Tìm theo
Clemastine
Các tên gọi khác (6 ) :
  • (+)-(2R)-2-(2-(((R)-P-chloro-alpha-Methyl-alpha-phenylbenzyl)oxy)ethyl)-1-methylpyrrolidine
  • (+)-(2R)-2-[2-[[(R)-P-chloro-alpha-Methyl-alpha-phenylbenzyl]oxy]ethyl]-1-methylpyrrolidine
  • Clemastina
  • Clemastine
  • Clemastinum
  • Meclastin
Thuốc chống dị ứng
Thuốc Gốc
Small Molecule
CAS: 15686-51-8
ATC: R06AA04, D04AA14
ĐG : Apotex Inc. , http://www.apotex.com
CTHH: C21H26ClNO
PTK: 343.89
An ethanolamine-derivative, first generation histamine H1 antagonist used in hay fever, rhinitis, allergic skin conditions, and pruritus. It causes drowsiness. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C21H26ClNO
Phân tử khối
343.89
Monoisotopic mass
343.170292166
InChI
InChI=1S/C21H26ClNO/c1-21(17-7-4-3-5-8-17,18-10-12-19(22)13-11-18)24-16-14-20-9-6-15-23(20)2/h3-5,7-8,10-13,20H,6,9,14-16H2,1-2H3/t20-,21-/m1/s1
InChI Key
InChIKey=YNNUSGIPVFPVBX-NHCUHLMSSA-N
IUPAC Name
(2R)-2-{2-[(1R)-1-(4-chlorophenyl)-1-phenylethoxy]ethyl}-1-methylpyrrolidine
Traditional IUPAC Name
clemastine
SMILES
CN1CCC[C@@H]1CCO[C@](C)(C1=CC=CC=C1)C1=CC=C(Cl)C=C1
Độ tan chảy
178 °C (hydrogen fumarate formulation)
Độ hòa tan
Soluble (hydrogen fumarate formulation)
logP
5.2
logS
-5.9
pKa (Strongest Basic)
9.55
PSA
12.47 Å2
Refractivity
101.65 m3·mol-1
Polarizability
39.06 Å3
Rotatable Bond Count
6
H Bond Acceptor Count
2
H Bond Donor Count
0
Physiological Charge
1
Number of Rings
3
Bioavailability
1
Rule of Five
true
Ghose Filter
true
MDDR-Like Rule
true
Dược Lực Học : Clemastine is an antihistamine with anticholinergic (drying) and sedative side effects. Antihistamines competitively antagonize various physiological effects of histamine including increased capillary permeability and dilatation, the formation of edema, the "flare" and "itch" response, and gastrointestinal and respiratory smooth muscle constriction. Within the vascular tree, H1- receptor antagonists inhibit both the vasoconstrictor and vasodilator effects of histamine. Depending on the dose, H1- receptor antagonists can produce CNS stimulation or depression. Most antihistamines exhibit central and/or peripheral anticholinergic activity. Antihistamines act by competitively blocking H1- receptor sites. Antihistamines do not pharmacologically antagonize or chemically inactivate histamine, nor do they prevent the release of histamine.
Cơ Chế Tác Dụng : An ethanolamine-derivative, first generation histamine H1 antagonist used in hay fever, rhinitis, allergic skin conditions, and pruritus. It causes drowsiness. [PubChem] Clemastine is a selective histamine H1 antagonist and binds to the histamine H1 receptor. This blocks the action of endogenous histamine, which subsequently leads to temporary relief of the negative symptoms brought on by histamine.
Dược Động Học :
▧ Absorption :
Rapidly absorbed from the gastrointestinal tract.
▧ Metabolism :
Antihistamines appear to be metabolized in the liver chiefly via mono- and didemethylation and glucuronide conjugation.
▧ Route of Elimination :
Urinary excretion is the major mode of elimination.
Độc Tính : Oral LD50 in rat and mouse is 3550 mg/kg and 730 mg/kg, respectively. Antihistamine overdosage reactions may vary from central nervous system depression to stimulation. In children, stimulation predominates initially in a syndrome which may include excitement, hallucinations, ataxia, incoordination, muscle twitching, athetosis, hyperthermia, cyanosis convulsions, tremors, and hyperreflexia followed by postictal depression and cardio-respiratory arrest. Convulsions in children may be preceded by mild depression. Dry mouth, fixed dilated pupils, flushing of the face, and fever are common. In adults, CNS depression, ranging from drowsiness to coma, is more common.
Chỉ Định : For the relief of symptoms associated with allergic rhinitis such as sneezing, rhinorrhea, pruritus and acrimation. Also for the management of mild, uncomplicated allergic skin manifestations of urticaria and angioedema. Used as self-medication for temporary relief of symptoms associated with the common cold.
Tương Tác Thuốc :
  • Donepezil Possible antagonism of action
  • Galantamine Possible antagonism of action
  • Rivastigmine Possible antagonism of action
  • Tacrine The therapeutic effects of the central acetylcholinesterase inhibitor, Tacrine, and/or the anticholinergic, Clemastine, 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 Clemastine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Triprolidine Concomitant therapy with triprolidine and clemastine, two anticholinergics and CNS depressants, may result in additive adverse/toxic effects. Monitor for enhanced anticholinergic and CNS depressant effects during concomitant therapy.
  • Trospium Trospium and Clemastine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Liều Lượng & Cách Dùng : Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Sản phẩm biệt dược : Agasten
  • Công ty :
    Sản phẩm biệt dược : Allerhist-1
  • Công ty : Novartis
    Sản phẩm biệt dược : Tavegil
  • Công ty : Novartis
    Sản phẩm biệt dược : Tavegyl
  • Công ty : Novartis
    Sản phẩm biệt dược : Tavist
  • Công ty : Novartis
    Sản phẩm biệt dược : Tavist-1
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00283
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=26987
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46506492
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00666
ChemSpider
http://www.chemspider.com/Chemical-Structure.25129.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50253157
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0781-1359-01
PharmGKB
http://www.pharmgkb.org/drug/PA164776997
Wikipedia
http://en.wikipedia.org/wiki/Clemastine
RxList
http://www.rxlist.com/cgi/generic3/clemast.htm
Drugs.com
http://www.drugs.com/cdi/clemastine.html
... loading
... loading