Drug intelligence / Profile preview

cyclobenzaprine

Development stage
Approved
Lead developer
Merck
Modality
Small Molecules
Administration
Oral
01

Overview

Cyclobenzaprine is a centrally acting skeletal muscle relaxant used as an adjunct to rest and physical therapy for the relief of muscle spasm associated with acute, painful musculoskeletal conditions. It is structurally related to tricyclic antidepressants and acts primarily within the central nervous system at the brainstem level. The precise mechanism of action is not fully understood, but it is believed to reduce tonic somatic motor activity influencing both alpha and gamma motor neurons. Cyclobenzaprine exhibits antagonistic activity at serotonin (5-HT2) receptors in the spinal cord, inhibits norepinephrine reuptake, and has anticholinergic effects. It does not act directly on skeletal muscle or neuromuscular junctions[1][2][4][5][6]. The drug is indicated for short-term use (typically 2–3 weeks) in adults and adolescents aged 15 years or older[1][7].

Brand names
AmrixFexmidFlexerilComfort Pac with Cyclobenzaprine
Other names
cyclobenzaprine hydrochloride
02

Targets

HTR2A (Serotonin receptor 5-HT2A)SERT (Sodium-dependent serotonin transporter)ADRA2C (α2C)

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