Arteether

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

3.6mg/kg single dose in healthy volunteers; Half-life: 23.1 hours; Volume of distribution: 28.5 L/kg; Table 5

Adverse Effects

Cardiac: QTc prolongation, bradycardia

Neurologic: Neurotoxic (by mostly in-vitro data)

Dosage

The recommended dose schedule is 3.2 mg beta-arteether/kg body weight on day 1, followed by 1.6 mg beta-arteether/kg on days 2 through 5.

Disease state based dosing

No data available

Contraindications/Warnings/Precautions

No data available

Drug Interactions

No data available

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