Martínková J, Chládková J, Kopecká J, Chládek J, Tilser I, Maresová J, Parízková E
Oddĕlení klinické farmakologie FN, Hradec Králové.
Cesk Pediatr. 1992 Apr;47(4):210-6.
The authors investigated in a group of 19 premature neonates with a low birthweight (0.65-2.1 kg) during the first four days of postnatal life the pharmacokinetics of gentamycin after indicated administration of 2 mg/kg of the antibiotic by the i.v. route by a 30-minute infusion in 18-hour intervals. Serum concentrations of gentamycin were assessed by immunoassay 0.5 hours before administration and then 0.5, 5.5, 11.5 and 17.5 hours after the 5th infusion, i.e. in a steady state. The maximum serum concentrations detected 0.5 hours after the completed infusion exceeded 10 mg/l in 21% of the neonates, while the minimal concentrations of the antibiotic before the next administration were above 2 mg/l in 42% of the infants. The calculation of pharmacokinetic parameters according to the one-compartment model revealed considerable interindividual differences of all values. The authors consider particularly important the low clearance value of the antibiotic (30.24 +/- 14.55 ml/kg.hour-1) which may lead to cumulation of gentamycin and its toxic action. Gentamycin administration to premature neonates should be associated with monitoring of serum concentrations of the drug which would make individual adjustment of the dosage possible.
作者对19名出生体重低(0.65 - 2.1千克)的早产新生儿在出生后前四天进行了研究,通过静脉途径以2毫克/千克的剂量每隔18小时输注30分钟庆大霉素,观察其药代动力学。在给药前0.5小时以及在第5次输注后处于稳态时的0.5、5.5、11.5和17.5小时,通过免疫测定法评估庆大霉素的血清浓度。在输注完成后0.5小时检测到的最大血清浓度在21%的新生儿中超过10毫克/升,而在下一次给药前抗生素的最低浓度在42%的婴儿中高于2毫克/升。根据单室模型计算药代动力学参数显示所有值存在相当大的个体间差异。作者特别认为抗生素的低清除率值(30.24±14.55毫升/千克·小时-1)很重要,这可能导致庆大霉素蓄积及其毒性作用。给早产新生儿使用庆大霉素时应监测药物的血清浓度,以便能够对剂量进行个体化调整。