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[PMID]:29342497
[Au] Autor:El-Sayeh HG; Rathbone J; Soares-Weiser K; Bergman H
[Ad] Endereço:Harrogate District Hospital, Tees, Esk & Wear Valleys NHS Foundation Trust, Briary Wing, Lancaster Park Road, Harrogate, North Yorkshire, UK, HG2 7SX.
[Ti] Título:Non-antipsychotic catecholaminergic drugs for antipsychotic-induced tardive dyskinesia.
[So] Source:Cochrane Database Syst Rev;1:CD000458, 2018 01 18.
[Is] ISSN:1469-493X
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Tardive dyskinesia (TD) is a disabling movement disorder associated with the prolonged use of antipsychotic medication. Several strategies have been examined in the treatment of TD. Currently, however, there is no clear evidence of the effectiveness of these drugs in TD and they have been associated with many side effects. One particular strategy would be to use pharmaceutical agents which are known to influence the catecholaminergic system at various junctures. OBJECTIVES: 1. To determine the effects of any of the following drugs for antipsychotic-induced TD in people with schizophrenia or other chronic mental illnesses.i. Drugs which influence the noradrenergic system.ii. Dopamine receptor agonists.iii. Dopamine receptor antagonists.iv. Dopamine-depletor drugs.v. Drugs that increase the production or release of dopamine.2. To examine whether any improvement occurred with short periods of intervention (less than 6 weeks) and, if this did occur, whether this effect was maintained at longer periods of follow-up.3. To examine if there was a differential effect for the various compounds.4. To examine whether the use of non-antipsychotic catecholaminergic drugs are most effective in those with more recent onset TD (less than five years). SEARCH METHODS: We retrieved 712 references from searching the Cochrane Schizophrenia Group Trials Register (July 2015 and April 2017). We also inspected references of all identified studies for further trials and contacted authors of trials for additional information. SELECTION CRITERIA: We selected studies if they were randomised controlled trials focusing on people with schizophrenia or other chronic mental illnesses and antipsychotic-induced tardive dyskinesia. We compared the use of catecholaminergic interventions versus placebo, no intervention, or any other intervention for the treatment of antipsychotic-induced tardive dyskinesia. DATA COLLECTION AND ANALYSIS: We independently extracted data from these trials and we estimated risk ratios (RRs) with 95% confidence intervals (CIs). We assumed that people who left the studies early had no improvement. MAIN RESULTS: There are 10 included trials (N = 261) published between 1973 and 2010; eight are new from the 2015 and 2017 update searches. Forty-eight studies are excluded. Participants were mostly chronically mentally ill inpatients in their 50s, and studies were primarily of short (2 to 6 weeks) duration. The overall risk of bias in these studies was unclear, mainly due to poor reporting of allocation concealment and generation of the sequence. Studies were also not clearly blinded and we are unsure if data are incomplete or selectively reported, or if other biases were operating.One small, three-arm trial found that both alpha-methyldopa (N = 20; RR 0.33, 95% CI 0.14 to 0.80; low-quality evidence) and reserpine (N = 20; RR 0.52 95% CI 0.29 to 0.96; low-quality evidence) may lead to a clinically important improvement in tardive dyskinesia symptoms compared with placebo after 2 weeks' treatment, but found no evidence of a difference between alpha-methyldopa and reserpine (N = 20; RR 0.60, 95% CI 0.19 to 1.86; very low quality evidence). Another small trial compared tetrabenazine and haloperidol after 18 weeks' treatment and found no evidence of a difference on clinically important improvement in tardive dyskinesia symptoms (N = 13; RR 0.93, 95% CI 0.45 to 1.95; very low quality evidence). No study reported on adverse events.For remaining outcomes there was no evidence of a difference between any of the interventions: alpha-methyldopa versus placebo for deterioration of tardive dyskinesia symptoms (1 RCT; N = 20; RR 0.33, 95% CI 0.02 to 7.32; very low quality evidence), celiprolol versus placebo for leaving the study early (1 RCT; N = 35; RR 5.28, 95% CI 0.27 to 102.58; very low quality evidence) and quality of life (1 RCT; N = 35; RR 0.87, 95% CI 0.68 to 1.12; very low quality evidence), alpha-methyldopa versus reserpine for deterioration of tardive dyskinesia symptoms (1 RCT; N = 20; not estimable, no reported events; very low quality evidence), reserpine or carbidopa/levodopa versus placebo for deterioration of tardive dyskinesia symptoms (2 RCTs; N = 37; RR 1.18, 95% CI 0.35 to 3.99; very low quality evidence), oxypertine versus placebo for deterioration of mental state (1 RCT; N = 42; RR 2.20, 95% CI 0.22 to 22.45; very low quality evidence), dopaminergic drugs (amantadine, bromocriptine, tiapride, oxypertine, carbidopa/levodopa) versus placebo for leaving the study early (6 RCTs; N = 163; RR 1.29, 95% CI 0.65 to 2.54; very low quality evidence), and tetrabenazine versus haloperidol for deterioration of tardive dyskinesia symptoms (1 RCT; N = 13; RR 1.17, 95% CI 0.09 to 14.92) and leaving the study early (1 RCT; N = 13; RR 0.23, 95% CI 0.01 to 4.00). AUTHORS' CONCLUSIONS: Although there has been a large amount of research in this area, many studies were excluded due to inherent problems in the nature of their cross-over designs. Usually data are not reported before the cross-over and the nature of TD and its likely response to treatments make it imprudent to use this data. The review provides little usable information for service users or providers and more well-designed and well-reported studies are indicated.
