Modelling the atypical absorption of menatetrenone and the metabolism to its epoxide: effect of VKORC1 polymorphism.

This study aimed to model the atypical absorption of menatetrenone and its epoxide metabolite and to examine the influence of the single nucleotide polymorphism (SNP) of vitamin K2 epoxide reductase complex subunit 1 (VKORC1) on the pharmacokinetics. After the administration of 30 mg of menatetrenon...

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Publicado en:Journal of Clinical Pharmacy & Therapeutics Vol. 36; no. 3; pp. 390 - 399
Autores principales: Baek, I. H., Kang, W., Yun, H. Y., Lee, S. S., Kwon, K. I.
Formato: equations & formulas pictorial research tables/charts Journal Article
Publicado: Wiley-Blackwell Jun2011
Acceso en línea:Ver este registro en EBSCOhost
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      dt: Jun2011
      vid: 36
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      pub: Wiley-Blackwell
      place: Malden, Massachusetts
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        10.1111/j.1365-2710.2010.01183.x
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        atl: Modelling the atypical absorption of menatetrenone and the metabolism to its epoxide: effect of VKORC1 polymorphism.
      aug:
        au:
          Baek, I. H.
          Kang, W.
          Yun, H. Y.
          Lee, S. S.
          Kwon, K. I.
        affil: College of Pharmacy, Chungnam National University, Daejeon
      sug:
        subj:
          Polymorphism, Genetic
          Vitamin K Pharmacokinetics
          Vitamin K Blood
          Models, Biological
          Vitamin K Administration and Dosage
          Vitamin K Metabolism
          Mass Spectrometry Methods
          Genotype
          Human
          Male
          South Korea
          Descriptive Statistics
          Young Adult
          Adult
          Chromatography, High Pressure Liquid
          Linear Regression
          Intestinal Absorption
          Polymerase Chain Reaction
          Mann-Whitney U Test
          Biological Availability
          Funding Source
          Adult: 19-44 years
          Male
      ab: This study aimed to model the atypical absorption of menatetrenone and its epoxide metabolite and to examine the influence of the single nucleotide polymorphism (SNP) of vitamin K2 epoxide reductase complex subunit 1 (VKORC1) on the pharmacokinetics. After the administration of 30 mg of menatetrenone to 26 healthy subjects, the plasma concentrations of menatetrenone and its epoxide were measured using LC-MS/MS. For the haplotype analysis, the SNP of the VKORC1 gene was investigated in the 26 volunteers. The model parameters were estimated using the ADAPT II program. A two-compartment model with Weibull-type absorption and saturable elimination described the pharmacokinetics of menatetrenone and its epoxide. The plasma concentrations of both tended to be lower in the H1/H7 genotype group than in the wild-type H1/H1 group. We present the first detailed pharmacokinetic modelling of menatetrenone in relation to VKORC1 genotype. This study suggests that VKORC1 genotype is unlikely to be helpful in dose-selection because of the very high inter-individual variation in systemic exposure within each genotype group, and the small inter-group difference observed.
      pubtype: Academic Journal
      doctype:
        equations & formulas
        pictorial
        research
        tables/charts
        Journal Article
      ougenre: Article
    language: English
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