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[PMID]:27977472
[Au] Autor:Wang Z; Chen Z; Wang X; Hao G; Ma L; Zhao X; Li Y; Zhang L; Zhu M
[Ad] Endereço:aDivision of Prevention and Community Health, National Center for Cardiovascular Diseases, Fuwai Hospital, Peking Union Medical College and Chinese Academy of Medical Sciences, Beijing, China bGeorgia Prevention Institute, Medical College of Georgia, Augusta University, Augusta, Georgia, USA cDivision of Information Consultation, National Center for Cardiovascular Diseases, Fuwai Hospital, Peking Union Medical College and Chinese Academy of Medical Sciences, Beijing, China dDepartment of Cardiology, the First Hospital of Jilin University, Jilin eInstitute of Medical Information, the Chinese Academy of Medical Sciences, Beijing, China.
[Ti] Título:Cost-effectiveness of nitrendipine and hydrochlorothiazide or metoprolol to treat hypertension in rural community health centers in China.
[So] Source:J Hypertens;35(4):886-892, 2017 Apr.
[Is] ISSN:1473-5598
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:OBJECTIVES: The objective of this article is to compare blood pressure (BP)-lowing effects of nitrendipine and hydrochlorothiazide and nitrendipine and metoprolol, and estimate the economic effect of these therapies on hypertension. METHODS: Outpatients (N = 793) 18-70 years of age with stage 2 or severe hypertension (SBP ≥ 160 mmHg and/or DBP ≥ 100 mmHg) were recruited from four randomly selected rural community health centers in Beijing and Jilin. After drug wash out, they were randomly divided into nitrendipine and hydrochlorothiazide group or nitrendipine and metoprolol group. The costs of drug treatment for hypertension were calculated and general estimation, whereas effectiveness was measured as a reduction in SBP and DBP at the end of a 24-week study period. RESULTS: Overall, 623 patients were eligible for the study and after a 24-week follow-up, SBP and DBP were 131.2/82.2 mmHg for the nitrendipine and hydrochlorothiazide group and 131.4/82.9 mmHg for the nitrendipine and metoprolol group and these were not significantly different (P = 0.7974 SBP and P = 0.1166 DBP). Comparing with nitrendipine and metoprolol, the cost of nitrendipine and hydrochlorothiazide was less, and its effectiveness was similar. The cost/effect ratio (US$/mmHg) was 1.4 for SBP and 2.8 for DBP for the nitrendipine and hydrochlorothiazide group, and 1.9 and 3.8 for the nitrendipine and metoprolol group's SBP and DBP values, respectively. The incremental cost per patient for achieving target BP was 5.1. Adverse events were mild or moderate and there were no differences between treatment groups. CONCLUSION: Treating hypertension with nitrendipine and hydrochlorothiazide was cost-effective than nitrendipine and metoprolol, and these data will allow more reasonable and efficient allocation of limited resources in low-income countries.
[Mh] Termos MeSH primário: Anti-Hipertensivos/uso terapêutico
Centros Comunitários de Saúde
Hidroclorotiazida/uso terapêutico
Hipertensão/tratamento farmacológico
Metoprolol/uso terapêutico
Nitrendipino/uso terapêutico
Serviços de Saúde Rural
[Mh] Termos MeSH secundário: Adolescente
Adulto
Idoso
Anti-Hipertensivos/economia
Pequim
Pressão Sanguínea/efeitos dos fármacos
Análise Custo-Benefício
Quimioterapia Combinada/economia
Feminino
Custos de Cuidados de Saúde
Seres Humanos
Hidroclorotiazida/economia
Hipertensão/fisiopatologia
Masculino
Metoprolol/economia
Metoprolol/farmacologia
Meia-Idade
Nitrendipino/economia
Estudos Prospectivos
Adulto Jovem
[Pt] Tipo de publicação:JOURNAL ARTICLE; MULTICENTER STUDY; RANDOMIZED CONTROLLED TRIAL
[Nm] Nome de substância:
0 (Antihypertensive Agents); 0J48LPH2TH (Hydrochlorothiazide); 9B627AW319 (Nitrendipine); GEB06NHM23 (Metoprolol)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:170822
[Lr] Data última revisão:
170822
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161216
[St] Status:MEDLINE
[do] DOI:10.1097/HJH.0000000000001209


  2 / 2078 MEDLINE  
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[PMID]:26827925
[Au] Autor:Druzbicki K; Pajzderska A; Kiwilsza A; Jenczyk J; Chudoba D; Jarek M; Mielcarek J; Wasicki J
[Ad] Endereço:Department of Radiospectroscopy, Faculty of Physics, Adam Mickiewicz University, Umultowska 85, 61-614 Poznan, Poland; Frank Laboratory of Neutron Physics, Joint Institute for Nuclear Research, 141980 Dubna, Russian Federation. Electronic address: kacper.druzbicki@amu.edu.pl.
