Department of Microbiology & Immunology, Columbia University College of Physicians and Surgeons, Hammer Health Sciences Center, Room 1502, 701 West 168th Street, New York 10032, New York, USA.
Nat Rev Microbiol. 2009 Dec;7(12):864-74. doi: 10.1038/nrmicro2239. Epub 2009 Nov 2.
Plasmodium falciparum resistance to chloroquine and sulphadoxine-pyrimethamine has led to the recent adoption of artemisinin-based combination therapies (ACTs) as the first line of treatment against malaria. ACTs comprise semisynthetic artemisinin derivatives paired with distinct chemical classes of longer acting drugs. These artemisinins are exceptionally potent against the pathogenic asexual blood stages of Plasmodium parasites and also act on the transmissible sexual stages. These combinations increase the rates of clinical and parasitological cures and decrease the selection pressure for the emergence of antimalarial resistance. This Review article discusses our current knowledge about the mode of action of ACTs, their pharmacological properties and the proposed mechanisms of drug resistance.
疟原虫对氯喹和磺胺多辛-乙胺嘧啶的耐药性导致了以青蒿素为基础的联合疗法(ACTs)最近被采用作为治疗疟疾的一线药物。ACTs 由半合成青蒿素衍生物与作用时间更长的不同化学类别的药物配对组成。这些青蒿素对疟原虫致病性的无性血期具有极强的作用,并且还作用于可传播的有性阶段。这些组合提高了临床和寄生虫学治愈率,并降低了抗疟药物耐药性出现的选择压力。这篇综述文章讨论了我们目前对 ACTs 的作用模式、药理学特性以及耐药性提出的机制的了解。