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1.
Radiol Med ; 116(1): 152-62, 2011 Feb.
Artículo en Inglés, Italiano | MEDLINE | ID: mdl-20852953

RESUMEN

PURPOSE: This study evaluated the appropriateness and accuracy of 500 radiology requests and their matched reports in order to identify recurring errors in both areas. MATERIALS AND METHODS: A randomly chosen sample consisting of 167 computed tomography (CT), 166 ultrasonography (US) and 167 radiographic examinations were collected and analysed according to national referral guidelines and to the principles of justification and optimisation (Law no. 187/2000). RESULTS: We identified a high rate of inappropriate requests (27.6%) and requests lacking a clinical question (22%). There was good precision in the anamnestic data (80.6%) and in the formulation of the diagnostic question (76.8%). Almost all requests were handwritten, and 12.5% lacked the referring physician's stamp and/or signature. No report mentioned the clinical information received or the equipment used. The use of contrast medium was always reported. Conclusions were reported in 9.8% of these reports. When further investigation would have been necessary, the radiologist omitted to report this in 60% of cases. CONCLUSIONS: Some important weaknesses emerged, especially regarding requests for radiological examinations (22% lacked the clinical question, 27.6% were inappropriate), potentially limiting the effectiveness of the diagnostic process and leading to negative effects on the correct risk management process. There emerges a need for better collaboration between clinicians and radiologists.


Asunto(s)
Derivación y Consulta/estadística & datos numéricos , Tomografía Computarizada por Rayos X/estadística & datos numéricos , Ultrasonografía/estadística & datos numéricos , Medios de Contraste , Humanos , Italia , Guías de Práctica Clínica como Asunto
2.
An Pediatr (Barc) ; 72(1): 62-6, 2010 Jan.
Artículo en Español | MEDLINE | ID: mdl-19836321

RESUMEN

INTRODUCTION: During the Influenza A H1N1 pandemic an aggressive manifestation of the disease was observed in children and some cases required admittance to intensive care unit. We describe the initial presentation and clinical behavior of critical pediatric patients treated in our unit. MATERIAL AND METHODS: Observational, descriptive and retrospective study performed in a 20 bed Pediatric Intensive Care Unit (PICU). All patients with H1N1 presence confirmed by Polymerase Chain Reaction (PCR) admitted from June 1st 2009 to August 1st 2009 were included. RESULTS: Influenza A HINI virus was positive in 20 out of 113 patients (17,7%) tested , with 95% (19) of these patients requiring mechanical ventilation. Out of these 20, 18 (90%) had respiratory distress, 16 of them (80%) at admittance and 2 (10%) during their stay in PICU. The mortality rate was 50%. CONCLUSION: We observed severe respiratory disease that required mechanical ventilation in confirmed cases admitted to the PICU and a mortality rate of 50%.


Asunto(s)
Subtipo H1N1 del Virus de la Influenza A , Gripe Humana , Argentina , Preescolar , Femenino , Humanos , Lactante , Gripe Humana/diagnóstico , Gripe Humana/epidemiología , Gripe Humana/terapia , Unidades de Cuidado Intensivo Pediátrico , Masculino , Estudios Retrospectivos
3.
Monaldi Arch Chest Dis ; 63(1): 13-6, 2005 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-16035559

