Nakamura T, Takano M, Yasuhara M, Inui K
Department of Pharmacy, Kyoto University Hospital, Faculty of Medicine, Kyoto University, Japan.
J Pharm Pharmacol. 1996 Nov;48(11):1197-200. doi: 10.1111/j.2042-7158.1996.tb03920.x.
The renal handling of vancomycin in rats and the effects of various drugs (probenecid, cimetidine and quinidine) on urinary excretion of the antibiotic were investigated by in-vivo clearance. The vancomycin-to-inulin excretion ratio (ER) was greater than unity at various infusion rates of vancomycin. Quinidine, co-administered with vancomycin, significantly decreased the total, renal and net secretory clearance of the antibiotic. Cimetidine also decreased, though not significantly, the secretory clearance of vancomycin by about 20%, but probenecid did not. These results suggested that vancomycin is secreted in renal tubules in rats, and that quinidine decreases the total clearance of vancomycin partly by inhibiting its tubular secretion in the kidney.
通过体内清除率研究了大鼠对万古霉素的肾脏处理以及各种药物(丙磺舒、西咪替丁和奎尼丁)对该抗生素尿排泄的影响。在万古霉素的不同输注速率下,万古霉素与菊粉的排泄率(ER)大于1。与万古霉素联合给药时,奎尼丁显著降低了该抗生素的总清除率、肾脏清除率和净分泌清除率。西咪替丁也降低了万古霉素的分泌清除率,虽然降幅不显著,但约降低了20%,而丙磺舒则没有。这些结果表明,万古霉素在大鼠肾小管中分泌,且奎尼丁部分通过抑制其在肾脏中的肾小管分泌来降低万古霉素的总清除率。