Artemether and lumefantrine are mainly available and taken orally in the form of tablets. The tablets are usually taken twice daily for three days with the first dose being taken as soon as malaria is diagnosed. The normal dosing calendar is stated below:
- Day 1: Artemether-lumefantrine 1 tablet every 12 hours; morning and evening.
- Day 2: One tablet plus every 12 hours.
- Day 3: One tablet every 12 hours.
Note: The tablets must be taken with food (preferably a fatty meal) so as to enhance the absorption of the drugs more so lumefantrine.
Dosage Shelf Guides (For Adults and Children):
- For weight ≥35kg, Adult Wafer (20mg Artemether + 120mg Lumefantrine) for every 12 hourly for 3 days.
• For children; The dosage modification is on the weight of the child. Correct dosages have pediatric formulations.
The treatment associated with artemether and lumefantrine is positively impacted by the synergistic effect of both of the agents:
- Artemether: The drug exhibits rapid absorption rates and quick destructive action due to the formation of free radicals that destroy cellular components of the malaria-causing pathogen and lead it to death, particularly the early blood stages of the parasite.
- Lumefantrine: The action of this agent develops slowly and lasts much longer than the action of artemether. It is directed primarily on the inhibition of the malaria parasite’s ability to metabolize food, which in this case is hemoglobin, the protein necessary for the existence of the malarial organism.
Mordant also does not allow a relapse to occur as it takes care of remaining parasites afte rartemether has done away with majority of the parasites
There are generally few concerns regarding artemether and lumefantrine usage in humans, however, some side effects do occur in certain populations.
Some of the most commonly seen include
:
- Gastrointestinal Effects: These are commonly nausea, vomiting, pain and diarrhea. Eating food may help in alleviating such effects when taking the drug.
- Headache: Some individuals may get slight to moderate head pain during the course of medication
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- Dizziness: There is also a possibility of dizziness or light-headedness, again, especially while getting up too quickly.
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- Heart effects: There are effects of artemether and lumefantrine that involve prolonged QT interval which is an alteration in the electrical depolarization of the heart rhythm and may cause the patient to have arrhythmias. Such patients especially those with heart arrhythmia and electrolyte imbalance are advised to be careful.
- Rash: In allergic reactions sometimes a rash and itchy skin develops.
Management of side effects in patients may be less often than that of those mentioned above but may include:
• Hepatic impairment: Some patients may experience elevating of liver enzymes which is rare, but in the instance of taking the medicine for a longer course, such case needs monitoring.
- Underlying Cardiac Disease: In addition to the above, QT intervals may also be further prolonged by this medication in individuals with previous arrhythmias, heart failure, or in those with an electrolyte imbalance, such as low potassium/magnesium levels.
Pregnancy: The U.S. FDA classifies artemether and lumefantrine as Category C, which implies that there are animal studies that show risks to the fetus, but very few human studies. It should, therefore, be taken during pregnancy only when the advantages surpass the risks involved, and there are no alternative medications that can be given.
Breastfeeding: Since both artemether and lumefantrine easily get into breast milk, it is advisable for breastfeeding mothers to seek medical advice before commencing the combination therapy.
CYP450 Enzyme Inhibitors/Inducers:
CYP3A4 inhibitors (ketoconazole, ritonavir): May increase the plasma concentration of lumefantrine, which may enhance the risk of side effects.
CYP3A4 inducers (rifampicin, phenytoin): May decrease the concentration of lumefantrine, which may reduce the effectiveness of the treatment.
Antimalarial Drugs:
Quinine: Co-administration of artemether-lumefantrine with quinine or quinine-based therapies may increase the risk of adverse effects, such as QT prolongation and cardiac toxicity.
Anticonvulsants:
Phenytoin and carbamazepine might decrease the artemether-lumefantrine activity because they can induce the drug-metabolizing enzyme which accelerates metabolism.
Anticoagulants:
Warfarin: Treatment with artemether-lumefantrine can cause an effect in warfarin’s anticoagulant profile, with higher risk for bleeding. Patients’ INR values should be followed closely.
Other Medications:
Mefloquine: Co-administration of mefloquine with artemether-lumefantrine increases the risk of adverse events, such as CNS toxicity or severe dizziness. The combination should be avoided whenever possible.
Dosing regimens for the combination of artemether and lumefantrine for uncomplicated malaria is:
- Adults and children ≥ 35 kg: 1 tablet every 12 hours for 3 days.
• Children < 35 kg: the Pediatric artemether-lumefantrine offers weighted specific dosages per age.
In many countries, Artemether and lumefantrine (Coartem) is available on a prescription only. The diagnosing and treating physician who identifies that the patient has malaria in which this combination therapy is appropriate should be the one to prescribe this therapy.