Tìm theo
Oxaprozin
Các tên gọi khác (9 ) :
  • Danoprox
  • Daypro
  • Dayrun
  • Deflam
  • Duraprox
  • Oxaprozina
  • Oxaprozine
  • Oxaprozinum
  • Walix
anti inflammatory agents non steroidal
Thuốc Gốc
Small Molecule
CAS: 21256-18-8
ATC: M01AE12
ĐG : Aidarex Pharmacuticals LLC , http://www.aidarex.com
CTHH: C18H15NO3
PTK: 293.3166
Oxaprozin is a non-narcotic, non-steroidal anti-inflammatory drug (NSAID), used to relieve the inflammation, swelling, stiffness, and joint pain associated with osteoarthritis and rheumatoid arthritis.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C18H15NO3
Phân tử khối
293.3166
Monoisotopic mass
293.105193351
InChI
InChI=1S/C18H15NO3/c20-16(21)12-11-15-19-17(13-7-3-1-4-8-13)18(22-15)14-9-5-2-6-10-14/h1-10H,11-12H2,(H,20,21)
InChI Key
InChIKey=OFPXSFXSNFPTHF-UHFFFAOYSA-N
IUPAC Name
3-(diphenyl-1,3-oxazol-2-yl)propanoic acid
Traditional IUPAC Name
oxaprozin
SMILES
OC(=O)CCC1=NC(=C(O1)C1=CC=CC=C1)C1=CC=CC=C1
Độ tan chảy
158-159 °C
Độ hòa tan
Insoluble
logP
4.19
logS
-4
pKa (strongest acidic)
4.95
pKa (Strongest Basic)
-0.59
PSA
63.33 Å2
Refractivity
81.88 m3·mol-1
Polarizability
31.69 Å3
Rotatable Bond Count
5
H Bond Acceptor Count
3
H Bond Donor Count
1
Physiological Charge
-1
Number of Rings
3
Bioavailability
1
Rule of Five
true
Ghose Filter
true
pKa
4.3
Dược Lực Học : Oxaprozin is a nonsteroidal anti-inflammatory drug (NSAID) with analgesic and antipyretic properties. Oxaprozin is used to treat rheumatoid arthritis, osteoarthritis, dysmenorrhea, and to alleviate moderate pain.
Cơ Chế Tác Dụng : Oxaprozin is a non-narcotic, non-steroidal anti-inflammatory drug (NSAID), used to relieve the inflammation, swelling, stiffness, and joint pain associated with osteoarthritis and rheumatoid arthritis. Anti-inflammatory effects of Oxaprozin are believed to be due to inhibition of cylooxygenase in platelets which leads to the blockage of prostaglandin synthesis. Antipyretic effects may be due to action on the hypothalamus, resulting in an increased peripheral blood flow, vasodilation, and subsequent heat dissipation. Oxaprozin is a non-selective NSAID, with a cell assay system showing lower COX-2 selectivity implying higher COX-1 selectivity.
Dược Động Học :
▧ Absorption :
Oxaprozin is 95% absorbed after oral administration. Food may reduce the rate of absorption of oxaprozin, but the extent of absorption is unchanged. Antacids do not significantly affect the extent and rate of oxaprozin absorption.
▧ Volume of Distribution :
* 11 to 17 L/70 kg
▧ Protein binding :
>99.5% bound to albumin
▧ Metabolism :
Hepatic. Ester and ether glucuronide are the major conjugated metabolites of oxaprozin, and do not have significant pharmacologic activity.
▧ Route of Elimination :
Oxaprozin is expected to be excreted in human milk based on its physical-chemical properties; however, the amount of oxaprozin excreted in breast milk has not been evaluated. Approximately 95% of oxaprozin is metabolized by the liver. Approximately 5% of the oxaprozin dose is excreted unchanged in the urine. Sixty-five percent (65%) of the dose is excreted in the urine and 35% in the feces as metabolite. Biliary excretion of unchanged oxaprozin is a minor pathway. Several oxaprozin metabolites have been identified in human urine or feces.
