Department of Clinical Pharmacology, Université Côte d'Azur Medical Center Pasteur hospital, Bât J4, 30, avenue de la Voie-Romaine, CS51069, Nice Cedex 01 06001, France.
RCPV of Grenoble. University of Grenoble Medical Center, Grenoble 38043, France.
Int J Cardiol. 2021 Feb 1;324:255-260. doi: 10.1016/j.ijcard.2020.10.028. Epub 2020 Oct 16.
The antiretroviral drug lopinavir/ritonavir has been recently repurposed for the treatment of COVID-19. Its empirical use has been associated with multiple cardiac adverse reactions pertaining to its ancillary multi-channel blocking properties, vaguely characterized until now. We aimed to characterize qualitatively the cardiotoxicity associated with lopinavir/ritonavir in the setting of COVID-19. Spontaneous notifications of cardiac adverse drug reactions reported to the national Pharmacovigilance Network were collected for 8 weeks since March 1st 2020. The Nice Regional Center of Pharmacovigilance, whose scope of expertise is drug-induced long QT syndrome, analyzed the cases, including the reassessment of all available ECGs. QTc ≥ 500 ms and delta QTc > 60 ms from baseline were deemed serious. Twenty-two cases presented with 28 cardiac adverse reactions associated with the empirical use of lopinavir/ritonavir in a hospital setting. Most adverse reactions reflected lopinavir/ritonavir potency to block voltage-gated potassium channels with 5 ventricular arrhythmias and 17 QTc prolongations. An average QTc augmentation of 97 ± 69 ms was reported. Twelve QTc prolongations were deemed serious. Other cases were likely related to lopinavir/ritonavir potency to block sodium channels: 1 case of bundle branch block and 5 recurrent bradycardias. The incidence of cardiac adverse reactions of lopinavir/ritonavir was estimated between 0.3% and 0.4%. These cardiac adverse drug reactions offer a new insight in its ancillary multi-channel blocking functions. Lopinavir/ritonavir cardiotoxicity may be of concern for its empirical use during the COVID-19 pandemic. Caution should be exerted relative to this risk where lopinavir/ritonavir summary of product characteristics should be implemented accordingly.
洛匹那韦/利托那韦这一抗逆转录病毒药物最近被重新用于治疗 COVID-19。其经验性使用与多种与辅助多通道阻滞特性相关的心脏不良反应相关,这些特性直到现在才被模糊描述。我们旨在定性地描述 COVID-19 背景下与洛匹那韦/利托那韦相关的心脏毒性。自 2020 年 3 月 1 日以来,我们收集了国家药物警戒网络自发报告的与心脏不良反应相关的药物不良反应报告,为期 8 周。尼斯区域药物警戒中心的专业范围是药物诱导的长 QT 综合征,对这些病例进行了分析,包括对所有可用心电图的重新评估。QTc 延长≥500ms 和与基线相比 delta QTc >60ms 被认为是严重的。在医院环境中,22 例病例出现 28 例与洛匹那韦/利托那韦经验性使用相关的心脏不良反应。大多数不良反应反映了洛匹那韦/利托那韦阻断电压门控钾通道的效力,其中 5 例为室性心律失常,17 例 QTc 延长。报告平均 QTc 增加 97 ± 69ms。12 例 QTc 延长被认为是严重的。其他病例可能与洛匹那韦/利托那韦阻断钠通道的效力有关:1 例束支传导阻滞和 5 例复发性心动过缓。洛匹那韦/利托那韦心脏不良反应的发生率估计在 0.3%至 0.4%之间。这些心脏药物不良反应为其辅助多通道阻滞功能提供了新的见解。洛匹那韦/利托那韦的心脏毒性可能是其在 COVID-19 大流行期间经验性使用的一个关注点。在实施洛匹那韦/利托那韦产品特性摘要时,应注意到这一风险。