Tìm theo
Nimesulide
Thuốc giảm đau, hạ sốt, chống viêm không steroid, điều trị Gút và các bệnh xương khớp
Thuốc Gốc
Small Molecule
CAS: 51803-78-2
ATC: M01AX17, M02AA26
CTHH: C13H12N2O5S
PTK: 308.31
Nimesulide is a relatively COX-2 selective, non-steroidal anti-inflammatory drug (NSAID) with analgesic and antipyretic properties. Its approved indications are the treatment of acute pain, the symptomatic treatment of osteoarthritis and primary dysmenorrhoea in adolescents and adults above 12 years old. Due to concerns about the risk of hepatotoxicity, nimesulide has been withdrawn from market in many countries.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C13H12N2O5S
Phân tử khối
308.31
Monoisotopic mass
308.046692194
InChI
InChI=1S/C13H12N2O5S/c1-21(18,19)14-12-8-7-10(15(16)17)9-13(12)20-11-5-3-2-4-6-11/h2-9,14H,1H3
InChI Key
InChIKey=HYWYRSMBCFDLJT-UHFFFAOYSA-N
IUPAC Name
N-(4-nitro-2-phenoxyphenyl)methanesulfonamide
Traditional IUPAC Name
nimesulide
SMILES
CS(=O)(=O)NC1=C(OC2=CC=CC=C2)C=C(C=C1)[N+]([O-])=O
Độ tan chảy
143-144.5 °C
Độ hòa tan
1.82e-02 g/l
logP
2.60
logS
-4.2
pKa (strongest acidic)
6.86
pKa (Strongest Basic)
-8.9
PSA
101.22 Å2
Refractivity
76.31 m3·mol-1
Polarizability
28.87 Å3
Rotatable Bond Count
4
H Bond Acceptor Count
4
H Bond Donor Count
1
Physiological Charge
-1
Number of Rings
2
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Food, gender and advanced age have negligible effects on nimesulide pharmacokinetics.
Cơ Chế Tác Dụng : Nimesulide is a relatively COX-2 selective, non-steroidal anti-inflammatory drug (NSAID) with analgesic and antipyretic properties. Its approved indications are the treatment of acute pain, the symptomatic treatment of osteoarthritis and primary dysmenorrhoea in adolescents and adults above 12 years old. Due to concerns about the risk of hepatotoxicity, nimesulide has been withdrawn from market in many countries. The therapeutic effects of Nimesulide are the result of its complete mode of action which targets a number of key mediators of the inflammatory process such as: COX-2 mediated prostaglandins, free radicals, proteolytic enzymes and histamine.
Dược Động Học :
▧ Absorption :
Rapidly absorbed following oral administration.
▧ Protein binding :
>97.5%
▧ Metabolism :
Hepatic. Extensive biotransformation, mainly to 4-hydroxynimesulide (which also appears to be biologically active).
▧ Route of Elimination :
Renal (50%), fecal (29%)
▧ Half Life :
1.8–4.7 hours
Độc Tính : Oral TDLO (human): 1.429 mg/kg; Oral TDLO (woman): 2 mg/kg; Oral LD50 (rat): 200 mg/kg; Oral LD50 (mouse): 392 mg/kg
Chỉ Định : For the treatment of acute pain, the symptomatic treatment of osteoarthritis and primary dysmenorrhoea in adolescents and adults above 12 years old.
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB04743
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D01049
PharmGKB
http://www.pharmgkb.org/drug/PA137179528
Wikipedia
http://en.wikipedia.org/wiki/Nimesulide
Drugs.com
http://www.drugs.com/international/nimesulide.html
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