摘要
本文选用６只家兔进行随机交叉实验，对家兔单用地尔硫 、美托洛尔及合用两药时的药动学过程作了比较。发现合用两药后，美托洛尔的Ｋ＿ｅ、Ｃｌ＿ｓ均较单用时小（Ｐ＜０．０５），Ｃ＿ｍａｘ和ＡＵＣ＿（０－∞）则明显增大。地尔硫的Ｋ＿ｅ在合用药时显著增大，其活性代谢物去乙酰地尔硫的Ｃ＿ｍａｘ和ＡＵＣ＿（０－∞）则也有显著提高。表明合用两药后美托洛尔的肝脏代谢受到抑制。本文证实的相互作用提示，临床合用两药时应同时监测患者血浓，并适当调整剂量，以免发生不良反应。
A randomised and crossover study was conducted in six healthy rabbits. The
pharmacokinetic action of dilti-azem and metoprolol in rabbits were compared between alone
administration treatment and combination treatment.For metoprolol,its Ke and Cl_s were
significantly reduced,Cmax and AUC_(0-∞)were significantly increased when it was
co-administered with diltiazem, Ke of diltiazem was evidently enhanced after combination
treatment, Cmax and AUC_(0-∞)of its active metabolite deacetyldiltiazem were also
augmented.The results showed that the metabolism of metoprolol in liver may be inhibited by
diltiazem when they are administered in combination. The pharmacokinetic interaction proved
in this study suggested that it is essential for clinicians to monitor drug concen-trations when
the two drugs are combined, and in some cases,dosage shoud be adjusted to avoid adverse
effects.
出处
《中国医院药学杂志》
CAS
CSCD
北大核心
1995年第10期439-441,共3页
Chinese Journal of Hospital Pharmacy
