Arteether  (PDF Version)

 

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