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[PMID]:28448397
[Au] Autor:Hirabayashi M; Doi K; Imamachi N; Kishimoto T; Saito Y
[Ad] Endereço:From the *Department of Anesthesiology, Hamada Medical Center, Hamada, Shimane, Japan; and †Department of Anesthesiology, Shimane University School of Medicine, Izumo, Japan.
[Ti] Título:Prophylactic Pentazocine Reduces the Incidence of Pruritus After Cesarean Delivery Under Spinal Anesthesia With Opioids: A Prospective Randomized Clinical Trial.
[So] Source:Anesth Analg;124(6):1930-1934, 2017 06.
[Is] ISSN:1526-7598
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: The incidence of pruritus after cesarean delivery under spinal anesthesia with opioids is high, ranging from 50% to 100%. Pruritus is difficult to prevent; however, pentazocine has been shown to be an effective treatment. Despite this, the prophylactic effect of pentazocine on pruritus has not been defined. This randomized double-blind trial aimed to evaluate the effect of intraoperative IV pentazocine on the incidence of opioid-induced pruritus within the first 24 hours after administration of neuraxial opioids. METHODS: We obtained institutional review board approval and written informed consent from the 122 patients (American Society of Anesthesiologists [ASA] physical status II; aged 20-40 years) scheduled for elective cesarean delivery who were included in this study. Spinal anesthesia was performed with 10 mg of 0.5% hyperbaric bupivacaine, 10 µg of fentanyl, and 100 µg of morphine. After delivery of the baby and placenta, the parturient women were randomized to intravenously receive 15 mg (1 mL) of pentazocine or 1 mL of saline. All women received postoperative analgesia with the epidural infusion of 0.15% levobupivacaine. The presence of pruritus within the first 24 hours after intrathecal administration of opioids was recorded, and severity of itch, numerical rating scale (NRS) for pain, and adverse effects were also recorded at the time of the arrival on the ward, as well as 3, 6, 12, and 24 hours after the intrathecal administration of opioids. RESULTS: A total of 119 women completed the study. IV pentazocine reduced the overall incidence of pruritus within the first 24 hours compared to IV saline, with an estimated relative risk of 69% (95% confidence interval [CI], 52%, 90%; P = .007). IV pentazocine also reduced the severity of pruritus. The incidence of nausea and vomiting was not significantly different. There were no significant differences in postoperative NRS scores. CONCLUSIONS: A single 15-mg dose of IV pentazocine after delivery can reduce both the incidence and severity of pruritus in women who have received subarachnoid opioids during cesarean delivery.
[Mh] Termos MeSH primário: Analgésicos Opioides/efeitos adversos
Raquianestesia/efeitos adversos
Antipruriginosos/administração & dosagem
Cesárea/efeitos adversos
Fentanila/efeitos adversos
Pentazocina/administração & dosagem
Prurido/prevenção & controle
[Mh] Termos MeSH secundário: Administração Intravenosa
Adulto
Analgésicos Opioides/administração & dosagem
Raquianestesia/métodos
Antipruriginosos/efeitos adversos
Cesárea/métodos
Método Duplo-Cego
Esquema de Medicação
Procedimentos Cirúrgicos Eletivos
Feminino
Fentanila/administração & dosagem
Seres Humanos
Incidência
Japão/epidemiologia
Pentazocina/efeitos adversos
Gravidez
Estudos Prospectivos
Prurido/induzido quimicamente
Prurido/diagnóstico
Prurido/epidemiologia
Fatores de Risco
Índice de Gravidade de Doença
Fatores de Tempo
Resultado do Tratamento
Adulto Jovem
[Pt] Tipo de publicação:JOURNAL ARTICLE; RANDOMIZED CONTROLLED TRIAL; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Analgesics, Opioid); 0 (Antipruritics); RP4A60D26L (Pentazocine); UF599785JZ (Fentanyl)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:180105
[Lr] Data última revisão:
180105
[Sb] Subgrupo de revista:AIM; IM
[Da] Data de entrada para processamento:170428
[St] Status:MEDLINE
[do] DOI:10.1213/ANE.0000000000002060


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[PMID]:28898265
[Au] Autor:Zhao J; Mysona BA; Wang J; Gonsalvez GB; Smith SB; Bollinger KE
[Ad] Endereço:James and Jean Culver Vision Discovery Institute, Augusta, Georgia, United States of America.
