Pharmacokinetics of azithromycin in normal and impaired renal function

Pharmakokinetik von Azithromycin bei normaler und eingeschränkter Nierenfunktion

Summary

Plasma and urine levels of 12 healthy subjects and 30 patients with renal insufficiency of different degrees were examined after oral administration of four 250 mg capsules azithromycin (total daily dose 1,000 mg). The concentrations were determined by cup plate method. The pharmacokinetic parameters were determined model-dependent and noncompartmentally. Neither the area under the plasma concentration curve nor the distribution volume in steady state (16 l/kg body weight) nor the maximal plasma concentration were significantly affected by renal insufficiency. Thus the dosage regimen of azithromycin in renal impairment may (and should) be the same as in patients with normal renal function. The nonrenal clearance is not affected by renal insufficiency, but the concentration of the substance in the tubular lumen (the “tubular load”) may be increased.

Zusammenfassung

Plasma- und Urinspiegel von Azithromycin wurden bei 12 Normalpersonen und bei 30 Patienten mit Niereninsuffizienz verschiedenen Grades untersucht. Die Probanden hatten zuvor vier Kapseln zu 250 mg Azithromycin erhalten. Die Bestimmung erfolgte mittels des Platten-Loch-Testes. Die pharmakokinetischen Parameter wurden Modell-abhängig und Modell-unabhängig ermittelt. Weder die Fläche unter der Kurve (AUC) noch das Verteilungsvolumen im Steady State (16 l/kg Körpergewicht) noch die maximale Plasmakonzentration war bei Niereninsuffizienz signifikant verändert. Folglich kann und muß die Dosierung von Azithromycin bei Niereninsuffizienz genauso erfolgen wie bei Patienten mit normaler Nierenfunktion. Die nichtrenale Clearance ist bei Niereninsuffizienz nicht verändert, jedoch ist die Konzentration der Substanz im Tubuluslumen (das tubuläre load) erhöht.

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Höffler, D., Paeske, B. & Koeppe, P. Pharmacokinetics of azithromycin in normal and impaired renal function. Infection 23, 356–361 (1995). https://doi.org/10.1007/BF01713565

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Keywords

  • Pharmacokinetic Parameter
  • Renal Impairment
  • Renal Insufficiency
  • Azithromycin
  • Normal Renal Function