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Brand names,
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Analogs
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Brand Names Mixture
- Fansidar Tablets (Pyrimethamine + Sulfadoxine)
- Quinnoxine-S (Pyrimethamine + Sulfaquinoxaline)
- Sulfaquinoxaline-S Liq (Pyrimethamine + Sulfaquinoxaline)
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Chemical_Formula
C12H13ClN4
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RX_link
http://www.rxlist.com/cgi/generic2/pyrime.htm
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fda sheet
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msds (material safety sheet)
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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)
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Molecular Weight
248.711 g/mol
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Melting Point
233.5 oC
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H2O Solubility
121 mg/L
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State
Solid
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LogP
2.607
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Dosage Forms
Tablet
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Indication
For the treatment of toxoplasmosis and acute malaria; For the prevention of malaria in areas non-resistant to pyrimethamine
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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.
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Absorption
Well absorbed with peak levels occurring between 2 to 6 hours following administration
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side effects and Toxicity
No information avaliable
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Patient Information
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Organisms Affected
Plasmodium