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Lonart Tablet, Suspension and Suppository

Greenlife Pharmaceuticals Ltd
2, Bank Lane, Off Town Planning Way, Ilupeju, Lagos State, Nigeria
Email: info@greenlifepharmaceuticals.com, greenlife2001@yahoo.com
Tel: 01-737-8991; 01-871-3181; 0803-343-1338; 0803-569-9324

Brand Name

Lonart Tablet, Suspension and Suppository

Manufacturer

Therapeutic Class

Antimalarial drugs

Dosage Form, Composition & NAFDAC Registration Number (NRN)

Lonart Tablet

Tablet (NRN: 04-8969): Artemether 20 mg, Lumefantrine 120 mg.

Pack size: 3 x 8's (in blisters).

Lonart Suspension

Suspension (NRN: ): Artemether 180 mg, Lumefantrine 1080 mg per 60 mL.

Pack size: 60 mL bottle.

Lonart Suppository

Suppository (NRN: ): Artemether 20 mg, Lumefantrine 120 mg.

Pack size: 1 x 6's (in blisters).

Pharmacology

Artemether is the most active derivate of the artemisinines, a new class of antimalarial drugs derived from artemisinin. The later 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.

Pharmacodynamics:

Both Artemether and Lumefantrine have their own action site in the malarial parasite. The presence of the endoperioxide 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 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 derivate dihydroartemisinin (DHA). The elimination is rapid with a T½ of 2-4 hours. Dihydroartemisinin, being a potent antimalarial 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%. 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% in fasted 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 metabolites 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 treated patients will be 4 to 6 days. Lumefantrine and its metabolites are found in bile and faeces.

Indications

Treatment of malaria caused by all forms of Plasmodium including severe malaria caused by multiple drug resistant strains of P. falciparum

Contra-indications

Precautions/Warnings

Hypersensitivity to Artemether and Lumefantrine. There are no strict contraindications for the use of Artemether in children.

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 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 schizontocides 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 breastfeeding. Due to the long elimination half-life of Lumefantrine, it is recommended that breastfeeding should not start until at least one week after stopping an Artemether/Lumefantrine combination treatment.

Interactions

Artemether potentiates 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 Lonart.

Adverse 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 casual relationship is unclear.

Some antimalarials such as Halofantrine and Quinine can influence the ECG pattern. Attention should be made to patient previously treated with those antimalarials. A reasonable period should be taken into account before starting treatment with Lumefantrine combinations. For such patients, mono therapy with Artemisinin derivatives is recommended.

Sometimes rash, trouble sleeping, nausea, vomiting, diarrhea, coughing may occur. They need medical attention when persisting.

Dosage & Administration

Lonart Tablet:

Weight in kg Total Tablets Dosage Regimen
Day 1 Day 2 Day 3
0 Hr 8 Hrs 24 Hrs 36 Hrs 48 Hrs 60 Hrs
<10 Not recommended
 10 - 14  1  1
 15 - 24 12 
 25 - 34 18 
 ≥35 (Adult)  24

Lonart Suspension:

Weight in kg Dose (mL)
1st Day 2nd Day 3rd Day
5 kg 7 7 7
7.5 kg 10 10 10
10 kg 14 14 14
15 kg 20 20 20

Lonart Suppositories: (For Children):

Weight in kg Total Suppositories Dosage Regimen
Day 1 Day 2 Day 3
0 Hr 8 Hrs 24 Hrs 36 Hrs 48 Hrs 60 Hrs
<10 Not recommended
10 - 14 6 1 1 1 1 1 1
15 - 24 12 2 2 2 2 2 2
25 - 34 18 3 3 3 3 3 3

How to use Suppositories:

The suppositories should be inserted deeply into the anus, if possible after having the bowels open. Clean the area around the rectum with mild soap and warm water, and rinse thoroughly. Gently dry by patting or blotting with toilet tissue or a soft cloth.

Detach one suppository from the strip. Remove wrapper before inserting suppository by holding suppository upright and carefully peeling wrapper evenly down both sides of the suppository. Avoid excessive handling as the suppository is designed to melt at body temperatures. There is no need to refrigerate this product if stored below 80oF(27oC).

Position the patient flat on back or on one side, with anal opening exposed. Gently insert the suppository well into the rectum. Use fingertip to complete insertion. If necessary, hold buttocks together for 30-60 second to keep suppository in place.

Storage/Handling Recommendations

Tablet: Store below 25oC.

Suspension: Powder should be stored below 25oC. Once reconstituted, it is stable for a maximum of 14 days. Longer conservation is not recommended.

Suppository: Store below 25oC.

Review Date

2016-11-19 05:55:15