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[PMID]:28076656
[Au] Autor:Kirkland SW; Vandenberghe C; Voaklander B; Nikel T; Campbell S; Rowe BH
[Ad] Endereço:Department of Emergency Medicine, University of Alberta, Edmonton, AB, Canada.
[Ti] Título:Combined inhaled beta-agonist and anticholinergic agents for emergency management in adults with asthma.
[So] Source:Cochrane Database Syst Rev;1:CD001284, 2017 01 11.
[Is] ISSN:1469-493X
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Inhaled short-acting anticholinergics (SAAC) and short-acting beta2-agonists (SABA) are effective therapies for adult patients with acute asthma who present to the emergency department (ED). It is unclear, however, whether the combination of SAAC and SABA treatment is more effective in reducing hospitalisations compared to treatment with SABA alone. OBJECTIVES: To conduct an up-to-date systematic search and meta-analysis on the effectiveness of combined inhaled therapy (SAAC + SABA agents) vs. SABA alone to reduce hospitalisations in adult patients presenting to the ED with an exacerbation of asthma. SEARCH METHODS: We searched MEDLINE, Embase, CINAHL, SCOPUS, LILACS, ProQuest Dissertations & Theses Global and evidence-based medicine (EBM) databases using controlled vocabulary, natural language terms, and a variety of specific and general terms for inhaled SAAC and SABA drugs. The search spanned from 1946 to July 2015. The Cochrane Airways Group provided search results from the Cochrane Airways Group Register of Trials which was most recently conducted in July 2016. An extensive search of the grey literature was completed to identify any other potentially relevant studies. SELECTION CRITERIA: Included studies were randomised or controlled clinical trials comparing the effectiveness of combined inhaled therapy (SAAC and SABA) to SABA treatment alone to prevent hospitalisations in adults with acute asthma in the emergency department. Two independent review authors assessed studies for inclusion using pre-determined criteria. DATA COLLECTION AND ANALYSIS: For dichotomous outcomes, we calculated individual and pooled statistics as risk ratios (RR) or odds ratios (OR) with 95% confidence intervals (CI) using a random-effects model and reporting heterogeneity (I²). For continuous outcomes, we reported individual trial results using mean differences (MD) and pooled results as weighted mean differences (WMD) or standardised mean differences (SMD) with 95% CIs using a random-effects model. MAIN RESULTS: We included 23 studies that involved a total of 2724 enrolled participants. Most studies were rated at unclear or high risk of bias.Overall, participants receiving combination inhaled therapy were less likely to be hospitalised (RR 0.72, 95% CI 0.59 to 0.87; participants = 2120; studies = 16; I² = 12%; moderate quality of evidence). An estimated 65 fewer patients per 1000 would require hospitalisation after receiving combination therapy (95% 30 to 95), compared to 231 per 1000 patients receiving SABA alone. Although combination inhaled therapy was more effective than SABA treatment alone in reducing hospitalisation in participants with severe asthma exacerbations, this was not found for participants with mild or moderate exacerbations (test for difference between subgroups P = 0.02).Participants receiving combination therapy were more likely to experience improved forced expiratory volume in one second (FEV1) (MD 0.25 L, 95% CI 0.02 to 0.48; participants = 687; studies = 6; I² = 70%; low quality of evidence), peak expiratory flow (PEF) (MD 36.58 L/min, 95% CI 23.07 to 50.09; participants = 1056; studies = 12; I² = 25%; very low quality of evidence), increased percent change in PEF from baseline (MD 24.88, 95% CI 14.83 to 34.93; participants = 551; studies = 7; I² = 23%; moderate quality of evidence), and were less likely to return to the ED for additional care (RR 0.80, 95% CI 0.66 to 0.98; participants = 1180; studies = 5; I² = 0%; moderate quality of evidence) than participants receiving SABA alone.Participants receiving combination inhaled therapy were more likely to experience adverse events than those treated with SABA agents alone (OR 2.03, 95% CI 1.28 to 3.20; participants = 1392; studies = 11; I² = 14%; moderate quality of evidence). Among patients receiving combination therapy, 103 per 1000 were likely to report adverse events (95% 31 to 195 more) compared to 131 per 1000 patients receiving SABA alone. AUTHORS' CONCLUSIONS: Overall, combination inhaled therapy with SAAC and SABA reduced hospitalisation and improved pulmonary function in adults presenting to the ED with acute asthma. In particular, combination inhaled therapy was more effective in preventing hospitalisation in adults with severe asthma exacerbations who are at increased risk of hospitalisation, compared to those with mild-moderate exacerbations, who were at a lower risk to be hospitalised. A single dose of combination therapy and multiple doses both showed reductions in the risk of hospitalisation among adults with acute asthma. However, adults receiving combination therapy were more likely to experience adverse events, such as tremor, agitation, and palpitations, compared to patients receiving SABA alone.
