DHFR inhibitor (protozoal)
Protozoal dihydrofolate reductase inhibitor
- ↓ tetrahydrofolate → ↓ DNA synthesis in Plasmodium, Toxoplasma
- Selectivity is narrower — human marrow is hit at therapeutic doses
- Reduced folate bypasses the block → protects the marrow
- Leucovorin is given alongside, not to reverse the drug
Drugs with this mechanism (1)
- Pyrimethamine — Antifolate antiparasitic for toxoplasmosis.
Self-check
- Why accompany protozoal DHFR inhibitors with leucovorin?
To protect marrow. - Is protozoal DHFR selectivity sufficient to spare human marrow at therapeutic doses?
No.
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