Propofol exhibits inhibitory effect towards human liver microsomes (HLMs)- catalyzed glucuronidation of thienorphine

Drug-drug interaction (DDI) is a challenging problem in the process of drug utilization. Inhibition of glucuronidation reaction of drugs is a major reason for DDI. The aim of the present study is to predict propofol-thienorphine interaction from the perspective of propofol’s inhibition towards thien...

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Detalles Bibliográficos
Autores principales: Zhang, Shu-Yao, Chen, Lei, Lin, Chao-Xian, Zhu, Zhi-Wei, Fang, Ling, Xin, Dai-Shan, Guo, Dai-Nian
Formato: Articulo Comunicacion
Lenguaje:Inglés
Publicado: 2012
Materias:
Farmacia
Drug-drug interaction (DDI)
Propofol
Thienorphine
Acceso en línea:http://sedici.unlp.edu.ar/handle/10915/25730
http://www.latamjpharm.org/resumenes/31/6/LAJOP_31_6_2_5.pdf
Aporte de:
SEDICI (UNLP) de Universidad Nacional de La Plata
id I19-R120-10915-25730
record_format dspace
institution Universidad Nacional de La Plata
institution_str I-19
repository_str R-120
collection SEDICI (UNLP)
language Inglés
topic Farmacia
Drug-drug interaction (DDI)
Propofol
Thienorphine
spellingShingle Farmacia
Drug-drug interaction (DDI)
Propofol
Thienorphine
Zhang, Shu-Yao
Chen, Lei
Lin, Chao-Xian
Zhu, Zhi-Wei
Fang, Ling
Xin, Dai-Shan
Guo, Dai-Nian
Propofol exhibits inhibitory effect towards human liver microsomes (HLMs)- catalyzed glucuronidation of thienorphine
topic_facet Farmacia
Drug-drug interaction (DDI)
Propofol
Thienorphine
description Drug-drug interaction (DDI) is a challenging problem in the process of drug utilization. Inhibition of glucuronidation reaction of drugs is a major reason for DDI. The aim of the present study is to predict propofol-thienorphine interaction from the perspective of propofol’s inhibition towards thienorphine glucuronidation. The human liver microsomes (HLMs) incubation system supplemented with uridine 5’-diphosphoglucuronic acid (UDPGA) was used. The results showed that propofol inhibited HLMscatalyzed thienorphine glucuronidation in a concentration-dependent manner. Both Dixon plot and Lineweaver-Burk plot showed that the inhibition of thienorphine glucuronidation by propofol was best fit to competitive inhibition, and the second plot using slopes from Lineweaver-Burk plot versus thienorphine concentration was used to determine the inhibition kinetic parameter (Ki ) value to be 365.9 μM. Whether the in vitro inhibition of propofol towards thienorphine glucuronidation can induce the in vivo propofolthienorphine interaction might be influenced by many factors, including various pharmacokinetic factors influencing the in vivo concentration of propofol. These data should be carefully explained due to complicated factors influencing the in vitro-in vivo extrapolation (IVIVE) results.
format Articulo
Comunicacion
author Zhang, Shu-Yao
Chen, Lei
Lin, Chao-Xian
Zhu, Zhi-Wei
Fang, Ling
Xin, Dai-Shan
Guo, Dai-Nian
author_facet Zhang, Shu-Yao
Chen, Lei
Lin, Chao-Xian
Zhu, Zhi-Wei
Fang, Ling
Xin, Dai-Shan
Guo, Dai-Nian
author_sort Zhang, Shu-Yao
title Propofol exhibits inhibitory effect towards human liver microsomes (HLMs)- catalyzed glucuronidation of thienorphine
title_short Propofol exhibits inhibitory effect towards human liver microsomes (HLMs)- catalyzed glucuronidation of thienorphine
title_full Propofol exhibits inhibitory effect towards human liver microsomes (HLMs)- catalyzed glucuronidation of thienorphine
title_fullStr Propofol exhibits inhibitory effect towards human liver microsomes (HLMs)- catalyzed glucuronidation of thienorphine
title_full_unstemmed Propofol exhibits inhibitory effect towards human liver microsomes (HLMs)- catalyzed glucuronidation of thienorphine
title_sort propofol exhibits inhibitory effect towards human liver microsomes (hlms)- catalyzed glucuronidation of thienorphine
publishDate 2012
url http://sedici.unlp.edu.ar/handle/10915/25730
http://www.latamjpharm.org/resumenes/31/6/LAJOP_31_6_2_5.pdf
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