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Braz. j. med. biol. res ; 53(1): e8652, Jan. 2020. tab, graf
Article in English | LILACS | ID: biblio-1055481


Glycemic variability (GV) may be linked to the development of diabetic complications by inducing inflammation, oxidative stress, and endothelial dysfunction. Flash glucose monitoring (FGM) provides a novel method of continuously monitoring interstitial glucose levels for up to 14 days. This study randomly assigned poorly controlled type 2 diabetes mellitus patients treated with metformin and multiple daily injections of insulin (n=60) to either continuous subcutaneous insulin infusion (CSII) treatment or CSII in combination with liraglutide (CSII+Lira) treatment for 14 days during hospitalization. GV was assessed using a FGM system; weight and cardiometabolic biomarkers were also evaluated. The coefficient of variation was significantly reduced in the CSII+Lira group (P<0.001), while no significant change was observed in the CSII group. The changes differed significantly between the two groups in mean amplitude of glycemic excursions (P=0.004), standard deviation (P=0.006), and the percentage of time in the target range (4-10 mmol/L, P=0.005 and >10 mmol/L, P=0.028). The changes in mean of daily differences, interquartile range, and percentage of time in hypoglycemia (<3.3 mmol/L) and hyperglycemia (>13.9 mmol/L) identified by FGM showed no difference. Treatment with liraglutide increased serum adiponectin [33.5 (3.5, 47.7) pg/mL, P=0.003] and heme oxygenase-1 levels [0.4 (-0.0, 1.8) ng/mL, P=0.001] and reduced serum leptin levels [-2.8 (3.9) pg/mL, P<0.001]. Adding the glucagon-like peptide-1 analog liraglutide improved GV, weight, and some cardiometabolic risk markers. The FGM system is, therefore, shown to be a novel and useful method for glucose monitoring.

Humans , Male , Female , Adult , Middle Aged , Insulin Infusion Systems , Blood Glucose Self-Monitoring/methods , Diabetes Mellitus, Type 2/drug therapy , Liraglutide/administration & dosage , Hypoglycemic Agents/administration & dosage , Insulin/administration & dosage , Pilot Projects , Diabetes Mellitus, Type 2/blood
Article in Korean | WPRIM | ID: wpr-766554


Over the last 5 years, the Korean Ministry of Food and Drug Safety has approved four anti-obesity drugs for long-term weight management. In this review, the mechanisms of action and clinical applications of lorcaserin, naltrexone/bupropion, liraglutide, and phentermine/topiramate have been clarified. Lorcaserin stimulates proopiomelanocortin/cocaine- and amphetamine-regulated transcript neurons in the arcuate nucleus. Naltrexone/bupropion reduces body weight by controlling the hedonic reward system of food intake. The hypophagic effect of liraglutide depends on the direct activation of the proopiomelanocortin/cocaine- and amphetamine-regulated transcript neurons and indirect suppression of neuropeptide Y/agouti-related peptide neurons through gammaaminobutyric acid-dependent signaling, with an additional thermogenic effect. Phentermine/topiramate induces weight loss by elevating the norepinephrine levels in the hypothalamus, reducing energy deposition in the adipose tissue and skeletal muscle, and elevating the corticotropin-releasing hormone in the hypothalamus. In patients with high cardiovascular risks or type 2 diabetes mellitus, lorcaserin and liraglutide are appropriate. In patients with mood disorders, naltrexone/bupropion could be considered as the first choice of therapy. Notably, lorcaserin and liraglutide are neutral in the aspect of sleep disorder. In case of obese individuals with obstructive sleep apnea, liraglutide or phentermine/topiramate would be selected as the treatment option. These four drugs should be used after considering the patients' co-morbidities of obesity.

Adipose Tissue , Anti-Obesity Agents , Arcuate Nucleus of Hypothalamus , Body Weight , Corticotropin-Releasing Hormone , Diabetes Mellitus, Type 2 , Eating , Humans , Hypothalamus , Korea , Liraglutide , Mood Disorders , Muscle, Skeletal , Neurons , Neuropeptides , Norepinephrine , Obesity , Pharmacology , Reward , Sleep Apnea, Obstructive , Sleep Wake Disorders , Weight Loss
Article in English | WPRIM | ID: wpr-738872


The Korean Ministry of Food and Drug Safety has approved three anti-obesity drugs for long-term management in the past decade. In addition, since 2019, bariatric surgery has been financially supported by National Health Insurance Service in Korea. In this review, the mechanisms of action and the clinical implications of the recently approved anti-obesity drugs, lorcaserin, naltrexone/bupropion, and liraglutide are explained. Lorcaserin stimulates proopiomelanocortin (POMC)/cocaine- and amphetamine-regulated transcript (CART) neurons and inhibits neuropeptide Y (NPY)/agouti-related peptide (AgRP) neurons, which results in the activation of melanocortin 3/4 receptors. Naltrexone/bupropion stimulates POMC neurons through bupropion; this stimulation is augmented by blocking the autoinhibitory mechanism of POMC with naltrexone. The hypophagic effect of liraglutide is mediated through the direct activation of POMC/CART neurons and the indirect suppression of NPY/AgRP neurons through γ-aminobutyric acid-dependent signaling, with adjunctive suppression of the mesolimbic dopamine reward system. In addition to liraglutide, another glucagon-like peptide-1 receptor agonist, semaglutide, is expected to be added to the list of anti-obesity drugs in the near future. In patients with obesity and high cardiovascular risk, lorcaserin was considered neutral and liraglutide was considered favorable, whereas inconclusive results were obtained for naltrexone/bupropion.