[Mh] Termos MeSH primário: Agonistas de Receptores Adrenérgicos beta 2/uso terapêutico
Antiasmáticos/uso terapêutico
Asma/tratamento farmacológico
Antagonistas Colinérgicos/uso terapêutico
[Mh] Termos MeSH secundário: Albuterol/uso terapêutico
Atropina/uso terapêutico
Quimioterapia Combinada
Volume Expiratório Forçado/efeitos dos fármacos
Seres Humanos
Ipratrópio/uso terapêutico
Levalbuterol/uso terapêutico
Metaproterenol/uso terapêutico
Ensaios Clínicos Controlados Aleatórios como Assunto
Derivados da Escopolamina/uso terapêutico
[Pt] Tipo de publicação:JOURNAL ARTICLE; META-ANALYSIS; RESEARCH SUPPORT, NON-U.S. GOV'T; REVIEW
[Nm] Nome de substância:
0 (Adrenergic beta-2 Receptor Agonists); 0 (Anti-Asthmatic Agents); 0 (Cholinergic Antagonists); 0 (Scopolamine Derivatives); 53QOG569E0 (Metaproterenol); 7C0697DR9I (Atropine); 8G15T83E6I (oxitropium); EDN2NBH5SS (Levalbuterol); GR88G0I6UL (Ipratropium); QF8SVZ843E (Albuterol)
[Em] Mês de entrada:1704
[Cu] Atualização por classe:170428
[Lr] Data última revisão:
170428
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170112
[St] Status:MEDLINE
[do] DOI:10.1002/14651858.CD001284.pub2


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[PMID]:27751287
[Au] Autor:Dhariwal AK; Sanzgiri PS; Nagvekar V
[Ad] Endereço:DNB Cardiology Trainee, Lilavati Hospital & Research Centre, Bandra, Mumbai, India. Electronic address: aninder.k@gmail.com.
[Ti] Título:High degree atrioventricular block with ventricular asystole in a case of dengue fever.
[So] Source:Indian Heart J;68 Suppl 2:S194-S197, 2016 Sep.
[Is] ISSN:0019-4832
[Cp] País de publicação:India
[La] Idioma:eng
[Ab] Resumo:Cardiac rhythm abnormalities have been uncommonly observed in dengue fever and most of them have been reported in children. We discuss a 30-year-old female with dengue fever, who presented with repeated symptomatic episodes of high degree atrioventricular block with ventricular asystole, which responded to intravenous atropine and oral orciprenaline without recurrence on 6 months follow-up.
[Mh] Termos MeSH primário: Bloqueio Atrioventricular/etiologia
Atropina/administração & dosagem
Dengue/complicações
Parada Cardíaca/etiologia
Ventrículos do Coração/fisiopatologia
Metaproterenol/administração & dosagem
[Mh] Termos MeSH secundário: Administração Oral
Agonistas de Receptores Adrenérgicos beta 2/administração & dosagem
Adulto
Antiarrítmicos/administração & dosagem
Bloqueio Atrioventricular/tratamento farmacológico
Bloqueio Atrioventricular/fisiopatologia
Quimioterapia Combinada
Eletrocardiografia
Feminino
Seguimentos
Parada Cardíaca/tratamento farmacológico
Parada Cardíaca/fisiopatologia
Seres Humanos
Injeções Intravenosas
[Pt] Tipo de publicação:CASE REPORTS; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Adrenergic beta-2 Receptor Agonists); 0 (Anti-Arrhythmia Agents); 53QOG569E0 (Metaproterenol); 7C0697DR9I (Atropine)
[Em] Mês de entrada:1705
[Cu] Atualização por classe:170902
[Lr] Data última revisão:
170902
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161019
[St] Status:MEDLINE


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[PMID]:27032887
[Au] Autor:Bürkle G; Schäfer H; Marschall C; Brugada P; Ehrlich JR
[Ad] Endereço:Cardiology, St Josefs-Hospital, Wiesbaden, Germany.
