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Pyrimethamine (Daraprim®) is a medication used for protozoal infections. It is commonly used as an antimalarial drug (for both treatment and prevention), and is also used in the treatment of Toxoplasma gondii infections in immunocompromised patients, such as HIV-positive individuals.

Mechanism of action


Pyrimethamine interferes with folic acid synthesis by inhibiting the enzyme dihydrofolate reductase. Folic acid is needed for DNA and RNA synthesis in many species, including protozoa.

Mechanism of resistance


Resistance to pyrimethamine is widespread. Mutations in the gene for dihydrofolate reductase may reduce the effectiveness of pyrimethamine (PMID 15155209). These mutations decrease the binding affinity between pyrimethamine and dihydrofolate reductase by steric interactions (PMID 14711307).

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Daraprim - About Pyrimethamine.

Daraprim - Product information for US residents in PDF format. [Acrobat Reader required]

DrugDigest: Pyrimethamine ( Daraprim ) - Information on dosage, usage, side effects, interactions, and drug comparisons, including generics when available.

Pyrimethamine - Used for the treatment and prevention of malaria. Also used to treat AIDS-related diarrhea and as one of a combination of drugs to treat Toxoplasma gondii, a protozoal infection. Marketed as Daraprim and Fansidar. Site includes drug description, dosage, and side effects.

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