Anti-Obesity Agents , Bariatric Surgery , Bupropion , Dopamine , Glucagon-Like Peptide-1 Receptor , Humans , Korea , Liraglutide , Naltrexone , National Health Programs , Neurons , Neuropeptide Y , Obesity , Pro-Opiomelanocortin , Reward
Acta Physiologica Sinica ; (6): 514-526, 2019.
Article in English | WPRIM | ID: wpr-777160


Glucagon-like peptide-1 (GLP-1) expression is shared by both intestinal cells and neurons of brainstem, which plays anorexigenic role on food intake. However, the exact source of physiological GLP-1 influencing food intake and pertinent mechanism of GLP-1 receptor agonists (GLP-1RA) remain unelucidated. In this study, the immediate early gene product c-Fos was chosen as the specific antigen for immunohistochemistry to show the certain areas of central nervous system (CNS) activation by the GLP-1RA. Thirty normal SD rats were randomly assigned to 3 groups, which were single intraperitoneally injected with Liraglutide (200 μg/kg), Exenatide (10 μg/kg) and saline, respectively. After injection, the amount of food intake and acute glycemic variation were assessed for comparison. The results showed that acute pharmacological dosage of GLP-1RA (Liraglutide or Exenatide) could significantly influence food intake. However, glycemic change indicated that the anorexic effect was dissociated with change in blood glucose in normal rats. Moreover, c-Fos was expressed significantly higher in major critical nuclei related to food intake in GLP-1RA groups when compared with the control group, and its expression was also found in spinal cord. The results suggested that acute administration of pharmacological doses of GLP-1 influences CNS via circulation and vagal pathways, especially on the arcuate nucleus (ARC) and the nucleus of solitary tract (NTS), and GLP-1 modulates autonomic nervous activities.

Animals , Eating , Exenatide , Pharmacology , Glucagon-Like Peptide-1 Receptor , Liraglutide , Pharmacology , Random Allocation , Rats , Rats, Sprague-Dawley
Article in English | WPRIM | ID: wpr-763705


The prevalence of type 2 diabetes mellitus (T2DM), which is associated with cardiovascular morbidity and mortality, is increasing worldwide. Although there have been advances in diabetes treatments that reduce microvascular complications (nephropathy, neuropathy, retinopathy), many clinical studies have found that conventional oral hypoglycemic agents and glucose control alone failed to reduce cardiovascular disease. Thus, incretin-based therapies including glucagon-like peptide 1 (GLP-1) receptor agonists (RAs) and sodium-glucose cotransporter 2 inhibitors (SGLT-2Is) represent a new area of research, and may serve as novel therapeutics for treating hyperglycemia and modifying other cardiovascular risk factors. Recently, it has been confirmed that several drugs in these classes, including canagliflozin, empagliflozin, semaglutide, and liraglutide, are safe and possess cardioprotective effects. We review the most recent cardiovascular outcome trials on GLP-1RAs and SGLT-2Is, and discuss their implications for treating patients with T2DM in terms of protective effects against cardiovascular disease.

Canagliflozin , Cardiovascular Diseases , Diabetes Mellitus , Diabetes Mellitus, Type 2 , Glucagon-Like Peptide 1 , Glucose , Heart Failure , Humans , Hyperglycemia , Hypoglycemic Agents , Liraglutide , Mortality , Myocardial Ischemia , Prevalence , Risk Factors
Journal of Korean Diabetes ; : 149-156, 2019.
Article in Korean | WPRIM | ID: wpr-761490


According to the American Diabetes Association (ADA) and the European Association for the Study of Diabetes guideline for treatment of diabetes, glucagon-like peptide-1 receptor agonist (GLP-1 RA) is recommended in diabetic patients with established atherosclerotic cardiovascular disease. This recommendation is based on the results of recent cardiovascular outcome trials of this kind of medications. GLP-1 RAs have a glucose lowering effect with weight loss and a lower incidence of hypoglycemia, and can improve cardiovascular outcomes such as three-point major cardiovascular events composed of death from cardiovascular causes, non-fatal myocardial infarction, and non-fatal stroke. Also, several GLP-1 RAs have beneficial effects on renal outcomes, mainly due to improvement in macroalbuminuria. In addition, high-dose liraglutide (3 mg/day subcutaneous injection) showed efficacy for reducing body weight. Therefore GLP-1 RA may be effective in patients with established cardiovascular disease, chronic kidney disease, and/or metabolic syndrome.

Body Weight , Cardiovascular Diseases , Diabetes Mellitus , Glucagon-Like Peptide 1 , Glucagon-Like Peptide-1 Receptor , Glucose , Humans , Hypoglycemia , Incidence , Kidney Diseases , Liraglutide , Myocardial Infarction , Obesity , Renal Insufficiency, Chronic , Stroke , Weight Loss
Rev. salud bosque ; 9(2): 47-55, 2019. tab
Article in Spanish | LILACS, COLNAL | ID: biblio-1103199


