Toxicityand Side Effects

In prophylactic doses of 200-300 mg/day, proguanil causes few side effects except occasional nausea and diarrhea. Large doses (1 g or more daily) may cause vomiting, abdominal pain, diarrhea, hematuria, and transient appearance of epithelial cells and casts in the urine. Overdose (up to 15 g) has been followed by complete recovery. Doses as high as 700 mg twice daily have been taken for >2 weeks without serious toxicity. Proguanil is considered safe during pregnancy. It is remarkably safe when coadministered with other antimalarial drugs.

QUINOLINES AND RELATED COMPOUNDS Chloroquine and Hydroxychloroquine

The structure of chloroquine is shown in Figure 39-3. A chlorine atom attached to position 7 of the quinoline ring confers the greatest antimalarial activity. Hydroxychloroquine (plaquenil) is essentially equivalent to chloroquine against P. falciparum malaria.

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