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1.
Braz. j. infect. dis ; 21(1): 79-87, Jan.-Feb. 2017. tab, graf
Artigo em Inglês | LILACS | ID: biblio-839188

RESUMO

Abstract The current increment of invasive fungal infections and the availability of new broad-spectrum antifungal agents has increased the use of these agents by non-expert practitioners, without an impact on mortality. To improve efficacy while minimizing prescription errors and to reduce the high monetary cost to the health systems, the principles of pharmacokinetics (PK) and pharmacodynamics (PD) are necessary. A systematic review of the PD of antifungals agents was performed aiming at the practicing physician without expertise in this field. The initial section of this review focuses on the general concepts of antimicrobial PD. In vitro studies, fungal susceptibility and antifungal serum concentrations are related with different doses and dosing schedules, determining the PD indices and the magnitude required to obtain a specific outcome. Herein the PD of the most used antifungal drug classes in Latin America (polyenes, azoles, and echinocandins) is discussed.


Assuntos
Humanos , Antifúngicos/farmacocinética , Polienos/uso terapêutico , Polienos/farmacocinética , Aspergilose/metabolismo , Aspergilose/tratamento farmacológico , Azóis/uso terapêutico , Azóis/farmacocinética , Triazóis/uso terapêutico , Triazóis/farmacocinética , Candidíase/metabolismo , Candidíase/tratamento farmacológico , Testes de Sensibilidade Microbiana , Área Sob a Curva , Relação Dose-Resposta a Droga , Equinocandinas/uso terapêutico , Equinocandinas/farmacocinética , América Latina , Antifúngicos/uso terapêutico
2.
Braz. j. microbiol ; 47(4): 911-916, Oct.-Dec. 2016. tab
Artigo em Inglês | LILACS | ID: biblio-828186

RESUMO

Abstract Objective Candida albicans is the primary causative agent of oral candidosis, and one of its key virulent attributes is considered to be its ability to produce extracellular phospholipases that facilitate cellular invasion. Oral candidosis can be treated with polyenes, and azoles, and the more recently introduced echinocandins. However, once administered, the intraoral concentration of these drugs tend to be sub-therapeutic and rather transient due to factors such as the diluent effect of saliva and cleansing effect of the oral musculature. Hence, intra-orally, the pathogenic yeasts may undergo a brief exposure to antifungal drugs. We, therefore, evaluated the phospholipase production of oral C. albicans isolates following brief exposure to sub-therapeutic concentrations of the foregoing antifungals. Materials and methods Fifty C. albicans oral isolates obtained from smokers, diabetics, asthmatics using steroid inhalers, partial denture wearers and healthy individuals were exposed to sub-therapeutic concentrations of nystatin, amphotericin B, caspofungin, ketoconazole and fluconazole for one hour. Thereafter the drugs were removed and the phospholipase production was determined by a plate assay using an egg yolk-agar medium. Results The phospholipase production of these isolates was significantly suppressed with a percentage reduction of 10.65, 12.14, 11.45 and 6.40% following exposure to nystatin, amphotericin B, caspofungin and ketoconazole, respectively. This suppression was not significant following exposure to fluconazole. Conclusions Despite the sub-therapeutic, intra oral, bioavailability of polyenes, echinocandins and ketoconazole, they are likely to produce a persistent antifungal effect by suppressing phospholipase production, which is a key virulent attribute of this common pathogenic yeast.


Assuntos
Humanos , Fosfolipases/biossíntese , Candida albicans/efeitos dos fármacos , Candida albicans/metabolismo , Candidíase Bucal/microbiologia , Candidíase Bucal/tratamento farmacológico , Antifúngicos/farmacologia , Polienos/uso terapêutico , Polienos/farmacologia , Azóis/uso terapêutico , Azóis/farmacologia , Candida albicans/isolamento & purificação , Candida albicans/patogenicidade , Fumar , Testes de Sensibilidade Microbiana , Dentaduras , Fatores de Virulência , Diabetes Mellitus , Ativação Enzimática , Espaço Extracelular , Equinocandinas/farmacologia , Antifúngicos/uso terapêutico
3.
Rev. chil. pediatr ; 86(4): 287-290, ago. 2015. ilus, graf
Artigo em Espanhol | LILACS | ID: lil-764087

