Revista Colombiana de Ciencias Químico - Farmacéuticas

Influence of silymarin and chromium picolinate on the pharmacotherapy of rats with induced diabetes

SUMMARY Food supplements are easily acquired and used in various countries. Silymarin has been indicated for diseases of the liver and Chromium picolinate has been indicated for body weight loss and for the improvement of glycemic index. The objective of the present study was to assess the effects of short-term treatment with a combination of silymarin (50 mg/kg) and chromium picolinate (5 µg/kg) on the standard glibenclamide treatment (10 mg/kg) of rats with induced diabetes. DM2 was induced with streptozotocin. Experimental groups of rats: healthy control group, glibenclamide diabetic group, silymarin diabetic group, and silymarin, chromium picolinate and glibenclamide group. After 10 days of oral treatment, we determined body weight, fasting glycemia, glycemia 1 h after gastric gavage with sucrose, and AST and ALT transaminases. Statistical analysis of the data indicated that there was no change in body weight or fasting glycemia, but that glycemia increased after gavage with sucrose in the group submitted to combined therapy. Thus, we concluded that the combination of silymarin and chromium picolinate reduced the efficacy of glibenclamide in the short term, although the two substances had a protective effect on the liver as observed by the reduction of blood transaminase levels.

RESUMO Suplementos alimentares são de fácil aquisição e uso em diversos países. A silimarina tem sido indicada para desordens hepáticas e o picolinato de cromo tem sido utilizado para perda de peso corporal e melhoria do índice glicêmico. O objetivo deste trabalho foi avaliar os efeitos do tratamento utilizando uma combinação de silimarina (50 mg/kg) e picolinato de cromo (5 µg/kg) sobre o tratamento com glibencla-mida (10 mg/kg) em ratos com diabetes induzida com estreptozotocina. Os grupos experimentais foram: grupo controle sadio, grupo diabético glibenclamida, grupo diabético silimarina e grupo diabético silimarina, picolinato de cromo e glibencla-mida. Após 10 dias de tratamento via oral, determinou-se o peso corpóreo, glicemia de jejum, glicemia após uma hora de gavagem gástrica com sacarose e transaminases hepáticas. A análise estatística dos dados indicou que não ocorreu alteração significativa no peso corpóreo e na glicemia de jejum, mas ocorreu aumento significativo dos níveis glicêmicos no grupo diabético silimarina, picolinato de cromo e glibenclamida após a gavagem com sacarose no grupo com a terapia combinada. Portanto, conclui-se que a combinação utilizada reduziu a eicácia da glibenclamida em curto prazo, embora ambas substancias tenham exibido efeito hepatoprotetor, observado pela redução dos níveis plasmáticos de transaminases.

Optimizing pharmacotherapy through deprescription: Case report

RESUMEN La polifarmacia es el uso simultáneo o excesivo de varios medicamentos y ha presentado una tendencia al aumento durante los últimos años, al igual que los cuadros clínicos asociados a interacciones farmacológicas secundarias, llevando así a adicionar cada vez más medicamentos, esto genera el fenómeno de cascada en la prescripción. En este artículo se presenta un caso de una mujer de 34 años, identificado desde una plataforma transaccional de registro de medicamentos prescritos de una EPS, a quien se realizó seguimiento de su tratamiento farmacológico ambulatorio durante 7 meses, en los cuales presentó persistencia de polifarmacia. Se identificó en el caso posibles errores en medicación y posibles ajustes a la terapia que disminuirían el riesgo de interacciones o cascada de prescripción.

SUMMARY Polypharmacy is the simultaneous use or excess of dosage of medicines and it has shown a tendency to increase in recent years, as well as the clinical symptoms associated with secondary drug interactions, thus leading to the addition of more and more medications, generating the cascade phenomenon of prescription. We present a case of a 34-year-old woman, identified from a transactional platform of registration of prescribed drugs of an EPS, who was followed up on her outpatient pharmacological treatment for 7 months, in which she presented persistent polypharmacy. It was identified in the case possible errors in medication and possible adjustments to the therapy that would decrease the risk of interactions or prescription cascade.

