The potential role of amlodipine on experimentally induced bacterial rhinosinusitis / O papel potencial da amlodipina na rinossinusite bacteriana induzida experimentalmente

Abstract Introduction: Antibiotics are frequently used for the treatment of rhinosinusitis. Concerns have been raised regarding the adverse effects of antibiotics and growing resistance. The lack of development of new antibiotic compounds has increased the necessity for exploration of non-antibiotic compounds that have antibacterial activity. Amlodipine is a non-antibiotic compound with anti-inflammatory activity. Objective: In this study we aimed to investigate the potential role of amlodipine in the treatment of rhinosinusitis by evaluating its effects on tissue oxidative status, mucosal histology and inflammation. Methods: Fifteen adult albino guinea pigs were inoculated with Staphylococcus aureus and treated with saline, cefazolin sodium, or amlodipine for 7 days. The control group was composed by five healthy guinea pigs. Animals were sacrificed after the treatment. Histopathological changes were identified using Hematoxylin-Eosin staining. Inflammation was assessed by Polymorphonuclear Leukocyte infiltration density. Tissue levels of antioxidants (superoxide dismutase, glutathione) and an oxidative product (malondialdehyde) were determined. Results: In rhinosinusitis induced animals, amlodipine reduced loss of cilia, lamina propria edema and collagen deposition compared to placebo (saline) and although not superior to cefazolin, amlodipine decreased polymorphonuclear leukocyte infiltration. The superoxide dismutase activity and glutathione levels were reduced, whereas the malondialdehyde levels were increased significantly in all three-treatment groups compared to the control group. Amlodipine treated group showed significantly increased superoxide dismutase and glutathione levels and decreased malondialdehyde levels compared to all treatment groups. Conclusion: The non-antibiotic compound amlodipine may have a role in acute rhinosinusitis treatment through tissue protective, antioxidant and anti-inflammatory mechanisms.

Resumo Introdução: Antibióticos são frequentemente usados para o tratamento de rinossinusite. Questões têm sido levantadas sobre os efeitos adversos dos antibióticos e a resistência crescente. A falta de desenvolvimento de novos compostos antibióticos aumentou a necessidade da exploração de compostos não antibióticos que têm atividade antibacteriana. A amlodipina é um composto não antibiótico com atividade anti-inflamatória. Objetivo: O objetivo desse estudo foi investigar o papel potencial da amlodipina no tratamento da rinossinusite, avaliando seus efeitos sobre o estado oxidativo do tecido, histologia da mucosa e inflamação. Método: Quinze cobaias albinas adultas foram inoculadas com Staphylococcus aureus e tratadas com solução salina, cefazolina ou amlodipina durante sete dias. O grupo controle incluiu cinco cobaias saudáveis. Os animais foram sacrificados após o tratamento. Alterações histopatológicas foram identificadas com a coloração de hematoxilina-eosina. A inflamação foi avaliada pela densidade de infiltração de leucócitos polimorfonucleares. Foram determinados os níveis teciduais de antioxidantes (superóxido dismutase, glutationa) e um produto de oxidação (malondialdeído). Resultados: Em animais com rinossinusite induzida, a amlodipina reduziu a perda dos cílios, edema da lâmina própria e deposição de colágeno em comparação com o grupo placebo (solução salina) e embora não seja superior à cefazolina, a amlodipina diminuiu a infiltração de leucócitos polimorfonucleares. Os níveis de atividade da superóxido dismutase e glutationa foram reduzidos, enquanto os níveis de malondialdeído aumentaram significativamente nos três grupos de tratamento em comparação ao grupo controle. O grupo tratado com amlodipina apresentou aumento significante dos níveis de superóxido dismutase e glutationa e diminuição dos níveis de malondialdeído em comparação com todos os grupos de tratamento. Conclusão: O composto não antibiótico amlodipina pode ter um papel no tratamento da rinossinusite aguda através de mecanismos protetores de tecido, antioxidantes e anti-inflamatórios.

