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Id: biblio-1041531
Autor: Wu, Wanting; Liang, Yuan; Wu, Guangchao; Su, Yinghang; Zhang, Hongying; Zhang, Zhenyan; Deng, Changsheng; Wang, Qi; Huang, Bo; Tan, Bo; Zhou, Chongjun; Song, Jianping.
Título: Effect of artemisinin-piperaquine treatment on the electrocardiogram of malaria patients
Fonte: Rev. Soc. Bras. Med. Trop;52:e20180453, 2019. tab, graf.
Idioma: en.
Projeto: Guangdong Provincial Chinese Medicine Bureau Project, Guangdong Traditional Chinese Medicine Letter; . Major projects of Guangdong Province; . Science and Technology Program of Guangzhou.
Resumo: Abstract INTRODUCTION: Concern regarding the cardiotoxicity of antimalarials has been renewed because of their potential to cause QT/QTc interval prolongation related to torsade de pointes (TdP). Artemisinin-piperaquine (AP) is considered an effective artemisinin-based combination therapy (ACT) for malaria. METHODS: This study involved a retrospective analysis of clinical data of 93 hospitalized malaria patients who had received AP orally. Electrocardiograms (ECGs) were obtained at specific time points in the original study. RESULTS: Some cases of QT prolongation were observed. However, no TdP was found. CONCLUSIONS: AP may cause QT interval prolongation in some malaria patients but may not lead to TdP.
Descritores: Quinolinas/efeitos adversos
Síndrome do QT Longo/induzido quimicamente
Malária Falciparum/tratamento farmacológico
Artemisininas/efeitos adversos
Antimaláricos/efeitos adversos
-Quinolinas/uso terapêutico
Síndrome do QT Longo/diagnóstico
Estudos Retrospectivos
Artemisininas/uso terapêutico
Quimioterapia Combinada
Eletrocardiografia
Pessoa de Meia-Idade
Antimaláricos/uso terapêutico
Limites: Humanos
Masculino
Feminino
Adulto
Responsável: BR1.1 - BIREME


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Machado, Ricardo Luiz Dantas
Castro, Ana Maria de
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Id: biblio-1041579
Autor: Chapadense, Francesca; Machado, Ricardo Luiz Dantas; Ventura, Ana Maria Revorêdo da Silva; Áreas, André; Machado, Renato Beilner; Viana, Giselle Rachid; Zalis, Mariano Gustavo; Castro, Ana Maria de; Cravo, Pedro.
Título: Plasmodium falciparum malarial parasites from Brazil lack artemisinin resistance-associated mutations in the kelch13 gene
Fonte: Rev. Soc. Bras. Med. Trop;52:e20180225, 2019. tab, graf.
Idioma: en.
Projeto: São Paulo Research Foundation; . National Council for Scientific and Technological Development.
Resumo: Abstract INTRODUCTION Mutations in the propeller domain of the Plasmodium falciparum kelch13 (k13) gene are associated with artemisinin resistance. METHODS: We developed a PCR protocol to sequence the pfk13 gene and determined its sequence in a batch of 50 samples collected from 2003 to 2016 in Brazil. RESULTS: We identified 1 K189T substitution located outside the propeller domain of the PfK13 protein in 36% of samples. CONCLUSIONS: Although the sample size is relatively small, these results suggest that P. falciparum artemisinin-resistant mutants do not exist in Brazil, thereby supporting the continuation of current treatment programs based on artemisinin-based combination therapy.
Descritores: Plasmodium falciparum/genética
Resistência a Medicamentos/genética
Proteínas de Protozoários/genética
Malária Falciparum/parasitologia
Artemisininas/farmacologia
Mutação/genética
-Fenótipo
Plasmodium falciparum/efeitos dos fármacos
Genótipo
Limites: Humanos
Responsável: BR1.1 - BIREME


