Pyrimethamine
Brand names,
Pyrimethamine
Analogs
Pyrimethamine
Brand Names Mixture
- Fansidar Tablets (Pyrimethamine + Sulfadoxine)
- Quinnoxine-S (Pyrimethamine + Sulfaquinoxaline)
- Sulfaquinoxaline-S Liq (Pyrimethamine + Sulfaquinoxaline)
Pyrimethamine
Chemical_Formula
C12H13ClN4
Pyrimethamine
RX_link
http://www.rxlist.com/cgi/generic2/pyrime.htm
Pyrimethamine
fda sheet
Pyrimethamine
msds (material safety sheet)
Pyrimethamine
Synthesis Reference
Russel, Hitchings, J. Am. Chem. Soc. 73, 3763 (1951); Hitchings et al., U.S. pats. 2,576,939; 2,579,259, and 2,602,794 (1951 and 1952 to Burroughs Wellcome); Jacob, U.S. pat 2,680,740 (1954 to Rhone-Poulenc)
Pyrimethamine
Molecular Weight
248.711 g/mol
Pyrimethamine
Melting Point
233.5 oC
Pyrimethamine
H2O Solubility
121 mg/L
Pyrimethamine
State
Solid
Pyrimethamine
LogP
2.607
Pyrimethamine
Dosage Forms
Tablet
Pyrimethamine
Indication
For the treatment of toxoplasmosis and acute malaria; For the prevention of malaria in areas non-resistant to pyrimethamine
Pyrimethamine
Pharmacology
Pyrimethamine is an antiparasitic compound commonly used as an adjunct in the treatment of uncomplicated, chloroquine resistant, P. falciparum malaria. Pyrimethamine is a folic acid antagonist and the rationale for its therapeutic action is based on the differential requirement between host and parasite for nucleic acid precursors involved in growth. This activity is highly selective against plasmodia and Toxoplasma gondii. Pyrimethamine possesses blood schizonticidal and some tissue schizonticidal activity against malaria parasites of humans. However, the 4-amino-quinoline compounds are more effective against the erythrocytic schizonts. It does not destroy gametocytes, but arrests sporogony in the mosquito. The action of pyrimethamine against Toxoplasma gondii is greatly enhanced when used in conjunction with sulfonamides.
Pyrimethamine
Absorption
Well absorbed with peak levels occurring between 2 to 6 hours following administration
Pyrimethamine
side effects and Toxicity
No information avaliable
Pyrimethamine
Patient Information
Pyrimethamine
Organisms Affected
Plasmodium