Engelhardt G
Arzneimittelforschung. 1978;28(11a):1977-80.
The results of comparative studies with respect to pharmacological, toxicological, pharmacokinetic and clinico-pharmacological effects of the non-steroid anti-inflammatory drugs 4-[4-(2'-fluorobiphenylyl)]-4-hydroxycrotonic acid and 3-(2'-fluoro-4-biphenylyl)-butyric acid as well as the intrinsic activities of their metabolites in vitro are discussed. The variation in gastrointestinal side effects caused by the two compounds in different species can conveniently be explained in terms of different pharmacokinetic pathways. This leads to a species dependent formation of pharmaco-dynamically active metabolites.
讨论了非甾体抗炎药4-[4-(2'-氟联苯基)]-4-羟基巴豆酸和3-(2'-氟-4-联苯基)丁酸的药理、毒理、药代动力学和临床药理作用的比较研究结果,以及它们代谢产物在体外的内在活性。两种化合物在不同物种中引起的胃肠道副作用差异,可以通过不同的药代动力学途径方便地解释。这导致了药效学活性代谢产物的物种依赖性形成。