RESUMEN

BACKGROUND: The association between weight loss and Chronic Obstructive Pulmonary Disease (COPD) has been recognised from many years. Based on the evidence that nutritional status reflects metabolic disturbances in COPD, the relationship between body mass index (BMI), severity of airflow obstruction and CO diffusing capacity (DL(CO)), that is the functional hallmark of emphysema, is relevant to the management of COPD phenotypes. METHODS: We reviewed 104 patients with COPD (82 males), aged 66 +/- 9 years (mean +/- SD). Height averaged 165 +/- 8 cm, weight 71 +/- 16 Kg, FEV1 50 +/- 18 (% of predicted), RV 169 +/- 49%, and DL(CO) 56 +/- 26%. Multiple linear regression was performed using BMI, FEV1 and RV, as explanatory variables for DL(CO). Patients were also classified into four groups according to BMI < or = 18.5 (low), > 18.5 and < or = 25 (ideal), > 25 and < or = 30 (overweight), > 30 (obese), and post-bronchodilator FEV1 < 50%. Using this categorisation, a two-factor analysis of variance, testing for interaction and main effects (BMI and FEV1) was performed as confirmatory analysis for the association between BMI (kg/m2), FEV1% and DL(CO)%. RESULTS: FEV1 and BMI were significantly and independently associated to DL(CO) according to the equation: DL(CO) = -18.32 + 0.65 x FEV1 + 1.59 x BMI (R2 = 0.40, p < 0.0001). The contribution of RV % to DL(CO) % was largely non-significant (p = 0.16). A close relationship was found between BMI (kg/m2) and DL(CO) %, for all of the four BMI groups segregated by post-bronchodilator FEV1 %, (p < .0001). No interaction was found between these two factors (p = 0.30). CONCLUSION: Nutritional status as assessed by BMI contributes substantially to impairment of DL(CO) independently of the severity of airflow obstruction. This data confirms the association between emphysematous process and weight loss in advanced COPD, independent of the airflow obstruction severity.


Asunto(s)
Monóxido de Carbono/metabolismo , Estado Nutricional , Enfermedad Pulmonar Obstructiva Crónica/fisiopatología , Adulto , Anciano , Anciano de 80 o más Años , Análisis de Varianza , Índice de Masa Corporal , Difusión , Femenino , Volumen Espiratorio Forzado , Humanos , Masculino , Persona de Mediana Edad , Pruebas de Función Respiratoria
4.
Pulm Pharmacol Ther ; 16(4): 231-6, 2003.
Artículo en Inglés | MEDLINE | ID: mdl-12850126

RESUMEN

To evaluate whether the peripherally acting antitussive levodropropizine could affect the respiratory drive and the breathing pattern, we performed a double-blind, randomised, cross-over trial in 12 healthy volunteers and 12 patients with chronic respiratory impairment associated with chronic obstructive pulmonary disease. Levodropropizine 6% drops (at the recommended dose for adults) or placebo were administered orally t.i.d. for 10 consecutive administrations. Mouth occlusion pressure (P0.1), minute ventilation (V(e)), tidal volume (V(t)), respiratory rate (RR), mean inspiratory flow (V(t)/T(i)), end-tidal CO(2) (EtCO(2)), oxygen saturation (SaO(2)), forced expiratory volume in 1 s (FEV(1)), and the response to a hypercapnic stimulus were measured before and 1 h after the first and the last drug administration. Levodropropizine did not modify P0.1 in basal conditions and after a hypercapnic stimulus, either in healthy volunteers or in patients. In parallel, levodropropizine did not significantly affect V(t), RR, V(e), V(t)/T(i) and EtCO(2) in both the populations. Minor changes were induced by levodropropizine on SaO(2) in healthy volunteers, which despite a statistical difference, were too low to gain a clinical significance. These results confirmed the respiratory safety of levodropropizine 6% drops administered at the recommended dosage either in healthy volunteers or patients with chronic respiratory impairment.


Asunto(s)
Antitusígenos/uso terapéutico , Glicoles de Propileno/uso terapéutico , Enfermedad Pulmonar Obstructiva Crónica/tratamiento farmacológico , Respiración/efectos de los fármacos , Adulto , Estudios Cruzados , Método Doble Ciego , Femenino , Humanos , Masculino , Pruebas de Función Respiratoria
6.
Sleep ; 23(6): 775-81, 2000 Sep 15.
Artículo en Inglés | MEDLINE | ID: mdl-11007444

