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Acesso aberto (Open Access)
Avaliação da terapêutica da malária por Plasmodium vivax: perfil cinético da cloroquina e primaquina
(Universidade Federal do Pará, 2011) TEIXEIRA, José Ribamar Mesquita; VIEIRA, José Luiz Fernandes; http://lattes.cnpq.br/2739079559531098; SOUZA, José Maria de; http://lattes.cnpq.br/6459204248879587
Today search - new strategies for improving the treatment and control of malaria. The monitoring of plasma concentrations of drugs is an important tool that aims to provide more knowledge on the kinetics of several antimalarial drugs, aiming to achieve rapid therapeutic effect with reduced risk of toxicity. Thus, this study aimed to evaluate the therapeutic response to chloroquine and primaquine for vivax malaria patients, the plasma concentrations correlate with parasitemia, epidemiological data and evaluation of liver and kidney function, aiming at the optimization of various therapeutic regimens employed, evaluating if the responses are due to ineffective treatment of Plasmodium resistance to chloroquine or the presence of sub-therapeutic concentrations of drugs. Thus, we evaluated 40 patients with vivax malaria in the Program in Clinical Trials of Malaria Institute Evandro Chagas (Belém, Pará) in the period 2008 to 2010. Hemogram and other biochemical parameters were performed. The research of plasmodia in blood smear was performed and the parasitemia averaged 7187.5 ± 6732.7 parasitos/mm3. The prevalence of males with 67.5% of cases. The locations of malaria infection ranged from 14 municipalities in the state of Pará, most of which originates in the city of Anajás. For 42.5% of patients it was the first episode of the disease and 57.5% of applicants. In the evaluation of anemia by hemoglobin, there - if the levels below reference values in 60% of patients and hematological and biochemical parameters showed that the mean values of hematocrit and red blood cells showed highly significant difference between subgroups of patients and non-anemic anemic. The determination of chloroquine and primaquine in patients on D0, D2, D7, D14 and D30 were performed. The mean values of 0, 1102.1, 546.7, 185.8 and 98.6 ng / ml for chloroquine and 0, 210.2, 345.0, 91.7 and 0 ng/ml for primaquine.
Acesso aberto (Open Access)
Caracterização comportamental e eletroencefalográfica das convulsões induzidas pelo cunaniol e acetato de cunaniol extraídos das folhas de Clibadium sylvestre, um modelo de convulsão generalizada experimental em ratos (Wistar)
(Universidade Federal do Pará, 2011-12-15) HAMOY, Moisés; NASCIMENTO, José Luiz Martins do; http://lattes.cnpq.br/7216249286784978
The Clibadium sylvestre is largely distribued in the Amazon region, where is know as cunambi or cunhambi, and its ingestion causes inebriation or even fish´s death, demonstrating ichthyotoxic property. The compounds existing in the leaf of Clibadium sylvestre are powerful of central nervous system stimulants, its leafs contain potential convulsivant substances. The electroencephalographic changes, seizure and drug effects on seizure behavior control were studied as well as metabolic pathway of compounds cunaniol acetate and cunaniol. The work was performed with adult male Wistar rats, treated with DE50 of 2,92 mg/kg or DL50 of 3,64 mg/kg of cunaniol, administration route used was intraperitoneal. After cunaniol administration, the seizure evolution was observed, it allows to classify them according to the presentation intensity relate to cunaniol plasma concentration. The eletroencefalografic parameters of the drugs action on the seizure control and the clinic characteristic were determined and evaluated. The plasma analysis obtained by liquid chromatography after the application of convulsivant substances indicates that the cunaniol acetate undergoes deacetylation giving rise to cunaniol, drug responsible for convulsive state. Data electrocorticography has been shown five different patterns of tracks during recording with 4 hours remaining changes outlined by 12 hours after application. Among the drugs used to prevent the onset of seizures, the most effective were diazepam, phenobarbital and ketamine. The convulsive behavior was classified into five stages. For the occurrence of stages 4 and 5 there was no statistical differences regarding plasma cunaniol.