[Ti] Título:In search of the mutual relationship between the structure, solid-state spectroscopy and molecular dynamics in selected calcium channel blockers.
[So] Source:Eur J Pharm Sci;85:68-83, 2016 Mar 31.
[Is] ISSN:1879-0720
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Three isostructural 1,4-dihydropyridines (DHPs), namely, nifedipine, nitrendipine and nimodipine were selected to characterize their structure, intermolecular interactions and molecular dynamics. The studied samples were analyzed using powder X-ray diffraction (XRD), neutron (INS) and infrared spectroscopy (FT-IR) as well as solid-state nuclear magnetic resonance (NMR), where each technique was supported by the state-of-the-art theoretical calculations for solid-state. By combining multiple experimental techniques with advanced theoretical calculations we were able to shed light on the mutual relation between the structure, stabilizing intermolecular interactions and their spectral response. For the first time, unambiguous computationally-supported assignment of the most prominent spectral features in DHPs is presented to give a valuable support for polymorph screening and drug control. Molecular motions were interpreted in details, revealing that a dynamic reservoir of each compound is dominated by intra-molecular reorientations of methyl groups and large-amplitude oscillations in terminal chains. Our study successfully validates the realm of applicability of first-principles solid-state calculations in search of the mutual relation between the structure and spectroscopy in this important class of drugs. Such approach gives a first necessary step to gather combined structure-dynamics data on functionalized DHPs, which are of importance to better understand crystallization and binding tendency. The NMR relaxation experiments reveal that nitro groups significantly hinder the reorientation of methyl rotors and provide the first evidence of low-temperature methyl-group tunneling in DHPs, an intriguing quantum-effect which is to be further explored.
[Mh] Termos MeSH primário: Bloqueadores dos Canais de Cálcio/química
[Mh] Termos MeSH secundário: Cristalização/métodos
Di-Hidropiridinas/química
Espectroscopia de Ressonância Magnética/métodos
Simulação de Dinâmica Molecular
Nifedipino/química
Nimodipino/química
Nitrendipino/química
Teoria Quântica
Espectrofotometria Infravermelho/métodos
Difração de Raios X/métodos
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Calcium Channel Blockers); 0 (Dihydropyridines); 57WA9QZ5WH (Nimodipine); 7M8K3P6I89 (1,4-dihydropyridine); 9B627AW319 (Nitrendipine); I9ZF7L6G2L (Nifedipine)
[Em] Mês de entrada:1612
[Cu] Atualização por classe:161230
[Lr] Data última revisão:
161230
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160202
[St] Status:MEDLINE


  3 / 2078 MEDLINE  
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[PMID]:26375758
[Au] Autor:Kumar Gaur P; Mishra S; Purohit S
[Ad] Endereço:a Department of Pharmaceutics , I.T.S. College of Pharmacy , Muradnagar, Ghaziabad , Uttar Pradesh , India .
[Ti] Título:Nanovesicles of nitrendipine with lipid complex for transdermal delivery: pharmacokinetic and pharmacodynamic studies.
[So] Source:Artif Cells Nanomed Biotechnol;44(7):1684-93, 2016 Nov.
[Is] ISSN:2169-141X
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:CONTEXT: Vesicular transdermal delivery can enhance the bioavailability of a drug especially affected by first-pass metabolism, e.g. nitrendipine. However effective transdermal delivery employs permeation enhancer, e.g oleic acid (OA) with ceramide 2, stearic acid, behenic acid, and cholesteryl sulfate lipid complex. OBJECTIVE: This study investigated the preparation, characterization of physicochemical properties, ex vivo permeation using human skin, pharmacokinetic parameters and antihypertensive potential in rats, of nitrendipine-loaded nanovesicles of ceramide 2, stearic acid, behenic acid and cholesteryl sulfate containing oleic acid gel (NOVG). MATERIALS AND METHODS: The nanovesicles were made using film hydration method and characterized for physicochemical properties, ex vivo permeation using human skin, pharmacokinetic parameters and antihypertensive potential. RESULTS: Nitrendipine-loaded nanovesicles of ceramide-2 containing oleic acid (NOV-5) have shown fluxes in the range of 4.88-24.72 µg/cm(2)/h nitrendipine oral suspension (NOS) at equal dose. NOVG-5 has shown almost 33% reduction in blood pressure in the first hour and a further decrease of 25% in the second hour to restore the normal pressure. DISCUSSION: The permeation increases with increase in OA content. OA gets integrated in vesicle wall and enhances its permeability, whereas ceramide content makes sure that skin does not become damaged even after permeation. CONCLUSION: NOVG-5 has shown the most favorable physicochemical properties and good permeation through skin providing good management of hypertension during crucial initial hours.
