|Artemether + Lumefantrine||Powder for Suspension||20mg+120mg||1000.0982|
|Artemether + Lumefantrine||Powder for Suspension||180mg+1080mg||1000.2501|
|Artemether + Lumefantrine||Powder for Suspension||240mg+1440mg||1000.2647|
ACTIVE INGREDIENTS: Artemether and Lumefantrine
PROPERTIES: Artemether is the most active derivate of the Atremisinines, a new class of antimalarial drugs from Artemisinin. The latter compound is extracted from the plant Artemisia Annua and Artemether is prepared semi-synthetically. Lumefantrine is a synthetic aryl amino alcohol similar to mefloquine and halo-fantrine.
Pharmacodynamics: Both components of artemether and lumefantrine have their own action site in the malarial parasite. The presence of the endoperioxide bridge in Artemether (generating single oxygen and free radicals: those are very cytotoxic to the plasmodia) appears to be essential for antimalarial activity. Morphological 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 nudleic acid synthesis. Inhibition of protein synthesis as the basic mechanism of action is suggested in studies which showed morphological changes in ribosomes as well in the endoplasmic reticulum. Although Artemether acts essentially as a blood schizonticide, the combination did clear gametocytes in comparative clinical trials.
Pharmacokinerics: Orally administered Artemether is rapidly absorbed reaching therapeutic levels within 10-90 minutes. Artemether is metabolized in the liver to the demethylated derivate dihydroartemisinin (DHA). The elimination is rapid, with a T1/2 of 2-4 hours. Dihydroartemisinin, being a potent antimalarial itself, has a T1/2 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%. Radioactivity distribution of 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 fasten 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 N-debutylated in human liver microsome. This metabolite has 5 to 8 fold higher antiparasitic 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 metabolities are found in bile and faeces.
Breastfeeding: Data on excretion in breast milk are not available for humans.
INDICATIONS: Oral Suspension is indicated for the treatment of malaria in children, caused by all forms of Plasmodium including severe malaria caused by multiple drug resistant strains of P. Falciparum.
PHARMACEUTICAL PRECAUTIONS AND CONTRA-INDICATIONS: No strict contra-indications for the use of Artemether in children. Nevertheless, no correlation has been found between QTc interval prolongation and plasma concentration of lumefantrine caution is advised to patients who are taking drugs that are known to prolong the QT interval, such as certain antibiotics (macrolides, fluoroquinolones, imidazole) or who are predisposed to cardiac arrhythmias. It is advisable not to use drugs during pregnancy but in view of the high risk of malaria during pregnancy for mother and foetus, the responsible physician may consider it essential, as in the case of cerebral malaria, to treat a pregnant woman. Artemisnin derivatives like Artemether are the fastest acting schizontocides and rapid clearance of parasites is essential. Since Artemether + Lumfantrine Powder for Suspension has been designed for its use in children it is unlikely that this problem arises. Artemether + Lumfantrine Powder for Suspension should not be taken during breast-feeding, due to the long elimination half-life of lumefantrine, it is recommended that breast-feeding should not start until at least one week after stopping an Artemether/ Lumefantrine combination treatment.
DRUG INTERACTION: Specific negative drug interactions were not seen. Artemether potentialises the antimalarial activity of other antimalarials. As grapefruit juice retards the metabolism of some antimalarials, it would be better not to drink grapefruit juice while taking Artemether + Lumfantrine Powder for Suspension.
SIDE EFFECTS: With Artemether virtually no side effects have been seen. Laboratory abnormalities such as slight rise in transaminases and a decrease in reticulocyte count are rare and transient. A lowering of sinus frequency without causing ECG changes has been noticed. At high doses transient abdominal pain, tinnitus and diarrhea have been described but a causal relationship is unclear. Some antimalarials as halofantrine and quinine can influence the ECG pattern. Attention should be made to patients previously treated with those antimalarials. A reasonable period should be taken into account before to start a treatment with lumefantrine combinations. For those patients physicians will be prescribed Artemisinin derivatives in mono therapy in cause of severe paludism. Sometimes it could be possible that the following common side effect occur; rash, check this with you doctor. Other common side effects may occur as trouble of sleeping, nausea, vomiting, diarrhea, coughing. They need medical attention when persisting.
RESISTANCE AND RECRUDESCENCE: Resistance of Plasmodia to artemether has not been observed. It is also unlikely to occur in view of the speciflc mechanism of action which is very cytotoxic for Plasmodia (opening of a peroxide bridge). An apparent resistance is sometimes seen but is mainly due to multiple broods of plasmodia (renal or apparent) a new complete treatment for three days is advisable.
Mercator's Other popular Antimalarial products according to the WHO guidelines include:
1. Arteether Injection
2 Artemether + Lumefantrine Powder for Suspension
3. Artemether + Lumefantrine Tablets
4. Artemether Injection
5. Artemisinin + Piperaquine Tablets
6. Artesunate + Amodiaquine Tablets
7. Artesunate + Mefloquine Tablets
8. Artesunate + Sulfadoxine + Pyrimethamine Tablets
9. Chloroquine Phosphate Injection
10. Dihydroartemisinin + Piperaquine Phosphate + Trimethoprim Powder for Suspension
11. Dihydroartemisinin + Piperaquine Phosphate + Trimethoprim Tablets
12. Dihydroartemisinin + Piperaquine Phosphate Powder for Suspension
13 Dihydroartemisinin + Piperaquine Phosphate Tablets
14. Quinine Dihydrochloride Injection
15. Sulfadoxine + Pyrimethamine Tablets