Tìm theo
Fexofenadine
Các tên gọi khác (6 ) :
  • 4-(1-Hydroxy-4-(4-(hydroxydiphenylmethyl)-1-piperidinyl)butyl)-alpha,alpha-dimethylbenzeneacetic acid
  • Carboxyterfenadine
  • Fexofenadine
  • Terfenadine acid metabolite
  • Terfenadine carboxylate
  • Terfenadine-COOH
Thuốc chống dị ứng & dùng trong các trường hợp quá mẫn
Thuốc Gốc
Small Molecule
CAS: 83799-24-0
ATC: R06AX26
ĐG : Amerisource Health Services Corp. , http://www.amerisourcebergen.com
CTHH: C32H39NO4
PTK: 501.6564
Fexofenadine hydrochloride (Allegra) is an antihistamine drug used in the treatment of hayfever and similar allergy symptoms. It was developed as a successor of and alternative to terfenadine. Fexofenadine, like other second and third-generation antihistamines, does not readily pass through the blood-brain barrier, and so causes less drowsiness than first-generation histamine-receptor antagonists.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C32H39NO4
Phân tử khối
501.6564
Monoisotopic mass
501.287908741
InChI
InChI=1S/C32H39NO4/c1-31(2,30(35)36)25-17-15-24(16-18-25)29(34)14-9-21-33-22-19-28(20-23-33)32(37,26-10-5-3-6-11-26)27-12-7-4-8-13-27/h3-8,10-13,15-18,28-29,34,37H,9,14,19-23H2,1-2H3,(H,35,36)
InChI Key
InChIKey=RWTNPBWLLIMQHL-UHFFFAOYSA-N
IUPAC Name
2-(4-{1-hydroxy-4-[4-(hydroxydiphenylmethyl)piperidin-1-yl]butyl}phenyl)-2-methylpropanoic acid
Traditional IUPAC Name
fexofenadine
SMILES
CC(C)(C(O)=O)C1=CC=C(C=C1)C(O)CCCN1CCC(CC1)C(O)(C1=CC=CC=C1)C1=CC=CC=C1
Độ tan chảy
142.5 °C
Độ hòa tan
Slightly soluble
logP
5.6
logS
-5.3
pKa (strongest acidic)
4.04
pKa (Strongest Basic)
9.01
PSA
81 Å2
Refractivity
147.98 m3·mol-1
Polarizability
57.42 Å3
Rotatable Bond Count
10
H Bond Acceptor Count
5
H Bond Donor Count
3
Physiological Charge
0
Number of Rings
4
Bioavailability
1
MDDR-Like Rule
true
Dược Lực Học : Fexofenadine is a second-generation, long lasting H1-receptor antagonist (antihistamine) which has a selective and peripheral H1-antagonist action. Histamine is a chemical that causes many of the signs that are part of allergic reactions, such as the swelling of tissues. Histamine is released from histamine-storing cells (mast cells) and attaches to other cells that have receptors for histamine. The attachment of the histamine to the receptors causes the cell to be "activated," releasing other chemicals which produce the effects that we associate with allergy. Fexofenadine blocks one type of receptor for histamine (the H1 receptor) and thus prevents activation of cells by histamine. Unlike most other antihistamines, Fexofenadine does not enter the brain from the blood and, therefore, does not cause drowsiness. Fexofenadine lacks the cardiotoxic potential of terfenadine, since it does not block the potassium channel involved in repolarization of cardiac cells.
Cơ Chế Tác Dụng : Fexofenadine hydrochloride (Allegra) is an antihistamine drug used in the treatment of hayfever and similar allergy symptoms. It was developed as a successor of and alternative to terfenadine. Fexofenadine, like other second and third-generation antihistamines, does not readily pass through the blood-brain barrier, and so causes less drowsiness than first-generation histamine-receptor antagonists. Like other H1-blockers, Fexofenadine competes with free histamine for binding at H1-receptors in the GI tract, large blood vessels, and bronchial smooth muscle. This blocks the action of endogenous histamine, which subsequently leads to temporary relief of the negative symptoms (eg. nasal congestion, watery eyes) brought on by histamine. Fexofenadine exhibits no anticholinergic, antidopaminergic, alpha1-adrenergic or beta-adrenergic-receptor blocking effects.
Dược Động Học :
▧ Absorption :
33%
▧ Protein binding :
60%-70%
▧ Metabolism :
Approximately 5% of the total dose is metabolized, by cytochrome P450 3A4 and by intestinal microflora.
▧ Half Life :
14.4 hours
Độc Tính : Side effects include dizziness, drowsiness, and dry mouth.
Chỉ Định : For management of Seasonal allergic rhinitis
Tương Tác Thuốc :
  • Cisapride Increased risk of cardiotoxicity and arrhythmias
  • Tacrine The therapeutic effects of the central acetylcholinesterase inhibitor, Tacrine, and/or the anticholinergic, Fexofenadine, 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 Fexofenadine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Triprolidine Triprolidine and Fexofenadine, 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 Fexofenadine, 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
  • Công ty :
    Sản phẩm biệt dược : Allegra
  • Công ty :
    Sản phẩm biệt dược : Fastofen
  • Công ty :
    Sản phẩm biệt dược : Fexidine
  • Công ty :
    Sản phẩm biệt dược : Telfast
  • Công ty :
    Sản phẩm biệt dược : Vifas
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00950
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=3348
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46504676
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C06999
ChemSpider
http://www.chemspider.com/Chemical-Structure.3231.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=22874
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0339-6461-11
PharmGKB
http://www.pharmgkb.org/drug/PA449621
Wikipedia
http://en.wikipedia.org/wiki/Fexofenadine
RxList
http://www.rxlist.com/cgi/generic/fexofen.htm
Drugs.com
http://www.drugs.com/cdi/fexofenadine.html
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