[Mh] Termos MeSH primário: Nanocápsulas/química
Nitrendipino
Absorção Cutânea/efeitos dos fármacos
[Mh] Termos MeSH secundário: Animais
Ceramidas/química
Ceramidas/farmacocinética
Ceramidas/farmacologia
Ésteres do Colesterol/química
Ésteres do Colesterol/farmacocinética
Ésteres do Colesterol/farmacologia
Ácidos Graxos/química
Ácidos Graxos/farmacocinética
Ácidos Graxos/farmacologia
Feminino
Seres Humanos
Masculino
Nitrendipino/química
Nitrendipino/farmacocinética
Nitrendipino/farmacologia
Ácido Oleico/química
Ácido Oleico/farmacocinética
Ácido Oleico/farmacologia
Ratos
Ratos Wistar
Ácidos Esteáricos/química
Ácidos Esteáricos/farmacocinética
Ácidos Esteáricos/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Ceramides); 0 (Cholesterol Esters); 0 (Fatty Acids); 0 (Nanocapsules); 0 (Stearic Acids); 2UMI9U37CP (Oleic Acid); 4ELV7Z65AP (stearic acid); 9B627AW319 (Nitrendipine); H390488X0A (behenic acid); KU576NT9O9 (cholesteryl sulfate)
[Em] Mês de entrada:1701
[Cu] Atualização por classe:170113
[Lr] Data última revisão:
170113
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:150917
[St] Status:MEDLINE
[do] DOI:10.3109/21691401.2015.1080170


  4 / 2078 MEDLINE  
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[PMID]:26166407
[Au] Autor:Zhao Y; Wu C; Zhao Z; Hao Y; Xu J; Yu T; Qiu Y; Jiang J
[Ad] Endereço:a Pharmacy School, Liaoning Medical University, Linghe District , Jinzhou , Liaoning Province , P.R. China.
[Ti] Título:Preparation of starch macrocellular foam for increasing the dissolution rate of poorly water-soluble drugs.
[So] Source:Pharm Dev Technol;21(6):749-54, 2016 Sep.
[Is] ISSN:1097-9867
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Starch macrocellular foam (SMF), a novel natural bio-matrix material, was prepared by the hard template method in order to improve the dissolution rate and oral bioavailability of poorly water-soluble drugs. Nitrendipine (NDP) was chosen as a model drug and was loaded into SMF by the solvent evaporation method. SMF and the loaded SMF samples (NDP-SMF) were characterized by scanning electron microscopy, differential scanning calorimetry, X-ray powder diffraction and Fourier transform infrared spectroscopy. In vitro drug release studies showed that SMF significantly increased the dissolution rate of NDP. In vivo studies showed that the NDP-SMF tablets clearly increased the oral bioavailability of NDP in comparison with the reference commercial tablets. All the results obtained demonstrated that SMF was a promising carrier for the oral delivery of poor water-soluble drugs.
[Mh] Termos MeSH primário: Nitrendipino/farmacocinética
Amido/farmacocinética
Substâncias Viscoelásticas/farmacocinética
Água/metabolismo
[Mh] Termos MeSH secundário: Administração Oral
Animais
Anti-Hipertensivos/administração & dosagem
Anti-Hipertensivos/química
Anti-Hipertensivos/farmacocinética
Liberação Controlada de Fármacos/efeitos dos fármacos
Liberação Controlada de Fármacos/fisiologia
Nitrendipino/administração & dosagem
Nitrendipino/química
Coelhos
Distribuição Aleatória
Solubilidade
Amido/química
Substâncias Viscoelásticas/administração & dosagem
Substâncias Viscoelásticas/química
Água/química
Difração de Raios X
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antihypertensive Agents); 0 (Viscoelastic Substances); 059QF0KO0R (Water); 9005-25-8 (Starch); 9B627AW319 (Nitrendipine)
[Em] Mês de entrada:1703
[Cu] Atualização por classe:170313
[Lr] Data última revisão:
170313
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:150714
[St] Status:MEDLINE
[do] DOI:10.3109/10837450.2015.1055763


  5 / 2078 MEDLINE  
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[PMID]:25758670
[Au] Autor:Lin BH; Tsai MH; Lii CK; Wang TS
[Ad] Endereço:School of Biomedical Sciences, Chung Shan Medical University, Taichung, Taiwan.
