Guglielmo B J, Flaherty J F, Batman R, Barriere S L, Gambertoglio J G
Antimicrob Agents Chemother. 1986 Sep;30(3):359-60. doi: 10.1128/AAC.30.3.359.
Certain antipseudomonal penicillins, such as mezlocillin, exhibit a nonlinear pharmacokinetic disposition with increasing doses. We evaluated the effect of a single low dose (50 mg/kg) compared with a high dose (80 mg/kg) on the pharmacokinetics of ticarcillin in a crossover trial of eight healthy volunteers. No significant alteration in plasma clearance (130.1 +/- 36.5 versus 120.5 +/- 38.0 ml/min), nonrenal clearance (36.5 +/- 8.4 versus 33.4 +/- 18.5 ml/min), or volume of distribution at steady state (12.8 +/- 3.5 versus 12.3 +/- 4.5 liters) was observed between the low- and high-dose regimens, respectively. The elimination half-life remained unchanged between the two doses (67.9 +/- 14.3 versus 68.0 +/- 12.2 min). Unlike other newer antipseudomonal penicillins, ticarcillin did not display dose-dependent pharmacokinetic behavior with the range of doses used in the clinical setting.
某些抗假单胞菌青霉素,如美洛西林,随着剂量增加呈现非线性药代动力学特征。在一项针对8名健康志愿者的交叉试验中,我们评估了单剂量低剂量(50mg/kg)与高剂量(80mg/kg)对替卡西林药代动力学的影响。低剂量组与高剂量组之间,血浆清除率(分别为130.1±36.5与120.5±38.0ml/min)、非肾清除率(36.5±8.4与33.4±18.5ml/min)或稳态分布容积(12.8±3.5与12.3±4.5升)均未观察到显著变化。两剂量之间消除半衰期保持不变(67.9±14.3与68.0±12.2分钟)。与其他新型抗假单胞菌青霉素不同,替卡西林在临床使用的剂量范围内未表现出剂量依赖性药代动力学行为。