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1.
Actual. nutr ; 24(2): 109-119, abr 2023. tab
Article in Spanish | LILACS, UNISALUD, BINACIS | ID: biblio-1511204

ABSTRACT

Introducción: La insatisfacción corporal se asocia a la morbilidad psicofísica. Uno de los factores estudiados como disparador de malestar sobre la imagen corporal es la exposición a mensajes culturales de ideales físicos o de belleza. El presente trabajo explora la relación entre el uso de las redes sociales y la preocupación por el propio cuerpo, el deseo de hacer dieta para bajar de peso, y la generación de pensamientos obsesivos por la forma y tamaño corporal durante el período de Aislamiento Social, Preventivo y Obligatorio (ASPO). Materiales y Métodos: Estudio transversal, descriptivo, realizado a través de un cuestionario online en participantes mayores de 18 años residentes en Argentina. Se evaluaron antecedentes demográficos, datos antropométricos, conformidad con la imagen corporal e influencia del uso de redes sociales sobre la imagen corporal y la conformidad con el propio cuerpo. Resultados: Un total de 2236 individuos (85,5% mujeres), con una media de edad de 38.88±15.20 años, y una media de IMC de 25.55±5.36 kg/m2, aceptó participar del presente estudio. El 34% de los encuestados manifestaron que nunca o rara vez se encontraban conformes con su cuerpo y el 66% refirió sentir culpa al excederse con la comida. El 68,1% manifestó haber sentido miedo a aumentar de peso en algún momento de su vida. El análisis multivariado arrojó una relación inversa entre la edad de los encuestados y la percepción de que las redes sociales influyeron negativamente sobre su imagen corporal, y que estas incrementaron su deseo de hacer una dieta destinada a bajar de peso. El efecto negativo de las redes sociales fue significativamente mayor en aquellos que presentaban disconformidad corporal previo al ASPO. Conclusión: El incremento del uso de las redes sociales en pandemia se vio reflejado en el grado de insatisfacción corporal en el grupo de mayor vulnerabilidad en la muestra estudiada


Introduction: Body image dissatisfaction is associated with psychophysical morbidity. Exposure to cultural messages about physical or beauty ideals is one of the studied factors which initiate body image dissatisfaction. This work explores the relationship between social media use and preoccupation with one's own body, the desire for a diet to lose weight, and the generation of obsessive thoughts about body shape and size during the period of Social Preventive and Mandatory Isolation (SPMI). Materials and methods: A cross-sectional study was carried out using an online questionnaire of participants over 18 years residing in Argentina. Demographic information, anthropometric data, conformity with body image and the influence of the use of social media on body image and conformity with one's own body were evaluated. Results: 2236 individuals participated in this study (85,5% women) with a mean age of 38.88±15.20 years and a mean IMC of 25.55±5.36 kg/m2. Thirty-four percent of the sample expressed that they never or hardly ever were satisfied with their bodies and 66% referred to a feeling of fault when they overindulge in food. Sixty-eight percent stated that they had been afraid of gaining weight at some moment in their life. The multivariate analysis showed an inverse relationship between age and perception of social media's negative influence on their body image, and that they increased their desire to diet to lose weight.The negative social media effect was significantly higher in participants who presented body dissatisfaction previous to the SPMI.Conclusion: The increase in social media use during the pandemic was reflected in the level of body dissatisfaction in the most vulnerable group of this sample


Subject(s)
Body Image , Body Dissatisfaction , Pandemics , Social Networking
2.
Front Public Health ; 10: 813378, 2022.
Article in English | MEDLINE | ID: mdl-35273939

