The clinical relevance of preclinical data: mirtazapine, a model compound.
The clinical relevance of preclinical data: mirtazapine, a model compound.
复制标题
临床前数据的临床相关性：米氮平，一种模型化合物。
DOI：
--
复制
发表时间：
1997
影响因子：
2.9
通讯作者：
R. Vos
中科院分区：
文献类型：
--
作者：
L. Delbressine;R. Vos
本文讨论了体外和临床前体内研究如何有助于解释和预测可能的临床相关影响。给出的例子是指米氮平获得的数据，米氮平是一种具有双重作用机制的新型抗抑郁药，最好总结为去甲肾上腺素能和特异性肾上腺素能抗抑郁药。米氮平的临床前数据表明：（i）其与血浆蛋白的结合相对较低且无特异性;（ii）其代谢产物对药理作用的贡献可忽略不计;（iii）其生物利用度高，导致个体间差异较小;（iv）其对肝P450酶无诱导或抑制作用;（v）它与其他药物发生临床相关药代动力学相互作用的可能性非常低;（vi）它的分布不依赖于多态性CYP 2D 6活性。现有的米氮平临床前数据可用于建议临床医生和指导临床实践。
This paper discusses how in vitro and preclinical in vivo studies might be of help for the interpretation and prediction of possible clinically relevant effects. The examples given refer to the data obtained with mirtazapine, a novel antidepressant with a dual mechanism of action, which can be best summarized as a noradrenergic and specific serotonergic antidepressant. Preclinical data on mirtazapine have shown that (i) its binding to plasma proteins is relatively low and non-specific; (ii) the contribution of its metabolites to the pharmacologic effect is negligible; (iii) it possesses high bioavailability, resulting in a low variance between individuals; (iv) it has no inducing or inhibiting effects on hepatic P450 enzymes; (v) it has a very low potential for clinically relevant pharmacokinetic interactions with other drugs; and (vi) its disposition is independent of polymorphic CYP2D6 activity. The available preclinical data on mirtazapine could be used to advise clinicians and to guide clinical practice.
DOI：
--
发表时间：
1994-07
期刊：
The Journal of pharmacology and experimental therapeutics
影响因子：
--
作者：
T. Shimada;H. Yamazaki;M. Mimura;Y. Inui;F. Guengerich
通讯作者：
T. Shimada;H. Yamazaki;M. Mimura;Y. Inui;F. Guengerich