Study of the chemical composition, toxicity and molluscicidal activity of the essential oil Citrus sinensis (L.) Osbeck

RESUMO Determinamos a composição química e testamos a toxicidade e a atividade moluscicida do óleo essencial extraído das cascas do Citrus sinensis (L.) Osbeck. Para isso, o óleo essencial foi extraído quantitativamente por hidrodestilação. Em seguida, as quantificações de seus componentes foram realizadas por cromatografía gasosa acoplada à espectrometria de massas (CG-MS) e a toxicidade e atividade moluscicida foram testadas, respectivamente, contra Artemia salina e caramujos Biomphalaria glabrata. Os resultados mostraram que o óleo contém 81,50% de D-limoneno (constituinte principal) e 0,06% de citronelal (componente menor) e este possui atividade moluscicida com concentração letal (CL50) de 100,08 mg.L-1 e atoxicidade, com CL50 de 321,84 mg.L-1 a um nível de confiança de 95%. Portanto, o óleo é ativo contra o caramujo Biomphalariaglabrata e atóxico para outros seres vivos.

SUMMARY In this present study, we determined the chemical composition and we tested the toxicity and the molluscicidal activity of the essential oil extracted from the barks of Citrus sinensis (L.) Osbeck. For this, the essential oil was extracted quantitatively by hydrodistillation. Then, quantifications of its components were performed by gas chromatography coupled to mass spectrometry (CG-MS) and the toxicity and molluscicidal activity were tested, respectively, against Artemia salina and snails Biomphalaria glabrata. The results showed that the oil contains 81.50% of D-limonene (main constituent) and 0.06% of citronellal (minor component) and it has lethal activity (LC50) of 100.08 mg.L-1 and a toxicity, with LC50 of321.84 mg.L -1 at a 95% confidence level. Therefore, the oil is active against the snail Biomphalaria glabrata and non-toxic to other living bein.

Thymol, menthol and eucalyptol as agents for microbiological control in the oral cavity: A scoping review

SUMMARY Dental plaque is a complex environment that maintains a balance with certain microbial communities; however, this microhabitat can be disturbed by some endogenous species causing disease. An exploratory systematic review was carried out using the PubMed, Scopus, Lilacs, and Science Direct databases, identifying that the thymol, menthol, and eucalyptol compounds present varying antimicrobial activity, intra- and interspecies discordance, and a strong antimicrobial intensity on Aggregatibacter actinomycetemcomitans, Candida albicans, Candida dubliniensis, Enterococcus faecalis, Escherichia coli, Lactobacillus plantarum, and Streptococcus mutans, indicating that these phytochemicals can be considered broad-spectrum antimicrobial substances, with an effect on microorganisms linked to oral diseases.

RESUMEN La placa dental es un ambiente complejo que mantiene un equilibrio con determinadas comunidades microbianas; sin embargo, este micro hábitat puede ser perturbado por algunas especies endógenas causando enfermedad. Se realizó una revisión sistemática exploratoria empleando las bases de datos Pubmed, Scopus, Lilacs y Science Direct y se identificó que los compuestos timol, mentol y eucaliptol presentan actividad antimicrobiana variable, discordancias intra e inter-especie y una intensidad antimicrobiana fuerte sobre Aggregatibacter actinomycetemcomitans, Candida albicans, Candida dubliniensis, Enterococcus faecalis, Escherichia coli, Lactobacillusplantarum and Streptococcus mutans; indicando que estos fitoquímicos pueden ser consideradas como sustancias antimicrobianas de amplio espectro, con efecto sobre microorganismos relacionados con enfermedades bucales.

A comparative study of extraction techniques for maximum recovery of bioactive compounds from Ganoderma lucidum spores

SUMMARY This study aimed at evaluating effective methods for breaking the hard and insoluble spores of Ganoderma lucidum to recover functional biomolecules. Rupture techniques were evaluated such as manual maceration (RM), maceration with spheres of various materials (BR), and microwave exposure plus maceration with steel/ chrome spheres (MBR1). Spore rupture was evaluated using UV-Vis spectroscopy, which showed vibrations of 2955, 1642, 1240, 1080 and 1746 cm-1 corresponding to changes in spore walls. The MBR1 extract contained the largest amounts of carbohydrates (19.80 mg.g-1 spores) and polyphenols (2.21 mg.g-1 spores), whereas the BR extract had higher antioxidant activity (57.22%Inb DPPH). The MBR1 and BR extracts contained 62.2 and 73.5% glucose, respectively. Both methods also involved significant extraction of carbohydrates and proteins. The best way to extract biomolecules from spore walls is to perform a microwave heat treatment and break the walls with steel/chrome spheres; this produces large quantities of carbohydrates with antioxidant properties.

