Drug intelligence / Profile preview

nimesulide + cyclobenzaprine

Development stage
Unknown
Lead developer
Boehringer Ingelheim
Modality
Small Molecules
Administration
Oral
01

Overview

Nimesulide + cyclobenzaprine is a combination drug consisting of two active pharmaceutical ingredients: - **Nimesulide** is a nonsteroidal anti-inflammatory drug (NSAID) that works by inhibiting the synthesis of prostaglandins, thereby reducing pain and inflammation. - **Cyclobenzaprine** is a centrally acting skeletal muscle relaxant. Its mechanism involves action at the brainstem to reduce skeletal muscle spasm, likely by inhibiting descending serotonergic pathways and diminishing activity of efferent alpha and gamma motor neurons. Cyclobenzaprine does not act directly on skeletal muscles or neuromuscular junctions. This combination would be used for the symptomatic treatment of acute musculoskeletal pain with associated muscle spasm, leveraging both anti-inflammatory/analgesic effects (from nimesulide) and muscle relaxation (from cyclobenzaprine). Both drugs are intended for short-term use due to safety concerns with long-term administration[4][9].

02

Targets

ADRA2A (α2A)SERT (Sodium-dependent serotonin transporter)HTR2B (5-Hydroxytryptamine Receptor 2B)HRH1 (Histamine H1 Receptor)HTR2C (5-hydroxytryptamine 2C receptor)ADRA1A (α1A)HTR2A (Serotonin receptor 5-HT2A)HTR1A (Serotonin receptor 1A (5-hydroxytryptamine receptor 1A))M1 (Muscarinic acetylcholine receptor M1)NET (Norepinephrine Transporter)DAT (Dopamine plasma membrane transport protein)PTGS2 (Prostaglandin-Endoperoxide Synthase 2)PGHS-1 (Prostaglandin G/H Synthase 1)

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