In vitro evaluation of quinidine sensitivity in Brazilian Plasmodium falciparum isolates: comparative analysis to quinine and chloroquine.
Falciparum malaria represents a serious and an increasing world public health problem due to the acquired parasite's resistance to the most available drugs. In some endemic areas, quinidine, a diastereoisomer of the antimalarial quinine, has been employed for replacing the latter. In order to evaluate the use of quinidine as an alternative to the increasing loss of quinine effectiveness in Brazilian P. falciparum strains, as has been observed in the Amazon area, we have assayed quinidine, quinine and chloroquine. The in vitro microtechnique was employed. All isolates showed to be highly resistant to chloroquine. Resistance to quinine was not noted although high MIC (minimal inhibitory concentration) values have been observed. These data corroborate the decreasing sensitivity to quinine in strains from Brazil. Quinidine showed IC50 from 0.053 to 4.577 micromol/L of blood while IC50 from 0.053 to 8.132 micromol/L of blood was estimated for quinine. Moreover, clearance of the parasitemia was observed in concentrations lower than that used for quinidine in antiarrhythmic therapy, confirming our previous data. The results were similar to African isolate.
Menezes
C M
CM
Faculdade de Ciências Farmacêuticas, Universidade de São Paulo, São Paulo, SP, Brasil.
Kirchgatter
K
K
Di Santi
S M
SM
Paula
G A
GA
Ferreira
E I
EI
D000818:Animals; D000962:Antimalarials / Q000494:pharmacology*; D001938:Brazil; D002738:Chloroquine / Q000494:pharmacology*; D016001:Confidence Intervals; D004351:Drug Resistance; D016014:Linear Models; D021261:Parasitic Sensitivity Tests; D010963:Plasmodium falciparum / Q000187:drug effects*; D011802:Quinidine / Q000494:pharmacology*; D011803:Quinine / Q000494:pharmacology*
D000962:Antimalarials; D002738:Chloroquine; D011803:Quinine; D011802:Quinidine