Drug intelligence / Profile preview

ibuprofen + cyclobenzaprine

Development stage
Unknown
Lead developer
Tonix Pharmaceuticals
Modality
Small Molecules
Administration
Oral
01

Overview

Ibuprofen + cyclobenzaprine is a combination of two small molecule drugs used together for the short-term management of acute musculoskeletal pain and muscle spasms. Ibuprofen is a nonsteroidal anti-inflammatory drug (NSAID) that works by inhibiting cyclooxygenase enzymes, thereby reducing prostaglandin synthesis and inflammation. Cyclobenzaprine is a centrally acting skeletal muscle relaxant structurally related to tricyclic antidepressants; it acts primarily by inhibiting serotonin and norepinephrine reuptake and blocking serotonin, adrenergic, histamine, and muscarinic acetylcholine receptors in the central nervous system. The combination may be prescribed to relieve pain associated with acute muscle injuries or strains. However, clinical studies have shown that adding cyclobenzaprine to ibuprofen does not significantly improve analgesia compared to ibuprofen alone but increases the risk of central nervous system side effects such as drowsiness and dizziness[6][7][9]. This combination should be used with caution in patients with certain comorbidities (e.g., renal or hepatic impairment), in elderly patients due to increased sensitivity to side effects, and only for short durations (typically 2–3 weeks)[1][4].

02

Targets

SERT (Sodium-dependent serotonin transporter)PGHS-1 (Prostaglandin G/H Synthase 1)HRH1 (Histamine H1 Receptor)M1 (Muscarinic acetylcholine receptor M1)ADRA2B (α2B)PTGS2 (Prostaglandin-Endoperoxide Synthase 2)NET (Norepinephrine Transporter)

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