[Mh] Termos MeSH primário: Antidiscinéticos/uso terapêutico
Antipsicóticos/efeitos adversos
Discinesia Induzida por Medicamentos/tratamento farmacológico
[Mh] Termos MeSH secundário: Inibidores da Captação Adrenérgica/uso terapêutico
Celiprolol/uso terapêutico
Progressão da Doença
Antagonistas de Dopamina/uso terapêutico
Haloperidol/uso terapêutico
Seres Humanos
Metildopa/uso terapêutico
Ensaios Clínicos Controlados Aleatórios como Assunto
Reserpina/uso terapêutico
Tetrabenazina/uso terapêutico
Cloridrato de Tiapamil/uso terapêutico
[Pt] Tipo de publicação:JOURNAL ARTICLE; META-ANALYSIS; RESEARCH SUPPORT, NON-U.S. GOV'T; REVIEW
[Nm] Nome de substância:
0 (Adrenergic Uptake Inhibitors); 0 (Anti-Dyskinesia Agents); 0 (Antipsychotic Agents); 0 (Dopamine Antagonists); 56LH93261Y (Methyldopa); 8B1QWR724A (Reserpine); DRB57K47QC (Celiprolol); J6292F8L3D (Haloperidol); V824N2T753 (Tiapamil Hydrochloride); Z9O08YRN8O (Tetrabenazine)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180226
[Lr] Data última revisão:
180226
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180118
[St] Status:MEDLINE
[do] DOI:10.1002/14651858.CD000458.pub3


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[PMID]:27417385
[Au] Autor:Bruchatá K; Némethy A; Cizmáriková R; Racanská E; Habala L
[Ad] Endereço:Faculty of Pharmacy, Department of Chemical Theory of Drugs, Comenius University in Bratislava, Bratislava, Slovakia.
[Ti] Título:Synthesis and In Vitro Pharmacological Evaluation of 5-(Alkoxymethyl)-2-(3-alkylamino-2-hydroxypropoxy)phenylethanones Related to Acebutolol and Celiprolol.
[So] Source:Arch Pharm (Weinheim);349(9):733-40, 2016 Sep.
[Is] ISSN:1521-4184
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:The structure-activity relationships of 13 analogs of aryloxyaminopropanol type derived from 2-hydroxyphenylethanone as potential ß-blockers are described. The synthesized compounds possess an isopropyl or a tert-butyl group in the hydrophilic part of the molecule and an alkoxymethyl substitution in the lipophilic moiety. The target compounds were prepared by an established four-step method and their structures were confirmed by interpretation of their UV, IR, (1) H NMR and (13) C NMR spectra, and by elemental analysis. The ß-adrenolytic efficacy of the prepared racemic compounds was determined on isolated guinea pig atria (ß1 ) and trachea (ß2 ) and expressed as pA2 values against isoprenaline tachycardia. The assumed cardioselectivity was expressed as ß1 /ß2 ratio and the values of compounds with an alkoxy group (CH3 O, iC3 H5 O, C5 H11 O, CH2 CHCH2 O, CH3 OCH2 CH2 O) in the lipophilic part and with tert-butyl in the hydrophilic part of the molecule were found to be comparable or higher than those of the standards acebutolol and celiprolol. All evaluated substances at a concentration of 10(-7) mol/dm(3) showed also negative chronotropic effects.
