Anti-inflammatory and antialgic actions of a nanoemulsion of Rosmarinus officinalis L. essential oil and a molecular docking study of its major chemical constituents.

We evaluate the anti-inflammatory and antialgic potency of a nanoemulsion (NEORO) containing the essential oil of Rosmarinus officinalis L. (EORO), which is composed primarily of limonene, camphor and 1,8-cineole. The EORO and NEORO were administered orally 30 min prior to starting the experiments. In a test of rat paw oedema induced by carrageenan, NEORO was effective in doses of 498 µg/kg, and it inhibited 46% of the maximum peak of the oedema; in a dose of 300 mg/kg, EORO inhibited 50% of the maximum peak of the oedema. In an acetic acid-induced writhing test, NEORO yielded a dose-dependent effect, and a dose of 830 µg/kg inhibited 84% of the algesic process; a dose of 100 mg/kg of EORO inhibited 55%. In an assay for H2S production in rat stomachs, a dose of 498 µg/kg of NEORO inhibited H2S production in all of the measurement phases, and a dose of 100 mg/kg EORO inhibited 60% and influenced the effect of the ethanol significantly, reducing the production of H2S. We suggest that NEORO potentiated the effect of EORO, demonstrating effectiveness in doses 600 times lower than those applied with EORO. Among the major compounds of EORO, the camphor molecule exhibited the largest number of interactions with the therapeutic targets related to the inflammatory process, suggesting that it is responsible for EORO's anti-inflammatory and antialgic effects. This work paves the way for future investigations related to the therapeutic role of NEORO in the inflammation process.

Molecular modeling of inhibitors against fructose bisphosphate aldolase from Candida albicans.

Candida albicans is an opportunistic pathogen that causes from vulvovaginal and oropharyngeal candidiasis to systemic infections. The enzyme 1,6-fructose bisphosphate aldolase class II (FBA II), is a macromolecule existing only in lower organisms, being essential for the survival of the pathogen due to its function of maintaining the glycolysis process. The aim of this paper was to evaluate the inhibitors of FBA II regarding their physicochemical, pharmacokinetic and toxicological properties and apply concepts of rational drug development to propose new compounds for the treatment of fungal infections of C. albicans. Physicochemical (HyperChem software and the webserver cactus) and ADME/Tox (PreADMET webserver) properties were calculated to four inhibitors described in the literature and three analogues. None of the compounds presented in this study violated RO5, however all inhibitors demonstrated low or moderate human intestinal absorption (HIA), as well as low or moderate permeability in Caco-2 and MDCK, poor plasma proteins binding (PPB) and low permeability of the blood-brain barrier (BBB); however, Compound 4 is the exception for BBB permeability, being also the only non-mutagenic compound, and therefore, used as a lead compound. Analogues B and C presented high HIA, weak PPB and low BBB permeability, as well as a positive prediction for carcinogenicity in rats and mouse and non-mutagenicity in the Ames test. Through the evaluations carried out, it was concluded that the analogues B and C have proved to be promising candidates for oral administration drugs in the treatment of fungal infections of the genus Candida.

Interações medicamentosas e consequentes intervenções farmacêuticas na Unidade de Terapia Intensiva de um hospital privado em Macapá, Amapá / Interactions medicative and consequents interventions pharmaceutics in the unity of intensive therapy in a private hospital in Macapa, Amapa

Introdução: Pacientes internados em Unidades de Terapia Intensiva (UTI) são submetidos a tratamentos com múltiplos fármacos, visto a gravidade dos problemas que são tratados. A interação medicamentosa é definida como um evento causado pela modificação do efeito ou aproveitamento de um fármaco no organismo em virtude de outro. A avaliação das potenciais interações medicamentosas pode auxiliar a equipe multiprofissional a promover um tratamento de qualidade, evitando que estas interações sejam danosas ao paciente, diminuindo o tempo de internação e consequentemente auxiliando na redução de custos. Objetivo: Avaliar as principais interações medicamentosas observadas nas UTI de um hospital privado na cidade de Macapá (Amapá, AP) através da análise das prescrições e das consequentes intervenções adotadas a fim de minimizar seus riscos. Método: Foram avaliadas prescrições de pacientes internados em UTI quanto à presença de potenciais interações medicamentosas e sua respectiva classificação, segundo seu risco e mecanismo. As principais interações foram destacadas a fim de destacar seu mecanismo e medidas adotadas pela equipe multidisciplinar. Resultados: Observou-se que a maioria das interações, tanto na UTI adulto quanto na UTI neonatal, foram consideradas de risco moderado. As interações farmacocinéticas foram mais comuns na UTI adulto, enquanto as farmacodinâmicas predominaram na UTI neonatal. O manejo no horário de administração dos medicamentos foi a intervenção mais adequada para a maioria dos casos das interações medicamentosas. Conclusões: o monitoramento das potenciais interações em pacientes críticos procura garantir a segurança do paciente, buscando diminuir os riscos potenciais aos quais estes estão expostos.

Introduction: Patients admitted to Intensive Care Units (ICU) are submitted to multiple drug treatments, considering the severity of their problems. Drug interaction is defined as an event caused by the modification of the effect or use of a drug in the body. The evaluation of potential drug interactions can help the multiprofessional team to promote a quality treatment, avoiding harmful interactions, reducing the length of hospitalization and consequently reducing costs. Objective: To evaluate the main drug interactions observed in the ICUs of a private hospital in the city of Macapá, Brazil, through the analysis of the prescriptions and the consequent interventions adopted in order to minimize their risks. Method: Prescriptions of patients admitted to the ICU were evaluated for the presence of potential drug interactions and their respective classification according to their risk and mechanism. A brief bibliographic study about the main interactions was carried out in order to highlight its mechanism and the measures adopted by the multidisciplinary team. Results: We observed that the majority of the interactions, both in the adult ICU and in the neonata ICU, were considered of moderate risk. Pharmacokinetic interactions were more common in the adult ICU, while pharmacodynamics predominated in the neonatal intensive care unit. Management during the administration of medications was the most appropriate intervention for most cases of drug interactions. Conclusions: Monitoring of potential interactions in critically ill patients seeks to ensure patient safety in order to reduce the potential risks to which they are exposed.