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药品详细

Orphenadrine(邻甲苯海拉明)

化学结构式图
中文名
邻甲苯海拉明
英文名
Orphenadrine
分子式
C18H23NO
化学名
dimethyl({2-[(2-methylphenyl)(phenyl)methoxy]ethyl})amine
分子量
Average: 269.3813
Monoisotopic: 269.177964363
CAS号
83-98-7
ATC分类
M03B 未知;N04A 未知
药物类型
small molecule
阶段
approved
商品名
Antiflex;Banflex;Biorphen;Brocadisipal;Brocasipal;Disipal;Flexoject;Mio-Rel;Myolin;Myotrol;Norflex;Orfro;
同义名
Mephenamine;O-Methyldiphenhydramine;Orphenadine;Orphenadrin;Orphenadrine Citrate;Orphenate;Orphenedrine;
基本介绍

A muscarinic antagonist used to treat drug-induced parkinsonism and to relieve pain from muscle spasm. [PubChem]

生产厂家
  • 3m pharmaceuticals inc
  • Akorn inc
  • Ascot hosp pharmaceuticals inc div travenol laboratories inc
  • Bedford laboratories
  • Gavis pharmaceuticals llc
  • Graceway pharmaceuticals llc
  • Impax pharmaceuticals
  • Kiel laboratories inc
  • Sandoz inc
  • Watson laboratories inc
封装厂家
参考
Synthesis Reference Not Available
General Reference
  1. Ji D, Sui ZY, Ma YY, Luo F, Cui CL, Han JS: NMDA receptor in nucleus accumbens is implicated in morphine withdrawal in rats. Neurochem Res. 2004 Nov;29(11):2113-20. Pubmed
剂型
规格
化合物类型
Type small molecule
Classes
  • Diphenhydramines
Substructures
  • Diphenhydramines
  • Benzyl Alcohols and Derivatives
  • Ethers
  • Benzene and Derivatives
  • Aliphatic and Aryl Amines
  • Diphenylmethanes
  • Aromatic compounds
适应症
PARKINSON 帕金森氏症;
药理
Indication Indicated for the treatment of Parkinson's disease.
Pharmacodynamics 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.
Absorption Orphenadrine is almost completely absorbed in the gastrointestinal tract.
Volume of distribution Not Available
Protein binding 95%
Metabolism
Biotransformation occurs mainly in the liver. Pharmacologically active metabolites are N-demethyl orphenadrine and N,N-didemethyl orphenadrine.

Important The metabolism module of DrugBank is currently in beta. Questions or suggestions? Please contact us.

Substrate Enzymes Product
Orphenadrine
    		N-demethyl orphenadrine Details
    Orphenadrine
      		N,N-didemethyl orphenadrine Details
      Route of elimination Not Available
      Half life 13-20 hours
      Clearance Not Available
      Toxicity Oral, mouse LD50 = 100 mg/kg; oral, rat LD50 = 255 mg/kg
      Affected organisms
      • Humans and other mammals
      Pathways Not Available
      理化性质
      Properties
      State solid
      Experimental Properties
      Property Value Source
      melting point < 25 °C PhysProp
      boiling point 195 °C at 1.20E+01 mm Hg PhysProp
      water solubility Sparingly soluble in water Not Available
      logP 3.77 SANGSTER (1993)
      pKa 8.91 SANGSTER (1994)
      Predicted Properties
      Property Value Source
      water solubility 3.00e-02 g/l ALOGPS
      logP 3.5 ALOGPS
      logP 4.17 ChemAxon
      logS -4 ALOGPS
      pKa (strongest basic) 8.87 ChemAxon
      physiological charge 1 ChemAxon
      hydrogen acceptor count 2 ChemAxon
      hydrogen donor count 0 ChemAxon
      polar surface area 12.47 ChemAxon
      rotatable bond count 6 ChemAxon
      refractivity 84.97 ChemAxon
      polarizability 31.83 ChemAxon
      药物相互作用
      Drug Interaction
      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.
      食物相互作用
      • Take without regard to meals. Avoid alcohol.

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