Drug intelligence / Profile preview

diclofenac + tizanidine

Development stage
Unknown
Lead developer
Novartis
Modality
Small Molecules
Administration
Oral
01

Overview

**Diclofenac + tizanidine** is a fixed-dose oral combination of two active ingredients: diclofenac, a non-steroidal anti-inflammatory drug (NSAID), and tizanidine, a centrally acting muscle relaxant. Diclofenac acts by inhibiting cyclooxygenase (COX) enzymes, reducing prostaglandin synthesis and thereby decreasing inflammation and pain. Tizanidine is an alpha-2 adrenergic receptor agonist that acts at the level of the central nervous system (spinal cord and brain) to reduce excitatory input to motor neurons, subsequently relieving skeletal muscle spasticity and spasms. This combination is primarily used in the short-term management of acute musculoskeletal pain, especially when associated with muscle spasm (such as low back pain, neck pain, and other musculoskeletal conditions). The dual mechanism targets both inflammation and muscle spasticity, enhancing symptomatic relief and functional recovery. The combination should be prescribed and monitored by a physician, especially due to potential central nervous system side effects and the risk of hepatotoxicity.

Other names
tizanidine + diclofenac
02

Targets

PGHS-1 (Prostaglandin G/H Synthase 1)ADRA2A (α2A)PTGS2 (Prostaglandin-Endoperoxide Synthase 2)ADRA1A (α1A)

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