Tìm theo
Lornoxicam
Các tên gọi khác (11 ) :
  • Acabel
  • chlortenoxicam
  • CLTX
  • Lorcam
  • Lorcam (TN)
  • Lornoxicamum
  • Safem
  • Taigalor
  • Telos
  • XEFO
  • Xefocam
Thuốc giảm đau, hạ sốt, chống viêm không steroid, điều trị Gút và các bệnh xương khớp
Thuốc Gốc
Small Molecule
CAS: 70374-39-9
ATC: M01AC05
CTHH: C13H10ClN3O4S2
PTK: 371.819
Lornoxicam (chlortenoxicam) is a new nonsteroidal anti-inflammatory drug (NSAID) of the oxicam class with analgesic, anti-inflammatory and antipyretic properties. Lornoxicam differs from other oxicam compounds in its potent inhibition of prostaglandin biosynthesis, a property that explains the particularly pronounced efficacy of the drug. Lornoxicam is approved for use in Japan.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C13H10ClN3O4S2
Phân tử khối
371.819
Monoisotopic mass
370.98012491
InChI
InChI=1S/C13H10ClN3O4S2/c1-17-10(13(19)16-9-4-2-3-5-15-9)11(18)12-7(23(17,20)21)6-8(14)22-12/h2-6,19H,1H3,(H,15,16)/b13-10+
InChI Key
InChIKey=OXROWJKCGCOJDO-JLHYYAGUSA-N
IUPAC Name
(3E)-6-chloro-3-{hydroxy[(pyridin-2-yl)amino]methylidene}-2-methyl-2H,3H,4H-1$l^{6},5,2-thieno[2,3-e][1$l^{6},2]thiazine-1,1,4-trione
Traditional IUPAC Name
(3E)-6-chloro-3-[hydroxy(pyridin-2-ylamino)methylidene]-2-methyl-1$l^{6},5,2-thieno[2,3-e][1$l^{6},2]thiazine-1,1,4-trione
SMILES
CN1\C(=C(\O)NC2=CC=CC=N2)C(=O)C2=C(C=C(Cl)S2)S1(=O)=O
Độ hòa tan
4.61e-02 g/l
logP
2.62
logS
-3.9
pKa (strongest acidic)
6.88
pKa (Strongest Basic)
4.78
PSA
99.6 Å2
Refractivity
97.02 m3·mol-1
Polarizability
33.77 Å3
Rotatable Bond Count
2
H Bond Acceptor Count
6
H Bond Donor Count
2
Physiological Charge
-1
Number of Rings
3
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Lornoxicam is a non-steroidal anti-inflammatory drug (NSAID) that belongs to the oxicam class. As with other NSAIDS, lornoxicam is a potent inhibitor of the cyclooxgenase enzymes, which are responsible for catalyzing the formation of prostaglandins (act as messenger molecules in the process of inflammation) and thromboxane from arachidonic acid. Unlike some NSAIDS, lornoxicam's inhibition of cyclooxygenase does not lead to an increase in leukotriene formation, meaning that arachidonic acid is not moved to the 5-lipoxygenase cascade, resulting in the minimization of the risk of adverse events.
Cơ Chế Tác Dụng : Lornoxicam (chlortenoxicam) is a new nonsteroidal anti-inflammatory drug (NSAID) of the oxicam class with analgesic, anti-inflammatory and antipyretic properties. Lornoxicam differs from other oxicam compounds in its potent inhibition of prostaglandin biosynthesis, a property that explains the particularly pronounced efficacy of the drug. Lornoxicam is approved for use in Japan. Like other NSAIDS, lornoxicam's anti-inflammatory and analgesic activity is related to its inhibitory action on prostaglandin and thromboxane synthesis through the inhibition of both COX-1 and COX-2. This leads to the reduction of inflammation, pain, fever, and swelling, which are mediated by prostaglandins. However, the exact mechanism of lornoxicam, like that of the other NSAIDs, has not been fully determined.
Dược Động Học :
▧ Absorption :
Lornoxicam is absorbed rapidly and almost completely from the GI tract (90-100%).
▧ Protein binding :
Lornoxicam is 99% bound to plasma proteins (almost exlusively to serum albumin).
▧ Metabolism :
Lornoxicam is metabolized completely by cyp 2C9 with the principal metabolite being 5'-hydroxy-lornoxicam and only negligible amounts of intact lornoxicam are excreted unchanged in the urine. Approximately 2/3 of the drug is eliminated via the liver and 1/3 via the kidneys in the active form.
▧ Half Life :
3-5 hours
Chỉ Định : For the treatment of acute mild to moderate pain, as well as pain and inflammation of the joints caused by certain types of rheumatic diseases.
Liều Lượng & Cách Dùng : Injection - Intravenous - 4 mg/ml
Tablet - Oral - 4 mg
Tablet - Oral - 8 mg
Dữ Kiện Thương Mại
Nhà Sản Xuất
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB06725
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=5282204
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=99443271
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D01866
ChemSpider
http://www.chemspider.com/Chemical-Structure.4445392.html
PharmGKB
http://www.pharmgkb.org/drug/PA165958395
Wikipedia
http://en.wikipedia.org/wiki/Lornoxicam
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