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首页> 外文期刊>Antimicrobial agents and chemotherapy. >Pharmacodynamics of RWJ-54428 against Staphylococcus aureus, Streptococcus pneumoniae, and Enterococcus faecalis in a neutropenic mouse thigh infection model.
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Pharmacodynamics of RWJ-54428 against Staphylococcus aureus, Streptococcus pneumoniae, and Enterococcus faecalis in a neutropenic mouse thigh infection model.

机译：RWJ-54428对金黄色葡萄球菌，肺炎链球菌和粪肠球菌在中性粒细胞减少症小鼠大腿感染模型中的药效学。

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摘要

RWJ-54428 (also known as MC-02,479) is a new cephalosporin with promising activity against gram-positive bacteria. The pharmacodynamics (PDs) of RWJ-54428 against Staphylococcus aureus, Streptococcus pneumoniae, and Enterococcus faecalis were studied in a neutropenic mouse thigh infection model. The RWJ-54428 MICs ranged from 0.25 to 1 mg/liter. Mice with ca. 10(6) CFU/thigh at the initiation of therapy were treated intraperitoneally with RWJ-54428 at doses that ranged from 3 to 1,200 mg/kg of body weight/day (in 2, 3, 4, 6, or 12 divided doses) for 24 h. The maximal reductions in bacterial counts in thigh tissues at 24 h for the methicillin-resistant S. aureus, penicillin-resistant S. pneumoniae, and E. faecalis strains were -2.8, -3.8, and -1.7 log10 CFU/thigh, respectively. The percentage of a 24-h dosing interval that the unbound serum RWJ-54428 concentrations exceeded the MIC (fT>MIC) was the pharmacokinetic (PK)-PD parameter that best described the efficacy of RWJ-54428. The fT>MICs for a bacteriostatic effect (no net change in the numbers of CFU/thigh over 24 h) ranged from 14 to 20% for staphylococci and streptococci; for maximal reductions in the numbers of CFU/thigh, the fT>MICs ranged from 22 to 36% for these strains. For E. faecalis, the ranges of fT>MICs for static and maximal effects were 30 to 46% and 55 to 60%, respectively. These data show that treatment with RWJ-54428 results in marked antibacterial effects in vivo, with the PK-PD parameters for efficacy being comparable to those for the efficacy of penicillins and carbapenems active against staphylococci and pneumococci.
机译：RWJ-54428（也称为MC-02,479）是一种新型头孢菌素，具有抗革兰氏阳性细菌的活性。在中性粒细胞减少的小鼠大腿感染模型中研究了RWJ-54428对金黄色葡萄球菌，肺炎链球菌和粪肠球菌的药效学（PDs）。 RWJ-54428 MIC的范围为0.25至1毫克/升。约有小鼠。在治疗开始时，以3至1,200 mg / kg体重/天的剂量（2、3、4、6或12个分剂量）用RWJ-54428腹膜内治疗10（6）CFU /大腿持续24小时。耐甲氧西林的金黄色葡萄球菌，耐青霉素的肺炎链球菌和粪肠球菌菌株在24 h时大腿组织中细菌计数的最大减少分别为-2.8，-3.8和-1.7 log10 CFU /大腿。未结合的血清RWJ-54428浓度超过MIC（fT> MIC）的24小时给药间隔百分比是最能描述RWJ-54428疗效的药代动力学（PK）-PD参数。对于葡萄球菌和链球菌，具有抑菌作用的fT> MIC（24小时内CFU /大腿数目无净变化）范围为14％至20％;为了最大程度降低CFU /大腿的数量，这些菌株的fT> MIC范围为22％至36％。对于粪肠球菌，静态和最大效应的fT> MIC范围分别为30％至46％和55％至60％。这些数据表明，用RWJ-54428处理可在体内产生显着的抗菌作用，其功效的PK-PD参数可与对葡萄球菌和肺炎球菌有活性的青霉素和碳青霉烯的功效相当。

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