[Ti] Título:IP3 and calcium signaling involved in the reorganization of the actin cytoskeleton and cell rounding induced by cigarette smoke extract in human endothelial cells.
[So] Source:Environ Toxicol;31(11):1293-1306, 2016 Nov.
[Is] ISSN:1522-7278
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Smoking increases the risk of cardiovascular disorders and leads to damage caused by inflammation and oxidative stress. The actin cytoskeleton is a key player in the response to inflammatory stimuli and is an early target of cellular oxidative stress. The purpose of this study was to investigate the changes in actin cytoskeleton dynamics in human endothelial EA.hy926 cells exposed to cigarette smoke extract (CSE). Immunostaining revealed that CSE exposure resulted in modification of the actin cytoskeleton and led to cell rounding in a dose- and time-dependent manner. In addition, the intracellular calcium concentration was increased by treatment with CSE. Pretreatment with antioxidants (lipoic acid, glutathione, N-acetyl cysteine, aminoguanidine, α-tocopherol, and vitamin C) significantly attenuated the CSE-induced actin cytoskeleton reorganization and cell rounding. Calcium ion chelators (EGTA, BAPTA-AM AM) and a potent store-operated calcium channel inhibitor (MRS 1845) also reduced CSE-induced intracellular calcium changes and attenuated actin cytoskeleton reorganization and cell morphology change. Moreover, the CSE-induced intracellular calcium increase was suppressed by pretreatment with the inositol trisphosphate receptor (IP3R) inhibitor xestospongin C, the phospholipase C (PLC) inhibitor U-73122, and the protein kinase C (PKC) inhibitor GF109203X. These results suggest that reactive oxygen species production and intracellular calcium increase play an essential role in CSE-induced actin disorganization and cell rounding through a PLC-IP3-PKC signaling pathway. © 2015 Wiley Periodicals, Inc. Environ Toxicol 31: 1293-1306, 2016.
[Mh] Termos MeSH primário: Citoesqueleto de Actina/metabolismo
Sinalização do Cálcio
Receptores de Inositol 1,4,5-Trifosfato/metabolismo
Fumaça
Tabaco/química
[Mh] Termos MeSH secundário: Acetilcisteína/farmacologia
Citoesqueleto de Actina/efeitos dos fármacos
Antioxidantes/farmacologia
Sinalização do Cálcio/efeitos dos fármacos
Linhagem Celular
Quelantes/farmacologia
Células Endoteliais/citologia
Células Endoteliais/efeitos dos fármacos
Células Endoteliais/metabolismo
Estrenos/farmacologia
Glutationa/metabolismo
Seres Humanos
Indóis/farmacologia
Receptores de Inositol 1,4,5-Trifosfato/antagonistas & inibidores
Compostos Macrocíclicos/farmacologia
Maleimidas/farmacologia
Microscopia de Fluorescência
Nitrendipino/análogos & derivados
Nitrendipino/farmacologia
Oxazóis/farmacologia
Estresse Oxidativo/efeitos dos fármacos
Proteína Quinase C/antagonistas & inibidores
Proteína Quinase C/metabolismo
Pirrolidinonas/farmacologia
Espécies Reativas de Oxigênio/metabolismo
Tabaco/metabolismo
Fosfolipases Tipo C/antagonistas & inibidores
Fosfolipases Tipo C/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antioxidants); 0 (Chelating Agents); 0 (Estrenes); 0 (Indoles); 0 (Inositol 1,4,5-Trisphosphate Receptors); 0 (MRS 1845); 0 (Macrocyclic Compounds); 0 (Maleimides); 0 (Oxazoles); 0 (Pyrrolidinones); 0 (Reactive Oxygen Species); 0 (Smoke); 0 (xestospongin C); 112648-68-7 (1-(6-((3-methoxyestra-1,3,5(10)-trien-17-yl)amino)hexyl)-1H-pyrrole-2,5-dione); 9B627AW319 (Nitrendipine); EC 2.7.11.13 (Protein Kinase C); EC 3.1.4.- (Type C Phospholipases); GAN16C9B8O (Glutathione); L79H6N0V6C (bisindolylmaleimide I); WYQ7N0BPYC (Acetylcysteine)
[Em] Mês de entrada:1703
[Cu] Atualização por classe:170817
[Lr] Data última revisão:
170817
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:150312
[St] Status:MEDLINE
[do] DOI:10.1002/tox.22133


  6 / 2078 MEDLINE  
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[PMID]:25362529
[Au] Autor:Cabuk H; Avci A; Durmaz H; Cabuk FK; Ertem F; Muhittin Sener I
[Ad] Endereço:Department of Orthopedics and Traumatology, Okmeydani and Research Hospital, Sisli, Turkey, halukcabuk@hotmail.com.
