Pharmacokinetics and metabolism of idebenone in healthy male subjects.

PURPOSE: Idebenone is a synthetic analogue of ubiquinone that may be beneficial in the treatment of Friedreich's ataxia. Since in previous pharmacokinetic trials only lower doses were studied, it was the aim of this study to evaluate the pharmacokinetics of idebenone in higher doses of up to 2,250 m...

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Publicado en:European Journal of Clinical Pharmacology Vol. 65; no. 5; pp. 493 - 502
Autores principales: Bodmer M, Vankan P, Dreier M, Kutz KW, Drewe J
Formato: equations & formulas research tables/charts Journal Article
Publicado: Springer Nature May2009
Acceso en línea:Ver este registro en EBSCOhost
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      dt: May2009
      vid: 65
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      pub: Springer Nature
      place: New York, New York
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        2010261634
        10.1007/s00228-008-0596-1
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        atl: Pharmacokinetics and metabolism of idebenone in healthy male subjects.
      aug:
        au:
          Bodmer M
          Vankan P
          Dreier M
          Kutz KW
          Drewe J
        affil: Department of Clinical Pharmacology, University Hospital Basel, Basel, Switzerland.
      sug:
        subj:
          Quinones Metabolism
          Quinones Pharmacokinetics
          Adult
          Coenzyme Q Metabolism
          Coenzyme Q Pharmacokinetics
          Data Analysis Software
          Descriptive Statistics
          Friedreich's Ataxia Therapy
          Male
          Pharmacy and Pharmacology
          Quinones Blood
          Quinones Urine
          Human
          Adult: 19-44 years
          Male
      ab: PURPOSE: Idebenone is a synthetic analogue of ubiquinone that may be beneficial in the treatment of Friedreich's ataxia. Since in previous pharmacokinetic trials only lower doses were studied, it was the aim of this study to evaluate the pharmacokinetics of idebenone in higher doses of up to 2,250 mg/day. METHODS: In this open, randomized trial, 25 healthy male subjects received first either a single oral dose of 150 mg or 750 mg of idebenone, then the same dose given at 8-h intervals for 14 days. RESULTS: Idebenone and its metabolites appeared in the plasma quickly. Over 99% of parent idebenone was metabolized, indicating a high first-pass effect. C(max) and AUC(0-t) values for parent idebenone and its metabolites increased in a dose-proportional manner. There was virtually no accumulation of parent drug or metabolites following multiple dosing. CONCLUSIONS: Idebenone exhibited dose-dependent pharmacokinetics in daily doses up to 2,250 mg. In 6/14 subjects, adverse events of mild to moderate severity were observed.
      pubtype: Academic Journal
      doctype:
        equations & formulas
        research
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      ougenre: Article
    language: English
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