Estimation of CYP2 D6*10 genotypes on citalopram disposition in Chinese subjects by population pharmacokinetic assay.

What is known and objective There is great interindividual variability in citalopram ( CIT) pharmacokinetics. We attempted to establish a population pharmacokinetic ( PPK) model of CIT in Chinese healthy subjects, to evaluate the effect of genetic polymorphism on CIT pharmacokinetics and to compare...

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Publicado en:Journal of Clinical Pharmacy & Therapeutics Vol. 38; no. 6; pp. 504 - 512
Autores principales: Chen, B., Xu, Y., Jiang, T., Feng, R., Sun, J., Zhang, W., Yang, W., Li, J., Adeniyi, O., Chen, H.
Formato: equations & formulas research tables/charts randomized controlled trial Journal Article
Publicado: Wiley-Blackwell Dec2013
Acceso en línea:Ver este registro en EBSCOhost
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      dt: Dec2013
      vid: 38
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      pub: Wiley-Blackwell
      place: Malden, Massachusetts
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        104150457
        91673870
        10.1111/jcpt.12029
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        atl: Estimation of CYP2 D6*10 genotypes on citalopram disposition in Chinese subjects by population pharmacokinetic assay.
      aug:
        au:
          Chen, B.
          Xu, Y.
          Jiang, T.
          Feng, R.
          Sun, J.
          Zhang, W.
          Yang, W.
          Li, J.
          Adeniyi, O.
          Chen, H.
        affil: Department of Pharmacy, Ruijin Hospital School of Medicine Shanghai Jiaotong University
      sug:
        subj:
          Oxidoreductases
          Genotype
          Biological Assay
          Citalopram Pharmacokinetics
          Human
          Citalopram Blood
          Biological Availability
          Models, Statistical
          Chromatography, Liquid Methods
          Mass Spectrometry Methods
          Descriptive Statistics
          Goodness of Fit Chi Square Test
          Randomized Controlled Trials
          Crossover Design
          China
          Male
          Adult
          Polymerase Chain Reaction
          Data Analysis Software
          Post Hoc Analysis
          Kruskal-Wallis Test
          Mann-Whitney U Test
          Analysis of Variance
          Confidence Intervals
          Funding Source
          Adult: 19-44 years
          Male
      ab: What is known and objective There is great interindividual variability in citalopram ( CIT) pharmacokinetics. We attempted to establish a population pharmacokinetic ( PPK) model of CIT in Chinese healthy subjects, to evaluate the effect of genetic polymorphism on CIT pharmacokinetics and to compare the PPK and non-compartmental ( NCA) assays in the estimation of CIT bioequivalence. Methods Blood samples of 23 healthy subjects were collected after administration of CIT; plasma concentration of CIT was analysed using LC/ MS- MS. CYP2 C19 and CYP2 D6*10 genotypes were determined. PPK model was established by using nonlinear mixed-effect modelling ( NONMEM). The model was evaluated using goodness-of-fit plots and relative error measurements. Bioequivalence of CIT was evaluated by both PPK and NCA method. Results and discussion The estimated population absorption rate constant ( ka), clearance ( CL/ F) and volume of distribution (Vd/F) in Chinese healthy subjects are 0.64 L/h, 12.7 L/h and 705 L, respectively. Different CYP2 C19 and CYP2 D6 genotypes have impacts on CIT pharmacokinetics. There is about 5.5% decrement of CL/ F for each CYP2 C19*2 or CYP2 D6*10 allele. The 90% confidence interval of CIT bioavailability obtained from NCA and PPK model were 96.4-105.4% and 92.5-103.4%, respectively. What is new and conclusion The PPK of CIT is best characterized by a one-compartment disposition model with first-order absorption. CYP2 C19 and CYP2 D6 genotypes have impacts on the CL/F of CIT. Bioequivalence of CIT can be estimated by both NCA and PPK model.
      pubtype: Academic Journal
      doctype:
        equations & formulas
        research
        tables/charts
        randomized controlled trial
        Journal Article
      ougenre: Article
    language: English
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