Summary
In this review the pharmacokinetic properties of trimethoprim (TMP) and TMP/sulphonamide combinations are discussed. The concentration of both substances in the various body fluids and tissues differ considerably from the concentrations in blood due to the different distribution of TMP and sulphonamides in the body. As a rule the ratio of the concentration of TMP to sulphonamide is higher in most body fluids and secretions than in blood. If inflammation is present, the concentrations vary considerably. The pharmacokinetic data must be taken into account when making in vitro tests. At the site of inflammation a TMP/sulphonamide concentration factor of 1:0.5 to 1:4 can be expected in urine and of 1:2 to 1:5 in tissue.
Zusammenfassung
In dieser Übersicht werden die pharmakokinetischen Eigenschaften von Trimethoprim (TMP) und TMP-/Sulfonamid-Kombinationen diskutiert. Auf Grund der unterschiedlichen Verteilung von TMP und Sulfonamiden im Körper weichen die Konzentrationsverhältnisse der beiden Substanzen in verschiedenen Körperflüssigkeiten und Geweben erheblich von den Konzentrationen im Blut ab. In der Regel ist das Verhältnis der Konzentration von TMP zu Sulfonamid in den meisten Körperflüssigkeiten und Sekreten größer als im Blut. Bei Entzündung variieren die Konzentrationsverhältnisse erheblich. Bei der In-vitro-Testung sollten die pharmakokinetischen Daten unbedingt berücksichtigt werden. Am Ort der Entzündung ist mit einem TMP-/Sulfonamid-Konzentrations-Faktor von 1:0,5 bis 1:4 im Urin und mit einem Faktor von 1:2 bis 1:5 im Gewebe zu rechnen.
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Reeves, D.S., Wilkinson, P.J. The pharmacokinetics of trimethoprim and trimethoprim/sulphonamide combinations, including penetration into body tissues. Infection 7 (Suppl 4), S330–S341 (1979). https://doi.org/10.1007/BF01639009
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DOI: https://doi.org/10.1007/BF01639009