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Id: biblio-1155593
Autor: Wu, Wanting; Lu, Chenguang; Liang, Yuan; Zhang, Hongying; Deng, Changsheng; Wang, Qi; Xu, Qin; Tan, Bo; Zhou, Chongjun; Song, Jianping.
Título: Electrocardiographic effect of artemisinin-piperaquine, dihydroartemisinin-piperaquine, and artemether-lumefantrine treatment in falciparum malaria patients
Fonte: Rev. Soc. Bras. Med. Trop;54:e05362020, 2021. tab, graf.
Idioma: en.
Projeto: Traditional Chinese Medicine Bureau of Guangdong Province; . Ministry of Science and Technology of the People's Republic of China; . Guangdong province of the People's Republic of China.
Resumo: Abstract INTRODUCTION: Artemisinin-based combination therapy (ACT), such as artemisinin-piperaquine (AP), dihydroartemisinin-piperaquine (DP), and artemether-lumefantrine (AL), is the first-line treatment for malaria in many malaria-endemic areas. However, we lack a detailed evaluation of the cardiotoxicity of these ACTs. This study aimed to analyze the electrocardiographic effects of these three ACTs in malaria patients. METHODS: We analyzed the clinical data of 89 hospitalized patients with falciparum malaria who had received oral doses of three different ACTs. According to the ACTs administered, these patients were divided into three treatment groups: 27 treated with AP (Artequick), 31 with DP (Artekin), and 31 with AL (Coartem). Electrocardiograms and other indicators were recorded before and after the treatment. The QT interval was calculated using Fridericia's formula (QTcF) and Bazett's formula (QTcB). RESULTS: Both QTcF and QTcB interval prolongation occurred in all three groups. The incidence of such prolongation between the three groups was not significantly different. The incidence of both moderate and severe prolongation was not significantly different between the three groups. The ΔQTcF and ΔQTcB of the three groups were not significantly different. The intra-group comparison showed significant prolongation of QTcF after AL treatment. CONCLUSIONS: Clinically recommended doses of DP, AL, and AP may cause QT prolongation in some malaria patients but do not cause torsades de pointes ventricular tachycardia or other arrhythmias.
Descritores: Malária Falciparum/tratamento farmacológico
Artemisininas/efeitos adversos
Malária/tratamento farmacológico
Antimaláricos/efeitos adversos
-Quinolinas
Combinação de Medicamentos
Eletrocardiografia
Artemeter/uso terapêutico
Combinação Arteméter e Lumefantrina/uso terapêutico
Limites: Humanos
Responsável: BR1.1 - BIREME


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Id: biblio-1118972
Autor: SILVA, Nazaré Carneiro da; GONÇALVES, Suellen Ferreira; ARAÚJO, Luciana Silva de; KASPER, Aline Aparecida München; FONSECA, Amanda Luisa da; SARTORATTO, Adilson; CASTRO, Kelly Christina Ferreira; MORAES, Tânia Mara Pires; BARATTO, Leopoldo Clemente; VAROTTI, Fernando de Pilla; BARATA, Lauro Euclides Soares; MORAES, Waldiney Pires.
Título: In vitro and in vivo antimalarial activity of the volatile oil of Cyperus articulatus (Cyperaceae)
Fonte: Acta amaz;49(4):334-342, out. - dez. 2019.
Idioma: en.
Resumo: Malaria is a disease of global tropical distribution, being endemic in more than 90 countries and responsible for about 212 million cases worldwide in 2016. To date, the strategies used to eradicate this disease have been ineffective, without specific preventive measures such as vaccines. Currently, the existing therapeutic arsenal is limited and has become ineffective against the expansion of artemisinin-resistant Plasmodium, demonstrating the need for studies that would allow the development of new compounds against this disease. In this context, we studied the volatile oil obtained from rhizomes of Cyperus articulatus (VOCA), a plant species commonly found in the Amazon region and popularly used as a therapeutic alternative for the treatment of malaria, in order to confirm its potential as an antimalarial agent by in vitro and in vivo assays. We cultured Plasmodium falciparum W2 (chloroquine-resistant) and 3D7 (chloroquine-sensitive) strains in erythrocytes and exposed them to VOCA at different concentrations in 96-well microplates. In vivo antimalarial activity was tested in BALB/c mice inoculated with approximately 106 erythrocytes infected with Plasmodium berghei. VOCA showed a high antimalarial potential against the two P. falciparum strains, with IC50 = 1.21 µg mL-1 for W2 and 2.30 µg mL-1 for 3D7. VOCA also significantly reduced the parasitemia and anemia induced by P. berghei in mice. Our results confirmed the antimalarial potential of the volatile oil of Cyperus articulatus. (AU)
Descritores: Plasmodium berghei
Plasmodium falciparum
Cloroquina
Artemisininas
Malária
Responsável: BR6.1 - BCS - Biblioteca de Ciências da Saúde


