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J. Health Biol. Sci. (Online) ; 10(1): 1-12, 01/jan./2022. tab, graf
Article in English | LILACS | ID: biblio-1382369


Objective: this systematic review aims to compile literature data on the antimicrobial action of Selective Serotonin Reuptake Inhibitors (SSRI). Methods: To this end, the articles in this review were searched in the PubMed database between the years 2010 to 2020, using terms found in MESH as descriptors. The PRISMA flow diagram was used to analyze the process flow of the research. Later, inclusion and exclusion criteria and eligibility for data extraction and statistical analysis were applied. Results: Thus, of 252 articles found, 13 were used for this systematic review. The period in which there were more publications was in 2016-2017. All articles demonstrated the antimicrobial activity of ISRS, such as sertraline, fluoxetine, and paroxetine, in addition to their synergistic activity with some antifungals and antibacterial. Conclusion: With this, it could be concluded that the repositioning of non-antibiotic drugs that have antimicrobial activity is a promising alternative for the scientific community and, in the future, in clinical practice

Objetivo: compilar dados da literatura sobre a ação antimicrobiana dos Inibidores Seletivos de Recaptação de Serotonina (ISRS). Métodos: os artigos desta revisão foram pesquisados na base de dados PubMed, entre os anos de 2010 a 2020, utilizando, como descritores, termos encontrados no MESH. O fluxograma PRISMA foi utilizado para analisar o fluxo do processo da pesquisa. Posteriormente, foram aplicados os critérios de inclusão e exclusão e de elegibilidade para extração de dados e análise estatística. Resultados: dos 252 artigos encontrados, 13 foram utilizados para esta revisão sistemática. O período em que houve mais publicações foi em 2016-2017. Todos os artigos demonstraram a atividade antimicrobiana do ISRS, como sertralina, fluoxetina e paroxetina, além de sua atividade sinérgica com alguns antifúngicos e antibacterianos. Conclusão: o reposicionamento de medicamentos não antibióticos que possuam atividade antimicrobiana é uma alternativa promissora para a comunidade científica e, futuramente, na prática clínica.

Selective Serotonin Reuptake Inhibitors , Anti-Bacterial Agents , Antifungal Agents , Bacteria , Serotonin , Fluoxetine , Selective Serotonin Reuptake Inhibitors , Paroxetine , Sertraline , PubMed , Fungi
Braz. J. Pharm. Sci. (Online) ; 58: e18943, 2022. graf
Article in English | LILACS | ID: biblio-1364427


Abstract The objective of this study was to evaluate drug interactions based on medical records of patients hospitalized in University Hospital Lauro Wanderley (UHLW) in João Pessoa-PB, Brazil. This was a quantitative, descriptive study with a cross-sectional design. This research was conducted in the medical clinic of the above hospital by analyzing pharmaceutical intervention in medical records. The investigated samples consisted of all medical profiles with drug interaction information of patients hospitalized from June 2016 to June 2017. Most of these drug interactions were determined and classified by Micromedex® Solutions database. This research was approved by the Ethics Committee in Institutional Human Research, protocol number 2.460.206. In total, 331 drug interactions were found in 131 medical profiles. Dipyrone, enoxaparin, sertraline, ondansetron, quetiapine, tramadol, bromopride, amitriptyline, and simvastatin were medications that showed highest interactions. According to Anatomical Therapy Classification (ATC), drugs that act on the central nervous system result in more interactions. The most prevalent interaction was between dipyrone and enoxaparin. Some limitations of this study are the lack of notifications and data on drug interactions.

Humans , Male , Female , Research , Medical Records/classification , Drug Interactions , Evaluation Studies as Topic , Inpatients/classification , Universities , Pharmaceutical Preparations , Dipyrone/adverse effects , Enoxaparin/supply & distribution , Simvastatin/supply & distribution , Sertraline/supply & distribution , Quetiapine Fumarate/supply & distribution , Amitriptyline/supply & distribution , Hospitals, University/organization & administration
Braz. J. Pharm. Sci. (Online) ; 58: e20584, 2022. tab, graf
Article in English | LILACS | ID: biblio-1403761


Abstract Personalized medicine is gaining importance in pharmacotherapeutics as it allows tailoring the drug treatment to achieve the best patient response. Orodispersible film (ODF) is easy to formulate in hospitals, produces dose flexibility to suit an individual needs, particularly for patients suffer from swallowing issues or prohibited to take fluids. Sertraline Hydrochloride (SRT) was solubilized in several cosolvents, then different SRT ODFs based on five hydrophilic polymers namely; polyvinyl alcohol (PVA), hydroxylethyl cellulose (HEC), hydroxypropyl methylcellulose E5 LV (HPMC E5 LV), sodium alginate (NaAlg) and gelatin at two concentrations (2% and 4%) were developed and characterized. The outcomes were exposed to response surface analysis to obtain the desirability results to obtain the optimized formulation. Blended ODFs were developed from 4% PVA and 2% HEC in different blends and then potassium chloride (KCl) as a pore-forming agent was added to the best formulation to investigate its dissolution enhancement effect. F14 containing 4% PVA: 2% HEC 2:1 with 5% KCl showed best physicochemical properties of suitable pH (5.6), disintegration time (6 sec), good folding endurance which released 91 % SRT after 15 min. SRT ODF is an encouraging delivery system in the course of personalized medicine for the management of depression.

