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Oxaprozin

产品号 DB00991 公司名称 DrugBank
CAS号 21256-18-8 公司网站 http://www.ualberta.ca/
分子式 C18H15NO3 电 话 (780) 492-3111
分子量 293.3166 传 真
纯 度 电子邮件 david.wishart@ualberta.ca
保 存 Chembase数据库ID: 865

产品价格信息

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产品别名

标题
Oxaprozin
IUPAC标准名
3-(diphenyl-1,3-oxazol-2-yl)propanoic acid
IUPAC传统名
oxaprozin
商标名
Daypro
Voir
Alvo
Daypro Alta
Deflam
别名
Oxaprozina [INN-Spanish]
Oxaprozinum [INN-Latin]
Oxaprozine [INN-French]

产品登记号

PubChem CID 4614
PubChem SID 46506429
CAS号 21256-18-8

产品性质

疏水性(logP) 3.7
溶解度 Insoluble

产品详细信息

详细说明 (English)
Item Information
Drug Groups approved
Description 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.
Indication Used to relieve the inflammation, swelling, stiffness, and joint pain associated with rheumatoid arthritis and osteoarthritis.
Pharmacology 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.
Toxicity Oral, mouse: LD50 = 1210 mg/kg; Oral, rabbit: LD50 = 172 mg/kg; Oral, rat: LD50 = 4470 mg/kg
Affected Organisms
Humans and other mammals
Biotransformation Hepatic. Ester and ether glucuronide are the major conjugated metabolites of oxaprozin, and do not have significant pharmacologic activity.
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.
Half Life 54.9 hours
Protein Binding >99.5% bound to albumin
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.
Distribution * 11 to 17 L/70 kg
References
Heller B, Tarricone R: Oxaprozin versus diclofenac in NSAID-refractory periarthritis pain of the shoulder. Curr Med Res Opin. 2004 Aug;20(8):1279-90. [Pubmed]
Zhou XP, Zhang MX, Sun W, Yang XH, Wang GS, Sui DY, Yu XF, Qu SC: Design, synthesis, and in-vivo evaluation of 4,5-diaryloxazole as novel nonsteroidal anti-inflammatory drug. Biol Pharm Bull. 2009 Dec;32(12):1986-90. [Pubmed]
External Links
Wikipedia
RxList
Drugs.com

参考文献

  • Heller B, Tarricone R: Oxaprozin versus diclofenac in NSAID-refractory periarthritis pain of the shoulder. Curr Med Res Opin. 2004 Aug;20(8):1279-90. PubmedZhou XP, Zhang MX, Sun W, Yang XH, Wang GS, Sui DY, Yu XF, Qu SC: Design, synthesis, and in-vivo evaluation of 4,5-diaryloxazole as novel nonsteroidal anti-inflammatory drug. Biol Pharm Bull. 2009 Dec;32(12):1986-90. Pubmed