Lonart Dose, Use, Composition, Side Effect
Lonart is an antimalarial. It contains artemether and lumefantrine. It is made in India by bliss GVS pharma limited founded in 1984. Lonart is marketed in Nigeria by greenlife pharmaceuticals and was introduced in 2006.
Lonart comes in different dosage forms with different strengths for different age groups. Lonart syrup comes in a powdered form to be reconstituted into a 60 ml solution. The tablet and syrup (5 ml) comes in 24, 18, 12 and 6 tablets of 20/120mg artemether and lumefantrine each and 80/480mg each of 6 of the same active pharmaceutical ingredient (API).
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| Lonart |
Composition Of Lonart
Composition Of Lonart Syrup
Each 5ml suspension after reconstitution contains:
Artemether 20mg
Lumefantrine 120 mg
Excipients q.s
Color: Sunset Yellow FCF
Composition Of Lonart Tablet
Composition Of Lonart DS
Each coated tablet contains:
Artemether 80mg
Lumefantrine 4800 mg
Excipients q.s
Color: Sunset Yellow FCF
Composition Of Lonart Tablet (6, 12, 18 and 24)
Artemether 20mg
Lumefantrine 120 mg
Excipients q.s
Color: Sunset Yellow FCF
Properties Of Lonart
Artmether was the most active derivative of the Artemisinins, a new class of antimalarial-drugs derived from Artemisinin. The latter compound is extracted from the plant Artemisia Annua and Artemether is prepared synthetically. Lumefantrine is a synthetic aryl amino alcohol similar to mefloquine and halo-fantrine.
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Indications And Use Of Lonart
Lonart is 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 Of Lonart
Pharmacodynamics
Both components of Lonart 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 as being the result of free-radical action.
Lumefantrine interferes more in the polymerization processes.
Other in vitro tests 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 as in the endoplasmic reticulum. Although Artemether acts essentially as a blood schizonticide, Lonart 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 derivatives 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 fasting to 100% at normal diet). Therefore patients 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 microsomes. This metabolite has 5 to 8 fold higher antiparasitic effects than Lumatantrine. 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 its metabolites are found in bile and feces.
Direction For Reconstitution Of Lonart Suspension
Add boiled and cooled water upto 60ml mark on the bottle, invert bottle and shake vigorously until all the powder is dispersed, then slowly add more water (if required) upto 60 ml mark on the bottle and again shake vigorously.
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Shake well before use. Use the reconstituted suspension within 7 days. The reconstituted suspension should be stored in a refrigerator (2°C to 8°C).
Direction For Reconstitution Of Lonart Dispersible Tablets
Dosage And Administration Of Lonart
The usual dose for children (5-14 kg or 6 month to 3 years) is 5 ml or 1 tablet of 6 (20 mg/120 mg) as a single initial dose, repeated as 5ml or 1 tablet of 6 (20 mg/120 mg) after 8 hours in a day and then followed by one dose 5 ml or 1 tablet of 6 (20 mg/120 mg) twice daily for the following two days.
The dose for children (15- 24 kg or 4 to 8 years) is 10 ml or 2 tablet of lonart 12 (40 mg/240 mg) as a single initial dose, repeated as 10 ml or 2 tablet of lonart 12 (40 mg/240 mg) after 8 hours in a day and then followed by one dose 10 ml or 2 tablet of lonart 12 (40 mg/240 mg) twice daily for the following two days.
The dose for children (24- 36 kg or 9 to 14 years) is 3 tablet if lonart 18 (60 mg/360 mg) as a single initial dose, repeated as 3 tablet of lonart 18 (60 mg/360 mg) after 8 hours in a day and then followed by one dose 3 tablet of lonart 18 (60 mg/360 mg) twice daily for the following two days.
The typical dose of Lonart 24 is 4 tablets (80 mg/480 mg) as a single initial dose, repeated as 4 tablets (80 mg/480 mg) after 8 hours in a day and then followed by four doses (80 mg/480 mg) twice daily for the following two days.
The typical dose of Lonart DS is 1 tablet (80 mg/480 mg) as a single initial dose, repeated as 1 tablet (80 mg/480 mg) after 8 hours in a day and then followed by 1 dose (80 mg/480 mg) twice daily for the following two days.
The maximum adult dose of Lonart is 160 mg/960 mg in a day.
Second dose to be taken strictly after 8 hours of the first dose. After each dose give your child a fatty meal or something to eat or drink.
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If you vomit within 1 hour of taking lonart repeat the dose immediately. Take dosage exactly as recommended, otherwise infection may return.
Precautions And Contraindications
Lonart is contraindicated in individuals hypersensitive to artemether and Lumefantrine. Therefore, there are no strict contra-indications for the use of Artemether. Nevertheless, no correlation has been found between QTc interval prolongation and plasma concentrations 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 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 fast acting schizonticides and rapid clearance of parasites is essential. Since lonart has been designed for its use in children it is unlikely that this problem arises.
Lonart 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 drug interactions were not seen. Artemether potentialises the antimalarial activity of other antimalarials.
As grapefruit juice retards the the absorption of some antimalarials, it would be better not to drink grapefruit juice while taking Lonart.
Side Effects Of Lonart
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.
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Some antimalarials such 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 starting a treatment with Lumefantrine combinations. For those patients physicians will be prescribed Artemisinin derivatives in monotherapy in case of severe paludisme.
Sometimes it could be possible that the following common side effects occur; rash, check this with your doctor. Other common side effects may occur as trouble 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 Plasmodial (Opening of a partide 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, recruitment does not exceed 10%. In case of recrudescence (renal or apparent) a new complete treatment for three days is advisable.
Breastfeeding: data on excretion in breast milk are not available for humans.
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