Price R N
Centre for Tropical Diseases, Nuffield Department of Clinical Medicine, John Radcliffe Hospital, Headington, Oxford, UK.
Expert Opin Investig Drugs. 2000 Aug;9(8):1815-27. doi: 10.1517/13543784.9.8.1815.
Artemisinin and its derivatives, artesunate and artemether, represent a new class of antimicrobial drug with potent activity against Plasmodium falciparum. Although they show excellent efficacy in both severe and uncomplicated malaria, dosage regimens still need to be optimised and pharmacokinetic profiles defined. In the treatment of uncomplicated malaria, the artemisinin drugs should be used in combination with a long acting antimalarial to protect both drugs against the emergence of resistance. In the treatment of severe malaria, parenteral artemether is at least as effective as quinine and is simpler to use. The use of rectal preparations of artesunate and artemisinin at the rural health level will facilitate early initiation of the treatment of falciparum malaria and this may reduce the proportion of patients progressing to severe disease. All of the artemisinin drugs have comparable efficacy; the choice of derivative should be based upon availability, cost and quality of the preparation. Artemisinin, artesunate and artemether are well-tolerated in both adults and children, with no evidence to date of serious clinical toxicity.
青蒿素及其衍生物青蒿琥酯和蒿甲醚是一类新型抗菌药物，对恶性疟原虫具有强大活性。尽管它们在重症和非重症疟疾中均显示出卓越疗效，但给药方案仍需优化，药代动力学特征也有待明确。在治疗非重症疟疾时，青蒿素类药物应与长效抗疟药联合使用，以防止两种药物产生耐药性。在治疗重症疟疾时，蒿甲醚注射液至少与奎宁一样有效，且使用更简便。在农村卫生机构使用青蒿琥酯和青蒿素的直肠制剂将有助于早期开展恶性疟的治疗，这可能会降低进展为重症疾病的患者比例。所有青蒿素类药物疗效相当；衍生物的选择应基于制剂的可得性、成本和质量。青蒿素、青蒿琥酯和蒿甲醚在成人和儿童中耐受性良好，迄今尚无严重临床毒性的证据。
