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Praziquantel for Schistosomiasis: Single-Drug Metabolism Revisited, Mode of Action, and Resistance

Vale, Nuno ; Gouveia, Maria João ; Rinaldi, Gabriel ; Brindley, Paul J ; Gärtner, Fátima ; Correia da Costa, José M

Antimicrobial agents and chemotherapy, 2017-05, Vol.61 (5) [Periódico revisado por pares]

United States: American Society for Microbiology

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  • Título:
    Praziquantel for Schistosomiasis: Single-Drug Metabolism Revisited, Mode of Action, and Resistance
  • Autor: Vale, Nuno ; Gouveia, Maria João ; Rinaldi, Gabriel ; Brindley, Paul J ; Gärtner, Fátima ; Correia da Costa, José M
  • Assuntos: Africa South of the Sahara ; Animals ; Drug Resistance ; Humans ; Minireview ; Praziquantel ; Praziquantel - analogs & derivatives ; Praziquantel - metabolism ; Praziquantel - therapeutic use ; Schistosoma ; Schistosoma - drug effects ; Schistosoma - metabolism ; Schistosomiasis ; Schistosomiasis - drug therapy ; Schistosomicides ; Schistosomicides - metabolism ; Schistosomicides - therapeutic use
  • É parte de: Antimicrobial agents and chemotherapy, 2017-05, Vol.61 (5)
  • Notas: ObjectType-Article-1
    SourceType-Scholarly Journals-1
    ObjectType-Feature-2
    content type line 23
    Present address: Nuno Vale, Laboratory of Pharmacology, Department of Drug Sciences, Faculty of Pharmacy, University of Porto, Porto, Portugal; Gabriel Rinaldi, Wellcome Trust Sanger Institute, Wellcome Genome Campus, Hinxton, Cambridge, United Kingdom.
    Citation Vale N, Gouveia MJ, Rinaldi G, Brindley PJ, Gärtner F, Correia da Costa JM. 2017. Praziquantel for schistosomiasis: single-drug metabolism revisited, mode of action, and resistance. Antimicrob Agents Chemother 61:e02582-16. https://doi.org/10.1128/AAC.02582-16.
  • Descrição: Schistosomiasis, a major neglected tropical disease, affects more than 250 million people worldwide. Treatment of schistosomiasis has relied on the anthelmintic drug praziquantel (PZQ) for more than a generation. PZQ is the drug of choice for the treatment of schistosomiasis; it is effective against all major forms of schistosomiasis, although it is less active against juvenile than mature parasites. A pyrazino-isoquinoline derivative, PZQ is not considered to be toxic and generally causes few or transient, mild side effects. Increasingly, mass drug administration targeting populations in sub-Saharan Africa where schistosomiasis is endemic has led to the appearance of reduced efficacy of PZQ, which portends the selection of drug-resistant forms of these pathogens. The synthesis of improved derivatives of PZQ is attracting attention, e.g., in the (i) synthesis of drug analogues, (ii) rational design of pharmacophores, and (iii) discovery of new compounds from large-scale screening programs. This article reviews reports from the 1970s to the present on the metabolism and mechanism of action of PZQ and its derivatives against schistosomes.
  • Editor: United States: American Society for Microbiology
  • Idioma: Inglês
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