Artesunate

Mechanism :

There are three common forms of artemisinin. The water-soluble form is called artesunate. It is the most active and the least toxic within the body. Artemether is the lipid soluble form. It has the longest life but also the most toxic in high dosage which is seldom needed. The biggest advantage of artemether is that it can cross the blood brain barrier. Artemisinin is the active parent compound of the plant. Its half-life is intermediate. It is also very safe and can cross the blood-brain barrier. Artemisinin has been shown to work through oxygen and carbon based free radical mechanisms.

Indication :

Malaria

Contraindications :

First trimester of pregnancy.

Dosing :

In children <20 kg: 3 mg/kg/day IM or IV. In children >20 kg: 2.4 mg/kg/dose IM or IV till the child can eat orally. Then shift to oral therapy. As part of artemisinin combination therapy (ACT): 4 mg/kg/day for 3 days.

Artesunate + Amodiaquine: (Available as FDC containing 25 mg + 67.5 mg, 50 mg + 135 mg or 100 mg + 270 mg of artesunate +amodiaquine respectively) Oral therapy for 3 days.

4 mg/kg/day of artesunate and 10 mg/kg/day of amodiaquine

Artesunate + Mefloquine: (Available as FDC containing 25 mg + 55 mg or 100 mg + 220 mg of artesunate + mefloquine respectively).

4 mg/kg/day of artesunate and 8.3 mg/kg/day of mefloquine.

As per weight bands:

5 to <9 kg: 25 mg + 55 mg of artesunate + mefloquine OD.

9 to <18 kg: 50 mg + 110 mg of artesunate + mefloquine OD.

18 to <30 kg: 100 mg + 220 mg of artesunate + mefloquine OD.

>30 kg: 200 mg + 440 mg of artesunate + mefloquine OD.

Adverse Effect :

Gastrointestinal disturbances, dizziness, tinnitus and prolongation of QT interval.

Interaction :

Quinidine and halofantrine: Caution in concurrent usage with drugs that prolong QT interval.