Introducción. El sobrepeso y la obesidad son condiciones que vienen en aumento en Colombia y en el mundo, lo cual es preocupante ya que gene-ran predisposición para enfermedades que causan alta morbimortalidad. El tratamiento para estas enfermedades necesita un enfoque multidiscipli-nario que incluya hábitos saludables con cambios en la dieta, aumento de la actividad física y, en ocasiones, uso de fármacos y cirugía bariá-trica como tratamiento coadyuvante. Algunos medicamentos GLP-1 han demostrado eficacia en la pérdida de peso, en especial la liraglutida, un medicamento usado como complemento de la dieta y el ejercicio para lograr mayor control glucémico en adultos con diabetes mellitus tipo 2 que también tienen enfermedad cardiovascular.Objetivo.Evaluar la eficacia y seguridad de la liraglutida como medica-mento coadyuvante para disminuir el índice de masa corporal (IMC) en personas con sobrepeso (IMC=25-30 kg/m2)y obesidad (IMC>30 kg/m2).Materiales y métodos. Se realizó una búsqueda en las bases de datos Trip Database, Embase, PubMed, Scopus y Clinical Key sobre estudios que cumplieran los criterios de inclusión y que evaluaran la disminución de peso con el uso de liraglutida. Conclusiones. La liraglutida es un medicamento que reduce el IMC en personas con sobrepeso y obesidad; sin embargo, presenta efectos ad-versos que deben ser evaluados, razón por la cual es necesario ampliar la literatura y las líneas de investigación para, de esta manera, tener evi-dencia clara con la cual sea posible discutir su eficacia y seguridad como tratamiento coadyuvante en personas con sobrepeso

Introduction: Overweight and obesity are two conditions that have been increasing in Colombia and worldwide, what is wo-rry in about this is the predispose that illness can cause high mortality and mobility. Treatment of overweight and obesity needs multidisciplinary approach in which should be included healthy habits with change in diet and increase physical activi-ty, sometimes the use of medications and bariatric surgery can be taken in mind as adjuvant therapy. Different characteristics have been demonstrated in medications like GLP-1 specially liraglutide for weight lossObjective: Evaluate the efficacy and safety of liraglutide as a adjuvant medication to reduce the body mass index (BMI) in overweight (BMI: 25-30 Kg / m2) and obesity (BMI:> 30 Kg / m2) worldwideMaterials and methods: We will search for studies in the di-fferent databases (TRIP, Embase, Pubmed, Scopus and Clini-calKey), which must meet inclusion criteria and evaluate weight reduction with the use of liraglutide.Conclusions: Liraglutide is a medicine that reduces BMI in people with overweight and obesity, however, it has adverse effects that must be evaluated. Therefore, the li-terature and lines of research should be expanded in the future; and in this way have clear evidence to discuss the efficacy and safety of liraglutide as a adjuvant treatment in overweight people.

Introdução. Sobrepeso e obesidade são condições que estão aumentando na Colômbia e no mundo, o que é preocupante, pois gera predisposição para doenças que causam alta mor-bimortalidade. O tratamento para essas doenças requer uma abordagem multidisciplinar que inclua hábitos saudáveis com mudanças na dieta, aumento da atividade física e, às vezes, uso de drogas e cirurgia bariátrica como tratamento adjuvante. Alguns medicamentos para o GLP-1 provaram ser eficazes na perda de peso, especialmente o liraglutido, um medicamento usado como complemento à dieta e ao exercício para obter maior controle glicêmico em adultos com diabetes mellitus tipo 2 que também apresentam doenças cardiovasculares.Objetivo. Avaliar a eficácia e segurança do liraglutido como medicamento adjuvante para reduzir o índice de massa corpo-ral (IMC) em pessoas com sobrepeso (IMC = 25-30 kg /m2) e obesidade (IMC> 30 kg /m2).Materiais e métodos. Pesquisamos os bancos de dados Trip Database, Embase, PubMed, Scopus e Clinical Key em estudos que atenderam aos critérios de inclusão e que avaliaram a per-da de peso com o uso de liraglutido.Conclusões. O liraglutido é um medicamento que reduz o IMC em pessoas com sobrepeso e obesidade; no entanto, apresenta efeitos adversos que devem ser avaliados, motivo pelo qual é necessário ampliar a literatura e as linhas de pesquisa para, dessa forma, ter evidências claras com as quais é possível dis-cutir sua eficácia e segurança como tratamento adjuvante em pessoas com excesso de peso.

Humans , Male , Female , Overweight/drug therapy , Liraglutide/therapeutic use , Overweight , Obesity Management
Braz. arch. biol. technol ; 62: e19180563, 2019. tab, graf
Article in English | LILACS | ID: biblio-1039120


Abstract The objective of this study was to evaluate the effect of liraglutide, an analog of glucagon-like peptide-1 (GLP-1) in association with physical exercise, on the metabolic and biochemical parameters of rats induced to obesity with a cafeteria diet. Male Wistar rats, aged 21 days, were randomly divided into: Controls (CON) receiving standard feed and water ad libitum; and obese (OBESE) receiving cafeteria diet ad libitum, added to the standard diet. Groups were then subdivided into: Liraglutide animals that received subcutaneous injections of liraglutide from 80 to 90 days of life; exercised (EXE) animals submitted to swimming sessions, three days a week (15 min); and liraglutide + EXE animals that received liraglutide in association with physical exercise. Treatment with liraglutide reduced deposits of mesenteric and periepididymal fat, HOMA-IR, triglycerides, glucose and insulin in obese group. It is important to note that the association of the two treatments reduced the body weight in animals, deposits of mesenteric and periepididymal fat, HOMA-IR, blood triglyceride levels, glucose and insulin in obese rats. As such, the association of liraglutide with exercise potentiated the effects of the drug and ameliorated obesity pathology more effectively. retirar

Animals , Metabolic Syndrome , Liraglutide/therapeutic use , Motor Activity , Obesity/drug therapy , Rats, Wistar
MedUNAB ; 22(3): 314-321, 29-11-2019.
Article in English, Spanish | LILACS | ID: biblio-1026871


