The role of plasma protein binding on the metabolism and renal excretion of sulphadimethoxine and its metabolite N4-acetylsulphadimethoxine in pigs

The Veterinary Quarterly
M ShimodaT H Arts

Abstract

The effects of plasma protein binding on the elimination of sulphadimethoxine (SDM) were examined after intravenous administration of 6.25, 12.5, 25, 50, 100 and 150 mg/kg to pigs. At an early stage of the experiment, the animals were anaesthetised by inhalation of enflurane to obtain a more exact relationship between plasma concentration and the renal excretion. SDM and its acetylated conjugate, N4-acetylsulphadimethoxine (N4-SDM) were detected in plasma and urine of all animals, and the recovery of the doses was almost complete in two animals with negligible renal excretion of SDM. The percentages of plasma protein binding of SDM and N4-SDM were almost similar, and ranged from 30 to 95%, depending on the plasma concentration. The metabolic clearance of SDM by acetylation increased when the plasma protein binding decreased. These results suggested that the main elimination route of SDM in pigs is acetylation, and that the plasma protein binding can have a large effect on the elimination of SDM in pigs. The effect of plasma protein binding on the renal clearance of SDM was not so evident, because urine pH had a much greater effect on it. The deacetylation of N4-SDM was detected after 25 mg/kg intravenous administration of N4-SD...Continue Reading

References

Aug 1, 1975·British Journal of Clinical Pharmacology·D C Brown, J G Collier
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Aug 1, 1988·Journal of Pharmacobio-dynamics·M ShimodaT Hayama
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Citations

Apr 27, 1990·Pharmaceutisch Weekblad. Scientific Edition·T B VreeM Shimoda
Oct 18, 1991·Pharmaceutisch Weekblad. Scientific Edition·T B VreeY A Hekster
Dec 1, 1994·Antimicrobial Agents and Chemotherapy·J D ColmeneroE Valverde
Oct 1, 1991·The Veterinary Quarterly·T B VreeA Peeters
Feb 24, 2001·Journal of Veterinary Medicine. A, Physiology, Pathology, Clinical Medicine·Naoto Furusawa
Jan 1, 1992·Biopharmaceutics & Drug Disposition·T B VreeT Miura
May 31, 2001·Journal of Veterinary Medicine. A, Physiology, Pathology, Clinical Medicine·Naoto Furusawa

Related Concepts

N(4)-acetylsulfadimethoxine
Acetylation
Metazoa
Serum Proteins
Krebiozen
Hydrogen-Ion Concentration
Kidney
Plasma Protein Binding Capacity
Deposul
Family suidae

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