[Mh] Termos MeSH primário: Acebutolol/análogos & derivados
Acebutolol/farmacologia
Celiprolol/análogos & derivados
Celiprolol/farmacologia
Propanolaminas/química
Propanolaminas/farmacologia
[Mh] Termos MeSH secundário: Antagonistas Adrenérgicos beta/síntese química
Antagonistas Adrenérgicos beta/farmacologia
Animais
Cobaias
Átrios do Coração/efeitos dos fármacos
Frequência Cardíaca/efeitos dos fármacos
Histamina/farmacologia
Isoproterenol/farmacologia
Propanolaminas/síntese química
Relação Estrutura-Atividade
Traqueia/efeitos dos fármacos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Adrenergic beta-Antagonists); 0 (Propanolamines); 67P356D8GH (Acebutolol); 820484N8I3 (Histamine); DRB57K47QC (Celiprolol); L628TT009W (Isoproterenol)
[Em] Mês de entrada:1703
[Cu] Atualização por classe:170315
[Lr] Data última revisão:
170315
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160716
[St] Status:MEDLINE
[do] DOI:10.1002/ardp.201600136


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[PMID]:25577782
[Au] Autor:Eguchi K; Hoshide S; Kario K
[Ad] Endereço:Division of Cardiovascular Medicine, Department of Medicine, Jichi Medical University, Shimotsuke, Tochigi, Japan. ke112@jichi.ac.jp.
[Ti] Título:Effects of Celiprolol and Bisoprolol on Blood Pressure, Vascular Stiffness, and Baroreflex Sensitivity.
[So] Source:Am J Hypertens;28(7):858-67, 2015 Jul.
[Is] ISSN:1941-7225
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: We tested the hypothesis that celiprolol and bisoprolol have differential effects on blood pressure (BP), flow-mediated dilation (FMD), and vascular stiffness. METHODS: We analyzed 102 hypertensives (mean age: 59±14 years) who were being treated other than beta-blockers. They were randomized to receive add-on treatment with either celiprolol 100-200mg (C group) or bisoprolol 2.5-5mg (B group), and followed up for 3 months. In addition to clinic, home, and ambulatory BP monitoring, the FMD, radial augmentation index (AI), brachial-ankle pulse wave velocity (baPWV), urine albumin-to-creatinine ratio, and baroreflex sensitivity (BRS) were measured at baseline and at the end of the study. RESULTS: Compared to the baseline values, home and 24-hour BP were significantly lowered in the third month in both groups (all Ps < 0.05). Pulse rate (PR) and baPWV were reduced (P < 0.001), and BRS was increased significantly only in the B group (P = 0.02). Radial AI was unchanged in the C group but was significantly increased in the B group (P < 0.001). Central BP was significantly reduced in the C group (P = 0.003) but was unchanged in the B group. FMD was significantly increased in both groups (both P < 0.01). CONCLUSION: Bisoprolol achieved the greater reduction of PR and improved BRS and vascular stiffness, whereas, celiprolol reduced the central BP level. In treated hypertensive patients, add-on use of celiprolol may be favorable in uncomplicated stage of hypertension. On the other hand, bisoprolol may be useful in hypertensives with cardiac or vascular diseases who have advanced atherosclerotic changes and sympathetic nervous system activation.
[Mh] Termos MeSH primário: Antagonistas de Receptores Adrenérgicos beta 1/uso terapêutico
Anti-Hipertensivos/uso terapêutico
Barorreflexo/efeitos dos fármacos
Bisoprolol/uso terapêutico
Pressão Sanguínea/efeitos dos fármacos
Celiprolol/uso terapêutico
Hipertensão/tratamento farmacológico
Rigidez Vascular/efeitos dos fármacos
[Mh] Termos MeSH secundário: Antagonistas de Receptores Adrenérgicos beta 1/efeitos adversos
Adulto
Idoso
Índice Tornozelo-Braço
Anti-Hipertensivos/efeitos adversos
Bisoprolol/efeitos adversos
Monitorização Ambulatorial da Pressão Arterial
Celiprolol/efeitos adversos
Feminino
Seres Humanos
Hipertensão/diagnóstico
Hipertensão/fisiopatologia
Japão
Masculino
Meia-Idade
Seleção de Pacientes
Valor Preditivo dos Testes
Estudos Prospectivos
Análise de Onda de Pulso
Fatores de Tempo
Resultado do Tratamento
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE; RANDOMIZED CONTROLLED TRIAL
[Nm] Nome de substância:
0 (Adrenergic beta-1 Receptor Antagonists); 0 (Antihypertensive Agents); DRB57K47QC (Celiprolol); Y41JS2NL6U (Bisoprolol)
[Em] Mês de entrada:1603
[Cu] Atualização por classe:150613
[Lr] Data última revisão:
150613
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:150112
[St] Status:MEDLINE
[do] DOI:10.1093/ajh/hpu245


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[PMID]:24905309
[Au] Autor:Andrzejczak D; Górska D
[Ad] Endereço:Department of Pharmacodynamics, Medical University of Lodz, Lodz, Poland. Electronic address: dariusz.andrzejczak@umed.lodz.pl.
