Pharmacokinetics of rufloxacin once daily in patients with lower respiratory tract infections
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Summary
The pharmacokinetic properties of rufloxacin, a new quinolone antibacterial agent, were evaluated in ten patients with lower respiratory tract infections. Patients were given 400 mg of rufloxacin once a day for seven to nine days. Plasma concentrations of the drug were determined by high-performance liquid chromatography and bioassay at regular intervals during treatment. After the first administration, maximal plasma concentrations were 3.17±0.36 mg/l (mean ± SEM) and were reached at 4.2±0.7 h. At the end of treatment peak plasma concentrations increased to 7.26±0.52 mg/l. Elimination half-life was 38.2±2.9 h, with a mean extent of accumulation of 2.96±0.30. Treatment was well tolerated, with no abnormalities noted during routine laboratory examinations. Two days after the last administration, measurable levels of rufloxacin were still observed in plasma, indicating that the long half-life of rufloxacin assures valuable antibacterial activity even after discontinuation of treatment.
Keywords
Plasma Concentration Quinolone Pharmacokinetic Property Antibacterial Agent Peak Plasma ConcentrationPharmakokinetik von Rufloxacin bei Patienten mit tiefen Atemwegsinfektionen und einmal täglicher Gabe
Zusammenfassung
Bei zehn Patienten mit tiefen Atemwegsinfektionen wurden die pharmakokinetischen Eigenschaften von Rufloxacin, einem neuen Chinolon, untersucht. Die Patienten erhielten sieben bis zehn Tage lang einmal täglich 400 mg Rufloxacin. Während der Therapiephase wurden in regelmäßigen Abständen Messungen der Plasmakonzentrationen der Substanz mittels Hochdruckflüssigkeitchromatographie und mit Bioassay vorgenommen. Nach der ersten Dosis wurden Spitzenkonzentrationen von 3,17±0,36 mg/l (Mittelwert ± SEM) gemessen, die nach 4,2±0,7 h ereicht wurden. Am Ende der Therapiephase waren die Plasmaspitzenspiegel auf 7,26±0,52 mg/l angestiegen. Die Plasma-Eliminations-Halbwertszeit betrug 38,2±2,9 h mit einer mittleren Kumulation von 2,96±0,30. Die Therapie wurde gut vertragen, in den Routine-Laborparametern fanden sich keine Anomalien. Zwei Tage nach der letzten Dosis fanden sich im Plasma immer noch meßbare Rufloxacin-Spiegel, was zeigt, daß selbst nach Therapieende noch brauchbare Spiegel an Rufloxacin mit antibakteriellem Potential vorhanden sind.
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