[Ti] Título:The effect of diclofenac on matrix metalloproteinase levels in the rotator cuff.
[So] Source:Arch Orthop Trauma Surg;134(12):1739-44, 2014 Dec.
[Is] ISSN:1434-3916
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:INTRODUCTION: Matrix metalloproteinases (MMPs) are involved in physiological events such as restructuring of the tissue, morphogenesis, wound healing and normal developmental process. Use of diclofenac sodium following rotator cuff repair can disrupt healing of tendon through acting on MMPs. MATERIALS AND METHODS: Supraspinatus tendons of rats (n = 84) were detached from their insertion on humerus, and repaired to anatomic footprint. Rats were divided into study group (n = 42) and control group (n = 42). Study group received a dose of 1 mg/kg daily diclofenac sodium subcutaneously. The rats were killed at weeks 1, 3 and 6, and seven rats from each groups were included in biomechanical and immunohistological examinations. Immunohistological staining of MMP-2, MMP-3 and MMP13 were used. RESULTS: Maximum load was reduced in the study group at the end of week 1 (8.76 vs. 5.28 N) (p = 0.01). MMP-3 level was statistically significantly lower in the study group at the end of week 1. MMP-13 level and stiffness decreased towards week 6 in the study group while in the control group the level of MMP-2 decreased towards week 6. CONCLUSION: Diclofenac has an impact on the levels of MMP-2, MMP-3 and MMP-13, which are needed for normal healing process, and it can also lead to disruption of tendon healing.
[Mh] Termos MeSH primário: Anti-Inflamatórios não Esteroides/farmacologia
Diclofenaco/farmacologia
Metaloproteinases da Matriz/metabolismo
Manguito Rotador/enzimologia
Cicatrização/efeitos dos fármacos
[Mh] Termos MeSH secundário: Animais
Imuno-Histoquímica
Masculino
Metaloproteinase 13 da Matriz/metabolismo
Metaloproteinase 2 da Matriz/metabolismo
Metaloproteinase 3 da Matriz/metabolismo
Nitrendipino
Ratos Wistar
Manguito Rotador/fisiopatologia
Manguito Rotador/cirurgia
Tendões/cirurgia
Cicatrização/fisiologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Inflammatory Agents, Non-Steroidal); 144O8QL0L1 (Diclofenac); 9B627AW319 (Nitrendipine); EC 3.4.24.- (Matrix Metalloproteinase 13); EC 3.4.24.- (Matrix Metalloproteinases); EC 3.4.24.17 (Matrix Metalloproteinase 3); EC 3.4.24.24 (Matrix Metalloproteinase 2)
[Em] Mês de entrada:1504
[Cu] Atualização por classe:141118
[Lr] Data última revisão:
141118
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:141103
[St] Status:MEDLINE
[do] DOI:10.1007/s00402-014-2099-0


  7 / 2078 MEDLINE  
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[PMID]:25100767
[Au] Autor:Yamada Y; Kinoshita H; Kuwahara K; Nakagawa Y; Kuwabara Y; Minami T; Yamada C; Shibata J; Nakao K; Cho K; Arai Y; Yasuno S; Nishikimi T; Ueshima K; Kamakura S; Nishida M; Kiyonaka S; Mori Y; Kimura T; Kangawa K; Nakao K
[Ad] Endereço:Department of Medicine and Clinical Science, Kyoto University Graduate School of Medicine, 54 Shogoin Kawaharacho, Sakyo-ku, Kyoto 606-8507, Japan Department of Peptide Research, Kyoto University Graduate School of Medicine, Kyoto 606-8507, Japan.