RESUMO

Introducción: La telorragia es un síntoma poco frecuente en pacientes pediátricos, la causa más frecuente en esta población es la ectasia ductal mamaria (EDM), que es una afección benigna y autolimitada, caracterizada por la dilatación del conducto mamario, fibrosis e inflamación periductal. Objetivo: Presentar un caso de EDM, para facilitar el rápido reconocimiento por parte de los médicos, y evitar estudios y tratamientos agresivos. Caso clínico: Lactante de sexo masculino de 6 meses de edad, sano, alimentado por lactancia materna exclusiva; consultó por un nódulo retroareolar derecho y telorragia unilateral. Se realizó una ecografía Doppler que mostró una lesión multiquística, sugerente de una EDM. Se planteó tratamiento expectante y acudió a control a los 6 meses con excelente evolución. Conclusiones: La EDM es la principal causa de telorragia en niños, corresponde a una afección benigna, y la resolución generalmente es espontánea, antes de los 9 meses. Por lo que su conocimiento es de gran relevancia para el adecuado diagnóstico y manejo de estos pacientes.


Introduction: Bloody nipple discharge is an infrequent symptom during childhood. The most common cause in this population is mammary duct ectasia (MDE), which is a benign and self-limiting condition, that is characterized by dilatation of the mammary ducts, fibrosis and periductal inflammation. Objective: Report of a case of MDE in order to improve physicians’ diagnosis accuracy and avoid aggressive studies and treatments. Case report: Six-months old male healthy infant, exclusively breastfeeded, that visited our clinic with a lump beneath his right nipple and bloody discharge from the same nipple. An ultrasound was performed which showed a multicystic lesion suggestive of MDE. Watchful waiting was decided as treatment, with good evolution after six months of follow up. Conclusions: The MDE is the leading cause of bloody discharge in pediatric population, being a benign condition that resolves spontaneously before nine months. The knowledge of this condition is essential so as to accurately diagnose and treat it.


Assuntos
Humanos , Cátions/química , Indicadores e Reagentes/química , Lipídeos/química , Polienos/química , RNA Interferente Pequeno/química , Linhagem Celular Tumoral , Química Farmacêutica/métodos , Técnicas de Transferência de Genes , Vetores Genéticos/genética , Células HeLa , Lipossomos/química , Luciferases/química , Fosfolipídeos/química , RNA Interferente Pequeno/genética , Transfecção/métodos
5.
Rev. bras. oftalmol ; 72(2): 132-141, mar.-abr. 2013. ilus, tab
Artigo em Português | LILACS | ID: lil-678383

RESUMO

O tratamento das infecções oculares por fungos representa um desafio à prática oftalmológica. Para obtermos resposta terapêutica adequada, além do uso da droga correta, é necessária a administração desta de forma eficaz. Este manuscrito reúne informações a respeito das principais drogas antifúngicas utilizadas em infecções oculares, suas concentrações e principais vias de administração.


Treatment of fungal eye infections represents a challenge to the ophthalmology practice. For an adequate therapeutic response, besides correct drug choice, it is necessary an effectively administration. This script gathers information about the major antifungal drugs used in eye infections, their concentrations and main administration routes.


Assuntos
Humanos , Antifúngicos/administração & dosagem , Antifúngicos/uso terapêutico , Interações Medicamentosas , Infecções Oculares Fúngicas/tratamento farmacológico , Azóis/administração & dosagem , Azóis/uso terapêutico , Equinocandinas/administração & dosagem , Equinocandinas/uso terapêutico , Pirimidinas/administração & dosagem , Pirimidinas/uso terapêutico , Polienos/administração & dosagem , Polienos/uso terapêutico
6.
Braz. j. infect. dis ; 12(5): 400-404, Oct. 2008. ilus, graf, tab
Artigo em Inglês | LILACS | ID: lil-505354

