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Mammary and Renal Excretion of Sulphadoxine and Trimethoprim in Cows
Acta Veterinaria Scandinavica volume 15, pages 340–355 (1974)
Abstract
DAVITIYANANDA, DANIS and FOLKE RASMUSSEN: Mammary and renal excretion of sulphadoxine and trimethoprim in cows. Acta vet. scand. 1974, 15, 340–355. — In 21 experiments on 5 healthy, nonpregnant cows are sulphadoxine and trimethoprim infused intravenously for maintenance of constant levels of the drugs through the experimental periods. The experiments show that both sulphadoxine and trimethoprim are bound to the proteins in blood plasma and milk. Further it is demonstrated that sulphadoxine (an acid) is excreted into milk in concentrations lower than in blood plasma while trimethoprim (a base) is excreted into milk in concentrations higher than in blood plasma. Both results are consistent with the theory that drugs are excreted through the mammary gland by passive diffusion.
Glomerular filtration and back-diffusion are both involved in the renal handling of sulphadoxine and trimethoprim. For trimethoprim active tubular secretion is also demonstrated. Both the mammary and renal handling of sulphadoxine as well as trimethoprim are influenced by the pH of milk and urine, respectively. The experiments underline that it is the unionized, non-protein-bound fraction of the drugs which diffuses through biological membranes.
sulphadoxine; trimethoprim; mammary excretion; renal excretion; cow.
Sammanfattning
Mammær og renal ekskreiion af sulfadoxin og trimethoprim hos køer.
I 21 forsøg på normale, ikke drægtige køer er der ved intravenøs infusion af sulfadoxin og trimethoprim opretholdt konstante koncentrationer af disse lægemidler. Forsøgene viser, at bade sulfadoxin og trimethoprim bindes til proteinerne i blodplasma og mælk. Det fremgår endvidere af forsøgene, at sulfadoxin, som er en syre, udskilles i maelken i koncentrationer, der er lavere end i blodplasma, mens trimethoprim, som er en base, udskilles i maelken i koncentrationer, der er højere end i blodplasma. De opnåede resultater er i overensstemmelse med teorien om, at laegemidler udskilles med maelken ved passiv diffusion.
Den renale udskillelse af sulfadoxin og trimethoprim involverer glomerular filtration og tilbagediffusion. Hertil kommer, at trimethoprim tillige udskilles ved aktiv tubulær Sekretion. Såvel den mammære som den renale ekskretion af sulfadoxin og trimethoprim er påvirkelig af pH i mælk og urin. Forsøgene har vist, at det er den ikke-ioniserede og ikke-proteinbundne fraktion af lægemidler, der diffunderer gennem biologiske membraner.
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Supported by the Danish Agricultural and Veterinary Research Council.
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Davitiyananda, D., Rasmussen, F. Mammary and Renal Excretion of Sulphadoxine and Trimethoprim in Cows. Acta Vet Scand 15, 340–355 (1974). https://doi.org/10.1186/BF03547463
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DOI: https://doi.org/10.1186/BF03547463