RESUMEN El objetivo de este estudio fue evaluar varios métodos de ruptura de las esporas de Ganoderma lucidum y extraer sus propiedades bioactivas. Para este propósito se evaluaron diferentes técnicas de rompimiento como: la maceración manual (RM), la maceración con esferas de diversos materiales (BR) y la exposición a microondas junto la maceración de las esporas con esferas de acero/cromo (MBR1). La ruptura de las esporas fue evaluada por espectroscopia UV-Vis, la cual mostró que las vibraciones 2955, 1642, 1240, 1080 y 1746 cm-1 correspondieron a cambios estructurales en las paredes de las esporas. El extracto MBR1 presento el mayor contenido de carbohidratos (19,80 mg.g-1) y polifenoles (2,21 mg.g-1), mientras que el extracto BR tuvo una mayor actividad antioxidante (57,22% Inb DPPH). Los extractos MBR1 y BR también presentaron en el análisis de monosacáridos un 62,2 y 73,5% de contenido glucosa. Como conclusión la mejor metodología para extraer biomoléculas de las paredes de las esporas de G. lucidum fueron el tratamiento térmico con microondas y la ruptura de las paredes con esferas de acero/cromo, porque este proceso permitió la extracción de una mayor cantidad de carbohidratos con posibles propiedades antioxidantes.

Chemical composition and biological activity of the essential oil of the fruits Pimenta dioica against formae speciales of fungus Fusarium oxysporum

SUMMARY We determined the chemical composition and explored the hypothesis that the essential oil of the fruits of Pimenta dioica inhibits the mycelial development of fungi Fusarium oxysporum f. sp. lycopersici, F. oxysporum f. sp. passiflorae, F. subglutinans f. sp. ananas, F. oxysporum f. sp. vasinfectum e F. oxysporum f. sp. Cubense. To do this, we extracted the oil by hydrodistillation, identified its components by gas chromatography coupled to mass spectrometry (GC-MS) and determined the fungal activity against five special forms of Fusarium species. The results showed that the oil had 76.88% of eugenol and inhibited the mycelial development of fungi up to 97.78% in an average of 7.2 days. Therefore, oil is a potential natural fungicide.

RESUMEN Determinamos la composición química y exploramos la hipótesis de que el aceite esencial de los frutos de Pimenta dioica inhibe el desarrollo micelial de los hongos Fusarium oxysporum f. sp. lycopersici, F. oxysporum f. sp. passiflorae, F. subglutinans f. sp. ananas, F. oxysporum f. sp. vasinfectum e F. oxysporum f. sp. Cubense. Para hacer esto, extrajimos el aceite por hidrodestilación, identificamos sus componentes por cromatografía de gases acoplada a espectrometría de masas (GC-EM) y determinamos la actividad fúngica contra cinco formas especiales de especies de Fusarium. Los resultados mostraron que el aceite tenía 76,88% de eugenol e inhibió el desarrollo micelial de hongos hasta 97,78% en un promedio de 7,2 días. Por lo tanto, el aceite es un potencial fungicida natural.

Use of statins and the risk of developing pre-diabetes and diabetes: a longitudinal study in individuals aged 40 years or older

SUMMARY Background: Statins are the main therapeutic option for the control of dyslipidemias and cardiovascular prevention. However, studies indicate the possibility of the use of statins cause increases in blood glucose levels. Aim: The aim of the study was to analyze the use of statin and the risk of developing pre-diabetes (DM) or DM. Methods: This was a cohort study conducted with individuals aged 40 years or older, living in a medium-sized municipality in the north of Paraná, Brazil. Data were obtained through individual interviews and laboratory tests in the years 2011 (baseline) and 2015 (follow-up). Dependent variables were the development of DM (yes; no) and the development of pre-DM or DM (yes; no). The independent variable was the use of statins (no use; use only in 2011; use only in 2015; use in 2011 and 2015). Poisson (loglinear) regression analysis was used to calculate the relative risk (RR) and 95% confidence intervals (95% CI) in generalized linear models. Results: An association was observed between the use of statins and the incidence of DM (RR 2.89, 95% CI: 1.59-5.24) and the incidence of pre-DM or DM (RR 2.01, 95% CI: 1.39-2.92) for the group of individuals who used statins only in 2015. Conclusions: The present study identified an association between the use of statins and the incidence of pre-DM and DM only for those who used them exclusively in 2015.

