Determinação de mefloquina e carboximefloquina em pacientes com malária por plasmodium falciparum no estado do Amapá

Abstract

The determination of plasmatic and erythrocyte concentrations of mefloquine (MQ) and carboxymefloquine (CMQ) were studied in children and adults with malaria by Plasmodium falciparum not complicated in the Amapa state. The adult patients received oral outline of MQ 20 mg/kg divided in two days and artesunate 4 mg/kg/day for three days. For children the dose of MQ followed the schedule recommended by the manual of malaria therapy. Concentrations of MQ and CMQ in erythrocytes were quantified by high performance liquid chromatography on the third day of treatment (D3) and plasma levels were measured in the third and second fortieth day after the institution of therapy (D3 and D42). The average concentration of MQ and CMQ in plasma of children in D3 were 1.84 ± 0.83 μg/mL and 1.44 ± 0.70 μg/mL, and in erythrocytes 5.26 ± 1.46 μg/mL and 1.18 ± 0.65 μg/mL. In D42 the plasma concentrations were 0.45 ± 0.11 μg/mL and 0.51 ± 0.10 μg/mL, respectively. The relationship between plasma and erythrocytes concentrations of MQ and CMQ were 2.86 ± 1.27 and 0.75 ± 0.26. In adults, concentrations of MQ and CMQ in plasma were 2.43 ± 1.13 μg/mL and 1.10 ± 0.38 μg/mL, and in erythrocytes 5.51 ± 1.92 μg/mL and 1.08 ± 0.35 μg/mL, respectively. The plasma concentrations in D42 were 0.54 ± 0.15 μg/mL and 0.58 ± 0.93 μg/mL, respectively. The relationship erythrocyte:plasma for MQ was 3.03 ± 1.56 and 1.12 ± 0.29 to CMQ. The correlation coefficient between plasma and erythrocytes concentrations of MQ in children was 0.035 and adults 0.0436. For CMQ the correlation coefficient in children was 0.8722 and in adults 0.5155. The higher accumulation of MQ in the red blood cells allows us to emphasize the importance of the simple diffusion for the entry of the drug in the cell because of their physical and chemical characteristics.