Artemisinin

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

Single dose studies of 500mg in adult patients: Cmax: 428 mcg/L; Half-life: 2.5 hours; Table 1

Adverse Effects

Cardiac: QTc prolongation, bradycardia

Dosage

The conventional dosage regimen for orally administered Artemisinin is 500-1000 mg (10-20 mg/kg) on the first day, followed by 500 mg daily for 4 days.

Artemisinin suppositories have been given to patients with severe falciparum malaria, at doses of 600-1200 mg initially, followed by 400-600 mg 4 h later and 400-800 mg daily for 3 days.

Generally, mefloquine 15-25 mg/kg is given 24-72 h after commencement of Artemisinin therapy.

Disease state based dosing:

No data available

Contraindications/Warnings/Precautions

No data available

Drug Interactions

No data available

Pregnancy

The World Health Organization currently recommends artemisinin-based combination therapy (ACT) for three days in the treatment of uncomplicated falciparum malaria. Artemisinin compounds are considered acceptable in the 2nd and 3rd trimester of pregnancy, but not in the 1st trimester. In severe malaria, parenteral artesunate or artemether are preferred in the 2nd and 3rd trimester. Quinine may be preferred in the 1st trimester, but a risk:benefit assessment is required and artesunate may be considered as a treatment option.

Monitoring Requirements

None

Brand names/Manufacturer

Brand names and manufacturer are not available. Below are listed synonyms of Artemisinin:

Arteannuin; Artemisinina; Artemisinine; Artemisininum; Huanghuahaosu; Qinghaosu.