ABSTRACT

Background: In the absence of antiviral alternatives, interventions under research for COVID-19 might be offered following guidelines from WHO for monitored emergency use of unregistered and experimental interventions (MEURI). Ivermectin is among several drugs explored for its role against SARS-CoV-2, with a well-known safety profile but conflicting data regarding clinical utility for COVID-19. The aim of this report is to inform on the results of a MEURI Program of high-dose ivermectin in COVID-19 carried out by the Ministry of Health of the Province of La Pampa, Argentina. Methods: COVID-19 subjects, within 5 days of symptoms onset were invited to participate in the program, which consisted in the administration of ivermectin 0.6 mg/kg/day for 5 days plus standard of care. Active pharmacosurveillance was performed for 21 days, and hepatic laboratory assessments were performed in a subset of patients. Frequency of Intensive Care Unit (ICU) admission and COVID-19-related mortality of subjects in the ivermectin intention to treat group were compared with that observed in inhabitants of the same province during the same period not participating in the program. Results: From 21,232 subjects with COVID-19, 3,266 were offered and agreed to participate in the ivermectin program and 17,966 did not and were considered as controls. A total of 567 participants reported 819 adverse events (AEs); 3.13% discontinued ivermectin due to adverse events. ICU admission was significantly lower in the ivermectin group compared to controls among participants ≥40 year-old (1.2 vs. 2.0%, odds ratio 0.608; p = 0.024). Similarly, mortality was lower in the ivermectin group in the full group analysis (1.5 vs. 2.1%, odds ratio 0.720; p = 0.029), as well as in subjects ≥ 40 year- old (2.7 vs. 4.1%, odds ratio 0.655; p = 0.005). Conclusions: This report highlights the safety and possible efficacy of high dose ivermectin as a potentially useful intervention deserving public health-based consideration for COVID-19 patients.


Subject(s)
COVID-19 Drug Treatment , Ivermectin , Adult , Humans , Ivermectin/therapeutic use , SARS-CoV-2
3.
Actual. nutr ; 22(1): 9-15, ene. 2021.
Article in Spanish | LILACS | ID: biblio-1416643

ABSTRACT

Introducción: las situaciones con alta carga emotiva pueden favorecer la ganancia de peso. Objetivos: evaluar la asociación entre el fenotipo de comportamiento alimentario y la percepción de emociones y sentimientos con la ganancia de peso en el contexto de la pandemia por COVID-19. Materiales y métodos: estudio transversal, descriptivo, realizado a través de un cuestionario online en adultos residentes en Argentina. Se evaluaron antecedentes demográficos, datos antropométricos, nivel de actividad física, hábitos de sueño y fenotipo de comportamiento alimentario. Se indagó respecto del incremento en la percepción de diferentes emociones y sentimientos durante el período de confinamiento obligatorio. Resultados: se seleccionaron 2.619 participantes (84,9% mujeres, media de edad de 39,27±15,21 años). El 40,3% de los encuestados manifestó haber aumentado de peso durante el confinamiento. El 77,3% de los sujetos presentó algún tipo de alteración en el sueño. Los principales sentimientos y emociones que se expresaron e incrementaron fueron ansiedad (50,7% de los participantes), desmotivación (45,1%) y tristeza (38,9%). La disminución de la actividad física durante el confinamiento obligatorio y el índice de masa corporal al inicio del mismo se asociaron a ganancia de peso (p=0,066). El fenotipo de comportamiento alimentario comedor hedónico predijo la ganancia de peso (B=0,408). El incremento en la percepción de aburrimiento (B=0,255), desmotivación (B=0,244) y ansiedad (B=0,409) durante el confinamiento también se asoció a ganancia de peso durante este período, mientras que quienes manifestaron incremento en la percepción de fortaleza presentaron un menor riesgo (B=-0,536).Conclusiones: el fenotipo de comportamiento alimentario comedor hedónico y la percepción de emociones negativas se asociaron a ganancia de peso en el contexto de confinamiento obligatorio. Esto resalta la importancia del abordaje de los aspectos emocionales y la identificación de los fenotipos comportamentales de ingesta individual a fin de promover estrategias de prevención adecuadas


