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Home / Drugs / Starting with O / Orphenadrine

A muscarinic antagonist used to treat drug-induced parkinsonism and to relieve pain from muscle spasm. [PubChem]
CategoriesSkeletal Muscle Relaxants
Antiparkinson Agents
Muscarinic Antagonists
Muscle Relaxants, Central
ManufacturersGraceway pharmaceuticals llc
Akorn inc
Bedford laboratories
Watson laboratories inc
Ascot hosp pharmaceuticals inc div travenol laboratories inc
Gavis pharmaceuticals llc
Impax pharmaceuticals
Kiel laboratories inc
Sandoz inc
3m pharmaceuticals inc
PackagersAbraxis BioScience Inc.
Actavis Group
Aidarex Pharmacuticals LLC
Alba Pharmacal
A-S Medication Solutions LLC
Avkare Incorporated
Bedford Labs
Ben Venue Laboratories Inc.
Bryant Ranch Prepack
Clint Pharmaceutical Inc.
Corepharma LLC
DispenseXpress Inc.
Dispensing Solutions
Diversified Healthcare Services Inc.
Eon Labs
Gavis Pharmaceuticals LLC
Global Pharmaceuticals
Graceway Pharmaceuticals
H.J. Harkins Co. Inc.
Impax Laboratories Inc.
Innoviant Pharmacy Inc.
International Ethical Labs Inc.
Kiel Laboratories Inc.
Lake Erie Medical and Surgical Supply
Major Pharmaceuticals
Murfreesboro Pharmaceutical Nursing Supply
Nucare Pharmaceuticals Inc.
Palmetto Pharmaceuticals Inc.
PD-Rx Pharmaceuticals Inc.
Pharma Pac LLC
Pharmaceutical Utilization Management Program VA Inc.
Physicians Total Care Inc.
Preferred Pharmaceuticals Inc.
Prepak Systems Inc.
Rebel Distributors Corp.
Redpharm Drug
Resource Optimization and Innovation LLC
Sandhills Packaging Inc.
Southwood Pharmaceuticals
St Mary's Medical Park Pharmacy
Stat Rx Usa
Watson Pharmaceuticals
Orphenadrine Citrate


Indicated for the treatment of Parkinson's disease.


Orphenadrine is indicated as an adjunct to rest, physical therapy, and other measures for the relief of discomfort associated with acute painful musculoskeletal conditions. Orphenadrine is an anticholinergic with a predominantly central effect and only a weak peripheral effect. In addition, it has mild antihistaminic and local anaesthetic properties. Parkinson's syndrome is the consequence of a disturbed balance between cholinergic and dopaminergic neurotransmission in the basal ganglia caused by a decrease in dopamine. Orphenadrine restores the physiological equilibrium and has a favourable effect on the rigidity and tremor of Parkinson's disease and Parkinsonian syndromes. The effect is somewhat less on bradykinesia.

mechanism of action

Orphenadrine binds and inhibits both histamine H1 receptors and NMDA receptors. It restores the motor disturbances induced by neuroleptics, in particular the hyperkinesia. The dopamine deficiency in the striatum increases the stimulating effects of the cholinergic system. This stimulation is counteracted by the anticholinergic effect of orphenadrine. It may have a relaxing effect on skeletal muscle spasms and it has a mood elevating effect.


Oral, mouse LD50 = 100 mg/kg; oral, rat LD50 = 255 mg/kg


Biotransformation occurs mainly in the liver. Pharmacologically active metabolites are N-demethyl orphenadrine and N,N-didemethyl orphenadrine.


Orphenadrine is almost completely absorbed in the gastrointestinal tract.

half life

13-20 hours

drug interactions

Docetaxel: Orphenadrine may increase the serum levels and toxicity of docetaxel.

Donepezil: Possible antagonism of action

Galantamine: Possible antagonism of action

Haloperidol: The anticholinergic increases the risk of psychosis and tardive dyskinesia

Rivastigmine: Possible antagonism of action

Tacrine: The therapeutic effects of the central acetylcholinesterase inhibitor, Tacrine, and/or the anticholinergic, Orphenadrine, may be reduced due to antagonism. The interaction may be beneficial when the anticholinergic action is a side effect. Monitor for decreased efficacy of both agents.

Trimethobenzamide: Trimethobenzamide and Orphenadrine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.

Triprolidine: Triprolidine and Orphenadrine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Additive CNS depressant effects may also occur. Monitor for enhanced anticholinergic and CNS depressant effects.

Trospium: Trospium and Orphenadrine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.