Solvents , Sertraline/analysis , Precision Medicine , Excipients , Process Optimization
Chinese Acupuncture & Moxibustion ; (12): 1005-1009, 2021.
Article in Chinese | WPRIM | ID: wpr-921000


OBJECTIVE@#To observe the effect of auricular acupuncture on reduction rate of sertraline hydrochloride, and to explore the long-term efficacy of auricular acupuncture in patients with depression.@*METHODS@#Seventy-two patients with depression were randomly divided into an observation group (36 cases, 1 case dropped off) and a control group (36 cases, 2 cases dropped off). The patients in the control group were treated with conventional dosage reduction method, that is, the dosage of sertraline hydrochloride was reduced by 25% every week until the dosage was stopped completely on the premise of no aggravation of depressive symptoms. Based on the conventional dosage reduction method used in the control group, the patients in the observation group were treated with auricular acupuncture at Xin (CO@*RESULTS@#The dosage of sertraline hydrochloride in the observation group was less than that in the control group after 2, 3, 4 weeks of dosage reduction and during follow-up (@*CONCLUSION@#Auricular acupuncture could effectively reduce the dosage of sertraline hydrochloride, improve the dosage reduction rate, reduce the incidence of withdrawal syndrome and reduce the risk of long-term recurrence in patients with depression.

Acupuncture Points , Acupuncture Therapy , Acupuncture, Ear , Depression/drug therapy , Humans , Sertraline , Treatment Outcome
Rev. pediatr. electrón ; 17(3): 44-48, oct. 2020.
Article in Spanish | LILACS | ID: biblio-1367339


La Organización Mundial de la Salud recomienda amamantar a los recién nacidos, pero resulta contraproducente si la madre presenta una enfermedad que afecte este proceso natural, como la depresión postparto (DPP), una complicación psiquiátrica frecuente en el puerperio que influye en la salud de la madre y del lactante. El tratamiento farmacológico consiste en la administración de antidepresivos, considerándose los riesgos y ventajas, algunos ISRS se destacan por su menor detección en la leche materna; por ello la Sertralina puede ser el más seguro, el lactante ingiere cantidades pequeñas y generalmente no se detectan en el plasma. También se requiere de consejería por la incertidumbre de continuar o no amamantando.

The World Health Organization recommends breastfeeding newborns,but it is counterproductive if the mother presents a disease that affects this natural process, such as possible acute or chronic pathologies in the life cycle of pregnancy, as well as in lactation; one of them is postpartum depression (PPD), a frequent psychiatric complication in the puerperium that influences the health of the mother and the infant, such as early interruption or continued breastfeeding. Pharmacological treatment consists of the administration of antidepressants, considering the risks and advantages, some SSRIs stand out for their lower detection in breast milk; for this reason Sertraline may be the safest, the infant ingests small amounts and is generally not detected in the plasma. It is also the most used during lactation according to most researchers. Mothers may need breastfeeding counseling due to the uncertainty of continuing or not breastfeeding

Humans , Female , Breast Feeding , Depression, Postpartum/drug therapy , Sertraline/therapeutic use , Antidepressive Agents/therapeutic use , Antidepressive Agents/pharmacology
Gastroenterol. latinoam ; 31(2): 90-93, 2020. tab, graf
Article in Spanish | LILACS | ID: biblio-1292375


We report the case of a 19-year-old patient, with a history of traumatic liver damage, but with a normal liver profile at her first discharge; 1 month after the event, with post-traumatic stress disorder, treatment with 25 mg of sertraline was started every day; one month later, she develops severe hepatotoxicity without a specific etiology. According to the Naranjo algorithm, it is attributed as a probable case of sertraline hepatotoxicity. Management is carried out with support measures and suspension of the medication, and the patient recovers until she is asymptomatic, currently has normal liver tests

Reportamos el caso de una paciente de 19 años, con antecedentes de daño hepático traumático, pero con un perfil hepático normal en su primer alta; después de 1 mes del evento, con trastorno de estrés postraumático se inició tratamiento con 25 mg diarios de sertralina; un mes después, desarrolla una hepatotoxicidad severa sin etiología determinada. De acuerdo con el algoritmo de Naranjo, se atribuye como caso probable de hepatotoxicidad por sertralina. El manejo se realiza con medidas de apoyo y suspensión del medicamento, y la paciente se recupera hasta que se encuentra asintomática, actualmente tiene pruebas hepáticas normales

