Tìm theo
Montelukast
Các tên gọi khác (5 ) :
  • (R-(e))-1-(((1-(3-(2-(7-Chloro-2-quinolinyl)ethenyl)phenyl)-3-(2-(1-hydroxy-1-methylethyl)phenyl)propyl)thio)methyl)cyclopropaneacetic acid
  • 1-[[[(1 R)-1-[3-[(1e)-2-(7-chloro-2-Quinolinyl)ethenyl] phenyl]-3-[2-(1-hydroxy-1-methylethyl)phenyl]propyl]sulfanyl]methyl]cyclopropaneacetic acid
  • Montelukast
  • Montélukast
  • Montelukastum
Thuốc chống loạn nhịp
Thuốc Gốc
Small Molecule
CAS: 158966-92-8
ATC: R03DC03
ĐG : Advanced Pharmaceutical Services Inc.
CTHH: C35H36ClNO3S
PTK: 586.183
Montelukast is a leukotriene receptor antagonist (LTRA) used for the maintenance treatment of asthma and to relieve symptoms of seasonal allergies. It is usually administered orally. Montelukast blocks the action of leukotriene D4 on the cysteinyl leukotriene receptor CysLT1 in the lungs and bronchial tubes by binding to it. This reduces the bronchoconstriction otherwise caused by the leukotriene, and results in less inflammation. Because of its method of operation, it is not useful for the treatment of acute asthma attacks. Again because of its very specific locus of operation, it does not interact with other allergy medications such as theophylline. Montelukast is marketed in United States and many other countries by Merck & Co. with the brand name Singulair®. It is available as oral tablets, chewable tablets, and oral granules. In India and other countries, it is also marketed under the brand name Montair®, produced by Indian company Cipla.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C35H36ClNO3S
Phân tử khối
586.183
Monoisotopic mass
585.21044242
InChI
InChI=1S/C35H36ClNO3S/c1-34(2,40)30-9-4-3-7-25(30)13-17-32(41-23-35(18-19-35)22-33(38)39)27-8-5-6-24(20-27)10-15-29-16-12-26-11-14-28(36)21-31(26)37-29/h3-12,14-16,20-21,32,40H,13,17-19,22-23H2,1-2H3,(H,38,39)/b15-10+/t32-/m1/s1
InChI Key
InChIKey=UCHDWCPVSPXUMX-TZIWLTJVSA-N
IUPAC Name
2-[1-({[(1R)-1-{3-[(E)-2-(7-chloroquinolin-2-yl)ethenyl]phenyl}-3-[2-(2-hydroxypropan-2-yl)phenyl]propyl]sulfanyl}methyl)cyclopropyl]acetic acid
Traditional IUPAC Name
montelukast
SMILES
OC(=O)CC1(CC1)CS[C@H](CCC1=CC=CC=C1C(O)(C)C)C1=CC=CC(\C=C\C2=NC3=C(C=CC(Cl)=C3)C=C2)=C1
Độ hòa tan
8.20e-06 g/l
logP
7.9
logS
-7.8
pKa (strongest acidic)
4.4
pKa (Strongest Basic)
3.12
PSA
70.42 Å2
Refractivity
169.5 m3·mol-1
Polarizability
66.36 Å3
Rotatable Bond Count
12
H Bond Acceptor Count
4
H Bond Donor Count
2
Physiological Charge
-1
Number of Rings
5
Bioavailability
0
MDDR-Like Rule
true
Dược Lực Học : Montelukast, like zafirlukast, is a leukotriene receptor antagonist used as an alternative to anti-inflammatory medications in the management and chronic treatment of asthma and exercise-induced bronchospasm (EIB). Unlike zafirlukast, montelukast does not inhibit CYP2C9 or CYP3A4 and is, therefore, not expected to affect the hepatic clearance of drugs metabolized by these enzymes.
Cơ Chế Tác Dụng : Montelukast is a leukotriene receptor antagonist (LTRA) used for the maintenance treatment of asthma and to relieve symptoms of seasonal allergies. It is usually administered orally. Montelukast blocks the action of leukotriene D4 on the cysteinyl leukotriene receptor CysLT1 in the lungs and bronchial tubes by binding to it. This reduces the bronchoconstriction otherwise caused by the leukotriene, and results in less inflammation. Because of its method of operation, it is not useful for the treatment of acute asthma attacks. Again because of its very specific locus of operation, it does not interact with other allergy medications such as theophylline. Montelukast is marketed in United States and many other countries by Merck & Co. with the brand name Singulair®. It is available as oral tablets, chewable tablets, and oral granules. In India and other countries, it is also marketed under the brand name Montair®, produced by Indian company Cipla. Montelukast selectively antagonizes leukotriene D4 (LTD4) at the cysteinyl leukotriene receptor, CysLT1, in the human airway. Montelukast inhibits the actions of LTD4 at the CysLT1 receptor, preventing airway edema, smooth muscle contraction, and enhanced secretion of thick, viscous mucus.
Dược Động Học :
▧ Absorption :
Rapidly absorbed following oral administration (bioavailability is 64%)
▧ Volume of Distribution :
* 8 to 11 L
▧ Protein binding :
99% (to plasma proteins)
▧ Metabolism :
Hepatic
▧ Route of Elimination :
Coupled with estimates of montelukast oral bioavailability, this indicates that montelukast and its metabolites are excreted almost exclusively via the bile.
▧ Half Life :
2.7-5.5 hours
▧ Clearance :
* 45 mL/min [healthy adults]
Độc Tính : Side effects include headache, abdominal or stomach pain, cough, dental pain, dizziness, fever, heartburn, skin rash, stuffy nose, weakness or unusual tiredness.
Chỉ Định : For the treatment of asthma
Tương Tác Thuốc :
  • Tolbutamide Tolbutamide, a strong CYP2C9 inhibitor, may decrease the metabolism and clearance of Montelukast. Consider alternate therapy or monitor for changes in Montelukast therapeutic and adverse effects if Tolbutamide is initiated, discontinued or dose changed.
Liều Lượng & Cách Dùng : Granule - Oral
Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Lukotas
  • Công ty : Allenge
    Sản phẩm biệt dược : Molly
  • Công ty : Beximco
    Sản phẩm biệt dược : Monocast
  • Công ty :
    Sản phẩm biệt dược : Monteflo
  • Công ty :
    Sản phẩm biệt dược : Montelo-10
  • Công ty : Square
    Sản phẩm biệt dược : Montene
  • Công ty : Santa-Farma
    Sản phẩm biệt dược : Respaire
  • Công ty : Merck
    Sản phẩm biệt dược : Singulair
  • Công ty : Sandoz
    Sản phẩm biệt dược : Surfair
  • Công ty : Actavis
    Sản phẩm biệt dược : Telumantes
  • Công ty : Searle
    Sản phẩm biệt dược : Ventek
  • Công ty : Gutis
    Sản phẩm biệt dược : Ventilar
  • Công ty : Unimed
    Sản phẩm biệt dược : Xalar
  • Công ty : Bilim
    Sản phẩm biệt dược : Zespira
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00471
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=5281040
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46505585
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07482
ChemSpider
http://www.chemspider.com/Chemical-Structure.4444507.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0006-0275-82
PharmGKB
http://www.pharmgkb.org/drug/PA450546
Wikipedia
http://en.wikipedia.org/wiki/Montelukast
RxList
http://www.rxlist.com/cgi/generic3/monteluk.htm
Drugs.com
http://www.drugs.com/cdi/montelukast.html
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