Summary
Co-trimazine is a new drug combination especially designed for the treatment of urinary tract infections. It consists of trimethoprim (90 mg) and sulphadiazine (410 mg). When combined in vitro, the components show high activity and a high frequency of synergy against urinary tract pathogens. After oral absorption sulphadiazine has a serum half-life similar to that of trimethoprim and is excreted in active form into the urine to a much higher degree than sulphamethoxazole. The ratio of the concentrations of trimethoprim and sulphadiazine in the urine following co-trimazine is favourable for a strong synergistic action between the compounds. In cross-over studies in volunteers receiving repeated daily doses of co-trimazine, either 500 mg twice daily or 1000 mg once daily, it was found that the antibacterial activity in the urine was at least as high as that provided by co-trimoxazole (2 × 960 mg) and considerably higher and more uniform than that given by nitrofurantion (3 × 50 mg).
Zusammenfassung
Co-trimazine ist eine neue Kombination aus Trimethoprim (90 mg) und Sulfadiazin (410 mg), die besonders für die Behandlung von Harnwegsinfektionen entwickelt worden ist. Kombinationen von Trimethoprim und Sulfadiazin zeigen in vitro eine hohe Aktivität und in hohem Ausmaße synergistische Wirkung gegen Erreger der Harnwegsinfektionen. Nach oraler Gabe zeigt Sulfadiazin praktisch dieselbe Halbwertszeit in Serum wie Trimethoprim und wird in viel höherem Ausmaß als Sulfametoxazol in aktiver Form in den Harn ausgeschieden. Das Konzentrationsverhältnis Trimethoprim zu Sulfadiazin, das in Harn von Co-trimazine gegeben wird, begünstigt eine synergistische Wirkung zwischen den beiden Komponenten. In Cross-over-Versuchen bei Freiwilligen mit wiederholter Gabe zeigte Co-trimazine (2 × 500 mg und 1 × 1000 mg) eine antibakterielle Aktivität im Harn, die mindestens so hoch war wie die von Co-trimoxazole (2 × 960 mg) und deutlich höher und gleichmäßiger als die von Nitrofurantoin (3 × 50 mg).
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Ekström, B., Fellner, H., Magni, L. et al. Antibacterial activity of Co-trimazine in vitro and in vivo. Infection 7, 74–80 (1979). https://doi.org/10.1007/BF01641617
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DOI: https://doi.org/10.1007/BF01641617