[Ti] Título:Inhibition of N-type Ca2+ channels ameliorates an imbalance in cardiac autonomic nerve activity and prevents lethal arrhythmias in mice with heart failure.
[So] Source:Cardiovasc Res;104(1):183-93, 2014 Oct 01.
[Is] ISSN:1755-3245
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:AIMS: Dysregulation of autonomic nervous system activity can trigger ventricular arrhythmias and sudden death in patients with heart failure. N-type Ca(2+) channels (NCCs) play an important role in sympathetic nervous system activation by regulating the calcium entry that triggers release of neurotransmitters from peripheral sympathetic nerve terminals. We have investigated the ability of NCC blockade to prevent lethal arrhythmias associated with heart failure. METHODS AND RESULTS: We compared the effects of cilnidipine, a dual N- and L-type Ca(2+) channel blocker, with those of nitrendipine, a selective L-type Ca(2+) channel blocker, in transgenic mice expressing a cardiac-specific, dominant-negative form of neuron-restrictive silencer factor (dnNRSF-Tg). In this mouse model of dilated cardiomyopathy leading to sudden arrhythmic death, cardiac structure and function did not significantly differ among the control, cilnidipine, and nitrendipine groups. However, cilnidipine dramatically reduced arrhythmias in dnNRSF-Tg mice, significantly improving their survival rate and correcting the imbalance between cardiac sympathetic and parasympathetic nervous system activity. A ß-blocker, bisoprolol, showed similar effects in these mice. Genetic titration of NCCs, achieved by crossing dnNRSF-Tg mice with mice lacking CACNA1B, which encodes the α1 subunit of NCCs, improved the survival rate. With restoration of cardiac autonomic balance, dnNRSF-Tg;CACNA1B(+/-) mice showed fewer malignant arrhythmias than dnNRSF-Tg;CACNA1B(+/+) mice. CONCLUSIONS: Both pharmacological blockade of NCCs and their genetic titration improved cardiac autonomic balance and prevented lethal arrhythmias in a mouse model of dilated cardiomyopathy and sudden arrhythmic death. Our findings suggest that NCC blockade is a potentially useful approach to preventing sudden death in patients with heart failure.
[Mh] Termos MeSH primário: Antiarrítmicos/farmacologia
Arritmias Cardíacas/prevenção & controle
Sistema Nervoso Autônomo/efeitos dos fármacos
Bloqueadores dos Canais de Cálcio/farmacologia
Canais de Cálcio Tipo N/efeitos dos fármacos
Morte Súbita Cardíaca/prevenção & controle
Di-Hidropiridinas/farmacologia
Insuficiência Cardíaca/tratamento farmacológico
Coração/inervação
[Mh] Termos MeSH secundário: Antagonistas Adrenérgicos beta/farmacologia
Animais
Arritmias Cardíacas/genética
Arritmias Cardíacas/metabolismo
Arritmias Cardíacas/fisiopatologia
Sistema Nervoso Autônomo/metabolismo
Sistema Nervoso Autônomo/fisiopatologia
Canais de Cálcio Tipo L/efeitos dos fármacos
Canais de Cálcio Tipo L/metabolismo
Canais de Cálcio Tipo N/genética
Canais de Cálcio Tipo N/metabolismo
Cardiomiopatia Dilatada/tratamento farmacológico
Cardiomiopatia Dilatada/genética
Cardiomiopatia Dilatada/metabolismo
Cardiomiopatia Dilatada/fisiopatologia
Morte Súbita Cardíaca/etiologia
Modelos Animais de Doenças
Insuficiência Cardíaca/genética
Insuficiência Cardíaca/metabolismo
Insuficiência Cardíaca/fisiopatologia
Camundongos Knockout
Camundongos Transgênicos
Nitrendipino/farmacologia
Proteínas Repressoras/genética
Proteínas Repressoras/metabolismo
Fatores de Tempo
Função Ventricular Esquerda/efeitos dos fármacos
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Adrenergic beta-Antagonists); 0 (Anti-Arrhythmia Agents); 0 (Cacna1b protein, mouse); 0 (Calcium Channel Blockers); 0 (Calcium Channels, L-Type); 0 (Calcium Channels, N-Type); 0 (Dihydropyridines); 0 (RE1-silencing transcription factor); 0 (Repressor Proteins); 97T5AZ1JIP (cilnidipine); 9B627AW319 (Nitrendipine)
[Em] Mês de entrada:1506
[Cu] Atualização por classe:140926
[Lr] Data última revisão:
140926
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:140808
[St] Status:MEDLINE
[do] DOI:10.1093/cvr/cvu185


  8 / 2078 MEDLINE  
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[PMID]:25005602
[Au] Autor:Mitsui T; Nemoto T; Miyake T; Nagao S; Ogawa K; Kato M; Ishigai M; Yamada H
[Ad] Endereço:Preclinical Research Department, Research Division, Chugai Pharmaceutical Co., Ltd., Shizuoka, Japan (Te.M., T.N.,Ta.M., S.N., K.O., M.K., M.I.); and Graduate School of Pharmaceutical Sciences, Kyushu University, Fukuoka, Japan (H.Y.) mitsuitty@chugai-pharm.co.jp.
