V-THER


Each Vial Contains:
Arteether

3 in Tray Rs 75

V-THER

Alpha, beta-Arteether is an ethyl ether derivative of artemisinin which is fast acting blood schizonticidal agent for P.falciparum malaria at the erythrocytic stage. Artemisinin is obtained from the sweet wormwood plant, Artemisia annua. Artemisinin is a sesquiterpene lactone (a compound made up of three isoprene units bound to cyclic organic esters) and is distilled from the dried leaves or flower clusters of A. annua. Malaria is caused by plasmodium and is transmitted to humans in the saliva of Anopheles mosquitoes—contains insoluble iron called hemozoin. Hemozoin is the endotoxin responsible for symptoms and is formed within schizonts as they feed on hemoglobin in the cytoplasm of human red blood cells. P group present in artemisinin reacts with hemozoin, and this reaction is suspected to result in the production of radicals that attack parasite proteins, thereby killing the organisms.

  • Severe malaria including cerebral malaria
  • As a second line treatment in chloroquine-resistant falciparum malaria
  • No cross resistance with chloroquine
  • Highly Effective Against Severe & Complicated Malaria

Mechanism of action-

Artemisinin: Endoperoxide bridges present is essential for antimalarial activity. The mechanism of artemisinin is still unknown however it appears to involve with heme-mediated decomposition of the endoperoxide bridge to produce carbon-centred free radicals. The selectivity to malaria parasites is described by involvement of heme (the iron portion in haemoglobin). The resulting carbon-centred free radicals are alkylating heme and proteins, one of which is the translationally controlled tumour protein. At high doses, the drug is neurotoxicity and mechanism may be similar to the mechanism of action.

Pharmacokinetics-

Oral bioavailability is 30% due to high first-pass metabolism
Plasma protein binding ranging from 43 to 81.5%
The metabolism of artemisinin is affected by the pH, enzymes in the tissue, blood, liver as well as the route of administration
Artemisinin is cleared by the liver
Half-life of artemisinin is 1–2 h
Common side effects of injection include:
  • Nausea
  • Dizziness
  • Headache
  • Vomiting
  • Dizziness
  • Diarrhoea
  • Pain at injection site
Do not use this injection in the following conditions:
  • Not to be used in pregnancy
  • Dose to be adjusted in hepatic and renal failure
Following drugs may interact with artemisinin:
  • Apomorphine
  • Betamethasone
  • Brompheniramine
  • Bupropion
  • Chlorpromazine
  • Cinnarizine
  • Cisapride
  • Clopidogrel
  • Desipramine
  • Dexamethasone
  • Diclofenac
  • Doxorubicin
  • Fluoxetine
  • Fluvoxamine