Influence of antihypertensive drugs on aortic and coronary effects of Ang-(1-7) in pressure-overloaded rats

This study investigated the influence of antihypertensive drugs, such as angiotensin-converting enzyme inhibitors (ACEIs), AT1 receptor blockers (ARBs), voltage-gated L-type calcium channel blockers, and mineralocorticoid receptor antagonists (MRAs), on the effects of angiotensin-(1-7) [Ang-(1-7)] on aorta and coronary arteries from pressure-overloaded rats. Pressure overload was induced by abdominal aortic banding (AB). To evaluate the role of antihypertensive drugs on the effect of Ang-(1-7), AB male Wistar rats weighing 250–300 g were treated with vehicle or low doses (5 mg·kg-1·day-1, gavage) of losartan, captopril, amlodipine, or spironolactone. Isolated aortic rings and isolated perfused hearts under constant flow were used to evaluate the effect of Ang-(1-7) in thoracic aorta and coronary arteries, respectively. Ang-(1-7) induced a significant relaxation in the aorta of sham animals, but this effect was reduced in the aortas of AB rats. Chronic treatments with losartan, captopril or amlodipine, but not with spironolactone, restored the Ang-(1-7)-induced aorta relaxation in AB rats. The coronary vasodilatation evoked by Ang-(1-7) in sham rats was blunted in hypertrophic rats. Only the treatment with losartan restored the coronary vasodilatory effect of Ang-(1-7) in AB rat hearts. These data support a beneficial vascular effect of an association of Ang-(1-7) and some antihypertensive drugs. Thus, this association may have potential as a new therapeutic strategy for cardiovascular diseases.

Renin-Angiotensin System Blockade Associated with Statin Improves Endothelial Function in Diabetics / Bloqueio do Sistema Renina-Angiotensina Associado a Estatina Melhora a Função Endotelial em Diabéticos

Abstract Background: Studies suggest that statins have pleiotropic effects, such as reduction in blood pressure, and improvement in endothelial function and vascular stiffness. Objective: To analyze if prior statin use influences the effect of renin-angiotensin-aldosterone system inhibitors on blood pressure, endothelial function, and vascular stiffness. Methods: Patients with diabetes and hypertension with office systolic blood pressure ≥ 130 mmHg and/or diastolic blood pressure ≥ 80 mmHg had their antihypertensive medications replaced by amlodipine during 6 weeks. They were then randomized to either benazepril or losartan for 12 additional weeks while continuing on amlodipine. Blood pressure (assessed with ambulatory blood pressure monitoring), endothelial function (brachial artery flow-mediated dilation), and vascular stiffness (pulse wave velocity) were evaluated before and after the combined treatment. In this study, a post hoc analysis was performed to compare patients who were or were not on statins (SU and NSU groups, respectively). Results: The SU group presented a greater reduction in the 24-hour systolic blood pressure (from 134 to 122 mmHg, p = 0.007), and in the brachial artery flow-mediated dilation (from 6.5 to 10.9%, p = 0.003) when compared with the NSU group (from 137 to 128 mmHg, p = 0.362, and from 7.5 to 8.3%, p = 0.820). There was no statistically significant difference in pulse wave velocity (SU group: from 9.95 to 9.90 m/s, p = 0.650; NSU group: from 10.65 to 11.05 m/s, p = 0.586). Conclusion: Combined use of statins, amlodipine, and renin-angiotensin-aldosterone system inhibitors improves the antihypertensive response and endothelial function in patients with hypertension and diabetes.

