Cen Yan-Yan, Zao Yi-Bo, Li Pan, Li Xiao-Li, Zeng Xiu-Xiu, Zhou Hong
Pharmacology Departemnt, Army Medical University, Chongqing 400038, China.
Chongqing Shenghuaxi Pharmaceutical Co., Ltd., Chongqing 401336, China.
Zhongguo Zhong Yao Za Zhi. 2018 Oct;43(19):3970-3978. doi: 10.19540/j.cnki.cjcmm.20180726.010.
Artesunate (AS), a famous derivative of the artemisinin, is the basic treatment globally for mild to severe malaria infection due to the prominent advantages such as high efficiency, fast effect, low toxicity and not easy to produce resistance. More and more research reports have shown that AS and its active metabolites dihydroartemisinin (DHA) had various bioactivities in addition to antimalarial activity, attracting researchers to further study its new pharmacological effects in order to explore new use of the old drug. A comprehensive understanding of the pharmacokinetic characteristics of AS will be conducive to the further development of new pharmacological actions and clinical application of AS. Therefore, this paper would review the absorption, distribution, metabolism and excretion of AS , as well as the pharmacokinetics characteristics of AS and DHA after clinical administration of AS by intravenous (IV), intramuscular (IM), oral or rectal routes. The process and pharmacokinetic parameters of AS and DHA were compared between healthy volunteers, malaria patients, and special populations (children, women). Meanwhile, the research progress on pharmacological effects of AS and active metabolite DHA such as anti-tumor, anti-inflammatory, anti septic, antiangiogenic, anti-fibrosis and immunoregulation activities would be also reviewed, hoping to provide a theoretical basis for the further development and utilization of AS and its metabolites.
青蒿琥酯（AS）是青蒿素的一种著名衍生物，由于其高效、速效、低毒且不易产生耐药性等突出优点，是全球治疗轻至重度疟疾感染的基本药物。越来越多的研究报告表明，AS及其活性代谢产物双氢青蒿素（DHA）除具有抗疟活性外，还具有多种生物活性，吸引研究人员进一步研究其新的药理作用，以探索这种老药的新用途。全面了解AS的药代动力学特征将有助于AS新的药理作用的进一步开发及其临床应用。因此，本文将综述AS的吸收、分布、代谢和排泄情况，以及静脉注射（IV）、肌肉注射（IM）、口服或直肠给药后AS和DHA的药代动力学特征。比较了健康志愿者、疟疾患者和特殊人群（儿童、妇女）中AS和DHA的过程及药代动力学参数。同时，还将综述AS及其活性代谢产物DHA在抗肿瘤、抗炎、抗感染、抗血管生成、抗纤维化和免疫调节等药理作用方面的研究进展，希望为AS及其代谢产物的进一步开发利用提供理论依据。