Introduction: situations characterized by a high emotional load might favor weight gain. Objectives: the aim of the present study was to evaluate the association between eating behavior phenotype, emotions and feelings perception and weight gaining in the context of COVID-19 pandemia. Materials and methods: a transversal, descriptive study was carried out by means of an online survey on adults participants, residents in Argentina. The evaluation consisted of demographic and anthropometric data, physical activity level, sleep habits and eating behavior phenotype. The increase in the perception of different emotions and feeling during the confinement was evaluated. Results: 2,619 participants (84.9 females, mean age 39.27±15.21 year old). 40.3% of the subjects reported having gained weight during the confinement. 77.3% of the subjects showed some sort of sleep disturbance. The main feelings and emotions that were reported to have increased were anxiety (50.7%), demotivation (45.1%) and sadness (38.9%). Logistic regression model evidenced that the diminishment in physical activity during the confinement, as well as basal body mass index were associated to weight gain. The hedonic eater eating behavior phenotype predicted weight gain (B=0,408).The increase in the perception of boring (B=0,255), demotivation (B=0,244) and anxiety (B=0,409) during the confinement was also associated to weigh gain during this period, meanwhile those who experienced an increase in the feeling of strength presented a lower risk (B=-0,536). Conclusions: the hedonic eater eating behavior phenotype and the perception of negative emotions were associated to weight gaining in the context of the confinement. This remarks the importance of the addressing emotional aspects and identifying individual eating behavior phenotypes in order to promote adequate preventive strategies


Subject(s)
Humans , Adult , Feeding Behavior , Obesity
4.
Endocrinol. nutr. (Ed. impr.) ; 59(5): 326-330, mayo 2012. tab
Article in Spanish | IBECS | ID: ibc-105165

ABSTRACT

Introducción El yodo es un micronutriente esencial en la alimentación de la embarazada que transfiere al embrión-feto a través del transporte placentario. Existen antecedentes de su importancia para el desarrollo neurológico, pero no ha sido estudiada la relación entre ingesta de yodo y peso placentario ni su repercusión en el neonato (RN).Materiales y métodos Se analizó ingesta de yodo en 77 embarazadas, mediante eliminación urinaria de yodo (EUI) con la técnica modificada por Pino (normal ≥150μg/l). Se midió el peso placentario (PP: normal ≥500g). En el recién nacido se evaluó peso, talla y perímetro cefálico (PC). Se obtuvo el índice placentario (IP: peso placentario/ peso recién nacido) considerando normal ≥0,15.ResultadosLa EUI fue normal en 50 embarazadas (media±DE, 279μg/l±70,22μg/l) y disminuida en 27 (94μg/l ±31,49μg/l). Los RN de madres con EUI baja tenían un peso (3.357g±416,30g; n: 27) no diferente a las madres con yodurias normales (3.489g±560,59g; n: 50). Pero las madres con EUI bajo tenían un 44% de placentas con PP<500g y el análisis de los PC en los RN con bajo PP mostró que eran estadísticamente menores (PP3500g: 36,05cm±0,55cm, n: 54; PP<500g: 33,93cm±15cm, n: 23, p<0,019). El estudio con los IP fue similar aunque no alcanzó la significación estadística 0,17±0,04 (p: 0,066). Los demás parámetros no mostraron diferencias significativas. Conclusión El estudio evidencia una relación entre el PP y PC. Este hallazgo puede ser relacionado con la ingesta de yodo durante el embarazo (AU)