Resumo Fundamentos: Estudos sugerem que as estatinas possuem efeitos pleotrópicos, como melhora da função endotelial, da rigidez vascular e redução da pressão arterial. Objetivo: Analisar se o uso prévio de estatina influenciou o efeito sobre a pressão arterial, a função endotelial e a rigidez vascular de drogas inibidoras do sistema renina-angiotensina-aldosterona. Métodos: Pacientes hipertensos e diabéticos com pressão arterial de consultório sistólica ≥ 130 mmHg e/ou diastólica ≥ 80 mmHg tiveram suas medicações anti-hipertensivas substituídas por anlodipino durante 6 semanas. Em seguida, foram randomizados para associação de benazepril ou losartana por mais 12 semanas. Pressão arterial (através da monitorização ambulatorial da pressão arterial), função endotelial (dilatação mediada por fluxo da artéria braquial) e rigidez vascular (velocidade da onda de pulso) foram avaliados antes e após o tratamento combinado. Neste trabalho, uma análise post-hoc foi realizada para comparar pacientes que vinham (grupo CE) ou não (grupo SE) em uso de estatina. Resultados: O grupo CE apresentou maior redução na pressão arterial sistólica nas 24 horas (134 para 122 mmHg, p = 0,007) e na dilatação mediada por fluxo da artéria braquial (6,5 para 10,9%, p = 0,003) quando comparado com o grupo SE (137 para 128 mmHg, p = 0,362, e 7,5 para 8,3%, p = 0,820). Não houve diferença estatisticamente significante na velocidade de onda de pulso (grupo CE 9,95 para 9,90 m/s, p = 0,650 e grupo SE 10,65 para 11,05 m/s, p = 0,586). Conclusão: O uso combinado de estatinas, anlodipino e inibidores do sistema renina-angiotensina-aldosterona melhora a resposta anti-hipertensiva e a função endotelial em pacientes hipertensos e diabéticos.

Evaluation of Nosocomial Infection Control Programs in health services / Avaliação dos Programas de Controle de Infecção Hospitalar em serviços de saúde / Evaluación de los Programas de Control de Infección Hospitalaria en servicios de salud

OBJECTIVES: to evaluate the Nosocomial Infection Control Programs in hospital institutions regarding structure and process indicators. METHOD: this is a descriptive, exploratory and quantitative study conducted in 2013. The study population comprised 13 Nosocomial Infection Control Programs of health services in a Brazilian city of the state of São Paulo. Public domain instruments available in the Manual of Evaluation Indicators of Nosocomial Infection Control Practices were used. RESULTS: The indicators with the highest average compliance were "Evaluation of the Structure of the Nosocomial Infection Control Programs" (75%) and "Evaluation of the Epidemiological Surveillance System of Nosocomial Infection" (82%) and those with the lowest mean compliance scores were "Evaluation of Operational Guidelines" (58.97%) and "Evaluation of Activities of Control and Prevention of Nosocomial Infection" (60.29%). CONCLUSION: The use of indicators identified that, despite having produced knowledge about prevention and control of nosocomial infections, there is still a large gap between the practice and the recommendations. .

OBJETIVOS: avaliar os Programas de Controle de Infecção Hospitalar nas instituições hospitalares, quanto aos indicadores de estrutura e processo. MÉTODO: trata-se de um estudo descritivo, exploratório e quantitativo, realizado em 2013. A população foi composta por 13 Programas de Controle de Infecção Hospitalar de serviços de saúde, de uma cidade brasileira do interior paulista. Foram utilizados instrumentos de domínio público, disponibilizados no Manual de Indicadores de Avaliação de Práticas de Controle de Infecção Hospitalar. RESULTADOS: os indicadores com maior média de conformidade foram "Avaliação da Estrutura dos Programas de Controle de Infecção Hospitalar" (75%) e "Avaliação do Sistema de Vigilância Epidemiológica de Infecção Hospitalar" (82%) e os com menores médias foram "Avaliação das Diretrizes Operacionais" (58,97%) e "Avaliação das Atividades de Controle e Prevenção de Infecção Hospitalar" (60,29%). CONCLUSÃO: o uso de indicadores identificou que, apesar do conhecimento produzido sobre ações de prevenção e controle de infecções hospitalares, ainda existe um grande hiato entre prática e recomendações. .

OBJETIVOS: evaluar los Programas de Control de Infección Hospitalaria en las instituciones hospitalarias respecto a los indicadores de estructura y proceso. MÉTODO: se trata de un estudio descriptivo, exploratorio y cuantitativo, desarrollado en 2013. La población fue compuesta por 13 Programas de Control de Infección Hospitalaria de servicios de salud de una ciudad brasileña del interior paulista. Fueron utilizados instrumentos de dominio público, disponibles en el Manual de Indicadores de Evaluación de Prácticas de Control de Infección Hospitalaria. RESULTADOS: los indicadores con mayor promedio de conformidad fueron "Evaluación de la Estructura de los Programas de Control de Infección Hospitalaria" (75%) y "Evaluación del Sistema de Vigilancia Epidemiológica de Infección Hospitalaria" (82%) y aquellos con menores promedios "Evaluación de las Directivas Operacionales" (58,97%) y "Evaluación de las Actividades de Control y Prevención de Infección Hospitalaria" (60,29%). CONCLUSIÓN: el uso de indicadores posibilitó identificar que, a pesar del conocimiento producido sobre acciones de prevención y control de infecciones hospitalarias, todavía existe un gran hiato entre la práctica y las recomendaciones. .