Introducción. El exceso de peso es una condición prevalente en Colombia. Esto conlleva a realizar múltiples intentos para perder peso, muchos autodirigidos y con riesgos, siendo un motivo de consulta frecuente en atención médica primaria y especializada. Metodología. Estudio de corte transversal con datos secundarios de la consulta de endocrinología de pacientes que consultaron por percepción de aumento de peso. Se indagó por 18 métodos convencionales y populares para perder peso, su duración, peso perdido y posterior re ganancia. Resultados. Se incluyeron 100 personas, 79% mujeres, con un promedio de edad de 41.1 años, índice de masa corporal de 32.9 ± 4.6 kg/m2 y perímetro abdominal de 102.7 ± 12.5 cm. En promedio se registraron entre 4 y 5 intentos para perder peso por persona antes de consultar al endocrinólogo, con una mediana de historia de exceso de peso de 10 años. Todos los intentos lograron alguna pérdida con posterior reganancia del total del peso perdido, excepto liraglutida. No se encontró asociación significativa entre variables antropométricas y el número de intentos para perder peso. Discusión. Los intentos de pérdida de peso más empleados por la población evaluadas son los que no están aprobados o carecen de evidencia científica robusta. Conclusiones. Los pacientes con sobrepeso y obesidad realizan múltiples intentos fallidos para perder peso antes de consultar al médico especialista. La reganancia es muy frecuente, independientemente del tipo de intento. Cómo citar. Wandurraga EA, Marín Carrillo LF, Ardila Gutiérrez MA, Serrano-Gómez SE. Intentos para perder peso en una población con sobrepeso y obesidad referida a un centro de endocrinología en Colombia. MedUNAB. 2019:22(3): 314-321. doi: 10.29375/01237047.3569

Introduction. Excess weight is a prevailing condition in Colombia. This leads to many weight loss attempts, many self-managed and with risks, being a frequent reason for consulting primary and specialized healthcare. Methodology. Cross-sectional study with secondary data from the endocrinology consultation of patients who made the appointment due to a perceived increase in weight. Eighteen conventional and popular ways of losing weight, their duration, the weight lost and the subsequent regained weight were investigated. Results. One hundred people were included, 79% women with an average age of 41.1 years, a body mass index of 32.9 ± 4.6 kg/m2 and a waist circumference of 102.7 ± 12.5 cm. Each person reported an average of four to five attempts to lose weight before consulting the endocrinologist, with a median history of being overweight of ten years. All of the attempts achieved some weight loss with subsequent regain of the total weight lost, except when using liraglutide. A significant association was not found between the anthropometric variables and the number of weight loss attempts. Discussion. The weight loss methods most used by the assessed population are ones that are not approved or that lack strong scientific evidence. Conclusions. Overweight or obese patients make multiple failed attempts to lose weight before consulting a specialist physician. Regain of the lost weight is frequent, regardless of the method used. Cómo citar. Wandurraga EA, Marín Carrillo LF, Ardila Gutiérrez MA, Serrano-Gómez SE. Intentos para perder peso en una población con sobrepeso y obesidad referida a un centro de endocrinología en Colombia. MedUNAB. 2019:22(3): 314-321. doi: 10.29375/01237047.3569

Introdução. Excesso de peso é uma condição prevalecente na Colômbia. Isso leva a várias tentativas de perda de peso, muitas auto-dirigidas e de risco, sendo motivo de consultas frequentes em atendimento médico primário e especializado. Metodologia. Estudo transversal com dados secundários da consulta de endocrinología de pacientes que consultaram para percepção do ganho de peso. Foram investigados 18 métodos convencionais e populares para perder peso, sua duração, peso perdido e subsequente reganho. Resultados. Foram incluídas 100 pessoas, 79% mulheres, com idade média de 41,1 anos, índice de massa corporal de 32,9 ± 4,6 kg / m2 e perímetro abdominal de 102,7 ± 12,5 cm. Em média, foram registradas entre quatro e cinco tentativas de perda de peso por pessoa antes de consultar o endocrinologista, com uma mediana de história de excesso de peso de 10 anos. Todas as tentativas alcançaram alguma perda com subsequente re-ganancia do peso total perdido, exceto o liraglutida. Não foi encontrada associação significativa entre as variáveis antropométricas e o número de tentativas de perda de peso. Discussão. As tentativas de perda de peso mais utilizadas pela população avaliada são aquelas que não são aprovadas ou não possuem evidências científicas robustas. Conclusões. Pacientes com sobrepeso e obesos fazem várias tentativas fracassadas de perder peso antes de consultar o especialista. A re-ganancia de peso é frequente, independentemente do tipo de tentativa. Cómo citar. Wandurraga EA, Marín Carrillo LF, Ardila Gutiérrez MA, Serrano-Gómez SE. Intentos para perder peso en una población con sobrepeso y obesidad referida a un centro de endocrinología en Colombia. MedUNAB. 2019:22(3): 314-321. doi: 10.29375/01237047.3569

Weight Loss , Anti-Obesity Agents , Overweight , Liraglutide , Obesity
Rev. colomb. cardiol ; 25(5): 333-339, sep.-oct. 2018. tab
Article in Spanish | LILACS, COLNAL | ID: biblio-1042771


Resumen Introducción: la enfermedad cardiovascular es la principal causa de muerte en el mundo, así como la primera causa de morbilidad y mortalidad en pacientes con diabetes mellitus; por tanto, es importante conocer los diferentes medicamentos que existen hoy para el manejo de la diabetes mellitus y sus efectos, tanto positivos como negativos a nivel cardiovascular. De ahí que las diferentes sociedades y asociaciones científicas del mundo hayan emitido la recomendación de que todos los medicamentos para el tratamiento de la diabetes mellitus tipo 2 deben ser evaluados y certificados como seguros a nivel cardiovascular. Metodología: se hizo una búsqueda ampliada de la literatura existente acerca de los antidiabéticos actuales y sus efectos cardiovasculares. Resultados: existen diferentes tipos de medicamentos que se han relacionado con disminución o aumento del riesgo cardiovascular. En la actualidad hay evidencia que relaciona la metformina (biguanida), la empagliflozina (inhibidor del cotransportador sodio- glucosa 2) y la liraglutide (análogo de péptido similar al glucagón) con menos muerte cardiovascular y eventos cardiovasculares en pacientes con enfermedad cardiovascular establecida. Conclusión: los pacientes con enfermedad cardiovascular conocida pueden tener un beneficio adicional seleccionando medicamentos hipoglucemiantes con un mejor perfil de seguridad cardiovascular.