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Id: lil-662953
Autor: Durand, Salomón; Sihuincha, Moisés; Lachira, Arnaldo; Chaves, Jorge; Cabezas, César.
Título: Necesidad de vigilar la resistencia del P. falciparum al artesunato en el Perú / A need to monitor P. falciparum resistance to artesunate in Peru
Fonte: Rev. peru. med. exp. salud publica;29(4):579-580, oct.-dic. 2012. ilus, graf, mapas, tab.
Idioma: es.
Descritores: Antimaláricos/farmacologia
Artemisininas/farmacologia
Plasmodium falciparum/efeitos dos fármacos
-Artemisininas/uso terapêutico
Resistência a Medicamentos
Malária Falciparum/tratamento farmacológico
Peru
Limites: Humanos
Tipo de Publ: Carta
Revisão
Responsável: BR1.1 - BIREME


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Id: biblio-1056435
Autor: Zaki, Mohamed Samir Ahmed; Haidara, Mohamed A; Alghamd, Mansour A; Shati, Ayed A; Wares, Adnan; Eid, Refaat A.
Título: Protective effect of dietary vitamin E (alpha; Tocopherol) on artemisinin induced oxidative liver tissue damage in rats / Efecto protector de la vitamina E en la dieta (alfa; tocoferol) sobre el daño oxidativo del tejido hepático inducido por artemisinina en ratas
Fonte: Int. j. morphol;38(2):278-288, abr. 2020. graf.
Idioma: en.
Projeto: Khalid University.
Resumo: This experiment was designed to study the effects of oral administration of artemether which is the most rapid-acting class of antimalarial drugs and the possible protective effect of vitamin E taken with it on the liver of albino rats. A total of twenty-four adult male albino rats were used in this study and were divided into four groups. Group one served as a control and rats in group two exposed to oral intake of artemether daily for fifteen days. The third and fourth groups treated with artemether plus low and high doses of vitamin E respectively. At the end of the experiment, the rats were sacrificed, and the livers were obtained and processed for histological, biochemical and statistical studies. Histological study of the hepatocytes of rats exposed to artemether showed nearly complete disintegration of most cellular contents except few numbers of mitochondria and rough endoplasmic reticulum. Also, the cytoplasm of these cells had few lysosomes, many vacuoles and irregular nuclei with abnormal distribution of chromatin and were shown. The hepatic sinusoids were dilated and filled with blood and vacuoles and bile ductules were abnormal in its structure. Treatment with low and high doses of vitamin E in concomitant with artemether ameliorated the hepatic histopathological lesions and its parenchyma attained nearly normal structure. As far as biochemical changes, alanine aminotransferase (ALT) and aspartate aminotransferase (AST) in rats treated with artemether were significantly elevated as compared to the control. Superoxide dismutase (SOD) and malondialdehyde (MDA) levels were significantly increased in the liver in rats treated with artemether. However, vitamin E ameliorated the rise in ALT and AST with decreased MDA concentration and levels of SOD as compared to the corresponding artemether group values. Results of the present suggest that artemether has a harmful and stressful effect on hepatic tissue and the treatment with vitamin E may alleviate this toxicity.

