Development of NSAIDs with lower gastric side effect
Development of NSAIDs with lower gastric side effect
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开发具有较低胃副作用的非甾体抗炎药
DOI：
10.1159/000338396
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发表时间：
2012
期刊：
影响因子：
--
通讯作者：
T
中科院分区：
文献类型：
--
作者：
Mizushima;T
非甾体抗炎药是世界上最常用的一类药物之一，占所有处方药的近5%。然而，非甾体抗炎药的使用与胃肠道并发症有关，如胃溃疡和出血，有时会成为危及生命的疾病。大约15-30%的非甾体抗炎药慢性服用者有胃肠道溃疡和出血。在美国，每年约有16500人死于与非甾体抗炎药相关的胃肠道并发症。因此，为了开发出没有这些副作用的新型非甾体抗炎药，需要阐明非甾体抗炎药诱导胃肠道损伤的分子机制。非甾体抗炎药对COX的抑制作用是其抗炎活性的主要原因，以前认为这是其胃肠道副作用的完全原因。COX至少有COX-1和COX-2两种亚型，分别负责胃粘膜和炎症组织的大部分COX活性。因此，我们有理由推测选择性COX-2抑制剂具有抗炎活性且无胃肠道副作用。事实上,
NSAIDs are one of the most frequently used classes of medicines in the world and account for nearly 5% of all prescribed medications1). However, NSAID administration is associated with gastrointestinal complications, such as gastric ulcers and bleeding, which sometimes become life-threatening diseases2). About 15-30% of chronic users of NSAIDs have gastrointestinal ulcers and bleeding. In the United States, about 16,500 people per year die as a result of NSAID-associated gastrointestinal complications3). Therefore, the molecular mechanism governing NSAID-induced gastrointestinal damage needs to be elucidated in order to develop new NSAIDs that do not have these side effects. Inhibition of COX by NSAIDs, which is responsible for their anti-inflammatory activity was previously thought to be fully responsible for their gastrointestinal side effects4). There are at least two subtypes of COX, COX-1 and COX-2, which are responsible for the majority of COX activity at the gastric mucosa and tissues with inflammation, respectively. Therefore, it is reasonable to speculate that selective COX-2 inhibitors have antiinflammatory activity without gastrointestinal side effects. In fact,
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影响因子：
12.4
作者：
Tsutsumi, S;Gotoh, T;Mizushima, T
通讯作者：
Mizushima, T
影响因子：
16
作者：
Yu, J;Zhang, L;Vogelstein, B
通讯作者：
Vogelstein, B
DOI：
10.1016/j.bbrc.2007.03.034
发表时间：
2007-05-11
影响因子：
3.1
作者：
Ishihara, Tomoaki;Hoshino, Tatsuya;Mizushima, Tohru
通讯作者：
Mizushima, Tohru
新合成非甾体抗炎药洛索洛芬钠与吲哚美辛对人胃粘膜血流动力学的影响
影响因子：
4.1
作者：
S. Kawano;Shingo Tsuji;N. Hayashi;Y. Takei;K. Nagano;H. Fusamoto;T. Kamada
通讯作者：
T. Kamada