Paper II
2019 July (Supplementary) (2010 Scheme)

Question

Artemisinin derivatives

Q63 marksShort Notes

Answer

Examples: Artesunate, Artemether, Arteether, Dihydroartemisinin

Mechanism of action

  • Contain an endoperoxide bridge that is cleaved by intraparasitic haem/iron, generating cytotoxic free radicals that damage parasite proteins and membranes
  • Produce the most rapid parasite clearance of any antimalarial class

Uses

  • Blood schizonticides for both uncomplicated and severe/complicated P. falciparum malaria
  • Always used in combination with a longer-acting partner drug (ACT) to prevent recrudescence and resistance
  • IV Artesunate is the treatment of choice for severe malaria

Adverse effects

  • Generally well tolerated: GI upset, dizziness
  • Rare: neutropenia, mild cardiotoxicity (with prolonged use)

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