A new drug-drug interaction-tilmicosin reduces the metabolism of enrofloxacin through CYP3A4. (November 2022)

• Record Type: Journal Article
• Authors: Zhang, Liyun; Wang, XiaoJing; Wang, Lei; Badawy, Sara; Liu, Zhenli; Xie, Changqing; Wang, Xu; Tao, Yanfei
• Is Part Of: Research in veterinary science. Volume 148(2022)
• Page Start: 33
• Page End: 41
• Publication Date: 2022-11
• Subjects: Enrofloxacin -- Tilmicosin -- Drug-drug interactions -- CYP3A4 -- Time of elimination; Veterinary medicine -- Periodicals; Veterinary Medicine -- Periodicals; Médecine vétérinaire -- Périodiques; Médecine vétérinaire -- Recherche -- Périodiques; Diergeneeskunde; 636.089
• DOI: 10.1016/j.rvsc.2022.05.004
• Languages: English
• ISSNs: 0034-5288

Abstract

Abstract: The monitoring results in China have shown that the phenomenon of single-pollutant residues exceeding the standard in food has decreased, while the coexistence of many low-level residual pollutants has increased significantly. Among these, the combined use of enrofloxacin (EF) and tilmicosin (TIM) is serious. Despite that, little is comprehended about influences of the drug-drug interactions (DDIs) caused by EF and TIM. The purpose of this work is to evaluate the effects caused by the combination of these two drugs on metabolism and residues in vivo and in vitro. The results showed that TIM affected the metabolism of EF by inhibiting CYP3A4 and increased the residual concentrations of EF in broilers. Moreover, the time of elimination of EF was prolonged. Thus, the combined use of TIM and EF must be reduced in veterinary drugs and feeds in order to ensure the safety of humans and animals. Highlights: CYP3A4 was the key metabolic enzyme of enrofloxacin in broilers. Tilmicosin inhibited the activity of the CYP3A4 subtype enzyme. Tilmicosin inhibited the metabolism and residues of enrofloxacin in vitro and in vivo. Drug-drug interactions caused by enrofloxacin-tilmicosin were related with CYP3A4