name: | Pyrimethamine |
ATC code: | P01BD01 | route: | oral |
n-compartments | 1 |
Pyrimethamine is an antiparasitic compound primarily used in combination therapy for the treatment and prevention of malaria, particularly due to its activity against Plasmodium falciparum. It has also been used to treat toxoplasmosis, in combination with a sulfonamide. The drug acts by inhibiting dihydrofolate reductase, disrupting folic acid metabolism in parasites. Pyrimethamine remains in clinical use today.
Pharmacokinetic parameters reported in healthy adult volunteers following oral administration.
Iida, T, et al., & Gross, AS (2020). Evaluation of the Pharmacokinetics, Safety, and Tolerability of a Single Oral Dose of Pyrimethamine in Healthy Male Subjects of Japanese and European Ancestry. Clinical pharmacology in drug development 9(6) 768–773. DOI:10.1002/cpdd.771 PUBMED:https://pubmed.ncbi.nlm.nih.gov/31950646
Hussein, Z, et al., & Canfield, CJ (1997). Population pharmacokinetics of atovaquone in patients with acute malaria caused by Plasmodium falciparum. Clinical pharmacology and therapeutics 61(5) 518–530. DOI:10.1016/S0009-9236(97)90132-6 PUBMED:https://pubmed.ncbi.nlm.nih.gov/9164414
Wang, NS, et al., & Arnold, K (1990). Pharmacokinetics of the combination pyrimethamine with sulfadoxine and mefloquine (FANSIMEF) in Chinese volunteers and the relative bioavailability of a lacquered tablet. Chemotherapy 36(3) 177–184. DOI:10.1159/000238764 PUBMED:https://pubmed.ncbi.nlm.nih.gov/2338028