Tìm theo
Orphenadrine
Các tên gọi khác (14 ) :
  • 2-(phenyl-o-tolylmethoxy)ethyldimethylamine
  • 2-methyldiphenhydramine
  • beta-Dimethylaminoethyl 2-methylbenzhydryl ether
  • Dimethyl-[2-(phenyl-O-tolyl-methoxy)-ethyl]-amine
  • N,N-Dimethyl-2-(alpha-2-tolylbenzoyloxy)ethylamine
  • N,N-Dimethyl-2-(phenyl(O-tolyl)methoxy)ethanamine
  • N,N-Dimethyl-2-[(O-methyl-alpha-phenylbenzyl)oxy]ethylamine
  • o-methyldiphenhydramine
  • o-monomethyldiphenhydramine
  • Orfenadrina
  • ORPHENADRINE
  • Orphenadrinum
  • Phenyl-O-tolylmethyl dimethyaminoethyl ether
  • β-dimethylaminoethyl 2-methylbenzhydryl ether
Thuốc chống Parkinson
Thuốc Gốc
Small Molecule
CAS: 83-98-7
ATC: M03BC01, N04AB02
ĐG : Abraxis BioScience Inc. , http://www.abraxisbio.com
CTHH: C18H23NO
PTK: 269.3813
A muscarinic antagonist used to treat drug-induced parkinsonism and to relieve pain from muscle spasm. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C18H23NO
Phân tử khối
269.3813
Monoisotopic mass
269.177964363
InChI
InChI=1S/C18H23NO/c1-15-9-7-8-12-17(15)18(20-14-13-19(2)3)16-10-5-4-6-11-16/h4-12,18H,13-14H2,1-3H3
InChI Key
InChIKey=QVYRGXJJSLMXQH-UHFFFAOYSA-N
IUPAC Name
dimethyl({2-[(2-methylphenyl)(phenyl)methoxy]ethyl})amine
Traditional IUPAC Name
orphenadrine
SMILES
CN(C)CCOC(C1=CC=CC=C1)C1=CC=CC=C1C
Độ tan chảy
< 25 °C
Độ sôi
195 °C at 1.20E+01 mm Hg
Độ hòa tan
Sparingly soluble in water
logP
3.77
logS
-4
pKa (Strongest Basic)
8.87
PSA
12.47 Å2
Refractivity
84.97 m3·mol-1
Polarizability
31.83 Å3
Rotatable Bond Count
6
H Bond Acceptor Count
2
H Bond Donor Count
0
Physiological Charge
1
Number of Rings
2
Bioavailability
1
Rule of Five
true
Ghose Filter
true
pKa
8.91
Dược Lực Học : 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.
Cơ Chế Tác Dụng : A muscarinic antagonist used to treat drug-induced parkinsonism and to relieve pain from muscle spasm. [PubChem] 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.
Dược Động Học :
▧ Absorption :
Orphenadrine is almost completely absorbed in the gastrointestinal tract.
▧ Protein binding :
95%
▧ Metabolism :
Biotransformation occurs mainly in the liver. Pharmacologically active metabolites are N-demethyl orphenadrine and N,N-didemethyl orphenadrine.
▧ Half Life :
13-20 hours
Độc Tính : Oral, mouse LD50 = 100 mg/kg; oral, rat LD50 = 255 mg/kg
Chỉ Định : Indicated for the treatment of Parkinson's disease.
Tương Tác Thuốc :
  • 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.
Liều Lượng & Cách Dùng : Liquid - Intravenous
Tablet - Oral
Tablet, extended release - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Antiflex
  • Công ty :
    Sản phẩm biệt dược : Banflex
  • Công ty :
    Sản phẩm biệt dược : Biorphen
  • Công ty :
    Sản phẩm biệt dược : Disipal
  • Công ty :
    Sản phẩm biệt dược : Flexoject
  • Công ty :
    Sản phẩm biệt dược : Mio-Rel
  • Công ty :
    Sản phẩm biệt dược : Myolin
  • Công ty :
    Sản phẩm biệt dược : Norflex
  • Công ty :
    Sản phẩm biệt dược : OrfenAce
  • Công ty :
    Sản phẩm biệt dược : Orfro
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01173
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=4601
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46506085
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07935
ChemSpider
http://www.chemspider.com/Chemical-Structure.4440.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0089-0221-10
PharmGKB
http://www.pharmgkb.org/drug/PA450715
Wikipedia
http://en.wikipedia.org/wiki/Orphenadrine
RxList
http://www.rxlist.com/cgi/generic/orphen.htm
Drugs.com
http://www.drugs.com/cdi/orphenadrine.html
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