RESUMEN

Erectile dysfunction (ED) is common in men with obstructive sleep apnea (OSAS) but no completely convincing hypotheses about the underlying pathogenic mechanisms have been published in the literature. The aims of the present study were to assess the presence of ED in a group of OSAS patients without daytime respiratory failure and to determine whether this dysfunction was related to peripheral nerve involvement. Evaluation of the bulbocavernosus reflex (BCR) and the somato-sensory evoked potentials of pudendal nerve (PSEPs), the most widely established method of documenting pudendal neuropathies as being the cause of impotence, was performed in 25 patients. Data on BCR were compared with those of 25 healthy males volunteers matched for age. BCR was altered in 17 patients: in 6 it was elicited while in 11 it had a prolonged latency and reduced amplitude. Patients with altered BCR presented an higher AHI, an higher percentage of sleep time spent with SaO2 <90% (TST90) and a lower daytime PaO2. Six patient had clinically silent neurophysiological signs of mild polyneuropathy. The degree of OSAS and gas exchange alteration was more severe in patients with polyneuropathy than in those with isolated BCR alteration. ED is a common finding in OSAS patients and this alteration seems to be related to a nerve dysfunction. The development of nerve dysfunction is associated with a more severe degree of OSAS and nocturnal hypoxia.


Asunto(s)
Disfunción Eréctil/etiología , Apnea Obstructiva del Sueño/complicaciones , Nivel de Alerta/fisiología , Disfunción Eréctil/diagnóstico , Disfunción Eréctil/fisiopatología , Potenciales Evocados Somatosensoriales/fisiología , Humanos , Masculino , Persona de Mediana Edad , Conducción Nerviosa/fisiología , Nervios Periféricos/fisiopatología , Polisomnografía , Estudios Prospectivos , Pruebas de Función Respiratoria , Apnea Obstructiva del Sueño/diagnóstico
7.
Org Lett ; 2(7): 933-6, 2000 Apr 06.
Artículo en Inglés | MEDLINE | ID: mdl-10768190

RESUMEN

Chiral copper complexes of C2-symmetrical phosphoroamidites were found to be highly effective catalysts for both kinetic resolution and novel desymmetrization reactions of new methylidene epoxycycloalkanes.

8.
Rev Assoc Med Bras (1992) ; 44(2): 99-105, 1998.
Artículo en Portugués | MEDLINE | ID: mdl-9699326

RESUMEN

BACKGROUND: Congenital lobar emphysema is an unusual condition and its pathogenesis remains unknown. The variety of findings in pathology studies of the resected specimens led to increasing academic interest. About 50 per cent of the cases have no definitive diagnosis in pathology. The most recent theory proposes an increased number of alveoli within each acinus (polyalveolar lobe). PURPOSE: The aim of this paper is to report the morphometric measures of surgical specimens of 12 patients with congenital lobar emphysema, using the Emery and Mithal technique (radial alveolar count). METHODS: We made a case-control study, classifying the cases by age. Mann-Whitney's U test and linear regression techniques were used in data analysis: Mann-Whitney's U in comparing the cases and respective controls and linear regression to evaluate the influence of age in the measures found. RESULTS: The results revealed a significantly higher radial alveolar count than expected for the age group under 3 years; no difference was observed in the age group between 3 and 7 years and in children older than 7, the radial alveolar count was lower than expected. The normal development of the lung consists in an increasing number of alveoli increase from birth until adulthood, but this number remains constant, independent of age in congenital lobar emphysema. CONCLUSIONS: Such findings allow us to conclude that polyalveolar lobe can and must be diagnosed by a simple and practical method, such as the radial alveolar count, which decreases the incidence of the unknown etiology. The findings of an increased number of alveoli on patients younger than 3 is related to congenital lobar emphysema, since the number of alveoli does not increase in congenital lobar emphysema, just the opposite to what one would expect in the normal development of the lung.


