[Current data on major novel antiamalaria drugs: Artemisinin (qinghaosu) derivatives].
Artemisinin or Qinghaosu (QHS) and its derivatives (mainly artemether and artesunate) are novel and the most rapidly acting antimalarial drugs, effective in adults and children against all the Plasmodium of humans, including multi-drug resistant Plasmodium falciparum. Resistance to these drugs has not been identified so far. QHS derivatives are very well tolerated and there is no evidence of serious clinical toxicity in man. The neurotoxicity seen in animals after high doses of certain compounds has not been reported in humans. In the treatment of severe malaria, QHS administered by either the intramuscular (artemether and artesunate) or intravenous (artesunate) route, are at least as effective as quinine, and are simpler to use. Intramuscular artemether appears to be an excellent alternative to intravenous quinine, which is specially important since quinine resistance is common in Asia and a decrease of sensitivity to quinine has been reported in Africa. For the treatment of uncomplicated malaria, the use of QHS must be highly selective. Treatment by QHS is only totally justifiable in areas where multi-drug resistant strains are prevalent and always concurrently with an other effective, longer-acting, antimalarial drug (mefloquine, preferably). This combination approach is associated with an accelerated antimalarial response. It avoids or limits the risk of recrudescences, and protects both drugs from the development of resistance. Artemether and artesunate have also been administered by the rectal route with highly promising results for treatment of severe malaria. This route eliminates several disadvantages or risks associated with injections. The best indication for rectal administration will be probably a rescue treatment of severe malaria in rural and poorly equipped dispensaries before transfer to hospital for treatment using conventional modalities. All QHS derivatives should not be used for chemophophylaxis.
Ambroise-Thomas
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Département de Parasitologie-Mycologie Médicale et Moléculaire, Faculté de Médecine, Université Joseph Fourier Grenoble UPRES-A CNRS 5082, La Tronche.
D000962:Antimalarials / Q000009:adverse effects / Q000493:pharmacokinetics / Q000627:therapeutic use*; D037621:Artemisinins; D002986:Clinical Trials as Topic; D004365:Drugs, Chinese Herbal / Q000009:adverse effects / Q000493:pharmacokinetics / Q000627:therapeutic use*; D006801:Humans; D016778:Malaria, Falciparum / Q000188:drug therapy / Q000378:metabolism; D012717:Sesquiterpenes / Q000009:adverse effects / Q000493:pharmacokinetics / Q000627:therapeutic use*; D016896:Treatment Outcome
D000962:Antimalarials; D037621:Artemisinins; D004365:Drugs, Chinese Herbal; D012717:Sesquiterpenes; C031327:artemisinin
Données actuelles sur de nouveaux antipaludiques majeurs: les dérivés de l'Artémisinine (Qinghaosu).