Humans , Female , Young Adult , Selective Serotonin Reuptake Inhibitors/adverse effects , Sertraline/adverse effects , Chemical and Drug Induced Liver Injury/etiology , Algorithms , Chemical and Drug Induced Liver Injury/therapy
Rev. Hosp. Ital. B. Aires (2004) ; 39(4): 128-134, dic. 2019.
Article in Spanish | LILACS | ID: biblio-1099754


Asociada o no a una enfermedad orgánica, la depresión tiene gran prevalencia en la práctica médica pero es subdiagnosticada. El trastorno del ánimo suele coexistir con variadas quejas somáticas y dolores crónicos, configurando síndromes mixtos con un diagnóstico diferencial complejo. En este artículo se describen distintas presentaciones clínicas de la depresión en medicina general, con énfasis en los estados depresivos atípicos, depresiones enmascaradas muy relevantes por su frecuencia y consecuencias: depresión posquirúrgica, cuadros dolorosos crónicos como cefaleas o lumbago, la fatiga crónica y la fibromialgia. Solo el reconocimiento y diagnóstico de la depresión subyacente posibilitará la implementación de las adecuadas intervenciones terapéuticas. Se revisan también algunas recomendaciones para el uso de antidepresivos en atención primaria y la eventual consulta psiquiátrica. (AU)

Associated or not with an organic disease, depression has a high prevalence in medical practice but is underdiagnosed. The mood disorder usually coexists with varied somatic complaints and chronic pain, forming mixed syndromes with a complex differential diagnosis. This article describes different clinical presentations of depression in general medicine, with emphasis on atypical depressive states, masked depressions very relevant for their frequency and consequences: post-surgical depression, chronic painful conditions such as headaches or lumbago, chronic fatigue and fibromyalgia. Only the recognition and diagnosis of the underlying depression will enable the implementation of appropriate therapeutic interventions. Some recommendations for the use of antidepressant drugs in primary care and the eventual psychiatric consultation are also reviewed. (AU)

Humans , Male , Female , Adult , Middle Aged , Aged , Young Adult , Primary Health Care/trends , Depression/diagnosis , Psychiatry/trends , Signs and Symptoms , Somatoform Disorders/diagnosis , Citalopram/adverse effects , Citalopram/therapeutic use , Fibromyalgia/complications , Fatigue Syndrome, Chronic/complications , Fluoxetine/adverse effects , Fluoxetine/therapeutic use , Selective Serotonin Reuptake Inhibitors/adverse effects , Low Back Pain/complications , Cholinergic Antagonists/adverse effects , Medical Errors , Sertraline/adverse effects , Sertraline/therapeutic use , Depression/classification , Depression/complications , Depression/therapy , Depression/epidemiology , General Practice , Chronic Pain/complications , Venlafaxine Hydrochloride/adverse effects , Venlafaxine Hydrochloride/therapeutic use , Duloxetine Hydrochloride/adverse effects , Duloxetine Hydrochloride/therapeutic use , Serotonin and Noradrenaline Reuptake Inhibitors/adverse effects , Headache/complications , Amitriptyline/adverse effects , Amitriptyline/therapeutic use , Antidepressive Agents/administration & dosage
J. bras. nefrol ; 41(4): 492-500, Out.-Dec. 2019. tab, graf
Article in English | LILACS | ID: biblio-1056600


Abstract Introduction: Intradialytic hypotension (IDH) is a major complication of hemodialysis, with a prevalence of about 25% during hemodialysis sessions, causing increased morbidity and mortality. Objective: To study the effects of sertraline to prevent IDH in hemodialysis patients. Methods: This was a double-blind, crossover clinical trial comparing the use of sertraline versus placebo to reduce intradialytic hypotension. Results: Sixteen patients completed the two phases of the study during a 12-week period. The IDH prevalence was 32%. A comparison between intradialytic interventions, intradialytic symptoms, and IDH episodes revealed no statistical difference in the reduction of IDH episodes (p = 0.207) between the two intervention groups. However, the risk of IDH interventions was 60% higher in the placebo group compared to the sertraline group, and the risk of IDH symptoms was 40% higher in the placebo group compared to the sertraline group. Survival analysis using Kaplan-Meier estimator supported the results of this study. Sertraline presented a number needed to treat (NNT) of 16.3 patients to prevent an episode from IDH intervention and 14.2 patients to prevent an episode from intradialytic symptoms. Conclusion: This study suggests that the use of sertraline may be beneficial to reduce the number of symptoms and ID interventions, although there was no statistically significant difference in the blood pressure levels.

