Tìm theo
Ethopropazine
Các tên gọi khác (11 ) :
  • 10-(2-Diethylaminopropyl)phenothiazine
  • 10-[2-(Diethylamino)-1-propyl]phenothiazine
  • 10-[2-(Diethylamino)-2-methylethyl]phenothiazine
  • 10-[2-(Diethylamino)propyl]phenothiazine
  • 2-Diethylamino-1-propyl-N-dibenzoparathiazine
  • Ethopropazine
  • N,N-Diethyl-1-(10H-phenothiazin-10-yl)-2-propanamine
  • N,N-Diethyl-alpha-methyl-10H-phenothiazine-10-ethanamine
  • Profenamina
  • Profenamine
  • Profenaminum
muscarinic antagonists, histamine antagonists, adrenergic antagonists, antidyskinetics
Thuốc Gốc
Small Molecule
CAS: 1094-08-2
ATC: N04AA05
CTHH: C19H24N2S
PTK: 312.472
Ethopropazine (also known as profenamine hydrochloride) is a medication derived from phenothiazine. It is primarily used as an antidyskinetic to treat parkinsonism. It is sold under the trade names Parsidol in the United States and Parsidan in Canada.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C19H24N2S
Phân tử khối
312.472
Monoisotopic mass
312.166019468
InChI
InChI=1S/C19H24N2S/c1-4-20(5-2)15(3)14-21-16-10-6-8-12-18(16)22-19-13-9-7-11-17(19)21/h6-13,15H,4-5,14H2,1-3H3
InChI Key
InChIKey=CDOZDBSBBXSXLB-UHFFFAOYSA-N
IUPAC Name
diethyl[1-(10H-phenothiazin-10-yl)propan-2-yl]amine
Traditional IUPAC Name
ethopropazine
SMILES
CCN(CC)C(C)CN1C2=CC=CC=C2SC2=CC=CC=C12
Độ tan chảy
166-168
Độ hòa tan
0.693 mg/L
logP
5.2
logS
-4.8
pKa (Strongest Basic)
9.6
PSA
6.48 Å2
Refractivity
98 m3·mol-1
Polarizability
36.34 Å3
Rotatable Bond Count
5
H Bond Acceptor Count
2
H Bond Donor Count
0
Physiological Charge
1
Number of Rings
3
Bioavailability
1
Ghose Filter
true
Dược Lực Học : Ethopropazine, a phenothiazine and antidyskinetic, is used in the treatment of Parkinson's disease. By improving muscle control and reducing stiffness, this drug permits more normal movements of the body as the disease symptoms are reduced. It is also used to control severe reactions to certain medicines such as reserpine, phenothiazines, chlorprothixene, thiothixene, loxapine, and haloperidol. Unlike other NMDA antagonists, ethopropazine — because of its anticholinergic action — is largely devoid of neurotoxic side effects. Ethopropazine also has a slight antihistaminic and local anesthetic effect.
Cơ Chế Tác Dụng : Ethopropazine (also known as profenamine hydrochloride) is a medication derived from phenothiazine. It is primarily used as an antidyskinetic to treat parkinsonism. It is sold under the trade names Parsidol in the United States and Parsidan in Canada. Ethopropazine's antiparkinson action can be attributed to its anticholinergic properties. Ethopropazine partially blocks central (striatal) cholinergic receptors, thereby helping to balance cholinergic and dopaminergic activity in the basal ganglia; salivation may be decreased, and smooth muscle may be relaxed. Drug-induced extrapyramidal symptoms and those due to parkinsonism may be relieved, but tardive dyskinesia is not alleviated and may be aggravated by anticholinergic effects. Ethopropazine's local anesthetic effect is due to its antagonism of the NMDA glutamate receptor. Glutamate is recognized as an important transmitter in nociceptive pathways, and the N-methyl-D-aspartate (NMDA) subtype of the glutamate receptor, in particular, has been implicated in the mediation of neuropathic pain. Excessive release of glutamate at NMDA receptors on dorsal horn neurons of the spinal cord results in hyperactivation and hypersensitivity of these receptors (perceived as hyperalgesia), thought to be an integral feature of neuropathic pain.
Dược Động Học :
▧ Absorption :
Well-absorbed from the gastrointestinal tract.
▧ Protein binding :
93%
▧ Half Life :
1 to 2 hours
Độc Tính : Symptoms of overdose include severe clumsiness or unsteadiness, severe drowsiness, severe dryness of mouth, nose, or throat, fast heartbeat, shortness of breath or troubled breathing, and warmth, dryness, and flushing of skin.
Chỉ Định : For use in the treatment of Parkinson's disease and also used to control severe reactions to certain medicines such as reserpine.
Tương Tác Thuốc :
  • Bromocriptine The phenothiazine decreases the effect of bromocriptine
  • Cisapride Increased risk of cardiotoxicity and arrhythmias
  • Dexfenfluramine Decreased anorexic effect, may increase psychotic symptoms
  • Diethylpropion Decreased anorexic effect, may increase psychotic symptoms
  • Donepezil Possible antagonism of action
  • Fenfluramine Decreased anorexic effect, may increase psychotic symptoms
  • Galantamine Possible antagonism of action
  • Guanethidine Ethopropazine may decrease the effect of guanethidine.
  • Haloperidol The anticholinergic increases the risk of psychosis and tardive dyskinesia
  • Mazindol Decreased anorexic effect, may increase psychotic symptoms
  • Phentermine Decreased anorexic effect, may increase psychotic symptoms
  • Phenylpropanolamine Decreased anorexic effect, may increase psychotic symptoms
Liều Lượng & Cách Dùng : Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
  • Biệt dược thương mại : Parsitan 50 mg Tablet
    Giá bán buôn : USD >0.23
    Đơn vị tính : tablet
Nhà Sản Xuất
  • Công ty : Bayer
    Sản phẩm biệt dược : Dibutil
  • Công ty : Tanabe
    Sản phẩm biệt dược : Parkin
  • Công ty :
    Sản phẩm biệt dược : Parsidan
  • Công ty :
    Sản phẩm biệt dược : Parsidol
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00392
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=3290
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46507375
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D01118
ChemSpider
http://www.chemspider.com/Chemical-Structure.3174.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=8958
PharmGKB
http://www.pharmgkb.org/drug/PA449531
Wikipedia
http://en.wikipedia.org/wiki/Ethopropazine
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