Introduction Iodine is considered to be an essential micronutrient in pregnant women. Iodine placental transport to the embryo-fetus is essential for hormone synthesis and is crucial for nervous system development. However, the relationship between iodine intake and placental weight and its potential implications for the newborn have not been studied. Material and methods Iodine intake was analyzed in 77 pregnant women based on urinary iodine excretion (UIE) levels, measured using Pino's modified method (normal value, ≥150μg/L). Placental weight was measured (PW: normal, ≥500g). In the newborn, weight, height, and head perimeter (HP) were also measured. Placental index (PI: placental weight/newborn weight) was calculated, and was considered normal if ≥0.15.ResultsUIE was normal in 50 pregnant women (mean±SD, 279±70.22μg/L) and decreased in 27 (94±31.49μg/L). Newborns of mothers with low UIE had a similar weight (3357±416.30g; n: 27) to those of mothers with normal UIE (3489±560.59g; n: 50). Forty-four percent of mothers with low UIE had PW <500g, and statistically lower HPs were found in newborns of mothers with low PW (PW3 500g: 36.05±0.55cm, n: 54; PW<500g: 33.93±15cm, n: 23, p<0.019). Similar results were found with PI, but they did not reach statistical significance (0.17±0.04; p=0.066). No differences were seen in all other parameters. Conclusion The study suggests the existence of a relationship between PW and HP. This finding may be related to iodine intake during pregnancy (AU)


Subject(s)
Humans , Female , Pregnancy , Adolescent , Young Adult , Adult , Iodine/deficiency , Maternal Nutrition , Placenta/abnormalities , Cephalometry , Iodine/urine , Nutrition Disorders/epidemiology , Fetal Nutrition Disorders/epidemiology
5.
Endocrinol Nutr ; 59(5): 326-30, 2012 May.
Article in English | MEDLINE | ID: mdl-22381147

ABSTRACT

INTRODUCTION: Iodine is considered to be an essential micronutrient in pregnant women. Iodine placental transport to the embryo-fetus is essential for hormone synthesis and is crucial for nervous system development. However, the relationship between iodine intake and placental weight and its potential implications for the newborn have not been studied. MATERIAL AND METHODS: Iodine intake was analyzed in 77 pregnant women based on urinary iodine excretion (UIE) levels, measured using Pinós modified method (normal value, ≥ 150 µg/L). Placental weight was measured (PW: normal, ≥500 g). In the newborn, weight, height, and head perimeter (HP) were also measured. Placental index (PI: placental weight/newborn weight) was calculated, and was considered normal if ≥0.15. RESULTS: UIE was normal in 50 pregnant women (mean ± SD, 279 µg/L ± 70.22 µg/L) and decreased in 27 (94 µg/L ± 31.49 µg/L). Newborns of mothers with low UIE had a similar weight (3357 g ± 416.30 g; n: 27) to those of mothers with normal UIE (3489 g ± 560.59 g; n: 50). Forty-four percent of mothers with low UIE had PW <500 g, and statistically lower HPs were found in newborns of mothers with low PW (PW(3)500 g: 36.05 cm ± 0.55 cm, n: 54; PW <500 g: 33.93 cm ± 15 cm, n:23, p<0.019). Similar results were found with PI, but they did not reach statistical significance (0,17 ± 0,04; p=0.066). No differences were seen in all other parameters. CONCLUSION: The study suggests the existence of a relationship between PW and HP. This finding may be related to iodine intake during pregnancy.


Subject(s)
Head/embryology , Infant, Newborn , Iodine/deficiency , Placenta/pathology , Placentation , Pregnancy Complications/physiopathology , Adolescent , Adult , Argentina , Birth Weight , Body Height , Cephalometry , Diet , Embryonic Development , Female , Head/anatomy & histology , Humans , Iodine/pharmacokinetics , Iodine/urine , Maternal-Fetal Exchange , Nutritional Requirements , Organ Size , Pregnancy , Pregnancy Complications/urine , Young Adult
6.
Xenobiotica ; 42(2): 206-19, 2012 Feb.
Article in English | MEDLINE | ID: mdl-21892881