RESUMO Introdução: As estatinas são a principal opção terapêutica para o controle de dislipidemias e prevenção cardiovascular. No entanto, estudos indicam a possibilidade do uso de estatinas causar aumentos nos níveis de glicose no sangue. Objetivo: O objetivo do estudo foi analisar o uso de estatina e o risco de desenvolver pré-diabetes (DM) ou DM. Métodos: Estudo de coorte realizado com indivíduos com 40 anos ou mais de idade, residentes em um município de médio porte no norte do Paraná. Os dados foram obtidos por meio de entrevistas individuais e exames laboratoriais nos anos de 2011 (linha de base) e 2015 (acompanhamento). As variáveis dependentes foram o desenvolvimento de DM (sim; não) e o desenvolvimento de pré-DM ou DM (sim; não). A variável independente foi o uso de estatinas (sem uso; uso apenas em 2011; uso apenas em 2015; uso em 2011 e 2015). A análise de regressão de Poisson (log-linear) foi utilizada para calcular o risco relativo (RR) e os intervalos de confiança de 95% (IC95%) em modelos lineares generalizados. Resultados: Observou-se associação entre o uso de estatinas e a incidência de DM (RR 2,89, IC 95%: 1,59-5,24) e a incidência de pré-DM ou DM (RR 2,01, IC 95%: 1,39-2,92) para o grupo de indivíduos que usaram estatinas apenas em 2015. Conclusões: O presente estudo identificou associação entre o uso de estatinas e a incidência de pré-DM e DM apenas para aqueles que as usaram exclusivamente em 2015.

RESUMEN Introducción: las estatinas son la principal opción terapéutica para el control de la dislipidemia y la prevención cardiovascular. Sin embargo, los estudios indican la posibilidad de que el uso de estatinas pueda causar aumentos en los niveles de glucosa en sangre. Objetivo: analizar el uso de estatinas y el riesgo de desarrollar prediabetes (DM) o DM. Métodos: estudio de cohorte realizado con individuos de 40 años o más, que viven en un municipio de tamaño medio en el norte de Paraná, Brasil. Los datos se obtuvieron mediante entrevistas individuales y pruebas de laboratorio en los años 2011 (línea de base) y 2015 (seguimiento). Las variables dependientes fueron el desarrollo de DM (sí; no) y el desarrollo de pre-DM o DM (sí; no). La variable independiente fue el uso de estatinas (sin uso; uso solo en 2011; uso solo en 2015; uso en 2011 y 2015). El análisis de regresión de Poisson (log-lineal) se utilizó para calcular el riesgo relativo (RR) y los intervalos de confianza del 95% (IC del 95%) en modelos lineales generalizados. Resultados: Se observó una asociación entre el uso de estatinas y la incidencia de DM (RR 2,89, IC 95%: 1,59-5,24) y la incidencia de pre-DM o DM (RR 2,01, IC 95%: 1,39-2,92) para el grupo de individuos que usaron estatinas solo en 2015. Conclusiones: el presente estudio identificó una asociación entre el uso de estatinas y la incidencia de pre-DM y DM solo para aquellos que las usaron exclusivamente en 2015.

Drug discovery based on live cell imaging

RESUMEN El diseño eficiente de compuestos aprovechando las características estructurales de las moléculas y la búsqueda eficiente de dianas terapéuticas, ha proporcionado herramientas efectivas en la investigación de nuevos tratamientos cuando esta se enfoca en mecanismos celulares de la enfermedad. Los cambios fenotípicos producidos por la interacción in vitro entre molécula-diana, pueden controlarse cuantitativamente mediante imagenología de células vivas. Para garantizar una interacción adecuada, es necesario considerar diferentes elementos cruciales: 1. Las características estructurales y la dinámica molecular del compuesto a evaluar. 2. La relevancia del blanco para la fisiopatología de interés. Sin embargo, el desconocimiento del panorama general en el descubrimiento de fármacos, desde problemáticas estructurales y celulares, ha enlentecido la búsqueda de nuevos tratamientos. Esta revisión descriptiva de tema presenta algunos aspectos estructurales importantes para la caracterización de compuestos como candidatos terapéuticos, y aproximaciones experimentales para desarrollo de sistemas celulares. Los tópicos discutidos se enfocan en la monitorización por imagenología de células vivas y así mismo proporcionamos ejemplos relevantes. La monitorización de efectos fenotípicos producidos por interacciones entre candidato químico y blanco terapéutico en un sistema celular puede favorecer la búsqueda eficiente de moléculas potencialmente terapéuticas.

SUMMARY The efficient compounds' design taking advantage of the molecule's structural characteristics and efficient search for therapeutic targets has provided effective tools for the research of new treatments when this is focused on disease cellular mechanisms. Phenotypic changes produced by in vitro interaction between molecules and targets can be monitored quantitatively by live cell imaging. To guarantee adequate interaction, it is necessary to consider different crucial elements: 1. Structural characteristics and molecular dynamics of the evaluated compound. 2. Target relevance for the concern physiopathology. However, overview's ignorance of the drug discovery, from structural and cellular problems, has slowed the new treatments research. This literature review presents some important structural aspects for compounds' characterization as therapeutic candidates and experimental approaches for cellular systems development. Subjects discussed are focused on live cell imaging and we also provide relevant examples. Phenotypic monitoring of interactions' produced effects between the chemical candidate and therapeutic target in a cellular system can favor the efficient search of potentially therapeutic molecules.