[Ti] Título:A useful model capable of predicting the clearance of cytochrome 3A4 (CYP3A4) substrates in humans: validity of CYP3A4 transgenic mice lacking their own Cyp3a enzymes.
[So] Source:Drug Metab Dispos;42(9):1540-7, 2014 Sep.
[Is] ISSN:1521-009X
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The accurate prediction for the body clearance of a novel drug candidate by humans during the preclinical stage contributes to its successful development. To improve the predictability of human hepatic clearance, we focused on CYP3A4, which is involved in the metabolism of more than 50% of all currently marketed drugs. In this study, we investigated the validity of the in vivo model using transgenic mice carrying the human CYP3A4 gene and lacking their own Cyp3a genes (CYP3A4-Tg mice). The CYP3A4 activity toward its substrates in liver microsomes was similar in CYP3A4-Tg mice and humans. As for the clearance, six CYP3A4 substrates (alprazolam, felodipine, midazolam, nifedipine, nitrendipine, and quinidine) were given intravenously to CYP3A4-Tg mice, and their hepatic intrinsic clearance (CLint,h) was evaluated. A regression analysis of the data obtained indicated that the CLint,h values of six substrates in CYP3A4-Tg mice were highly correlated with those in humans (R(2) = 0.95). This correlation could be improved by correcting the CLint,h values by the relative contribution of artificially expressed CYP3A4 to the overall metabolism in the mice. From these findings, it is reasonable to expect that the CLint,h of a particular drug in humans is predictable by applying the CLint,h obtained in CYP3A4-Tg mice to a regression line prepared in advance. The variance of the CLint,h prediction by this method was evaluated and found to be within a range of 2-fold of the regression value. These results suggest that the CYP3A4-Tg mouse model has the potential to accurately predict the human hepatic clearance of CYP3A4 substrates.
[Mh] Termos MeSH primário: Citocromo P-450 CYP3A/metabolismo
Sistema Enzimático do Citocromo P-450/metabolismo
Microssomos Hepáticos/metabolismo
[Mh] Termos MeSH secundário: Alprazolam/metabolismo
Animais
Felodipino/metabolismo
Seres Humanos
Masculino
Camundongos
Camundongos Transgênicos
Midazolam/metabolismo
Nifedipino/metabolismo
Nitrendipino/metabolismo
Quinidina/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
9035-51-2 (Cytochrome P-450 Enzyme System); 9B627AW319 (Nitrendipine); EC 1.14.13.67 (CYP3A4 protein, human); EC 1.14.14.1 (CYP3A protein, mouse); EC 1.14.14.1 (Cytochrome P-450 CYP3A); I9ZF7L6G2L (Nifedipine); ITX08688JL (Quinidine); OL961R6O2C (Felodipine); R60L0SM5BC (Midazolam); YU55MQ3IZY (Alprazolam)
[Em] Mês de entrada:1503
[Cu] Atualização por classe:140807
[Lr] Data última revisão:
140807
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:140710
[St] Status:MEDLINE
[do] DOI:10.1124/dmd.114.057935


  9 / 2078 MEDLINE  
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[PMID]:24905310
[Au] Autor:Türkes C; Söyüt H; Beydemir S
[Ad] Endereço:Department of Chemistry, Faculty of Science, Atatürk University, Erzurum, Turkey.
[Ti] Título:Effect of calcium channel blockers on paraoxonase-1 (PON1) activity and oxidative stress.
[So] Source:Pharmacol Rep;66(1):74-80, 2014 Feb.
