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European Journal of Clinical Pharmacology

, Volume 53, Issue 2, pp 127–133 | Cite as

Comparative pharmacokinetics of dirithromycin and erythromycin in normal volunteers with special regard to accumulation in polymorphonuclear leukocytes and in saliva

  • H. F. Geerdes-Fenge
  • B. Goetschi
  • M. Rau
  • K. Borner
  • P. Koeppe
  • K. Wettich
  • H. Lode
PHARMACOKINETICS AND DISPOSITION

Abstract

Objective: In a randomized cross-over study, we assessed pharmacokinetics and intracellular concentrations in polymorphonuclear leukocytes (PMN) and saliva of erythromycin and erythromycylamine, the active metabolite of dirithromycin.

Methods: Ten healthy volunteers received 1 g erythromycin b.i.d. or 500 mg dirithromycin qd for 5 days (wash out period, 35 days). Concentrations of erythromycin and erythromycylamine were measured in serum, urine, saliva, and granulocytes by bioassay and high-performance liquid chromatography (HPLC) on days 1, 3, and 5 of each study period, respectively.

Results: While maximal serum concentrations (Cmax) and the area under the data (AUDtot) of erythromycin were significantly higher (Cmax 1.44 mg · l−1, AUDtot 5.66 mg · h · l−1) than those of erythromycylamine (Cmax 0.29 mg · l−1, AUDtot 1.96 mg · h · l−1), erythromycylamine had a significantly higher mean residence time (21 h) than erythromycin (5.5 h). Erythromycylamine accumulated significantly more in PMN than erythromycin;␣the accumulation factor of erythromycylamine was 100 with a maximal intracellular concentration of 13.4 mg · l−1, whereas the maximal accumulation factor of erythromycin was 4 with a maximal intracellular concentration of 6.1 mg · l−1. There were no significant differences in maximal saliva concentrations (erythromycin 0.35 mg · l−1, erythromycylamine 0.31 mg · l−1).

Key words Dirithromycin Erythromycin; polymorphonuclear leukocytes saliva accumulation 

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Copyright information

© Springer-Verlag Berlin Heidelberg 1997

Authors and Affiliations

  • H. F. Geerdes-Fenge
    • 1
  • B. Goetschi
    • 1
  • M. Rau
    • 1
  • K. Borner
    • 2
  • P. Koeppe
    • 3
  • K. Wettich
    • 4
  • H. Lode
    • 1
  1. 1.Department of Pulmonary and Infectious Diseases City Hospital Lungenklinik Heckeshorn, affil. Freie Universität Berlin Zum Heckeshorn 33 D-14109 Berlin, GermanyDE
  2. 2.Department of Clinical Chemistry and Biochemistry, Klinikum Benjamin Franklin, Freie Universität Berlin, D-12200 Berlin, GermanyDE
  3. 3.Department of Medical Physics and Laser Medicine, Klinikum Benjamin Franklin, Freie Universität Berlin, D-12200 Berlin, GermanyDE
  4. 4.Medical Department Lilly Deutschland GmbH, D-61350 Bad Homburg, GermanyDE

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