Functional Vascular Study in Hypertensive Subjects with Type 2 Diabetes Using Losartan or Amlodipine / Estudo Vascular Funcional em Hipertensos com Diabetes Tipo 2 em uso de Losartana ou Anlodipina

Background: Antihypertensive drugs are used to control blood pressure (BP) and reduce macro- and microvascular complications in hypertensive patients with diabetes. Objectives: The present study aimed to compare the functional vascular changes in hypertensive patients with type 2 diabetes mellitus after 6 weeks of treatment with amlodipine or losartan. Methods: Patients with a previous diagnosis of hypertension and type 2 diabetes mellitus were randomly divided into 2 groups and evaluated after 6 weeks of treatment with amlodipine (5 mg/day) or losartan (100 mg/day). Patient evaluation included BP measurement, ambulatory BP monitoring, and assessment of vascular parameters using applanation tonometry, pulse wave velocity (PWV), and flow-mediated dilation (FMD) of the brachial artery. Results: A total of 42 patients were evaluated (21 in each group), with a predominance of women (71%) in both groups. The mean age of the patients in both groups was similar (amlodipine group: 54.9 ± 4.5 years; losartan group: 54.0 ± 6.9 years), with no significant difference in the mean BP [amlodipine group: 145 ± 14 mmHg (systolic) and 84 ± 8 mmHg (diastolic); losartan group: 153 ± 19 mmHg (systolic) and 90 ± 9 mmHg (diastolic)]. The augmentation index (30% ± 9% and 36% ± 8%, p = 0.025) and augmentation pressure (16 ± 6 mmHg and 20 ± 8 mmHg, p = 0.045) were lower in the amlodipine group when compared with the losartan group. PWV and FMD were similar in both groups. Conclusions: Hypertensive patients with type 2 diabetes mellitus treated with amlodipine exhibited an improved pattern of pulse wave reflection in comparison with those treated with losartan. However, the use of losartan may be associated with independent vascular reactivity to the pressor effect. .

Fundamento: A escolha dos fármacos anti-hipertensivos no tratamento de hipertensos diabéticos tem como objetivos o controle da pressão arterial (PA) e a redução das complicações macro/microvasculares. Objetivos: O objetivo deste estudo foi comparar as alterações vasculares funcionais em pacientes hipertensos e diabéticos tipo 2 após seis semanas de anlodipina ou losartana. Métodos: Pacientes com diagnóstico prévio de hipertensão arterial e diabetes melito tipo 2 foram randomizados e divididos em dois grupos, sendo avaliados na sexta semana de uso de losartana 100 mg/dia ou anlodipina 5 mg/dia, com medida da PA, realização de monitoração ambulatorial da pressão arterial e testes para avaliação de parâmetros vasculares, como tonometria de aplanação, velocidade de onda de pulso (VOP) e dilatação mediada por fluxo (DMF) da artéria braquial. Resultados: Foram incluídos 42 pacientes, 21 em cada grupo, com predominância do sexo feminino (71%) nos dois grupos. Os grupos anlodipina e losartana apresentaram média de idade semelhante (54,9 ± 4,5 e 54,0 ± 6,9 anos, respectivamente) e sem diferença estatística na média da PA (145 ± 14/84 ± 8 e 153 ± 19/90 ± 9 mmHg). O augmentation index (30 ± 9% × 36 ± 8%, p = 0,025), assim como a augmentation pressure (16 ± 6 mmHg × 20 ± 8 mmHg, p = 0,045) foram menores no grupo anlodipina que no grupo losartana. Os valores obtidos para VOP e DMF foram semelhantes nos dois grupos. Conclusões: Em hipertensos e diabéticos tipo 2, o uso de anlodipina demonstrou um padrão de reflexão da onda de pulso mais favorável nesse grupo, mas o uso de losartana pode estar associado com ações vasculares independentes do efeito pressórico. .