Asunto(s)
Alveolos Pulmonares/anomalías , Enfisema Pulmonar/congénito , Adolescente , Estudios de Casos y Controles , Niño , Preescolar , Humanos , Lactante , Recién Nacido , Pulmón/patología , Enfisema Pulmonar/etiología , Enfisema Pulmonar/patología
9.
Rev. Assoc. Med. Bras. (1992, Impr.) ; Rev. Assoc. Med. Bras. (1992, Impr.);44(2): 99-105, abr.-jun. 1998. ilus, tab, graf
Artículo en Portugués | LILACS | ID: lil-212837

RESUMEN

Introduçao. O enfisema lobar congênito é doença rara, cuja patogênese permanece desconhecida. O interesse acadêmico reside na falta de uniformidade dos achados anatomopatológicos. Em cerca de 50 por cento, nao se consegue definir a lesao anatomopatológica. A teoria mais recente relaciona esta doença com um número aumentado de alvéolos dentro de cada ácino pulmonar. Objetivo. O objetivo deste trabalho é efetuar uma revisao do estudo anatomopatológico original de 12 crianças com diagnóstico de enfisema lobar congênito, procurando, mediante método quantitativo, pesquisar a presença do aumento do número de alvéolos no ácido pulmonar. Método. Os autores realizaram um estudo caso-controle pareado pela idade. O número de alvéolos em cada ácino pulmonar foi pesquisado pela técnica da contagem radial de alvéolos. Para comparar as medidas obtidas nos casos e seus respectivos controles, utilizaram a prova U de Mann-Whitney Regressao linear avaliou a influência da idade sobre as medidas. Resultados. Encontraram um número elevado de alvéolos nos portadores de enfisema lobar congênito operados com idade inferior a 3 anos, um número semelhante entre as idade de 3 e 7 anos e um número diminuído a partir dessa idade. Na criança normal, ocorre um aumento no número de alvéolos com o aumento da idade. No enfisema lobar congênito, esse número se mantém praticamente constante, independente da idade. Conclusao. Os achados permitiram concluir que: o lobo polialveolar pode ser diagnosticado por um método simples e prático como a contagem radial de alvéolos, colaborando para diminuir a freqüência de casos de etiologia desconhecida, um número de alvéolos maior que o esperado para idade encontra-se associado ao enfisema lobar congênito no paciente (operado) antes dos 3 anos de idade e que, ao contrário do que ocorre no pulmao normal, no lobo acometido por enfisema lobar congênito nao ocorre aumento no número de alvéolos com o aumento na idade.


Asunto(s)
Niño , Preescolar , Lactante , Recién Nacido , Adolescente , Humanos , Alveolos Pulmonares/anomalías , Enfisema Pulmonar/congénito , Enfisema Pulmonar/etiología , Alveolos Pulmonares/química , Enfisema Pulmonar/patología , Estudios de Casos y Controles , Estadísticas no Paramétricas , Pulmón/patología
10.
J Environ Pathol Toxicol Oncol ; 13(4): 221-6, 1994.
Artículo en Inglés | MEDLINE | ID: mdl-7658330

RESUMEN

The mutagenicity of some hexahydrophenanthrenes and their corresponding arene oxides was assayed in histidine-dependent mutants of Salmonella typhimurium TA98 and TA100. All the arene epoxides examined were devoid of mutagenic activity, although some of them could alkylate nicotinamide. By contrast, the 1,2,3,9,10, 10a-hexahydrophenanthrene, trans-1,2,3,4,4a,10a-hexahydrophenanthrene, 9-methyl-, 6-methoxy-trans-1,2,3,4,4a,10a-hexahydrophenanthrene, 7-bromo-trans-1,2,3,4,4a,10a-hexahydrophenanthrene and 9-methyl-trans-1,2,3,4,4a,10a-hexahydrophenanthrene were active as mutagens in the presence of S9 mix. A negative result was obtained with octahydrophenanthrene, suggesting that the benzylic double bond is a prerequisite for the mutagenic activities of hexahydrophenanthrenes. Thus, probably a very reactive intermediate (aryloxirane) formed by a secondary metabolism following the primary oxidation of the benzylic double bond by S9 mix could be responsible for the mutagenicity of the hexahydrophenanthrenes.