Este experimento fue diseñado para estudiar los efectos de la administración oral de arteméter, la clase de medicamentos antipalúdicos de acción rápida, y el posible efecto protector de la vitamina E en el hígado de ratas albinas. Se utilizaron un total de 24 ratas albinas machos adultas y se dividieron en cuatro grupos. El grupo uno sirvió como control y las ratas en el grupo dos recibieron la dosis oral de arteméter diariamente durante 15 días. Los grupos tres y cuatro fueron tratados con arteméter, más dosis bajas y altas de vitamina E, respectivamente. Al final del experimento, se sacrificaron las ratas y se obtuvieron y procesaron los hígados para estudios histológicos, bioquímicos y estadísticos. El estudio histológico de los hepatocitos de ratas expuestas a arteméter mostró una desintegración casi completa de la mayoría de los contenidos celulares, excepto algunos mitocondrias y retículo endoplásmico rugoso. Además, el citoplasma de estas células tenía pocos lisosomas, muchas vacuolas y núcleos irregulares con distribución anormal de cromatina. Los sinusoides hepáticos estaban dilatados y llenos de sangre y vacuolas, y los conductos biliares tenían una estructura anormal. El tratamiento con dosis bajas y altas de vitamina E en forma concomitante con arteméter mejoró las lesiones histopatológicas hepáticas y su parénquima alcanzó una estructura casi normal. En cuanto a los cambios bioquímicos, la alanina aminotransferasa (ALT) y la aspartato aminotransferasa (AST) en ratas tratadas con arteméter se elevaron significativamente en comparación con el control. Los niveles de superóxido dismutasa (SOD) y malondialdehído (MDA) aumentaron significativamente en el hígado en ratas tratadas con arteméter. Sin embargo, la vitamina E mejoró el aumento de ALT y AST con una disminución de la concentración de MDA y los niveles de SOD en comparación con los valores correspondientes del grupo de arteméter. Los resultados del presente estudio sugieren que el arteméter tiene un efecto dañino y estresante sobre el tejido hepático y el tratamiento con vitamina E puede aliviar esta toxicidad.
Descritores: Vitamina E/farmacologia
Artemisininas/toxicidade
Doença Hepática Crônica Induzida por Substâncias e Drogas/enzimologia
-Aspartato Aminotransferases/análise
Vitamina E/administração & dosagem
Microscopia Eletrônica de Transmissão
Alanina Transaminase/análise
Modelos Animais de Doenças
Fígado/efeitos dos fármacos
Antimaláricos/toxicidade
Limites: Animais
Masculino
Ratos
Responsável: CL1.1 - Biblioteca Central


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Alecrim, Maria das Graças Costa
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Id: biblio-1002690
Autor: Pinto, Raquel de Medeiros; Sampaio, Vanderson de Souza; de Melo, Gisely Cardoso; Alecrim, Maria das Graças Costa; Mattos, Karine; Perdomo, Renata Trentin; Cordeiro, Sabrine da Costa; Parente, Ana Flávia Alves; de Carvalho, Lídia Raquel; Mendes, Rinaldo Pôncio; Lacerda, Marcus Vinícius Guimarães; Monteiro, Wuelton Marcelo; Weber, Simone Schneider.
Título: Overview of artemisinin effectiveness during outset years of its implementation in the western Brazilian Amazon
Fonte: Mem. Inst. Oswaldo Cruz;114:e190075, 2019. tab, graf.
Idioma: en.
Projeto: CAPES; . RMP; . KM; . CAPES.
Resumo: BACKGROUND The elimination of malaria depends on the blocking of transmission and of an effective treatment. In Brazil, artemisinin therapy was introduced in 1991, and here we present a performance overview during implementation outset years. METHODS It is a retrospective cohort (1991 to 2002) of patients treated in a tertiary centre of Manaus, with positive microscopic diagnosis of Plasmodium falciparum malaria, under treatment with using injectable or rectal artemisinin derivatives, and followed over 35-days to evaluate parasite clearance, death and recurrence. FINDINGS This cohort outcome resulted 97.6% (1554/1593) of patients who completed the 35-day follow-up, 0.6% (10/1593) of death and 1.8% (29/1593) of follow-up loss. All patients that died and those that presented parasitaemia recurrence had pure P. falciparum infections and received monotherapy. Considering patients who completed 35-day treatment, 98.2% (1527/1554) presented asexual parasitaemia clearance until D4 and 1.8% (27/1554) between D5-D10. It is important to highlight that had no correlation between the five treatment schemes and the sexual parasite clearance. Finally, it is noteworthy that we were able to observe also gametocytes carriage during all follow-up (D0-D35). MAIN CONCLUSIONS Artemisinin derivatives remained effective in the treatment of falciparum malaria during first 12-years of use in north area of Brazil.
Descritores: Plasmodium falciparum
Artemisininas
-Resistência a Medicamentos
Controle de Doenças Transmissíveis
Estudos de Coortes
Limites: Humanos
Responsável: BR1.1 - BIREME


