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Pyrimethamine
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. Additional recommended knowledge
Mechanism of actionPyrimethamine 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 resistanceResistance 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). Clinical usePyrimethamine is typically given with a sulfonamide and folinic acid:
Side effectsPyrimethamine may deplete folic acid in humans, resulting in hematologic side effects associated with folate deficiency. Side effects include:
ContraindicationsPyrimethamine is contraindicated in patients with:
References
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This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Pyrimethamine". A list of authors is available in Wikipedia. |