[Ti] Título:Pharmacological Provocation of Outflow-Tract Tachycardia in a Patient With Brugada Syndrome.
[So] Source:Can J Cardiol;32(12):1577.e5-1577.e7, 2016 Dec.
[Is] ISSN:1916-7075
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:We present a case of a symptomatic patient with Brugada syndrome, who had sustained right ventricular outflow tract tachycardia after pronounced exercise-induced ST segment elevation in V and V . In electrophysiological study he developed right ventricular outflow tract tachycardia provoked by combined infusion of ajmaline and orciprenaline. After ablation no further arrhythmia was provoked by pharmacological stimulation.
[Mh] Termos MeSH primário: Síndrome de Brugada
Ablação por Cateter/métodos
Taquicardia Ventricular
[Mh] Termos MeSH secundário: Ajmalina/administração & dosagem
Ajmalina/efeitos adversos
Antiarrítmicos/administração & dosagem
Antiarrítmicos/efeitos adversos
Síndrome de Brugada/diagnóstico
Síndrome de Brugada/fisiopatologia
Síndrome de Brugada/terapia
Eletrocardiografia/métodos
Sistema de Condução Cardíaco/efeitos dos fármacos
Sistema de Condução Cardíaco/fisiopatologia
Seres Humanos
Masculino
Metaproterenol/administração & dosagem
Metaproterenol/efeitos adversos
Meia-Idade
Estimulação Química
Taquicardia Ventricular/induzido quimicamente
Taquicardia Ventricular/fisiopatologia
Taquicardia Ventricular/prevenção & controle
Resultado do Tratamento
[Pt] Tipo de publicação:CASE REPORTS; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Arrhythmia Agents); 1PON08459R (Ajmaline); 53QOG569E0 (Metaproterenol)
[Em] Mês de entrada:1707
[Cu] Atualização por classe:170720
[Lr] Data última revisão:
170720
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160402
[St] Status:MEDLINE


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[PMID]:26627004
[Au] Autor:Calvano J; Achanzar W; Murphy B; DiPiero J; Hixson C; Parrula C; Burr H; Mangipudy R; Tirmenstein M
[Ad] Endereço:Drug Safety Evaluation, Bristol-Myers Squibb, 1 Squibb Drive, New Brunswick, NJ 08903, United States. Electronic address: Jacqueline.Calvano@bms.com.
[Ti] Título:Evaluation of microRNAs-208 and 133a/b as differential biomarkers of acute cardiac and skeletal muscle toxicity in rats.
[So] Source:Toxicol Appl Pharmacol;312:53-60, 2016 Dec 01.
[Is] ISSN:1096-0333
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Conventional circulating biomarkers of cardiac and skeletal muscle (SKM) toxicity lack specificity and/or have a short half-life. MicroRNAs (miRNAs) are currently being assessed as biomarkers of tissue injury based on their long half-life in blood and selective expression in certain tissues. To assess the utility of miRNAs as biomarkers of cardiac and SKM injury, male Sprague-Dawley rats received a single dose of isoproterenol (ISO); metaproterenol (MET); allylamine (AAM); mitoxantrone (MIT); acetaminophen (APAP) or vehicle. Blood and tissues were collected from rats in each group at 4, 24 and 48h. ISO, MET, and AAM induced cardiac and SKM lesions and APAP induced liver specific lesions. There was no evidence of tissue injury with MIT by histopathology. Serum levels of candidate miRNAs were compared to conventional serum biomarkers of SKM/cardiac toxicity. Increases in heart specific miR-208 only occurred in rats with cardiac lesions alone and were increased for a longer duration than cardiac troponin and FABP3 (cardiac biomarkers). ISO, MET and AAM induced increases in MyL3 and skeletal muscle troponin (sTnl) (SKM biomarkers). MIT induced large increases in sTnl indicative of SKM toxicity, but sTnl levels were also increased in APAP-treated rats that lacked SKM toxicity. Serum levels of miR-133a/b (enriched in cardiac and SKM) increased following ISO, MET, AAM and MIT treatments but were absent in APAP-treated rats. Our results suggest that miR-133a/b are sensitive and specific markers of SKM and cardiac toxicity and that miR-208 used in combination with miR-133a/b can be used to differentiate cardiac from SKM toxicity.
