Ar

Ar Uses, Dosage, Side Effects, Food Interaction and all others data.

This formulation contains a fixed ratio of 1 : 6 parts of Artemether and Lumefantrine. The site of antiparasitic action of both components is the food vacuole of the malarial parasite, where they are thought to interfere with the conversion of haem, a toxic intermediate produced during haemoglobin breakdown, to the non-toxic haemozoin (malaria pigment). Lumefantrine is thought to interfere with the polymerisation process, while Artemether generates reactive metabolites as a result of the interaction between its peroxide bridge and haem iron. Both Artemether and Lumefantrine have a secondary action involving inhibition of nucleic acid and protein synthesis within the malarial parasite.

Trade Name Ar
Generic Artemether + Lumefantrine
Type L Tablet, Gel, Injection
Therapeutic Class Anti-malarial drugs
Manufacturer American Biocare, Tetramed Biotek Pvt Ltd
Available Country India
Last Updated: September 19, 2023 at 7:00 am
Ar
Ar

Uses

Artemether-Lumefantrine is used for the treatment of adults, children and infants with acute, uncomplicated infections due to Plasmodium falciparum or mixed infections including P. falciparum. Because this combination 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.

Stand-by emergency treatment: Prescribers are advised to issue Artemether-Lumefantrine combination (to be carried for self-administration) to those tourists and business travelers who are considered to be non-immune and may be unable to obtain medical care within 24 hours of the onset of symptoms of malaria.

Ar is also used to associated treatment for these conditions: Plasmodium Infections, Acute, uncomplicated Malaria caused by plasmodium falciparumUncomplicated Malaria caused by Plasmodium falciparum

How Ar works

Involves an interaction with ferriprotoporphyrin IX (“heme”), or ferrous ions, in the acidic parasite food vacuole, which results in the generation of cytotoxic radical species.

The generally accepted mechanism of action of peroxide antimalarials involves interaction of the peroxide-containing drug with heme, a hemoglobin degradation byproduct, derived from proteolysis of hemoglobin. This interaction is believed to result in the formation of a range of potentially toxic oxygen and carbon-centered radicals.

The exact mechanism by which lumefantrine exerts its antimalarial effect is unknown. However, available data suggest that lumefantrine inhibits the formation of β-hematin by forming a complex with hemin and inhibits nucleic acid and protein synthesis.

Dosage

Ar dosage

The treatment should be administered at the time of initial diagnosis or at onset of symptoms. This combination should be taken with food or drinks rich in fat (such as milk). The treatment schedule is as follows:Patient TypeFrist daySecond dayThird day

Children (weighing 5 kg to less than 15 kg)

1 tablet at the time of initial diagnosis, 1 tablet again after 8 hours

1 tablet twice daily (morning and evening)

1 tablet twice daily (morning and evening)

Children (weighing 15 kg to less than 25 kg and 12 years of age or less)

2 tablets as a single dose at the time of initial diagnosis, 2 tablets again after 8 hours

2 tablets twice daily (morning and evening)

2 tablets twice daily (morning and evening)

Children (weighing 25 kg to less than 35 kg and 12 years of age or less)

3 tablets as a single dose at the time of initial diagnosis, 3 tablets again after 8 hours

3 tablets twice daily (morning and evening)

3 tablets twice daily (morning and evening)

Adults and children (weighing 35 kg and above or more than 12 years of age)

4 tablets as a single dose at the time of initial diagnosis, 4 tablets again after 8 hours

4 tablets twice daily (morning and evening)

4 tablets twice daily (morning and evening)

Side Effects

This formulation is generally well tolerated. However, few side effects such as anorexia, headache, dizziness, sleep disorder, palpitation, pruritus, rash, abdominal pain, nausea and vomiting have been reported.

Toxicity

Animal studies on acute toxicity show that the LD50 of Artemether in mice is a single i.g. administration of 895mg/kg and a single i.m. injection of 296mg/kg dose; in rats, the LD50 is a single i.m. injection of 597mg/kg dose.

Common side effects of combination artemether/lumefantrine therapy in adults include headache, anorexia, dizziness, and asthenia. Common side effects in children include pyrexia, cough, vomiting, anorexia, and headache. Possible serious adverse effects include QT prolongation, bullous eruption, urticaria, splenomegaly (9%), hepatomegaly (adults, 9%; children, 6%), hypersensitivty reaction, and angioedema.

Precaution

If a patient deteriorates whilst taking this combination, alternative treatment for malaria should be started without delay. The long elimination half-life of Lumefantrine must be taken into account when administering quinine in patients previously treated with this combination. This combination has not been evaluated for: prophylaxis; treatment of cerebral malaria; treatment of severe malaria including pulmonary oedema or renal failure; treatment of malaria due to P. vivax, P. malariae or P. ovale.

Interaction

Dose adjustment of this combination is considered unnecessary when administered in association with ketoconazole. The likelihood of interactions with other drugs is minimal in view of its short duration of administration and wide therapeutic index. From study it was found that, the risk of QTc-prolongation associated with IV quinine was enhanced by prior administration of this combination.

Elimination Route

Food increases absorption.

Food increases absorption.

Half Life

Artemether, 1.6 +/- 0.7 and 2.2 +/- 1.9 hr; Dihydroartemisinin, 1.6 +/- 0.6 and 2.2 +/- 1.5 hr

~ 4.5 days

Pregnancy & Breastfeeding use

Pregnancy: Based on animal data, this combination is suspected to cause serious birth defects during the first trimester of pregnancy. Artemether has demonstrated teratogenic potential with an increased risk during early gestation. This combination 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.

Lactation: Breast-feeding women should not take Artemether-Lumefantrine combination.

Contraindication

Hypersensitivity to any of the ingredients or excipients; Patients with severe malaria according to WHO definition; First trimester of pregnancy; Patients with a family history of congenital 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 disturbance of electrolyte balance e.g. hypokalaemia or hypomagnesemia; Patients taking any drug which is metabolized by the cytochrome enzyme CYP2D6 (e.g. flecainide, metoprolol, imipramine, amitriptyline, clomipramine).

Acute Overdose

In cases of suspected overdosage, symptomatic and supportive therapy should be given as appropriate. ECG and electrolytes (e.g. potassium) should be monitored.

Interaction with other Medicine

Dose adjustment of Artemether-Lumefantrine is considered unnecessary when administered in association with ketoconazole. The likelihood of interactions with other drugs is minimal in view of its short duration of administration and wide therapeutic index. From study it was found that, the risk of QTc-prolongation associated with IV quinine was enhanced by prior administration of this combination.

Storage Condition

Keep out of the reach of children. Store in a cool and a dry place protected from light.

Innovators Monograph

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*** Taking medicines without doctor's advice can cause long-term problems.
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