Anticoagulant use profile in hospitalized patients, drug interactions and identified adverse reactions

RESUMEN Son conocidos los efectos de los anticoagulantes como tratamiento o profilaxis de eventos trombóticos, esto permitió establecer una terapia individualizada según sus necesidades. Se realizó un estudio descriptivo, transversal, no aleatorizado, en 138 pacientes hospitalizados mayores de edad en una institución de cuarto nivel de atención con tratamiento anticoagulante terapéutico y profiláctico, se abordó el tipo de fármaco indicado, periodicidad, efectos adversos, controles de laboratorio, interacciones farmacológicas y causalidad de las reacciones adversas. Se encontró que el anticoagulante con mayor frecuencia de uso fue enoxaparina (68%), el control más utilizado fue el tiempo de protrombina (60,39%), interacciones farmacológicas se identificaron en 47,1%, las más frecuentes con ácido acetil salicílico (29,7% del total de interacciones), las reacciones adversas más frecuentes fueron de índole hematológico (58,3%); y la evaluación de causalidad de reacciones adversas fue 4,2% probable. El estudio mostró que el anticoagulante más utilizado fue enoxaparina. Las interacciones farmacológicas de los anticoagulantes fueron muy frecuentes, especialmente con warfarina. Las reacciones adversas de mayor ocurrencia fueron las de tipo hemorrágico ; y la evaluación de causalidad fue de categoría posible para la mayoría de estas reacciones adversas.

SUMMARY The effects of anticoagulants are known as treatment or prophylaxis of thrombotic events, allowing to establish an individualized therapy according to their needs. A descriptive cross-sectional, non-randomized study was carried out in 138 hospitalized patients of legal age in a fourth-level care institution with therapeutic and prophylactic anticoagulant treatment, addressing the type of drug indicated, periodicity, side effects, laboratory controls, pharmacological interactions and causality of adverse reactions. It was found that the anticoagulant with the highest frequency of use was enoxaparin (68%), the most used control was the prothrombin time (60.39%), pharmacological interactions were identified in 47.1%, being the most frequent with acetylsalicylic acid (29.7% of the total number of interactions), the most frequent adverse reactions were of a hematological nature (58.3%); and the causality assessment of adverse reactions was 4.2% probable. The study showed that the most used anticoagulant was enoxaparin. The pharmacological interactions of anticoagulants were very frequent, especially with warfarin. The most frequent adverse reactions were those of hemorrhagic type; and the causality assessment was of possible category for most of these adverse reactions.

Formulation of cosmetic products from Cucurbita argyrosperma C. Huber seed oil

RESUMEN El presente trabajo tiene como objetivo aprovechar el aceite de las semillas de Cucurbita argyrosperma C. Huber (sin. Cucurbita mixta Pangalo), como fitoingrediente en la elaboración de productos cosméticos. El aceite empleado se obtuvo por extracción con soxhlet y se realizó su caracterización fisicoquímica. Se elaboraron emulgeles (O/W) variando el agente viscosante y emulgente. Las formulaciones logradas se valoraron mediante la evaluación de las propiedades organolépticas (color, olor, brillo), fisicoquímicas (pH, conductividad) y extensibilidad y fueron sometidas a estudios de estabilidad. Se obtuvieron productos tipo emulgel de color amarillento con ligero olor ceroso, con pH aceptable para la piel. Todas las formulaciones resultaron estables. Los resultados demostraron que las formulaciones propuestas permitieron incorporar el aceite de origen vegetal logrando un preparado cosmético de características y estabilidad aceptables.

SUMMARY The objective of this work is to take advantage of the oil of the seeds of Cucurbita argyrosperma C. Huber (sin. Cucurbita mixta Pangalo), as a phytoingredient in the elaboration of cosmetic products. The oil used was obtained by extraction with soxhlet and its physicochemical characterization was carried out. Emulgels (O/W) were prepared by varying the viscosifying and emulsifying agent. The formulations achieved were evaluated by evaluating the organoleptic properties (color, odor, brightness), physicochemical (pH, conductivity) and extensibility and were subjected to stability studies. Emulgel type products with yellowish color with slight waxy odor were obtained, with acceptable pH for the skin. All the formulations were stable. The results showed that the proposed formulations allowed incorporating the oil of vegetable origin achieving a cosmetic preparation of acceptable characteristics and stability.

