Pyrimethamine
- Atc Codes:P01BD01
- CAS Codes:58-14-0
- PHARMGKB ID:58-14-0
Table of contents
- Brand Names
- Drug Combinations
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Caution and personalized dose adjustment in patients with the following genotypes
- Other genes that may be involved
- Inhibits
- Drug Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Belgium: Daraprim; Cyprus: Daraprim; France: Malocide; Germany: Daraprim; Greece: Daraprim; Luxembourg: Daraprim; Netherlands: Daraprim; Poland: Daraprim, Pyrimen; Portugal: Pirimetamina; Spain: Daraprim; UK: Daraprim.
North America
Canada: Daraprim; USA: Daraprim.
Latin America
Argentina: Daraprim; Brazil: Daraprim; Mexico: Daraprim.
Drug combinations
Pyrimethamine and Sulfadoxine
Chemistry
Pyrimethamine: C~12~H~13~ClN~4~. Mw: 248.71. (1) 2,4-Pyrimidinediamine, 5-(4-chlorophenyl)-6-ethyl-; (2) 2,4-Diamino-5-(p-chlorophenyl)-6-ethylpyrimidine. CAS-58-14-0.
Pharmacologic Category
Antiprotozoals; Antimalarials. (ATC-Code: P01BD01).
Mechanism of action
Inhibits parasitic dihydrofolate reductase, resulting in inhibition of vital tetrahydrofolic acid synthesis.
Therapeutic use
Prophylaxis of malaria due to susceptible strains of plasmodia. Used in conjunction with quinine and sulfadiazine for treatment of uncomplicated attacks of chloroquine-resistant P. falciparum malaria. Used in conjunction with fast-acting schizonticide to initiate transmission control and suppression cure. Synergistic combination with sulfonamide in treatment of toxoplasmosis.
Pregnancy and lactiation implications
There are no adequate, well-controlled studies in pregnant women. Teratogenicity reported in animal studies. Not recommended during lactation.
Unlabeled use
Contraindications
Hypersensitivity to pyrimethamine or any component of the formulation. Chloroguanide. Resistant malaria. Megaloblastic anemia secondary to folate deficiency.
Warnings and precautions
Use caution in possible folate deficiency (e.g. malabsorption syndrome, pregnancy, alcoholism), in G6PD deficiency, in hepatic/renal impairment, and in history of seizure disorders. When used for more than 3-4 days, it may be advisable to administer leucovorin to prevent hematologic complications.