[Ti] Título:Sigma 1 receptor regulates ERK activation and promotes survival of optic nerve head astrocytes.
[So] Source:PLoS One;12(9):e0184421, 2017.
[Is] ISSN:1932-6203
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The sigma 1 receptor (S1R) is a unique transmembrane protein that has been shown to regulate neuronal differentiation and cellular survival. It is expressed within several cell types throughout the nervous system and visceral organs, including neurons and glia within the eye. S1R ligands are therapeutic targets for diseases ranging from neurodegenerative conditions to neoplastic disorders. However, effects of S1R activation and inhibition within glia cells are not well characterized. Within the eye, the astrocytes at the optic nerve head are crucial to the health and survival of the neurons that send visual information to the brain. In this study, we used the S1R-specific agonist, (+)-pentazocine, to evaluate S1R activation within optic nerve head-derived astrocytes (ONHAs). Treatment of ONHAs with (+)-pentazocine attenuated the level and duration of stress-induced ERK phosphorylation following oxidative stress exposure and promoted survival of ONHAs. These effects were specific to S1R activation because they were not observed in ONHAs that were depleted of S1R using siRNA-mediated knockdown. Collectively, our results suggest that S1R activation suppresses ERK1/2 phosphorylation and protects ONHAs from oxidative stress-induced death.
[Mh] Termos MeSH primário: Astrócitos/metabolismo
Nervo Óptico/metabolismo
Receptores sigma/metabolismo
[Mh] Termos MeSH secundário: Analgésicos Opioides/farmacologia
Animais
Astrócitos/efeitos dos fármacos
Células Cultivadas
Células HeLa
Seres Humanos
Proteína Quinase 1 Ativada por Mitógeno/metabolismo
Proteína Quinase 3 Ativada por Mitógeno/metabolismo
Nervo Óptico/citologia
Estresse Oxidativo
Pentazocina/farmacologia
Ratos
Ratos Sprague-Dawley
Receptores sigma/agonistas
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Analgesics, Opioid); 0 (Receptors, sigma); 0 (sigma-1 receptor); EC 2.7.11.24 (Mitogen-Activated Protein Kinase 1); EC 2.7.11.24 (Mitogen-Activated Protein Kinase 3); RP4A60D26L (Pentazocine)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171012
[Lr] Data última revisão:
171012
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170913
[St] Status:MEDLINE
[do] DOI:10.1371/journal.pone.0184421


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[PMID]:28549090
[Au] Autor:Ellis DZ; Li L; Park Y; He S; Mueller B; Yorio T
[Ad] Endereço:Department of Pharmaceutical Sciences, University of North Texas Systems College of Pharmacy, University of North Texas Health Science Center, Fort Worth, Texas, United States 2North Texas Eye Research Institute, University of North Texas Health Science Center, Fort Worth, Texas, United States.
[Ti] Título:Sigma-1 Receptor Regulates Mitochondrial Function in Glucose- and Oxygen-Deprived Retinal Ganglion Cells.
[So] Source:Invest Ophthalmol Vis Sci;58(5):2755-2764, 2017 May 01.