Resumo Introdução: A hipotensão intradialítica (HID) é uma das principais complicações da hemodiálise, com uma prevalência de cerca de 25% durante as sessões de hemodiálise, causando aumento da morbimortalidade. Objetivo: Estudar os efeitos da sertralina na prevenção da HID em pacientes em hemodiálise. Métodos: Este foi um ensaio clínico duplo-cego, cruzado, comparando o uso de sertralina versus placebo para reduzir a hipotensão intradialítica. Resultados: Dezesseis pacientes completaram as duas fases do estudo durante um período de 12 semanas. A prevalência de HID foi de 32%. Uma comparação entre intervenções intradialíticas, sintomas intradialíticos (ID) e episódios de HID não revelou diferença estatística na redução dos episódios de HID (p = 0,207) entre os dois grupos de intervenção. No entanto, o risco de intervenções para HID foi 60% maior no grupo placebo em comparação com o grupo Sertralina, e o risco de sintomas ID foi 40% maior no grupo placebo em comparação com o grupo Sertralina. A análise de sobrevida utilizando o estimador de Kaplan-Meier corroborou os resultados deste estudo. A sertralina apresentou um número necessário para tratar (NNT) de 16,3 pacientes para prevenir um episódio de intervenção de HID e 14,2 pacientes para prevenir um episódio de sintomas intradialíticos. Conclusão: Este estudo sugere que o uso de sertralina pode ser benéfico para reduzir o número de sintomas e intervenções de HID, embora não tenha havido diferença estatisticamente significante nos níveis pressóricos.

Humans , Male , Female , Middle Aged , Aged , Renal Dialysis/adverse effects , Selective Serotonin Reuptake Inhibitors/therapeutic use , Sertraline/therapeutic use , Renal Insufficiency/therapy , Hypotension/physiopathology , Placebos/administration & dosage , Blood Pressure/drug effects , Blood Pressure/physiology , Double-Blind Method , Prevalence , Renal Dialysis/mortality , Cross-Over Studies , Renal Insufficiency/complications , Hypotension/prevention & control , Hypotension/epidemiology
Int. braz. j. urol ; 45(6): 1209-1215, Nov.-Dec. 2019. tab
Article in English | LILACS | ID: biblio-1056348


ABSTRACT Purpose: To compare the efficacy and safety of available selective serotonin reuptake inhibitors (SSRIs) in order to find the most effective drug with the least number of side effects in treatment of premature ejaculation (PE). Materials and Methods: This study was a randomized clinical trial. Four hundred and eighty patients with PE in the 4 groups referred to Imam Reza hospital Tehran, Iran from July 2018 to February 2019 were enrolled in the study. The patients received sertraline 50mg, fluoxetine 20mg, paroxetine 20mg and citalopram 20mg, every 12 hours daily. The intravaginal ejaculatory latency time (IELT) before treatment, fourth and eighth weeks after treatment was recorded by the patient's wife with a stopwatch. Results: Mean IELT before, 4 and 8 weeks after treatment in four groups were: sertraline 69.4±54.3, 353.5±190.4, 376.3±143.5; fluoxetine 75.5±64.3, 255.4±168.2, 314.8±190.4; paroxetine 71.5±69.1, 320.7±198.3, 379.9±154.3; citalopram 90.39±79.3, 279.9±192.1, 282.5±171.1 seconds, respectively. The ejaculation time significantly increased in all groups (p <0.05), but there was no significant difference between the groups (P=0.75). Also, there was no significant difference in drugs side effects between groups (p >0.05). The most common side effects were drowsiness and dyspepsia, which were not severe enough to cause discontinuation of the drug. Conclusions: All available SSRIs were effective and usually had no serious complications. In patients who did not respond to any of these drugs, other SSRI drugs could be used as a salvage therapy.

Humans , Male , Adult , Aged , Young Adult , Citalopram/therapeutic use , Fluoxetine/therapeutic use , Selective Serotonin Reuptake Inhibitors/therapeutic use , Paroxetine/therapeutic use , Sertraline/therapeutic use , Premature Ejaculation/drug therapy , Reaction Time/drug effects , Time Factors , Treatment Outcome , Ejaculation/drug effects , Middle Aged
Rev. otorrinolaringol. cir. cabeza cuello ; 79(3): 323-328, set. 2019. tab, graf
Article in Spanish | LILACS | ID: biblio-1058703


RESUMEN Los trastornos vestibulares funcionales se constituyen como una de las causas más frecuentes de consulta por vértigo y trastornos del equilibrio. El mareo postural perceptual persistente (MPPP) es un síndrome recientemente definido, enmarcado en la categoría de síndromes vestibulares crónicos, que agrupa trastornos vestibulares funcionales crónicos como el vértigo postural fóbico, el malestar con el movimiento espacial, el vértigo visual y el mareo subjetivo crónico. El MPPP se manifiesta por síntomas de mareo, inestabilidad y/o vértigo no rotatorio, persistentes, exacerbados por cambios posturales, movimientos y exposición a distintos estímulos visuales. El tratamiento de este cuadro es más sencillo de lo que parece, basado en psicoeducación efectiva respecto a la patología como primer abordaje, adicionando o no rehabilitación vestibular, uso de inhibidores selectivos de la recaptación de serotonina y/o terapia cognitivo conductual. Se presentan dos casos clínicos de pacientes diagnosticados con MPPP y su respuesta a tratamiento.

