Cycloguanil (active metabolite)

Figure 7.9 • Conversion of proguanil to cycloguanil by CYP2C19.


Figure 7.10 • Fosmidomycin and a fosmidomycin analog.

elimination half-life of 111 hours). The combination is effective against both erythrocytic and exoerythrocytic Plasmodium. This drug combination is indicated for malaria resistant to chloroquine, halofantrine, mefloquine, and amodiaquine. Its main site is the sporozoite stage (site 1 in Fig. 7.1).

Artemether and Lumefantrine. These two antimalarials interfere with heme metabolism, thereby stopping development of the parasite in the erythrocyte states. Artemether, with its endoperoxide, acts oxidatively and lumefantrine may form a complex with hemin.

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