[Is] ISSN:1552-5783
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Purpose: Understanding the role of mitochondria in retinal ganglion cells (RGCs) is relevant to human disease as studies have shown mitochondrial abnormalities in primary open-angle glaucoma patients. This study seeks to determine the effects of the sigma-1 receptor (σ-1r) and its agonists on mitochondrial function in oxygen- and glucose- deprived (OGD) purified neonatal RGCs. Methods: Retinal ganglion cells were isolated from rat pups and subjected to OGD in varying conditions in the presence or absence of σ-1r agonist and antagonist and following addition of an AAV2-σ-1r vector that was used to increase σ-1r expression. Western blots and immunofluorescence microscopy validated findings. Mitochondrial function was determined by measuring mitochondrial membrane potential (Δψm) using the dye, fluorescence tetraethylbenzimidazolylcarbocyanineiodide (JC-1), and determination of cytochrome c oxidase activity using a cytochrome c oxidase assay kit. Caspase 3 and 7 activities were also measured using a luminescent assay kit. Results: Oxygen and glucose deprivation in RGCs resulted in decreased mitochondrial membrane potential and cytochrome c oxidase activity when compared with normoxic RGCs. σ-1r agonists or overexpression of the σ-1r restored the mitochondrial membrane potential comparable to normoxic conditions, while σ-1r antagonists abolished these effects. Oxygen and glucose depreavtation induced decreases in cytochrome c activity were partially restored by overexpression or activation of σ-1r. Caspase activity was increased in response to OGD and was decreased by the addition of σ-1r agonist, pentazocine, and following σ-1r overexpression. Conclusions: These data suggest that activation and/or overexpression of σ-1r restores RGCs mitochondrial function following OGD and that mitochondrial function is vital to the function of RGCs.
[Mh] Termos MeSH primário: Glucose/metabolismo
Mitocôndrias/fisiologia
Oxigênio/metabolismo
Receptores sigma/metabolismo
Células Ganglionares da Retina/metabolismo
[Mh] Termos MeSH secundário: Animais
Animais Recém-Nascidos
Benzimidazóis/farmacologia
Western Blotting
Carbocianinas/farmacologia
Caspase 3/metabolismo
Caspase 7/metabolismo
Hipóxia Celular/fisiologia
Dependovirus/genética
Complexo IV da Cadeia de Transporte de Elétrons/metabolismo
Vetores Genéticos
Potencial da Membrana Mitocondrial/fisiologia
Microscopia de Fluorescência
Pentazocina/farmacologia
Ratos
Ratos Sprague-Dawley
Receptores sigma/agonistas
Receptores sigma/antagonistas & inibidores
Células Ganglionares da Retina/efeitos dos fármacos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Benzimidazoles); 0 (Carbocyanines); 0 (Receptors, sigma); 0 (sigma-1 receptor); 21527-78-6 (5,5',6,6'-tetrachloro-1,1',3,3'-tetraethylbenzimidazolocarbocyanine); EC 1.9.3.1 (Electron Transport Complex IV); EC 3.4.22.- (Casp3 protein, rat); EC 3.4.22.- (Caspase 3); EC 3.4.22.- (Caspase 7); IY9XDZ35W2 (Glucose); RP4A60D26L (Pentazocine); S88TT14065 (Oxygen)
[Em] Mês de entrada:1707
[Cu] Atualização por classe:170717
[Lr] Data última revisão:
170717
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170527
[St] Status:MEDLINE
[do] DOI:10.1167/iovs.16-19199


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[PMID]:28544475
[Au] Autor:Kokornaczyk AK; Schepmann D; Yamaguchi J; Itami K; Laurini E; Fermeglia M; Pricl S; Wünsch B
[Ad] Endereço:Institut für Pharmazeutische und Medizinische Chemie der, Universität Münster, Corrensstraße 48, 48149, Münster, Germany.
[Ti] Título:Thiazole-Based σ Receptor Ligands: Diversity by Late-Stage C-H Arylation of Thiazoles, Structure-Affinity and Selectivity Relationships, and Molecular Interactions.
[So] Source:ChemMedChem;12(13):1070-1080, 2017 Jul 06.