Effects of captopril vs amlodipine on blood pressure, serum glucose and lipid profile in overweight and obese hypertensive patients

To investigate the effects of captopril vs amlodipine on blood pressure, BMI, serum glucose concentration and lipid profile in overweight and obese hypertensive patients. This study was conducted on two groups of overweight and obese newly diagnosed stage 1 hypertensive patients; captopril group included 42 patients who were kept on captopril monotherapy and amlodipine group included 41 patients who were kept on amlodipine monotherapy. Another 40 apparently healthy normotensive individuals were used as a control group. The patients were placed on captopril or amlodipine for 8 weeks. Systolic and diastolic BP, body weight, BMI, fasting serum glucose and lipid profile were measured before and at the end of trial. After 8 weeks of treatment with captopril or amlodipine the measured parameters are significantly reduced but comparison of each group revealed no significant differences except Fasting Glucose, where a higher reduction was seen with captopril. Both captopril and amlodipine were effective in the treatment of hypertension in overweight and obese patients. In addition, both drugs had beneficial effects on body weight, serum glucose concentration and lipid profile

Hepatoprotective effect of some drugs in experimental model of acute liver injury

Acute liver injury is a clinical condition that results from severe extensive damage of liver tissue associated with Jaundice and it is experimentally induced by hepatotoxic agents like ccl[4]. Thirty five healthy rabbits were involved in the present study. They were allocated to five groups. Each group was given one of the following agents: vitamin E, zinc sulfate, amlodipine besylate, distilled water two hours before administration of ccl[4]. The same doses of the tested agents were continued for two days after ccl[4] administration. The effect of drugs was evaluated at two occasions 24 and 72 hours after ALI induction on the basis of biochemical analysis of liver function tests as well as histopathological examination to the liver of treated animals. All the tested agents produced significant reduction in ALT, AST, ALP, and TSB with a significant elevation of TSP levels as compared with treated control group. The histopathological examination showed clear improvements in the sections of liver tissue that support the effect of these agents on the liver. The study showed that 30% of women were anemic; the effect of anemia on thyroid function was not clear as 98% of the studied women have normal thyroxin and only 1% has low thyroxin level while 1% showed high concentration of thyroxin level. All the tested agents proved to have hepatoprotective effect of varying degree on ALI model

Comparison of the effects of losartan and amlodipine on plasma leptin and insulin sensitivity in hypertensive obese patients

Aim of this study was to compare the effect of losartan and amlodipine on blood pressure [BP] plasma leptin [L] and insulin sensitivity in obese hypertensive patients. Forty- eight obese patients [body mass index [BMI] >/= 30 kg/m2] with mild to moderate essential hypertension [diastolic blood pressure [DBF] >90 and <110 mmHg, as evaluated with an appropriately sized cuff] aged 30-70 years, were randomized to a losartan [50 mg/day for 12 weeks; n=24] or amlodipine [5 mg/day for 12 weeks; n=24] treatment group after a 2-week wash-out period, After the first 4 weeks of treatment there was a titration with dose-doubling in non responder patients [DBP > 90 mmHg]. At the end of the wash out period and of active treatment period, BP and BMI were evaluated and a venous sample was drawn at the same hour in the morning to evaluate plasma L and Insulin resistance index [HOMA-IR] was calculated. No dietary advice was prescribed. Both losartan and amlodipine significantly decreased BP values and HOMA-IR INDEX with no difference between treatments. However, amlodipine had no effect on L and body weight, while losartan produced a significant reduction in L and BMI. These results suggest that in hypertensive obese subjects, treatment with losartan might offer an advantage over treatment with amlodipine, since losartan may help to improve obesity-related disorders in addition to lowering BP

Kinetics and mechanisms of cholesterol esterase inhibition by cardiovascular drugs in vitro.