Asunto(s)
Mutágenos/toxicidad , Fenantrenos/toxicidad , Compuestos Epoxi/metabolismo , Compuestos Epoxi/toxicidad , Pruebas de Mutagenicidad , Fenantrenos/metabolismo , Salmonella typhimurium
11.
Eur Respir J ; 7(1): 17-22, 1994 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-8143818

RESUMEN

The purpose of this study was to evaluate whether chronic heart failure (CHF) may induce changes in breathing pattern and ventilatory neural drive. We studied 45 male inpatients with CHF, (25 patients in NYHA class II, 20 in class III) and 22 sex-matched post myocardial infarction patients without left ventricular dysfunction who served as controls. CHF patients underwent right heart catheterization and assessment of cardiac output by thermodilution technique. Patients and controls underwent evaluation of left ventricular ejection fraction by 2D echocardiography, spirometry, diffusion capacity, blood gases, breathing pattern, mouth occlusion pressure and respiratory muscle strength determination. Results of CHF patients were compared to controls and evaluated for differences according to the degree in severity of functional impairment. CHF patients showed a slight reduction in lung volumes and in diffusion capacity. In CHF neural drive, as assessed by mouth occlusion pressure (P0.1), was significantly increased in comparison to controls (P0.1 = 1.86 (0.7) and 1.4 (0.6) cmH2O in CHF and controls respectively). Analysis of breathing pattern showed only a slight yet significant increase in respiratory frequency while respiratory muscle strength, as assessed by measurement of maximal inspiratory and expiratory pressures (MIP and MEP respectively) was slightly reduced (MIP = 79(27) and 104(28); MEP = 111(32) and 142(33) cmH2O respectively). Observed changes were more relevant in patients with advanced NYHA functional classes whereas no relationship among indices of cardiac and respiratory function was found. We conclude that chronic heart failure induces changes in neural ventilatory drive and respiratory muscle strength related to the severity of the disease.


Asunto(s)
Insuficiencia Cardíaca/fisiopatología , Respiración/fisiología , Músculos Respiratorios/fisiopatología , Gasto Cardíaco , Enfermedad Crónica , Humanos , Mediciones del Volumen Pulmonar , Masculino , Persona de Mediana Edad , Capacidad de Difusión Pulmonar/fisiología
12.
Thorax ; 48(7): 702-7, 1993 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-8153917

RESUMEN

BACKGROUND: A study was undertaken to determine the level of recruitment of the muscles used in the generation of respiratory muscle force, and to ascertain whether maximal diaphragmatic force and maximal inspiratory muscle force need to be measured by separate tests. The level of activity of three inspiratory muscles and one expiratory muscle during three maximal respiratory manoeuvres was studied: (1) maximal inspiration against a closed airway (Muller manoeuvre or maximal inspiratory pressure (MIP)); (2) maximal inspired manoeuvre followed by a maximal expiratory effort (combined manoeuvre); and (3) maximal inspiratory sniff through the nose (sniff manoeuvre). METHODS: All the manoeuvres were performed from functional residual capacity. The gastric (PGA) and oesophageal (POES) pressures and their difference, transdiaphragmatic pressure (PDI), and the integrated EMG activity of the diaphragm (EDI), the sternomastoid (ESTR), the intercostal parasternals (ERIC), and the rectus abdominis muscles (ERA) were recorded. RESULTS: Mean (SD) PDI values for the Muller, combined, and sniff manoeuvres were: 127.6 (19.4), 162.7 (22.2), and 136.6 (24.8) cm H2O, respectively. The pattern of rib cage muscle recruitment (POES/PDI) was similar for the Muller and sniff manoeuvres (88% and 80% respectively), and was 58% in the combined manoeuvre, confirming data previously reported in the literature. Peak EDI amplitude was greater during the sniff manoeuvre in all subjects (100%) than during the combined (88.1%) and Muller (61.1%) manoeuvres. ESTR and EIC were more active in the Muller and the sniff manoeuvres. The contribution of the expiratory muscle (ERA) to the three manoeuvres was 100% in the combined, 26.1% for the sniff, and 11.5% for the Muller manoeuvre. CONCLUSIONS: Each of these three manoeuvres results in different mechanisms of inspiratory and expiratory muscle activation and the intrathoracic and intra-abdominal pressures generated are a reflection of the interaction between the various muscle groups. The Muller and sniff manoeuvres reflect mainly the force of the inspiratory muscles and the combined manoeuvre that of the diaphragm.