[Is] ISSN:1734-1140
[Cp] País de publicação:Poland
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: In this study, we investigated the in vitro effects of calcium channel blockers (nifedipine, nitrendipine, isradipine, and amlodipine besylate) on the activity of paraoxonase-1 (PON1). METHODS: PON1 was purified from human serum using simple chromatographic methods, including DEAE-Sephadex anion-exchange and Sephadex G-200 gel filtration chromatography. RESULTS: The calcium channel blockers decreased the in vitro PON1 activity. The inhibition mechanism of amlodipine besylate was noncompetitive, whereas nifedipine, nitrendipine, and isradipine were competitive inhibitors. CONCLUSIONS: Our results showed that calcium channel blockers exhibit inhibitory effects on PON1 at low concentrations. The IC(50) values for nifedipine, nitrendipine, isradipine, and amlodipine besylate were determined to be 0.121 mM, 0.130 mM, 0.255 mM, and 0.304 mM, respectively, and the K(i) constants were calculated to be 0.222 ± 0.049 mM, 0.151 ± 0.067 mM, 0.286 ± 0.137 mM, and 0.321 ± 0.002 mM, respectively.
[Mh] Termos MeSH primário: Arildialquilfosfatase/metabolismo
Bloqueadores dos Canais de Cálcio/farmacologia
Estresse Oxidativo/efeitos dos fármacos
[Mh] Termos MeSH secundário: Anlodipino/farmacologia
Arildialquilfosfatase/antagonistas & inibidores
Seres Humanos
Isradipino/farmacologia
Nifedipino/farmacologia
Nitrendipino
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Calcium Channel Blockers); 1J444QC288 (Amlodipine); 9B627AW319 (Nitrendipine); EC 3.1.8.1 (Aryldialkylphosphatase); EC 3.1.8.1 (PON1 protein, human); I9ZF7L6G2L (Nifedipine); YO1UK1S598 (Isradipine)
[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


  10 / 2078 MEDLINE  
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[PMID]:24850215
[Au] Autor:Sweeney D; Hollins F; Gomez E; Saunders R; Challiss RA; Brightling CE
[Ad] Endereço:Institute for Lung Health, Department of Infection, Immunity and Inflammation, NIHR Biomedical Unit, Glenfield Hospital, University of Leicester, Leicester, UK; Department of Cell Physiology and Pharmacology, University of Leicester, Leicester, UK.
[Ti] Título:[Ca2+]i oscillations in ASM: relationship with persistent airflow obstruction in asthma.
[So] Source:Respirology;19(5):763-6, 2014 Jul.
[Is] ISSN:1440-1843
[Cp] País de publicação:Australia
[La] Idioma:eng
[Ab] Resumo:The cause of airway smooth muscle (ASM) hypercontractility in asthma is not fully understood. The relationship of spontaneous intracellular calcium oscillation frequency in ASM to asthma severity was investigated. Oscillations were increased in subjects with impaired lung function abolished by extracellular calcium removal, attenuated by caffeine and unaffected by verapamil or nitrendipine. Whether modulation of increased spontaneous intracellular calcium oscillations in ASM from patients with impaired lung function represents a therapeutic target warrants further investigation.
[Mh] Termos MeSH primário: Asma/fisiopatologia
Sinalização do Cálcio/fisiologia
Músculo Liso/fisiopatologia
Doença Pulmonar Obstrutiva Crônica/fisiopatologia
Músculos Respiratórios/fisiopatologia
Índice de Gravidade de Doença
[Mh] Termos MeSH secundário: Adulto
Idoso
Biópsia
Cafeína/farmacologia
Sinalização do Cálcio/efeitos dos fármacos
Estudos de Casos e Controles
Feminino
Volume Expiratório Forçado/fisiologia
Seres Humanos
Masculino
Meia-Idade
Músculo Liso/efeitos dos fármacos
Músculo Liso/patologia
Nitrendipino/farmacologia
Músculos Respiratórios/efeitos dos fármacos
Músculos Respiratórios/patologia
Verapamil/farmacologia
Capacidade Vital/fisiologia
[Pt] Tipo de publicação:LETTER
[Nm] Nome de substância:
3G6A5W338E (Caffeine); 9B627AW319 (Nitrendipine); CJ0O37KU29 (Verapamil)
[Em] Mês de entrada:1507
[Cu] Atualização por classe:170922
[Lr] Data última revisão:
170922
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:140523
[St] Status:MEDLINE
[do] DOI:10.1111/resp.12318



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