[Ti] Título:The effects of celiprolol on serum concentrations of proinflammatory cytokines in hypertensive (SHR) and normotensive (WKY) rats.
[So] Source:Pharmacol Rep;66(1):68-73, 2014 Feb.
[Is] ISSN:1734-1140
[Cp] País de publicação:Poland
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: A growing body of evidence suggests that some cardiovascular drugs could modulate the level of proinflammatory cytokines. Therefore, the aim of the present study was to investigate whether celiprolol, a third generation ß-adrenoceptor blocker, affects lipopolysaccharide (LPS)-induced serum concentrations of TNF-α, IL-1ß, IL-6 in normotensive (WKY) and spontaneously hypertensive (SHR) rats. METHODS: Celiprolol (150 mgkg(-1)) or vehicle was administered by gavage once daily for 21 days. Arterial blood pressure was measured in conscious rats, using the tail-cuff method. Serum concentrations of proinflammatory cytokines were measured with enzyme-linked immunosorbent assay kits. Additionally, plasma concentrations of total cholesterol, HDL-cholesterol and triglycerides were evaluated. RESULTS: In normotensive WKY rats celiprolol did not affect heart rate, blood pressure, or the serum concentrations of triglycerides, total cholesterol or HDL-cholesterol. In hypertensive animals the drug decreased lipid parameters, increased diastolic and mean blood pressure after the first week of administration, and produced a small but significant decrease in heart rate after the first two weeks of the treatment. In both groups of animals, celiprolol decreased LPS-stimulated serum concentration of IL-6 but did not affect levels of TNF-α and IL-1ß. CONCLUSIONS: It is suggested that the IL-6-modulating properties of celiprolol could provide additional value to the therapeutic effectiveness of the drug in the treatment of hypertension.
[Mh] Termos MeSH primário: Antagonistas de Receptores Adrenérgicos beta 1/farmacologia
Anti-Hipertensivos/farmacologia
Celiprolol/farmacologia
Citocinas/sangue
[Mh] Termos MeSH secundário: Animais
Pressão Sanguínea/efeitos dos fármacos
Frequência Cardíaca/efeitos dos fármacos
Hipertensão/tratamento farmacológico
Hipertensão/fisiopatologia
Interleucina-6/fisiologia
Lipídeos/sangue
Masculino
Ratos
Ratos Endogâmicos SHR
Ratos Endogâmicos WKY
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Adrenergic beta-1 Receptor Antagonists); 0 (Antihypertensive Agents); 0 (Cytokines); 0 (Interleukin-6); 0 (Lipids); DRB57K47QC (Celiprolol)
[Em] Mês de entrada:1502
[Cu] Atualização por classe:140609
[Lr] Data última revisão:
140609
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:140607
[St] Status:MEDLINE


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[PMID]:24292052
[Au] Autor:Tanaka S; Uchida S; Miyakawa S; Inui N; Takeuchi K; Watanabe H; Namiki N
[Ad] Endereço:Department of Pharmacy Practice & Science, School of Pharmaceutical Sciences, University of Shizuoka.
[Ti] Título:Comparison of inhibitory duration of grapefruit juice on organic anion-transporting polypeptide and cytochrome P450 3A4.
[So] Source:Biol Pharm Bull;36(12):1936-41, 2013.