[Is] ISSN:1860-7187
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:Spirocyclic thiophene derivatives represent promising σ ligands with high σ affinity and selectivity over the σ subtype. To increase ligand efficiency, the thiophene ring was replaced bioisosterically by a thiazole ring, and the pyran ring was opened. Late-stage diversification by regioselective C-H arylation of thiazoles 9 a-c resulted in a set of 53 compounds with high diversity. This set of compounds was analyzed with respect to σ affinity, σ /σ selectivity, lipophilicity (logD ), lipophilicity-corrected ligand efficiency (LELP), and molecular target interactions. The most promising candidates were pyridyl-substituted thiazole derivatives 33 c (2-(1-benzyl-4-ethoxypiperidin-4-yl)-5-(pyridin-3-yl)thiazole) and 34 c (2-(1-benzyl-4-ethoxypiperidin-4-yl)-5-(pyridin-4-yl)thiazole), possessing low-nanomolar σ affinity (K =1.3 and 1.9 nm), high σ /σ selectivity (>1500-fold), low lipophilicity (logD =1.8) and very good ligand efficiency (LELP=5.5), indicating promising pharmacodynamics and pharmacokinetics. Molecular simulation studies, including docking and deconvolution of the free binding energy into its major components, led to decreased hydrophobic stabilization of pyridyl derivatives 33 c and 34 c, which was compensated by lower desolvation energy.
[Mh] Termos MeSH primário: Piperidinas/farmacologia
Piridinas/farmacologia
Receptores sigma/metabolismo
Tiazóis/farmacologia
[Mh] Termos MeSH secundário: Animais
Guanidinas/farmacologia
Cobaias
Haloperidol/farmacologia
Ligantes
Microssomos Hepáticos/metabolismo
Simulação de Acoplamento Molecular
Pentazocina/farmacologia
Piperidinas/síntese química
Piperidinas/química
Piridinas/síntese química
Piridinas/química
Ratos
Tiazóis/síntese química
Tiazóis/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Guanidines); 0 (Ligands); 0 (Piperidines); 0 (Pyridines); 0 (Receptors, sigma); 0 (Thiazoles); 0 (sigma-1 receptor); J6292F8L3D (Haloperidol); LL2P01I17O (1,3-ditolylguanidine); RP4A60D26L (Pentazocine)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170929
[Lr] Data última revisão:
170929
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170526
[St] Status:MEDLINE
[do] DOI:10.1002/cmdc.201700166


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[PMID]:28364693
[Au] Autor:Gasparre G; Abate C; Carlucci R; Berardi F; Cassano G
[Ad] Endereço:Department of Biosciences, Biotechnologies and Biopharmaceutics, Università di Bari, Bari, Italy.
[Ti] Título:The σ receptor agonist (+)-pentazocine increases store-operated Ca entry in MCF7σ and SK-N-SH cell lines.
[So] Source:Pharmacol Rep;69(3):542-545, 2017 Jun.
[Is] ISSN:1734-1140
[Cp] País de publicação:Poland
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: The intracellular [Ca ] is modulated by σ receptors. An important component of the cellular machinery governing the intracellular [Ca ] is Store-Operated Calcium Entry (SOCE). Here we want to investigate whether ligands of σ receptors affect SOCE. METHODS: The intracellular [Ca ] was monitored, with the fluorescent Ca -sensitive probe Fura-2, in four cell lines with a different expression of σ receptors, namely MCF7 (expressing σ receptors with a low density and overexpressing σ receptors), MCF7σ (overexpressing σ receptors), SK-N-SH, and HT-29. RESULTS: When thapsigargin was used to deplete intracellular Ca stores, in a Ca -free incubation medium, the Ca influx (following Ca re-addition) was significantly increased by 1µM (+)-pentazocine (σ receptor agonist) in MCF7σ (by 22.5%) and SK-N-SH (by 45.6%), but not in HT-29 and MCF7 cells. We have used, as a second approach, the "Mn quenching" protocol. In MCF7σ cells, after thapsigargin treatment, the fluorescence quenching induced by Mn influx (evidence of Ca influx) was significantly increased (by 25.8%) by 1µM (+)-pentazocine, significantly decreased (by 18.0%) by BD1063 (σ receptor antagonist), and not affected by the presence of both ligands. These effects were not observed in MCF7 cells. Finally, in MCF7 cells, 1µM PB28 (σ receptor agonist), did not affect both the Ca response after Ca re-addition and the fluorescence quenching induced by Mn influx. CONCLUSIONS: We propose that the σ receptor agonist (+)-pentazocine increases SOCE in MCF7σ and SK-N-SH cell lines. The σ receptor agonist PB28 does not affect SOCE in MCF7 cells.
