论文部分内容阅读
美洛昔康(Meloxicom)是最新的环氧化酶—2抑制剂之一。环氧化酶(COX)存在两种形式:环氧化酶—1(COX—1)和环氧化酶—2(COX—2)。两者之间具有较高同源性(约67%)。 非甾体抗炎药(NASIDs)按化学结构不同可分成:吡唑酮类,邻氨基苯甲酸类,吲哚乙酸类,芳基烷酸类,苯噻嗪类(昔康类)等等。NASIDs的作用机理主要是通过抑制COX来阻断PG的合成。但由于COX—1和COX—2结构相似而作用差异,大多数NASIDs在抑制COX时对这两种类型的酶不能区分,往往在抑制炎症的同时,带来较多的副作用,如胃肠道刺激及肾脏损伤等。
Meloxicom is one of the latest cyclooxygenase-2 inhibitors. There are two forms of cyclooxygenase (COX): cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2). The two have high homology (about 67%). Non-steroidal anti-inflammatory drugs (NASIDs) according to the chemical structure can be divided into: pyrazolones, anthranilates, indoles acetic acid, arylalkanoic acids, phenothiazines (oxicams) and so on. The mechanism of action of NASIDs is mainly to block the synthesis of PG by inhibiting COX. However, due to the similar structure and function of COX-1 and COX-2, most NASIDs can not distinguish these two types of enzymes when they inhibit COX, and often bring more side effects such as inhibition of inflammation and gastrointestinal tract Irritation and kidney damage.