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新型合成单环β-内酰胺类抗生素卡芦莫南的药代动力学及组织穿透性

Pharmacokinetics and tissue penetration of carumonam, a new synthetic monobactam.

作者信息

McNulty C A, Garden G M, Ashby J, Wise R

出版信息

Antimicrob Agents Chemother. 1985 Sep;28(3):425-7. doi: 10.1128/AAC.28.3.425.

DOI:10.1128/AAC.28.3.425
PMID:4073864
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC180266/
Abstract

The pharmacokinetics of the monobactam carumonam (Ro 17-2301) as derived from serial measurement of the concentrations of this agent in serum, blister fluid, and urine were studied in six male volunteers subsequent to intravenous infusion of a single 2-g dose. Drug levels in serum in excess of 75 micrograms/ml were achieved 0.5 h after the end of infusion, declining to 2.9 micrograms/ml at 8 h. The mean serum and blister fluid elimination half-lives were 1.68 and 1.7 h, respectively. The urinary recovery of the drug by 24 h was 80.6% (range, 68.3 to 91.1%). Carumonam penetrated blister fluid well, the mean percentage penetration (as measured by the ratio of areas under curves) being 101.6%.

摘要

在6名男性志愿者静脉输注单次2克剂量后,通过连续测定血清、水疱液和尿液中单环β-内酰胺类药物卡芦莫南(Ro 17 - 2301)的浓度,研究了其药代动力学。输注结束后0.5小时血清药物水平超过75微克/毫升,8小时时降至2.9微克/毫升。血清和水疱液的平均消除半衰期分别为1.68小时和1.7小时。24小时药物经尿液回收量为80.6%(范围为68.3%至91.1%)。卡芦莫南能很好地渗透入水疱液,平均渗透百分比(通过曲线下面积比测量)为101.6%。

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Pharmacokinetics and tissue penetration of carumonam, a new synthetic monobactam.新型合成单环β-内酰胺类抗生素卡芦莫南的药代动力学及组织穿透性
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本文引用的文献

1
The influence of protein binding upon tissue fluid levels of six beta-lactam antibiotics.蛋白质结合对六种β-内酰胺类抗生素组织液水平的影响。
J Infect Dis. 1980 Jul;142(1):77-82. doi: 10.1093/infdis/142.1.77.
2
Pharmacokinetics of the monobactam SQ 26,776 after single intravenous doses in healthy subjects.
J Antimicrob Chemother. 1981 Dec;8 Suppl E:131-40. doi: 10.1093/jac/8.suppl_e.131.
3
Pharmacokinetics and tissue penetration of azthreonam.氨曲南的药代动力学及组织穿透性。
Antimicrob Agents Chemother. 1982 Dec;22(6):969-71. doi: 10.1128/AAC.22.6.969.
4
Single-dose pharmacokinetics of Ro 17-2301 (AMA-1080), a monocyclic beta-lactam, in humans.单环β-内酰胺类药物Ro 17-2301(AMA-1080)在人体中的单剂量药代动力学。
Antimicrob Agents Chemother. 1984 Dec;26(6):898-902. doi: 10.1128/AAC.26.6.898.
5
The in-vitro activity of Ro 17-2301, a new monobactam, compared with other antimicrobial agents.新型单环β-内酰胺类抗生素Ro 17-2301与其他抗菌药物的体外活性比较。
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