Abstract
This chapter discusses several antiprotozoal drugs and their adverse effects. Antimalarial drugs cause a wide range of dose-dependent, idiosyncratic, and cumulative adverse effects, which is of concern in the setting of chemoprophylaxis when the benefits of a drug must clearly outweigh its risks. This is mainly of concern to travelers because most residents of endemic areas cannot afford chemoprophylaxis. Prophylaxis is advisable in areas of intense transmission, even for relatively short visits and for subjects who may originally have come from the area. Artemisinin is the pharmacologically active component of the Chinese herbal remedy qing hao su, which was isolated by Chinese scientists in 1974. Artemether, arteether, and artesunate are semisynthetic derivatives with enhanced activities. The first two are formulated for intramuscular use, while artesunate is given intravenously. Although each has pharmacological activity in vitro, it is thought that all are metabolized in vivo to dihydroartemisinin, which is an active metabolite. Amodiaquine, which is a 4-aminoquinoline-like chloroquine, is no longer used for chemoprophylaxis because of the risk of agranulocytosis and hepatotoxicity. Amodiaquine readily forms a chemically reactive derivative, a quinoneimine, which by acting as a hapten can initiate an immune response.
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