ABSTRACT Functional vestibular disorders are one of the most frequent causes of consultation due to vertigo and balance disorders. Persistent postural-perceptual dizziness (PPPD) is a recently defined syndrome, categorized as a chronic vestibular syndrome, that includes functional vestibular disorders such as phobic postural vertigo, space-motion discomfort, visual vertigo and chronic subjective dizziness. PPPD manifests with dizziness, unsteadiness and/or non-spinning vertigo, which are persistent, exacerbated by postural changes, movements and exposure to various visual stimuli. PPPD treatment is simpler than it may seem initially. It is based on effective psychoeducation related to the pathology in the first place, followed, or not, by vestibular rehabilitation, use of selective serotonin reuptake inhibitors and/or cognitive behavioral therapy. We present two clinical cases of patients diagnosed with PPPD and their response to treatment.

Humans , Male , Female , Middle Aged , Dizziness/diagnosis , Dizziness/therapy , Posture , Visual Perception , Cognitive Behavioral Therapy , Vestibular Diseases , Chronic Disease , Selective Serotonin Reuptake Inhibitors/therapeutic use , Sertraline/therapeutic use , Dizziness/physiopathology
Article in Chinese | WPRIM | ID: wpr-775898


OBJECTIVE@#To compare the clinical effects of acupuncture combined with sertraline hydrochloride and simple sertraline hydrochloride on tumor-related depression.@*METHODS@#Sixty patients with tumor-related depression who met the inclusion criteria were randomly assigned to an observation group and a control group, 30 patients in each group. The routine treatment in department of oncology were given in both groups, oral sertraline hydrochloride (25 mg daily for the first 5 days, then 50 mg daily) was given in the control group; on the basis of the treatment in the control group, and acupuncture was applied at Hegu (LI 4), Neiguan (PC 6), Taichong (LR 3), Shenmen (HT 7),etc. in the observation group,twice a week .The two groups were treated continuously for 4 weeks. The Hamilton depression scale (HAMD) score and the quality of life score (QLQ-C30 questionnaire) were compared between the two groups before and after treatment.@*RESULTS@#After treatment, the HAMD scores in the two groups were significantly lower than those before treatment (both <0.05), and the HAMD scores in the observation group were lower than those in the control group (<0.05). In the observation group, the symptom scores of fatigue, pain, nausea and vomiting, dyspnea, insomnia, loss of appetite, constipation, and diarrhea were significantly lower than those before treatment (all <0.05), and the physical, cognitive, emotional function, and the overall quality of life score were significantly higher than those before treatment (all <0.05); in the control group, the symptom scores of insomnia decreased compared with that before treatment (<0.05), and the emotional function and overall quality of life score were higher than those before treatment (both <0.05); in addition to economic difficulties, roles and social functions, the other scores after treatment in the observation group were significantly improved than those in the control group (all <0.05).@*CONCLUSION@#The combination of acupuncture and sertraline hydrochloride tablets is better than simple sertraline hydrochloride in the treatment of tumor-related depression, and it can improve the accompanying symptoms and improve quality of life.

Acupuncture Therapy , Depression , Therapeutics , Humans , Quality of Life , Sertraline , Tablets , Treatment Outcome
Rev. Hosp. Ital. B. Aires (2004) ; 38(1): 31-33, mar. 2018.
Article in Spanish | LILACS | ID: biblio-1046195


El médico de familia está capacitado para resolver la mayoría de los problemas de salud de sus pacientes. Dentro del consultorio, el cansancio constituye un motivo de consulta muy frecuente. Su abordaje debe incluir la evaluación del contexto del paciente y un enfoque sistémico que incluya otros niveles diagnósticos y terapéuticos. Se presenta el caso de una paciente que, a partir de este motivo de consulta tan frecuente y junto a intervenciones de su médico de cabecera, logró modificar el foco del problema y comenzar un tratamiento acorde. (AU)

Family physicians are able to solve the majority of their patients' health issues. In the office, fatigue is a common complaint. Its approach should include the evaluation of the context of the patient and a systemic approach that includes other diagnostic and therapeutic levels. We present the case of a patient who went to his doctor with a common complaint and was able to change the focus of the problem and begin a consistent treatment. (AU)

Humans , Female , Adult , Physician-Patient Relations , Stress, Psychological/psychology , Vaginismus/psychology , Fatigue/diagnosis , Physician's Role , Sex Offenses/psychology , Stress, Psychological/therapy , Sertraline/therapeutic use , Vaginismus/diagnosis , Family Practice , Fatigue/therapy , Patient Comfort
Dement. neuropsychol ; 12(1): 97-100, Jan.-Mar. 2018.
Article in English | LILACS | ID: biblio-891058


