Autmizguine Julie, Guptill Jeffrey T, Cohen-Wolkowiez Michael, Benjamin Daniel K, Capparelli Edmund V
Duke Clinical Research Institute, 2400 Pratt St, PO Box 17969, Durham, NC, 27705, USA.
Drugs. 2014 Jun;74(8):891-909. doi: 10.1007/s40265-014-0227-3.
Invasive fungal disease (IFD) remains life threatening in premature infants and immunocompromised children despite the recent development of new antifungal agents. Optimal dosing of antifungals is one of the few factors clinicians can control to improve outcomes of IFD. However, dosing in children cannot be extrapolated from adult data because IFD pathophysiology, immune response, and drug disposition differ from adults. We critically examined the literature on pharmacokinetics (PK) and pharmacodynamics (PD) of antifungal agents and highlight recent developments in treating pediatric IFD. To match adult exposure in pediatric patients, dosing adjustment is necessary for almost all antifungals. In young infants, the maturation of renal and metabolic functions occurs rapidly and can significantly influence drug exposure. Fluconazole clearance doubles from birth to 28 days of life and, beyond the neonatal period, agents such as fluconazole, voriconazole, and micafungin require higher dosing than in adults because of faster clearance in children. As a result, dosing recommendations are specific to bracketed ranges of age. PD principles of antifungals mostly rely on in vitro and in vivo models but very few PD studies specifically address IFD in children. The exposure-response relationship may differ in younger children compared with adults, especially in infants with invasive candidiasis who are at higher risk of disseminated disease and meningoencephalitis, and by extension severe neurodevelopmental impairment. Micafungin is the only antifungal agent for which a specific target of exposure was proposed based on a neonatal hematogenous Candida meningoencephalitis animal model. In this review, we found that pediatric data on drug disposition of newer triazoles and echinocandins are lacking, dosing of older antifungals such as fluconazole and amphotericin B products still need optimization in young infants, and that target PK/PD indices need to be clinically validated for almost all antifungals in children. A better understanding of age-specific PK and PD of new antifungals in infants and children will help improve clinical outcomes of IFD by informing dosing and identifying future research areas.
尽管近年来新型抗真菌药物不断涌现,但侵袭性真菌病(IFD)对早产儿和免疫功能低下的儿童来说仍然危及生命。抗真菌药物的最佳剂量是临床医生能够控制的少数几个可改善IFD治疗效果的因素之一。然而,儿童用药剂量不能从成人数据推断得出,因为IFD的病理生理学、免疫反应和药物代谢与成人不同。我们严格审查了关于抗真菌药物药代动力学(PK)和药效学(PD)的文献,并着重介绍了治疗儿童IFD的最新进展。为使儿科患者达到与成人相当的药物暴露水平,几乎所有抗真菌药物都需要调整剂量。在幼儿中,肾脏和代谢功能迅速成熟,这会显著影响药物暴露。氟康唑清除率从出生到出生后28天会增加一倍,在新生儿期之后,由于儿童清除速度更快,氟康唑、伏立康唑和米卡芬净等药物的给药剂量需要高于成人。因此,给药建议是针对特定年龄范围的。抗真菌药物的PD原则大多依赖体外和体内模型,但很少有PD研究专门针对儿童IFD。与成人相比,年幼儿童的暴露-反应关系可能有所不同,尤其是侵袭性念珠菌病患儿,他们发生播散性疾病和脑膜脑炎的风险更高,进而发生严重神经发育障碍的风险也更高。基于新生儿血源性念珠菌性脑膜脑炎动物模型,米卡芬净是唯一一种提出了特定暴露目标的抗真菌药物。在本综述中,我们发现缺乏关于新型三唑类和棘白菌素类药物在儿童体内药物代谢的数据,氟康唑和两性霉素B等老一代抗真菌药物在幼儿中的给药剂量仍需优化,而且几乎所有抗真菌药物在儿童中的目标PK/PD指标都需要进行临床验证。更好地了解婴儿和儿童新型抗真菌药物的年龄特异性PK和PD,将有助于通过指导给药和确定未来研究领域来改善IFD的临床治疗效果。