Abstract Introduction: Cardiovascular disease is the main cause of death worldwide, as well as the first cause of morbidity and mortality in patients with diabetes mellitus. For these reasons it is important to know the different drugs currently available to manage diabetes mellitus and their positive and negative effects at cardiovascular level. Hence, different scientific societies and associations of the world have issued the recommendation that all drugs for the treatment of type 2 diabetes mellitus must be evaluated and certified as safe at cardiovascular level. Methodology: An extensive search was carried out on the existing literature on current antidiabetic drugs and their cardiovascular effects. Results: There are different types of drugs that are associated with a decrease or increase in cardiovascular risk. Currently, there is evidence that associated metformin (biguanide), empagliflozin (sodium-glucose cotransporter 2 inhibitor), and liraglutide (a glucagon-like peptide analogue), with less cardiovascular deaths and cardiovascular events in patients with established cardiovascular disease. Conclusion: Patients with known cardiovascular disease may have an additional benefit in selecting glucose-lowering drugs with a better cardiovascular safety profile.

Humans , Male , Female , Middle Aged , Heart Disease Risk Factors , Hypoglycemic Agents , Liraglutide
Medicina (B.Aires) ; 78(4): 225-233, ago. 2018. graf, tab
Article in Spanish | LILACS | ID: biblio-954988


La diabetes mellitus es una verdadera pandemia; la diabetes tipo 2 en particular, con su carácter progresivo, constituye un grave problema de salud. A pesar de los avances e innovaciones en el tratamiento, continúa generando una alta morbimortalidad, debido a que muchos pacientes no logran los objetivos de control metabólicos, entre otras causas por la inercia clínica, el temor a la hipoglucemia, el aumento de peso, la complejidad del tratamiento y la falta de adherencia al mismo. En el último tiempo, se ha evaluado con éxito los resultados clínicos del uso combinado de insulina basal y agonistas del receptor del péptido similar al glucagón tipo 1 (AR-GLP1). Se propone, por lo tanto, el uso combinado de una insulina basal (insulina degludec) con un AR-GLP1 (liraglutida), en un único dispositivo (IdegLira), como una alternativa terapéutica eficaz y segura para la intensificación del tratamiento de las personas con diabetes tipo 2. IdegLira ha demostrado mayores reducciones de HbA1c comparado con sus componentes individuales, con un bajo riesgo de hipoglucemia y pérdida de peso, tanto en pacientes naive de insulina como en aquellos previamente insulinizados. En esta revisión se describe la farmacología, el racional de la combinación y la evidencia clínica relevante de la seguridad y eficacia de IdegLira.

Diabetes mellitus is a true pandemic; type 2 diabetes in particular, with its progressive nature, constitutes a serious health problem. Despite advances and innovations in treatment, it continues to generate high morbidity and mortality.Many patients do not achieve their metabolic control objectives, due to clinical inertia, fear of hypoglycaemia, weight gain, the complexity of the treatment and the lack of adherence to it. Recently, the clinical results of the combined use of basal insulin and agonist receptor of the glucagon-like peptide type 1 (AR-GLP1) have been successfully evaluated. Therefore, the combined use of a basal insulin (insulin degludec) with an AR-GLP1 (liraglutide), in a single device (IdegLira), is proposed as an effective and safe therapeutic alternative for the treatment intensification in people with type 2 diabetes. IdegLira has shown greater reductions in HbA1c compared to its individual components, with a low risk of hypoglycaemia and weight loss, both in insulin naïve patients and in those previously insulinized. In this review we describe the pharmacology, the rational of the combination and the most relevant clinical evidence on IdegLira safety and efficacy.

Humans , Insulin, Long-Acting/administration & dosage , Diabetes Mellitus, Type 2/drug therapy , Liraglutide/administration & dosage , Hypoglycemic Agents/administration & dosage , Clinical Trials as Topic , Drug Combinations , Drug Therapy, Combination
Article in Korean | WPRIM | ID: wpr-714786


In 2008, the United States Food and Drug Administration issued guidance which mandated long-term cardiovascular outcome trials (CVOTs) to assess the safety of new antidiabetic drugs for type 2 diabetes. Since 2008, three CVOTs that have studied dipeptidyl peptidase-4 (DPP-4) inhibitors and four CVOTs of a glucagon-like peptide-1 (GLP-1) receptor agonist (GLP-1RA) have been reported. Each of the completed CVOTs showed the noninferiority of respective drugs to placebo for primary CV composite endpoint. Among them, liraglutide and semaglutide showed a reduction of major adverse cardiovascular events. However, the mechanisms for the observed cardiovascular differences between DPP-4 inhibitors and GLP-1RA, and across individual GLP-1RA are not clearly understood. Therefore, this review will summarize the CVOTs of the DPP-4 inhibitors and GLP-1RA, interpretation of cardioprotective results of incretin-based therapy and the possible mechanism of action.