[Mh] Termos MeSH primário: Analgésicos Opioides/farmacologia
Cálcio/metabolismo
Pentazocina/farmacologia
Receptores sigma/agonistas
[Mh] Termos MeSH secundário: Linhagem Celular Tumoral
Fluorescência
Células HT29
Seres Humanos
Ligantes
Células MCF-7
Neuroblastoma/metabolismo
Receptores sigma/metabolismo
Tapsigargina/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Analgesics, Opioid); 0 (Ligands); 0 (Receptors, sigma); 67526-95-8 (Thapsigargin); RP4A60D26L (Pentazocine); SY7Q814VUP (Calcium)
[Em] Mês de entrada:1711
[Cu] Atualização por classe:171107
[Lr] Data última revisão:
171107
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170402
[St] Status:MEDLINE


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[PMID]:28163081
[Au] Autor:Heiss K; Raffaele M; Vanella L; Murabito P; Prezzavento O; Marrazzo A; Aricò G; Castracani CC; Barbagallo I; Zappalà A; Avola R; Li Volti G
[Ad] Endereço:Department of Biomedical and Biotechnological Sciences, University of Catania, Via S. Sofia 64, 95100 Catania, Italy.
[Ti] Título:(+)-Pentazocine attenuates SH-SY5Y cell death, oxidative stress and microglial migration induced by conditioned medium from activated microglia.
[So] Source:Neurosci Lett;642:86-90, 2017 Mar 06.
[Is] ISSN:1872-7972
[Cp] País de publicação:Ireland
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Sigma receptors (σ R) are expressed both in neurons and microglia and can be considered as a promising target for developing pharmacological strategies for neuroprotection in various experimental models. The aim of the present study was to test the effect of (+)-pentazocine, a putative σ R agonist, in an in vitro model of neuron/microglia crosstalk following hypoxia/reoxygenation. METHODS: Microglia (BV2 cells) was exposed (3h) to 1% oxygen and reoxygenation was allowed for 24h. Conditioned media obtained from this experimental condition was used to treat neuroblast-like cell line (SH-SY5Y cells) in the presence or absence of (+)-pentazocine (25µM). Cell viability was measured by cytofluorimetric analysis, whereas inflammation and oxidative stress were evaluated by the expression of Hsp70, GAD, SOD and p65. Microglial cell migration was also evaluated by Xcelligence technology. RESULTS: Our results showed that (+)-pentazocine was able to increase SH-SY5Y cell viability following exposure to microglial-conditioned medium. Furthermore, (+)-pentazocine was also able to inhibit microglial cell toward neuron treated with hypoxic conditioned medium. Finally, pharmacological treatment reduced the expression of inflammatory and oxidative stress markers (GAD, SOD and p65). Interestingly, hypoxic medium was able to reduce the expression of Hsp70 and such effect was prevented by (+)-pentazocine treatment. CONCLUSIONS: (+)-Pentazocine exhibits significant neuroprotective effects in our in vitro model of SH-SY5Y/microglial crosstalk thus suggesting that σ R may represent a possible strategy for neuroprotection.