Asunto(s)
Reclutamiento Neurofisiológico , Respiración/fisiología , Músculos Respiratorios/fisiología , Adulto , Diafragma/fisiología , Electromiografía , Esófago/fisiología , Humanos , Presión , Estómago/fisiología
13.
Monaldi Arch Chest Dis ; 48(1): 16-22, 1993.
Artículo en Inglés | MEDLINE | ID: mdl-8472057

RESUMEN

It has been shown that chronic oral steroid therapy (ST) does not induce respiratory muscle dysfunction in normal and asthmatic subjects. As corticosteroids are sometimes chronically used in the treatment of the patients with chronic obstructive pulmonary disease (COPD), the aim of our study was to verify whether ST could cause respiratory muscle impairment and, since ST also affects the central nervous system, whether ST could influence the ventilatory pattern. We retrospectively studied 12 COPD patients (group A), on long-term therapy (for at least 4 consecutive months, range 4-18 months) with an oral steroid, deflazacort, 15 mg.d-1. The subjects were strictly matched, with regard to age, sex, height, weight, forced expiratory volume in one second (FEV1), residual volume (RV), arterial oxygen tension (PaCO2), arterial carbon dioxide tension (PaCO2) and pH, with 12 COPD patients (Group B) who had never taken oral steroids. To assess respiratory muscle strength, we measured maximal inspiratory (MIP) and expiratory (MEP) pressures, while mouth occlusion pressure (P0.1) was employed to assess neuromuscular drive; ventilatory pattern and airway impedence were also evaluated. Effectiveness of ST was confirmed by the plasmatic levels of endogenous cortisol. No significant differences were observed between the two groups with regard to MIP (A 72.2 +/- 9.7 vs B: 70 +/- 7.2 cmH2O) and MEP (A 91.6 +/- 10.5 vs B 94.4 +/- 7.6 cmH2O) whilst P0.1 was significantly higher in group A (2.6 +/- 0.3 cmH2O) than in group B (1.8 +/- 0.1 cmH2O). No significant differences were found among all the ventilatory parameters, but the impedence was significantly higher in group A.(ABSTRACT TRUNCATED AT 250 WORDS)


Asunto(s)
Corticoesteroides/administración & dosificación , Mecánica Respiratoria/efectos de los fármacos , Músculos Respiratorios/efectos de los fármacos , Administración Oral , Corticoesteroides/efectos adversos , Anciano , Humanos , Enfermedades Pulmonares Obstructivas/tratamiento farmacológico , Enfermedades Pulmonares Obstructivas/epidemiología , Enfermedades Pulmonares Obstructivas/fisiopatología , Persona de Mediana Edad , Pruebas de Función Respiratoria , Mecánica Respiratoria/fisiología , Músculos Respiratorios/fisiopatología , Estudios Retrospectivos , Factores de Tiempo
14.
Chest ; 101(1): 133-40, 1992 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-1345900

RESUMEN

The effect of broxaterol, a new beta 2-agonist, on respiratory muscle endurance and strength was studied in a double-blind, placebo-controlled, randomized crossover clinical trial in 16 patients with chronic obstructive pulmonary disease (COPD) with irreversible airway obstruction (FEV1 = 57.1 percent of predicted). One patient withdrew from the study because of acute respiratory exacerbation. Inspiratory muscle strength was assessed by maximal inspiratory pressure (MIP) and endurance time was determined as the length of time a subject could breathe against inspiratory resistance (target mouth pressure = 70 percent of MIP, Ti/Ttot = 0.4). Broxaterol (B) or placebo (P) was given orally for seven days at the dose of 0.5 mg three times a day with a washout period of 72 h between study treatments. Measurements were performed before administration of B or P and 2 h (six patients) or 8 h (nine patients) after the end of each treatment. No significant changes in FEV1 or FRC were observed after B or P suggesting that diaphragmatic length was maintained constant with each treatment. The MIP did not significantly change, while endurance time increased after B in the patients tested at 2 h (from 234.8 +/- 48.1 s to 284.0 +/- 48.0 s, p less than 0.05) and at 8 h (from 187.2 +/- 31.1 s to 258.2 +/- 40.4 s, p less than 0.005). No changes were observed after P. Minute ventilation, airway occlusion pressure (P0.1), integrated electromyographic activities of the diaphragm (Edi), and intercostal parasternals (Eic) (normalized to the value obtained during MIP) showed no change during the endurance run with different treatments. We conclude that in a group of COPD patients with irreversible airway obstruction, B significantly improves respiratory muscle endurance, and that this does not arise as a result of an effect on neuromuscular drive or pulmonary mechanics, but may be mediated by peripheral factors.


