Atc Classification & Description:
P01BE02 - ; Belongs to the class of artemisinin and derivative antimalarials.
The chemical name of is (3R,5aS,6R,8aS,9R,10S,12R,12aR)-decahydro-10-methoxy-3,6,9-trimethyl-3,12-epoxy-12H-pyrano[4,3-j]-1,2benzodioxepine. is a white, crystalline powder that is freely soluble in acetone, soluble in methanol and ethanol, and practically insoluble in water. It has the empirical formula C16H26O5 with a molecular weight of 298.4, and the following structural formula::
Mechanism of Action:
is a potent and rapidly acting blood schizontocide, which is highly efficacious in treating chloroquine-resistant falciparum malaria, and complicated falciparum malaria including cerebral malaria. Its quick onset of effect and high efficacy in bringing down the parasite load are the properties which make this drug a suitable therapeutic option against falciparum infection.
: Rapidly hydrolysed to the active metabolite dihydroartemisinin.
: Elimination half-life: about 4-11 hr after IM or oral admin.
For the treatment of all kinds of malaria including the chloroquine-resistant P. falciparum malaria and the first aid of critical malaria.
Dosage and administration:
The drug is used for intramuscular injection, five days course with the initial dose of 3.2mg/kg, followed by 1.6rng/kg for the following 4 days.
The initial dose for adults is 160mg (2 ampoules), followed by 80mg (1 ampoule) every time from the 2" to 5th day. The dose for children or overweight patients should be decreased or increased on the basis of the individual weight or under the doctor's prescription.
Administration For Children:
For children, the dose should be chosen as follows:
Adverse Drug Reactions
Mild GI disturbance, dizziness, tinnitus, reduction in reticulocyte and leucocyte counts, nausea, vomiting, abdominal pain, bradycardia, 1st-degree heart block, transient increase in serum transaminases.
is contra-indicated to those patients which have a history of hypersensitivity to .
Pregnancy and lactation. Avoid concomitant use of drugs known to prolong QT interval or monitor such patients.
excretes into breast milk. It should not be taken by breast-feeding women.
Drug Interactions :
causes QT prolongation in some patients. Thus concomitant use of erythromycin, , procainamide, quinidine, , amiodarone, bretylium, bepridil, , astemizole, probucol, tricyclic antidepressants, s may be avoided.
Manufacture in India for:
- Each pack contains 10 ampoules of 80 mg/1ml.
Cygnus Healthcare Specialities Pvt Ltd.
Thane -400607 India