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头孢吡肟脓肿穿透:脓液中的浓度和模拟药代动力学特征。

Abscess penetration of cefpirome: concentrations and simulated pharmacokinetic profiles in pus.

机构信息

Department of Clinical Pharmacology, Medical University of Vienna, Währinger Gürtel 18-20, 1090, Vienna, Austria.

出版信息

Eur J Clin Pharmacol. 2012 Oct;68(10):1419-23. doi: 10.1007/s00228-012-1270-1. Epub 2012 Mar 23.

Abstract

PURPOSE

Abscess patients frequently receive antibiotic therapy when incision cannot be performed or in addition to incision. However, antibiotic concentrations in human abscesses are widely unknown.

METHODS

Pharmacokinetics of cefpirome in 12 human abscesses located in different body regions was studied. Cefpirome (2 g) was administered as an intravenous short infusion, and concentrations were measured in plasma over an 8-h period and in abscesses at incision. A pharmacokinetic two-stage model was applied.

RESULTS

At abscess incision performed 158 ± 112 min after the start of the infusion, the cefpirome concentrations in the abscess fluid varied markedly, ranging from ≤0.1 (limit of quantification) to 47 (mean 8.4 ± 14.1 ) mg/L. Cefpirome was detectable in nine of 12 abscesses. Maximum concentrations were calculated to be 183 ± 106 mg/L in plasma and 12 ± 16 mg/L in the abscess. A cefpirome concentration of 2 mg/L, which is the minimum concentration inhibiting growth of 90% of the most relevant bacterial pathogens, was exceeded spontaneously in six of 12 abscesses after a single dose. Cefpirome concentrations in the abscess did not correlate with either the pH or the ratio of surface area to volume of the abscesses, nor with plasma pharmacokinetics.

CONCLUSIONS

Cefpirome may be useful to treat abscess patients because it was detectable in most abscesses after a single dose. However, the penetration of cefpirome into abscesses is extremely variable and cannot be predicted by measuring other available covariates.

摘要

目的

当无法进行切开引流或切开引流之外还需要使用抗生素治疗脓肿患者。然而,人体脓肿中的抗生素浓度却知之甚少。

方法

研究了 12 例位于不同身体部位的人类脓肿中头孢吡肟的药代动力学。静脉内短时间输注头孢吡肟(2 g),在 8 小时内测量血浆中的浓度,并在切开引流时测量脓肿中的浓度。应用两阶段药代动力学模型。

结果

在输注开始后 158±112 分钟进行脓肿切开引流时,脓肿液中的头孢吡肟浓度差异很大,范围从≤0.1(定量下限)至 47(平均 8.4±14.1)mg/L。在 12 个脓肿中有 9 个可检测到头孢吡肟。最大浓度计算为血浆中 183±106 mg/L 和脓肿中 12±16 mg/L。单次剂量后,6 个脓肿中的头孢吡肟浓度自发超过 2 毫克/升,这是抑制 90%最相关细菌病原体生长的最小浓度。脓肿中的头孢吡肟浓度与 pH 值或脓肿表面积与体积比均无相关性,也与血浆药代动力学无关。

结论

头孢吡肟可能对治疗脓肿患者有用,因为它在单次剂量后可在大多数脓肿中检测到。然而,头孢吡肟进入脓肿的渗透情况极其多变,无法通过测量其他可用的协变量来预测。

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