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Id: biblio-839493
Autor: Ye, Xuan-Yi; Ling, Qing-Zhi; Chen, Shao-Jun.
Título: Identification of neprilysin as a potential target of arteannuin using computational drug repositioning
Fonte: Braz. J. Pharm. Sci. (Online);53(2):e16087, 2017. tab, graf.
Idioma: en.
Projeto: Zhejiang Provincial Natural Science Foundation of China; . Ningbo Municipal Natural Science Foundation; . Administration of Traditional Chinese Medicine of Zhejiang Province.
Resumo: ABSTRACT The discovery of arteannuin (qinghaosu) in the 20th Century was a major advance for medicine. Besides functioning as a malaria therapy, arteannuin is a pharmacological agent in a range of other diseases, but its mechanism of action remains obscure. In this study, the reverse docking server PharmMapper was used to identify potential targets of arteannuin. The results were checked using the chemical-protein interactome servers DRAR-CPI and DDI-CPI, and verified by AutoDock Vina. The results showed that neprilysin (also known as CD10), a common acute lymphoblastic leukaemia antigen, was the top disease-related target of arteannuin. The chemical-protein interactome and docking results agreed with those of PharmMapper, further implicating neprilysin as a potential target. Although experimental verification is required, this study provides guidance for future pharmacological investigations into novel clinical applications for arteannuin.
Descritores: Simulação por Computador/classificação
Neprilisina/farmacologia
Artemisininas/análise
-Reposicionamento de Medicamentos/estatística & dados numéricos
Responsável: BR1.1 - BIREME


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Id: biblio-911265
Autor: Okunlola, A. I; Okunlola, C. K; Okani, C. O; Adewole, O. S; Ofusori, D. A; Komolafe, O. A; Ojo, S. K; Bejide, R. A; Ayoka, A. O; Ojewole, J. A. O.
Título: Histological studies on the retina and cerebellum of Wistar rats treated with ArteetherTM
Fonte: Braz. j. morphol. sci = Rev. bras. ciênc. morfol;31(1):28-32, 1/3/2014. ilus.
Idioma: en.
Resumo: Introduction: Arteether TM, a derivative of artemisinin, is among the recent drugs that have given renewed hope for combating malarial menace. The present study investigated the effects of arteetherTM on the histology of the retina and cerebellum of Wistar rats. Materials and Methods: Twenty adult albino Wistar rats weighing 150-200 g, were randomly divided into four groups (A, B, C and D) of five animals each and used for this study. Group A rats were given intramuscular (i.m.) arteetherTM (3 mg/kg b.w.) daily for 3 days. Group B rats were given i.m. arteetherTM (6 mg/kg b.w.) daily for 3 days. Group C rats were also given i. m. of arteetherTM (3 mg/kg b. w.) daily for 3 days, and the same dose was repeated at two-weekly intervals for 4 further weeks; while Group D rats which received normal saline (0.9 % w/v, 3 ml/kg b.w.), served as controls. At the end of the experiment, the rats were sacrificed by cervical dislocation. The retina and cerebellum were excised and processed routinely for histopathology changes, using haematoxylin and eosin stain (H & E), as well as Nissl stain. Results: Results obtained showed normal cellular components of the retina and cerebellum in all groups, and no cyto-pathological changes were observed. Conclusion: Thus, this study showed that under light microscopic examination, therapeutic doses of arteetherTM caused no significant cyto-pathologic changes in the retina and cerebellum of Wistar rats.(AU)
Descritores: Retina/anatomia & histologia
Cerebelo/anatomia & histologia
Artemisininas/farmacologia
Malária/prevenção & controle
-Técnicas Histológicas
Ratos Wistar
Limites: Animais
Ratos
Responsável: BR1.1 - BIREME


