Artemether+Lumefantrine for Oral Suspension 15mg+90mg/60ml

• Application: Internal Medicine
• Usage Mode: For oral administration
• Suitable for: Elderly, Adult
• State: Powder
• Shape: Powder
• Type: Organic Chemicals
• Model NO.: AMC16008
• Pharmaceutical Technology: Chemical Synthesis
• Transport Package: 1 Bottle/Box
• Specification: 105mg/60ml
• Trademark: AMC
• Origin: China
• HS Code: 3004909099

Product Description

Product Description

ACTIVE INGREDIENTS: Artemether and Lumefantrine
COMPOSITION:
Artemether + lumefantrine suspension (Artemether 180mg+Lumefantrine 1080mg in 100ml bottle).
ARTEMETHER + LUMEFANTRINE SUSPENSION:
Artemether is the most active derivative of the Artemisinin, a new class of antimalarial drugs derived 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 halofantrine.
PHARMACOLOGICAL PROPERTIES:
Pharmacodynamics: Both components of artemether + lumefantrine suspension have their own action site in the malarial parasite. The presence of the endoperoxide bridge in Artemether (generating singlet 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 nucleic 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, artemether + lumefantrine suspension did clear gametocytes in comparative clinical trials.
Pharmacokinetics: Orally administered Artemether is rapidly absorbed reaching therapeutic levels within 60-90 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 T 1/2 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-demethylated 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 in malaria attaint patients will be 4 to 6 days. Lumefantrine and his metabolites are found in bile and faeces.
Breastfeeding: Date on excretion in breast milk are not available for humans.
INDICATIONS:
ARTEMETHER + LUMEFANTRINE 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:
Artemether + lumefantrine suspension is contraindicated in individuals hypersensitive to Artemether and Lumefantrine. Therefore, there are no strict contra-indications for the use of Artemether in children. Nevertheless, no correlation has been found between QT 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 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, Artemisinin derivatives like Artemether are the fastest acting schizonticides and rapid clearance of parasites is essential. Since artemether + lumefantrine suspension has been designed for its use in children it is unlikely that this problem arises. Artemether + lumefantrine 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 potentialize 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 + lumefantrine suspension.
SIDE EFFECTS:
With Artemether virtually no side effect has been seen. Laboratory abnormalities such as slight raised 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 acausal 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 be taken in account before to start 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 specific 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 developing at different times in the same patient. In controlled studies recrudescence does not exceed 10%. In case of recrudescence (renal or apparent) a new complete treatment for three days is advisable.
DOSAGE AND ADMINISTRATION:

Body weight	Number of Milliliters
	1"Day	2" Day	3" Day
5 Kgs	7 ml	7 ml	7 ml
7.5 Kgs	10 ml	10 ml	10 ml
10 Kgs	14 ml	14 ml	14 ml
15 Kgs	20 ml	20 ml	20 ml

PHARMACEUTICAL PRECAUTIONS:
Artemether + lumefantrine suspension bottles should be stored below 25ºC. in a closed bottle artemether + lumefantrine suspension powders are stable. Once the suspension has been made up, it is stable for a minimum of 14 days. Longer conservation is not recommended.
SHELF LIFE: 3 Years.
DISPENSING CATEGORY: Prescription medicine.
PRESENTATION: Each cardboard box contains 1 bottle.