ABSTRACT An elderly patient, aged 76 years, diagnosed with dysphagia, depression, hypothyroidism, Alzheimer's disease and mild cognitive deficit, was identified with sertraline and levothyroxine- drug-related problems. Medication Therapy Management (MTM) was used to adjust therapy to the patient's needs by macerating sertraline tablets and solubilizing them in 10-30 mL of orange juice. The patient was advised to take levothyroxine after fasting. Six months later, pharmaceutical follow-up identified an increase in the Mini-Mental State Exam score from 22 to 26 and a decrease in the Clinical Dementia Rating (CDR) scale score from 1.0 to 0.5 in conjunction with mood and physical improvements, as well as a significant decrease in aggressiveness and agitation. Cognitive deficit may be a result of poor drug administration procedures, leading to drug ineffectiveness. Optimizing levothyroxine and sertraline administration, based on knowledge of their physicochemical properties, improves their clinical effectiveness, including the cognition of patients with Alzheimer's disease and dysphagia.

RESUMO Paciente idosa, 76 anos, diagnosticada com disfagia, depressão, hipotireoidismo, doença de Alzheimer e déficit cognitivo leve, foram identificados problemas relacionados com a sertralina e levotiroxina. O Gerenciamento da Terapia Medicamentosa foi usado para ajustar a terapia às necessidades da paciente, macerando comprimidos de sertralina e solubilizando-os em 10-30 mL de suco de laranja. Foi recomendado a paciente tomar levotiroxina após o jejum. Seis meses depois, o seguimento farmacêutico identificou um aumento no score da escala Mini-Mental de 22 para 26 e Avaliação Clínica da Demência (CDR) de 1,0 para 0,5 em conjunto com melhorias físicas e de humor, bem como uma diminuição significativa na agressividade e agitação. O déficit cognitivo pode ser o resultado de procedimentos de administração inadequada de fármacos, levando à ineficácia do fármaco. A otimização da administração de levotiroxina e sertralina, com conhecimento de suas propriedades físico-químicas, melhora sua efetividade clínica, incluindo a cognição do paciente com a doença de Alzheimer e disfagia.

Humans , Pharmaceutical Services , Deglutition Disorders , Sertraline , Cognitive Dysfunction , Drug Misuse , Medication Errors
Braz. J. Pharm. Sci. (Online) ; 54(1): e17232, 2018. tab, graf
Article in English | LILACS | ID: biblio-951908


The purpose of the study was to combine the advantages of self-nanoemulsifying drug delivery systems and tablets as a conventional dosage form. Self-nanoemulsifying drug delivery system (SNEDDS) was prepared to enhance the solubility and thus oral bioavailability of sertraline. Aqueous titration method was used to prepare the liquid SNEDDS; ternary phase diagrams were constructed and based on smaller droplet size (24.8 nm), minimum viscosity (153.63 cP) and polydispersity index (0.182), higher percentage transmittance (95%) and in vitro drug release (97%), an optimum system was designated. Liquid SNEDDS was transformed into free-flowing powder by solid adsorption technique followed by compression into tablets. In vitro release of sertraline from liquid and solid SNEDDS was found to be highly significant compared to plain sertraline (p<0.01). Pharmacokinetic studies after oral administration of liquid and solid SNEDDS in rats showed about 6-and 5-fold increased absorption of sertraline compared to the aqueous suspension of sertraline. These studies demonstrate that the solid SNEDDS are promising strategies for successful delivery of poorly water-soluble drug like sertraline

Tablets/analysis , Biological Availability , Sertraline/pharmacology , Solubility , Administration, Oral , Emulsifying Agents
São Paulo; s.n; 2018. 107 p. graf, ilus, mapas, tab.


