ARTEMISININ
BRAND NAME:- no specific brand available.
ARTEMISININ is the active principal of the plant artemisia annua used in Chinese traditional medicine as ' Quinghaosu ' . It is a sesquiterpine lactones endoperoxide active against P. Falciparum resistant to all other antimalarial drugs as well as sensitive strains and other malarial species.
MECHANISM OF ACTION:-
Of artemisinin is not definitely known. The endoperoxide brige in its molecules appears to interact with haeme in the parasite. Ferrous iron- mediated clevage of the brige release a highly reactive free radicals species that binds to membrane proteins, causes lipid peroxidation , damages endoplasmic reticulum ,and ultimately result in lysis of the parasite. Another line of evidence has shown that the artemisinin free radicals specifically inhibits a plasmodial sarcoplasma - endoplasmic calcium ATPase labelled 'PF ATP6'.
Pharmacodynamic:-
🚫 Not available.
Pharmacokinetics:-
poor pharmacokinetic properties and high cost of the drugs are major drawbacks of their use.
USE:-
Treatment of malaria .
WHO recommends three days of oral treatment with any of five artemisinin-based combination therapies (ACTs): artemether/lumefantrine, artesunate/amodiaquine (ASAQ), artesunate/mefloquine, dihydroartemisinin/piperaquine, or artesunate/sulfadoxine/pyrimethamine. In each of these combinations, the artemisinin derivative rapidly kills the parasites, but is itself rapidly cleared from the body.The longer-lived partner drug kills the remaining parasites and provides some lingering protection from reinfection.
SIDE EFFECTS:-
Nausea, vomiting, loss of appetite, and dizziness. Mild blood abnormalities have also been noted.
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