| |
| Lonart Tablets / Forte Tablets / DS Tablets |
| Composition |
| LONART TABLETS |
(Arlemelher 20 mg + Lumefantrine120mg) |
| LONARTFORTE TABLETS |
(Artemether 40 mg + Lumefantrine 240 mg) |
| LONART DS |
(Artemether 80 mg + Lumefantrine 480 mg) |
|
| Properties |
Artemether is the
most active derivate of the Artemismines, a new class of antimalanal 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 halo-fantrine. |
| Indications |
LONART
/ LONART FORTE / LONART DS Tablets 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 |
Pharmacodynamics :
Both components of
LONART/ LONART FORTE / LONART DS have their own
action site in the
malarial parasite. The presence of the endoperioxide bridge in
Aflemelner
(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 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
/LONART FORTE / LONART
DS 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 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 celts 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.
Lumeiantrine is N-debutylated in human liver microsomes. This metabolite
has 5 to 8 fold higher antiparasitic effects than lumefantrine. Lumefantnne is
found to
be highly protein Pound (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. |
| Pharmaceutical
Precautions and Contra-Indications |
LONART
/ LONART FORTE / LONART DS 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 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 / LONART FORTE/
LONARTDS® has oeen designed
for its use in children it is unlikely that this problem arises.
LONART
/ LONART FORTE / LONART DS should not be taken during breast-feeding. Due to
the long elimination hall-life of lumefantrine, it is recommended that breast-feeding
should not start until at least one week after stopping an
Artemelher/Lumefantnne 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
metabolism of some antimalarials. it would be better not to drink grapefruit
juice while taking LONART / LONART FORTE / LONART DS. |
| 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 beendescribed 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
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 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 not exceed 10%. In
case of recrudescence (renal or apparent) a new complete treatment for three
days is advisable. |
| Dosage and
Administration |
| Lonart Tables : |
| Weight |
Total |
DOSAGE REGIMEN |
| in Kg |
Tablets |
Day-1 |
Day-2 |
Day-3 |
| |
|
0 hr. |
8 hr. |
24 hrs. |
36 hrs. |
48 hrs. |
60 hrs. |
| 5-14 |
6 |
1 |
1 |
1 |
1 |
1 |
1 |
| 15-24 |
12 |
2 |
2 |
2 |
2 |
2 |
2 |
| 25-34 |
1S |
3 |
3 |
3 |
3 |
3 |
3 |
| 35 - and more
(admits) |
24 |
4 |
4 |
4 |
4 |
4 |
4 |
| |
| LONART FORTE TABLETS : |
| Weight |
Total |
DOSAGE REGIMEN |
| in Kg |
Tablets |
Day-1 |
Day-2 |
Day-3 |
| |
|
0 hr. |
8 hr. |
24 hrs. |
36 hrs. |
48 hrs. |
60 hrs. |
| 10-14 |
3 |
1/2 |
1/2 |
1/2 |
1/2 |
1/2 |
1/2 |
| 15-24 |
6 |
1 |
1 |
1 |
1 |
1 |
1 |
| 25-34 |
9 |
11/2 |
11/2 |
11/2 |
11/2 |
|
|
| 35 - and more (adrults) |
12 |
2 |
2 |
2 |
2 |
2 |
2 |
| |
| LONART DS TABLETS : |
| Weight |
Total |
DOSAGE REGIMEN |
| in Kg |
Tablets |
Day-1 |
Day-2 |
Day-3 |
| |
|
0 hr. |
8 hr. |
24 hrs. |
36 hrs. |
48 hrs. |
60 hrs. |
| Adults |
6 |
1 |
1 |
1 |
1 |
1 |
1 |
|
|
|
|
|
|
|
|
|
|
| Breast-feeding |
| Data on excretion in
breast milk are not available for humans. |
| Shelf Life |
| 2 Years
from the Date of Manufacturing. |
| Dispensing Category |
| Prescription only Medicine. |
| Presentation |
LONART TABLETS - Each
carton contains blisters of 3x8 Tablets
LONART FORTE TABLETS - Each carton contains
blisters of 2x6 Tablets.
LONART DS TABLETS - Each carton contains blisters of 1
x 6 Tablets. |
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