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Co-Artesiane Suspension

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

Co-Artesiane Suspension

Manufacturer

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

Therapeutic Class

Antimalarial drugs

Dosage Form, Composition & NAFDAC Registration Number (NRN)

Suspension (NRN: 04-8765): Plastic vial containing Artemeter and Lumefantrine in a dry powder mixture for making up suspension with water. After adding water the solution becomes yellow and the product has a pleasant taste of coconut.

Each packaging carries a package leaflet and a graded beaker with marks at 5 mL intervals. One bottle contains 180 mg of beta-Artemether and 1080 mg of Lumefantrine for 60 mL suspension.

Pack size: Each cardboard box contains 1 bottle.

Pharmacology

drugs derived from artemisinin which is extracted from the plant Artemisia annua. Lumefantrine is a synthetic aryl amino alcohol similar to mefloquine and halofantrine.

Pharmacodynamics: Both components of Co-Artesiane have their own action site in the malarial parasites. The presence of the endoperoxide bridge in Artemether (generating singlet oxygen and free radicals, those are very cytotoxic to the Plasmodia) appears to be essential for antimalarial activity. Morphologic changes of the parasitic membranes induced by Artemether have been described, being the result of free-radical action.

Lumefantrine interferes more in the polymerisation processes. Other in vitro tests suggest that both cause a marked diminution of nucleic acid synthesis. Inhibition of protein synthesis as the basic mechanism of action is suggested in studies which showed morphological changes in ribosomes as well as in the endoplasmic reticulum. Although Artemether acts essentially as a blood schizonticide, Co-Artesiane did clear gametocytes in comparative clinical trials.

Pharmacokinetics: Orally administered Artemether is rapidly absorbed reaching therapeutic levels within 60-90 minutes. Artemether is metabolized in the liver to dihydroartemisinin (DHA). The elimination of artemether is rapid, with a T½ of 2-4 hours. Dihydroartemisinln, being a potent antimalarial itself has a T½ of about 2-4 hours. The degree of binding to plasma proteins varied markedly according to the species studied. The binding of artemether with plasma protein in amn is about 50%. Distribution of radioactive labelled Artemether was found to be equal between cells and plasma.

The absorption of Lumefantrine is highly influenced by lipids and food intake (from 10% by fasting to 100% at normal diet). Therefore, parents should be encouraged to give the medication with some fatty food as soon as it can be tolerated.

Lumefantrine is metabolised in human liver microsomes. The metabolite has 5 to 8 fold higher anti-parasitic effects than lumefantrine. Lumefantrine is found to be highly protein bound (95%). the elimination half-life in malaria-attaint patients will be 4 to 6 days. Lumefantrine and its metabolites are found in bile and faeces.

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 10%. In case of recrudescence (real or apparent) a new complete treatment for three days is advisable.

Indications

Co-Artesiane is indicated for the treatment of malaria in children, caused by all forms of Plasmodium including severe malaria caused by multiple drug resistant strains of P. falciparum.

Contra-indications

Co-artesiane is contra-indicated in individuals hypersensitive to any of the ingredients

Precautions/Warnings

No correlation has been found between QTc interval prolongation and plasma concentrations of lumefantrine. Caution is advised to patients who are taking drugs that are known to prolong the QT interval, such as certain antibiotics (macrolides, fluoroquinolones, imidazole) or who are predisposed to cardiac arrhythmias.

Pregnancy and lactation: 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.

Co-Artesiane should not be taken during breast-feeding. Due to the long elimination half-life of lumefantrine, it is recommend that breast-feeding should not start until at least one week after stopping an Artemether/lumefantrine combination treatment.

Children: There are no strict contra-indications for the use of Artemether in children. Co-Artesiane has been especially designed for paediatric use.

Interactions

Specific negative drug-drug interaction were not seen. Artemether potentiates the antimalarial activity of other antimalarials.

As grape fruits juice retards the metabolism of some antimalarials, it would be better not to drink grape fruit juice while taking Co-Artesiane.

Adverse Effects

With Artemether virtually no side effects have been seen. Laboratory abnormalities such as a slight rise in transaminases and a decrease in reticulocyte count are rare and transient. A lowering of sinus frequency without causing ECG changes has been noticed. At high doses transient abdominal pain, tinnitus and diarrhea have been described but a causal relationship is unclear.

Some antimalarials as halofantrine and quinine can influence the ECG pattern. Attention should be made to patients previously treated with those antimalarials. A reasonable period should be taken in account before to start a treatment with lumefantrine combinations.

Sometimes it could be possible that the following common side effects occur: rash, check this with your doctor. Other common side effects may occur: trouble of sleeping, nausea, vomiting, diarrhoea, coughing. They need medical attention when persisting.

Dosage & Administration

Co-Artesiane suspension has especially been designed for use in children up to 15 kg. The dose depends on the severity of the case and the clinical situation of the patient.  

In general: 4 mg Artemether/kg body weight per day, in combination with Lumefantrine.

This dose should be maintained during three consecutive days. The daily dose should be administered in one gift.

Note: A full course therapy for three dialysis essential in order to avoid recrudence. Vomiting within one hour requires repeating the dose.

Making up the Co-Artesiane suspension:

- Open the bottle by breaking the seal and add tap water of a good quality.

- Fill the bottle up to the 60 mL mark.

- Shake well until all the powder has disappeared from the bottom and the solution has become yellow.

 

- This should only take a few seconds. It may be necessary to add a little bit more water to readjust the volume  to 60 mL.

- The suspension is stable for 14 days. It is advisable to shake the bottle before each use.

Each subunit of 5 mL contains 15 mg Artemether and 90 mg Lumefantrine.

Practical scheme for administering the correct dose of Co-Artesiane:

Body Weight             Number of Millilitres

                                 1st Day            2nd Day           3rd Day

5 Kgs                            7 mL                 7 mL                7 mL

7.5 Kgs                        10 mL               10 mL              10 mL

10 Kgs                         14 mL               14 mL              14 mL

15 Kgs                         20 mL               20 mL              20 mL

Storage/Handling Recommendations

Store in a cool dry place out of the reach of children.

Review Date

2016-02-16 08:16:28