Kelly H C, Hutchison M, Haworth S J
Zeneca Pharmaceuticals, Mereside, Macclesfield, Cheshire, UK.
J Antimicrob Chemother. 1995 Jul;36 Suppl A:35-41. doi: 10.1093/jac/36.suppl_a.35.
The pharmacokinetics of meropenem were determined in healthy volunteers after intravenous injection over 5 min or iv infusion over 30 min. Five volunteers received meropenem 500 mg and six volunteers received 1000 mg. For both doses, administration over 5 rather than 30 min doubled the plasma concentrations observed at the end of the dosing period. Comparison of the other data derived from the two modes of administration indicated that rapid administration of meropenem did not appreciably alter its disposition pharmacokinetics. Plasma clearance, renal clearance, non-renal clearance, terminal half-life and volume of distribution were unchanged. Within 1 h of dosing, the plasma concentrations were very similar indicating that dosing over either time period would result in similar antimicrobial cover and thus should not affect efficacy. There were no changes in tolerability of meropenem associated with more rapid administration.
在健康志愿者中,通过5分钟静脉注射或30分钟静脉输注测定了美罗培南的药代动力学。5名志愿者接受了500毫克美罗培南,6名志愿者接受了1000毫克美罗培南。对于这两种剂量,5分钟给药而非30分钟给药使给药期结束时观察到的血浆浓度加倍。对两种给药方式得出的其他数据进行比较表明,美罗培南的快速给药并未明显改变其处置药代动力学。血浆清除率、肾清除率、非肾清除率、终末半衰期和分布容积均未改变。给药后1小时内,血浆浓度非常相似,表明在任何一个时间段给药都会产生相似的抗菌覆盖,因此不应影响疗效。美罗培南的耐受性没有因更快给药而发生变化。