Cardiovascular drugs such as lovastatin, simvastatin, amlodipine besylate, nifedipine, and hydralazine hydrochloride inhibit cholesterol esterase (CEase) in vitro. In the present paper, an attempt was made to determine kinetically the reaction mechanism for CEase inhibition by these drugs. The inhibition constant, Ki, for the mixed-type inhibition of CEase by these drugs in the presence of triton-X-100 or taurochloate were measured. Moreover, the pKi values were correlated with the molecular weights of these drugs. In conclusion, the fact that these drugs lower cholesterol levels in the plasma low-density lipoprotein may be partially due to the CEase inhibition by these drugs.

Effect of nifedipine and amlodipine on dead space wound healing in rats.

Effect of two calcium channel blockers (CCBs) nifedipine and amlodipine, was studied on normal and steroid depressed wound healing in albino rats, using the dead space wound model. The drugs enhanced normal healing as evidenced by increase in tensile strength of 10 days old granulation tissue. There was neither a significant change in the hydroxyproline level (or collagen) nor a change in the glycosaminoglycan content in granulation tissue. However, lysyloxidase level was increased significantly. The increase in tensile strength could thus be attributed to better cross-linking and maturation of collagen rather than collagen synthesis per se. The drugs were also able to overcome steroid depressed wound healing. It is likely that the prohealing effects may be related to the improved antioxidant status too, since superoxide dismutase levels were observed to be higher in the CCB- treated animals.

mechanism of action of calcium channel blockers in the treatment of diabetic nephropathy

Three types of calcium channels have been identified voltage-sensitive, receptor operated [cardiac muscle and vascular smooth muscle] and stretch operated [in some blood vessels] channels. Using electrophysiological and pharmacological techniques, three different types of voltage-gated calcium channels have been identified, namely, L-type [for long lasting, large channels], T-type [for transient, tiny channels] and N-type [for neuronal, neither L nor T]. Many compounds are known to have a calcium channel inhibitory effect. Calcium antagonists, based on the specificity of inhibition of the slow calcium current, can be classified into three groups: Group A: for 90 to 100 percent inhibition of calcium influx without change in the sodium current [verapamil, diltiazem and the dihydropyridines]; Group B: for 50 to 70 percent inhibition of calcium influx current without change in the sodium current [bepridil, cinnarizine and prenylamine] and Group C: for agents exhibiting some inhibition of calcium influx [phenytoin, indomethacin and propranolol]. There is now increasing evidence that, certain calcium channel blockers especially the dihydropyridines are more strongly associated with vasodilation of afferent arterioles than of efferent arterioles and also with increase intraglomerular pressure and albuminuria. Thus they have a beneficial effect in terms of reducing proteinuria and slowing the progression of diabetic renal failure

Effect of nifedipine and amlodipine on wound healing in rats.

The wound healing effect of two calcium channel blockers, nifedipine and amlodipine was studied in rats using incision and excision wound models. In incision wound, two straight paravertebral skin thickness incision were made and on tenth day skin tensile strength was measured by using continuous water flow technique. In excision wound, circular piece of skin excised in its full thickness and wound contraction monitored by alternate day wound tracing and epithelisation period was monitored by noting the number of days required for escher to fall. Drugs enhanced the skin tensile strength in incision wound model. In excision wound model, wound contraction is increased on 4th and 16th day but epithlisation period was not significantly altered. In conclusion, calcium channel blockers can be used to enhance wound healing, especially if wound healing was suppressed by steroids.

Pharmacokinetics of phenytoin: unaltered by enalapril and amlodipine in rhesus monkeys.

A cross over single and multiple dose study was carried out to find out pharmacokinetic interactions between diphynylhydantoin (DPH) (35 mg/kg, p.o.) and antihypertensives enalapril (1.6 mg/kg; p.o.) and amlodipine (0.4 mg/kg, p.o.) in rhesus monkeys. Neither the plasma concentrations nor the pharmacokinetic parameters of DPH were altered by coadministration of enalapril or amlodipine, suggesting that enalapril and amlodipine can be safely administered to epileptic patients receiving phenytoin.

A study of pulmonary profile of hypertensive patients--comparison of atenolol vs amlodipine.

