Antimalarials26

Falk R. Ochsendorp

In 1934, Andersag synthesized chloroquine as a succession to chinine for the prophylaxis and treatment of malaria. Hydroxychloroquine is ß-hydroxylated chloroquine. Since 1960, these substances as well as quinacrine, an acridine derivative widely used during World War II as an antimalarial (3 million soldiers for up to 4 years), were also successfully used for the therapy of noninfectious diseases, such as lupus erythe-matosus (LE) or rheumatoid arthritis. Their side effects, especially the fear of an irreversible retinopathy, limited their use. These unwanted effects, however, are primarily related to an excessive daily dosage and can be prevented by observing the maximal daily dosage of 3.5 (to 4) mg for chloroquine and 6 (to 6.5) mg for hydroxychloroquine per kilogram of ideal body weight. If these limits and the following information are taken into consideration, the therapy is rather safe.

These "antimalarials" are losing their primary indication, malaria, owing to the increasing resistance of plasmodia and newer compounds. On the other hand, even today there are new indications for chloroquine and hydroxychloroquine, for example, the treatment of human immunodeficiency virus infections (Boelaert et al. 2001, Savarino et al. 2001) (see also Table 26.1).

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