Effect of genetic polymorphism of CYP2B6 * 6 on pharmacokinetics and pharmacodynamics of single dose propofol in Chinese healthy subjects
10.13699/j.cnki.1001-6821.2018.09.013
- VernacularTitle:CYP2B6*6基因多态性对中国健康受试者单次注射丙泊酚的药代动力学和药效学影响
- Author:
An-Cheng GU
1
;
Wan-Wen CAO
;
Jian-Ping ZHANG
;
Zai-Sheng QIN
;
Bin CHEN
;
Peng-Xiang HUANG
;
Zhong-Yuan XU
Author Information
1. 南方医科大学南方医院药物临床试验中心
- Keywords:
CYP2B6 * 6;
propofol;
pharmacokinetics;
pharmacodynamics
- From:
The Chinese Journal of Clinical Pharmacology
2018;34(9):1052-1055
- CountryChina
- Language:Chinese
-
Abstract:
Objective To investigate the effects of CYP2B6 * 6 gene polymorphism on the pharmacokinetics and pharmacodynamics of propofol in Chinese healthy subjects.Methods Twenty male healthy subjects were intravenously injected a single dose of 2.0 mg · kg-1 propofol.The plasma concentration of propofol was examined by HPLC-MS/MS method.The genotype of the subjects was determined by pyrosequencing.The pharmacokinetics and pharmacodynamic parameters of different genotype were compared.Results Among the 20 subjects,there were 14 cases of G516T-GG,6 cases of G516T-GT/TT,10 cases of A785G-AA and 10 cases of A785G-AG/GG.The bispectral index-loss of conscious (BIS-LOC) of G516T-GT/TT group and G516T-GG group were 74.33 ± 7.20 and 60.43 ± 13.64,the t1/2β of A785G-AG/GG group and A785G-AA group were (0.13 ±0.06) and (0.41 ±0.38)h,with significant difference (P ＜ 0.05).Other parameters like Cmax,tmax,AUC0-t,AUC0-∞,t1/2α,MRT0-∞,t-LOC,BIS-LOC,BIS-ROC,t-BISmin,BISmin,d-LOC all had no statistical significance (all P ＞ 0.05).Conclusion The pharmacokine-tics and pharmacodynamics of propofol are correlated with the polymorphism of CYP2B6 * 6,individualized dosing regimens based on genotypes contribute to the rational use of propofol.
