中国药业2015，Vol.24Issue(23)：1-6,6.
酮洛芬药理研究进展
Progresses in Pharmacological Study of Ketoprofen
摘要
Abstract
Ketoprofen is a good 2-arylpropionic acid non-steroidal anti-inflammatory drug ( NSAID ) . It performs it's significant activi-ties on antipyretic, analgesic and anti-inflammatory by inhibiting the enzyme activities of cyclooxygenases ( COXs ) , proinflammatory pep-tides and/or lipoxygenases ( LOXs ) , further inhibiting the biosynthesis of those inflammatory substances such as prostaglandins ( PGs ) , bradykinins, leukotrienes ( LTs ) and thromboxanes ( TXs ) . The antiplatelet aggregation activity of ketoprofen quantitatively depends on the acidity. Its anti-inflammatory activity, which is strengthened by selectively inhibiting neutrophil chemotaxis induced by the interleukin-8 ( IL-8 ) , may be partly due to the abilities to scavenge reactive oxygen species ( ROS ) and reactive nitrogen species ( RNS ) , as well as the abilities to inhibit the respiratory burst of neutrophils triggered by various activating agents. Because of unselectively inhibiting COX-1 and COX-2, ketoprofen may prevent the biosynthesis of prostaglandin E2 ( PGE2 ) in gastric mucosal and further produce gastro-toxic activity, cause gastric mucosa damage or bleeding. Moreover, by inhibiting the COX-2 activity, ketoprofen reduce the concentration of endogenous PGF2α, and this may increase the potential risk of seizures. Local usage of ketoprofen may produce photosensitive toxic side effects caused by typeⅠfree radical reaction and contact dermatitis caused by the carboxyl group ( -COOH ) separated from the aromatic structure. In general, this paper systematically summarizes the progresses in pharmacological study of Ketoprofen, reveals its molecular mechanism of pharmacology, and illustrates the efficacy and side effects from its chemical structure nature. This paper may be helpful for the design and development of new products of ketoprofen class and the rational clinical use.关键词
非甾体抗炎药物/酮洛芬/环氧合酶/脂氧化酶/二苯甲酮生色基团/光敏毒性副反应/综述Key words
non-steroidal anti-inflammatory drugs/ketoprofen/cyclooxygenases/lipoxygenases/benzophenone chromophore/photosensitive toxic effects/review分类
医药卫生引用本文复制引用
石开云,余清宝..酮洛芬药理研究进展[J].中国药业,2015,24(23):1-6,6.基金项目
重庆市教育委员会科学技术研究项目资助,项目编号:KJ131513 （）
重庆市高校创新团队建设计划项目资助,项目编号:KTTD201325. （）
