Naber K, Adam D
Arzneimittelforschung. 1983;33(3):429-32.
In severe, sometimes life-threatening infections azlocillin (Securopen) is administered in single doses up to 10 g in order to increase therapeutic efficacy. Therefore the serum concentrations and urinary excretion of azlocillin were investigated in 2 healthy volunteers and in 11 patients after intravenous injection (5 min) of 2 g followed by intravenous infusion of 2 g/h over 4 h. The serum concentrations increased during infusion in patients up to a median concentration of 317 mg/l. The median serum concentrations decreased down to 94 mg/l at 2 h, 43 mg/l at 4 h and 11 mg/l at 6 h after the end of infusion. 24-h urinary excretion in patients was 54.3%. Serum half-life from the last five serum concentrations (6-10 hours after start of administration) calculated amounts to a median half life of 100 min (range 60-180 min). The study showed, that using this dose and kind of administration high serum concentrations can be maintained over many hours, sufficiently high also for life threatening and difficult-to-treat infections, if administered at intervals of 12 hours.
在严重的、有时甚至危及生命的感染中，为提高治疗效果，阿洛西林（舒氨西林）单次给药剂量可达10g。因此，对2名健康志愿者和11名患者进行了研究，静脉注射2g（5分钟）后，接着4小时内以2g/小时的速度静脉输注，然后测定阿洛西林的血清浓度和尿排泄情况。在输注过程中，患者的血清浓度升高，中位浓度达到317mg/l。输注结束后2小时，中位血清浓度降至94mg/l，4小时降至43mg/l，6小时降至11mg/l。患者24小时尿排泄率为54.3%。根据最后五个血清浓度（给药开始后6 - 10小时）计算得出的血清半衰期，中位半衰期为100分钟（范围60 - 180分钟）。研究表明，采用这种剂量和给药方式，如果每12小时给药一次，可在数小时内维持较高的血清浓度，对于危及生命和难以治疗的感染来说，该浓度也足够高。
