pyrimethamine

Ligand id: 4800

Name: pyrimethamine

IUPHAR Pharmacology Education Project (PEP) logo

View more information in the IUPHAR Pharmacology Education Project: pyrimethamine

Structure and Physico-chemical Properties

2D Structure
Click here for structure editor
Calculated Physico-chemical Properties
Hydrogen bond acceptors 4
Hydrogen bond donors 2
Rotatable bonds 2
Topological polar surface area 77.82
Molecular weight 248.08
XLogP 2.68
No. Lipinski's rules broken 0

Molecular properties generated using the CDK

No information available.
Summary of Clinical Use
Pyrimethamine is used in the treatment of toxoplasmosis and acute malaria. Also used for the prevention of malaria in areas without resistance to pyrimethamine.
Pyrimethamine is listed in the World Health Organisation's 21st Essential Medicines List (2019) as a curative treatment for uncomplicated P. falciparum malaria in combination with sulfadoxine and artesunate. This is one of the artemisinin-based combination therapies (ACTs) recommended in the WHO's Guidelines for the treatment of malaria [6]
Mechanism Of Action and Pharmacodynamic Effects
Interferes with the formation of malarial schizont in erthrocytes and the liver. This is via the inhibition of the dihydrofolate reductase-thymidylate synthase in plasmodia which blocks the biosynthesis of purines and pyrimidines, leading to failure of nuclear division.
External links