A leishmaniose visceral (LV) é uma protozoose negligenciada fatal se não tratada, afetando 1,5 milhões de pessoas em todo o mundo. Na América Latina, o Brasil é responsável por 90% dos casos de LV, sendo seu tratamento um grande desafio, por apresentar alta toxicidade. Desta forma, a busca por alternativas terapêuticas é uma necessidade iminente. O reposicionamento de fármacos vem sendo uma abordagem importante na redução do custo e do tempo nas pesquisas. Além disso, sistemas de entrega de fármacos (Drug Delivery) como lipossomos, têm contribuído para a redução de dose terapêutica e consequentemente, dos efeitos adversos dos fármacos. Sendo assim, neste trabalho, foi avaliado o potencial anti-Leishmania do antidepressivo sertralina (SERT) em modelos in vitro e in vivo, utilizando tanto o fármaco livre (SERT), como encapsulado em nanolipossomos (SERT-LP). A SERT apresentou atividade contra formas promastigotas e amastigotas intracelulares com valores de Concentração Efetiva 50% (CE50) de 0,7 µM e 4 µM, respectivamente. A associação in vitro da SERT com miltefosina demonstrou valores da média das somatórias das Concentrações Inibitórias Fracionárias (X∑CIF) de 0,64 e 1,32 em promastigotas e amastigotas, respectivamente, resultando em uma associação aditiva. Visando verificar a eficácia in vivo, foi realizado um estudo farmacocinético da SERT em modelo murino, resultando em uma meia vida plasmática (T1/2) de aproximadamente 8 horas. O estudo in vivo da eficácia da SERT demonstrou falha terapêutica, tanto na administração pela via oral, como subcutânea. Porém, quando encapsulada em lipossomos (125 nm) de carga negativa, resultou em uma significativa redução (89%) da carga parasitária no fígado de camundongos tratados, pela via de administração subcutânea, por 10 dias a 1 mg/kg/dia. Inesperadamente, em uma dose 15 vezes maior, foi observado um aumento de 100% da carga parasitária, valor este, correlacionado ao aumento dos níveis séricos da citocina IL-6 e da quimiocina MCP-1. Estudos de biodistribuição da SERT-LP, demonstraram a presença da formulação no fígado e baço - 12 a 48 horas após administração subcutânea. Estudos histopatológicos dos animais tratados a 1 e 15 mg/kg/dia por 10 dias demonstraram a presença de múltiplos 6 focos de infiltrado inflamatório linfohistiocitário, formando esboços granulomatosos, em parênquima hepático. No baço, foi observado a presença de hiperplasia linfóide reativa, não diferindo do grupo controle. Os dados obtidos no estudo histopatológico corroboram os níveis de citocinas observados por citometria de fluxo, resultando em um infiltrado inflamatório. O presente estudo demonstra a eficácia da sertralina encapsulada em lipossomos na LV experimental, e sugere pela primeira vez, uma correlação entre o aumento da carga parasitária com a imunomodulação dose-dependente do fármaco. (AU)

Visceral leishmaniasis (VL) is a fatal neglected protozoan, affecting 1.5 million people in all the world. In Latin America, Brazil is responsible for 90% of cases of VL, and its treatment is a challenge once it shows high toxicity. Thats why it's important to search for therapeutic alternatives. Drug repositioning has been an important approach in reducing cost and time for the research. In addition, controlled drug delivery systems such as liposomes have contributed to the reduction of the therapeutic dose and, consequently, to the adverse effects of the drugs. In this study, the anti-Leishmania potential of sertraline antidepressant (SERT) was evaluated in in vitro and in vivo models, using the free drug (SERT) and the encapsulated in nanoliposomes (SERT-LP). SERT showed a potent activity against promastigotes and intracellular amastigotes with concentrations of 50% Effective Concentration (EC50) of 0.7 µM and 4 µM, respectively. The in vitro association of SERT with miltefosine demonstrated mean values of the sum of Fractional Inhibitory Concentrations (XΣCIF) of 0.64 and 1.32 in promastigotes and amastigotes, respectively, resulting in an additive association. Aiming for in vivo efficacy studies, a pharmacokinetic study of free sertraline in the murine model was performed, resulting in a plasma halflife (T1/2) of approximately 8 hours. In vivo study of the efficacy of SERT demonstrated therapeutic failure, in oral and subcutaneous administration. However, when encapsulated in nanoliposomes (125 nm) charge negativelly (SERT-LP), it resulted in a significant reduction (89%) of the parasite burden in the liver of mice treated for 10 days at 1 mg/kg. Unexpectedly, at a dose 15 times higher, showed 100% of increase in the parasite burden, which was correlated with increased of cytokine IL-6 and chemokine MCP-1 levels. Studies of biodistribution of SERT-LP, demonstrated the presence of the formulation in liver and spleen - 12 to 48 hours after subcutaneous administration. Histopathological studies of animals treated at 1 and 15 mg/kg for 10 days showed the presence of multiple foci of inflammatory lymphohistiocytic infiltrate, forming granulomatous sketches in hepatic parenchyma. In the spleen, the presence of reactive lymphoid hyperplasia was observed, not differing from the control group. The data obtained in the histopathological study corroborate with 8 the levels of cytokines observed in the flow cytometry, resulting in an inflammatory infiltrate. The present study demonstrates the potential of this new sertraline nanoformulation in experimental LV and suggests for the first time a correlation between increased parasite burden with dose-dependent immunomodulation of the drug. (AU)

Leishmaniasis , Leishmaniasis, Visceral , Sertraline , Biological Therapy
J. venom. anim. toxins incl. trop. dis ; 24: 30, 2018. tab, graf, ilus
Article in English | LILACS, VETINDEX | ID: biblio-976028