Fatty acid compositions of ether extracts of Bryophyllumpinnatum Lam., Ficus exasperata Vahl., Gossypium herbaceum Linn. and Hilleria latifolia (Lam.) H. Walt

SUMMARY Currently, there is a growing interest in identifying alternative sources of fatty acids due to the present increasing demand for oil-rich botanicals in industrial applications. The main objective of this work was to identify the fatty acid compositions of ether extracts of dried leaves of Bryophyllum pinnatum Lam., Ficus exasperata Vahl., Gossypium herbaceum Linn. and Hilleria latifolia (Lam.) H. Walt. The fatty acids were analyzed by gas chromatography with flame ionization detector. Among the evaluated ether extracts, the higher contents of saturated fatty acids were found in H. latifolia (27.96%) with the principal presence of stearic acid compared to the content of the saturated fatty acids in B. pinnatum (0.53%), F. exasperata (0.04%) and G. herbaceum (0.47%). Equally, the result showed that H. latifolia contained the highest percentage of unsaturated fatty acids with the predominant presence of oleic acid with the amount of 41.04%. Linoleic acid was also found to have the highest value in H. latifolia with the amount of 20.41%. Stearic acid, oleic acid, and linoleic acid were found in all the samples. The extract of H. latifolia contained a healthy mixture of different types of fatty acids thus suggesting it as a probable source of suitable fatty acids.

RESUMEN Actualmente, existe un creciente interés en identificar fuentes alternativas de ácidos grasos debido a la creciente demanda actual de productos botánicos ricos en aceite en aplicaciones industriales. El objetivo principal de este trabajo fue identificar las composiciones de ácidos grasos de extractos de éter de hojas secas de Bryophyllum pinnatum Lam., Ficus exasperata Vahl., Gossypium herbaceum Linn. y Hilleria latifolia (Lam.) H. Walt. Los ácidos grasos fueron analizados por cromatografía de gases con detector de ionización de llama. Entre los extractos de éter evaluados, los mayores contenidos de ácidos grasos saturados se encontraron en H. latifolia (27,96%) con presencia principal de ácido esteárico en comparación con el contenido de los ácidos grasos saturados en B. pinnatum (0,53%), F. exasperata (0,04%) y G. herbaceum (0,47%). Igualmente, el resultado mostró que la H. latifolia contenía el mayor porcentaje de ácidos grasos insaturados con presencia predominante de ácido oleico con una cantidad de 41,04%. También se encontró que el ácido linoleico tiene el valor más alto en H. latifolia con una cantidad de 20,41%. Se encontró ácido esteárico, ácido oleico y ácido linoleico en todas las muestras. El extracto de H. latifolia contenía una mezcla saludable de diferentes tipos de ácidos grasos, lo que sugiere que es una fuente probable de ácidos grasos adecuados.

Antidepressive use and self-rated health among adults of 40 years and older: longitudinal study

RESUMO Os efeitos dos antidepressivos sobre a qualidade de vida dos usuários ainda é controverso. O objetivo do estudo foi verificar a relação entre o uso de antidepressivos e a autopercepção de saúde em população de 40 anos ou mais. Trata-se de um estudo longitudinal, de base populacional, em município de médio porte no Brasil com coleta de dados em 2011 e 2015. A variável dependente foi a autopercepção da saúde (2015) e a independente foi a utilização de medicamentos antidepressivos, categorizada em "usavam somente em 2011", "usavam somente em 2015", "usavam em 2011 e 2015" e "não usavam". A associação entre o uso de antidepressivos e autopercepção de saúde foi verificada pela Regressão de Poisson com variância robusta. Fizeram parte do estudo 885 pessoas. A autopercepção negativa da saúde esteve presente em 44% da população estudada. A prevalência do uso de antidepressivos foi 17,6% em 4 anos. O uso de antidepressivos esteve associado à autopercepção negativa da saúde para os indivíduos que estavam em uso somente no ano de 2015 na população geral (RP 1,082; IC 95% 1,004-1,166). Não foi verificada relação entre uso antidepres-sivos e autopercepção da saúde, salvo para os que utilizavam antidepressivos apenas em 2015.

SUMMARY Antidepressants are one of the fastest growing classes of prescription drugs in the world and their effects on users' quality of life are still controversial. The aim of the study was verify the relationship between antidepressant use and self-rated health in a population aged 40 years or older. This was a population-based longitudinal study with adults of 40 years or older in a medium-sized municipality in Brazil with data collection in 2011 and 2015. The dependent variable was self-rated health (2015) and the independent the use of antidepressant medications, categorized as "used only in 2011", "used only in 2015", "used in 2011 and 2015" and "not used". The Poisson regression with robust variance was used to verify the association between antidepressant use and self-rated health. The study included 885 people. Negative self-rated health was present in 44% of the study population. The prevalence of antidepressant use was 17.6% over 4 years. The use of antidepressants was associated with negative self-rated health for individuals who were only using 2015 in the general population (PR 1.082; 95% CI 1.004-1.166). There was no relationship between antidepressant use and self-rated health, except for those who used antidepressants only in 2015.

