Division of Thoracic and Hyperbaric Surgery, Medical University of Graz, Graz, Austria.
J Antimicrob Chemother. 2011 Jan;66(1):160-4. doi: 10.1093/jac/dkq413. Epub 2010 Nov 16.
the objective of the present investigation was to measure the extracellular concentrations of cefpirome in unaffected and infected lung tissue of septic patients.
a single intravenous dose of 30 mg/kg total body weight of cefpirome was administered to eight patients every 12 h prior to insertion of microdialysis probes into lung tissue.
the median (minimum, maximum) peak concentration (C(max)), time to C(max) (T(max)), area under the concentration-time curve from 0 to 4 h (AUC(0-4)) and AUC(0-∞) of unbound cefpirome for unaffected lung were 48 (32, 107) mg/L, 0.83 (0.17, 3.17) h, 117 (60, 177) mg · h/L and 182 (80, 382) mg · h/L, respectively. The corresponding values for infected lung tissue were 45 (6, 122) mg/L, 1.17 (0.83, 2.83) h, 92 (17, 253) mg · h/L and 206 (49, 379) mg · h/L, respectively. The median apparent terminal elimination half-lives (t(½z)) of cefpirome were 2.61, 3.05 and 3.39 h for plasma, unaffected lung and infected lung, respectively. The median ratios of the AUC(0)(-∞) for lung to the AUC(0)(-∞) for plasma were 0.63 (0.19, 1.55) and 0.46 (0.32, 0.98) for unaffected and infected lung, respectively.
we provide strong evidence that cefpirome penetrates effectively into the extracellular space fluid of lung tissue. Under steady-state conditions, the median concentrations of cefpirome in plasma, unaffected lung and infected lung exceeded the MICs of the majority of relevant bacteria over the entire dosing interval of up to 12 h after intravenous administration of a dose of 30 mg/kg total body weight.
本研究旨在测量脓毒症患者未感染和感染肺组织中海头孢吡肟的细胞外浓度。
在向肺组织插入微透析探针之前，每 12 小时给 8 名患者静脉注射 30mg/kg 体重的头孢吡肟单剂量。
未感染肺组织中海头孢吡肟游离药物的峰浓度（Cmax）（最小值，最大值）、达峰时间（Tmax）、0 至 4 小时的浓度-时间曲线下面积（AUC（0-4））和 AUC（0-∞）中位数分别为 48（32，107）mg/L、0.83（0.17，3.17）h、117（60，177）mg·h/L 和 182（80，382）mg·h/L。感染肺组织的相应值分别为 45（6，122）mg/L、1.17（0.83，2.83）h、92（17，253）mg·h/L 和 206（49，379）mg·h/L。头孢吡肟的中位表观终末消除半衰期（t1/2z）分别为血浆、未感染肺和感染肺中的 2.61、3.05 和 3.39h。肺组织 AUC（0）（-∞）与血浆 AUC（0）（-∞）的中位数比值分别为 0.63（0.19，1.55）和 0.46（0.32，0.98），用于未感染和感染的肺组织。
我们提供了强有力的证据表明头孢吡肟有效地渗透到肺组织的细胞外液中。在稳态条件下，静脉注射 30mg/kg 体重剂量后，头孢吡肟在血浆、未感染肺和感染肺中的浓度中位数在整个 12 小时的给药间隔内超过了大多数相关细菌的 MIC。
