| |
| Lonart Suspension |
| Composition |
| LONART Oral
Suspension
(Artemether 180 mg +
Lumefantrine 1080 mg in 6O ml bottle) 24gms |
| Properties |
Artemether is the most active
derivate of the Arternisinines, 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 helo-fantrine. |
| Pharmacological Properties |
Pharmacodynamics
: Both components of LONART have their own action site in the malarial parasite
The presence of the endoperioxide bridge in Aftemelher (generating singlel oxygen and
Tree radicals: those are very cytotoxrc 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 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 elimmation is rapid, with a T1/2 of 2-4 hours.
Dihydroartemisinln, 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 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-debutylaledi in human
liver microsomes. This metabolite 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, attaint patients will be 4 to 6 days. Lumefantrine and his metabolities are found
in bile and faeces.
Breastfeeding : Data
on excretion in breast milk are not available for humans |
| Indications |
LONART
Oral 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 |
LONART 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 QTc interval prolongation and plasma concentrations of
lumefantrine caution is advised to patients who are taking drugs that are know
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 lor 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 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 Artefnether / Lumelantrine combination treatment. |
| Drug Interactions |
Specific negative drug drug interactions were nor seen. Artemether
potentialises the antimalarial activity of other antimalariaIs. As grapefruit
juice retards
the metabolism of some antimalarials, it would be better not to drink
grapefruit juice while taking LONART. |
| Side Effects |
With Artemether virtually no side effect 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. 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 should be taken in account before to start a. treatment
with lumefantrine combinations. For those patients physicians will be prescribed Artemismin
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 Recurdescence |
| 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
nor 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 Millilitres |
|
|
1st Day |
2nd Day |
3rd Day |
| 5 Kgs |
7 ml |
7 ml |
7 ml |
| 7.5 Kgs |
10 ml |
10ml |
10 ml |
| 10 Kgs |
14 ml |
14 ml |
14 ml |
| 15 Kgs |
20 ml |
20 ml |
20 ml |
|
| Pharmaceutical
Precautions |
| LONART bottles should be stored below 25'C.
In a closed bottle
LONART powders are stable Once the suspension has been made up. ii is
stable lor a minimum of 14 days. Longer conservation is not recommended |
| Shelf Life |
| 2 Years |
| Dispensing Category |
| Prescription Medicine. |
| Presentation |
| Each carboard box contains 1 bottle |
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