Tìm theo
Terfenadine
Các tên gọi khác (6 ) :
  • (RS)-1-(4-tert-butylphenyl)-4-{4-[hydroxy(diphenyl)methyl]piperidin-1-yl}-butan-1-ol
  • Terfenadin
  • Terfenadina
  • Terfénadine
  • Terfenadine
  • Terfenadinum
Thuốc chống loạn nhịp
Thuốc Gốc
Small Molecule
CAS: 50679-08-8
ATC: R06AX12
ĐG : Pharmaceutical Utilization Management Program VA Inc.
CTHH: C32H41NO2
PTK: 471.6734
In the U.S., Terfenadine was superseded by fexofenadine in the 1990s due to the risk of cardiac arrhythmia caused by QT interval prolongation.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C32H41NO2
Phân tử khối
471.6734
Monoisotopic mass
471.313729561
InChI
InChI=1S/C32H41NO2/c1-31(2,3)26-18-16-25(17-19-26)30(34)15-10-22-33-23-20-29(21-24-33)32(35,27-11-6-4-7-12-27)28-13-8-5-9-14-28/h4-9,11-14,16-19,29-30,34-35H,10,15,20-24H2,1-3H3
InChI Key
InChIKey=GUGOEEXESWIERI-UHFFFAOYSA-N
IUPAC Name
1-(4-tert-butylphenyl)-4-[4-(hydroxydiphenylmethyl)piperidin-1-yl]butan-1-ol
Traditional IUPAC Name
terfenadine
SMILES
CC(C)(C)C1=CC=C(C=C1)C(O)CCCN1CCC(CC1)C(O)(C1=CC=CC=C1)C1=CC=CC=C1
Độ tan chảy
147 °C
Độ hòa tan
0.0963 mg/L (at 25 °C)
logP
7.1
logS
-6
pKa (strongest acidic)
13.2
pKa (Strongest Basic)
9.02
PSA
43.7 Å2
Refractivity
146.27 m3·mol-1
Polarizability
56.45 Å3
Rotatable Bond Count
9
H Bond Acceptor Count
3
H Bond Donor Count
2
Physiological Charge
1
Number of Rings
4
Bioavailability
1
MDDR-Like Rule
true
Dược Lực Học : Terfenadine, an H1-receptor antagonist antihistamine, is similar in structure to astemizole and haloperidol, a butyrophenone antipsychotic. The active metabolite of terfenadine is fexofenadine.
Cơ Chế Tác Dụng : In the U.S., Terfenadine was superseded by fexofenadine in the 1990s due to the risk of cardiac arrhythmia caused by QT interval prolongation. Terfenadine competes with histamine for binding at H1-receptor sites in the GI tract, uterus, large blood vessels, and bronchial muscle. This reversible binding of terfenadine to H1-receptors suppresses the formation of edema, flare, and pruritus resulting from histaminic activity. As the drug does not readily cross the blood-brain barrier, CNS depression is minimal.
Dược Động Học :
▧ Absorption :
On the basis of a mass balance study using 14C labeled terfenadine the oral absorption of terfenadine was estimated to be at least 70%
▧ Protein binding :
70%
▧ Metabolism :
Hepatic
▧ Half Life :
3.5 hours
Độc Tính : Mild (e.g., headache, nausea, confusion), but adverse cardiac events including cardiac arrest, ventricular arrhythmias including torsades de pointes and QT prolongation have been reported. LD50=mg/kg (orally in mice)
Chỉ Định : For the treatment of allergic rhinitis, hay fever, and allergic skin disorders.
Tương Tác Thuốc :
  • Acetophenazine Increased risk of cardiotoxicity and arrhythmias
  • Alimemazine Increased risk of cardiotoxicity and arrhythmias
  • Amiodarone Increased risk of cardiotoxicity and arrhythmias
  • Amitriptyline Increased risk of cardiotoxicity and arrhythmias
  • Amoxapine Increased risk of cardiotoxicity and arrhythmias
  • Amprenavir Increased risk of cardiotoxicity and arrhythmias
  • Aprepitant Increased risk of cardiotoxicity and arrhythmias
  • Bepridil Increased risk of cardiotoxicity and arrhythmias
  • Chlorpromazine Increased risk of cardiotoxicity and arrhythmias
  • Cimetidine Increased risk of cardiotoxicity and arrhythmias
  • Cisapride Increased risk of cardiotoxicity and arrhythmias
  • Clarithromycin Increased risk of cardiotoxicity and arrhythmias
  • Clomipramine Increased risk of cardiotoxicity and arrhythmias
  • Delavirdine Increased risk of cardiotoxicity and arrhythmias
  • Desipramine Increased risk of cardiotoxicity and arrhythmias
  • Diltiazem Increased risk of cardiotoxicity and arrhythmias
  • Disopyramide Increased risk of cardiotoxicity and arrhythmias
  • Doxepin Increased risk of cardiotoxicity and arrhythmias
  • Efavirenz Increased risk of cardiotoxicity and arrhythmias
  • Erythromycin Increased risk of cardiotoxicity and arrhythmias
  • Flecainide Increased risk of cardiotoxicity and arrhythmias
  • Fluconazole Increased risk of cardiotoxicity and arrhythmias
  • Fluoxetine Increased risk of cardiotoxicity and arrhythmias
  • Fluphenazine Increased risk of cardiotoxicity and arrhythmias
  • Fluvoxamine Increased risk of cardiotoxicity and arrhythmias
  • Fosamprenavir Increased risk of cardiotoxicity and arrhythmias
