COMPOSITION AND PHARMACEUTICAL FORM
Active Substance: Artemether and Lumefantrine.
One tablet contains 40mg Artemether and 240mg Lumefantrine.
Artelum® is a fixed combination of Artemether and Lumefantrine which acts as a blood schizontocide. Its Indications include:
-Treatment of adults and children and infants with acute, uncomplicated infections due to plasmodium falciparum or mixed infections including P. falciparum. Because Artelum® is effective against both drug-sensitive and drug- resistant P.falciparum it is also recommended for malaria infections acquired in areas where the parasites may be resistant to other antimalarials.
DOSAGE AND ADMINISTRATION
Tablets for oral administration
The dosage is two tablets to be taken twice daily, morning and night for three days for the treatment of malaria. Patients with acute malaria are frequently averse to food. The dose should be taken with fat food or drinks such as milk.
Patients should be encouraged to resume normal eating as soon as food can be tolerated since this improves absorption of artemether and lumefantrine. In the event of vomiting within 1 hour of administration a repeat dose should be taken.
Treatment and Stand-by emergency treatment
Dosage in adults and children weighing 35kg and above.
A standard 3 days treatment schedule with a total of 6 doses is recommended as follows.
Two tablets as a single dose at a time of initial diagnosis, again 2 tablets after 8 hours and then 2 tablets twice daily (morning and evening) on each of the following two days (total course comprises 12tablet).
Dosage in elderly patients
Although no studies have been carried out in the elderly, no special precautions or dosage adjustments are considered necessary in such patients.
Dosage in patients with mild to moderate renal or hepatic Impairment
No specific studies have been carried out in these groups of patients and no specific dose adjustment recommendations can be made for these patients (for patients with severe renal and/or hepatic insufficiency). Most patients with acute malaria present with some degree of related hepatic impairment. The adverse event profile did not differ in patients with and those without hepatic impairment. Moreover, baseline abnormalities in liver function tests improved in nearly all patients after treatment with Artelum®.
New and recrudescent infections in adults and children
Data for a limited number of patients show that new and recrudescent infections can be treated with a second course of Artelum®.
Artelum® is contraindicated in:
– Hypersensitivity to Artemether, Lumefantrine or to any of the excipients of Artelum®).
– Patients with severe malaria according to WHO definition.
– First trimester of pregnancy.
– Patients with family history of cogenital prolongation of the Qtc interval or sudden death or with any other clinical condition known to prolong the QTc interval such as patients with a history of symptomatic cardiac arrythmias, with clinically relevant bradycardia or with severe cardiac disease.
– Patients with known disturbances of electrolyte balance e.g. Hypokalaemia or hypomagnesaemia.
– Patients taking any drug which is metabolized by the cytochrome enzymes CYP2D6 (e.g. Flecainide, metoprolol, imipramine, amitrityline, clomipramine).
– Patients taking drugs that are known to prolong the Qtc interval such as antarrhymics of classes 1A and III, neuroleptics, antidepressant agents, certain antibotics including some agents of the following classes: macrolides, fluoroquinolones, imidazole, and triazole antifungal agents, certain non-sedating antihistaminics (terfenadine, astemizole), cisapride.
SPECIAL WARNINGS AND PRECAUTIONS FOR USE
Artelum® has not been evaluated for prophylaxis and is therefore not indicated.
Artelum® has not been evaluated for the treatment of cerebral malaria or other severe manifestations of severe malaria including pulmonary oedema or renal failure.
Artelum® has not been studied for efficacy and safety in patients with severe hepatic or renal insufficiency and therefore no recommendations can be made for these groups of patients.
If a patient deteriorates whilst taking Artelum®, alternative treatment for malaria should be taken without delay. In such cases, monitoring of the ECG is recommended and steps should be taken to correct any electrolyte disturbances. The long elimination half-life of lumefantrine must be taken into account when administering quinine in patients previously treated with artelum®.
Artelum® is not indicated for, and has not been evaluated in, the treatment of malaria due to P. 0vale, although some patients in clinical studies had co-infections with P. Falciparum and P. Vivax at baseline. Artelum® is active against blood stages of plasmodium vivax, but is not active against hypozoites. Therefore, sequential treatment with primaquine should be used to achieve hypozoite eradication in case of co-infections with P. Vivax.
Patients who remain averse to food during treatment should be closely monitored as the risk of recrudescent may be greater.
In children and infants with bodyweight between 5 and 25kg, QTc prolongation of 30-60msecs was seen in up to 35% of treated subjects. In those suffering from dehydration and/or electrolyte imbalance, a minority of subjects (9%) showed QTc prolongation of >6Omsesc. It was not possible either to confirm or to rule out whether these changes were associated with the disease and its course, or with the use of Artelum®.
Interaction with other antimalarials: Data on safety and efficiency are limited, and Artelum® should therefore not be given concurrently with other antimalarials unless there is another treatment option. The long elimination half-life of lumefantrine must be taken into account when administering quinine in patients previously treated with Artelum®.
If Artelum® is given following administration of mefloquine or quinine, close monitoring of food intake (for mefloquine) or of ECG (for quinine) is advised. In patients previously treated with halofantrine, Artelum® should not be administered earlier than one month after last halofantrine dose. Caution is recommended when combining Artelum® with substrates, inhibitors or inducers of CYP3AA.
PREGNANCY AND LACTATION
Based on animal data, Artelum® is suspected to cause serious birth defects when administered during the first trimester of pregnancy. Reproductive toxicity studies with artermether have shown evidence of post implantation losses and teratogenicity in rats. Artelum® treatment is contraindicated during the first trimester of pregnancy. During the second and the third trimester, treatment should only be considered if the expected benefit to the mother outweighs the risk to the foetus.
Women of child- bearing potential
Artelum® is contraindicated in the first trimester of pregnancy, women should not conceive while on Artelum® treatment for malaria.
Animal data suggest excretion into breast milk but no data is available in humans. Breast-feeding women should not take Artelum® due to the long elimination half-life of lumefantrine (4 to 6 days), it is recommended that breast-feeding should not resume before day 28 unless potential benefits to mother and child outweigh the risks of Artelum® treatment.
In cases of suspected overdosage, symptomatic and supportive therapy should be given as appropriate. ECG and blood potassium should be monitored.
See box folding.
Artelum® should not be used after the date marked ‘EXP” on the pack.
INSTRUCTIONS FOR USE AND HANDLING
Note: Artelum should be kept out of the reach and sight of children.
Artelum® 40mg and 240mg tablets by 12’s.
May & Baker Nigeria PLC
315, Sapara Street, Industrial Estate,
P.M.B. 21049, Ikeja, Nigeria.