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Folate antagonist (antimalarial/antiprotozoal)

Pyrimethamine

Brand names: Daraprim

Adult dose

Dose: Toxoplasmosis: 50–75mg PO OD with sulfadiazine + folinic acid (specialist)
Route: PO
Frequency: OD

Clinical pearls

  • Toxoplasmosis (with sulfadiazine + folinic acid); cerebral toxoplasmosis in HIV
  • Always co-prescribe folinic acid 15mg/day to prevent cytopenias

Contraindications

  • Megaloblastic anaemia (folate deficiency)
  • Severe renal/hepatic impairment
  • Hypersensitivity

Side effects

  • Megaloblastic anaemia
  • Neutropenia
  • Thrombocytopenia
  • GI upset
  • Rash
  • SJS/TEN (with sulfonamide)

Interactions

  • Trimethoprim (additive folate antagonism)
  • Sulfonamides
  • Methotrexate
  • Phenytoin
  • Zidovudine

Monitoring

  • FBC weekly initially

Reference: BNF; BHIVA; https://bnf.nice.org.uk/drugs/pyrimethamine/. Verify against your local formulary and the latest BNF before prescribing.

Related

Curated clinical cross-links plus same-class fallbacks.