  • Grepafloxacin Increased risk of cardiotoxicity and arrhythmias
  • Imipramine Increased risk of cardiotoxicity and arrhythmias
  • Indinavir Increased risk of cardiotoxicity and arrhythmias
  • Itraconazole Increased risk of cardiotoxicity and arrhythmias
  • Josamycin Increased risk of cardiotoxicity and arrhythmias
  • Ketoconazole Increased risk of cardiotoxicity and arrhythmias
  • Mesoridazine Increased risk of cardiotoxicity and arrhythmias
  • Methdilazine Increased risk of cardiotoxicity and arrhythmias
  • Methotrimeprazine Increased risk of cardiotoxicity and arrhythmias
  • Mexiletine Increased risk of cardiotoxicity and arrhythmias
  • Mibefradil Increased risk of cardiotoxicity and arrhythmias
  • Nefazodone Increased risk of cardiotoxicity and arrhythmias
  • Nelfinavir Increased risk of cardiotoxicity and arrhythmias
  • Nicardipine Increased risk of cardiotoxicity and arrhythmias
  • Nortriptyline Increased risk of cardiotoxicity and arrhythmias
  • Perphenazine Increased risk of cardiotoxicity and arrhythmias
  • Posaconazole Contraindicated co-administration
  • Procainamide Increased risk of cardiotoxicity and arrhythmias
  • Prochlorperazine Increased risk of cardiotoxicity and arrhythmias
  • Promazine Increased risk of cardiotoxicity and arrhythmias
  • Promethazine Increased risk of cardiotoxicity and arrhythmias
  • Propafenone Increased risk of cardiotoxicity and arrhythmias.
  • Propericiazine Increased risk of cardiotoxicity and arrhythmias
  • Propiomazine Increased risk of cardiotoxicity and arrhythmias
  • Protriptyline Increased risk of cardiotoxicity and arrhythmias
  • Quinidine Increased risk of cardiotoxicity and arrhythmias
  • Quinine Increased risk of cardiotoxicity and arrhythmias
  • Quinupristin This combination presents an increased risk of toxicity
  • Ritonavir Increased risk of cardiotoxicity and arrhythmias
  • Saquinavir Increased risk of cardiotoxicity and arrhythmias
  • Sotalol Increased risk of cardiotoxicity and arrhythmias
  • Sparfloxacin Increased risk of cardiotoxicity and arrhythmias
  • Telavancin Additive QTc-prolongation may occur. Concomitant therapy should be avoided.
  • Telithromycin Increased risk of cardiotoxicity and arrhythmias
  • Thiethylperazine Increased risk of cardiotoxicity and arrhythmias
  • Thioridazine Increased risk of cardiotoxicity and arrhythmias
  • Tipranavir Tipranavir, co-administered with Ritonavir, may increase the plasma concentration of Terfenadine. Concomitant therapy is contraindicated.
  • Tocainide Increased risk of cardiotoxicity and arrhythmias
  • Trifluoperazine Increased risk of cardiotoxicity and arrhythmias
  • Triflupromazine Increased risk of cardiotoxicity and arrhythmias
  • Trimipramine Increased risk of cardiotoxicity and arrhythmias
  • Troleandomycin Increased risk of cardiotoxicity and arrhythmias
  • Verapamil Increased risk of cardiotoxicity and arrhythmias
  • Voriconazole Increased risk of cardiotoxicity and arrhythmias
Liều Lượng & Cách Dùng : Tablet - Oral
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty : Galenika
    Sản phẩm biệt dược : Bronal
  • Công ty : Micro Labs
    Sản phẩm biệt dược : Daylert
  • Công ty :
    Sản phẩm biệt dược : Seldane
  • Công ty : Novartis
    Sản phẩm biệt dược : Servinin
  • Công ty :
    Sản phẩm biệt dược : Teldane
  • Công ty : Cipla
    Sản phẩm biệt dược : Terfed
  • Công ty : Aliud
    Sản phẩm biệt dược : Terfenadin AL
  • Sản phẩm biệt dược : Terfenadine FLX
  • Công ty : Interbat
    Sản phẩm biệt dược : Terfin
  • Công ty : Dunar
    Sản phẩm biệt dược : Ternadin
  • Công ty : Ranbaxy
    Sản phẩm biệt dược : Trexyl
  • Công ty :
    Sản phẩm biệt dược : Triludan
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00342
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=5405
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46507007
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07463
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00521
ChemSpider
http://www.chemspider.com/Chemical-Structure.5212.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50017376
PharmGKB
http://www.pharmgkb.org/drug/PA451619
Wikipedia
http://en.wikipedia.org/wiki/Terfenadine
RxList
http://www.rxlist.com/cgi/generic/terfen.htm
Drugs.com
http://www.drugs.com/mtm/terfenadine.html
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