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At a glance

Pyrimethamine is a folic acid antagonist used for acute malaria (in combination with sulfonamide), malaria prophylaxis, and toxoplasmosis.

Indications
  • Acute malaria (in combination with sulfonamide)
  • Malaria prophylaxis
  • Toxoplasmosis
Pharmacology

Pyrimethamine inhibits parasitic dihydrofolate reductase, preventing tetrahydrofolic acid synthesis essential for parasite growth and replication. It is active against pre-erythrocytic forms and is a slow-acting schizontocide.

Dosage

Adult Dose (Oral):

  • Acute malaria: 75 mg pyrimethamine + 1.5 g sulfadoxine (single dose)
  • Malaria prophylaxis: 25 mg once weekly; start 1-2 days before arrival in endemic area, continue for 4-6 weeks after leaving
  • Toxoplasmosis: 50-75 mg/day + 1-4 g sulfadiazine/day (1-3 weeks); then half dose for 4-5 weeks

Pediatric Dose (Oral):

  • Acute malaria (7-13 years): 50 mg + 1 g sulfadoxine; (1-6 years): 25 mg + 500 mg sulfadoxine; (5-11 months): 12.5 mg + 250 mg sulfadoxine
  • Malaria prophylaxis (<4 years): 6.25 mg/week; (4-10 years): 12.5 mg/week; (>10 years): 25 mg/week
  • Congenital toxoplasmosis (>2 months): Loading 2 mg/kg/day for 2 days; Maintenance 1 mg/kg/day (2-6 months) then 1 mg/kg 3 times/week
Side effects

Side Effects:

  • Skin rash
  • Macrocytic anemia (high dose)
  • Leukopenia
  • Thrombocytopenia
  • Megaloblastic anemia
  • Pancytopenia
  • Abdominal pain
  • Vomiting
  • Atrophic glossitis
  • Depression, fever, insomnia, lightheadedness
  • Potentially fatal: Erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis (with sulfadoxine at large doses)
Use in pregnancy

Use in Pregnancy: Unsafe during pregnancy; evidence of risk to the fetus; consult your doctor.

Pregnancy Category: D — always consult a doctor before taking during pregnancy.

Precautions & warnings
  • Caution in renal or hepatic impairment
  • Folate deficiency
  • Monitor blood and platelet counts every 2 weeks with prolonged treatment and large doses
  • Discontinue use if skin reactions, sore throat, or shortness of breath occurs
  • Do not use during pregnancy
  • Do not use during lactation
Overdose effects

Overdose: Folate deficiency symptoms (megaloblastic anemia, pancytopenia); treatment: folic acid or leucovorin, symptomatic supportive care.

Storage conditions

Store in a cool and dry place, away from light; keep out of reach of children.

Pyrimethamine — see the full informationPharmacology, precautions, pregnancy, overdose and the rest on the generic page
⚠️ This information is for educational purposes only — not a substitute for medical advice. Consult a registered physician before taking any medicine.