Lokmal Composition, Use, Dose, Side Effect

Lokmal is another product from the stables of emzor pharmaceutical industries limited, Nigeria. It is an antimalarial containing two active ingredients. It comes in a dispersible tablet, suspension, forte and by 24.

Lokmal

Composition Of Lokmal

Composition Of Lokmal Dispersible (6) Tablet

Each dispersible tablet contains:

Artemether 20 mg plus lumefantrine 120 mg

Composition Of Lokmal Oral Pediatric Suspension (60 ml)

Each 5 ml contains:

Artemether 20 mg plus lumefantrine 120 mg

Composition Of Lokmal (24) Tablet

Each tablet contains:

Artemether 20 mg plus lumefantrine 120 mg

Composition Of Lokmal QS Caplet

Each caplet contains:

Artemether 80 mg plus lumefantrine 480 mg

Composition Of Emzor Paracetamol

Each tablet contains:

Paracetamol 500 mg

Pharmacological Action

Artemether: is a semisynthetic chiral acetal derivative of artemisinin. It interferes with parasite transport proteins, produces disruption of mitochondrial function, inhibits angiogenesis, and modulates host immune function. Artemether and its active metabolite have been estimated to reduce parasite biomass by approximately 10,000-fold per reproductive cycle (every 2 days).

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Lumefantrine: is a racemic mixture of a synthetic fluorine derivative and is structurally related to guanine, mefloquine, and halofantrine. It interferes with the conversion of heme, the toxic intermediate step produced during hemoglobin break-down, to non-toxic hemozoin. Accumulation of heme and free radicals results in parasite death.

Artemether, like other artemisinin derived compounds, acts quickly to rapidly reduce the parasite burden, while lumefantrine serves as a longer acting agent to eliminate remaining parasites. The combination is effective in strains known to be resistant to traditional antimalarials such as chloroquine, and can be used for infections acquired in areas known to have parasites that are multidrug-resistant.

The mechanism of action of paracetamol is believed to be inhibition of cyclooxygenase (COX), with a predominant effect on COX-2. Inhibition of COX enzymes prevent the metabolism of arachidonic acid to prostaglandin H2, an unstable intermediate byproduct which is converted to pro-inflammatory compounds.

In the central system, inhibition of COX enzymes reduces concentrations of prostaglandin E2, which lowers the hypothalamic set point to reduce fever, and activation of descending inhibitory serotonergic pathways to produce analgesia.

Indications Of Lokmal

Lokmal is indicated for the treatment of malaria in children and adults caused by all forms of plasmodium including severe malaria caused by multiple drug resistant strains of P. falciparum.

Indication Of Paracetamol Tablet

Paracetamol is indicated for the relief of pain, headache and feverish conditions.

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Pharmaceutical Precautions And Contraindications

Lokmal is contraindicated in individuals who are hypersensitive to artemether and lumefantrine and in the first trimester of pregnancy, except otherwise prescribed by a physician.

Due to the long elimination of half-life of lumefantrine, it is recommended that breastfeeding should not start until at least one week after stopping artemether/lumefantrine combination treatment.

Drug Interactions

Specific negative drug-drug interaction was not seen. Artemether potentiates the antimalarials. Grapefruit is known to reduce the absorption and metabolism of Artemether/lumefantrine.

Side Effect Of Lokmal

With Artemether, visually no side effects have been reported. Laboratory abnormalities such as slight rise in transaminases and a decrease in reticulocyte count are rare and transient. A reasonable period should be taken into account before starting a treatment with lumefantrine combinations. Other common side effects may occur such as insomnia, nausea, vomiting, diarrhea, coughing and there may be need for medical attention if persistent.

Resistance And Recrudescence

Resistance of plasmodium to artemether has not been observed. An apparent resistance is sometimes seen but it's mainly due to multiple broods of plasmodia developing at different times in the same patient. In controlled studies, recrudescence does not exceed 10%. In case of recrudescence, (real or apparent) a new complete treatment for 3 days is advisable.

Pregnancy And Lactation

Lokmal is contraindicated in the first trimester of pregnancy and should only be given in the second and third trimester of pregnancy with a medical doctor's prescription if the benefits outweigh the potential risk. Due to the long elimination of half-life of lumefantrine, it is recommended that breastfeeding mothers should not start until at least one week after stopping lokmal combination treatments.

Dosage And Treatment Of Lokmal

Lokmal Dispersible Tablet Dose

5-15 kg (1-3 years): 1 tablet in the morning, second tablet 8 hours later, third tablet 24 hours and another at 36 hours and the fifth tablet at 48 hours and the last tablet at 60 hours.

Lokmal Oral Pediatric Suspension Dose

5-14 kg (6 months-3 years): 5 ml in the morning, another 5 ml 8 hours later, third dose of 5 ml at 24 hours and another 5 ml at 36 hours and the fifth 5 ml at 48 hours and the last 5 ml at 60 hours.

15-25 kg (4-8 years): 10 ml in the morning, another 10 ml 8 hours later, third dose of 10 ml at 24 hours and another 10 ml at 36 hours and the fifth 10 ml at 48 hours and the last 10 ml at 60 hours.

Lokmal Tablet (24) Dose

15-25 kg (4-8 years): 2 tablets in the morning, another 2 tablets 8 hours later, and yet another 2 tablets 24 hours and another 2 tablets at 36 hours and the fifth dose of 2 tablets at 48 hours and the last 2 tablets at 60 hours.

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25-35 kg (9-13 years): 3 tablets in the morning, another 3 tablets 8 hours later, and yet another 3 tablets 24 hours and another 3 tablets at 36 hours and the fifth dose of 3 tablets at 48 hours and the last 3 tablets at 60 hours.

Adults and children 35 kg (14 years) and above: 4 tablets in the morning, another 4 tablets 8 hours later, and yet another 4 tablets 24 hours and another 4 tablets at 36 hours and the fifth dose of 4 tablets at 48 hours and the last 4 tablets at 60 hours.

Lokmal QS Dose

Adults and children 35 kg (14 years) and above: 1 tablet in the morning and another 1 tablet 8 hours later. From the next day, 1 tablet morning and night for a complete 3 days.

Emzor Paracetamol Tablets Dose

Adult and children > 35kg (14 years and above): 

2 tablets (1000 mg) three times a day for two days.

Directions For Reconstitution

Suspension: to reconstitute the suspension, add about 45 ml of freshly boiled and cooled water to the powder in the bottle. Shake well until all the powder has dispersed; this makes 60 mL of the suspension.

Dispersible tablet: to reconstitute, place a single tablet in 5 ml of freshly boiled and cooled water. Mixed water and children on the tablet have dispersed.