Welling P G, Dean S, Selen A, Kendall M J, Wise R
Br J Clin Pharmacol. 1979 Nov;8(5):491-5. doi: 10.1111/j.1365-2125.1979.tb01032.x.
1 The influence of probenecid on serum levels and urinary excretion of orally administered cephradine and cefaclor has been investigated. 2 Probenecid caused serum levels of both antibiotics to be increased and also prolonged. Urinary excretion of antibiotic activity was slightly but not significantly decreased by probenecid during the initial 6 h postdosing. It was significantly increased in 6-12 h urine, but only a small percentage of the doses were excreted during that period. 3 The increased serum levels of antibiotic were greater than could be accounted for by reduced elimination rate alone. Possible mechanisms to account for increased circulating levels of antibiotic in the presence of probenecid are discussed in the light of previous observations on probenecid induced changes in tissue distribution of beta-lactam antibiotics.
1 已研究了丙磺舒对口服头孢拉定和头孢克洛的血清水平及尿排泄的影响。2 丙磺舒使两种抗生素的血清水平升高且持续时间延长。给药后最初6小时内,丙磺舒使抗生素活性的尿排泄略有减少,但不显著。在6 - 12小时的尿液中排泄显著增加,但在此期间仅排出少量剂量。3 抗生素血清水平的升高幅度大于仅由消除率降低所能解释的程度。根据先前关于丙磺舒引起β-内酰胺类抗生素组织分布变化的观察结果,讨论了在丙磺舒存在下抗生素循环水平升高的可能机制。