Study patterns of prescribing and dispensing of drugs to outpatients four IPS the municipality of Villavicencio

RESUMEN Justificación: el cumplimiento de las características y el contenido de la prescripción de medicamentos contribuyen a disminución de errores de medicación. Objetivo: identificar algunos patrones de la prescripción y dispensación ambulatoria de medicamentos en 4 IPS del municipio de Villavicencio. Método: estudio descriptivo observacional, de corte transversal durante un mes, utilizando indicadores de prescripción OMS, y verificando el cumplimiento de la normatividad colombiana vigente. Resultados: 1493 prescripciones analizadas (28,8% elaboradas por profesionales no autorizados; 2,9% con enmendaduras; 6% sin diagnóstico; 9,2% ilegibles; 6,7% contenían al menos 1 antibiótico sistémico; 3,4% contenían al menos un inyectable). Del total de medicamentos prescritos: 99,79% con denominación común internacional; 99,22% incluidos en el Plan Obligatorio de Salud, 99,18% dispensados. El 96,6% de las prescripciones presentaban al menos 1 incumplimiento ; el 31,4% contenía la unidad de dosis; el 32,8% la vía de administración y el 35,3% la duración del tratamiento. Las prescripciones de medicamentos con señales de uso inapropiado fueron menores del 0,4%. Conclusiones: se identificó el no cumplimiento de las 4 IPS de algunos requisitos exigidos en la normatividad colombiana para la prescripción médica, lo que puede contribuir a la generación de errores de medicación en los procesos de prescripción y dispensación de medicamentos.

SUMMARY Justification: compliance of characteristics and content of prescriptions drugs help to decrease medication errors. Objective: to identify some patterns of prescription and dispensing of drugs for outpatient in 4 IPS the municipality of Villavicencio. Method: observational descriptive study, cross-sectional for a month, using WHO prescribing indicators, and verifying compliance with current Colombian law. Results: 1493 analyzed prescriptions (28.8% developed by professionals unauthorized, 2.9% with erasures; 6% without diagnosis 9.2%, 6.7% contained at least one systemic antibiotic, 3.4% contained at least one injection). Of all prescription drugs: 99.79% generic name; 99.22% included in the list of essential medicines, 99.18% dispensed. 96.6 % had at least 1 prescription failure: only 31.4% contained unit dose; 32.8% of route of administration and 35.3% the duration of treatment. Prescriptions drugs misuse signals did not exceed 0.4%. Conclusions: the non-compliance with the 4 IPS of some requirements demanded in the Colombian regulations for medical prescription was identified, which may contribute to the generation of medication errors in the prescription and dispensing processes of medications.

Antibacterial, antifungal, and antiviral activities of chalcone-bearing tetrahydropyranyl and 2,4-dihydroxyl moieties

SUMMARY Chalcones highlights as an important structure in medicinal chemistry and thus has been widely used as a template in the development of new drugs. In this study, we aim to determine the antibacterial, anti-Candida, and anti-Dengue potential of new chalcone-bearing 2,4-dihydroxyl and tetrahydropyranyl moieties. Antimicrobial activity assays showed that microorganism of the Staphylococcus genus (including methicillin-resistant strains) were susceptible to 2,4-dihydroxychalcones, with minimum inhibitory concentrations (MICs) ranging of 19.5 to 125 µg.mL-1. Compound 4e, which showed the highest bacteriostatic effect, also has bactericidal activity from of 80 µg.mL-1. The growth of oral isolates of Candida albicans was also efficiently inhibited with compound 4e (MIC: 15.6-32.3 µg.mL-1), which was fungicidal at 15.6 µg.mL-1. However, the presence of the tetrahydropyranyl moiety impaired both the antibacterial and antifungal effects. None of the chalcones tested were actives against Dengue virus serotype 2. In conclusion, the compound 4e showed good anti-Staphylococci and anti-Candida activity and may be a promising prototype for the development of new antimicrobial agents.

