Hernandez Maldonado Joyce, Grundmann Oliver
Department of Medicinal Chemistry, College of Pharmacy, University of Florida, Gainesville, Florida, USA.
J Clin Pharmacol. 2022 Oct;62(10):1197-1205. doi: 10.1002/jcph.2073. Epub 2022 Jun 1.
Artemisinin is an antimalarial compound derived from the plant Artemisia annua L., also known as sweet wormwood. According to the World Health Organization, artemisinin-based combination therapy (ACT) is an essential treatment for malaria, specifically Plasmodium falciparum, which accounts for most malaria-related mortality. ACTs used to treat uncomplicated malaria include artemether-lumefantrine, artesunate-amodiaquine, artesunate-mefloquine, artesunate-sulphadoxine-pyrimethamine, and dihydroartemisinin-piperaquine. Although the mechanism of action and clinical capabilities of artemisinin in malaria treatment are widely known, more information on the potential for drug interactions needs to be further investigated. Some studies show pharmacokinetic and pharmacodynamic drug interactions with HIV antiviral treatment but few studies have been conducted on most other drug classes. Based on known genotypes of cytochrome P450 (CYP) enzymes, CYP2B6 and CYP3A are primarily involved in the metabolism of artemisinin and its derivatives. Reduced functions in these enzymes can lead to subtherapeutic concentrations of the active metabolite, dihydroartemisinin, that may cause treatment failure, which has been shown in some studies with cardiovascular, antibiotic, and antiparasitic drugs. Although the clinical importance remains unclear to date, clinicians should be aware of potential drug-drug interactions and monitor patients on ACT closely.
青蒿素是一种从植物黄花蒿（也称为甜艾蒿）中提取的抗疟化合物。根据世界卫生组织的说法，以青蒿素为基础的联合疗法（ACT）是治疗疟疾，特别是恶性疟原虫（导致大多数疟疾相关死亡的原因）的重要治疗方法。用于治疗非复杂性疟疾的ACT包括蒿甲醚-本芴醇、青蒿琥酯-阿莫地喹、青蒿琥酯-甲氟喹、青蒿琥酯-磺胺多辛-乙胺嘧啶和双氢青蒿素-哌喹。尽管青蒿素在疟疾治疗中的作用机制和临床疗效广为人知，但关于药物相互作用可能性的更多信息仍需进一步研究。一些研究表明，青蒿素与HIV抗病毒治疗存在药代动力学和药效学药物相互作用，但针对大多数其他药物类别的研究较少。根据已知的细胞色素P450（CYP）酶基因型，CYP2B6和CYP3A主要参与青蒿素及其衍生物的代谢。这些酶功能的降低会导致活性代谢物双氢青蒿素的浓度低于治疗水平，这可能会导致治疗失败，一些针对心血管、抗生素和抗寄生虫药物的研究已经证明了这一点。尽管目前临床重要性尚不清楚，但临床医生应意识到潜在的药物相互作用，并密切监测接受ACT治疗的患者。
