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.
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.
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.
BG MAL SUSPENSION is an artemisinin-based combination therapy (ACT) 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.
BG MAL SUSPENSION is contra-indicated in individuals hypersensitive to any of the ingredients.
No correlation has been found between Qtc interval prologation and plasma concentrations of lumefantrine.
Caution is advised patients who are taking drugs that are known to prolong the QT interval. Such as certain antibiotics (macrolides, Fluroquinolones, imdazole) or who are predisposed to cardiac arrhythmias.
there are no strict contra-indications for the use of artemether in children BG MAL SUSPENSION has been especially designed for paediatric use.
Pregnancy and breast-feeding:
It is adviseable not to use drugs during pregnancy.
Inview of the high risk of malaria during pregnancy for mother foetus, the responsible physician may consider it essential, as in the case of cerebral malaria, to treat pregnant woman.
BG MAL 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.
Specific negative drug-drug interactions were not seen.
Artemether potentialises the antimalaria activity of other antimalarials.
As grapefruit juice retards the metabolism of some antimalarials, it would be better not to drink grapefruit juice while taking BG MAL SUSPENSION.
With Artemether virtually no side effect has been seen. Laboratory abnomalities such as a slight rise in transminases and a decrease in reticulocyte count are rare 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 casual relationship is nuclear.
Some antimalaria are 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 in account before to start a treatment with lumefantrine combinations.
Sometimes it could be possible that the following common side effect occur: rash check this with your doctor.
Other common side effects may occur: 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 the plasmodia (opening of a peroxide bridge).
An apparent resistance is sometimes seen but is mainly due to mutiple broods of plasmodia developing at different times in the same patient.
In controlled studies recrudescence does not exceed 10%. In case of recrudescene (real or apparent) a new complete treatment for three days advisable.
Dosage & Administration
A bottle containing Artemether and Lumefantrine in a dry powder mixture for making up a suspention with water.
After adding water the solution becomes yellow and the product has a pleasant taste of pineapple.
One bottle contains 180 mg of Artemether and 1080 mg of Lumefantrine for 60 mL suspension.
BG MAL SUSPENSION has especially been designed for use in children up to 15 kg. The dose depends on the severity of the case and the clinical situation of the patient.
4 mg Artemether/kg body weight per day, in combination with lumefantrine.
This dose should be maintained during three consecutive days.
The daily dose should be administered in one gift.
A full course therapy of three days is essential in order to avoid recrudescence.
Vomiting within one hour require repeating the dose.
Making up the BG MAL SUSPENSION
• Open the bottle by the breaking the seal and add tap water of a good quality.
• Fill the bottle up to the making point indicating 60 mL.
• Shake well until all powder has disappeared from the bottle. This should only take a few seconds. It may be necessary to add a little bit more water to readjust the volume to 60 mL. The suspension is stable for 7 days.
It is advisable to shake the bottle before you use BG MAL SUSPENSION.
Each sub unit of 5 mL contains 15 mg Artemether and 90 mg Lumefantrine. For each patient your physician or pharmacist will calculate how many milliliters should be administered.
It is recommended to round off the dosage to the nearest subdivision. Practical scheme for administering the correct dose of BG MAL SUSPENSION
DOSAGE AND ADMINISTRATION:
|Body Wt. (Age Group)||Day 1||Day 2||Day 3|
|5-14 kgs (6 months-3yrs)||0 hr||8 hr.||24 hrs.||36 hrs.||48 hrs.||60 hrs.|
|5 mL||5 mL||5 mL||5 mL||5 ml||5 mL|
|15-24 kgs (4-8 yrs)||10 mL||10 mL||10 mL||10 mL||10 mL||10 mL|
Overdose: Incase of overdosage, emergency symtomatic treatment in a specialist facility is required, which should include ECG and potassium monitoring.
BG MAL SUSPENSION bottle should be stored at room temperature below 30°C.
Protect from light and humidity.
KEEP MEDICINE OUT OF REACH OF CHIDREN.
In a close bottle, once the suspension has been made up, it is stable for 7 days.
Longer conservation is not recommended.
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