Drug intelligence / Profile preview

orphenadrine

Development stage
Approved
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral, Intramuscular, Intravenous
01

Overview

Orphenadrine is a centrally acting skeletal muscle relaxant and anticholinergic agent of the ethanolamine antihistamine class. It is primarily used as an adjunct to rest and physical therapy for the relief of discomfort associated with acute painful musculoskeletal conditions such as strains and sprains. Orphenadrine also has applications in managing motor symptoms (tremor, rigidity) in Parkinson's disease due to its anticholinergic effects[1][2][4][5]. Its mechanism of action involves antagonism at muscarinic acetylcholine receptors (anticholinergic), histamine H1 receptors (antihistaminic), NMDA glutamate receptors (NMDA antagonist), inhibition of norepinephrine and dopamine reuptake, and blockade of certain sodium channels[4][5][6]. These combined actions contribute to its muscle relaxant properties and efficacy in pain management.

Brand names
NorflexBanflexOrphenateFlexojectFlexon
Other names
orphenadrine citrate
02

Targets

HRH1 (Histamine H1 Receptor)NET (Norepinephrine Transporter)SCN10A (Sodium channel protein type X alpha subunit)NMDAR (Glutamate receptor ionotropic, NMDA)

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