Summary
The concentration of antibiotic in a focus of infection depends both on the peak serum concentration and on the area under the serum concentration time curve (AUC). A knowledge of the relationship between increased doses and the corresponding response in serum concentration would be relevant as a basis for determining an adequate clinical dosage. Dose-related changes in the two pharmacokinetic variables, peak serum concentration and AUC, after single doses of bacampicillin are compared with data on different aminopenicillins from other studies. With ampicillin there is a nonlinear relationship between both dose-peak and dose-AUC. The results indicate that the poor absorption of oral ampicillin can only be partially compensated for by increasing the oral dose. But with amoxycillin and the ampicillin esters the absorbed amount (AUC) is a linear function of the dose in the dosage range investigated. The increase in peak serum level with high doses of oral ampicillin is far less than proportional, while this tendency was less pronounced for amoxycillin and still less for pivampicillin, talampicillin and bacampicillin.
Zusammenfassung
Die Konzentration eines Antibiotikums in einem Infektionsherd hängt sowohl von der Serumspitzenkonzentration als auch von der Fläche unter der Serum Konzentrations-Zeitkurve (AUC) ab. Die Kenntnis der Beziehung zwischen Dosiserhöhung und dem folgenden Verhalten der Serumkonzentration wäre entscheidend als Basis für die Festlegung einer angemessenen klinischen Dosierung. Dosis-abhängige Veränderungen in den beiden pharmakokinetischen Variablen, der Serum Spitzenkonzentration und der AUC nach Einzeldosen Bacampicillin werden mit Daten von verschiedenen Aminopenicillinen aus anderen Studien verglichen. Bei Ampicillin besteht eine nicht-lineare Beziehung zwischen Dosis und Spitzenspiegel und Dosis und AUC. Die Ergebnisse zeigen, daß die schlechte Absorption von oralem Ampicillin nur teilweise durch Erhöhung der oralen Dosis kompensiert werden kann. Bei Amoxycillin und den Ampicillin Estern hingegen ist die absorbierte Menge (AUC) eine lineare Funktion der Dosis im untersuchten Dosierungsbereich. Die Erhöhung des Serumspitzenspiegels mit hohen Dosen oralem Ampicillin ist wesentlich geringer als proportional, bei Amoxycillin ist diese Tendenz weniger und bei Pivampicillin, Talampicillin und Bacampicillin entschieden weniger ausgeprägt.
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Sjövall, J. Dose dependence in human absorption of aminopenicillins. Infection 7 (Suppl 5), S458–S462 (1979). https://doi.org/10.1007/BF01659771
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DOI: https://doi.org/10.1007/BF01659771