The Effect of Famotidine on the Metabolism of Metoprolol Tartrate in Human Liver Microsomes
10.12259/j.issn.2095-610X.S20250203
- VernacularTitle:法莫替丁对酒石酸美托洛尔在人肝微粒体中代谢的影响
- Author:
Ran XU
1
;
Enfu FENG
;
Yuyu XIONG
;
Jiade ZHU
;
Gonghao HE
Author Information
1. 中国人民解放军联勤保障部队第九二〇医院 临床药学科,云南 昆明 650032
- Keywords:
Metoprolol tartrate;
Famotidine;
Human liver microsomes;
LC-MS/MS;
Kinetics of enzymatic reactions
- From:
Journal of Kunming Medical University
2025;46(2):17-22
- CountryChina
- Language:Chinese
-
Abstract:
Objective To explore the enzymatic reaction kinetics of metoprolol tartrate in an in vitro human liver microsome incubation experiment and to explore the effect of famotidine on the metabolism of metoprolol tartrate.Methods An LC-MS/MS method was developed to accurately measure the concentration of metoprolol tartrate in a human liver microsomal incubation system.A human liver microsome incubation system was established to determine the optimal incubation time and protein concentration;using the substrate depletion method,the enzymatic reaction kinetics parameters of metoprolol tartrate(such as Vmax and Km).Series concentrations of famotidine were co-incubated with metoprolol tartrate,and the concentration of metoprolol tartrate was measured to evaluate the effect of famotidine on its metabolism.Results The optimal incubation time for metoprolol tartrate in human liver microsomes was found to be 60 minutes,with an optimal protein concentration of 1.0 mg/mL.The enzymatic reaction kinetics parameters were Vmax=0.07 μmol/min/mg protein and Km=7.84 μmol/L.Conclusion The results indicated that famotidine did not produce a significant inhibitory effect on the metabolism of metoprolol tartrate in human liver microsome incubation system,suggesting that the combination of these two drugs may be relatively safe.
