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


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


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


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.



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