RESUMO

Voriconazole is a novel broad-spectrum antifungal drug, employed in the treatment of invasive fungal infections, and represents an alternative to amphotericin B treatment. The manufacturer recommends that any unused reconstituted product should be stored at 2ºC to 8ºC, for no more than 24 h, but no recommendations about i.v. infusion solutions are given. Previous works have reported on the stability of voriconazole in polyolefin bags and just one in 5 percent dextrose polyvinyl chloride (PVC) bags, at a 4 mg.mL-1 concentration. In this work, the stability of voriconazole as an i.v. infusion solution in 0.9 percent sodium chloride and in 5 percent dextrose, in PVC bags, at 0.5 mg.mL-1, stored at 4 ºC and at room temperature, protected from light, was evaluated. These infusion solutions were analyzed for a 21-day period. Chemical stability was evaluated by HPLC assay. Visual inspection was performed and pH of the solutions was measured. No color change or precipitation in the solutions was observed. The drug content remained above 90 percent for 11 days in 0.9 percent sodium chloride and for 9 days in 5 percent dextrose solutions. The i.v. infusion solutions stored at room temperature were not stable. At room temperature, the voriconazole content dropped down to 88.3 and 86.6 percent, in 0.9 percent sodium chloride or 5 percent dextrose solutions, respectively, two days after admixture. Assays performed at the end of the study suggest the sorption of voriconazole by the PVC bags. The results of this study allow cost-effective batch production in the hospital pharmacy.


Assuntos
Antibacterianos/química , Embalagem de Medicamentos/instrumentação , Polienos , Cloreto de Polivinila , Pirimidinas/química , Triazóis/química , Antibacterianos/administração & dosagem , Cromatografia Líquida de Alta Pressão , Estabilidade de Medicamentos , Embalagem de Medicamentos/economia , Armazenamento de Medicamentos/métodos , Concentração de Íons de Hidrogênio , Infusões Parenterais/economia , Infusões Parenterais/instrumentação , Micoses/tratamento farmacológico , Pirimidinas/administração & dosagem , Fatores de Tempo , Triazóis/administração & dosagem
7.
Rev. cuba. farm ; 39(2)mayo-ago. 2005. ilus
Artigo em Espanhol | LILACS | ID: lil-439491

RESUMO

Evitar la proliferación de enfermedades fúngicas sigue siendo una ardua tarea para el siglo XXI, es por ello que continúa el desarrollo de nuevos antifúngicos cada vez más potentes. En la síntesis de estos fármacos es muy importante tener en cuenta la relación de su estructura-función, pues sobre la base de ellos se garantiza la muerte del hongo sin provocar graves daños al organismo hospedero. El presente trabajo es una revisión bibliográfica en la que se plantean las clasificaciones, mecanismo de acción, la estructura de varios de estos fármacos, algunos muy conocidos y otros en vías de desarrollo, su interacción con el sitio activo y se compara la actividad así como la toxicidad de muchos antifúngicos


Assuntos
Alilamina , Antifúngicos , Azóis , Peptídeos , Polienos , Pirimidinas
8.
RBCF, Rev. bras. ciênc. farm. (Impr.) ; 39(2): 149-158, abr.-jun. 2003. tab, graf
Artigo em Português | LILACS | ID: lil-348744

RESUMO

Várias amostras de solo do Brasil foram semeadas em placas de ágar e diversas cepas de actinomicetos produtoras de antibióticos antifúngicos foram isoladas. Foram desenvolvidos meios para eliciação da biossíntese dos antibióticos e métodos para determinação rápida do seu rendimento. Ao todo, foram isoladas 41 cepas de actinomicetos aeróbios produtoras de metabólitos antifúngicos. Destes, 11 (26,8 por cento) eram macrolídeos tetraênicos, 13 (31,7 por cento) macrolídeos pentaênicos, 1 (2,4 por cento) macrolídeo oxopentaênico, 1 (2,4 por cento) macrolídeo hexaênico e 6 (14,6 por cento) macrolídeos heptaênicos. Os antibióticos antifúngicos produzidos pelas restantes 9 cepas ativas (21,9 por cento) não eram poliênicos


