Bacterial resistance has propelled one of the most serious public health problems in the world. In this sense, drug repurposing has emerged for faster identification of effective drugs. The aim of this study was to investigate the repurposing of escitalopram oxalate and clonazepam drugs individually and in combination with antibiotics ciprofloxacin and sulfamethoxazole-trimethoprim to treat multidrug-resistant microorganisms (MDR) and to evaluate the chemical nuclease capacity. The minimum inhibitory concentration (MIC), minimum bactericidal concentration (MBC), fractional inhibitory concentration index (FICI) and tolerance level were determined against each microorganism tested. In vitro antibacterial activity was evaluated against forty-seven multidrug-resistant clinical isolates and eleven standard bacterial strains of the American Type Culture Collection (ATCC). Escitalopram oxalate was active mainly against Gram-positive and clonazepam against Gram-positive and Gram-negative bacteria. When associated with the two antibiotics mentioned, they had a significant synergistic effect. Clonazepam was able to cleave plasmid DNA and the mechanisms involved were oxidative and hydrolytic. These results allow us to suggest repurposing these non-antibiotic drugs to treat bacterial infections. However, further studies on the mechanism of action of these drugs should be performed, including to increase safety in use.
Objetivo: avaliar as toxicidades mais frequentes baseadas nos efeitos do 5-fluorouracil em pacientes com neoplasia colorretal submetidos à quimioterapia com 5-fluorouracil em associação com ácido folínico, oxaliplatina (FOLFOX) e irinotecano (FOLFIRI). Métodos: Estudo transversal conduzido em uma instituição pública brasileira em pacientes com diagnóstico prévio de câncer colorretal que receberam ciclos de quimioterapia infusional durante 48 horas a cada duas semanas, num total de 12 ciclos ou 24 semanas de tratamento. As variáveis estudadas foram obtidas pela revisão dos prontuários, através de um levantamento no serviço de arquivo médico e estatístico (SAME). Resultados: A idade variou de 35 a 84 anos com média total de 60,75 anos, sendo 56,25% do gênero feminino e 43,75% do masculino. As toxicidades mais comumente observadas foram náuseas, dor no estômago e fraqueza muscular. Nenhum paciente se encontrava nos estádios 0 e I, 25% (n= 4) em II, 31,25% (n= 5) em III e 43,75% (n= 7) em IV. Conclusões: Nota-se que as fluorpirimidinas continuam a ser o pilar no tratamento do câncer. Sendo assim, nessa perspectiva a identificação da atividade enzimática da Dihidropirimidina Desidrogenase (DPD) está fortemente relacionada a farmacologia do 5-FU, com isso, a determinação desta enzima antes no início da terapia tem-se demonstrado fundamental para identificar pacientes com alto risco de doença grave e toxicidade potencialmente fatal.
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