[Mh] Termos MeSH primário: Morte Celular/efeitos dos fármacos
Movimento Celular/efeitos dos fármacos
Microglia/metabolismo
Neurônios/efeitos dos fármacos
Estresse Oxidativo/efeitos dos fármacos
Pentazocina/farmacologia
Receptores sigma/agonistas
[Mh] Termos MeSH secundário: Analgésicos Opioides/farmacologia
Linhagem Celular
Sobrevivência Celular/efeitos dos fármacos
Meios de Cultivo Condicionados
Seres Humanos
Neurônios/metabolismo
Fármacos Neuroprotetores/farmacologia
Espécies Reativas de Oxigênio/metabolismo
Superóxido Dismutase/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Analgesics, Opioid); 0 (Culture Media, Conditioned); 0 (Neuroprotective Agents); 0 (Reactive Oxygen Species); 0 (Receptors, sigma); EC 1.15.1.1 (Superoxide Dismutase); RP4A60D26L (Pentazocine)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170908
[Lr] Data última revisão:
170908
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170207
[St] Status:MEDLINE


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[PMID]:27984382
[Au] Autor:Dhooria S; Sehgal IS; Gupta N; Aggarwal AN; Behera D; Agarwal R
[Ad] Endereço:Departments of *Pulmonary Medicine †Cytology, Postgraduate Institute of Medical Education and Research (PGIMER), Chandigarh, India.
[Ti] Título:Diagnostic Yield and Complications of EBUS-TBNA Performed Under Bronchoscopist-directed Conscious Sedation: Single Center Experience of 1004 Subjects.
[So] Source:J Bronchology Interv Pulmonol;24(1):7-14, 2017 Jan.
[Is] ISSN:1948-8270
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Endobronchial ultrasound-guided transbronchial needle aspiration (EBUS-TBNA) can be performed under either conscious sedation or general anesthesia. Herein, we describe the diagnostic yield and complications of EBUS-TBNA performed under bronchoscopist-directed conscious sedation. METHODS: This is a retrospective analysis of data collected in the bronchoscopy suite of this center on EBUS-TBNA or endoscopic ultrasound with a bronchoscope-guided fine needle aspiration (EUS-B-FNA) procedures performed between July 2011 and January 2016. All procedures were performed under bronchoscopist-directed conscious sedation with midazolam and pentazocine. The diagnostic yield, sample adequacy rate, complications, and doses of sedative agents are presented. RESULTS: Of the total 1005 EBUS-TBNA/EUS-B-FNA procedures performed during the study period, 1004 were performed under conscious sedation in spontaneously breathing subjects [mean (SD) age, 45.9 (15.8) years; 378 (37.6%) women]. The mean (SD) doses of midazolam and pentazocine used were 2.53 (1.8) mg and 30.9 (6.9) mg, respectively. The diagnostic yield of the procedure (972 subjects) was 61.2%. Complications related to EBUS were observed in 60 (5.9%) subjects. Majority of them were minor and self-limiting; major complications occurred in 11 (1.1%) subjects and included respiratory failure requiring assisted ventilation (n=6), arrhythmia (n=3), and hypotension (n=2). Escalation of the level of care was needed in only 8 (0.8%) subjects. CONCLUSION: EBUS-TBNA/EUS-B-FNA performed under bronchoscopist-guided conscious sedation was found to be safe and is associated with a reasonable diagnostic yield.
[Mh] Termos MeSH primário: Broncoscopia/métodos
Sedação Consciente/instrumentação
Aspiração por Agulha Fina Guiada por Ultrassom Endoscópico/efeitos adversos
Linfonodos/patologia
[Mh] Termos MeSH secundário: Adulto
Feminino
Seres Humanos
Masculino
Mediastino
Midazolam/administração & dosagem
Meia-Idade
Pentazocina/administração & dosagem
Estudos Retrospectivos
Sensibilidade e Especificidade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
R60L0SM5BC (Midazolam); RP4A60D26L (Pentazocine)
[Em] Mês de entrada:1705
[Cu] Atualização por classe:170530
[Lr] Data última revisão:
170530
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161217
[St] Status:MEDLINE


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[PMID]:27569039
[Au] Autor:Motonobu A; Hidemichi Y; Eri U; Takashi T; Kenichi K
[Ad] Endereço:Oral and Maxillofacial Surgery, Gamagori City Hospital, Gamagori City, Aichi-Pref, Japan.
[Ti] Título:Cohort study of pain symptoms and management following impacted mandibular third molar extraction.
[So] Source:Oral Dis;23(1):78-83, 2017 Jan.
