Tìm theo
Valdecoxib
Thuốc giảm đau, hạ sốt, chống viêm không steroid, điều trị Gút và các bệnh xương khớp
Thuốc Gốc
Small Molecule
CAS: 181695-72-7
ATC: M01AH03
ĐG : Cardinal Health , http://www.cardinal.com
CTHH: C16H14N2O3S
PTK: 314.359
Valdecoxib was removed from the Canadian, U.S., and E.U. markets in 2005 due to concerns about possible increased risk of heart attack and stroke.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C16H14N2O3S
Phân tử khối
314.359
Monoisotopic mass
314.072513014
InChI
InChI=1S/C16H14N2O3S/c1-11-15(12-7-9-14(10-8-12)22(17,19)20)16(18-21-11)13-5-3-2-4-6-13/h2-10H,1H3,(H2,17,19,20)
InChI Key
InChIKey=LNPDTQAFDNKSHK-UHFFFAOYSA-N
IUPAC Name
4-(5-methyl-3-phenyl-1,2-oxazol-4-yl)benzene-1-sulfonamide
Traditional IUPAC Name
valdecoxib
SMILES
CC1=C(C(=NO1)C1=CC=CC=C1)C1=CC=C(C=C1)S(N)(=O)=O
Độ hòa tan
3.48e-02 g/l
logP
3.2
logS
-4
pKa (strongest acidic)
10.06
pKa (Strongest Basic)
0.42
PSA
86.19 Å2
Refractivity
84.71 m3·mol-1
Polarizability
31.76 Å3
Rotatable Bond Count
3
H Bond Acceptor Count
3
H Bond Donor Count
1
Physiological Charge
0
Number of Rings
3
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Valdecoxib, a selective cyclooxygenase-2 (COX-2) inhibitor, is classified as a nonsteroidal anti-inflammatory drug (NSAID). Valdecoxib is used for its anti-inflammatory, analgesic, and antipyretic activities in the management of osteoarthritis (OA) and for the treatment of dysmenorrhea or acute pain. Unlike celecoxib, valdecoxib lacks a sulfonamide chain and does not require CYP450 enzymes for metabolism.
Cơ Chế Tác Dụng : Valdecoxib was removed from the Canadian, U.S., and E.U. markets in 2005 due to concerns about possible increased risk of heart attack and stroke. Both COX-1 and COX-2 catalyze the conversion of arachidonic acid to prostaglandin (PG) H2, the precursor of PGs and thromboxane. Valdecoxib selectively inhibits the cyclooxygenase-2 (COX-2) enzyme, important for the mediation of inflammation and pain. Unlike non-selective NSAIDs, valdecoxib does not inhibit platelet aggregation.
Dược Động Học :
▧ Absorption :
Oral bioavailability is 83%.
▧ Volume of Distribution :
* 86 L
▧ Protein binding :
98%
▧ Metabolism :
Hepatic (involves CYP3A4 and 2C9)
▧ Route of Elimination :
Valdecoxib is eliminated predominantly via hepatic metabolism with less than 5% of the dose excreted unchanged in the urine and feces. About 70% of the dose is excreted in the urine as metabolites, and about 20% as valdecoxib N-glucuronide.
▧ Half Life :
8-11 hours
▧ Clearance :
* oral cl=6 L/h * 6 – 7 L/h [In patients undergoing hemodialysis] * 6 – 7 L/h [healthy elderly subjects]
Độc Tính : Symptoms following acute NSAID overdoses are usually limited to lethargy, drowsiness, nausea, vomiting, and epigastric pain, which are generally reversible with supportive care. Gastrointestinal bleeding can occur. Hypertension, acute renal failure, respiratory depression and coma may occur, but are rare.
Chỉ Định : For the treatment of osteoarthritis and dysmenorrhoea
Tương Tác Thuốc :
  • Fluconazole Fluconazole may increase the effect and toxicity of valdecoxib.
  • Ketoconazole Ketoconazole may increase the effect and toxicity of valdecoxib.
  • Lithium The COX-2 inhibitor increases serum levels of lithium
Liều Lượng & Cách Dùng : Tablet - Oral
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Bextra
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00580
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=119607
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46506229
ChemSpider
http://www.chemspider.com/Chemical-Structure.106796.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=13063
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0025-1975-31
PharmGKB
http://www.pharmgkb.org/drug/PA10226
Wikipedia
http://en.wikipedia.org/wiki/Valdecoxib
RxList
http://www.rxlist.com/cgi/generic/bextra.htm
Drugs.com
http://www.drugs.com/mtm/valdecoxib.html
... loading
... loading