Faculty of Pharmacy, University of Sydney, Camperdown, Australia.
Antimicrob Agents Chemother. 2012 Sep;56(9):4793-9. doi: 10.1128/AAC.00626-12. Epub 2012 Jul 2.
Voriconazole is a first-line agent in the treatment of many invasive fungal infections and is known to display highly variable pharmacokinetics. Previous studies of voriconazole therapeutic drug monitoring (TDM) have suggested concentration monitoring to be clinically useful but have been limited by small patient samples at a single institution. This multicenter retrospective study aimed to investigate relationships between voriconazole concentration and clinical outcomes and adverse events and to assess clinical factors and drug interactions that may affect voriconazole concentration. Medical records were reviewed for patients who received voriconazole and had at least 1 concentration measured at seven hospitals in Australia. The study included 201 patients with 783 voriconazole trough concentrations. Voriconazole concentrations of <1.7 mg/liter were associated with a significantly greater incidence of treatment failure (19/74 patients [26%]) than concentrations of ≥1.7 mg/liter (6/89 patients [7%]) (P < 0.01). Neurotoxic adverse events (visual and auditory hallucinations) occurred more frequently at voriconazole concentrations of >5 mg/liter (10/31 patients [32%]) than at concentrations of ≤5 mg/liter (2/170 patients [1.2%]) (P < 0.01). Multiple regression analysis of voriconazole concentration identified associations between increasing patient weight, oral administration of voriconazole, and coadministration of phenytoin or rifampin and significantly reduced concentrations, and associations between increasing patient age and coadministration of proton pump inhibitors and increased concentrations. Coadministration of glucocorticoids was found to significantly reduce voriconazole concentrations, inferring a previously unreported drug interaction between glucocorticoids and voriconazole.
伏立康唑是治疗多种侵袭性真菌感染的一线药物,其药代动力学变化较大。既往伏立康唑治疗药物监测(TDM)的研究表明,浓度监测具有临床意义,但受到单个机构小样本量的限制。本多中心回顾性研究旨在探讨伏立康唑浓度与临床结局和不良事件的关系,并评估可能影响伏立康唑浓度的临床因素和药物相互作用。对在澳大利亚 7 家医院接受伏立康唑治疗且至少有 1 次浓度检测的患者的病历进行了回顾。该研究纳入了 201 例患者,共检测了 783 次伏立康唑谷浓度。浓度<1.7mg/L 的患者治疗失败发生率(19/74 例[26%])显著高于浓度≥1.7mg/L 的患者(6/89 例[7%])(P<0.01)。浓度>5mg/L 的患者(10/31 例[32%])更常出现神经毒性不良事件(视觉和听觉幻觉),而浓度≤5mg/L 的患者(2/170 例[1.2%])则较少发生(P<0.01)。对伏立康唑浓度的多元回归分析发现,患者体重增加、口服伏立康唑、同时合用苯妥英或利福平与浓度显著降低有关,患者年龄增加、同时合用质子泵抑制剂与浓度增加有关。发现合用糖皮质激素可显著降低伏立康唑浓度,提示糖皮质激素和伏立康唑之间存在先前未报道的药物相互作用。