ABSTRACT

Cardiovascular effects and pharmacokinetics of carvedilol were assessed in fructose-fed rats using pharmacokinetic-pharmacodynamic (PK-PD) modeling. Male Sprague-Dowley rats were randomly assigned to receive tap water (C rats) or fructose solution (10% w/v) (F rats) during 6 weeks. Effects of carvedilol (1-3 mg/kg i.v.) on blood pressure, heart rate and blood pressure variability were recorded. Carvedilol plasma pharmacokinetics was studied by traditional blood sampling. Relationship between carvedilol concentrations and their hypotensive and bradycardic effects was established by PK-PD modeling. Vascular sympatholytic activity of carvedilol was assessed by estimation of drug effects on low frequency blood pressure variability using spectral analysis. A greater volume of distribution and clearance of S-carvedilol compared to R-enantiomer was found in both experimental groups. Although PK-PD properties of S-carvedilol chronotropic effect were not altered in F rats, hypertensive rats showed greater efficacy to the carvedilol hypotensive response after administration of the higher dose. A similar potency of carvedilol to inhibit sympathetic vascular activity was found in F rats. Carvedilol showed enantioselective pharmacokinetic properties with increased distribution in F rats compared with normotensive animals. An enhanced hypotensive activity of carvedilol was found in F rats compared with C rats, which is not related to enhance sympatholytic activity.


Subject(s)
Antihypertensive Agents/pharmacokinetics , Carbazoles/pharmacokinetics , Hypertension/drug therapy , Propanolamines/pharmacokinetics , Animals , Antihypertensive Agents/chemistry , Antihypertensive Agents/pharmacology , Blood Pressure/drug effects , Carbazoles/chemistry , Carbazoles/pharmacology , Carvedilol , Fructose , Heart Rate/drug effects , Hypertension/metabolism , Male , Propanolamines/chemistry , Propanolamines/pharmacology , Rats , Rats, Sprague-Dawley
7.
J Pharm Pharmacol ; 62(7): 890-900, 2010 Jul.
Article in English | MEDLINE | ID: mdl-20636877

ABSTRACT

OBJECTIVES: The role of vascular sympatholytic activity of carvedilol in its antihypertensive effect in N(G)-nitro-l-arginine methyl ester (L-NAME) hypertensive rats was assessed by means of enantioselective pharmacokinetic-pharmacodynamic (PK-PD) modelling. METHODS: Male Wistar rats were randomly divided into two groups: control rats received tap water to drink for 2 weeks while L-NAME rats received L-NAME solution to drink for 2 weeks. The effects of carvedilol (1 and 5 mg/kg i.v.) on blood pressure, heart rate and blood pressure variability were recorded. Enantioselective carvedilol plasma pharmacokinetics were studied by means of traditional blood sampling. The relationship between carvedilol concentrations and their hypotensive and bradycardic effects was established by means of PK-PD modelling. Vascular sympatholytic activity of carvedilol was assessed by the estimation of drug effects on low frequency blood pressure variability by means of spectral analysis. KEY FINDINGS: A dose-dependent increase in volume of distribution, as well as a greater volume of distribution and clearance of S-carvedilol as compared with the R-enantiomer was found in both experimental groups. Although the PK-PD properties of the S-carvedilol chronotropic effect were not altered in L-NAME rats, hypertensive rats showed greater potency and efficacy to the carvedilol hypotensive response. Greater potency of carvedilol for inhibition of sympathetic vascular activity was found in L-NAME rats. CONCLUSIONS: Carvedilol showed enantioselective non-linear pharmacokinetic properties in both groups. An enhanced hypotensive activity of carvedilol was found in L-NAME hypertensive rats compared with control rats, which may be explained by the greater potency of carvedilol for sympathetic vascular tone inhibition.


Subject(s)
Antihypertensive Agents/pharmacology , Carbazoles/pharmacology , Hypertension/drug therapy , Propanolamines/pharmacology , Sympatholytics/pharmacology , Animals , Antihypertensive Agents/pharmacokinetics , Antihypertensive Agents/therapeutic use , Blood Pressure/drug effects , Carbazoles/pharmacokinetics , Carbazoles/therapeutic use , Carvedilol , Disease Models, Animal , Dose-Response Relationship, Drug , Hypertension/chemically induced , Inactivation, Metabolic , Male , Models, Biological , NG-Nitroarginine Methyl Ester , Propanolamines/pharmacokinetics , Propanolamines/therapeutic use , Random Allocation , Rats , Rats, Wistar , Stereoisomerism , Sympatholytics/pharmacokinetics , Sympatholytics/therapeutic use
8.
Expert Opin Drug Metab Toxicol ; 6(2): 199-211, 2010 Feb.
Article in English | MEDLINE | ID: mdl-20095790

