The Effects Of Fatty Food On The Pharmacology Of Artemether/Lumenfantrine

Malaria treatment with Artemether/Lumefantrine

Many persons fail to heed the counsel of pharmacist as to how to take their medications. Take, for instance, the malaria drug artemether/lumefantrine is advised to be used with fatty food. Very few people really do keep to this kind of information.

The good news is that majority of local food content contains the quantity needed to achieve this.

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However, you may still want to know the rationale behind this. Let us take a dive into the life cycle of the malaria parasite. The good news is that majority of local food content contains the quantity needed to achieve this. However, you may still want to know the rationale behind this. Let us take a dive into the life cycle of the malaria parasite.

Malaria is a major cause of death and morbidity worldwide. Nigeria is not an exception. The majority of malaria infection in Nigeria arise from the parasite, Plasmodium falciparum. However, the other species still have their own share of infection.

Life Cycle Of Malaria Plasmodium Falciparum

The life cycle starts from the female Anopheles mosquito. This is known as the sexual stage. A bite from the mosquito sends Plasmodium sporozoites into the body through the mosquito saliva. The number could range from 20 – 200. However, very few get to the next stage as the immune system clears the majority of them. These migrate into the liver instantly in less than 30 minutes. Inside the liver, they infect hepatocytes cells. This is known as the asexual stage. They can live here between 5 – 14 days. Inside this cell, it multiplies rapidly and then differentiates into schizonts. This schizont is like a ball. Inside the balls are Plasmodium cells now known as merozoites. However, not all develop into merozoites as others develop into gametophytes and matures within 7 – 15 days. Once these schizonts are release from the liver, it burst open. A schizont may contain between 16 – 18 merozoites. The schizont release is so much that the total number of merozoites will amount to about 90,000. However, gametophytes will remain in the blood stream for the mosquito to suck up while feeding.

These merozoites will in less than a minute invade the Red Blood Cells (R.B.C). They end up replicating using up part of the RBC. This leads to the destruction of the structure of the RBC. At the end of about some hours, the RBC rupture releasing merozoites, which will further enter other healthy RBC and the cycle, continues. The time of rupture leads to the manifestation of signs and symptoms of malaria parasite due to loss of function of RBC.

This whole cycle is about 36 – 48 hours. The signs and symptoms of malaria start as from the 10^th day and can be detected in the blood at this time. The liver phase occurs just once during infection while the RBC phase occurs multiple times. Since the rate of growth is constant, the rupture of RBC falls into a particular period every time it occurs. This is while symptoms occur during a particular time of the day for sufferers. Since the life cycle is about 48 hours, signs and symptoms occur almost every evening. This especially true when the person suffers from multiple bites from an infected mosquito.

Treatment Of Malaria Parasite

There are several treatment options from malaria. However, the recommended drug for use in Africa is the Artemeter Combination Therapy (A.C.T). This could be attributed to the success stories recorded so far based on the effect on the parasite with fewer side effects.

One of the popular combination therapy is the Arteeter/lumefantrine. It is a fixed dosed combination therapy with a ratio of 1:6.

Artemether interferes with parasite transport protein, produce disruption of mitochondrial function, inhibits angiogenesis, and modulates host immune function. It is rapidly absorbed into the body in less than 2 hours after oral administration reaching its peak plasma concentration in 2 – 3 hours. However, the bad news is that it has a half-life of 2 – 3 hours. What this means is that it clears those parasites in the blood stream at that time. Now for those that are still inside the RBC, they will escape the effect of the drug. When they burst from the RBC, they are free to invade other RBC. Then comes lumefantrine.

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Lumefantrine interferes with the conversion of heme, the toxic chemical the parasite used to destroy RBC to non-toxic hemoin. Accumulation of this leads to parasite death.

Lumefantrine is absorbed in 2 hours after oral administration. It reaches its peak plasma concentration in 3 – 4 hours. The good news is that its half-life is up to 3 – 6 days. This half-life is the reason while the remaining parasites that will come out from the RBC will be cleared of the system.

However, in the beginning of the post, we talked about how fatty foods enhanced the effects of Artemether/lumefantrine. Here is the catch. Fatty foods from experiments enhanced the oral absorption of artemether twice while lumefantrine by 16 times. That means that the drug when fully absorbed will produce mark therapeutic effects. However, there is another school of thought that believed that the food also delays the absorption of the lumefantrine. This delayed absorption will kind of space the time the effects of the two drugs will take effects in the body. This will then provide complete double protection to the body while destroying the parasite.

Effect of Fatty Food On Artemether/Lumefantrine

If the two drugs are absorbed equally and reach peak plasma concentration at the same time, dosing would have increased leading to adherence problems. Another thing is that a lot of patients suffering from malaria do not have an appetite for food making them skip the food. This practice is very bad and can reduce the therapeutic effect of the drug a lot. 

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