Détail de la notice
Titre du Document
Clinical pharmacology and therapeutic potential of artemisinin and its derivatives in the treatment of malaria
Auteur(s)
DE VRIES P. J. ; DIEN T. K.
Résumé
Artemisinin and its derivatives are renowned for their potent antimalarial activity. They have found their way into clinical use in many areas where malaria is endemic. The in vitro concentration at which artemisinin can inhibit 50% of the growth of Plasmadium falciparum ranges from 3 to 30 μg/L. The fat-soluble derivatives artemether and arteether are approximately twice as active. The watersoluble dihydro-artemisinin and artesunate are 4 to 5 times more active in vitro. Artemisinin is available only for oral and rectal administration. Absorption is incomplete and elimination is fast, with an elimination half-life of 2 to 5 hours. Plasma concentrations after a single 500 mg oral dose most often exceed 200 μg/L. Artesunate and artemether can be considered as prodrugs. Biotransformation into the active metabolite dihydro-artemisinin occurs rapidly - almost immediately for artesunate. The reported elimination half-life of artesunate is less than 1 hour, and for artemether the figure is 3 to 11 hours. The pharmacokinetics of dihydro-artemisinin are not yet completely clear. Elimination is probably also rapid, with an elimination half-life of a few hours. Arteether, dissolved in oil for intramuscular administration, has a much longer elimination half-life of over 20 hours. The clinical efficacy of this group of drugs is characterised by an almost immediate onset and rapid reduction of parasitaemia, with complete clearance in most cases within 48 hours. Efficacy is high even in
Editeur
Adis International
Identifiant
PMID : 8957153 ISSN : 0012-6667 CODEN : DRUGAY
Source
Drugs (Basel) A. 1996, vol. 52, n° 6, pp. 818-836 [bibl. : 116 ref.]
Langue
Anglais
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