EMAZA α-β Arteether Injection 150mg/2ml

EMAZA.

Composition, Description, Pharmacology, Pharmacokinetics, Clinical data, Indications, Contraindications, Dosage and administration, Overdosage, Precautions, Drug interactions, Adverse effects, Storage, Presentation, NAFDAC registration, Manufacturers and Exporters of Emaza α-β Arteether Injection Medicine for Malaria.

COMPOSITION

Each 2ml contains α-β Arteether 150 mg

Arachis Oil BP q.s.

DESCRIPTION

α-β Arteether is a synthetic derivative of artemisinin, a product of Chinese plant Artemisia annua.

α-β Ateether is fast acting blood schizonticide specifically indicated for the treatment of chloroquine resistant P. falciparum malaria and cerebral malaria cases. α-β Arteether is developed by Centrl Drug Research Institute (C.D.R.I.), Lucknow, and Themis Medicare Limited after extensive preclinical, clinical and toxicological studies.

PHARMACOLOGY

α-β Arteether is fast acting blood schizonticidal agent for P. falciparum Malaria at the erythrocytic stage. Arteether is concentrated in parasitized erythroctytes. The functional group responsible for antimalarial activity of α-β Arteether is “endoperoxide bridge.” The researchers believe that iron from the digested haemoglobin of the parasite’s victim reduces this bridge releasing a highly reactive free radical iron (IV) oxo species which rips apart the parasitic cells. It is proposed that α-β Arteether inhibits the protein synthesis and alter the ribosomal orgranisation and endoplasmic reticulum.
α-β Arteether also acts on the membranes of the parasites through lipid peroxidation.

PHARMACOKINETICS

Main metabolite of α-β Arteether is Dihydroartemisinin. The half life of Dihydroarternisinin is more than 20 hours. The elimination of the drug is through hepatic metabolism and gets eliminated at a low rate as compared to other artemisinin derivatives.

CLINICAL DATA

In multicentric clinical evaluation of α-β Arteether in complicated and uncomplicated P. falciparum malaria, a total of 267 patients of uncomplicated P. falciparum malaria, having fever with chill/rigor and 211 patients of complicated P. falciparum malaria having fever, headache, vomiting, diarrhoea, convulsions, renal impairment, severe anaemia, spleenomegaly, hypotension and coma were treated with α-β Arteether. Most of the cases became afebrile within 36 hours without the use of antipyretic drugs and parasite free within 72 hours. The cure rate in uncomplicated malaria was nearly 100% and in complicated P. falciparum malaria about 90%. Recrudescence was less 7%. α-β Arteether is more lipophillic and has the advantage of greater accumulation in brain tissue, hence a potential drug for the treatment of cerebral malaria. α-β Arteether also exhibits gametocytocidal action on P. falciparum which will be an added advantage in cutting down the transmission of P. falciparum malaria. α-β is well tolerated and compliance is very good with virtually no drug related side effects.

INDICATIONS

α-β Arteether is indicated for use in severe P. falciparum malaria including cerebral malaria and as a second line treatment  in chloroquine resistant malaria. No cross resistance detected with Chloroquine.

CONTRAINDICATION

α-β Arteether is contra indicated in patients hypersensitive to artemisinin derivatives.

DOSAGE AND ADMINISTRATION

α-β Arteether Injection is for INTRAMUSCULAR USE ONLY.

Adult: 150mg i.e. 1 ampoule of α-β Arteether once daily for 3 consecutive days or as directed by the physician.

Children: 3mg/kg per day administered by intramuscular injection over a 3 day period or as directed by the physician.

The injection must be given in aseptic conditions, deep intramuscularly in the upper-external quadrant of the buttocks. No other drug should be mixed in the syringe.

OVERDOSAGE

The pre-clinical studies of α-β Arteether have shown that LD50 value is more than 1000 mg/kg, whereas the maximum dose injected in adult is about 2.5 mg/kg, per day per day. This confirms that the safety window for the dose administered is very wide. Hence this study concludes that α-β Arteether is well tolerated even when over dose is administered.

PRECAUTIONS

Pregnancy: Since no clinical data is available for the use of α-β Arteether during pregnancy, it should be used with caution in pregnant women, if the potential benefits justify the potential risk to the foetus.

Nursing Mother: It is not known whether α-β Arteether is excreted in human milk, because many drugs are excreted in human milk, caution should be exercised while using α-β Arteether.

DRUG INTERACTIONS

α-β Arteether does not interfere with the action of other commonly used drugs for treatment of P. falciparum malaria e.g. Quinine and can be administered along with these drug for the treatment of severe form of malaria. (Except for other Artemisinin Derivative like Artesunate and Artemether).

ADVERSE EFFECTS

Neurotoxicty is the common side effect associated with all artemisinin compounds in high doses. Neurotoxicity manifests as gait disturbances, loss of spinal cord pain responses, incoordination, respiratory depression, convulsions and cardio respiratory arrest. Other side effects are nausea, dizziness and depressed GIT activity. Clinical, neurological, electro-cardiographic and biochemical abnormality were seen. In the multi centric trails of α-β Arteether involving 478 patients suffering from P. falciparum malaria, no significant side effects were observed.

STORAGE

Keep in a cool place, protect from light.

KEEP ALL MEDICINES OUT OF REACH OF CHILDREN.

PRESENTATION

3 x 2ml Ampoules

NAFDAC REG. NO.: B4-5074

Manufactured for

Medicrown Nigeria Ltd.

7 Ilaro Road, Off Airport Road,

Sabon Gari, Kano, Kano State, Nigeria

Exported by

Sanghars H LIFECARE PVT. LTD

Ahmedabad, Gujarat, India.

Manufactured by

Divine Laboratories Pvt. Ltd.

Dist Vadodara-391 440,Gujarat, India

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