[Mh] Termos MeSH primário: Biomarcadores/sangue
Coração/efeitos dos fármacos
MicroRNAs/sangue
Músculo Esquelético/efeitos dos fármacos
[Mh] Termos MeSH secundário: Acetaminofen/toxicidade
Alilamina/toxicidade
Animais
Isoproterenol/toxicidade
Masculino
Metaproterenol/toxicidade
Mitoxantrona/toxicidade
Ratos
Ratos Sprague-Dawley
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Biomarkers); 0 (MIRN133 microRNA, human); 0 (MIRN208 microRNA, human); 0 (MicroRNAs); 362O9ITL9D (Acetaminophen); 48G762T011 (Allylamine); 53QOG569E0 (Metaproterenol); BZ114NVM5P (Mitoxantrone); L628TT009W (Isoproterenol)
[Em] Mês de entrada:1705
[Cu] Atualização por classe:170523
[Lr] Data última revisão:
170523
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:151203
[St] Status:MEDLINE


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[PMID]:25349222
[Au] Autor:Bollmann A; Hilbert S; John S; Kosiuk J; Hindricks G
[Ad] Endereço:Department of Electrophysiology, Heart Center, Leipzig, Strümpellstr. 39, Leipzig 04289, Germany rhythmo@med.uni-leipzig.de.
[Ti] Título:Insights from preclinical ultra high-density electroanatomical sinus node mapping.
[So] Source:Europace;17(3):489-94, 2015 Mar.
[Is] ISSN:1532-2092
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:AIMS: Although sinus node modification by catheter ablation is an established therapy for the treatment of inappropriate sinus tachycardia, there is incomplete understanding of sinus node anatomy and function but also limited electroanatomical mapping data. Recently, an automatic, ultra high-resolution mapping system has been presented to accurately and quickly identify right atrial (RA) geometry and activation patterns but detailed assessment of sinus node activation has not been performed which was one aim of this study. Preclinical experiences are compared with previous sinus node mapping studies in animals and humans, and potential clinical implications for catheter ablation are discussed. METHODS AND RESULTS: In anaesthetized and ventilated 14 pigs, 30 endocardial and 2 eipcardial RA maps were generated using the Rhythmia™ mapping system without complications and earliest activation sites (EAS) and sinus break-out (SBO) were determined. At baseline, EAS and SBO were located anterior to the middle (n = 6) or lower third (n = 8) of the crista terminalis exhibiting a unicentric activation pattern in all cases. Conduction pathways were directed anterior, posterior, superior, or inferior with substantial inter-individual variation in direction, pathway distance, and conduction time. Orciprenaline, propranolol, or amiodarone shifted endocardial activation with considerable variation between animals with inconsistent patterns. Multicentric activation was found in one case after orciprenaline infusion. Sequential endocardial and epicardial high-density mapping of the RA was performed in two animals and showed a high congruence of the sinus node activation in the endo- and the epicardial map. CONCLUSION: Ultra high-density mapping allows fast, simple, and very detailed assessment of sinus node activation. Future studies are clearly needed to evaluate novel mapping and ablation strategies for an improved understanding of sinus node disease and better outcomes.
