Drug intelligence / Profile preview

cyclobenzaprine + caffeine

Development stage
Preclinical
Modality
Small Molecules
Administration
Oral
01

Overview

Cyclobenzaprine + caffeine is a combination of two active pharmaceutical ingredients. Cyclobenzaprine is a skeletal muscle relaxant that acts primarily at the brainstem to reduce muscle spasms of local origin, commonly used for relief of muscle spasm associated with acute musculoskeletal conditions. Caffeine is a central nervous system stimulant that can counteract drowsiness and sedation caused by cyclobenzaprine. The combination has been proposed and patented as a treatment for muscle spasm, aiming to maintain the efficacy of cyclobenzaprine while reducing its sedative side effects by including caffeine[5][1]. Cyclobenzaprine’s mechanism involves antagonism at serotonin and histamine receptors in the central nervous system, while caffeine acts as an adenosine receptor antagonist.

02

Targets

ADORA2A (Adenosine A₂A Receptor)5-HT (Serotonin receptors)ADORA1 (Adenosine receptor A1 subtype)HRH1 (Histamine H1 Receptor)

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