Diabetes Mellitus, Type 2 , Dipeptidyl-Peptidase IV Inhibitors , Glucagon-Like Peptide 1 , Hypoglycemic Agents , Incretins , Liraglutide , United States Food and Drug Administration
Korean Journal of Medicine ; : 501-508, 2018.
Article in Korean | WPRIM | ID: wpr-718868


Obesity is a chronic disorder that is a significant risk factor for diabetes, cardiovascular diseases, malignancy, and other chronic diseases. Lifestyle modifications form the basis of most treatments for obesity, but it has become clear that such modifications alone are not enough for many obese patients. When a behavioral approach is insufficient, pharmacological treatment may be recommended. In recent years, the US Food and Drug Administration (FDA) has withdrawn several therapeutic options for obesity due to their side effects, but has approved four novel anti-obesity agents. Until recently, orlistat was the only drug approved for the management of long-term obesity, but the US FDA approved the novel anti-obesity drugs lorcaserin and phentermine/topiramate in 2012, and naltrexone/bupropion and liraglutide in 2014. The present review discusses the different pharmacotherapeutic options for the treatment of obesity.

Anti-Obesity Agents , Cardiovascular Diseases , Chronic Disease , Humans , Life Style , Liraglutide , Obesity , Risk Factors , United States Food and Drug Administration
São Paulo; HSPM; 2018.
Non-conventional in Portuguese | ColecionaSUS, LILACS, ColecionaSUS, SMS-SP, HSPM-Producao, SMS-SP | ID: biblio-1254741


RESUMO O baypass gástrico em Y de Roux(GYR) é um dos principais procedimentos utilizados para tratamento da obesidade quando dieta e medição não funcionam, porém a longo prazo pode levar a uma complicação rara e de etiologia ainda imprecisa, a Hipoglicemia pós-prandial (HPP). Surge 1 a 3 anos após o procedimento, acredita-se que em reposta ao aumento da secreção de GLP-1 e consequente aumento de insulina, levando a hipoglicemia. É percebido na maioria das vezes na presença de alguns sintomas, como tontura, fadiga, fraqueza, sudorese, entre outros; com a detecção de hipoglicemia no momento, e melhora após consumo de carboidrato, podendo ser realizados exames posteriormente para confirmação. O tratamento inicial pode ser feito com uma dieta restrita em carboidrato, podendo ser associado medicação, entre elas, o análogo de GLP-1, medidas mais invasivas, como pancreatectomia são utilizadas em casos refratários ou com sintomas mais graves. Foi utilizado Victoza no tratamento de uma paciente que desenvolveu HPP um ano e meio após cirurgia, com sintomas principalmente após o janta, realizou-se teste oral de tolerância a glicose com e sem o uso da medicação, sendo comprovado a eficácia do tratamento com ausência de hipoglicemia no primeiro teste, e 2 episódios de hipoglicemia e aumento de curva de insulina na segunda etapa. Palavras-chave: cirurgia bariátrica, hipoglicemia, liraglutida

Humans , Male , Female , Bariatric Surgery , Liraglutide , Hypoglycemia
Article in English, Portuguese | LILACS | ID: biblio-909292


Nos últimos anos, os avanços nas descobertas da terapêutica para o DM2 entusiasmaram os clínicos e especialistas no que diz respeito à redução dos eventos cardiovasculares, internações e mortalidade. Outros estudos ainda estão em andamento e prometem fortalecer a expectativa de mudança nos desfechos cardiovasculares dessa população. O objetivo dessa revisão consiste em reunir os principais estudos clínicos que demonstraram a segurança e/ou redução na ocorrência de eventos cardiovasculares com uso de fármacos anti-hiperglicemiantes.

In recent years, breakthroughs in therapeutic findings for DM2 have encouraged physicians and specialists with regards to the reduction of cardiovascular events, hospitalization and mortality. Other studies are underway, and promise to strengthen the prospects of change in cardiovascular outcomes for this population. The goal of this review is to bring together the most important clinical trials that have demonstrated safety and/or a decrease in cardiovascular events with the use of antihyperglycemic drugs.

Humans , Cardiovascular Diseases/diagnostic imaging , Diabetes Mellitus/drug therapy , Insulin/history , Metformin/history , Liraglutide/administration & dosage , Hypoglycemic Agents/economics , Hypoglycemic Agents/adverse effects
Rev. colomb. nefrol. (En línea) ; 4(1): 69-73, Jan.-June 2017.
Article in English | LILACS, COLNAL | ID: biblio-1092983


Abstract In recent years, several new antidiabetic drugs have been developed, among which only two have demonstrated superiority in cardiovascular protection. They are liraglutide and empagliflozine, which belong, respectively, to GLP-1 RA and SGLT-2Í. These medications have also shown benefits in kidney protection. However, in a recent survey of the author among nephrologists in a large colombian city, it has been detected that most do not use these drugs. The greater resistance to the limitation in its use is due to the advanced stages of chronic kidney disease where they are contraindicated, but also to the anawareness of their potential benefits. In this regard, the nephrologists accepted they should learn more about these antidiabetic medicines, because the type of patient that is frequently attended in their consultation will undoubtly benefit, and considering they are obligated to handle the diabetic patient directly.

Resumen En los últimos años se han desarrollado nuevos fármacos antidiabéticos, entre los que sólo dos han demostrado superioridad en protección cardiovascular. Son liraglutida y empagliflozina, que pertenecen, respectivamente, a los grupos GLP-1 RA y SGLT-2Í. Estos medicamentos también han demostrado beneficios en nefroprotección. Sin embargo, en una reciente encuesta del autor entre nefrólogos, en una gran ciudad colombiana, se ha detectado que la mayoría no utilizan estos fármacos. La mayor resistencia a su uso se debe a consideraciones sobre su restricción en etapas avanzadas de la enfermedad renal crónica, pero también al desconocimiento de sus beneficios potenciales. Al respecto, los nefrólogos aceptaron que deberían aprender más acerca de estos medicamentos antidiabéticos, porque el tipo de paciente que frecuentemente asiste a su consulta sin duda se beneficiaría, y más teniendo en cuenta que por el gran número de diabéticos los nefrólogos están obligados a manejar directamente al paciente con esta patología.