Asunto(s)
Agonistas Adrenérgicos beta/uso terapéutico , Isoxazoles/uso terapéutico , Enfermedades Pulmonares Obstructivas/tratamiento farmacológico , Músculos Respiratorios/fisiopatología , Agonistas Adrenérgicos beta/efectos adversos , Agonistas Adrenérgicos beta/farmacocinética , Anciano , Dióxido de Carbono/sangre , Método Doble Ciego , Humanos , Isoxazoles/efectos adversos , Isoxazoles/farmacocinética , Enfermedades Pulmonares Obstructivas/sangre , Enfermedades Pulmonares Obstructivas/fisiopatología , Persona de Mediana Edad , Contracción Muscular/efectos de los fármacos , Oxígeno/sangre , Mecánica Respiratoria/efectos de los fármacos , Músculos Respiratorios/efectos de los fármacos
15.
J Med Chem ; 24(5): 525-32, 1981 May.
Artículo en Inglés | MEDLINE | ID: mdl-7241510

RESUMEN

The (E)- and (Z)-m-(trifluoromethyl)-alpha, beta-dimethylcinnamamides and some of their N-alkyl derivatives were prepared and pharmacologically tested as anticonvulsant agents in order to verify if a ring substituent, like the m-CF3 group, different from a halogen but possessing the same electronic effect could lead to equally active compounds. Some (E)-m-(trifluoromethyl)-alpha-methyl- and -non-methyl-substituted-cinnamamides were also prepared and tested. In the alpha, beta-dimethyl series the results show that the m-CF3 group leads to products more active than the ones unsubstituted on the phenyl ring but still less active than the p-halogen-substituted compounds previously studied. In the alpha-methyl and non-methyl-substituted series, the trend shows the m-CF3 group being able to produce less toxic and, in some cases, more active products than the previously studied amides.


Asunto(s)
Anticonvulsivantes/síntesis química , Cinamatos/síntesis química , Animales , Fenómenos Químicos , Química , Cinamatos/farmacología , Masculino , Ratones , Estereoisomerismo , Relación Estructura-Actividad
16.
J Med Chem ; 22(6): 738-41, 1979 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-37340

RESUMEN

A series of 1-(p-nitrophenyl)-2-aminoethanol derivatives and their morpholine analogues have been synthesized and pharmacologically investigated in order to confirm some pharmacological observations made with the N-isopropyl-substituted compounds. In agreement with the previously obtained results, the weak alpha-adrenergic-stimulating activity and the potentiating effect on the responses to norepinephrine found in the open-chain compounds persist in their corresponding semirigid cyclic analogues. The results are discussed in the light of common knowledge of the structure-activity relationships of alpha-adrenergic drugs.


