Ertapenem sodium (L-749345) is a β-lactam antibiotic of the carbapenem class with a modal MIC of 0.12μg/ml, which is active against both aerobic and anaerobic microorganisms[1-2]. Ertapenem sodium is highly stable against nearly all beta-lactamases, including AmpC and extended-spectrum beta-lactamases, except metallo-β-lactamases[3-4].
In vitro, using the broth microdilution method, 99.1% of the 556 clinical anaerobic isolates were inhibited by Ertapenem sodium at a concentration of 4μg/ml, with a modal MIC of 0.12μg/ml[1]. By using an agar dilution method, the comparative in vitro activities of Ertapenem sodium were studied against 1,001 anaerobes isolated from human intra-abdominal infections in 17 countries worldwide. Ertapenem sodium was uniformly active against all isolates, including all Bacteroides fragilis group species isolates, except for 12 of 61 (20%) strains of Bilophila wadsworthia, 3 strains of lactobacilli, and 1 isolate of Acidaminococcus fermentans[5].
In vivo, after a single intraperitoneal injection of Ertapenem sodium (10mg/kg of body weight) to CD-1 mice, the CFU of Staphylococcus aureus in the mice decreased[6]. After intravenous administration of Ertapenem sodium (10-180mg/kg) in rats, Ertapenem sodium exhibited extensive plasma protein binding in rat plasma, with the extent of binding being concentration-dependent at the plasma concentrations achieved following these doses[7].
References:
[1] Aldridge KE. Ertapenem (MK-0826), a new carbapenem: comparative in vitro activity against clinically significant anaerobes. Diagn Microbiol Infect Dis. 2002;44(2):181-186.
[2] Pedroso TM, Salgado HR. A Critical Review of Analytical Methods for Determination of Ertapenem Sodium. Crit Rev Anal Chem. 2016;46(1):15-21.
[3] Parakh A, Krishnamurthy S, Bhattacharya M. Ertapenem. Kathmandu Univ Med J (KUMJ). 2009;7(28):454-460.
[4] Kilińska K, Cielecka-Piontek J, Skibiński R, et al. The Radiation Sterilization of Ertapenem Sodium in the Solid State. Molecules. 2019;24(16):2944.
[5] Goldstein EJ, Citron DM, Vreni Merriam C, Warren Y, Tyrrell KL. Comparative In vitro activities of ertapenem (MK-0826) against 1,001 anaerobes isolated from human intra-abdominal infections. Antimicrob Agents Chemother. 2000;44(9):2389-2394.
[6] Gill CJ, Jackson JJ, Gerckens LS, et al. In vivo activity and pharmacokinetic evaluation of a novel long-acting carbapenem antibiotic, MK-826 (L-749,345). Antimicrob Agents Chemother. 1998;42(8):1996-2001.
[7] Wong BK, Bruhin PJ, Lin JH. Dose-dependent plasma clearance of MK-826, a carbapenem antibiotic, arising from concentration-dependent plasma protein binding in rats and monkeys. J Pharm Sci. 1999;88(2):277-280.
Ertapenem sodium (L-749345)是一种碳青霉烯类的β-内酰胺抗生素，其MIC众数为0.12μg/ml，对需氧和厌氧微生物都具有活性[1-2]。Ertapenem sodium对几乎所有β-内酰胺酶（包括AmpC和广谱β-内酰胺酶）都非常稳定，但对金属β-内酰胺酶除外[3-4]。
在体外，采用肉汤微量稀释法，99.1%的556株临床厌氧菌分离株被Ertapenem sodium在4μg/ml的浓度下抑制，其MIC众数为0.12μg/ml[1]。采用琼脂稀释法，研究了Ertapenem sodium对来自全球17个国家的人类腹腔内感染的1001株厌氧菌的体外活性。Ertapenem sodium对所有菌株，包括所有脆弱拟杆菌群种的菌株，均表现出均匀的活性，但有61株沃氏双叶菌中的12株（20%）、3株乳杆菌和1株发酵酸胺菌例外[5]。
在体内，对CD-1小鼠进行单次腹腔注射Ertapenem sodium（10mg/kg体重）后，小鼠体内金黄色葡萄球菌的CFU减少[6]。在大鼠中静脉注射Ertapenem sodium（10-180mg/kg）后，Ertapenem sodium在大鼠血浆中与血浆蛋白广泛结合，且在这些剂量给药后达到的血浆浓度下，结合程度呈浓度依赖性[7]。