Humans , Cardiovascular Agents , Nephrologists , Hypoglycemic Agents , Cardiotonic Agents , Colombia , Diabetes Mellitus, Type 2 , Liraglutide
Article in English | WPRIM | ID: wpr-43211


Non-alcoholic steatohepatitis (NASH) is the more aggressive form of non-alcoholic fatty liver disease (NAFLD). NASH can progress to hepatic fibrosis, cirrhosis, portal hypertension and primary liver cancer. Therapy is evolving with a substantial number of trials of promising new agents now in progress. In this article however, we will examine data for several older forms of therapy which have been fairly extensively studied over the years: Polyunsaturated Fatty Acid (PUFA) supplements, vitamin E, insulin sensitizing agents with a focus on pioglitazone and statin agents. Early interest in PUFA derived from their potential benefit in cardio-metabolic disease and the close association of NAFLD/NASH with Metabolic Syndrome. Results have been variable although most studies show reduction of liver fat without other major effects and their effects are influenced by concomitant weight loss and underlying genetic factors. Vitamin E has had some efficacy in pediatric NASH but questionable efficacy in even mild NASH among adults. Pioglitazone has shown significant histological benefit in a number of trials but concern over side-effects (especially weight gain) have dampened enthusiasm. A newer insulin sensitizer, liraglutide, has also shown promise in a small randomized, controlled trial. Very limited data exists regarding the histological effects of the statins in NASH and these agents appear to be fairly neutral with neither clear cut benefit nor detriment. Their use is best guided by cardiovascular risks rather than liver histology.

Adult , Fatty Liver , Fibrosis , Humans , Hydroxymethylglutaryl-CoA Reductase Inhibitors , Hypertension, Portal , Insulin , Liraglutide , Liver , Liver Neoplasms , Non-alcoholic Fatty Liver Disease , Vitamin E , Vitamins , Weight Loss
Lima; s.n; nov. 2016.
Non-conventional in Spanish | LILACS, BRISA | ID: biblio-848202


INTRODUCCIÓN: Antecedentes: El presente dictamen expone la evaluación de tecnología de la eficacia y seguridad de Liraglutida en pacientes con diabetes melitus tipo 2 y sobrepeso, sin control metabólico adecuado (según HbA1c) a pesar de tratamiento bolo-basal con dosis altas de Insulina. Aspectos Generales: La diabetes melittus tipo 2 (conocida previamente como diabetes no insulino-dependiente o diabetes de inicio en el adulto) aparece por el uso inefectivo de la insulina por el organismo. Este tipo de diabetes incluyer a la mayoria de casos de diabetes en el mundo, y por contar con sintomas poco marcados o ausentes, puede no ser diagnosticada por varios años hasta la aparición de sus complicaciones. Tecnología Sanitaria de Interés: Los agonistas de receptores GLP-1 (Péptido similiar a1 glucagón tipo 1, por sus siglas en inglés) son un tipo de medicamentos antidiabéticos inyectables que pueden mejorar el control glicémico e inducir la disminución de peso. Estos medicamentos funcionan promoviendo la secreción de insulina dependiente de glucosa e inhibiendo la liberación promoviendo la secreción de insulina dependiente de glucosa e inhibiendo la liberación de glucagón. METODOLOGÍA: Estrategia de Búsqueda: Se realizó una estrategia de búsqueda sistemática de la evidencia científica con respecto a la eficacia y seguridad de liraglutida en pacientes con diabetes mellitus tipo 2 y sobrepeso, sin control metabólico adecuado (según HbA1c) a pesar de tratamiento bolo-basal con dosis altas de insulina. Se dio preferencia a estudios de tipo meta-análisis, revisiones sistemáticas y ensayos clínicos aleatorizados; así como a guías de práctica clínica de grupos o instituciones relevantes al tema analizado. RESULTADOS: Sinopsis de la Evidencia: Se realizó la búsqueda y revisión de la evidencia científica actual para la evaluación de la eficacia y seguridad de Liraglutida en pacientes con diabetes mellitus tipo 2 y sobrepeso, sin control metabólico adecuado a pesar de tratamiento bolo-basal con dosis altas de Insulina. Se presenta la información encontrada de acuerdo al tipo de evidencia revisada. CONCLUSIONES: La población de interés de la presente evaluación de tecnología sanitaria comprende los pacientes con diabetes mellitus tipo 2 y sobrepeso, sin control metabólico adecuado (según HbA1c) a pesar de tratamiento bolo-basal con dosis altas de Insulina. LOs ensayos clínicos revisados presentan un cambio significativo en los valores de HbA1c en pacientes que recibieron la intervención evaluada en comparación a los valores basales y al uso de insulina sola. Asimismo, se observa un resultado similar para el peso y dosis total de insulina diaria de los participantes. La frecuencia de efectos adversos severos asociados al uso de Liraglutida en combinación con Insulina bolo-basal es baja y el medicamento es bien tolerado. Las características de los GLP-1-RA los hacen útiles en casos en los que los pacientes reciben dosis altas de insulina y sus consecuentes efectos adversos. Se requiere la ejecución de estudios de costo-efectividad de uso de Liraglutida en combinación con insulina bolo-basal comparando dicho tratamiento con la Insulina bolo-basal sola para evaluar el impacto real de ambas terapias sobre los pacientes de interés. El Instituto de Evaluación de Tecnologías Sanitarias-IETSI, aprueba el uso de Liraglutida en apcientes con diabetes mellitus tipo 2 y sobrepeso, sin control metabólico adecuado a pesar de tratamiento bolo-basal con dosis altas de Insulina. El período de vigencia de este dictamen es de dos años y la continuación de dicha aprobación estará sujeta a los resultados obtenidos de los pacientes que se beneficien con dicho tratamiento y a nueva evidencia que pueda surgir en el tiempo.

