LumeTRUST Artemether and Lumefantrine Tablets

 



LumeTRUST-140 (20/120 mg) 
Composition:
Each uncoated tablet contains:
Artemether                         20 mg
Lumefantrine                     120 mg

LumeTRUST-DS (40/240 mg)

Composition:

Each uncoated tablet contains:
Artemether                         40 mg
Lumefantrine                     240 mg

LumeTRUST-FORTE (80/480 mg)
Composition:
Each uncoated tablet contains: 

Artemether                               80 mg
Lumefantrine                          480 mg

PROPERTIES

• Excipients: Artemether is the most active derivative of the artemisinines, 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 acylamino alcohol similar to mefloquine and halo-fantrine.
• Indications: Artemether and Lumefantrine Tablets are indicated for the treatment of malaria. Caused by all forms of Plasmodium including severe malaria caused by multiple drug resistant strains of P. Falciparum.

PHARMACOLOGICAL PROPERTIES

Pharmacodynamics:
Both components of Artemether and Lumefantrine Tablets have their own action site in the malarial parasite. The presence of the endoperoxide bridges in artemether
(generating singlet oxygen and free radicals: those are very cytotoxic to 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 tests suggest that both caused 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 as in the endoplasmic reticulum.
Although artemether acts essentially as a blood schizonticide, Artemether and Lumefantrine Tablets 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 derivative of dihydroartemisinic (DHA). The elimination is rapid with a T1/2 of 2-4 Hours.

 Dihydroartemisinic, being a potent anti-malarial 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 microsomes. This metabolite has 5-to-8-fold higher antiparasitic effects than Lumefantrine is found to be highly protein bound (95%). The elimination of half-life in malaria attaint patients will be 4 to 6 days. Lumefantrine and its metabolites are found in bile and faeces. 

PHARMACEUTICAL PRECAUTIONS AND CONTRA-INDICATIONS

Tablets are contraindicated in individuals hypersensitive to Artemether and Lumefantrine. Therefore, there are no strict contra- indications for the use of Artemether in the children.

Nevertheless, no correlation has been found between OTC interval prolongation and plasma concentrations of Lumefantrine caution is advised to patients who are talking drugs that are known to prolong the OT interval. Such as certain antibiotics (Macrolides, Fluroquinolones, imidazole) or those 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 fetus. 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. It is essential, since Artemether and Lumefantrine Tablets have been designed for their use in children, it's unlikely that this problem will arise. Artemether and Lumefantrine Tablets 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 INTERACTIONS

Specific negative drug-interactions were not seen. Artemether potentializes 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 and Lumefantrine Tablets.

SIDE EFFECTS

With Artemether virtually no side effects have been. Laboratory abnormalities such as slight increase in transaminases and a decrease in reticulocyte count are and transient. A lowering of its frequency without causing ECG changes has been noticed. At high doses transient abdominal tinnitus and Dianthia have been described but a causal relationship is unclear.
Some antimalarials such as halofantrine and quinine can influence the ECG pattern, Attention should be made to patients previously treated with those antimalarial. A reasonable period should be taken into account before starting a treatment with Lumefantrine Combinations. For those physicians 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 the doctor. Other common side effects may occur such as trouble sleeping, nausea, vomiting, diarrhea, coughing. They need medical attention when persisting.

RESISTANCE AND RUDESCENCE

Resistance of Plasmodia to Artemether has not been observed. It is also unlikely to occur in the specific mechanism of action which is very cytotoxic for plasmodia (Opening of a Pere bridge). An apparent resistance is sometime seen but is mainly due to multiple broods of plasma developing at different times in the same patient. In controlled studies recrudescence does exceed 10% in case of recrudescence (renal or apparent) a new complete treatment for three is advisable.