Tìm theo
Chlorphenamine
Các tên gọi khác (17 ) :
  • 1-(p-chlorophenyl)-1-(2-pyridyl)-3-dimethylaminopropane
  • 1-(P-Chlorophenyl)-1-(2-pyridyl)-3-N,N-dimethylpropylamine
  • 2-[P-chloro-alpha-[2-(dimethylamino)Ethyl]benzyl]pyridine
  • 3-(P-Chlorophenyl)-3-(2-pyridyl)-N,N-dimethylpropylamine
  • Chlorophenylpyridamine
  • Chlorphenamin
  • Chlorphenamine
  • Chlorphenaminum
  • Chlorpheniramine
  • Chlorpheniraminum
  • Clofeniramina
  • Clorfenamina
  • Clorfeniramina
  • gamma-(4-Chlorophenyl)-gamma-(2-pyridyl)propyldimethylamine
  • gamma-(4-Chlorophenyl)-N,N-dimethyl-2-pyridinepropanamine
  • Haynon
  • γ-(4-chlorophenyl)-γ-(2-pyridyl)propyldimethylamine
histamine h1 antagonists, histamine antagonists
Thuốc Gốc
Small Molecule
CAS: 132-22-9
ATC: R06AB02, R06AB04
ĐG : Amend
CTHH: C16H19ClN2
PTK: 274.788
A histamine H1 antagonist used in allergic reactions, hay fever, rhinitis, urticaria, and asthma. It has also been used in veterinary applications. One of the most widely used of the classical antihistaminics, it generally causes less drowsiness and sedation than promethazine. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C16H19ClN2
Phân tử khối
274.788
Monoisotopic mass
274.123676325
InChI
InChI=1S/C16H19ClN2/c1-19(2)12-10-15(16-5-3-4-11-18-16)13-6-8-14(17)9-7-13/h3-9,11,15H,10,12H2,1-2H3
InChI Key
InChIKey=SOYKEARSMXGVTM-UHFFFAOYSA-N
IUPAC Name
[3-(4-chlorophenyl)-3-(pyridin-2-yl)propyl]dimethylamine
Traditional IUPAC Name
chlorpheniramine
SMILES
CN(C)CCC(C1=CC=C(Cl)C=C1)C1=CC=CC=N1
Độ sôi
142 °C
Độ hòa tan
5500 mg/L (at 37 °C)
logP
3.38
logS
-3.7
pKa (Strongest Basic)
9.47
PSA
16.13 Å2
Refractivity
80.85 m3·mol-1
Polarizability
30.82 Å3
Rotatable Bond Count
5
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
9.13 (at 25 °C)
Dược Lực Học : In allergic reactions an allergen interacts with and cross-links surface IgE antibodies on mast cells and basophils. Once the mast cell-antibody-antigen complex is formed, a complex series of events occurs that eventually leads to cell-degranulation and the release of histamine (and other chemical mediators) from the mast cell or basophil. Once released, histamine can react with local or widespread tissues through histamine receptors. Histamine, acting on H1-receptors, produces pruritis, vasodilatation, hypotension, flushing, headache, tachycardia, and bronchoconstriction. Histamine also increases vascular permeability and potentiates pain. Chlorpheniramine, is a histamine H1 antagonist (or more correctly, an inverse histamine agonist) of the alkylamine class. It competes with histamine for the normal H1-receptor sites on effector cells of the gastrointestinal tract, blood vessels and respiratory tract. It provides effective, temporary relief of sneezing, watery and itchy eyes, and runny nose due to hay fever and other upper respiratory allergies.
Cơ Chế Tác Dụng : A histamine H1 antagonist used in allergic reactions, hay fever, rhinitis, urticaria, and asthma. It has also been used in veterinary applications. One of the most widely used of the classical antihistaminics, it generally causes less drowsiness and sedation than promethazine. [PubChem] Chlorpheniramine 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 :
Well absorbed in the gastrointestinal tract.
▧ Protein binding :
72%
▧ Metabolism :
Primarily hepatic via Cytochrome P450 (CYP450) enzymes.
▧ Half Life :
21-27 hours
Độc Tính : Oral LD50 (rat): 306 mg/kg; Oral LD50 (mice): 130 mg/kg; Oral LD50 (guinea pig): 198 mg/kg [Registry of Toxic Effects of Chemical Substances. Ed. D. Sweet, US Dept. of Health & Human Services: Cincinatti, 2010.] Also a mild reproductive toxin to women of childbearing age.
Chỉ Định : For the treatment of rhinitis, urticaria, allergy, common cold, asthma and hay fever.
Tương Tác Thuốc :
  • Donepezil Possible antagonism of action
  • Ethotoin The antihistamine increases the effect of hydantoin
  • Fosphenytoin The antihistamine increases the effect of hydantoin
  • Galantamine Possible antagonism of action
  • Mephenytoin The antihistamine increases the effect of hydantoin
  • Phenytoin The antihistamine increases the effect of hydantoin
  • Rivastigmine Possible antagonism of action
  • Tacrine The therapeutic effects of the central acetylcholinesterase inhibitor, Tacrine, and/or the anticholinergic, Chlorpheniramine, 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.
  • Telithromycin Telithromycin may reduce clearance of Chlorpheniramine. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Chlorpheniramine if Telithromycin is initiated, discontinued or dose changed.
  • Trimethobenzamide Trimethobenzamide and Chlorpheniramine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Triprolidine Triprolidine and Chlorpheniramine, 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 Chlorpheniramine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Voriconazole Voriconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of chlorpheniramine by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of chlorpheniramine if voriconazole is initiated, discontinued or dose changed.
Liều Lượng & Cách Dùng : Syrup - Oral
Tablet - Oral
Tablet, extended release - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : Rugby
    Sản phẩm biệt dược : Aller-Chlor
  • Công ty :
    Sản phẩm biệt dược : Chlo-Amine
  • Công ty : Schering-Plough
    Sản phẩm biệt dược : Chlor-Trimeton
  • Công ty :
    Sản phẩm biệt dược : Chlor-Tripolon
  • Công ty :
    Sản phẩm biệt dược : Haynon
  • Công ty : GlaxoSmithKline
    Sản phẩm biệt dược : Piriton
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01114
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=2725
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46508253
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C06905
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D07398
ChemSpider
http://www.chemspider.com/Chemical-Structure.2624.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=35938
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/60432-539-04
PharmGKB
http://www.pharmgkb.org/drug/PA448960
Wikipedia
http://en.wikipedia.org/wiki/Chlorpheniramine
RxList
http://www.rxlist.com/cgi/generic/chlorpheniramine.htm
Drugs.com
http://www.drugs.com/cdi/chlorpheniramine.html
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