Pyrimethamine molecular structure

Pyrimethamine

Also known as: Daraprim, Fansidar (with sulfadoxine), Malocide, Pyrimon

CAS Number: 58-14-0

Antimalarial / Antiprotozoal (Dihydrofolate Reductase Inhibitor)

Pharmacopeia Standards

USPBPIPEPWHO

Mechanism of Action

Pyrimethamine selectively inhibits plasmodial and toxoplasmal dihydrofolate reductase, an enzyme for which it has orders of magnitude greater affinity than for the human isoform. Blocking the reduction of dihydrofolate to tetrahydrofolate halts thymidylate synthesis and therefore parasite DNA replication. Combined with a sulfonamide acting one step upstream, the two-point folate blockade produces strong synergy.

Technical Specifications

Generic / INN NamePyrimethamine
CAS Registry Number58-14-0
Molecular FormulaC12H13ClN4
Molecular Weight248.71 g/mol g/mol
Typical PurityNot less than 99.0% (assay), on the dried basis
Storage ConditionsStore in tight, light-resistant containers below 30°C; protect from light
Shelf Life60 months in original sealed packaging
CategoryAntimalarials

Specifications are indicative and intended for sourcing reference only. Always confirm against the supplier's Certificate of Analysis and the applicable pharmacopeial monograph before issuing a purchase specification.

Typical Applications

Fixed-dose sulfadoxine-pyrimethamine tablets for malaria chemoprevention; combination therapy with sulfadiazine for toxoplasmosis; veterinary antiprotozoal use.

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