[Is] ISSN:1601-0825
[Cp] País de publicação:Denmark
[La] Idioma:eng
[Ab] Resumo:OBJECTIVE: The aim of this study was to investigate the possibility of intravenous sedation as a useful pain-relieving option for impacted third molar extractions. SUBJECTS AND METHODS: A prospective cohort study was conducted among patients who underwent bilateral mandibular third molar extractions under local anaesthesia and intravenous sedation (sedation group) and patients who underwent unilateral mandibular third molar extraction under local anaesthesia alone (local anaesthesia group). The frequency of use of postoperative oral analgesia and the intensity of pain assessed using the full cup test were compared between the two groups. RESULTS: The maximum pain intensity (0-100) on postoperative day 1 in the sedation and local anaesthesia groups was 72.8 ± 16.98 and 84.8 ± 15.84, respectively, and the mean pain intensity was 42.2 ± 16.00 and 49.6 ± 18.94. The maximum and mean pain intensities in the sedation group were significantly milder than those in the local anaesthesia group. The number of oral analgesic doses in the sedation group was significantly smaller on the day of surgery and on postoperative day 1 than in the local anaesthesia group. CONCLUSIONS: The results of this study suggest that bilateral impacted mandibular third molar extractions under intravenous sedation could be a recommended treatment option.
[Mh] Termos MeSH primário: Dor Facial/etiologia
Dente Serotino/cirurgia
Manejo da Dor/métodos
Extração Dentária/efeitos adversos
Dente Impactado/cirurgia
[Mh] Termos MeSH secundário: Administração Intravenosa
Adulto
Analgésicos Opioides/administração & dosagem
Analgésicos Opioides/uso terapêutico
Sedação Consciente/métodos
Dor Facial/tratamento farmacológico
Feminino
Seres Humanos
Masculino
Medição da Dor
Dor Pós-Operatória/tratamento farmacológico
Pentazocina/administração & dosagem
Pentazocina/uso terapêutico
[Pt] Tipo de publicação:CLINICAL TRIAL; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Analgesics, Opioid); RP4A60D26L (Pentazocine)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170922
[Lr] Data última revisão:
170922
[Sb] Subgrupo de revista:D
[Da] Data de entrada para processamento:160830
[St] Status:MEDLINE
[do] DOI:10.1111/odi.12576


  9 / 2183 MEDLINE  
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[PMID]:27504867
[Au] Autor:van Niel JC; Schneider J; Tzschentke TM
[Ad] Endereço:Grünenthal GmbH, Global Late Stage Clinical Development, Aachen, Germany.
[Ti] Título:Efficacy of Full µ-Opioid Receptor Agonists is not Impaired by Concomitant Buprenorphine or Mixed Opioid Agonists/Antagonists - Preclinical and Clinical Evidence.
[So] Source:Drug Res (Stuttg);66(11):562-570, 2016 Nov.
[Is] ISSN:2194-9387
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:Buprenorphine and the mixed agonists/antagonists nalbuphine and pentazocine, formerly classified as µ-opioid (MOP) receptor antagonists, have more recently been shown to be partial to full agonists of the human MOP receptor. These receptors do not necessarily have to be maximally activated for a full physiological response. Partial agonists can also sufficiently stimulate signaling processes leading to a full analgesic response, as shown by the effectiveness of buprenorphine, nalbuphine and pentazocine in animal pain models and in clinical settings where these drugs induce analgesia with full efficacy without a ceiling effect. Submaximal doses of MOP receptor analgesics combined with submaximal doses of buprenorphine, pentazocine, or nalbuphine result in additive to over-additive antinociceptive effects in animal experiments. Only when doses are given that exceed the therapeutic dose range may the antinociceptive effect be reduced to the effect of either opioid alone. The analgesic effects of pentazocine and nalbuphine combined with morphine are reported to be additive or over-additive in various clinical pain conditions. Buprenorphine, which clinically behaves as a full MOP receptor agonist for pain relief, can be combined with full opioid agonists without precipitating withdrawal. Thus, the overall evidence on the analgesic effects of buprenorphine, pentazocine or nalbuphine combined with opioid analgesics under various clinical pain conditions contradicts the consensus that these compounds diminish MOP receptor analgesia when co-administered with a full MOP receptor agonist.
