Zusammenfassung
Oralcephalosporine (Cefixim, Cefdinir, Cefetamet, Ceftibuten, Cefpodoxim, Loracarbef, Cefprozil, Cefuroxim, Cefaclor, Cefadroxil und BAY 3522) wurden nach antibakteriellem Profil und Stabilität gegenüber neuen β-Laktamasen verglichen. Erhöhte Aktivität plus Erweiterung des antibakteriellen Spektrums wurde insbesondere bei den von parenteralen Cephalosporinen (vom Oximino-Typ) hergeleiteten Substanzen wie Cefixim, Cefdinir, Cefetamet, Ceftibuten und Cefpodoxim festgestellt. Die höchste Antistaphylokokkenwirkung unter den Oralcephalosporinen liegt vor bei Cefdinir, Cefprozil und BAY 3522. Cefetamet, Ceftibuten und Cefixim verfügen über keine klinisch relevante Antistaphylokokkenwirkung, die übrigen Substanzen unterscheiden sich nur unwesentlich in ihrer Aktivität gegenüber Staphylokokken. Die größte Breite im antibakteriellen Spektrum erreichen Cefdinir und Cefpodoxim. Wirkungslücken im Spektrum der bisherigen Oralcephalosporine, die auch durch die neuen Substanzen nicht geschlossen werden, bestehen beiEnterobacter-Arten,Morganella, Listeria, Pseudomonas- undAcinetobacter-Arten, methicillinresistenten Staphylokokken,Enterococus-Arten, penicillinresistenten Pneumokokken und Anaerobiern. Neue β-Laktamasen (TEM-3, TEM-5, TEM-6, TEM-7, SHV-2, SHV-3, SHV-4, SHV-5, CMY-1, CMY-2, CTX-M) hydrolysieren die Mehrzahl der Oralcephalosporine. Über β-Laktamase-Stabilität, die zum Teil deutlich höher liegt als die parenteraler Cephalosporine, verfügen jedoch Ceftibuten, Cefetamet, Cefixim und Cefdinir. Neue Oralcephalosporine lassen aufgrund ihres antibakteriellen Profils einen Fortschritt in der Therapie mit resorbierbaren Cephalosporinen erwarten, und zwar einmal bei Erregern aus dem Wirkungsspektrum bisheriger Oralcephalosporine (günstigere Relation zwischen MHK und Serumspitzenspiegel), insbesondere aber bei Infektionen mit Erregern außerhalb des Spektrums der älteren Oralcephalosporine (z. B.Proteus spp.,Providencia spp.Citrobacter spp.,Serratia spp.).
Summary
Oral cephalosporins (cefixime, cefdinir, cefetamet, ceftibuten, cefpodoxime, loracarbef, cefprozil, cefuroxime, cefaclor, cefadroxil and BAY 3522) were compared by their antibacterial profile including stability against new betalactamases. Both activity and antibacterial spectrum of compounds structurally related to third generation parenteral cephalosporins (of the oximino class) were superior to established compounds. Activity against staphylococci was found to be highest for cefdinir, cefprozil and BAY 3522. Cefetamet, ceftibuten and cefixime demonstrate no clinically meaningful antistaphylococcal activity while the other compounds investigated demonstrate intermediate activity. The antibacterial spectrum was broadest for cefdinir and cefpodoxime. New oral cephalosporins are equally inactive as established compounds againstEnterobacter spp.,Morganella, Listeria, Pseudomonas andAcinetobacter spp., methicillin-resistant staphylococci,Enterococcus spp., penicillin-resistant pneumococci and anaerobes. New extended broad-spectrum betalactamases (TEM-3, TEM-5, TEM-6, TEM-7, SHV-2, SHV-3, SHV-4, SHV-5, CMY-1, CMY-2, and CTX-M) are active against the majority of oral cephalosporins. Ceftibuten, cefetamet, cefixime and cefdinir were stable against some of these enzymes even to a higher extent than parenteral cephalosporins. New oral cephalosporins should improve the therapeutic perspectives of oral cephalosporins due to their higher activity against pathogens marginally susceptible to established compounds (higher multiplicity of maximum plasma concentrations over MICs of the pathogens) and furthermore by including in their spectrum organisms resistant to established absorbable cephalosporins (e. g.Proteus spp.,Providencia spp.,Citrobacter spp., andSerratia spp.).
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Bauernfeind, A., Jungwirth, R., Schweighart, S. et al. Antibakterielle Aktivität und β-Laktamase-Stabilität von elf Oralcephalosporinen. Infection 18 (Suppl 3), S155–S167 (1990). https://doi.org/10.1007/BF01644637
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DOI: https://doi.org/10.1007/BF01644637