[Mh] Termos MeSH primário: Função do Átrio Direito
Mapeamento Epicárdico/métodos
Nó Sinoatrial/fisiologia
[Mh] Termos MeSH secundário: Agonistas de Receptores Adrenérgicos beta 2/farmacologia
Antagonistas Adrenérgicos beta/farmacologia
Amiodarona/farmacologia
Animais
Antiarrítmicos/farmacologia
Técnicas Eletrofisiológicas Cardíacas
Átrios do Coração/efeitos dos fármacos
Metaproterenol/farmacologia
Propranolol/farmacologia
Nó Sinoatrial/efeitos dos fármacos
Suínos
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Adrenergic beta-2 Receptor Agonists); 0 (Adrenergic beta-Antagonists); 0 (Anti-Arrhythmia Agents); 53QOG569E0 (Metaproterenol); 9Y8NXQ24VQ (Propranolol); N3RQ532IUT (Amiodarone)
[Em] Mês de entrada:1512
[Cu] Atualização por classe:150227
[Lr] Data última revisão:
150227
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:141029
[St] Status:MEDLINE
[do] DOI:10.1093/europace/euu276


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[PMID]:24085370
[Au] Autor:Janssens U
[Ad] Endereço:St. Antonius Hospital Eschweiler.
[Ti] Título:[Why isn't orciprenaline approved as antiarrhythmic agent?].
[Ti] Título:Warum ist Orciprenalin nicht mehr als Antiarrhythmikum zugelassen?.
[So] Source:Dtsch Med Wochenschr;138(41):2114, 2013 Oct.
[Is] ISSN:1439-4413
[Cp] País de publicação:Germany
[La] Idioma:ger
[Mh] Termos MeSH primário: Antiarrítmicos/uso terapêutico
Bradicardia/tratamento farmacológico
Aprovação de Drogas/legislação & jurisprudência
Metaproterenol/uso terapêutico
[Mh] Termos MeSH secundário: Antiarrítmicos/efeitos adversos
Atropina/uso terapêutico
Relação Dose-Resposta a Droga
Epinefrina/efeitos adversos
Epinefrina/uso terapêutico
Alemanha
Seres Humanos
Metaproterenol/efeitos adversos
Uso Off-Label/legislação & jurisprudência
[Pt] Tipo de publicação:LETTER
[Nm] Nome de substância:
0 (Anti-Arrhythmia Agents); 53QOG569E0 (Metaproterenol); 7C0697DR9I (Atropine); YKH834O4BH (Epinephrine)
[Em] Mês de entrada:1311
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:131003
[St] Status:MEDLINE
[do] DOI:10.1055/s-0033-1349546


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[PMID]:23920058
[Au] Autor:Brunelli M; Raffa S; Große A; Hanazawa K; Sammut M; Roos M; Frommhold M; Wauters K; Geller JC
[Ad] Endereço:Zentralklinik Bad Berka, Arrhythmia and Electrophysiology Section, Division of Cardiology, Germany; Department of Internal Medicine, Division of Cardiology, University of Genova, Italy. Electronic address: michele.brunelli@zentralklinik.de.
[Ti] Título:Residual conduction after pulmonary vein isolation with a circular multielectrode radiofrequency ablation catheter: the role of adenosine and orciprenalin during a prolonged observation time.
[So] Source:Int J Cardiol;168(4):4122-31, 2013 Oct 09.
[Is] ISSN:1874-1754
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:INTRODUCTION: Recurrences after pulmonary vein isolation (PVI) in patients (pts) with paroxysmal atrial fibrillation (AF) are mostly due to PV reconnection. The effect of adenosine, orciprenalin and their combination on left atrial PV conduction after PVI with a phased radiofrequency (RF) circular multielectrode ablation catheter (Pulmonary Vein Ablation Catheter, PVAC) was prospectively evaluated during a prolonged waiting time. In addition, it was assessed whether pharmacological reconnection characterizes veins requiring use of an irrigated catheter. METHODS AND RESULTS: In 116 consecutive pts [age 62 (IQR:52,68) years, 46% female], PVI was achieved with the PVAC alone in 114/116 (98%) pts and 461/464 (99%) veins after a median of 26 (IQR:22,32) applications delivering 1782 s (IQR:1518,2197) of RF. Mostly transient PV reconnections were observed in 40/116 (34%) pts and 57/464 (12%) PVs, a median of 44 (IQR:30,58) min after initial isolation. Adenosine, alone (43/57, 75%) or during orciprenalin infusion (7/57, 12%), unmasked residual conduction in the majority of veins (50/57, 88%). Additional PVAC applications less frequently achieved permanent isolation in veins showing reconnection compared to those that didn't (52/57, 91% vs. 404/407, 99%; P < .001). All PVs that could not be isolated with the PVAC were successfully treated with a standard irrigated catheter. CONCLUSIONS: After apparent PVI with the PVAC, drug-challenge after prolonged observation unmasked residual PV conduction in a significant number of pts, and adenosine was the most effective strategy. Drug-induced PV reconnection was difficult to treat with the PVAC. Whether this strategy improves clinical outcome of PVI with phased RF needs to be investigated.
