Orphenadrine: profile and news

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Other information

Indication
Indicated for the treatment of Parkinson's disease.

Pharmacology
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 to 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.

Drug Category
Muscle Relaxants; Antiparkinson Agents; Antidyskinetics; Skeletal Muscle Relaxants; ATC:M03BC01; ATC:N04AB02

Brand Names/Synonyms
Antiflex; BS-5930; Banflex; Biorphen; Brocadisipal; Brocasipal; Disipal; Flexoject; Mephenamine; Mio-Rel; Myolin; Myotrol; Norflex; O-Methyldiphenhydramine; Orfro; Orphenadine; Orphenadrin; Orphenadrine; Orphenadrine Citrate; Orphenate; Orphenedrine; WS 2434

Dosage Forms
TABLET (EXTENDED-RELEASE)

Absorption
Orphenadrine is almost completely absorbed in the gastrointestinal tract.

Interactions
Interactions for Orphenadrine:

No information provided.

Chemical IUPAC Name
N,N-dimethyl-2-[(2-methylphenyl)-phenyl-methoxy]-ethanamine

Chemical Formula
C18H23NO

Half Life
13-20 hours

Drug Type
Approved Drug

# Accession No
APRD00097

CAS Registry Number
83-98-7