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Titre du document / Document title

Clinical pharmacology and therapeutic potential of artemisinin and its derivatives in the treatment of malaria

Auteur(s) / Author(s)

DE VRIES P. J. (1) ; DIEN T. K. (2 3) ;

Affiliation(s) du ou des auteurs / Author(s) Affiliation(s)

(1) Division of Infectious Diseases, Tropical Medicine and AIDS, Department of Internal Medicine, Academic Medical Center, Amsterdam, PAYS-BAS
(2) Institute of Clinical Research in Tropical Medicine, Bach Mai Hospital, Hanoi, VIET NAM
(3) Department of Clinical Pharmacology and Pharmacotherapy, Academic Medical Center, Amsterdam, PAYS-BAS

Résumé / Abstract

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 areas with multidrug-resistant parasite strains. To prevent recrudescence with monotherapy of these compounds, treatment needs to be extended beyond the disappearance of parasites. After 5 days of therapy the rate of recrudescence is approximately 10%. Alternatively, combination with other drugs can be used. Combination with mefloquine is recommended for areas with multidrug-resistant P. falciparum.

Revue / Journal Title

Drugs    ISSN  0012-6667   CODEN DRUGAY 

Source / Source

1996, vol. 52, no6, pp. 818-836 (116 ref.)

Langue / Language

Anglais

Editeur / Publisher

Adis International, Auckland, NOUVELLE-ZELANDE  (1962) (Revue)

Mots-clés anglais / English Keywords

Artemisinin

;

Antimalarial

;

Parasiticid

;

Biological activity

;

Chemotherapy

;

Malaria

;

Treatment efficiency

;

Human

;

Toxicity

;

Review

;

Artemether

;

Artesunate

;

Protozoal disease

;

Parasitosis

;

Infection

;

Mots-clés français / French Keywords

Artémisinine

;

Antipaludique

;

Antiparasitaire

;

Activité biologique

;

Chimiothérapie

;

Paludisme

;

Efficacité traitement

;

Homme

;

Toxicité

;

Article synthèse

;

Artéméther

;

Artésunate

;

Artééther

;

Protozoose

;

Parasitose

;

Infection

;

Mots-clés espagnols / Spanish Keywords

Artemisinina

;

Antipalúdico

;

Antiparasitario

;

Actividad biológica

;

Quimioterapia

;

Paludismo

;

Eficacia tratamiento

;

Hombre

;

Toxicidad

;

Artículo síntesis

;

Artemetero

;

Artesunato

;

Protozoosis

;

Parasitosis

;

Infección

;

Localisation / Location

INIST-CNRS, Cote INIST : 15326, 35400006079868.0030

Nº notice refdoc (ud4) : 2488974



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