Two groups of drugs commonly used for the treatment of hypertension are atenolol and amlodipine. These drugs are reported to have conflicting changes on pulmonary responses. In order to study the effect of hypertension and antihypertensive treatment on pulmonary responses, 40 patients with essential hypertension having diastolic blood pressure between 90-114 mmHg on three consecutive weekly visits were taken. Pulmonary responses were tested at the end of 2 weeks of placebo washout period and then at the end of 6 weeks of treatment with either atenolol or amodipine. Using a computerized autospiror along with the weekly recordings of heart rate and blood pressure, the various pulmonary and cardiac parameters were taken. Analysis of the result showed that atenolol treatment resulted in significant decline of forced vital capacity (FVC), % forced vital capacity (%FVC), and forced expiratory volume in first second (FEV1) whereas amlodipine did not show any significant change on pulmonary parameters.

Cambios hemodinámicos en la función sistólica, diastólica y la circulación periférica inducidas por amlodipina en pacientes con hipertensión arterial esencial asociada con disfunción ventricular izquierda / Hemodynamic changes in systolic and diastolic function and in the peripheral circulation induced by amlodipine in patients with essencial hypertension with left ventricular dysfunction

La hipertensión arterial afecta la función y la estructura cardiovascular, con hipertrofia y disfunción ventricular frecuentes, en especial en pacientes con cardiopatía isquémica asociada. Evaluamos 20 pacientes entre 40 y 70 años de edad, con diagnóstico de hipertensión esencial (presión arterial diastólica entre 95 y 115 mmHg) asociada a disfunción ventricular (fracción de eyección ó 45 por ciento). Se estudiaron por angiografía radioisotópica la función sistólica, la función diastólica y la circulación periférica en las siguientes etapas: A) al final del período lavado-placebo (pretratamiento); B) en fase aguda, a las 6 horas de amlodipina (10 mg) por vía oral; C) en fase crónica, al final de 8 semanas de igual tratamiento con monodosis. El tratamiento en fase aguda y crónica mostró una disminución significativa de la presión arterial sistólica, diastólica y de la resistencia periférica total (en un 15 por ciento, 14 por ciento y 20 por ciento respectivamente). El pico de llenado del ventrículo izquierdo basal fue 1,9 ñ 0,4 (VFD/S), mejorando un 21 por ciento en el tratamiento crónico en reposo y 17 por ciento durante el ejercicio ergométrico, lo que evidenció una mejoría de la función diastólica del ventrículo izquierdo (p<0,01). El volumen de fin de sístole o residual, aumentado como expresión de la falla de bomba, disminuyó en 15 y 19 por ciento en reposo y esfuerzo. En el pretratamiento los parámetros hemodinámicos muestran disfunción ventricular sistólica y diastólica del ventrículo izquierdo con compromiso del ventrículo derecho, tanto en reposo como en esfuerzo, con disminución de la reserva cardíaca. El efecto vasodilatador de la amlodipina, con disminución de la poscarga, produjo efectos hemodinámicos favorables, tanto en el control de la hipertensión arterial como en la mejoría de la disfunción biventricular asociada

Estudio clínico de eficacia y seguridad de amlodipina en hipertensión arterial / Amlodipine in hypertension: a clinical study of safety and efficacy

Se presenta un estudio prospectivo, abierto, no controlado, realizado para evaluar la eficacia y seguridad de la amlodipina en el tratamiento de la hipertensión arterial esencial. El mismo tuvo dos fases: placebo durante las primeras 2 semanas e intervención farmacológica en las siguientes 12 semanas, con una dosis diaria de 5 a 10 mg de amlodipina oral. Se evaluaron 70 pacientes adultos. La edad promedio fue 59,2 ñ 10,1 (34-84) años, siendo el 74 por ciento de sexo femenino. Veintitrés pacientes (32,9 por ciento) fueron clasificados como hipertensos leves, 41 (58,6 por ciento) como moderados y 6 (8,5 por ciento) como severos. La presión arterial sistólica inicial fue de 161,2 ñ 10,8 y la diastólica de 101,3 ñ 4,2 mmHg, con valores finales de 133,6 ñ 10,7 y 82,5 ñ 5,6 mmHg, respectivamente. Los descensos logrados, -17,1 por ciento y -18,6 por ciento fueron estadísticamente significativos (p<0,05). La hipertensión arterial sistólica se controló exitosamente en el 85,7 por ciento y la diastólica en el 98,6 por ciento de los pacientes. El 65,7 por ciento de los pacientes recibió amlodipina como monoterapia

