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| Product name | Lumefantrine |
| Synonyms | Benflumetol, CGP 56695, 9H-Fluorene-4-methanol,82186-77-4 |
| Brands containing Lumefantrine | Coartem, Riamet |
| CAS number | 82186-77-4 |
| Molecular formula (MF) | C30H32NOCl3 |
| Molecular Weigt (MW) | 528.95 |
| Benefits | antimalaria Combination with other drugs |
What is Lumefantrine?
Lumefantrine, also known as benflumetol before, is an antimalarial drug used only in combination with artemether. Lumefantrine was synthesized originally by the Academy of Military Medical Sciences in Beijing, China. It is a racemic fluorine derivative with the chemical name 2-dibutylamino-1-[2,7-dichloro-9-(4-chlorobenzylidene)-9H-fluoren-4-yl]-ethanol. It conforms structurally, physicochemically, and in mode of action to the aryl amino alcohol group of antimalarial agents including quinine, mefloquine, and halofantrine. Preliminary studies of the pharmacokinetic properties of lumefantrine are reminiscent of those of halofantrine, with variable oral bioavailability (augmented considerably by fats), a large apparentvolume of distribution, and a terminal elimination half-life for malaria estimated initially at approximately 4 to 5 days. A four-dose regimen of artemether-lumefantrine has proved highly effective in studies conducted in Africa, India, and China, but in Thailand, which harbors the most drug-resistant Plasmodium falciparum in the world, cure rates were inferior to those seen with the 3-day artesunate-mefloquine combination. Previous studies had suggested that the area under the plasma lumefantrine concentration-time curve was the principal determinant of cure, and it was predicted that an increase in dose should improve efficacy. These earlier studies also suggested an increase in oral bioavailability with time but were confined to only four dose schedules. When we talk about lumefantrine, we always have to think about artemether first. The term "co-artemether" is sometimes used to describe this combination.
The combination of the artemisinin derivative artemetherand lumefantrine (previously called benflumetol) in a 1:6 ratio is a new, effective, and well-tolerated antimalarial therapy. Trials, first in China (where the drugs were discovered) and subsequently in Asia and Africa, have shown that this combination is active even against multidrug-resistant falciparum malaria and is associated with no serious toxicity.
Both artemether and lumefantrine are blood schizontocides. The antimalarial activity of artemether (and its active metabolite) is attributed to endoperoxide moiety. The exact mechanism of action of lumefantrine is not well defined; it may inhibit the formation of beta-hematin by forming a complex with hemin. Both artemether and lumefantrine inhibit nucleic acid and protein synthesis.
The individual drugs were both initially developed in China. Artemether is one of the semi-synthetic derivatives of artemisinin, and lumefantrine is purely synthetic. The combination is an effective and well-tolerated malaria treatment, providing high cure rates even in areas of multi-drug resistance.
In 2001, Coartem became the first fixed dose artemisinin-based combination therapy to meet the World Health Organization's (WHO) pre-qualification criteria for efficacy, safety and quality. In 2002, artemether/lumefantrine tablets were added to the WHO's Essential Medicines list, an index of essential drugs which help guide the purchasing decisions of Member States and UN agencies. Coartem is approved in over 80 countries worldwide, including various countries in Africa, as well as Swissmedic, the European Medicines Agency (EMA) and the U.S. Food and Drug Administration (FDA).
Pharmacokinetics of artemether
After oral administration, artemether peak plasma concentrations are reached after about 2 hours. Concomitant intake of a high fat meal enhances the absorption of artemether, resulting in an increase in the relative bioavailability by more than 2-fold. Artemether is rapidly and extensively metabolized (substantial first pass metabolism) into its main active metabolite, dihydroartemisinin. This metabolite is further converted to inactive metabolites. Artemether and dihydroartemisinin are rapidly cleared from plasma with an elimination half-life of about 2 hours.
Pharmacokinetics of lumefantrine
After oral administration of lumefantrine, peak plasma concentrations are observed after about 6 – 8 hours. Concomitant intake of a high fat meal enhances the absorption of lumefantrine, resulting in an increase in the relative bioavailability by more than 16-fold. In patients with malaria, this increase was only 2-fold, probably due to the lower fat content of the food ingested by acutely ill patients. Patients should therefore be encouraged to take the medication with a normal diet as soon as food can be tolerated.
Lumefantrine is metabolised into the active desbutyl-lumefantrine, however, the systemic exposure to this metabolite is low. Lumefantrine is eliminated very slowly with a terminal half-life of 2-3 days in healthy volunteers and 4-6 days in patients with falciparum malaria.
Mechanism of Action of artemether and lumefantrine
Coartem Tablets, a fixed ratio of 1:6 parts of artemether and lumefantrine, respectively, is an antimalarial agent. Artemether and lumefantrine work by interfering with the growth of parasites in the red blood cells of the human body. Parasites that cause malaria typically enter the body through the bite of a mosquito. Malaria is common in areas such as Africa, South America, and Southern Asia. The combination of artemether and lumefantrine is used to treat non-severe malaria. This medication is used only to treat malaria. Artemether is rapidly metabolized into an active metabolite dihydroartemisinin (DHA). The antimalarial activity of artemether and DHA has been attributed to endoperoxide moiety. The exact mechanism by which lumefantrine, exerts its antimalarial effect is not well defined. Available data suggest lumefantrine inhibits the formation of -hematin by forming a complex with hemin. Both artemether and lumefantrine were shown to inhibit nucleic acid and protein synthesis.
Side effects of taking lumefantrine-containing drugs
Coartem can cause anaphylactic reactions. The drug frequently causes headache, dizziness and anorexia, although mild forms in most cases. Other fairly common side effects (more than 3% of patients) include sleep disorder, tinnitus, tremor, palpitation, as well as unspecific reactions likevertigo, gastrointestinal disorders, itch and nasopharyngitis
What is Artemether-lumefantrine?
Do not use artemether and lumefantrine to prevent malaria. Artemether and lumefantrine may also be used for other purposes not listed in this medication guide.
How should I take Artemether-lumefantrine?
Take this medication exactly as it was prescribed for you. Do not take the medication in larger amounts, or take it for longer than recommended by your doctor. Follow the directions on your prescription label.
Take artemether and lumefantrine with food, milk, oatmeal, or broth. The tablet may be crushed and mixed with 1 or 2 teaspoons of water for easier swallowing. You may also mix a crushed tablet with infant pudding when giving this medication to a child.
Start eating normally as soon as possible to help your body better absorb the medication.
If you vomit within 1 to 2 hours after taking this medication, take another dose. If your vomiting continues or you cannot eat, call your doctor.
Artemether and lumefantrine is usually given as a total of 6 doses over a period of 3 days. Carefully follow your doctor's instructions about how many tablets to take per dose. Artemether and lumefantrine doses are based on weight and age. The usual doses are as follows, unless your doctor tells you otherwise.