[Mh] Termos MeSH primário: Adenosina/administração & dosagem
Fibrilação Atrial/tratamento farmacológico
Fibrilação Atrial/cirurgia
Ablação por Cateter/métodos
Metaproterenol/administração & dosagem
Veias Pulmonares/cirurgia
[Mh] Termos MeSH secundário: Idoso
Fibrilação Atrial/diagnóstico
Quimioterapia Combinada
Feminino
Seres Humanos
Infusões Intravenosas
Masculino
Meia-Idade
Estudos Prospectivos
Veias Pulmonares/patologia
Fatores de Tempo
Resultado do Tratamento
[Pt] Tipo de publicação:JOURNAL ARTICLE; OBSERVATIONAL STUDY; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
53QOG569E0 (Metaproterenol); K72T3FS567 (Adenosine)
[Em] Mês de entrada:1501
[Cu] Atualização por classe:131021
[Lr] Data última revisão:
131021
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:130808
[St] Status:MEDLINE


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[PMID]:23270716
[Au] Autor:Moteki H; Kimura M; Sunaga K; Tsuda T; Ogihara M
[Ad] Endereço:Department of Clinical Pharmacology, Faculty of Pharmaceutical Sciences, Josai University, 1-1 Keyakidai, Sakado, Saitama 350-0295, Japan.
[Ti] Título:Signal transduction mechanism for potentiation by α1- and ß2-adrenoceptor agonists of L-ascorbic acid-induced DNA synthesis and proliferation in primary cultures of adult rat hepatocytes.
[So] Source:Eur J Pharmacol;700(1-3):2-12, 2013 Jan 30.
[Is] ISSN:1879-0712
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:We investigated the effects of α- and ß-adrenoceptor agonists on L-ascorbic acid-induced hepatocyte DNA synthesis and proliferation in primary cultures of adult rat hepatocytes. The results showed that phenylephrine (10(-6) M) and metaproterenol (10(-6) M) alone did not induce hepatocyte DNA synthesis and proliferation. However, when combined with L-ascorbic acid (10(-6) M), these adrenoceptor agonists potentiated the hepatocyte DNA synthesis and proliferation induced by L-ascorbic acid. Then intracellular signal transduction mechanisms for the effects of phenylephrine and metaproterenol on L-ascorbic acid-induced hepatocyte mitogenesis were examined. Western blot analysis showed that phenylephrine and metaproterenol did not potentiate L-ascorbic acid-induced insulin-like growth factor I receptor tyrosine kinase phosphorylation. In contrast, they both significantly potentiated L-ascorbic acid-induced extracellular-signal regulated kinase-2 (ERK2) phosphorylation within 5 min. Moreover, cell-permeable second messenger analogs phorbol ester (10(-7) M) and 8-bromo cAMP (10(-7) M) mimicked the effects of phenylephrine and metaproterenol on L-ascorbic acid-induced ERK2 phosphorylation. The effects of these adrenoceptor agents were specifically antagonized by GF109203X and H-89, respectively. These results indicate that activation of ERK2 via protein kinas C and protein kinase A represents a mechanism for potentiation of L-ascorbic acid-induced hepatocyte DNA synthesis and proliferation in primary cultures of adult rat hepatocytes.
