Tìm theo
Phenylbutazone
Các tên gọi khác (8 ) :
  • 3,5-Dioxo-1,2-diphenyl-4-n-butylpyrazolidine
  • 4-BUTYL-1,2-diphenyl-pyrazolidine-3,5-dione
  • 4-n-Butyl-1,2-diphenyl-3,5-pyrazolidinedione
  • Fenilbutazona
  • Phenbutazone
  • Phenylbutazon
  • Phenylbutazone
  • Phenylbutazonum
anti inflammatory agents non steroidal
Thuốc Gốc
Small Molecule
CAS: 50-33-9
ATC: M01AA01, M02AA01
ĐG : C.O. Truxton Inc.
CTHH: C19H20N2O2
PTK: 308.3743
A drug that has anti-inflammatory, antipyretic, and analgesic activities. It is especially effective in the treatment of ankylosing spondylitis. It also is useful in rheumatoid arthritis and Reiter's syndrome (investigational indication). Although phenylbutazone is effective in gouty arthritis, risk/benefit considerations indicate that this drug should not be employed for this disease. (From AMA Drug Evaluations Annual, 1994, p1822)
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C19H20N2O2
Phân tử khối
308.3743
Monoisotopic mass
308.152477894
InChI
InChI=1S/C19H20N2O2/c1-2-3-14-17-18(22)20(15-10-6-4-7-11-15)21(19(17)23)16-12-8-5-9-13-16/h4-13,17H,2-3,14H2,1H3
InChI Key
InChIKey=VYMDGNCVAMGZFE-UHFFFAOYSA-N
IUPAC Name
4-butyl-1,2-diphenylpyrazolidine-3,5-dione
Traditional IUPAC Name
phenylbutazone
SMILES
CCCCC1C(=O)N(N(C1=O)C1=CC=CC=C1)C1=CC=CC=C1
Độ tan chảy
105 °C
Độ hòa tan
47.5 mg/L (at 30 °C)
logP
3.16
logS
-3.81
pKa (strongest acidic)
5.13
PSA
40.62 Å2
Refractivity
88.76 m3·mol-1
Polarizability
34.15 Å3
Rotatable Bond Count
5
H Bond Acceptor Count
2
H Bond Donor Count
0
Physiological Charge
-1
Number of Rings
3
Bioavailability
1
Rule of Five
true
Ghose Filter
true
pKa
4.5
Dược Lực Học : Phenylbutazone is a synthetic, pyrazolone derivative. It is a nonhormonal anti-inflammatory, antipyretic compound useful in the management of inflammatory conditions. The apparent analgesic effect is probably related mainly to the compound's anti-inflammatory properties and arise from its ability to reduce production of prostaglandin H and prostacyclin. Prostaglandins act on a variety of cells such as vascular smooth muscle cells causing constriction or dilation, on platelets causing aggregation or disaggregation and on spinal neurons causing pain. Prostacylcin causes vascular constriction platelet disaggregation
Cơ Chế Tác Dụng : A drug that has anti-inflammatory, antipyretic, and analgesic activities. It is especially effective in the treatment of ankylosing spondylitis. It also is useful in rheumatoid arthritis and Reiter's syndrome (investigational indication). Although phenylbutazone is effective in gouty arthritis, risk/benefit considerations indicate that this drug should not be employed for this disease. (From AMA Drug Evaluations Annual, 1994, p1822) Phenylbutazone binds to and inactivates prostaglandin H synthase and prostacyclin synthase through peroxide (H2O2) mediated deactivation. The reduced production of prostaglandin leads to reduced inflammation of the surrounding tissues.
Độc Tính : Oral, LD50 = 238 mg/kg (mouse); Oral, LD50 = 781 mg/kg (rabbit); Oral, LD50 = 245 mg/kg (rat); Oral, LD50 = 375 mg/kg (rat)
Chỉ Định : For the treatment of backache and ankylosing spondylitis
Tương Tác Thuốc :
  • Acenocoumarol The NSAID, phenylbutazone, may increase the anticoagulant effect of acenocoumarol.
  • Acetohexamide Phenylbutazone may increase the effect of acetohexamide.
  • Anisindione The NSAID, phenylbutazone, may increase the anticoagulant effect of anisindione.
  • Chlorpropamide Phenylbutazone increases the effect of the hypoglycemic agent
  • Dicoumarol The NSAID, phenylbutazone, may increase the anticoagulant effect of dicumarol.
  • Ethotoin The NSAID, phenylbutazone, may increase the hydantoin effect of ethotoin.
  • Fosphenytoin The NSAID, phenylbutazone, may increase the hydantoin effect of fosphenytoin.
  • Gliclazide Phenylbutazone increases the effect of the hypoglycemic agent
  • Glipizide Phenylbutazone increases the effect of the hypoglycemic agent
  • Glisoxepide Phenylbutazone increases the effect of the hypoglycemic agent
  • Glyburide Phenylbutazone increases the effect of the hypoglycemic agent
  • Glycodiazine Phenylbutazone increases the effect of the hypoglycemic agent
  • Lithium The NSAID, phenylbutazone, may decrease the renal excretion of lithium. Increased risk of lithium toxicity.
  • Mephenytoin The NSAID, phenylbutazone, may increase the hydantoin effect of mephenytoin.
  • Methotrexate The NSAID, phenylbutazone, may decrease the renal excretion of methotrexate. Increased risk of methotrexate toxicity.
  • Phenytoin The NSAID, phenylbutazone, may increase the therapeutic and adverse effects of phenytoin.
  • Tolazamide Phenylbutazone increases the effect of the hypoglycemic agent
  • Tolbutamide Phenylbutazone increases the effect of the hypoglycemic agent
  • Warfarin The NSAID, phenylbutazone, may increase the anticoagulant effect of warfarin.
Liều Lượng & Cách Dùng : Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Azolid
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00812
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=4781
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46507038
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07440
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00510
ChemSpider
http://www.chemspider.com/Chemical-Structure.4617.html
PharmGKB
http://www.pharmgkb.org/drug/PA450932
Wikipedia
http://en.wikipedia.org/wiki/Phenylbutazone
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