The product is indicated for children and adolescents up to the age of 16. Administration, by intramuscular injection over three days, is restricted to hospitals. It is a blood schizonticide active against all stages of P. falciparum , including the very early ring forms. In in vitro studies, artemotil has been shown to be effective against parasite strains resistant to other antimalarials, though this has not yet been confirmed formally in clinical studies. Fortunately, this metabolite has similar levels of antimalarial activity to artemotil.
Excretion is as the glucuronide of artenimol, principally in the faeces and urine.
Clinical studies in patients with severe malaria were carried out first in adults and later in children who could not be treated with oral medication, or who had critical cerebral malaria, in Africa and Thailand. No serious or inconvenient side effects were reported. Although, with artemisinin compounds in general, degenerative neurotoxic effects have been reported during pre-clinical safety studies in animals, these have occured at cumulative doses above 100 mg per kg body weight, whereas, in clinical treatment with artemotil, the cumulative dose reached is 11.2 mg per kg. Also, throughout the world, during treatment of millions of patients with various artemisinin derivatives, no neurotoxic effects have been reported. Nor has neurotoxicity been observed during controlled studies in volunteers and patients.