Wuyts Stephanie C M, Moor Joris De, Jochmans Kristin, Cortoos Pieter-Jan, Vandervorst Fenne, Steurbaut Stephane, Dupont Alain G, Cornu Pieter
Pharmacy Department, Universitair Ziekenhuis Brussel (UZ Brussel), Brussels, Belgium.
Research Centre for Digital Medicine, Vrije Universiteit Brussel (VUB), Brussels, Belgium.
Br J Clin Pharmacol. 2025 Apr;91(4):1114-1131. doi: 10.1002/bcp.70007. Epub 2025 Feb 24.
Direct oral anticoagulants (DOACs) are frequently used for the treatment and prevention of ischaemic stroke in patients with non-valvular atrial fibrillation. Compared to vitamin K antagonists, DOACs have significant advantages, although their drug-drug interaction (DDI) profile may complicate drug efficacy and safety. This narrative review addresses the clinical challenges posed by these DDIs and the potential pharmacological alternatives and monitoring strategies available. A PubMed search was conducted (1 January 2000-31 December 2023) including human DDI studies on DOAC use and CYP3A4/P-gp inducers in adult patients, evaluating patient outcome data and recommendations for DDI management. Twenty-two studies were included. Case reports (n = 6) indicated that antiepileptic drugs such as carbamazepine, phenobarbital and phenytoin may be associated with thromboembolic events. The nested case-control studies (n = 2) and cohort studies (n = 9) found that co-administration of DOACs and CYP3A4/P-gp inducers, particularly carbamazepine and phenytoin, increased the risk of thromboembolic events. Pharmacovigilance database analyses indicated a significant association between DOAC DDIs and increased reported stroke rates. Management recommendations in systematic reviews (n = 5) highlighted monitoring when DOACs were combined with inducers. Strategies included using alternative drugs with a weaker or preferentially absent inducing profile. Limited evidence suggests that edoxaban may be an acceptable option in case of DOAC and CYP3A4/P-gp inducer interactions; however, robust clinical data confirming safety are needed. Present literature indicates a higher thromboembolic risk in patients on DOAC treatment combining CYP3A4- and/or P-gp inducers. DOAC management should be tailored to the individual patient through collaboration between expert healthcare professionals.
直接口服抗凝剂(DOACs)常用于治疗和预防非瓣膜性心房颤动患者的缺血性中风。与维生素K拮抗剂相比,DOACs具有显著优势,尽管其药物相互作用(DDI)情况可能会使药物疗效和安全性变得复杂。本叙述性综述探讨了这些DDI带来的临床挑战以及可用的潜在药理学替代方案和监测策略。我们进行了一项PubMed搜索(2000年1月1日至2023年12月31日),纳入了关于成年患者使用DOACs和CYP3A4/P-糖蛋白诱导剂的人体DDI研究,评估患者结局数据以及DDI管理的建议。共纳入22项研究。病例报告(n = 6)表明,卡马西平、苯巴比妥和苯妥英等抗癫痫药物可能与血栓栓塞事件有关。巢式病例对照研究(n = 2)和队列研究(n = 9)发现,联合使用DOACs和CYP3A4/P-糖蛋白诱导剂,尤其是卡马西平和苯妥英,会增加血栓栓塞事件的风险。药物警戒数据库分析表明,DOAC DDI与报告的中风率增加之间存在显著关联。系统评价(n = 5)中的管理建议强调,当DOACs与诱导剂联合使用时需进行监测。策略包括使用诱导作用较弱或无诱导作用的替代药物。有限的证据表明,在DOAC与CYP3A4/P-糖蛋白诱导剂相互作用的情况下,依度沙班可能是一个可接受的选择;然而,需要有力的临床数据来证实其安全性。现有文献表明,接受DOAC治疗并联合使用CYP3A4和/或P-糖蛋白诱导剂的患者发生血栓栓塞的风险更高。DOAC的管理应通过专业医疗保健人员之间的合作,根据个体患者情况进行调整。