Artesiane 80 Artemether Injection

ARTESIANE® 80
Artemether 80mg/ml

 
Presentation

ARTEMETHER 80 mg/ml ampoules. Box of 5 ampoules of 1ml containing Artemether 80mg/ml in fractionated coconut oil. Sterile and colourless solution.

 
Indications

ARTEMETHER 80 mg/ml is indicated for the treatment of malaria caused by all species of Plasmodium, including severe malaria caused by multiple drug resistant strains of Plasmodium falciparum.

 

Dosage and administration

The dosage depends on the severity of the case and the clinical state of the patient. Formulations for intramuscular injection of Artemether are mostly used in case of severe malaria, such as cerebral malaria, but also in case of patients showing gastrointestinal problems.

Loading dose for adults and children: 3.2 mg/kg body weight administered as a single intramuscular injection on the first day.

Maintenance dose for adults and children: 1.6 mg/kg/day administered as intramuscular injection once a day during the following four days.

Maintenance treatment can also be continued by oral Artemisinin-based combination therapy (ACT) if the patient’s condition does not require injections.

The drug is given by intramuscular injection in the gluteal muscle or the quadriceps. Combination of other drugs in the same syringe should be avoided. Aseptic conditions must be respected when injecting Artemether.

 
Note

a) A full course therapy of five days is essential in order to avoid recrudescence.

b) In case of 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.

 
Precautions and Contra-indications

Artemether 80 mg/ml is indicated for use in children and adults.

There is no known contra-indication for the use of Artemether in the treatment of malaria. The use of Artemether should be avoided during pregnancy, particularly during the first trimester.

Drug interactions: specific drug interactions were not observed. Artemether potentialises the antimalarial activity of other antimalarials.

 
Overdosage

Do not exceed the prescribed dose. A specific antidote is not known. The administration, of several times the therapeutic dose was not reported to cause serious adverse events. In case of accidental and severe overdose, symptomatic treatment in a specialized center is recommended.

 
Adverse events

Adverse events were usually not reported with the recommended dose. Laboratory abnormalities such as increase in transaminases and decrease in reticulocyte count are rare and transient and usually without clinical manifestations. A decrease in sinus frequency without changes in the electrocardiogram has also been reported. At high doses, transient abdominal pain, tinnitus and diarrhea have been described.

 
Resistance and recrudescence

Resistance of Plasmodium to Artemether has not been observed. Resistance is unlikely to occur in view of the specific mechanism of action of Artemether which is very cytotoxic for the Plasmodia (opening of a peroxide bridge). An apparent resistance is sometimes seen but it 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 complete new treatment of 5 days is recommended.

 
Pharmacological properties

PHARMACODYNAMICS: Artemether acts essentially as a blood schizonticide. The presence of the endoperoxide bridge (generating singlet oxygen and free radicals) appears to be essential for the antimalarial activity. Inhibition of protein synthesis as the basic mechanism of action was suggested in studies showing morphological changes in ribosomes as well as in the endoplasmic reticulum. Morphological changes of the parasitic membranes induced by Artemether have been described, being the result of free radical action and of the oxidative effect caused by the opening of the peroxide group. Other in vitro tests suggest that Artemether causes a marked diminution of nucleic acid synthesis.

Recent studies using electronic microscopy showed rupture of membrane structures of the parasites, leading to destruction of the parasite within a few hours.

PHARMACOKINETICS: intramuscular Artemether is rapidly absorbed, reaching therapeutic levels within the first hour and C-max within 4 – 9 hours, Artemether is metabolized in the liver to the demethylated derivative dihydroartemisinin. The elimination is rapid with a T½ of about 1 – 3 hours. Dihydroartemisinin, being a potent antimalarial itself, has a T½ of about 1 – 3 hours. The degree of binding to plasma proteins varied markedly according to the studied species, but it is about 50% in man. The distribution of radioactive marked Artemether was found to be equal between cells and plasma.

Breastfeeding: data on excretion in breastmilk are not available.

 
Pharmaceutical precautions

Artemether 80mg/ml ampoules should be stored at room temperature and protected from light.

Under these conditions, the ampoules have a shelf life of 4 years.

 
License holder

Dafra Pharma Ltd., Amplak Plaza, Plot 3, Otunba Jobi – Fele Way,

CBD Alausa, Ikeja, Lagos – NIGERIA

Nafdac Reg. No.: 04-8257

 
Manufacturer

ROTEXMEDICA GmbH, Bunsenstrasse 4, 22946 Trittau, GERMANY

 

Date
February 2010

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