Tìm theo
Sulfinpyrazone
Các tên gọi khác (6 ) :
  • 1,2-Diphenyl-3,5-dioxo-4-(2-phenylsulfinylethyl)pyrazolidine
  • 1,2-Diphenyl-4-(2'-phenylsulfinethyl)-3,5-pyrazolidinedione
  • 4-(2-Benzenesulfinylethyl)-1,2-diphenylpyrazolidine-3,5-dione
  • Anturane (tn)
  • Sulfinpyrazone
  • Sulfoxyphenylpyrazolidine
uricosuric agents
Thuốc Gốc
Small Molecule
CAS: 57-96-5
ATC: M04AB02
ĐG : Barr Pharmaceuticals
CTHH: C23H20N2O3S
PTK: 404.482
A uricosuric drug that is used to reduce the serum urate levels in gout therapy. It lacks anti-inflammatory, analgesic, and diuretic properties. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C23H20N2O3S
Phân tử khối
404.482
Monoisotopic mass
404.119463206
InChI
InChI=1S/C23H20N2O3S/c26-22-21(16-17-29(28)20-14-8-3-9-15-20)23(27)25(19-12-6-2-7-13-19)24(22)18-10-4-1-5-11-18/h1-15,21H,16-17H2
InChI Key
InChIKey=MBGGBVCUIVRRBF-UHFFFAOYSA-N
IUPAC Name
4-[2-(benzenesulfinyl)ethyl]-1,2-diphenylpyrazolidine-3,5-dione
Traditional IUPAC Name
sulfinpyrazone
SMILES
O=C1C(CCS(=O)C2=CC=CC=C2)C(=O)N(N1C1=CC=CC=C1)C1=CC=CC=C1
Độ tan chảy
136-137 °C
Độ hòa tan
31.2 mg/L
logP
2.30
logS
-3.1
pKa (strongest acidic)
3.41
pKa (Strongest Basic)
-6.7
PSA
57.69 Å2
Refractivity
113.62 m3·mol-1
Polarizability
42.15 Å3
Rotatable Bond Count
6
H Bond Acceptor Count
3
H Bond Donor Count
0
Physiological Charge
-1
Number of Rings
4
Bioavailability
1
Rule of Five
true
Ghose Filter
true
MDDR-Like Rule
true
pKa
3.25
Dược Lực Học : Sulfinpyrazone's pharmacologic activity is the potentiation of the urinary excretion of uric acid. It is useful for reducing the blood urate levels in patients with chronic tophaceous gout and acute intermittent gout, and for promoting the resorption of tophi.
Cơ Chế Tác Dụng : A uricosuric drug that is used to reduce the serum urate levels in gout therapy. It lacks anti-inflammatory, analgesic, and diuretic properties. [PubChem] Sulfinpyrazone is an oral uricosuric agent (pyrazolone derivative) used to treat chronic or intermittent gouty arthritis. Sulfinpyrazone competitively inhibits the reabsorption of uric acid at the proximal convoluted tubule, thereby facilitating urinary excretion of uric acid and decreasing plasma urate concentrations. This is likely done through inhibition of the urate anion transporter (hURAT1) as well as the human organic anion transporter 4 (hOAT4). Sulfinpyrazone is not intended for the treatment of acute attacks because it lacks therapeutically useful analgesic and anti-inflammatory effects. Sulfinpyrazone and its sulfide metabolite possess COX inhibitory effects. Sulfinpyrazone has also been shown to be a UDP-glucuronsyltransferase inhibitor and a very potent CYP2C9 inhibitor. Sulfinpyrazone is also known to be a cystic fibrosis transmembrane conductance regulator (CFTR) inhibitor as well as an inhibitor of several multridrug resistance proteins (MRPs).
Dược Động Học :

▧ Protein binding :
98-99%
▧ Half Life :
Approximately 4-6 hours
Độc Tính : Symptoms of overdose include nausea, vomiting, diarrhea, epigastric pain, ataxia, labored respiration, convulsions, coma. Possible symptoms, seen after overdosage with other pyrazolone derivatives: anemia, jaundice, and ulceration.
Chỉ Định : For the treatment of gout and gouty arthritis.
Tương Tác Thuốc :
  • Cyclosporine Sulfinpyrazone decreases the effect of cyclosporine
  • Tolbutamide Tolbutamide, a strong CYP2C9 inhibitor, may decrease the metabolism and clearance of Sulfinpyrazone. Consider alternate therapy or monitor for changes in Sulfinpyrazone therapeutic and adverse effects if Tolbutamide is initiated, discontinued or dose changed.
  • Warfarin Sulfinpyrazone may increase the anticoagulant effect of warfarin by decreasing its metabolism and protein binding.
Liều Lượng & Cách Dùng : Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Anturane
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01138
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=5342
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46504918
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07317
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00449
ChemSpider
http://www.chemspider.com/Chemical-Structure.5149.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0083-0041-30
PharmGKB
http://www.pharmgkb.org/drug/PA451550
Wikipedia
http://en.wikipedia.org/wiki/Sulfinpyrazone
RxList
http://www.rxlist.com/cgi/generic3/sulfinpyrazone.htm
Drugs.com
http://www.drugs.com/mtm/sulfinpyrazone.html
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