Dihydroartemisinin

Class:

Sesquiterpene with an endoperoxide moeity

Antiparasitic Activity:

Active against all human malarial parasites, including multi-drug resistant Plasmodium falciparum strains.

Mechanism of Action:

Several proposed including the production of free radicals, other reactive metabolites, and altered membrane transport properties of membranes which may inhibit nutrient flow to the parasite.

Pharmacodynamics:

No data available

Pharmacokinetics:

1.2mg/kg dose in adult patients with P. falciparum malaria: Cmax: 490 mcg/L; Half-life: 58 minutes; Table 3

Adverse Effects:

Cardiac: QTc prolongation, bradycardia

Neurologic: Neurotoxic (by mostly in-vitro data)

Dosage:

The recommended dose for dihydroartemisinin is 120 mg initially, then 60 mg daily for a further 4 to 6 days.

Disease state based dosing:

Ascites/Edema: No data, however due to relatively low volume of distribution, dose calculations based on ideal body weight may be appropriate.

Contraindications/Warnings/Precautions:

No data available

Drug Interactions:

Concomitant administration of mefloquine and dihydroartemisinin leads to a modest increase in mefloquine absorption rate

Pregnancy:

Not established. The World Health Organization currently advises against the use of artemisinins in the first trimester of pregnancy, unless in a lifesaving situation where other drugs are not suitable. In the second and third trimesters of pregnancy, artemisinin and its derivatives are not recommended unless alternative drug treatments are unsuitable.

Monitoring Requirements:

None

Brand names/Manufacturer:

Information not currently available