Antimalarial Agents

Review
In: LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [Internet]. Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases; 2012.
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Excerpt

Malaria is one of the world’s most common and important infectious diseases, affecting 200 to 300 million persons and accounting for half a million deaths yearly, mostly children. Malaria in humans is caused by four Plasmodium species, P. falciparum, vivax, ovale and malariae and is spread by the bite of the female Anopheles mosquito. The majority of infections and deaths due to malaria occur in Africa and Asia. Between 1000 and 1500 cases are reported in the United States each year, virtually all being related to travel to endemic areas, and deaths being very rare and usually associated with misdiagnosis, inadequate therapy or lack of compliance.

The major drugs used to treat malaria include amodiaquine (Camoquin, Flavoquine), artemisinin derivatives (artesunate: Adamsunate; artemether-lumefantrine, Coartem), atovaquone/proguanil (Malarone), chloroquine (Aralen), mefloquine (Lariam), mepacrine or quinacrine (Atabrine), primaquine (generic only), sulfadoxine/pyrimethamine (Fansidar), and quinine (Qualaquin). Not all of these agents are available in the United States, but the majority of therapy of malaria is administered in Africa and Asia where these agents and others are available.

Quinine was the initial drug used for prophylaxis and therapy of malaria, being the active component of Cinchona bark that was used for centuries in South America for chills and fever, and that was introduced into Western medicine by Jesuit priests returning from Peru in the 17th Century. Quinine is active against malaria, but has been replaced by synthetic aminoquinolone derivatives such as chloroquine that are more potent and better tolerated. Quinine is still used rarely for therapy of chloroquine-resistant P. falciparum malaria. Quinine can cause an acute allergic response with fever, nausea, abdominal pain and liver injury, but it is rarely severe.

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