▧ Half Life :
54.9 hours
Độc Tính : Oral, mouse: LD50 = 1210 mg/kg; Oral, rabbit: LD50 = 172 mg/kg; Oral, rat: LD50 = 4470 mg/kg
Chỉ Định : Used to relieve the inflammation, swelling, stiffness, and joint pain associated with rheumatoid arthritis and osteoarthritis.
Tương Tác Thuốc :
  • Acenocoumarol The NSAID, oxaprozin, may increase the anticoagulant effect of acenocoumarol.
  • Alendronate Increased risk of gastric toxicity
  • Anisindione The NSAID, oxaprozin, may increase the anticoagulant effect of anisinodione.
  • Azilsartan medoxomil Increases toxicity of each. May deteriorate renal function, particularly in volume depleted or elderly patients. Decreases effects of azilsartan by antagonism.
  • Colesevelam Bile acid sequestrants may decrease the absorption of Nonsteroidal Anti-Inflammatory Agents. Monitor for decreased serum concentrations/therapeutic effects of nonsteroidal anti-inflammatory agents (NSAID) if coadministered with bile acid sequestrants. Separating the administration of doses by 2 or more hours may reduce (but not eliminate) the risk of interaction. The manufacturer of colesevelam recommends that drugs should be administered at least 1 hour before or 4 hours after colesevelam.
  • Cyclosporine Monitor for nephrotoxicity
  • Dicoumarol The NSAID, oxaprozin, may increase the anticoagulant effect of dicumarol.
  • Ginkgo biloba Additive anticoagulant/antiplatelet effects may increase bleed risk. Concomitant therapy should be avoided.
  • Methotrexate The NSAID, oxaprozin, may decrease the renal excretion of methotrexate. Increased risk of methotrexate toxicity.
  • Pralatrexate NSAIDs increase the risk of toxicity due to impairment of renal clearance of pralatrexate thus increasing exposure. Monitor for adverse effects or adjust dose of pralatrexate.
  • Telmisartan Concomitant use of Telmisartan and Oxaprozin may increase the risk of acute renal failure and hyperkalemia. Monitor renal function at the beginning and during treatment.
  • Timolol The NSAID, Oxaprozin, may antagonize the antihypertensive effect of Timolol.
  • Trandolapril The NSAID, Oxaprozin, may reduce the antihypertensive effect of Trandolapril. Consider alternate therapy or monitor for changes in Trandolapril efficacy if Oxaprozin is initiated, discontinued or dose changed.
  • Treprostinil The prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the NSAID, Oxaprozin. Monitor for increased bleeding during concomitant thearpy.
  • Warfarin The antiplatelet effects of oxaprozin may increase the bleed risk associated with warfarin. Consider alternate therapy or monitor for signs and symptoms of bleeding during concomitant therapy.
Liều Lượng & Cách Dùng : Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
  • Biệt dược thương mại : Oxaprozin 600 mg tablet
    Giá bán buôn : USD >1.54
    Đơn vị tính : tablet
  • Biệt dược thương mại : Daypro 600 mg caplet
    Giá bán buôn : USD >2.87
    Đơn vị tính : caplet
  • Biệt dược thương mại : Daypro 600 mg tablet
    Giá bán buôn : USD >2.98
    Đơn vị tính : tablet
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Alvo
  • Công ty :
    Sản phẩm biệt dược : Daypro
  • Công ty :
    Sản phẩm biệt dược : Daypro Alta
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00991
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=4614
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46506429
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07356
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00463
ChemSpider
http://www.chemspider.com/Chemical-Structure.4453.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50002861
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0025-1381-31
PharmGKB
http://www.pharmgkb.org/drug/PA450730
Wikipedia
http://en.wikipedia.org/wiki/Oxaprozin
RxList
http://www.rxlist.com/cgi/generic/oxaproz.htm
Drugs.com
http://www.drugs.com/cdi/oxaprozin.html
... loading
... loading