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Id: biblio-906979
Autor: Brasil. Ministério da Saúde. Secretaria de Ciência, Tecnologia e Insumos Estratégicos.
Título: Desinvestimento do medicamento artemeter para o tratamento de Malária Grave / Disinvestment of the drug artemether for the treatment of Serious Malaria.
Fonte: Brasília; CONITEC; out. 2017. tab.
Idioma: pt.
Resumo: CONTEXTO: A malária é uma doença parasitária infecciosa aguda causada por protozoários do gênero Plasmodium e representa um grave problema de saúde pública. No Brasil, há três espécies associadas à malária em seres humanos: P. falciparum, P. vivax e P. malariae. O demandante solicitou o desinvestimento do medicamento artemeter 80 mg/ml, mantendo apenas o artesunato 60 mg/ml como opção de tratamento injetável com derivado de artemisinina para malária grave. A recomendação de retirada do artemeter fundamenta-se em orientação do guia de tratamento da Organização Mundial de Saúde (OMS), publicado em 2015, que orienta que o tratamento de adultos e crianças com malária grave (incluindo as gestantes em todos os trimestres e mulheres lactantes) deve ser feito, preferencialmente, com artesunato intravenoso ou intramuscular. TECNOLOGIA SOLICITADA PARA DESINVESTIMENTO: Artemeter 80 mg/ml.: Tratamento da malária grave. EVIDÊNCIAS CIENTÍFICAS: Com o objetivo de avaliar se artesunato injetável é uma melhor opção terapêutica que o artemeter injetável para o tratamento da malária grave, em termos de eficácia, efetividade e segurança, foram pesquisadas evidências científicas comparando os dois medicamentos. Foi selecionada uma revisão sistemática da Cochrane que mostrou que o risco de mortalidade por todas as causas foi significativamente menor com o artesunato do que com o artemeter. O artesunato reduziu o risco de hipoglicemia, como evento adverso aos tratamentos, em relação ao artemeter. Não houve diferenças significativas entre os tratamentos na resolução do coma, no tempo para clearance do parasita e no tempo para desaparecimento da febre. IMPACTO ORÇAMENTÁRIO: Embora o custo de tratamento com artesunato 60 mg/mL seja maior do que com o artemeter 80 mg/ml, o demandante informou que não vai aumentar a quantidade de artesunato comprada, visto que os casos de malária grave estão diminuindo. RECOMENDAÇÃO DA CONITEC: Pelo exposto, os membros do Plenário da CONITEC, presentes na 56ª reunião ordinária, deliberaram que o tema fosse submetido à consulta pública com recomendação preliminar favorável ao desinvestimento do artemeter para tratamento da malária grave. CONSULTA PÚBLICA: Foi recebida somente 1 contribuição sobre experiência de profissional de saúde que concordou totalmente com a recomendação da CONITEC. : Os membros da CONITEC deliberaram por recomendar a exclusão do medicamento artemeter para o tratamento de malária grave. DECISÃO: A Portaria nº 42, de 9 de outubro de 2017, tornou pública a decisão de excluir o medicamento artemeter para o tratamento de Malária Grave, no âmbito do Sistema Único de Saúde ­ SUS.(AU)
Descritores: Artemisininas/efeitos adversos
Artemisininas/uso terapêutico
Recall de Medicamento
Malária/tratamento farmacológico
-Brasil
Análise Custo-Benefício
Avaliação da Tecnologia Biomédica
Sistema Único de Saúde
Limites: Humanos
Tipo de Publ: Revisão
Relatório Técnico
Estudo de Avaliação
Responsável: BR1.1 - BIREME



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