Rodriguez N, Madsen P O, Welling P G
Antimicrob Agents Chemother. 1979 Mar;15(3):465-9. doi: 10.1128/AAC.15.3.465.
Serum levels and urinary excretion of cinoxacin were examined in healthy individuals after a two-step intravenous infusion in the presence and absence of probenecid. After dosing cinoxacin alone, steady-state serum levels were approached in 1 h and were maintained for an additional 2 h with a reduced infusion rate. After probenecid pretreatment, serum levels of cinoxacin continued to increase during 3 h of infusion, reaching levels approximately double those obtained with cinoxacin alone. The mean elimination half-life of cinoxacin from serum was increased from 1.3 to 3.5 h in the presence of probenecid, and renal clearance was significantly reduced, with 46% of dosed drug appearing in 7-h urines of probenecid-treated subjects compared with 68% in subjects receiving cinoxacin alone. Probenecid had no apparent influence on cinoxacin distribution in the body but caused a significant decrease in the rate of cinoxacin extrarenal elimination, possibly due to competition for a common metabolic pathway.
在健康个体中，于有丙磺舒和无丙磺舒存在的情况下，通过两步静脉输注来检测西诺沙星的血清水平和尿排泄情况。单独给予西诺沙星后，1小时内达到稳态血清水平，并以降低的输注速率再维持2小时。在丙磺舒预处理后，西诺沙星的血清水平在输注3小时期间持续升高，达到约为单独使用西诺沙星时两倍的水平。在丙磺舒存在的情况下，西诺沙星从血清中的平均消除半衰期从1.3小时增加到3.5小时，肾清除率显著降低，丙磺舒治疗组受试者给药剂量的46%出现在7小时尿中，而单独接受西诺沙星治疗的受试者这一比例为68%。丙磺舒对西诺沙星在体内的分布无明显影响，但导致西诺沙星肾外消除速率显著降低，这可能是由于对共同代谢途径的竞争所致。