Assuntos
Actinomycetales , Antibacterianos , Antifúngicos , Meios de Cultura , Polienos , Espectrofotometria
9.
Rev. chil. infectol ; 19(supl.1): S22-S25, 2002.
Artigo em Espanhol | LILACS | ID: lil-314906
12.
Braz. j. med. biol. res ; 26(10): 1105-10, Oct. 1993. tab, graf
Artigo em Inglês | LILACS | ID: lil-148788

RESUMO

Rapamycin is a macrolide antibiotic whose potent immunosuppressor activity was recently described in vivo and in vitro. The aim of the present work was to determine if rapamycin could affect an established inflammatory response. Conscious pathogen-free Dunkin-Hartley guinea pigs (300-400 g) were injected intravenously with Sephadex beads (G50, superfine, 10 to 40 microns, 24 mg/kg) to induce lung inflammation and bronchial hyperreactivity. Bronchoalveolar lavage (BAL) fluid was collected 2, 12 and 24 h after Sephadex administration and the cells were counted. Bronchial tissue was used to construct dose-response (contraction, g) curves to histamine and acetylcholine 24 h after the Sephadex injection, using a cascade system. Results are presented as area under the log dose-response curves. Test animals were injected with rapamycin (5 mg/kg) or its vehicle by the intramuscular route either 2 or 12 h after Sephadex injection and BAL fluid collected 24 h after Sephadex administration. Rapamycin administration 2 h after Sephadex reduced eosinophil and lymphocyte numbers in BAL by 52 and 55 per cent , respectively, but not ex vivo bronchial hyperreactivity induced by Sephadex injection. However, rapamycin administration 12 h after Sephadex reduced BAL eosinophil and lymphocyte numbers (55 and 62 per cent , respectively) and bronchial hyperreactivity. The increase in neutrophil numbers in BAL induced by Sephadex injection was not modified by rapamycin. Since lymphocyte numbers in BAL were significantly increased in Sephadex-treated animals at 12 h but not at 2 h after Sephadex injection, the present results suggest that the inhibition of bronchial hyperreactivity by rapamycin may be dependent on the presence of lymphocytes elicited into the airways by Sephadex injection


Assuntos
Animais , Cobaias , Hiper-Reatividade Brônquica/tratamento farmacológico , Pneumopatias/etiologia , Polienos/farmacologia , Contagem de Células , Dextranos , Esquema de Medicação , Hiper-Reatividade Brônquica/induzido quimicamente , Inflamação/induzido quimicamente , Líquido da Lavagem Broncoalveolar/citologia , Polienos/administração & dosagem
15.
Rev. microbiol ; 20(1): 102-7, jan.-mar. 1989. tab
Artigo em Português | LILACS | ID: lil-75271

RESUMO

Foram estudadas as incidências de leveduras isoladas de pacientes com câncer e submetidos a radioterapia ou a quimioterapia e a sensibilidade destes fungos a antibióticos poliênicos. De 227 desses pacientes, também com suspeita clínica de micose, foram desses pacientes, também com suspeita clínica de micose, foram isoladas 200 cepas que incluiam apenas espécies de Candida. C. albicans foi a espécie de maior incidência (87.5%), seguindo-se C. tropicalis (9.0%), C. parapsilosis (6.0%), C. brusei (4,0%), C. guilliermondii, C. pseudotropicalis (3,0% e C. famata (1,0%). Em concentracöes dos antibióticos consideradas eficazes para amostras sensíveis, todas as leveduras foram inibidas pela nistatina (8 microng/ml) e 97,4% o foram pela anfotericina B (2 microng/ml) e pela pimaricina (10microng/ml). Nessas concentraçöes, 10,6% das leveduras mostraram-se resistentes a açäo letal da nistatina, 32,6% a da anfotericina B e 38,7% a da pimaricina


Assuntos
Humanos , Masculino , Feminino , Polienos/farmacologia , Leveduras/isolamento & purificação , Candida albicans/isolamento & purificação , Micoses/diagnóstico , Neoplasias/microbiologia , Candida/isolamento & purificação , Nistatina/farmacologia
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