In vitro chloroquine resistance modulation study on fresh isolates of Brazilian Plasmodium falciparum: intrinsic antimalarial activity of phenothiazine drugs

Memórias do Instituto Oswaldo Cruz

Carla Ms Menezes²  Karin Kirchgatter¹  Sílvia M Di Santi¹  Carine Savalli¹  Fabiola G Monteiro¹  Gilberto A Paula¹  Elizabeth I Ferreira² 

[1] ,Universidade de São Paulo Faculdade de Ciências Farmacêuticas

关键词: antimalarial;    chloroquine;    multidrug resistance;    phenothiazines;    modulating agents;    chemosensitizer agents;   

DOI  :  10.1590/S0074-02762002000700018

来源: SciELO

【 摘 要 】

Phenothiazine drugs - fluphenazine, chlorpromazine, methotrimeprazine and trifluoperazine - were evaluated as modulating agents against Brazilian chloroquine-resistant fresh isolates of Plasmodium falciparum. Aiming to simulate therapeutic schedules, chloroquine was employed at the concentration used for sensitive falciparum malaria treatment and anti-psychotic therapeutic concentrations of the phenothiazine drugs were adopted in two-fold serial dilutions. The in vitro microtechnique for drug susceptibility was employed. Unlike earlier reported data, the phenothiazine modulating effect was not observed. However, all the drugs demonstrated intrinsic antiplasmodial activity in concentrations lower than those described in the literature. In addition, IC50 estimates have been shown to be inferior to the usual anti-psychotic therapeutic concentrations. Statistical analysis also suggested an increase in the parasitaemia rate or, even, a predominant antiparasitic effect of phenothiazine over chloroquine when used in combination.

【 授权许可】

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