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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
 
 
 

Plasma protein binding of sulphadiazine, sulphamethoxazole and trimethoprim determined by ultrafiltration.

The plasma protein binding of trimethoprim, sulphadiazine and sulphamethoxazole was studied at 37 degrees C by ultrafiltration. Plasma samples contained steady state levels of the drugs from ten volunteers from a cross-over comparative pharmacokinetic study on co-trimazine and co-trimoxazole. The three compounds were determined in plasma and ultrafiltrate by HPLC, the recoveries being close to 100% in each case. Freezing of spiked samples had no influence on the binding. Trimethoprim was 48.5-52.2% bound (mean 50.0%); sulphadiazine was 50.9-60.6% bound (mean 56.2%); and sulphamethoxazole was 74.3-80.8% bound (mean 76.9%). The significantly lower protein binding of sulphadiazine compared to sulphamethoxazole means that equivalent non-protein bound plasma levels of the two sulphonamides are achieved from smaller doses of co-trimazine than co-trimoxazole. Use of co-trimazine may thus minimize the risk of adverse reactions.[1]

References

  1. Plasma protein binding of sulphadiazine, sulphamethoxazole and trimethoprim determined by ultrafiltration. Wijkström, A., Westerlund, D. Journal of pharmaceutical and biomedical analysis. (1983) [Pubmed]
 
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