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Transintestinal elimination of ciprofloxacin in humans — Concomitant assessment of its metabolites in serum, ileum and colon

Transintestinale Elimination von Ciprofloxacin beim Menschen — gleichzeitige Bestimmung seiner Metaboliten in Ileum und Colon

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Summary

Ciprofloxacin (200 mg) was infused to seven patients at the beginning of elective colorectal surgery. Thirty minutes after the end of infusion (i.e. 60 min after the start of the operation) ciprofloxacin reached concentrations of 1.60 mg/l in serum and of 3.42–6.07 mg/kg fresh weight in the ileum and colon. During the next 30 min (90 min after the start of operation) the concentration of ciprofloxacin in serum decreased to 86% of its initial level, but this decrease was less rapid than that observed in the ileal (to 56.8%) or colonic (to 74.8%) mucosa. Three metabolites could be identified (desethylen-, sulpho-, oxociprofloxacin). Initially, at 60 min the amount of these metabolites was about 15% of the total drug concentration in serum, but only 2–3% of that in the tissues. At 90 min the relative amount of metabolites was increased in serum as well as in the gut tissues. It is concluded that transintestinal elimination of ciprofloxacin is a general feature of the whole gut. Obviously, the elimination process is not due to degradation of ciprofloxacin within the gut wall.

Zusammenfassung

Ciprofloxacin (200 mg) wurde sieben Patienten zu Beginn eines Elektiveingriffs am Colorectum infundiert (für 30 Minuten). 30 Minuten nach Ende der Infusion (d.h. 60 Minuten nach Beginn der Operation) lag die Serumkonzentration des Antibiotikums bei 1,60 mg/l, im Ileum und Colon zwischen 3,42 – 6,07 mg/kg Frischgewicht. Während der nächsten 30 Minuten (90 Minuten nach Operationsbeginn) fiel die Konzentration im Serum signifikant auf 86%, aber weniger rasch als in der Ileum-Mucosa (auf 56%) oder Colon-Mucosa (auf 74,8%). Drei Metaboliten konnten identifiziert werden (Desethylen-, Sulpho- und Oxociprofloxacin). Ihr Gesamtanteil im Serum lag anfangs (60 Minuten nach Operationsbeginn) bei 15%, in den getesteten Darmbereichen aber nur bei 2 bis 3%. 90 Minuten nach OP-Beginn war ihr Gehalt sowohl im Serum als auch im Darmgewebe angestiegen. Die Ergebnisse führen zu dem Schluß, daß eine transintestinale Elimination von Ciprofloxacin über den gesamten Darm möglich ist. Offensichtlich erfolgt die Elimination aber nicht durch extensiven Abbau des Antibiotikums in der Darmwand.

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Authors and Affiliations

  1. II. Chirurgischer Lehrstuhl der Universität, Ostmerheimer Str. 200, W-5000, Köln 91, Germany

    B. Viell, Bettina Krause & S. Schaaf

  2. Abt. Allgemeinchirurgie, Städtisches Krankenhaus, Zentrum für operative Medizin, Dhünnberg 60, W-5090, Leverkusen 1, Germany

    K. Vestweber

  3. Bayer AG, Geschäftsbereich Pharma, Ressort Analytik und Qualitätskontrolle, Aprather Weg, W-5600, Wuppertal 1, Germany

    H. Scholl

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  1. B. Viell
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  2. Bettina Krause
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  3. S. Schaaf
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  4. K. Vestweber
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  5. H. Scholl
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Viell, B., Krause, B., Schaaf, S. et al. Transintestinal elimination of ciprofloxacin in humans — Concomitant assessment of its metabolites in serum, ileum and colon. Infection 20, 324–327 (1992). https://doi.org/10.1007/BF01710676

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