Malaria is the number one infectious disease in the world today. Worldwide, over two million people die each year from malaria. This shocking reality is largely due to the emergence of drug resistant strains of Plasmodium falciparum. Artemisinin, a sesquiterpene lactone endoperoxide isolated from Artemesia annua has been shown to be a fast acting, safe and effective drug against multidrug-resistant and sensitive strains of P. falciparum. This article reports a survey of the literature dealing with artemisinin related antimalarial issues that have appeared from 1980s to the beginning of 2003. A broad range of medical and pharmaceutical disciplines is covered, including a brief introduction about discovery, phytochemical aspects, antimalarial mechanism of action, pharmacokinetics, and major drawbacks and various structural modifications made to overcome them.