Acesso aberto (Open Access)
Estimativa da não adesão ao tratamento da malária em área endêmica no Marajó estado do Pará
(Universidade Federal do Pará, 2014) ALMEIDA, Eduardo Dias; VIEIRA, José Luiz Fernandes; http://lattes.cnpq.br/2739079559531098
The association of Chloroquine (CQ) and Primaquine (PQ) is used as first-line treatment for malaria caused by Plasmodium vivax in Brazil. Treatment failure of this association is recognized worldwide and frequently reported. Multifactorial, involving related to the host, the vector and the etiological agent variables. Among these, treatment adherence is critical to establish the efficacy and effectiveness of antimalarial drugs, because the behavior of non-compliance tends to increase the rates of parasite recurrence and foster the emergence of strains resistant to antimalarial drugs. Despite the high incidence of P. vivax malaria in the Brazilian Amazon basin, few studies have evaluated treatment adherence and behavioral factors and environmental determinants. This study aimed to estimate the rate of non-adherence to treatment of P. vivax malaria in the municipality of Anajás, PA. We conducted a survey of demographic data (age, location, gender) and observational studies on the perception of the local population about the disease and its treatment. Then become a validated instrument to measure non-adherence to treatment in different metrics, based on the study by Morisky et al. (1986), with the addition of an item on the self-replication of doses for use in patients with P. vivax malaria. Finally, we proposed an evaluation model of non-adherence based on therapeutic drug monitoring of pharmacokinetic parameters of CQ, considering different scenarios of noncompliance. The results showed that the disease occurs in both sexes and in most cases are from rural areas. Risk factors such as gender, origin, parasitaemia at admission to treatment and age had no significant impact on rates of nonadherence. However, the abandonment of treatment to feel better, the need to return to work, or worse activities, the adverse effects of CQ, were the key behaviors for non-compliance to full treatment regimen. The instrument for measuring non-adherence, consisting of five items presented satisfactory validation parameters, in particular in its Likert scale dichotomized so that estimated non-adherence to the therapeutic regimen in 33.3%. After construction and validation of the mono-compartmental pharmacokinetic model by non-linear regression and evaluation of various scenarios for non-adherence, it is found that the loss of two consecutive doses without replacement was regarded as the only scenario that can significantly change the pharmacokinetic parameters and CK interfere with the therapeutic response.
Acesso aberto (Open Access)
Marcadores de estresse oxidativo e concentrações de primaquina e carboxiprimaquina em pacientes com malária por Plasmodium vivax
(Universidade Federal do Pará, 2014-11-06) RODRIGUES, Luiz Carlos de Souza; VIEIRA, José Luiz Fernandes; http://lattes.cnpq.br/2739079559531098
The changes in redox cycle has been associated with the physiopathology of severity of malaria in experimental models and in humans. However, a few studies evaluated the changes in redox equilibrium of patients with no severe malaria by P.vivax, which comprise the majority of the cases of disease. The variations of oxidative damage and the respective antioxidant response of human host were not compared before, during and after chemotherapy. Also, the mechanisms responsible by the generation of free radical in each phase that is, the heme degradation, respiratory burst of macrophages or antimalarials uses, were not determined. The objective of this study was to estimate the levels of biomarkers of oxidative damage and the respective antioxidant response, as well as primaquine and carboxyprimaquine whole blood levels in malaria by P. vivax. Therefore, were enrolled 38 patients with slide confirmed infection by P. vivax followed by 28 days. Serial blood samples were collected on pre-doses samples (D0) and on D2, D7 and D14. The oxidative damage and the antioxidant defense were estimated by the spectrophotometric measures of thiobarbituric acid reatives substances and methemoglobinemia, and by total antioxidant capacity and reduced glutathione, respectively. The control group consisted of 19 healthy volunteers matched for age and gender ratio. Primaquine and its major metabolite were determined by high performance liquid chromatography. The results revealed that the disease occurred in male patients of working age. Haematological parameters remained constant during the study. Biochemical evaluation showed a significant decrease in HDL-cholesterol levels during the study. Methemoglobinemia was associated with antimalarials uses, because the levels were similar to control group and increased significantly during the treatment. The levels of thiobarbituric acid reatives substances were associated with plasmodium and probably respiratory burst of macrophages, because they were higher than control group on D0, and no significant changes were observed after antimalarials usage. Total antioxidant capacity and oxidative stress levels were similar during the study as well as in the control group. The levels of reduced glutathione decreased significantly during the study and doesn’t be associated with both parasitaemia. Primaquine does not show a significant accumulation, and the concentrations of parent drug and its carboxyl metabolite were not associated with methemoglobinemia and thiobarbituric acid reatives substances levels.