IINFACTS - Institute of Research and Advanced Training in Health Sciences and Technologies, Department of Sciences, University Institute of Health Sciences (IUCS), Advanced Polytechnic and University Cooperative (CESPU), CRL, Gandra, Portugal.
Department of Public Health and Forensic Sciences, and Medical Education, Faculty of Medicine, University of Porto, Porto, Portugal.
Drug Metab Rev. 2021 Aug;53(3):375-383. doi: 10.1080/03602532.2021.1917599. Epub 2021 Apr 27.
Ulipristal acetate is a drug used as emergency contraceptive (30 mg) and for the treatment of moderate to severe symptoms of uterine myomas (5 mg). After commercialization, and although the exact number is unknown, serious cases implying ulipristal acetate 5 mg as a contributing factor of liver injury, some leading to transplantation, were reported. These cases prompted to a restrict use of the drug in January 2021 by the European Medicines Agency. This work aimed to fully review pharmacokinetic aspects, namely focusing in the ulipristal acetate metabolism and other hypothetical toxicological underlying mechanisms that may predispose to drug-induced liver injury (DILI). The high lipophilicity, the extensive hepatic metabolism, the long half-life of the drug and of its major active metabolite, the long-term course of treatment, and possibility due to the formation of epoxide reactive may be contributing factors. Scientific results also points evidence to consider monitorization of liver function during ulipristal acetate treatment.
醋酸乌利司他是一种药物，既可用作紧急避孕药（30 毫克），也可用于治疗子宫肌瘤的中度至重度症状（5 毫克）。商业化后，尽管确切数字未知，但有严重病例报告称，5 毫克醋酸乌利司他是导致肝损伤的一个因素，其中一些导致肝移植。这些病例促使欧洲药品管理局在 2021 年 1 月限制该药物的使用。本研究旨在全面审查药代动力学方面，特别是关注醋酸乌利司他的代谢以及其他可能导致药物性肝损伤（DILI）的潜在毒理学机制。该药物具有高亲脂性、广泛的肝代谢、较长的半衰期和其主要活性代谢物的半衰期、长期的治疗过程，以及由于形成环氧化物反应性可能是促成因素。科学研究结果还表明，在使用醋酸乌利司他期间，有必要监测肝功能。