ABSTRACT

Several first-line antihypertensive drugs, including calcium channel blockers, beta-adrenergic blockers and angiotensin receptor blockers, undergo metabolism through different CYP isoforms. As a consequence of CYP-dependent metabolism, wide interindividual variability of plasma concentrations of antihypertensive drugs has been found in clinical practice compromising blood pressure lowering response and clinical outcomes. Several factors, including aging, hepatic impairment, drug interactions, conditions affecting hepatic blood supply and polymorphisms, contribute to changes in oral and systemic clearance affecting drug exposure during antihypertensive therapy and cardiovascular response. Considering that the degree of blood pressure reduction is related to antihypertensive drug plasma concentrations, a greater knowledge of the sources of pharmacokinetic variability of hepatically eliminated antihypertensive drugs and the applicability of an individualized approach in hypertension management by means of pharmacokinetic/pharmacodynamic modeling and pharmacogenetic testing could enhance blood pressure lowering response to pharmacological therapy. The aim of the present review is to discuss the relevance of drug metabolism in the treatment of hypertension.


Subject(s)
Adrenergic beta-Antagonists/metabolism , Angiotensin II Type 1 Receptor Blockers/metabolism , Antihypertensive Agents/metabolism , Calcium Channel Blockers/metabolism , Adrenergic beta-Antagonists/pharmacology , Aging/metabolism , Angiotensin II Type 1 Receptor Blockers/pharmacology , Angiotensin II Type 1 Receptor Blockers/therapeutic use , Antihypertensive Agents/pharmacology , Antihypertensive Agents/therapeutic use , Calcium Channel Blockers/pharmacology , Calcium Channel Blockers/therapeutic use , Dose-Response Relationship, Drug , Drug Interactions , Humans , Hypertension/drug therapy , Hypertension/metabolism , Pharmacogenetics , Polymorphism, Genetic
9.
J Pharmacol Toxicol Methods ; 59(1): 13-20, 2009.
Article in English | MEDLINE | ID: mdl-18973819

ABSTRACT

INTRODUCTION: The aim of the work was to establish the impact of urethane-chloralose anaesthesia on pharmacokinetic-pharmacodynamic (PK-PD) properties of carvedilol in control rats and L-NAME hypertensive animals. METHODS: Male Wistar Rats were randomly divided into: control (n=12) with tap water to drink and L-NAME rats (n=12) with L-NAME solution (40 mg/kg/day) to drink for 2 weeks. Effects of carvedilol (1 mg kg(-1), i.v.) on blood pressure and heart rate were recorded during 3 h in conscious and urethane (500 mg kg(-1), i.p.) - chloralose (50 mg kg(-1), i.p.) anaesthetized rats. Carvedilol plasma pharmacokinetics was studied by means of traditional blood sampling. PK-PD modeling of carvedilol was made by means of an effect compartment model. RESULTS: Neither urethane-chloralose nor L-NAME modified estimation of pharmacokinetic parameters of carvedilol. Although urethane-chloralose did not modify potency of carvedilol comparing with awake animals in control and hypertensive group, maximal negative chronotropic response was significantly greater in anaesthetized L-NAME rats in comparison to awake animals. Conversely, anaesthesia did not modify maximal chronotropic response to carvedilol in control rats. Whilst no differences were found in the estimated potency of carvedilol hypotensive response comparing control and L-NAME rats in both awake and anaesthetized conditions, maximal hypotensive effect of carvedilol was significantly greater in anaesthetized control and L-NAME animals in comparison to conscious rats. L-NAME rats showed a greater maximal hypotensive response comparing to control group. DISCUSSION: Urethane-chloralose anaesthesia is an acceptable experimental condition for the evaluation of PK-PD properties of carvedilol, considering that it does not affect the potency of carvedilol for its chronotropic and hypotensive effect. Conclusions obtained from urethane-chloralose anaesthetized animals, regarding the impact of l-NAME treatment on PK-PD properties of carvedilol, did not differ from those obtained from conscious animals. Anaesthesia did not modify pharmacokinetic behaviour of carvedilol in both normotensive and L-NAME hypertensive rats.


