA-A receptor subunit rho)

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