[Mh] Termos MeSH primário: Ácido Ascórbico/farmacologia
DNA/biossíntese
Hepatócitos/citologia
Hepatócitos/efeitos dos fármacos
Receptores Adrenérgicos alfa 1/metabolismo
Receptores Adrenérgicos beta 2/metabolismo
Transdução de Sinais/efeitos dos fármacos
[Mh] Termos MeSH secundário: 8-Bromo Monofosfato de Adenosina Cíclica/farmacologia
Agonistas de Receptores Adrenérgicos alfa 1/farmacologia
Agonistas de Receptores Adrenérgicos beta 2/farmacologia
Animais
Proliferação Celular/efeitos dos fármacos
Células Cultivadas
Sinergismo Farmacológico
MAP Quinases Reguladas por Sinal Extracelular/metabolismo
Hepatócitos/metabolismo
Masculino
Metaproterenol/farmacologia
Fenilefrina/farmacologia
Fosforilação/efeitos dos fármacos
Ratos
Ratos Wistar
Receptor IGF Tipo 1/metabolismo
Acetato de Tetradecanoilforbol/farmacologia
Fatores de Tempo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Adrenergic alpha-1 Receptor Agonists); 0 (Adrenergic beta-2 Receptor Agonists); 0 (Receptors, Adrenergic, alpha-1); 0 (Receptors, Adrenergic, beta-2); 1WS297W6MV (Phenylephrine); 23583-48-4 (8-Bromo Cyclic Adenosine Monophosphate); 53QOG569E0 (Metaproterenol); 9007-49-2 (DNA); EC 2.7.10.1 (Receptor, IGF Type 1); EC 2.7.11.24 (Extracellular Signal-Regulated MAP Kinases); NI40JAQ945 (Tetradecanoylphorbol Acetate); PQ6CK8PD0R (Ascorbic Acid)
[Em] Mês de entrada:1308
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:121229
[St] Status:MEDLINE


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[PMID]:22817559
[Au] Autor:Bosak A; Gazic Smilovic I; Sinko G; Vinkovic V; Kovarik Z
[Ad] Endereço:Institute for Medical Research and Occupational Health , Ksaverska cesta 2, HR-10000 Zagreb, Croatia.
[Ti] Título:Metaproterenol, isoproterenol, and their bisdimethylcarbamate derivatives as human cholinesterase inhibitors.
[So] Source:J Med Chem;55(15):6716-23, 2012 Aug 09.
[Is] ISSN:1520-4804
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Metaproterenol and isoproterenol are bronchodilators that provide a structural basis for many other bronchodilators currently in use. One of these structurally related bronchodilators is terbutaline; it is administered as a prodrug, bambuterol, and is metabolized (bioconverted) into terbutaline by butyrylcholinesterase (BChE). The metabolism rate can be affected by BChE gene polymorphism in the human population and BChE stereoselectivity. The aim of our study was to investigate inhibition of human BChE and acetylcholinesterase (AChE) with metaproterenol, isoproterenol, and newly synthesized racemic bisdimethylcarbamate derivatives of metaproterenol (metacarb) and isoproterenol (isocarb) and their (R)-enantiomers to see if their bioconversion is affected by BChE inhibition in the same way as that for bambuterol. Metacarb and isocarb proved to be selective BChE inhibitors, as they progressively inhibited AChE 960 to 80 times more slowly than BChE(UU). All studied cholinesterases displayed poor affinity for metaproterenol and isoproterenol, yet BChE(UU) had an affinity about five times higher than that of AChE.
[Mh] Termos MeSH primário: Carbamatos/química
Inibidores da Colinesterase/química
Isoproterenol/análogos & derivados
Isoproterenol/química
Metaproterenol/análogos & derivados
Metaproterenol/química
[Mh] Termos MeSH secundário: Acetilcolinesterase/química
Butirilcolinesterase/química
Carbamatos/síntese química
Inibidores da Colinesterase/síntese química
Ensaios Enzimáticos
Seres Humanos
Isoproterenol/síntese química
Metaproterenol/síntese química
Modelos Moleculares
Estereoisomerismo
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Carbamates); 0 (Cholinesterase Inhibitors); 53QOG569E0 (Metaproterenol); EC 3.1.1.7 (Acetylcholinesterase); EC 3.1.1.8 (Butyrylcholinesterase); L628TT009W (Isoproterenol)
[Em] Mês de entrada:1211
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:120724
[St] Status:MEDLINE
[do] DOI:10.1021/jm300289k


  10 / 1493 MEDLINE  
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[PMID]:22592732
[Au] Autor:Fedorowicz Z; Nasser M; Jagannath VA; Beaman JH; Ejaz K; van Zuuren EJ
[Ad] Endereço:UKCC (Bahrain Branch), College of Medicine, AMA International University of Bahrain, Awali, Bahrain.. zbysfedo@batelco.com.bh
[Ti] Título:Beta2-adrenoceptor agonists for dysmenorrhoea.
