Artesunate
Indications
Artesunate is used for:
Malaria, Schistosomiasis
Adult Dose
Falciparum malaria especially in quinidine-resistant patients
Adult: PO: 4 mg/kg once daily x3 days (with mefloquine)
Child Dose
Renal Dose
Administration
Contra Indications
Hypersensitivity.
Precautions
Hepatic or renal insufficiency. Pregnancy and lactation.
Lactation: unknown
Pregnancy-Lactation
Pregnancy
May administer to pregnant women in second and third trimesters
Data are limited for first trimester of pregnancy; no harmful effects have been observed
Animal studies
Causes fetal toxicity in rats and rabbits resulting in fetal resorption and abortion
Low incidence of cardiac malformations and skeletal defects also observed
Clinical considerations
Severe malaria is life-threatening for pregnant women and their fetuses, and artesunate should not be withheld if quinidine is unavailable, contraindicated, ineffective, and/or not tolerated
Lactation
Limited distribution into human breast milk
LactMed states limited information indicates that a maternal dose of 200 mg PO produced low levels in milk and would not be expected to cause any adverse effects in breastfed infants, especially if aged >2 months
Withholding breastfeeding for 6 hr after dose should markedly reduce amount infant receives
Interactions
Antimalarial potentiating action seen with mefloquine, primaquine and tetracycline. Additive effect with chloroquine. Antagonistic effect with pyrimethamine and sulphonamides.
Adverse Effects
Side effects of Artesunate :
Generally well-tolerated, Cardiotoxicity (high doses), Neurotoxicity observed in animal studies, Drug induced fever, Skin rash
Mechanism of Action
Artesunate is a potent and rapidly-acting blood schizontocide derived from the leaves of the chinese herb, Armesia annua. The exact mode of action is not clear but clinical studies have confirmed the effectiveness of artesunate in P. vivax and falciparum malaria. Unclear, may inhibit DNA replication & transcription.