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Artesiane 80, 20 & Suppogel

Reals Pharmaceuticals Limited
Plot 1 Junaid Dosunmu Street,Central Business District, Alausa, P.0. Box 3560 Ikeja, Lagos, Nigeria.
Email: reals@realsgroup.com
Tel: + 234-1-774-1205
Fax: +234-1-263-0919
Website: http://realsgroup.com

Brand Name

Artesiane 80, 20 & Suppogel

Manufacturer

Dafra Pharma nv/sa, Slachthuisstraat 30 Bus 7, 2300 Turnhout, Belgium.

Therapeutic Class

Antimalarial drugs

Dosage Form, Composition & NAFDAC Registration Number (NRN)

Injection (NRN: 04-8257): Clear glass ampoules containing 80 mg of Artemether in a 1 mL solution of frationated coconut oil. The solution is sterile and colourless.

Pack size: Each pack contains 5 ampoules of Artemether 80 mg/mL.

 

Injection (NRN: 04-8240): Clear glass ampoules containing 20 mg of Artemether in a 1 mL solution of frationated coconut oil. The solution is sterile and colourless.

Pack size: Each pack contains 10 ampoules of Artemether 20 mg/mL.

 

Suppogel (NRN: 04-8258): Artemether 40 mg.

Pack size: 6’s.

Pharmacology

Pharmacodynamics: Artemether is a typical blood schizonticide. Artemether has a peroxide bond releasing inside the parasite singlet oxygen as well as free radicals. Both exert a direct cytotoxic effect on the cells. This forms the essential part of the mechanism of action of Artemether and explains its rapid effect as well as its efficacy.

Pharmacokinetics: Intramuscular Artemether is rapidly absorbed, reaching therapeutic levels within the first hour. Cmax is obtained within 4-6 hours. It is metabolized in the liver to the demethylated derivative dihydroartemisinin. The elimination is rapid, with a T½ of 1-3 hours. Dihydroartemisinin, being a potent antimalarial itself, has a similar T½.

The degree of binding to plasma proteins varied markedly according to the species studied. The binding of Artemether with plasma protein is of the order of 50% - distribution of radioactive labelled Artemether was found to be equal between cells and plasma.

Resistance and recrudescence: Resistance of Plasmodia to artemether has not been observed. It is also unlikely to occur in view of the specific mechanism of action which is very cytotoxic for the Plasmodia (opening of a peroxide bridge). An apparent resistance is sometimes seen but is mainly due to multiple broods of Plasmodia developing at different times in the same patient. In controlled studies, recrudescence does not exceed 3%. In case of recrudescence (real or apparent), a new complete treatment for five days is advisable.

Indications

Artemether is indicated for the treatment of malaria caused by all forms of Plasmodium including severe malaria caused by multiple drug resistant strains of P. falciparum.

In case of an infection caused by P.vivax recrudescence is common. A combination treatment with Primaquine is recommended.

Contra-indications

Pregnancy: It is advisable not to use drugs during pregnancy. In view of the high risk of malaria during pregnancy for mother and foetus, the responsible physician may consider it essential, as in the case of cerebral malaria, to treat a pregnant woman. Artemisinin derivatives like Artemether are the fastest acting schizontocides and rapid clearance of parasites is essential.

Breast-feeding: Data on excretion in breastmilk are not available, but the metabolites DHA may be found.

Precautions/Warnings

Do not exceed the prescribed dose. In case of overdosage, symptomatic treatment in a specialized unit is recommended.

The administration of several times the therapeutic dose was not reported to give serious side effects.

Interactions

Specific untoward drug interactions have not been found.

Potentiation of other antimalarial drugs is a common feature. Loading dose of Artemether followed by other antimalarial drugs have shown to potentiate each other.

Adverse Effects

At the therapeutic dose, there are very few side effects. There are reports of laboratory abnormalities, ie a decrease in reticulocyte count, a transient increase in transaminases and ECG changes (lowering of sinus heart rate, but effects on conduction or on repolarisation have not been observed).

At high doses, transient abdominal pain, diarrhoea and tinnitus were reported.

Dosage & Administration

Artesiane 80

Adults: Optimal results have been obtained when Artemether is administered in doses of 160 to 320 mg as a loading dose the first day of treatment. This should be followed by additional injection of one to two ampoules per day during the following four days as a maintenance dose. However, treatment can also be continued by oral therapy with one of the Artemisinine derivatives like Artesunate tablets, if the patient’s condition does not require injections.

Artesiane 20

Children: Optimal results have been obtained when Artemether is administered as a loading dose of 3.2 mg/kg on day one and 1.6 mg/kg for the next 4 days as a maintenance dose. For the maintenance treatment, oral formulations should be considered when the clinical condition permits.

Artesiane Suppogel (Children and babies): 4 mg/kg body-weight

Weight of child Total dose Daily Dose (# of Suppogels)
Day-1 Day-2 Day-3 Day-4 Day-5
5-9 kg 20-36 mg 1 1 1 1 1
10-19 kg 40-76 mg 2 1 1 1 1
20-29 kg 80-116 kg 3 2 2 2 2

Note: A full course therapy of five days is essential in order to avoid recrudescence. In severe malaria it may be necessary to increase the loading dose and to prolong treatment for seven days if parasitaemia is not cleared during the first few days.

Storage/Handling Recommendations

Artemether ampoules should be protected from light and stored at room temperature below 30oC.

Shelf life is 4 years.

Review Date

2015-11-19 03:17:15