[Is] ISSN:1347-5215
[Cp] País de publicação:Japan
[La] Idioma:eng
[Ab] Resumo:Recently, a new type of interaction has been reported in which fruit juices diminish oral drug bioavailability through inhibition of organic anion-transporting polypeptide (OATP). In this study, we aimed to clarify the duration of OATP inhibition by grapefruit juice (GFJ), and to compare it with the duration of GFJ-induced inhibition of cytochrome P450 (CYP) 3A4 activity. Seven healthy volunteers were enrolled in this open-label, single-sequence study. They were orally administered celiprolol (100 mg) and midazolam (15 µg/kg) with water on the control day. Three days later, they ingested GFJ (200 mL) 3 times a day for 3 d. On day 1, the same drugs were administered with GFJ. On days 3 and 7, the same drugs were administered with water. Pharmacokinetics of both drugs were evaluated on each trial day. The peak plasma concentration (Cmax) and the area under the plasma concentration-time curve from 0 to 8 h (AUC0-8) of celiprolol significantly decreased on day 1, and the mean ratios of these values and the corresponding control-day values were 0.18 and 0.25, respectively. The Cmax and AUC0-8 returned to the control levels on days 3 and 7. In contrast, AUC0-8 of midazolam were higher on days 1 and 3 than on the control day (mean ratio, 2.12 and 1.47, respectively). The AUC0-8 returned to the control level on day 7. In conclusion, results of this study indicated that the OATP inhibition caused by GFJ dissipated faster than GFJ-mediated alterations in CYP3A4 activity, which were sustained for at least 48 h.
[Mh] Termos MeSH primário: Bebidas
Celiprolol/farmacocinética
Citrus paradisi
Inibidores do Citocromo P-450 CYP3A
Midazolam/farmacocinética
Transportadores de Ânions Orgânicos/antagonistas & inibidores
[Mh] Termos MeSH secundário: Adulto
Celiprolol/sangue
Citocromo P-450 CYP3A
Interações Alimento-Droga
Seres Humanos
Masculino
Midazolam/sangue
Adulto Jovem
[Pt] Tipo de publicação:CLINICAL TRIAL; COMPARATIVE STUDY; JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Cytochrome P-450 CYP3A Inhibitors); 0 (Organic Anion Transporters); DRB57K47QC (Celiprolol); EC 1.14.13.67 (CYP3A4 protein, human); EC 1.14.14.1 (Cytochrome P-450 CYP3A); R60L0SM5BC (Midazolam)
[Em] Mês de entrada:1407
[Cu] Atualização por classe:151119
[Lr] Data última revisão:
151119
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:131203
[St] Status:MEDLINE


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[PMID]:24144049
[Au] Autor:Abdelkrim MA; Martignat L; Gogny M; Desfontis JC; Noireaud J; Mallem MY
[Ad] Endereço:a L'Université Nantes Angers Le Mans (LUNAM) - Oniris, UPSP 5304 de physiopathologie animale et de pharmacologie fonctionnelle, Atlanpole-La Chantrerie, B.P. 40706, Nantes F-44307, France.
[Ti] Título:Celiprolol induces ß(3)-adrenoceptors-dependent relaxation in isolated porcine coronary arteries.
[So] Source:Can J Physiol Pharmacol;91(10):791-6, 2013 Oct.
[Is] ISSN:1205-7541
[Cp] País de publicação:Canada
[La] Idioma:eng
[Ab] Resumo:In porcine coronary arteries (PCAs), celiprolol, a selective ß(1)-adrenoceptors antagonist, induces vasodilatation by an endothelium- and nitric oxide (NO)-dependent pathway. However, the mechanisms of that vascular effect have not been precisely established. ß(3)-Adrenoceptors have been shown to be involved in the relaxation per se of various vascular beds, including coronary vessels. Thus, we evaluated (i) the presence of ß(3)-adrenoceptors in the PCA and (ii) their role in celiprolol-induced vasodilatation. PCA rings were placed in organ baths and preconstricted with KCl. All experiments were performed in the presence of nadolol (a ß(1)/ß(2)-adrenoceptor antagonist). Cumulative concentration-response curves to SR 58611A and ICI 215001 (2 ß(3)-adrenoceptor agonists) and to celiprolol were constructed. We also used semiquantitative reverse transcription - polymerase chain reaction, which clearly showed the presence of ß(3)-adrenoceptor transcripts. SR 58611A, ICI 215001, and celiprolol induced concentration-dependent relaxations in PCA rings. SR 58611A-induced relaxation was almost abolished after removal of endothelium or pretreatment with L-NAME (a NO synthase inhibitor). The vasorelaxations induced by SR 58611A and celiprolol were inhibited in the presence of SR 59230A and L-748337 (2 selective ß(3)-adrenoceptor antagonists). We showed (i) that PCAs possess functional ß(3)-adrenoceptors mediating endothelium- and NO-dependent relaxation, and (ii) that celiprolol exerts a ß(3)-adrenoceptor agonistic activity in this vascular bed.
