Department of Pharmacology, University of Padua, Italy.
Int J Antimicrob Agents. 1993 Jul;3(1):65-9. doi: 10.1016/0924-8579(93)90007-r.
The penetration of carumonam into the pleural exudate of rats was compared after intravenous administration of 30 mg kg(-1) of the drug as a bolus dose or by continuous infusion over 60 min. Both methods of administration ensured a good penetration of carumonam in pleural exudate, as measured by the areas under the concentration-time curves (AUC). The mean values of the ratio of AUC in exudate to AUC in serum (1.07 +/- 0.11 and 0.96 +/- 0.13 for bolus injection and continuous infusion, respectively) were not significantly different. Administration as a bolus dose resulted in significantly higher peak concentrations in pleural exudate as well as in shorter peak times, whereas continuous infusion produced carumonam levels above the MIC for consistently longer times. The pharmacokinetic parameters obtained by analysis of serum carumonam concentrations proved to be independent of the mode of administration. The foregoing results suggest that carumonam may constitute an effective therapeutic alternative to existing antibiotics for the treatment of pleurisy caused by susceptible organisms. No clear superiority of either method of administration could be established on the basis of pharmacokinetic data.
静脉注射 30mg/kg 剂量的卡芦莫南作为推注或持续输注 60 分钟后，比较了卡芦莫南在大鼠胸腔渗出液中的渗透情况。两种给药方式均能确保卡芦莫南在胸腔渗出液中有良好的渗透，这可以通过浓度-时间曲线下面积（AUC）来衡量。渗出液 AUC 与血清 AUC 比值的平均值（分别为 1.07±0.11 和 0.96±0.13，推注和持续输注）无显著差异。推注给药可使胸腔渗出液中的峰浓度显著升高，达峰时间缩短，而持续输注则可使卡芦莫南的浓度持续高于 MIC。通过分析血清卡芦莫南浓度得到的药代动力学参数与给药方式无关。上述结果表明，卡芦莫南可能成为治疗敏感菌引起的胸膜炎的一种有效治疗选择。根据药代动力学数据，两种给药方式均无明显优势。
