Bookmark
Forward
QuickView for Orphenadrine (compound)
PubChem
| Name: | Orphenadrine |
|---|---|
| PubChem Compound ID: | 20846 |
| Description: | A muscarinic antagonist used to treat drug-induced parkinsonism and to relieve pain from muscle spasm. |
| Molecular formula: | C24H31NO8 |
| Molecular weight: | 461.505 g/mol |
| Synonyms: |
2-Dimethylaminoethyl-2-methyl-benzhydryl ether citrate; Ethanamine, N,N-dimethyl-2-((2-methylphenyl)phenylmethoxy)-, 2-hydroxy-1,2,3-propanetricarboxylate; N,N-Dimethyl-2-((o-methyl-alpha-phenyl-benzyl)oxy)-ethylamine citrate; ETHYLAMINE, N,N-DIMETHYL-2-((o-METHYL-alpha-PHENYLBENZYL)OXY)-, CITRATE; 4724-58-7; R-528; Benhexal
|
DrugBank
Identification
| Name: | Orphenadrine |
|---|---|
| Name (isomeric): | DB01173 |
| Drug Type: | small molecule |
| Description: | A muscarinic antagonist used to treat drug-induced parkinsonism and to relieve pain from muscle spasm. |
| Synonyms: |
Orphenadrin; Orphenate; Orphenadrine Citrate; Mephenamine; O-Methyldiphenhydramine; Orphenadine; Orphenedrine
|
| Brand: | Myolin, Antiflex, Norflex, Myotrol, Biorphen, Brocadisipal, Flexoject, Disipal, Mio-Rel, Brocasipal, Banflex, Orfro |
| Category: | Muscarinic Antagonists, Parasympatholytics, Antidyskinetics, Muscle Relaxants, Central, Antiparkinson Agents, Skeletal Muscle Relaxants |
| CAS number: | 83-98-7 |
Pharmacology
| 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 propertie...
show more » |
| 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 orphenadrin...
show more » |
| Absorption: | Orphenadrine is almost completely absorbed in the gastrointestinal tract. |
| Protein binding: | 95% |
| Biotransformation: | Biotransformation occurs mainly in the liver. Pharmacologically active metabolites are N-demethyl orphenadrine and N,N-didemethyl orphenadrine. |
| Half Life: | 13-20 hours |
| Toxicity: | Oral, mouse LD50 = 100 mg/kg; oral, rat LD50 = 255 mg/kg |
| Affected organisms: | Humans and other mammals |
Interactions
| Food interaction: |
| ||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| Drug interaction: |
|
Targets
Enzymes
