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Comparative in vivo activity of bacampicillin and amoxycillin

Vergleichendè In vivo-Aktivität von Bacampicillin und Amoxycillin

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Summary

Bacampicillin is an orally well-absorbed pro-drug of ampicillin giving high in vivo levels of the latter. Its therapeutic activity was compared with that of amoxycillin in two experimental infection models in mice. The animals were infected with suspensions ofEscherichia coli III andHaemophilus influenzae 22863 intraperitoneally and treated orally four hours afterwards with one of the two compounds. The antibacterial activity of the compounds was determined as CD50 values or by making viable counts in the blood and in organ homogenates of the animals. Ampicillin and amoxycillin had the same inhibitory but different bactericidal activity against the test strains. Both compounds appeared to have similar therapeutic activity and were found to cause a rapid decrease of the bacterial counts in the animals. Bacampicillin appeared to give a more rapid bactericidal activity than amoxycillin against theHaemophilus influenzae strain, whereas amoxycillin initially appeared more bactericidal against theEscherichia coli infection.

Zusammenfassung

Bacampicillin ist ein oral gut absorbiertes Pro-Drug von Ampicillin, das hohe Serum- und Gewebespiegel des letzteren gibt. Seine therapeutische Aktivität wurde mit derjenigen des Amoxycillins in zwei experimentellen Infektionsmodellen bei Mäusen verglichen. Die Tiere wurden intraperitoneal mit Suspensionen vonEscherichia coli III undHaemophilus influenzae 22863 infiziert und vier Stunden danach mit Bacampicillin oder Amoxycillin oral behandelt. Die antibakterielle Aktivität der beiden Verbindungen wurde als CD50-Wert oder durch Keimzählung im Blut und in Organhomogenaten der Tiere gemessen. Ampicillin und Amoxycillin hatten die gleiche inhibitorische aber eine unterschiedliche bakterizide Aktivität gegen die Testkeime. Bacampicillin und Amoxycillin hatten ähnliche therapeutische Aktivität und verursachten beide eine schnelle Abnahme der Keimzahlen in den Tieren. Bacampicillin hatte eine schnellere bakterizide Wirkung als Amoxycillin gegen denHaemophilus influenzae-Stamm, während für Amoxycillin initial eine kräftigere Bakterizidie gegen dieEscherichia coli-Infektion gefunden wurde.

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Ekström, B., Jalar, L.-. & Magni, L. Comparative in vivo activity of bacampicillin and amoxycillin. Infection 7, S438–S442 (1979). https://doi.org/10.1007/BF01659766

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Keywords

  • Bactericidal Activity
  • Ampicillin
  • Rapid Decrease
  • Bacterial Count
  • Experimental Infection