BG Mal-560 80/480mg Tab X6
Artemether (beta-artemether) is an active derivative of the artemisinins. A new class of antimalarial drugs derived from artimisinin which is extracted from the plant Artemisia annua. Lumefantrine is a synthetic aryl amino alcohol similar to mefloquine and halofantrine.
Pharmacological Properties:
Pharmacodynamics:
Both components of BG MAL SUSPENSION have their own action site in the malarial parasite. The presence of the endoperoxide bridge in artemether (generating singlet oxygen and free radicals which are very cytotoxic to the plasmodia) appears to be essential for antimalaria activity. Morphologic changes of the parasitic membranes induced by artemether have been described, being the result of free-radical action.
Lumefantrine interferes more in the polymerization processes. Other in vitro test suggest that both cause a marked diminution of nucleic acidsynthesis. Inhibition of protein synthsis as the basic mechanism of action is suggested in studies which showed morphological changes in ribosomes as well as in the endoplasmic riticulum. Although Artemether act as a blood schizonticide. Lumenfantrine-Artemether did clear gametocytes in comperative clinical trials.
Pharmacokinetics:
Orally administered artemether is rapidly absorbed reaching therapeutic level within 60-90 minutes. Artemether is metabolized in the liver to dihydroartemisinin (DHA). The elimination of artemether is rapid, with a T½ of 2-4 hours. Dihydroarteminsinin, being a proponent of antimalaria itself, has a T½ of about 2-4 hours. The degree of binding to plasma proteins varied markedly according to the species studied. The binding of Artemether with plasma protein in man is about 50%. Distribution of radioactive labeled Artemether was found to be equal between cells and plasma.
The absorption of lumefantrine is highly influenced by lipids and food intake (from 10% by fasting to 100% at normal diet). Therefore parents should be encouraged to give the medication with some fatty food as soon as it can be tolerated. Lumefantrine is metabolized in human liver microsomes. The metabolite has 5 to 8 fold higher anti-parasific effects than lumefantrine. Lumefantrine is found to be highly protein bound (95%).
The elimination half life in malaria-attaint patients will be 4 to 6 days. Lumefantrine and his metabolites are found in bile and faeces. Breastfeeding: Data on excretion in breast milk are not available for humans.
