Drug intelligence / Profile preview

cyclobenzaprine + gamma-aminobutyric acid

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

Overview

This is a **combination drug** comprising cyclobenzaprine and gamma-aminobutyric acid (GABA). Cyclobenzaprine is a centrally acting muscle relaxant structurally similar to tricyclic antidepressants. It is used primarily for short-term treatment (2–3 weeks) of muscle spasms associated with acute painful musculoskeletal conditions. Its mechanism likely involves antagonism of serotonergic and noradrenergic pathways in the central nervous system with additional antihistaminic and antimuscarinic effects. Gamma-aminobutyric acid is the main inhibitory neurotransmitter in the CNS, involved in reducing neuronal excitability. While endogenous GABA does not cross the blood-brain barrier when administered exogenously, it is sometimes included in over-the-counter supplements or studied in combination for theoretical anxiolytic or calming effects. The mechanism of the combination would theoretically include both skeletal muscle relaxation (via cyclobenzaprine) and increased inhibitory neurotransmission (via GABA), though there is **no evidence of regulatory approval or standard clinical use for the cyclobenzaprine + GABA combination as a distinct pharmaceutical product**.

Brand names
therabenzaprine-90therabenzaprine90therabenzaprine 90
Other names
cyclobenzaprine hydrochloride + gamma-aminobutyric acid
02

Targets

HTR6 (5-hydroxytryptamine receptor 6)SERT (Sodium-dependent serotonin transporter)HRH1 (Histamine H1 Receptor)M1 (Muscarinic acetylcholine receptor M1)HTR2A (Serotonin receptor 5-HT2A)HTR7 (5-hydroxytryptamine receptor 7)ADRA1A (α1A)GABA-B (Gamma-aminobutyric acid receptor type B)CHRM2 (M2)HTR2C (5-hydroxytryptamine 2C receptor)ADRA2A (α2A)NET (Norepinephrine Transporter)HTR2B (5-Hydroxytryptamine Receptor 2B)CHRM3 (M3)

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