Pharmacokinetics of R- and S-Carvedilol in Routinely Treated Japanese Patients with Heart Failure

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Author(s)

Abstract

The purpose of this study was to evaluate the pharmacokinetics of <i>R</i>- and <i>S</i>-carvedilol in routinely treated Japanese patients with heart failure. We measured peak and trough blood concentrations at steady state following repeated oral administration to 24 patients. The blood concentration of <i>S</i>-carvedilol with potent β-blocking activity was lower than that of <i>R</i>-carvedilol. The mean oral clearance (<i>CL</i>/<i>F</i>) of <i>R</i>- and <i>S</i>-carvedilol was not altered by <i>CYP2D6*10</i>, <i>UGT2B7*3</i>, and the etiology of heart failure. In addition, the <i>CL</i>/<i>F</i> values of enantiomers were not correlated with age, creatinine clearance, and plasma concentrations of α<sub>1</sub>-acid glycoprotein and brain natriuretic peptide. On the other hand, the mean <i>CL</i>/<i>F</i> values of <i>R</i>- and <i>S</i>-carvedilol in patients with heart failure were 0.89 and 1.52 l/h/kg, respectively, considerably lower than those estimated previously in healthy subjects. These results suggested that the pharmacokinetics of <i>R</i>- and <i>S</i>-carvedilol was altered significantly by heart failure.

Journal

  • Biological and Pharmaceutical Bulletin

    Biological and Pharmaceutical Bulletin 31(5), 976-980, 2008-05-01

    The Pharmaceutical Society of Japan

References:  24

Cited by:  3

Codes

  • NII Article ID (NAID)
    110006663963
  • NII NACSIS-CAT ID (NCID)
    AA10885497
  • Text Lang
    ENG
  • Article Type
    Journal Article
  • ISSN
    09186158
  • NDL Article ID
    9474198
  • NDL Source Classification
    ZS51(科学技術--薬学)
  • NDL Call No.
    Z53-V41
  • Data Source
    CJP  CJPref  NDL  NII-ELS  J-STAGE 
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