Fillastre J P, Moulin B, Godin M, Frelon J H
U.E.R. Médecine, University of Rouen, France.
Antimicrob Agents Chemother. 1988 Jun;32(6):942-4. doi: 10.1128/AAC.32.6.942.
Apalcillin is a new semisynthetic penicillin used as a sodium salt. More than 4,000 patients have been treated with this antibiotic, but increased serum creatinine levels were noted in 18 cases. In 5 of these cases, apalcillin was possibly responsible, and in 13 it was doubtful. We decided to study renal function of normal volunteers treated with 4 g of apalcillin. Three periods were studied: a pretreatment control period of 80 min followed by a treatment period of 60 min and a posttreatment period of 40 min. Inulin and p-aminohippurate (PAH) infusion were continued during all three periods. At the beginning of the treatment period, 2 g of apalcillin was injected as a bolus, followed by infusion of 2 g of apalcillin over 1 h. Urinary volume was measured every 20 min. Creatinine, insulin, and PAH clearances and urinary excretion of sodium, potassium, calcium, and magnesium were calculated for each period. Urinary beta-2-microglobulin excretion was also assessed. Analysis of variance was done. We observed no variation in clearances of creatinine or inulin or in urinary electrolyte output. PAH clearance was significantly decreased during apalcillin infusion. Apalcillin appeared to compete with PAH for proximal tubular secretion but induced no further renal dysfunction.
阿帕西林是一种用作钠盐的新型半合成青霉素。已有4000多名患者接受了这种抗生素治疗，但有18例患者血清肌酐水平升高。其中5例可能与阿帕西林有关，13例情况存疑。我们决定研究4克阿帕西林治疗的正常志愿者的肾功能。研究了三个阶段：80分钟的治疗前对照期，随后是60分钟的治疗期和40分钟的治疗后期。在所有三个阶段均持续输注菊粉和对氨基马尿酸（PAH）。在治疗期开始时，静脉推注2克阿帕西林，随后在1小时内输注2克阿帕西林。每20分钟测量一次尿量。计算每个阶段的肌酐、胰岛素和PAH清除率以及钠、钾、钙和镁的尿排泄量。还评估了尿β2微球蛋白排泄量。进行了方差分析。我们观察到肌酐或菊粉清除率以及尿电解质输出没有变化。在阿帕西林输注期间，PAH清除率显著降低。阿帕西林似乎与PAH竞争近端肾小管分泌，但未引起进一步的肾功能障碍。
