Navegando por Assunto "Mefloquina"

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Acesso aberto (Open Access)
Correlação dos teores séricos entre mefloquina e carboximefloquina com os teores de colesterol total e frações e triglicerídeos em pacientes com malária por Plasmodium falciparum não complicada
(Universidade Federal do Pará, 2010) RIVERA, Juan Gonzalo Bardález; VIEIRA, José Luiz Fernandes; http://lattes.cnpq.br/2739079559531098
Malaria is a major cause of morbidity and mortality worldwide, with over 100 million cases and at least one million deaths annually. It is a disease prevalent in the countries of tropical and subtropical climate of the planet. In Brazil, it occurs mainly in the Amazon region where climatic conditions favor the breeding of the vector and the spread of disease. With the emergence of vector resistance to insecticides, the lack of an effective vaccine, and especially the resistance of plasmodia to antimalarial drugs available today, there has been a resurgence and spread of the disease worldwide. Among the drugs used to treat the disease stands to mefloquine, which has high lipid solubility, being associated to a specific polipetídio (apo-A1) present in high density lipoproteins (HDL). Thus, infected erythrocytes tend to bind to circulating HDL particles to obtain the lipid supply, which would favor the passage and accumulation of the drug in these. However, malaria patients showed abnormal lipid profile, such as decreased levels of cholesterol total, HDL and LDL cholesterol, elevated values of lactate dehydrogenase, and a moderate increase of triglyceride level. This study is the correlation between serum concentrations of total cholesterol, HDL, LDL and triglycerides in serum levels of mefloquine (MQ) and carboximefloquina (CMC) in patients with falciparum malaria not complicated. For this we used the biochemical determination through self-plush Cobas analyzer to determine the levels of serum cholesterol and triglycerides and high performance liquid chromatography for determination of serum levels of mefloquine and carboximefloquina. Significant difference in serum total cholesterol, and HDL and LDL, which increased over the course of clinical evaluation, which corroborates findings in the literature and there was significant difference in serum triglycerides, which decreased with clinical outcome of patients.
Acesso aberto (Open Access)
Determinação de mefloquina e carboximefloquina em pacientes com malária por plasmodium falciparum no estado do Amapá
(Universidade Federal do Pará, 2008) BORGES, Larissa Maria Guimarães; VIEIRA, José Luiz Fernandes; http://lattes.cnpq.br/2739079559531098
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.
Acesso aberto (Open Access)
Estudo da eficácia e tolerância do artesunato oral isolado e em associação com mefloquina, no tratamento da malária falciparum não complicada em área endêmica do Pará, Brasil
(1996-06) CARDOSO, Bernardo da Silva; DOURADO, Heitor Vieira; PINHEIRO, Maria da Conceição Nascimento; CRESCENTE, Jose Angelo Barletta; AMORAS, Walter Wanderley; BAENA, Jorge; SARATY, Sandra
With the objective to evaluate the efficacy and tolerance of artesunate in the treatment of non-complicatedfalciparum malaria in endemic area of the State of Pará, 153 patients were randomized and studied in three groups, distributed by therapeutical scheme (I received mefloquine lOOOmg, II used artesunate 600mg followed by mefloquine 500mg). Evaluation was made by daily clinical and parasithological examination, in the first 7 days, and weekly until the 35th day of the follow up. Biochemical and hematological analysis previously done and on the 7th day, targetting cure control and identification of possible effects related to drugs administration. As to sex, parasitemy and fever, studied groups were homogeneous. Time for parasitemy disappearence was shorter in the groups II and III respectively, whose therapeutical schemes had artesunate. Fever disappereance was quicker in the group treated with the combination of drugs. Clinical and biochemical alterations associated with drugs administration did not show significant differences among the studied groups. Early disappearence of fever and parasitemy, and absence of important side effects suggest that artesunate, isolated or administrated in combination with mefloquine, constitutes an able therapeutical procedure to contribute for disease control in that region.
Acesso aberto (Open Access)
Validação de metodologia analítica por cromatografia liquida de alta eficiencia (CLAE), para determinação de mefloquina e carboximefloquina em amostras de sangue total adsorvidas em papel de filtro, em pacientes com malária por Plasmodium falciparum
(Universidade Federal do Pará, 2010) ATAIDE, Patrícia Marques de; VIEIRA, José Luiz Fernandes; http://lattes.cnpq.br/2739079559531098
Among the main challenges for malaria control in Brazil and in the world, the advent of resistance to the Plasmodium, particularly Plasmodium falciparum, is presented as the most relevant. Mefloquine is a drug of first line for the treatment of falciparum malaria, and the availability of sensitive methods and low cost for monitoring of blood concentrations of the drug and carboxymefloquine assists in the optimization of drug regimens. In this sense, analytical methodology was validated in accordance with the parameters suggested by official regulatory agency for determination of mefloquine and its carboxylated derivative on the whole blood sample adsorbed on filter paper. The method was employed using High Performance Liquid Chromatography after liquid-liquid extraction of the analytes. The detection was performed at 222nm. No interference was observed in other antimalarials commonly used. The method was linear in concentration range from 0.25 to 2.5 μg/mL for mefloquine and its carboxylated derivative. The detection and quantification limits were 35 ng/mL and 70 ng/mL for mefloquine and carboxymefloquine, respectively. The average intra assay precision was 31±4% for mefloquine and 21±5% for carboxymefloquine. The average inter assay precision was 38±4% for mefloquine and 25±7% for carboxymefloquine. The average of recovery for concentrations of mefloquine ranging from 0.25 to 2.5μg/mL was 83±14% and carboxymefloquine varying from 0.375 to 3740 μg/mL was 88±11%. The drug was stable in samples adsorbed on filter paper for a period of a month. . The method showed to be robust for small changes on pH of the mobile phase. To evaluate the applicability of the method was performed determination of analytes in blood samples adsorbed on filter paper from patients with falciparum malaria. The average concentration of mefloquine was 0.861±0.723 μg/mL and carboxymefloquine 0.472±0.086 μg/mL. The validation parameters of the analytical methodology followed the recommendations proposed by the official agencies and the method showed to be appropriate for determination of mefloquine and carboxymefloquine in whole blood samples adsorbed on filter paper.