These tools will no longer be maintained as of December 31, 2024. Archived website can be found here. PubMed4Hh GitHub repository can be found here. Contact NLM Customer Service if you have questions.


Pubmed for Handhelds

PUBMED FOR HANDHELDS

Search MEDLINE/PubMed

  • Title: CYP2D6 phenotype determines pharmacokinetic variability of propafenone enantiomers in 16 HAN Chinese subjects.
    Author: Cai WM, Chen B, Cai MH, Zhang YD.
    Journal: Zhongguo Yao Li Xue Bao; 1999 Aug; 20(8):720-4. PubMed ID: 10678105.
    Abstract:
    AIM: To determine the role of the CYP2D6 phenotype in the metabolism of propafenone (Pro) enantiomers in 16 HAN Chinese subjects. METHODS: Seven very extensive metabolizers (VEM) and nine intermediate metabolizers (IM) were enrolled from a Chinese population whose phenotype had been previously assessed with a dextromethorphan metabolic phenotyping. The blood samples (0-15 h) were taken after oral administration of a single dose (400 mg) of rac-Pro hydrochloride. Enantiomeric concentrations of propafenone in plasma were measured by a reverse-phase HPLC with precolumn derivatization. RESULTS: S-Pro was less metabolized and had higher plasma concentrations than R-Pro in both CYP2D6 phenotypes. Besides, the T1/2 of R-Pro was longer than that of S-Pro in IM, but not in VEM. However, there were significant differences in the metabolism of Pro enantiomers between VEM and IM. The Cmax and AUC of both isomers in the IM group were higher than those in the VEM group (P < 0.01). The Cl of Pro enantiomers in IM group was only about half of that in VEM group [(67 +/- 17) vs (133 +/- 28) L.h-1 for S-Pro, (90 +/- 24) vs (200 +/- 87) L.h-1 for R-Pro, P < 0.01]. The S/R ratios of T1/2, Tmax, Cmax, Cl, and AUC were not significantly different (P > 0.05). CONCLUSION: CYP2D6 phenotype determines the pharmacokinetic variability of propafenone enantiomers and existence of IM may be relevant to diminished capacity of CYP2D6 enzyme in Chinese subjects.
    [Abstract] [Full Text] [Related] [New Search]