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INTRODUCTION

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Diseases caused by protozoans constitute a worldwide health problem. This chapter concerns the drugs used to combat malaria, amebiasis, toxoplasmosis, pneumocystosis, trypanosomiasis, and leishmaniasis.

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DRUGS FOR MALARIA

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Malaria is one of the most common diseases worldwide and a leading cause of death. Four species of Plasmodium commonly infect humans (P falciparum, P malariae, P ovale, P vivax) and undergo a primary developmental stage in the liver and then parasitize erythrocytes. P falciparum and P malariae have only 1 cycle of liver cell invasion. The other species have a dormant hepatic stage responsible for recurrent infections and relapses. A fifth species, P knowlesi, has been recognized as a human pathogen but little is known about it. Primary tissue schizonticides (eg, primaquine) kill schizonts in the liver, whereas blood schizonticides (eg, chloroquine, artemisinins, quinine) kill these forms only in erythrocytes. Sporonticides (proguanil, pyrimethamine) prevent sporogony and multiplication in the mosquito.

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Drugs used for the treatment of malaria are shown in Table 52–1.

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Table Graphic Jump Location
TABLE 52–1Drugs used in the treatment of malaria.
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A. Chloroquine
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1. Classification and pharmacokinetics
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Chloroquine is a 4-aminoquinoline derivative. The drug is rapidly absorbed when given orally, is widely distributed to tissues, and has an extremely large volume of distribution. Antacids may decrease oral absorption of the drug. Chloroquine is excreted largely unchanged in the urine.

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2. Mechanism of action
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Chloroquine accumulates in the food vacuole of plasmodia and prevents polymerization of the hemoglobin breakdown product heme into hemozoin. Intracellular accumulation of heme is toxic to the parasite. Decreased intracellular accumulation via increased activity of membrane transporters is a mechanism of resistance to chloroquine and other antimalarial drugs. Resistance ...

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