Drug intelligence / Profile preview

carisoprodol + gamma-aminobutyric acid

Development stage
Unknown
Lead developer
Physician Therapeutics
Modality
Small Molecules
Administration
Oral
01

Overview

This is a **combination** of two drugs—**carisoprodol**, a centrally-acting muscle relaxant primarily used for the short-term relief of acute, painful musculoskeletal conditions, and **gamma-aminobutyric acid (GABA)**, which is the primary inhibitory neurotransmitter in the central nervous system but is also used as a dietary supplement. Carisoprodol exerts its pharmacologic effects mainly through the central nervous system by modulating activity at the **GABA-A receptor**. This effect is thought to be mediated both directly (carisoprodol acts as an allosteric modulator and direct activator at GABA-A receptors, with actions similar to barbiturates but via a distinct binding site) and indirectly through its primary metabolite, **meprobamate**, which also acts on GABA-A receptors and has well-established anxiolytic and sedative properties[1][2][3][7]. GABA itself, when ingested, does not have significant brain penetration due to the blood-brain barrier, so its central effects in this combination are minimal or unclear. Nevertheless, it is included in dietary supplements with putative calming effects. Primary indications for carisoprodol are the short-term treatment (up to 2-3 weeks) of musculoskeletal pain; GABA’s inclusion would theoretically target anxiety or promote relaxation, but evidence for clinical benefit from exogenous GABA in this context is limited.

Brand names
Prazolamine
Other names
carisoprodol + gamma-aminobutyric acidcarisoprodol + GABAGABA + carisoprodol
02

Targets

GABRR (GABA-A receptor subunit rho)

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