Sesquiterpene with an endoperoxide moeity
Active against all human malarial parasites, including multi-drug resistant Plasmodium falciparum strains.
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.
No data available
3.4mg/kg dose in adult patients; Cmax: 689 mcg/L; Half-life: 4.2 hours; Table 4
Cardiac: QTc prolongation, bradycardia
For both uncomplicated and severe falciparum malaria, the recommended dose schedule is 3.2 mg/kg on day 1, followed by 1.6 mg/kg daily for up to 7 days. An oral dose of approximately 2 mg/kg daily, for up to 7 days has also been suggested for the treatment of uncomplicated malaria.
For the combined artemether (20 mg)/ lumefantrine (120mg) tablet preparation, a dose of artemether (80 mg)/ lumefantrine (500 mg) given to adult patients (travellers returning to Europe after visiting tropical countries) at the time of diagnosis, and repeated at 6-8, 24 and 48 h is recommended.
For the treatment of patients who have no natural immunity, an adult dose of artemether 80 mg/ lumefantrine 500 mg given at the time of initial diagnosis, and repeated after 8, 24, 36, 48 and 60 h is suggested.
Children’s doses should be scaled appropriately as recommended in the manufacturer’s international product information.
Renal failure: Although clearance decreases in patients with acute renal failure, overall the data suggest no dosage adjustment is necessary.
Hepatic Insufficiency: no data available
No data available
Varying reports on interactions with mefloquine (significant decrase in the AUC). Concomitant administration of ketoconazole and artemether resulted in an increased AUC of artemether.
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.
None
PALUTHER (Aventis – BRAZIL, FRANCE)