Toxicologic and metabolic studies on 2, 4-dimethoxy-6-sulfanilamido-1, 3-diazine (madribon)

Autor: Recha Engelberg, Robert E. Bagdon, Lowell O. Randall
Rok vydání: 1959
Předmět:
Zdroj: Toxicology and applied pharmacology. 1(1)
ISSN: 0041-008X
Popis: Sulfadimethoxine (2,4-dimethoxy-6-sulfanilamido-1,3-diazine) is a new sulfonamide having low toxicity after single oral administration to rats and dogs. Chronic toxicity studies of sulfadimethoxine [Madribon (Ro-4-0517)] were conducted in rats at dose levels of 25, 50, 100, and 200 mg/kg and in dogs at 20, 40, 80, and 160 mg/kg. As the results of these studies do not indicate a direct toxic effect of sulfadimethoxine upon the tissues studied, the question of whether or not this new sulfonamide will produce hypersensitivity reactions awaits further evaluation in man. After oral administration to rats the tissue concentrations of sulfadimethoxine are, in decreasing order: blood, kidney, liver, muscle and brain. Repeated daily doses increase the concentration on the second or third day, but there is no further cumulative action. After single doses, the sulfonamide is present in tissues for at least 4 days. The half-life in blood is 48 hours. After a single dose, 59% was excreted in the urine in 48 hours. After multiple doses, 48–53% was excreted daily. A large proportion is excreted in the bound form in rats.
Databáze: OpenAIRE