Pyrimethamine

Author: Prof. Dr. med. Peter Altmeyer

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Last updated on: 29.10.2020

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Definition
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Chemotherapy, antimalarials.

Half-life
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> 4 days

Pharmacodynamics (Effect)
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Inhibition of dihydrofolate reductase.

Spectrum of action
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In combination with sulfones or sulfonamides effective against all human pathogenic Plasmodium spp., as single agent against Toxoplasma gondii.

Indication
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In combination preparations for malaria tertiana. Therapy of toxoplasmosis including ocular and congenital manifestations and immunodeficiency.

Limited indication
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Pregnancy, folic acid deficiency, liver dysfunction, megaloblastic anemia, renal insufficiency.

Dosage and method of use
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  • Curative malaria therapy (malaria without complications): Application in combination with sulfadoxin (combination preparation: Fansidar contains 500 mg pyrimethamine and 25 mg sulfadoxin): 1500 mg pyrimethamine/75 mg sulfadoxin p.o. as 1-day therapy. Dose reduction for children and adults < 45 kg bw.
  • Toxoplasmosis (in combination with 4 g sulfadiazin/day p.o.): adults and children > 6 years: 100 mg/day for 3 weeks in combination with folic acid 100 mg/day.
  • Toxoplasmosis encephalitis in AIDS: 100 mg/day in combination with sulfadiazine and folic acid, followed by recurrent prophylaxis at 50 mg/day.

Remember! Before therapy determination of glucose-6-phosphate dehydrogenase.

Undesirable effects
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Blood count changes, allergic reactions, headaches, heart rhythm disturbances, gastrointestinal complaints, insomnia, dry mouth, shock.

Interactions
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See Table 1.

Contraindication
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Severe hematopoiesis, lactation.

Preparations
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Daraprim; Fansidar (combination with sulfadoxine)

Tables
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Significant interactions of pyrimethamine

Dapson

Haematotoxicity ↑

Sulfonamides

Haematotoxicity ↑

Trimethoprim

Haematotoxicity ↑

Zidovudine

Zidovudine toxicity ↑

Cytostatics

Haematotoxicity ↑

Anticoagulants

Enhanced impact

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Last updated on: 29.10.2020