Efecto antihipertensivo de la amlodipina 48 a 72 horas después del tratamiento: un estudio con presurometría ambulatoria / Antihypertensive effect of amlodipine 48 a 72 hours after treatment: a study with ambulatory blood pressure monitoring

Se llevó a cabo este estudio abierto, simple ciego, no comparativo y controlado con placebo en 30 pacientes sin evidencia de hipertensión secundaria, para evaluar la eficacia de la amlodipina administrada en una sola dosis al día. Después de un período de placebo de dos semanas, siguió un período de 10 semanas de tratamiento activo; la dosis inicial de amlodipina fue de 5 mg una vez al día, la cual se aumentó a 10 mg a las cuatro semanas, en los pacientes en los que no se controló la hipertensión. La determinación de la presión arterial de manera convencional se efectuó en la semana 0, al final de la primera y segunda semanas y cada dos semanas en la fase de titulación y al fin del estudio; las cifras obtenidas al final de la segunda semana del período de placebo se tomaron como basales. El monitoreo ambulatorio de la presión arterial se llevó a cabo el último día del período placebo, el primer día de tratamiento activo, durante el último día del período de mantenimiento y durante las 48 a 72 horas que siguieron a la última dosis. Los resultados demuestran que la amlodipina es efectiva en el control de la presión arterial a lo largo de las 24 horas del día y que su actividad antihipertensiva perdura aún en el lapso entre las 48 y 72 horas posteriores a la suspensión del tratamiento

La necesidad de adecuar en cada paciente el tratamiento antihipertensivo y antianginoso: papel de los bloqueantes cálcicos de acción prolongada / The necessity of tailoring antihypertensive and antianginal therapy to the individual patient: the place of long-actin calcium channel blockers

La patología cardiovascular afecta a más de uno de cada cuatro habitantes en los países desarrollados y es la causa principal de mortalidad, en varones y mujeres, los avances en su tratamiento han contribuído a disminuir las tasas de mortalidad por enfermedad cardiovascular, pero las tasas de morbimortalidad asociadas a hipertensión, enfermedad coronaria y accidente cerebrovascular todavía son preocupantes. El manejo óptimo de la enfermedad cardiovascular requiere una elección individualizada del tratamiento para cada paciente en particular, de manera que, además de los efectos terapéuticos, se consiga una buena tolerancia durante largos períodos. Los bloqueantes cálcicos de acción prolongada, tales como la amlodipina, representan una opción importante en el tratamiento de la hipertensión y la angina. Los bloqueantes cálcicos de acción prolongada como la amlodipina son drogas de primera línea para el tratamiento individualizado de la enfermedad cardiovascular

Cumplimiento de la terapia antihipertensiva / Antihypertensive therapy compliance

El cumplimiento en el tratamiento antihipertensivo es muy importante para proteger al paciente de las complicaciones cardíacas y cerebrovasculares de la hipertensión. Con el régimen de dos veces al día, el 50 por ciento toman la medicación prescripta el 90 por ciento de los días de observación, comparado con el 70 por ciento cuando los pacientes cumplen la medicación una vez al día. la acción antihipertensiva de la amlodipina y el enalapril ha sido publicada recientemente por nuestro grupo de investigación, en un estudio controlado, paralelo, doble ciego y al azar. Después de cuatro semanas de recibir placebo en forma ciego-simple, los pacientes fueron asignados a recibir 20 mg de enalapril (15 pacientes) o 5 mg de amlodipina (15 pacientes) una vez al día. En la cuarta semana de medicación activa la dosis fue duplicada, en caso que la presión arterial diastólica en posición sentada fuera superior a 90 mmHg. Un monitoreo ambulatorio de presión arterial fue realizado al final de la etapa placebo por un período de 24 horas y al final de la semana 12 de tratamiento activo por un período de 48 horas. Las reducciones en la presión arterial fueron mayores en el grupo amlodipina