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Chinese Journal of Clinical Pharmacology and Therapeutics ›› 2018, Vol. 23 ›› Issue (12): 1368-1372.doi: 10.12092/j.issn.1009-2501.2018.12.009

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Effects of CYP2A6*4 gene polymorphism on dexmedetomidine pharmacokinetics

FENG Shuling 1,2, WANG Ling 1,2, WANG Shaoming 1,2, ZHUANG Jie 1,2, QI Juan 2,3, YU Rongguo 2,4   

  1. 1 Department of Pharmacy, Fujian Provincial Hospital; 2 Provincial Clinical College of Fujian Medical University; 3 Second Department of Anesthesiology, Fujian Provincial Hospital; 4 Surgery Intensive Care Unit, Fujian Provincial Hospital, Fuzhou 350001, Fujian, China
  • Received:2018-06-19 Revised:2018-08-01 Online:2018-12-26 Published:2018-12-27

Abstract:

AIM: To determine the dexmedetomidine pharmacokinetics of CYP2A6*4 allele in Chinese patients with high mutation frequency of CYP2A6*4 in order to provide clinical references. METHODS: Thirty-one surgery patients received 0.5 μg/kg dexmedetomidine via intravenous pump. Their plasma concentrations at multiple time-points and polymorphism of CYP2A6*4 were determined and statistically analyzed.RESULTS:Nine patients were *1/*4 or *4/*4 , and 22 patients were *1/*1. The main pharmacokinetic parameters were area under curve (AUC) (1 396.19±332.47)h·ng·L-1, peak blood concentration (Cmax) (495.50±104.90)ng/L, distribution volume (V) (0.68±0.20)L/kg, clearance (CL) (0.38±0.11)L·h-1·kg-1, distribution half-life (t1/2α) (0.05±0.01)h, elimination half-life (t1/2β) (2.53±0.04)h. No significant pharmacokinetic differences were found among CYP2A6*1/*1, *1/*4, and *4/*4 patients.CONCLUSION: In Chinese patients treated with dexmedetomidine, t1/2β is consistent with that published, but t1/2α, V and CL are lower. It is unnecessary to consider the mutation when developing the precision regimen of dexmedetomidine.

Key words: dexmedetomidine, CYP2A6, pharmacokinetics, gene polymorphism

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