Asunto(s)
Morfolinas/farmacología , Antagonistas Adrenérgicos alfa/farmacología , Animales , Interacciones Farmacológicas , Técnicas In Vitro , Masculino , Conformación Molecular , Morfolinas/síntesis química , Contracción Muscular/efectos de los fármacos , Músculo Liso/efectos de los fármacos , Norepinefrina/farmacología , Ratas , Relación Estructura-Actividad , Conducto Deferente/efectos de los fármacos
17.
J Med Chem ; 20(1): 48-53, 1977 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-833825

RESUMEN

Several (E)- and (Z)-N-alkyl-alpha,beta-dimethylcinnamamides variously substituted on the phenyl group were synthesized from their corresponding acids and characterized through their NMR spectra. The compounds were tested to determine the relationship existing between their action on the CNS and the activity exhibited by the corresponding amides unsubstituted on the phenyl, previously studied. Substitution with the same group always had the same effects on the biological activity of the (E)-N-alkyl-alpha,beta-dimethylcinnamamides selected; these effects mainly regarded anticonvulsant activity which is the most noteworthy action of these compounds. This activity was reduced by electron-donating substituents and increased by electron-withdrawing ones. In the Z series the p-phenyl substitution with a halogen reduced or suppressed the CNS stimulant activity exhibited by the parent compounds.


Asunto(s)
Amidas/síntesis química , Cinamatos/síntesis química , Alquilación , Amidas/farmacología , Animales , Anticonvulsivantes/síntesis química , Conducta Animal/efectos de los fármacos , Cinamatos/farmacología , Evaluación de Medicamentos , Espectroscopía de Resonancia Magnética , Metilación , Ratones , Relación Estructura-Actividad , Temblor/prevención & control
19.
J Med Chem ; 18(8): 842-6, 1975 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-1159703

RESUMEN

Two series of (E)- and (Z)-N-alkyl-alpha,beta-dimethylcinnamamide derivatives were prepared and the biological activity of these compounds was investigated in a series of pharmacological tests. All compounds tested had clear activity on the CNS; generally, this was depressant with E isomers, while Z isomers always caused marked stimulation (tremors and convulsions). Some of the E isomers also had a clear-cut anticonvulsant activity as shown by the antagonistic effect on pentylenetetrazole-induced seizures in the mouse. The NMR spectra of these compounds, which confirm their configurations, are discussed.


Asunto(s)
Cinamatos/síntesis química , Amidas/síntesis química , Amidas/farmacología , Amidas/toxicidad , Animales , Anticonvulsivantes/síntesis química , Conducta Animal/efectos de los fármacos , Sistema Nervioso Central/efectos de los fármacos , Cinamatos/farmacología , Cinamatos/toxicidad , Depresión Química , Femenino , Dosificación Letal Mediana , Espectroscopía de Resonancia Magnética , Masculino , Ratones , Actividad Motora/efectos de los fármacos , Pentilenotetrazol/antagonistas & inhibidores , Estereoisomerismo , Relación Estructura-Actividad
20.
J Med Chem ; 18(8): 836-8, 1975 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-1174140

RESUMEN

2-(p-Nitrophenyl)-4-isopropylmorphine (V), an analog of 1-(p-nitrophenyl)-2-isopropylaminoethanol (INPEA, I) in which the OCHCHN chain of I is locked in a morpholine ring, loses the beta-receptor blocking activity of I on various isolated preparations. The same ineffectiveness is observed in the O-methyl (II), N-methyl (III), and N,O-dimethyl analog (IV) of I. However, some other properties which are present in I, such as inhibitory effect on acetylcholine or on 5-HT, intrinsic alpha-sympathomimetic activity, and potentiation of catecholamines, are maintained; this demonstrates a complete dissociation of these effects from beta-receptor blockade. The interactions with the alpha-adrenoceptors and with the uptake mechanism are discussed on the basis of the structure-activity relationship between I and its analogs II-V.


Asunto(s)
Etanolaminas/síntesis química , Morfolinas/síntesis química , Animales , Colon/efectos de los fármacos , Ciclización , Estimulación Eléctrica , Etanolaminas/análogos & derivados , Etanolaminas/farmacología , Cobayas , Atrios Cardíacos/efectos de los fármacos , Frecuencia Cardíaca/efectos de los fármacos , Técnicas In Vitro , Masculino , Conformación Molecular , Morfolinas/farmacología , Contracción Muscular/efectos de los fármacos , Músculo Liso/efectos de los fármacos , Ratas , Receptores Adrenérgicos/efectos de los fármacos , Relación Estructura-Actividad , Conducto Deferente/efectos de los fármacos
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