[Mh] Termos MeSH primário: Agonistas de Receptores Adrenérgicos beta 3/farmacologia
Celiprolol/farmacologia
Vasos Coronários/efeitos dos fármacos
Receptores Adrenérgicos beta 3/efeitos dos fármacos
Vasodilatação/efeitos dos fármacos
Vasodilatadores/farmacologia
[Mh] Termos MeSH secundário: Antagonistas de Receptores Adrenérgicos beta 3/farmacologia
Animais
Vasos Coronários/metabolismo
Relação Dose-Resposta a Droga
Endotélio Vascular/efeitos dos fármacos
Endotélio Vascular/metabolismo
Inibidores Enzimáticos/farmacologia
Óxido Nítrico/metabolismo
Óxido Nítrico Sintase/antagonistas & inibidores
Óxido Nítrico Sintase/metabolismo
RNA Mensageiro/metabolismo
Receptores Adrenérgicos beta 3/genética
Receptores Adrenérgicos beta 3/metabolismo
Suínos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Adrenergic beta-3 Receptor Agonists); 0 (Adrenergic beta-3 Receptor Antagonists); 0 (Enzyme Inhibitors); 0 (RNA, Messenger); 0 (Receptors, Adrenergic, beta-3); 0 (Vasodilator Agents); 31C4KY9ESH (Nitric Oxide); DRB57K47QC (Celiprolol); EC 1.14.13.39 (Nitric Oxide Synthase)
[Em] Mês de entrada:1406
[Cu] Atualização por classe:131022
[Lr] Data última revisão:
131022
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:131023
[St] Status:MEDLINE
[do] DOI:10.1139/cjpp-2013-0091


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[PMID]:23980448
[Au] Autor:Björck M; Hägg A; Wanhainen A; Pigg MH; Bergqvist D
[Ad] Endereço:Uppsala universitet och Akademiska sjukhuset, Uppsala. martin.bjorck@surgsci.uu.se
[Ti] Título:[New treatment options for vascular Ehlers-Danlos syndrome].
[Ti] Título:Nya behandlingsmöjligheter vid vaskulärt Ehlers-Danlos syndrom..
[So] Source:Lakartidningen;110(29-31):1354-5, 2013 Jul 17-Aug 6.
[Is] ISSN:0023-7205
[Cp] País de publicação:Sweden
[La] Idioma:swe
[Mh] Termos MeSH primário: Antagonistas de Receptores Adrenérgicos beta 1/uso terapêutico
Anti-Hipertensivos/uso terapêutico
Celiprolol/uso terapêutico
Síndrome de Ehlers-Danlos
[Mh] Termos MeSH secundário: Antagonistas de Receptores Adrenérgicos beta 1/farmacologia
Anti-Hipertensivos/farmacologia
Celiprolol/farmacologia
Síndrome de Ehlers-Danlos/tratamento farmacológico
Síndrome de Ehlers-Danlos/genética
Síndrome de Ehlers-Danlos/cirurgia
Procedimentos Endovasculares/efeitos adversos
Seres Humanos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Adrenergic beta-1 Receptor Antagonists); 0 (Antihypertensive Agents); DRB57K47QC (Celiprolol)
[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:130829
[St] Status:MEDLINE


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[PMID]:23784509
[Au] Autor:Nishioka S; Yoshioka T; Nomura A; Kato R; Miyamura M; Okada Y; Ishizaka N; Matsumura Y; Hayashi T
[Ad] Endereço:Laboratory of Pathological and Molecular Pharmacology, Osaka University of Pharmaceutical Sciences, Osaka, Japan.
[Ti] Título:Celiprolol reduces oxidative stress and attenuates left ventricular remodeling induced by hypoxic stress in mice.
[So] Source:Hypertens Res;36(11):934-9, 2013 Nov.