Drug repurposing has been an interesting and cost-effective approach, especially for neglected diseases, such as Chagas disease. Methods: In this work, we studied the activity of the antidepressant drug sertraline against Trypanosoma cruzi trypomastigotes and intracellular amastigotes of the Y and Tulahuen strains, and investigated its action mode using cell biology and in silico approaches. Results: Sertraline demonstrated in vitro efficacy against intracellular amastigotes of both T. cruzi strains inside different host cells, including cardiomyocytes, with IC50 values between 1 to 10 µM, and activity against bloodstream trypomastigotes, with IC50 of 14 µM. Considering the mammalian cytotoxicity, the drug resulted in a selectivity index of 17.8. Sertraline induced a change in the mitochondrial integrity of T. cruzi, resulting in a decrease in ATP levels, but not affecting reactive oxygen levels or plasma membrane permeability. In silico approaches using chemogenomic target fishing, homology modeling and molecular docking suggested the enzyme isocitrate dehydrogenase 2 of T. cruzi (TcIDH2) as a potential target for sertraline. Conclusions: The present study demonstrated that sertraline had a lethal effect on different forms and strains of T. cruzi, by affecting the bioenergetic metabolism of the parasite. These findings provide a starting point for future experimental assays and may contribute to the development of new compounds.(AU)

Trypanosoma cruzi , In Vitro Techniques , Sertraline , Drug Repositioning
Article in English | WPRIM | ID: wpr-772288


Bone wound healing is a highly dynamic and precisely controlled process through which damaged bone undergoes repair and complete regeneration. External factors can alter this process, leading to delayed or failed bone wound healing. The findings of recent studies suggest that the use of selective serotonin reuptake inhibitors (SSRIs) can reduce bone mass, precipitate osteoporotic fractures and increase the rate of dental implant failure. With 10% of Americans prescribed antidepressants, the potential of SSRIs to impair bone healing may adversely affect millions of patients' ability to heal after sustaining trauma. Here, we investigate the effect of the SSRI sertraline on bone healing through pre-treatment with (10 mg·kg sertraline in drinking water, n = 26) or without (control, n = 30) SSRI followed by the creation of a 5-mm calvarial defect. Animals were randomized into three surgical groups: (a) empty/sham, (b) implanted with a DermaMatrix scaffold soak-loaded with sterile PBS or (c) DermaMatrix soak-loaded with 542.5 ng BMP2. SSRI exposure continued until sacrifice in the exposed groups at 4 weeks after surgery. Sertraline exposure resulted in decreased bone healing with significant decreases in trabecular thickness, trabecular number and osteoclast dysfunction while significantly increasing mature collagen fiber formation. These findings indicate that sertraline exposure can impair bone wound healing through disruption of bone repair and regeneration while promoting or defaulting to scar formation within the defect site.

Animals , Apoptosis , Bone Morphogenetic Protein 2 , Cell Culture Techniques , Cell Proliferation , Enzyme-Linked Immunosorbent Assay , Immunohistochemistry , Male , Mice , Mice, Inbred C57BL , Osteogenesis , Random Allocation , Real-Time Polymerase Chain Reaction , Selective Serotonin Reuptake Inhibitors , Pharmacology , Sertraline , Pharmacology , Skull , Diagnostic Imaging , Wounds and Injuries , Wound Healing , X-Ray Microtomography
Psychiatry Investigation ; : 147-155, 2018.
Article in English | WPRIM | ID: wpr-741904


OBJECTIVE: The aim of the present study was to provide clinical consensus and evidence regarding initial treatment strategies for the pharmacological treatment of social anxiety disorder (SAD) in Korea. METHODS: We prepared a questionnaire to derive a consensus from clinicians regarding their preference for the pharmacological treatment of SAD in Korea. Data regarding medication regimens and psychotropic drugs used during initial treatment, the doses used, and the pharmacological treatment duration were obtained. Responses were obtained from 66 SAD experts, and their opinions were classified into three categories (first-line, second-line, third-line) using a chi-square analysis. RESULTS: Clinicians agreed upon first-line regimens for SAD involving monotherapy with selective serotonin reuptake inhibitors (SSRIs) or the serotonin-norepinephrine reuptake inhibitor (SNRI) venlafaxine, or combined therapy using antidepressants with betablockers or benzodiazepines on a standing or as-needed basis. First-line psychotropic drug choices for initial treatment included the following: escitalopram, paroxetine, sertraline, venlafaxine, and propranolol. The medication dosage used by domestic clinicians was found to be comparable with foreign guidelines. Domestic clinicians tended to make treatment decisions in a shorter amount of time and preferred a similar duration of maintenance treatment for SAD when compared with foreign clinicians. CONCLUSION: This study may provide significant information for developing SAD pharmacotherapy guidelines in Korea, especially in the early stage of treatment.

Antidepressive Agents , Anxiety Disorders , Anxiety , Benzodiazepines , Citalopram , Consensus , Drug Therapy , Korea , Paroxetine , Propranolol , Psychotropic Drugs , Selective Serotonin Reuptake Inhibitors , Sertraline , Venlafaxine Hydrochloride