(Alpha beta Arteether Injection)
1.0 NAME OF THE MEDICINAL PRODUCT
2.0 QUALITATIVE AND QUANTITATIVE COMPOSITION
Each 2ml contains:
Alpha beta Arteether 150mg.
Arachis Oil B.P q.s.
3.0 PHARMACEUTICAL FORM
Light yellow liquid filled in amber colour ampoule.
4.0 MECHANISM OF ACTION
ᾀ/β arteether is a fast acting blood schizonticidal agent for P. falciparum malaria at the erythrocytic stage.
ᾀ/β arteether is concentrated in parasitized erythrocytes. The functional group responsible for antimalarial activity of ᾀ/β arteether is endoperoxide bridge. Iron from the digested haemoglobin of the parasite’s victim reduces this bridge, releasing a highly reactive free radical iron species which causes lysis of the parasitic cell.
Lysis of parasitic cell membrane occurs. Damage Includes swelling and deformity of food vacuoles membrane, nuclear membrane, endoplasmic reticulum and formation of autophagic vacuoles.
It is also proposed that ᾀ/β arteether inhibits the protein synthesis and alters the ribosomal organization and endoplasmic reticulum.
ᾀ/β arteether is transformed into dihydroartemisinin. It has a half life of 20 hours. It is eliminated by hepatic metabolism. The elimination is much slower compared to other compounds.
Severe malaria including cerebral malaria and as a second line drug in chloroquine resistant malaria cases only.
ᾀ/β arteether injection is contraindicated in patients hypersensitive to artemisinin derivatives.
Pregnancy – Adequate studies regarding safe use of artemisinm derivatives during pregnancy are not available. Artemisinin derivatives should not be used in pregnancy as primary drugs for uncomplicated malaria cases but these can be used for treatment of severe or complicated P. falciparum malaria infection in patients of multiple drug resistance, if the potential benefit justifies the potential risk to the fetus.
Nursing mothers – It is not known whether ᾀ/β arteether is excreted in human milk. Because many drugs are excreted in human milk caution should be exercised while using alpha/β arteether.
9.0 DRUG INTERACTIONS
Prolonged QT interval has been reported in some studies with high dosage of artemisinin derivatives. The cardiac effects of artemisinins are not very important from a clinical point of view, except that caution should be exercised against combinations with other drugs that prolong the QT interval, such as quinine and halofantrine.
10.0 AD VERSE EFFECTS
While neurotoxicity has been reported in experimental animals, there is no evidence of neurotoxicity in human beings with artemisinin derivatives alpha/β arteether is usually well tolerated. However, nausea, dizziness and depressed GIT activity can occur. Clinical, neurological, electrocardiographic and biochemical monitoring did not reveal significant toxicity.
Apart from some increase in eosinophil numbers, no haematological abnormality was seen.
11.0 DOSAGE AND ADMINISTRATION
Altaa (ᾀ/β arteether injection) is for intramuscular use only.
Adult – 150mg i.e. 1 ampoule of Altaa (ᾀ/β arteether injection ) once daily for 3 consecutive days.
Children -3mg/Kg per day administered by intramuscular injection over a 3-day period
The injection must be given under aseptic conditions, deep intramuscularly in the upper lateral quadrant of the buttock. No other drug should be mixed in the same syringe.
12. PHARMACEUTICAL PARTICULARS
12.1 List of excipients
Altaa injection 2ml ampoule contains 150mg alpha beta arteether.
Other excipients are arachis oil, ethyl oleate and benzyl alcohol.
12.3 SHELF LIFE
12.4 SPECIAL PRECAUTIONS FOR STORAGE
This medicine does not require any special conditions for storage.
12.5 NATURE AND CONTENTS OF CONTAINER
3 Ampoules packed in a Carton with tray.
12.6 SPECIAL PRECAUTIONS FOR DISPOSAL AND OTHER HANDLING
A score line allows adaptation of the dose in patients with impaired renal function.
As for all medicines, any unused medicinal product should be disposed off accordingly and in compliance with local environmental regulations.
Pace Pharmatech Pvt. Ltd.
Scott-Edil Pharmacia Ltd.
56, E.P.I.P., Phase-I, Jharmajri-173 205, INDIA