Humans , Diabetes Mellitus, Type 2/drug therapy , Diabetes Mellitus, Type 2/metabolism , Insulins/administration & dosage , Liraglutide/administration & dosage , Overweight , Technology Assessment, Biomedical , Treatment Outcome
National Journal of Andrology ; (12): 212-218, 2016.
Article in Chinese | WPRIM | ID: wpr-304726


<p><b>UNLABELLED</b>OCTOBER: To explore the effects of the glucagon-like peptide 1 (GLP-1) liraglutide on the penile erectile function of rats with diabetic erectile dysfunction (DED) by observing the impact of liraglutide on the expression of eNOS in the corpus cavernosum of diabetic rats.</p><p><b>METHODS</b>We randomly divided 30 six-week-old male SD rats into a normal control (n = 10) and an experimental group (n = 20) , established models of diabetes mellitus (DM) in the experimental rats, and subdivided them into a DM (n = 8) and a GLP-1 group (n = 8) to receive intramuscular injection of normal saline and liraglutide at 5 mg per kg of the body weight per day, respectively. After 12 weeks of intervention, we obtained the levels of FPG, FINS, TG, TC, HDL-C, LDL-C, testosterone, and IL-6 and the indexes of Homa-IR and Homa-β, detected the expressions of Akt/p-Akt and eNOS/p-eNOS in the corpus cavernosum by Western blot, and compared the erectile function between different groups.</p><p><b>RESULTS</b>The frequency and rate of penile erection were significantly lower in the DM group than in the GLP-1 and normal control groups (P < 0.05) and also lower in the GLP-1 group than in the normal controls (P < 0.05). Immunofluorescence staining showed the expression of eNOS mainly in the cytoplasm of the cavernosal vessels and sinusoidal endothelial cells, markedly lower in the DM and GLP-1 groups than in the normal rats (P < 0.05), but higher in the GLP-1 than in the DM group (P < 0.05). The level of eNOS/p-eNOS in the penile tissue was significantly decreased in the DM and GLP-1 groups in comparison with the normal controls (P < 0.01 or P < 0.05), while that of p-eNOS was markedly increased in the GLP-1 group as compared with the DM group (P < 0.05). No statistically significant differences were observed in the Akt level among the three groups of animals (P > 0.05). The expression of p-Akt was remarkably reduced in the DM and GLP-1 groups in comparison with the control rats (P < 0.01 or P < 0.05), but higher in the GLP-1 than in the DM group (P < 0.05).</p><p><b>CONCLUSION</b>GLP-1 can protect the function of endothelial cells in the corpus cavernosum and improve the erectile function of DED rats by regulating the Akt/ eNOS signaling pathway, which indicates that GLP-1 could be an important option for the treatment and prevention of DED.</p>

Animals , Blotting, Western , Diabetes Mellitus, Experimental , Erectile Dysfunction , Drug Therapy , Hypoglycemic Agents , Pharmacology , Liraglutide , Pharmacology , Male , Nitric Oxide Synthase Type III , Metabolism , Penile Erection , Penis , Random Allocation , Rats , Rats, Sprague-Dawley , Testosterone , Blood
Gastroenterol. latinoam ; 27(supl.1): S55-S59, 2016. ilus, tab, graf
Article in Spanish | LILACS | ID: biblio-907655


Non-alcoholic fatty liver disease (NAFLD) represents an increasing health problem in Chile and worldwide. In some cases NAFLD presents with a progressive form that can lead to liver fibrosis, cirrhosis and hepatocellular carcinoma. Current pharmacological therapies (pioglitazone and vitamin E) show limited response and are associated to significant adverse effects. During recent years several novel and promising pharmacological therapies have been developed to prevent fibrosis, liver cirrhosis and reduce liver related deaths. The present article summarizes some of these promising strategies, including reported efficacy in clinical trials and associated adverse effects. Hopefully in the near future these new therapies will help to improve NAFLD management and reduce liver related complications.

El hígado graso no alcohólico (HGNA) es un creciente problema de salud pública en Chile y el mundo. En un subgrupo de sujetos, el HGNA puede presentarse con un fenotipo de daño hepático progresivo que puede evolucionar a fibrosis progresiva, cirrosis y carcinoma hepatocelular. Las estrategias farmacológicas actuales (pioglitazona y vitamina E) presentan eficacia limitada y no están exentas de efectos adversos. Durante los últimos años se han desarrollado múltiples estrategias farmacológicas novedosas y promisorias que buscan evitar la progresión hacia cirrosis y reducir la mortalidad de causa hepática. El presente artículo resume los principales nuevos fármacos, los efectos beneficiosos reportados y sus efectos adversos. Es de esperar que en un futuro próximo estas terapias permitan cambiar el pronóstico de nuestros pacientes con HGNA.

Humans , Chenodeoxycholic Acid/analogs & derivatives , Chenodeoxycholic Acid/therapeutic use , Liraglutide/therapeutic use , Non-alcoholic Fatty Liver Disease/drug therapy , Propionates/therapeutic use , Chalcones/therapeutic use , Liver Cirrhosis/prevention & control