University Medical Center Utrecht, Clinical Pharmacy, Utrecht.
Haga Teaching Hospital, Pulmonary Diseases, The Hague.
Ther Drug Monit. 2020 Aug;42(4):595-599. doi: 10.1097/FTD.0000000000000743.
In the era of multiple daily dosing of systemic aminoglycosides, a circadian rhythm in the clearance of these vital antibiotics has been demonstrated in animals and healthy volunteers. Over the past decade, once-daily dosing regimens have been proved to be less nephrotoxic and were therefore adopted worldwide for most indications requiring treatment with an aminoglycoside. In this study, the effect of the time of administration on the pharmacokinetics of once-daily tobramycin in adults with cystic fibrosis (CF) experiencing a pulmonary exacerbation was investigated.
In this open randomized study, patients with CF received intravenous tobramycin at 8:00 or 22:00 hours. Pharmacokinetic and kidney function parameters were compared between the 2 groups.
Twenty-five patients were included. The mean weight-corrected clearances of tobramycin were 1.46 versus 1.43 mL/h*kg (P = 0.50) and mean volumes of distribution were 0.25 versus 0.27 L/kg (P = 0.54) for the 8:00 and 22:00 groups, respectively. In addition, no significant differences were detected in changes in estimated clearances of creatinine or tobramycin on day 1 and day 8 in the 8:00 or 22:00 group, indicating that there was no decline in clearance over time. At day 8 of therapy, the increase in serum blood urea nitrogen in the 22:00 group was significantly higher than that in the 8:00 group (1.8 versus 0.2 mmol/L, P = 0.015).
The time of administration (8:00 versus 22:00) did not affect tobramycin pharmacokinetics in the adult CF population studied. The increase in serum blood urea nitrogen in the 22:00 group requires further investigation.
在每日多次给予全身氨基糖苷类药物的时代,已在动物和健康志愿者中证明这些重要抗生素的清除具有昼夜节律。在过去的十年中,每日一次的给药方案已被证明肾毒性较小,因此已在全球范围内被用于大多数需要氨基糖苷类药物治疗的适应症。在这项研究中,研究了在经历肺部恶化的囊性纤维化(CF)成人中,给药时间对单次给予妥布霉素的药代动力学的影响。
在这项开放,随机研究中,CF 患者在 8:00 或 22:00 时接受静脉注射妥布霉素。比较两组之间的药代动力学和肾功能参数。
共纳入 25 例患者。妥布霉素的平均体重校正清除率分别为 1.46 与 1.43 mL/h*kg(P = 0.50),分布容积分别为 0.25 与 0.27 L/kg(P = 0.54),8:00 组和 22:00 组。此外,在第 1 天和第 8 天,8:00 或 22:00 组中,估计的肌酐或妥布霉素清除率没有明显变化,表明清除率没有随时间下降。在治疗的第 8 天,22:00 组的血清血尿素氮升高明显高于 8:00 组(1.8 与 0.2 mmol/L,P = 0.015)。
在研究的成年 CF 人群中,给药时间(8:00 与 22:00)并未影响妥布霉素的药代动力学。22:00 组中血清血尿素氮的增加需要进一步研究。