RESUMEN Las chalconas se destacan como una estructura importante en la química médica y, por lo tanto, se ha empleado como prototipo para el desarrollo de nuevos fármacos. En este estudio, nuestro objetivo fue determinar el potencial antibacteriano, anti Candida y anti-Dengue de las nuevas chalconas que poseen los grupos 2,4-dihidroxilo y tetrahidropiranilo. El ensayo de actividad antimicrobiana mostró que las bacterias del género Staphylococcus (incluidas las cepas resistentes a la meticilina) fueron sensibles a las 2,4-dihidroxicalconas estudiadas, con concentraciones inhibitorias mínimas (CIM) que oscilan entre 19,5 y 125 µg.mL-1. El compuesto 4e, que tuvo el mejor efecto bacteriostático, también mostró un efecto bactericida a partir de la concentración de 80 µg.mL-1. El crecimiento de los aislamientos orales de Candida albicans también se inhibió eficientemente con el compuesto 4e (CIM: 15.6-32.3 µg.mL-1), que fue fungicida a una concentración de 15.6 µg.mL-1. Sin embargo, la presencia del grupo tetrahidropiranilo perjudicó la actividad antibacteriana y anti-fúngica de los análogos de la chalcona. Además, ninguno de los compuestos evaluados mostró un efecto contra el virus del dengue serotipo 2. En conclusión, el compuesto 4e muestra una buena actividad anti-estafilocócica y anti-Candida y puede ser un prototipo prometedor para el desarrollo de nuevos agentes antimicrobianos.

RESUMO As chalconas se destacam como uma importante estrutura na química medicinal e dessa forma tem sido empregada como um protótipo para o desenvolvimento de novos fármacos. Nesse estudo, nós objetivamos determinar o potencial antibacteriano, anti-Candida, e anti-Dengue de novas chalconas que possuem os grupos 2,4-dihidroxil e tetrahidropiranil. O ensaio de atividade antimicrobiana mostrou que bactérias do gênero Staphylococcus (incluindo linhagens resistentes a meticilina) foram sensíveis para as 2,4-dihidroxichalconas estudadas, com concentrações inibitórias mínimas (CIM) variando de 19,5 para 125 Dengue potential of new chalcone µg.mL-1. O composto 4e, o qual apresentou o melhor efeito bacteriostático, também mostrou efeito bactericida a partir da concentração de 80 µg.mL-1. O crescimento de isolados orais de Candida albicans foi também eficientemente inibido com o composto 4e (CIM: 15.6-32.3 µg.mL-1), o qual foi fungicida a concentração de 15,6 µg.mL-1. Entretanto, a presença do grupo tetrahidropiranil prejudicou a atividade antibacteriana e antifúngica dos análogos de chalcona. Adicionalmente, nenhum dos compostos avaliados mostrou efeito contra o vírus da dengue sorotipo 2. Em conclusão, o composto 4e apresenta boa atividade anti-estafilocóccica e anti-Candida, e pode ser um promissor protótipo para o desenvolvimento de novos agentes antimicrobianos.

Thermodynamic analysis and applications of the Abraham solvation parameter model in the study of the solubility of some sulfonamides

SUMMARY Solubility of sulfadiazine (SD), sulfamerazine (SMR) and sulfamethazine (SMT) in cosolvent mixtures octanol+methanol was investigated to 278.15 K, 298.15 and 313.15 K. In all cases, the lowest solubility of each drug was obtained in pure octanol at 278.15 K. The maximum solubility depends on the polarity of the drug, thus SMR and SMT reached their maximum solubility in cosolvent mixtures methanol-rich. The solution thermodynamic functions were calculated from the experimental solubility data, using the van't Hoff and Gibbs equations, following the approach proposed by Krug et al. The enthalpy of solution is positive in all cases, which is an indication of the endothermic process with a marked entropic favor. Theoretical solubility and mean lethal concentration were calculated using the Abraham model.

RESUMEN Se investigó la solubilidad de sulfadiazina (SD), sulfamerazina (SMR) y sulfametazina (SMT) en mezclas codisolventes de octanol + metanol a 278,15 K, 298,15 y 313,15 K. En todos los casos, la solubilidad más baja de cada fármaco se obtuvo en octanol puro a 278,15 K. La solubilidad máxima depende de la polaridad del fármaco, por lo que SMR y SMT alcanzaron su máxima solubilidad en mezclas cosolventes ricas en metanol. Las funciones termodinámicas de solución se calcularon a partir de los datos experimentales de solubilidad, utilizando las ecuaciones de van't Hoff y Gibbs, siguiendo el enfoque propuesto por Krug et al. La entalpia de la solución es positiva en todos los casos, lo cual es una indicación del proceso endotérmico con un marcado favorecimiento entrópico. La solubilidad teórica y la concentración letal media se calcularon utilizando el modelo de Abraham.