Azanza Perea José Ramón, Sádaba Díaz de Rada Belén
Servicio de Farmacología Clínica, Clínica Universidad de Navarra, Pamplona, España.
Servicio de Farmacología Clínica, Clínica Universidad de Navarra, Pamplona, España.
Rev Iberoam Micol. 2018 Oct-Dec;35(4):186-191. doi: 10.1016/j.riam.2018.04.003. Epub 2018 Nov 23.
Isavuconazole is a new azole, structurally related to fluconazole and voriconazole, that presents a very high oral absorption with no first-pass effect which is not interfered by the presence of food, gastric pH modifications, or mucositis. Its distribution volume is very high, probably also to cerebrospinal fluid, in spite of the fact that it circulates highly bound to plasma proteins. It is extensively metabolized through the CYP3A4 isoenzyme. Due to this reason, it is recommended to avoid co-administration with strong CYP3A4 inducers. In addition, isavuconazole may inhibit CYP3A4. Moreover, it may induce CYP2B6 and P-glycoprotein. Interestingly, this inhibitory activity seems to be lower compared to other azoles. Therefore, the management of any interaction with other medicines is easier, which is probably the most important advantage of this antifungal.
艾沙康唑是一种新型唑类药物，在结构上与氟康唑和伏立康唑相关，具有很高的口服吸收率，无首过效应，不受食物、胃pH值改变或粘膜炎的影响。尽管它与血浆蛋白高度结合循环，但分布容积非常大，可能也能进入脑脊液。它通过CYP3A4同工酶广泛代谢。因此，建议避免与强效CYP3A4诱导剂合用。此外，艾沙康唑可能抑制CYP3A4。而且，它可能诱导CYP2B6和P-糖蛋白。有趣的是，与其他唑类相比，这种抑制活性似乎较低。因此，与其他药物相互作用的管理更容易，这可能是这种抗真菌药物最重要的优势。
