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QuickView for pyrimethamine (compound)


PubChem
Name: Pyrimethamine
PubChem Compound ID: 4993
Description: One of the FOLIC ACID ANTAGONISTS that is used as an antimalarial or with a sulfonamide to treat toxoplasmosis.
Molecular formula: C12H13ClN4
Molecular weight: 248.711 g/mol
Synonyms:
Diaminopyritamin; NSC-3061; 5-(4-Chlorophenyl)-6-ethyl-2,4-diaminopyrimidine; Pyremethamine; Malacid; NCI60_002604; Daraprim; 2,4-Pyrimidinediamine, 5-(4-chlorophenyl)-6-ethyl-; KBioGR_001007; Darapram.
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DrugBank
Identification
Name: Pyrimethamine
Name (isomeric): DB00205
Drug Type: small molecule
Description: One of the FOLIC ACID ANTAGONISTS that is used as an antimalarial or with a sulfonamide to treat toxoplasmosis.
Synonyms:
Diaminopyritamin; Pirimetamin; Ethylpyrimidine; CD; Pyrimethamine Hcl; Pyremethamine; Primethamine; Pirimetamina; Chloridine; Pyrimethamin.
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Brand: Tindurin, Darapram, Daraprim, Tinduring, Maloprim, Pirimecidan, Daraclor, Darachlor, Fansidar, Erbaprelina, Khloridin, Malocide, Malocid, Daraprime, Disulone, Malacid
Brand name mixture: Quinnoxine-S(Pyrimethamine + Sulfaquinoxaline), Fansidar Tablets(Pyrimethamine + Sulfadoxine), Sulfaquinoxaline-S Liq(Pyrimethamine + Sulfaquinoxaline)
Category: Antimalarials, Antiprotozoal Agents, Antiprotozoals, Folic Acid Antagonists
CAS number: 58-14-0
Pharmacology
Indication: For the treatment of toxoplasmosis and acute malaria; For the prevention of malaria in areas non-resistant to 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 growt...
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Mechanism of Action: Pyrimethamine inhibits the dihydrofolate reductase of plasmodia and thereby blocks the biosynthesis of purines and pyrimidines, which are essential for DNA synthesis and cell multiplication. This leads to failure of nuclear division at the time of schizont formation in erythrocytes and liver.
Absorption: Well absorbed with peak levels occurring between 2 to 6 hours following administration
Protein binding: 87%
Biotransformation: Hepatic
Half Life: 96 hours
Affected organisms: Plasmodium
Interactions
Food interaction:
Take with food to reduce irritation.
Folic acid needs increased.
Drug interaction:
TamoxifenPyrimethamine may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy.
LumefantrinePyrimethamine may increase the adverse effects of lumefantrine. Combination therapy is contraindicated unless there are no other treatment options.
ArtemetherPyrimethamine may increase the adverse effects of artemether. Combination therapy is contraindicated unless there are no other treatment options.
TamsulosinPyrimethamine, a CYP2D6 inhibitor, may decrease the metabolism and clearance of Tamsulosin, a CYP2D6 substrate. Monitor for changes in therapeutic/adverse effects of Tamsulosin if Pyrimethamine is initiated, discontinued, or dose changed.
TramadolPyrimethamine may decrease the effect of Tramadol by decreasing active metabolite production.

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