[Is] ISSN:1348-4214
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:We have previously reported that intermittent hypoxic stress, which is relevant to sleep apnea syndrome (SAS), increases oxidative stress and induces left ventricular (LV) remodeling. Celiprolol, a ß1-selective adrenoreceptor blocker, is known to have not only an antihypertensive effect but also an antioxidant effect through releasing nitric oxide. The aim of this study was to examine the hypothesis that celiprolol might ameliorate the LV remodeling induced by intermittent hypoxia through its antioxidant effect. Male C57BL/6J mice (8 weeks old) were exposed to intermittent hypoxia (30 s of 5% oxygen followed by 30 s of 21% oxygen) for 8 h day(-1) during the daytime for 10 consecutive days or were maintained under normoxic conditions. Animals were treated with either celiprolol (100 mg kg(-1) day(-1) by gavage) or vehicle. Hypoxic stress caused fluctuations in blood pressure (BP), an increase in the mean cardiomyocyte diameter, perivascular fibrosis and a decrease in endothelial nitric oxide synthase (eNOS) expression. These changes were associated with increased levels of 4-hydroxy-2-nonenal protein, superoxide, tumor necrosis factor-α mRNA and brain natriuretic peptide mRNA in the LV myocardium. Celiprolol significantly suppressed BP fluctuation, restored eNOS expression and reduced oxidative stress and superoxide production, thus ameliorating hypoxia-induced LV remodeling in mice. These findings suggest that treatment with celiprolol might prevent cardiovascular events in borderline hypertensive patients with SAS.
[Mh] Termos MeSH primário: Antagonistas de Receptores Adrenérgicos beta 1/farmacologia
Celiprolol/farmacologia
Hipóxia/tratamento farmacológico
Estresse Oxidativo/efeitos dos fármacos
Remodelação Ventricular/efeitos dos fármacos
[Mh] Termos MeSH secundário: Antagonistas de Receptores Adrenérgicos beta 1/uso terapêutico
Animais
Pressão Sanguínea/efeitos dos fármacos
Celiprolol/uso terapêutico
Coração/efeitos dos fármacos
Frequência Cardíaca/efeitos dos fármacos
Hipóxia/metabolismo
Masculino
Camundongos
Camundongos Endogâmicos C57BL
Miocárdio/metabolismo
Miócitos Cardíacos/efeitos dos fármacos
Miócitos Cardíacos/metabolismo
Superóxidos/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Adrenergic beta-1 Receptor Antagonists); 11062-77-4 (Superoxides); DRB57K47QC (Celiprolol)
[Em] Mês de entrada:1406
[Cu] Atualização por classe:161125
[Lr] Data última revisão:
161125
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:130621
[St] Status:MEDLINE
[do] DOI:10.1038/hr.2013.60


  9 / 386 MEDLINE  
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[PMID]:23419354
[Au] Autor:Miyazaki N; Misaka S; Ogata H; Fukushima T; Kimura J
[Ad] Endereço:Department of Pharmacology, School of Medicine, Fukushima Medical University, Fukushima, Japan.
[Ti] Título:Effects of itraconazole, dexamethasone and naringin on the pharmacokinetics of nadolol in rats.
[So] Source:Drug Metab Pharmacokinet;28(4):356-61, 2013.
[Is] ISSN:1880-0920
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:The aim of the present study was to clarify the involvement of P-glycoprotein (P-gp) or organic anion transporting polypeptide (Oatp) 1a5 in the pharmacokinetics of nadolol (NDL), a non-metabolized hydrophilic ß-adrenoceptor blocker, in rats. Pretreatment with itraconazole (ICZ, P-gp inhibitor, 50 mg/kg) for 30 min before oral administration of NDL (10 mg/kg) significantly increased the area under the plasma concentration-time curve (AUC0â‚‹∞)of NDL by 1.7-fold compared with control. Intragastric administration of dexamethasone (DEX, 8 mg/kg) for 4 consecutive days increased P-gp level in the intestine and the liver. In line with this, DEX pre-treatment decreased maximum plasma concentration (C(max)) of NDL by 28% of control. To inhibit the intestinal Oatp1a5, naringin (NRG, 0.145 mg/kg) was preadministered orally for 30 min before the oral administrations of NDL or celiprolol (CEL, 10 mg/kg, Oatp1a5 substrate). Although NRG markedly reduced C(max) and AUC0â‚‹∞ of CEL by 60% and 65% of control, respectively, little difference was observed in the plasma concentration of NDL between NRG and control. These results suggest that P-gp is greatly involved in the pharmacokinetics of NDL, while the involvement of Oatp1a5 in the pharmacokinetics of NDL may be less than that of celiprolol in rats.