[So] Source:Cochrane Database Syst Rev;(5):CD008585, 2012 May 16.
[Is] ISSN:1469-493X
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Dysmenorrhoea is a common gynaecological complaint that can affect as many as 50% of premenopausal women, 10% of whom suffer severely enough to be rendered incapacitated for one to three days during each menstrual cycle. Primary dysmenorrhoea is where women suffer from menstrual pain but lack any pathology in their pelvic anatomy. Beta2-adrenoceptor agonists have been used in the treatment of women with primary dysmenorrhoea but their effects are unclear. OBJECTIVES: To determine the effectiveness and safety of beta2-adrenoceptor agonists in the treatment of primary dysmenorrhoea. SEARCH METHODS: We searched the Cochrane Menstrual Disorders and Subfertility Group Specialised Register; CENTRAL (The Cochrane Library 2011, Issue 8); MEDLINE; EMBASE; PsycINFO and the EBM Reviews databases. The last search was on 22 August 2011. SELECTION CRITERIA: Randomised controlled trials comparing beta2-adrenoceptor agonists with placebo or no treatment, each other or any other conventional treatment in women of reproductive age with primary dysmenorrhoea. DATA COLLECTION AND ANALYSIS: Two review authors independently assessed trial quality and extracted the data. MAIN RESULTS: Five trials involving 187 women with an age range of 15 to 40 years were included. Oral isoxsuprine was compared with placebo in two trials; terbutaline oral spray, ritodrine chloride and oral hydroxyphenyl-orciprenalin were compared with placebo in a further three trials. Clinical diversity in the studies in terms of the interventions being evaluated, assessments at different time points and the use of different assessment tools mitigated against pooling of outcome data across studies in order to provide a summary estimate of effect for any of the comparisons. Only one study, with unclear risk of bias, reported pain relief with a combination of isoxsuprine, acetaminophen and caffeine. None of the other studies reported any significant clinical difference in effectiveness between the intervention and placebo. Adverse effects were reported with all of these medications in up to a quarter of the total number of participants. They included nausea, vomiting, dizziness, quivering, tremor and palpitations. AUTHORS' CONCLUSIONS: The evidence presented in this review was based on a few relatively small-sized studies that were categorised to have unclear to high risk of bias, which does not allow confident decision-making at present about the use of beta2-adrenoceptor agonists for dysmenorrhoea. The benefits as reported in one study should be balanced against the wide array of unacceptable side effects documented with this class of medication. We have emphasised the lack of precision and limitations in the reported data where appropriate.
[Mh] Termos MeSH primário: Agonistas de Receptores Adrenérgicos beta 2/uso terapêutico
Dismenorreia/tratamento farmacológico
[Mh] Termos MeSH secundário: Acetaminofen/uso terapêutico
Adolescente
Adulto
Cafeína/uso terapêutico
Feminino
Seres Humanos
Isoxsuprina/uso terapêutico
Metaproterenol/análogos & derivados
Metaproterenol/uso terapêutico
Ensaios Clínicos Controlados Aleatórios como Assunto
Ritodrina/uso terapêutico
Terbutalina/uso terapêutico
Adulto Jovem
[Pt] Tipo de publicação:JOURNAL ARTICLE; META-ANALYSIS; RESEARCH SUPPORT, NON-U.S. GOV'T; REVIEW
[Nm] Nome de substância:
0 (Adrenergic beta-2 Receptor Agonists); 22574-01-2 (hydroxyphenylorciprenaline); 362O9ITL9D (Acetaminophen); 3G6A5W338E (Caffeine); 53QOG569E0 (Metaproterenol); I0Q6O6740J (Ritodrine); N8ONU3L3PG (Terbutaline); R15UI3245N (Isoxsuprine)
[Em] Mês de entrada:1208
[Cu] Atualização por classe:160602
[Lr] Data última revisão:
160602
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:120518
[St] Status:MEDLINE
[do] DOI:10.1002/14651858.CD008585.pub2



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