Subject(s)
Adrenergic beta-Antagonists/pharmacokinetics , Anesthesia , Carbazoles/pharmacokinetics , Chloralose/pharmacokinetics , Propanolamines/pharmacokinetics , Urethane/pharmacokinetics , Administration, Oral , Adrenergic beta-Antagonists/administration & dosage , Adrenergic beta-Antagonists/blood , Algorithms , Animals , Area Under Curve , Blood Pressure/drug effects , Carbazoles/administration & dosage , Carbazoles/blood , Carvedilol , Chloralose/administration & dosage , Data Interpretation, Statistical , Disease Models, Animal , Drug Administration Schedule , Drug Synergism , Half-Life , Heart Rate/drug effects , Hypertension/chemically induced , Injections, Intraperitoneal , Injections, Intravenous , Male , Models, Biological , NG-Nitroarginine Methyl Ester/adverse effects , NG-Nitroarginine Methyl Ester/chemistry , Propanolamines/administration & dosage , Propanolamines/blood , Rats , Rats, Wistar , Solutions/chemistry , Urethane/administration & dosage
10.
J Cardiovasc Pharmacol ; 51(6): 532-41, 2008 Jun.
Article in English | MEDLINE | ID: mdl-18475202

ABSTRACT

BACKGROUND: This study of metoprolol pharmacokinetic and pharmacodynamic properties investigates cardiac beta1-adrenoceptors activity and its involvement in the hypertensive stage in 6-week-old fructose-fed male Sprague-Dawley rats. METHODS: A microdialysis probe was inserted in the carotid artery to monitor metoprolol levels, blood pressure, and heart rate after drug administration (3-10 mg/kg intravenously). The relationship between levels and cardiovascular effects was studied using a pharmacokinetic-pharmacodynamic model with effect compartment. Dissociation constant and inverse agonism were evaluated in isolated atria. RESULTS: Metoprolol pharmacokinetics were similar in both groups. Metoprolol induced a greater hypotensive effect in fructose-fed animals (Emax: -24 +/- 1 mm Hg, n = 6, P < 0.05 vs. control) than in control rats (Emax: -14 +/- 1 mm Hg, n = 6). Bradycardic response was similar in both groups; metoprolol chronotropic potency was greater in fructose-fed rats (IC50: 123 +/- 15 ng/mL, P < 0.05 vs. control) compared to control animals (IC50: 216 +/- 36 ng/mL) after administration of 3 mg/kg. Metoprolol constants of dissociation for beta1-adrenoceptors and inverse agonism were similar in both groups. CONCLUSION: Results demonstrate the beta1-adrenoceptors involvement in the fructose hypertension. A greater potency to metoprolol in vivo chronotropic effect was found in fructose-fed rats. This greater potency was not caused by alteration in the activity of beta1-adrenoceptors.


Subject(s)
Adrenergic beta-1 Receptor Antagonists , Antihypertensive Agents/pharmacology , Fructose/administration & dosage , Hypertension/drug therapy , Metoprolol/pharmacology , Animals , Antihypertensive Agents/pharmacokinetics , Area Under Curve , Disease Models, Animal , Dose-Response Relationship, Drug , Half-Life , Hypertension/metabolism , Hypertension/physiopathology , Male , Metoprolol/pharmacokinetics , Rats , Rats, Sprague-Dawley , Receptors, Adrenergic, beta-1/physiology
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