[Mh] Termos MeSH primário: Membro 1 da Subfamília B de Cassetes de Ligação de ATP/metabolismo
Dexametasona/farmacologia
Flavanonas/farmacologia
Itraconazol/farmacologia
Nadolol/farmacocinética
[Mh] Termos MeSH secundário: Antagonistas Adrenérgicos beta/farmacocinética
Animais
Celiprolol/farmacocinética
Absorção Intestinal/efeitos dos fármacos
Masculino
Transportadores de Ânions Orgânicos Sódio-Independentes/antagonistas & inibidores
Ratos
Ratos Sprague-Dawley
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (ATP-Binding Cassette, Sub-Family B, Member 1); 0 (Adrenergic beta-Antagonists); 0 (Flavanones); 0 (Organic Anion Transporters, Sodium-Independent); 0 (Slc21a1 protein, rat); 0 (Slco1a5 protein, rat); 304NUG5GF4 (Itraconazole); 42200-33-9 (Nadolol); 7S5I7G3JQL (Dexamethasone); DRB57K47QC (Celiprolol); N7TD9J649B (naringin)
[Em] Mês de entrada:1404
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:130220
[St] Status:MEDLINE


  10 / 386 MEDLINE  
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[PMID]:22893261
[Au] Autor:Mizuta E; Utami SB; Ohtahara A; Endo S; Mishima M; Hasegawa A; Yamada K; Kato M; Yamamoto K; Ogino K; Ninomiya H; Miyazaki S; Hamada T; Taniguchi SI; Cheng J; Hisatome I
[Ad] Endereço:Division of Molecular Medicine and Therapeutics, Tottori University Faculty of Medicine, Yonago, Japan.
[Ti] Título:A vasodilating ß1 blocker celiprolol inhibits muscular release of uric acid precursor in patients with essential hypertension.
[So] Source:Horm Metab Res;45(1):69-73, 2013 Jan.
[Is] ISSN:1439-4286
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:Although nonvasodilating ß1 blockers increase the levels of uric acid in serum, it is not known whether vasodilating ß1 blockers have a similar effect. In the present study, we evaluated the effect of celiprolol on the release of hypoxanthine, a uric acid precursor, from muscles after an exercise. We used the semi-ischemic forearm test to examine the release of lactate (ΔLAC), ammonia (ΔAmm), and hypoxanthine (ΔHX) before and 4, 10, and 60 min after an exercise in 18 hypertensive patients as well as 4 normotensive subjects. Before celiprolol treatment, all the levels of ΔHX and ΔAmm, and ΔLAC were increased by semi-ischemic exercise in hypertensive patients, and the increases were remarkably larger than those in normotensive subjects. Celiprolol decreased both systolic and diastolic pressure. It also decreased the levels of ΔHX and ΔAmm without changes in ΔLAC after an exercise. These findings also were confirmed by summation of each metabolite (ΣΔMetabolites). Celiprolol caused a marginal decrease of serum uric acid, but the difference was not statistically significant. On the other hand, nonvasodilating ß1 blockers did not suppress the levels of ΔHX and ΔAmm, whereas they significantly increased ΔLAC after an exercise. Celiprolol improved energy metabolism in skeletal muscles. It suppressed HX production and consequently did not adversely affect serum uric acid levels.
[Mh] Termos MeSH primário: Antagonistas de Receptores Adrenérgicos beta 1/uso terapêutico
Celiprolol/uso terapêutico
Hipertensão/tratamento farmacológico
Hipoxantina/metabolismo
Músculos/metabolismo
Ácido Úrico/sangue
Vasodilatadores/uso terapêutico
[Mh] Termos MeSH secundário: Antagonistas de Receptores Adrenérgicos beta 1/farmacologia
Idoso
Pressão Sanguínea/efeitos dos fármacos
Celiprolol/farmacologia
Teste de Esforço
Feminino
Antebraço/irrigação sanguínea
Antebraço/patologia
Frequência Cardíaca/efeitos dos fármacos
Seres Humanos
Hipertensão/sangue
Hipertensão/fisiopatologia
Isquemia/patologia
Masculino
Meia-Idade
Músculos/efeitos dos fármacos
Vasodilatadores/farmacologia
[Pt] Tipo de publicação:CLINICAL TRIAL; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Adrenergic beta-1 Receptor Antagonists); 0 (Vasodilator Agents); 268B43MJ25 (Uric Acid); 2TN51YD919 (Hypoxanthine); DRB57K47QC (Celiprolol)
[Em] Mês de entrada:1309
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:120816
[St] Status:MEDLINE
[do] DOI:10.1055/s-0032-1321872



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