Artelife α-β Arteether Injection

Artelife

α-β Arteether Injection

 

COMPOSITION

Each 2ml contains

α-β Arteether 150mg

Arachis Oil q.s.

 

PHARMACOLIGAL CLASSIFICATION

Anti-malarial.

 

INDICATION

It is indicated for the treatment of complicated and uncomplicated P. falciparum malaria, including cerebral malaria. It is available as injection for intramuscular use only.

It is indicated as second-line treatment of Chloroquine resistant malaria.

 

DESCRIPTION

α-β Arteether is an efficient erythrocytic schizontocidal drug. α-β Arteether is an oil-soluble ethyl ether derivative of dihydroartemisinin, which shows rapid schizonticidal action and brings about quick clinical improvement in falciparum malaria with low recrudescence rate. It has some gametocidal action too, which aids in cutting down the transmission of falciparum malaria.

 

PHARMACODYNAMICS

α-β Arteether acts at the erythrocytic stage of malarial parasite. It is proposed that the intra-parasitic haem reduces the endoperoxide bridge (the functional group responsible for antimalarial activity of α-β Arteether), releasing a highly reactive free radical iron (IV) oxo species, which alkalytes and oxidises proteins and lipids causing lysis of the parasitic cell. The membrane of the parasite is damaged by lipid peroxidation and channel proteins’ inactivation. It is also proposed that α-β Arteether may also inactivate ribosomes and inhibit protein synthesis. Parasitic clearance times of α-β Arteether are shorter than those with chloroquine and also the response is symptomatic.

 

PHARMACOKINETICS

• Route of administration: α-β Arteether is rapidly absorbed when administered intramuscularly.

• Metabolism: It is metabolized in the liver to the de-ethylated derivative dihydroartemisinin.

• Half-life: >20 hours.

• Elimination: Metabolized by the liver, it is eliminated slowly as compared to other artemisinin derivatives.

 

DOSAGE AND ADMINISTRATION

α-β arteether is for intramuscular use only.

Adult – 150mg i.e. 1 ampoule of α-β arteether once daily for 3 consecutive days.

The injection must be administered under aseptic conditions as deep intramuscular injection in the upper-lateral quadrant of the buttock.

No other drug should be mixed in the same syringe.

 

CONTRAINDICATIONS

α-β Arteether is contraindicated in patients showing hypersensitivity to artemisinin derivatives.

 

USE IN PREGNANCY

Safety of α-β Arteether during pregnancy is not established. However, in case of severe infection with P. falciparum in a pregnant woman, if the potential benefit to the patient justifies the potential risk to the fetus, it may be used with caution in these women.

 

USE IN LACTATION

It is not known whether α-β Arteether is secreted in human milk. As most of the drugs are, lactating women on α-β Arteether therapy should not breast-feed their infants.

 

WARNINGS AND PRECAUTIONS

During the treatment of cerebral malaria and complicated malaria, general supporting therapy should be carried out.

 

ADVERSE REACTIONS

• Adverse effects such as nausea, dizziness, tinnitus, depressed GI tract activity, neutropenia, ECG abnormalities including prolongation of QT interval may occur.

• α-β Arteether is generally well tolerated without any significant clinical, neurological and biochemical toxicity. Neurotoxicity (at high doses, seen in animals) is manifested as gait disturbances, loss of spinal cord pain responses, incoordination, respiratory depression, convulsions and cardio respiratory arrest.

• Apart from some increase in eosinophil count, no other haematological abnormality has been reported.

 

DRUG INTERACTIONS

Quinine and halofantrine are known to prolong the QT interval when used along with α-β Arteether.

Caution should be exercised while using these drugs.

 

OVERDOSAGE

There is no experience with overdosage of α-β Arteether.

 

STORAGE INSTRUCTIONS

Store below 25oC. Protect from light.

 

PRESENTATION AND PACKING

3 x 2 ml amber coloured ampoule.

 

NAFDAC Reg. No. B4-4774

 

Manufactured In India by

Ciron Drugs & Pharmaceuticals Pvt. Ltd.

N-118/119, M.I.D.C., Tarapur,

Boisar, Dist. Thane – 401 506.

www.cironpharma.com

 

Manufactured for

CHEZ RESOURCES PHARMA NIG. LTD.

7, Calabar Street,

Onitsha, Anambra State,

Nigeria.

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