[Mh] Termos MeSH primário: Analgésicos Opioides/farmacologia
Analgésicos Opioides/uso terapêutico
Buprenorfina/farmacologia
Buprenorfina/uso terapêutico
Antagonistas de Entorpecentes/farmacologia
Antagonistas de Entorpecentes/uso terapêutico
[Mh] Termos MeSH secundário: Animais
Seres Humanos
Nalbufina/farmacologia
Nalbufina/uso terapêutico
Dor/tratamento farmacológico
Pentazocina/farmacologia
Pentazocina/uso terapêutico
Receptores Opioides/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Analgesics, Opioid); 0 (Narcotic Antagonists); 0 (Receptors, Opioid); 40D3SCR4GZ (Buprenorphine); L2T84IQI2K (Nalbuphine); RP4A60D26L (Pentazocine)
[Em] Mês de entrada:1703
[Cu] Atualização por classe:170330
[Lr] Data última revisão:
170330
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160810
[St] Status:MEDLINE


  10 / 2183 MEDLINE  
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Fotocópia
[PMID]:27382814
[Au] Autor:Olateju SO; Adenekan AT; Olufolabi AJ; Owojuyigbe AM; Adetoye AO; Ajenifuja KO; Olowookere SA; Faponle AF
[Ti] Título:PENTAZOCINE VERSUS PENTAZOCINE WITH RECTAL DICLOFENAC FOR POSTOPERATIVE PAIN RELIEF AFTER CESAREAN SECTION- A DOUBLE BLIND RANDOMIZED PLACEBO CONTROLLED TRIAL IN A LOW RESOURCE AREA.
[So] Source:Middle East J Anaesthesiol;23(4):443-8, 2016 Feb.
[Is] ISSN:0544-0440
[Cp] País de publicação:Lebanon
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: The unimodal approach of using pentazocine as post-cesarean section pain relief is inadequate, hence the need for a safer, easily available and more effective multimodal approach. AIM: To evaluate the effectiveness of rectal diclofenac combined with intramuscular pentazocine for postoperative pain following cesarean section. METHODS: In this double blind clinical trial, 130 pregnant women scheduled for cesarean section under spinal anesthesia were randomly assigned to two groups. Group A received 100mg diclofenac suppository and group B received placebo suppository immediately following surgery, 12 and 24h later. Both groups also received intramuscular pentazocine 30mg immediately following surgery and 6 hourly postoperatively in the first 24 h. Postoperative pain was assessed by visual analogue scale at end of surgery and 2, 12 and 24 h after surgery. Patient satisfaction scores were also assessed. RESULTS: One hundred and sixteen patients completed the study. Combining diclofenac and pentazocine had statistically significant reduction in pain intensity at 2, 12, and 24 hours postoperatively compared to pentazocine alone (p <0.05). No significant side effects were noted in both groups. The combined group also had significantly better patient satisfaction scores. CONCLUSION: The addition of diclofenac suppository to intramuscular pentazocine provides better pain relief after cesarean section and increased patient satisfaction.
[Mh] Termos MeSH primário: Analgésicos Opioides/uso terapêutico
Anti-Inflamatórios não Esteroides/administração & dosagem
Diclofenaco/administração & dosagem
Dor Pós-Operatória/tratamento farmacológico
Pentazocina/uso terapêutico
[Mh] Termos MeSH secundário: Adulto
Método Duplo-Cego
Feminino
Recursos em Saúde
Seres Humanos
Satisfação do Paciente
Pentazocina/administração & dosagem
Gravidez
Supositórios
Escala Visual Analógica
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE; RANDOMIZED CONTROLLED TRIAL
[Nm] Nome de substância:
0 (Analgesics, Opioid); 0 (Anti-Inflammatory Agents, Non-Steroidal); 0 (Suppositories); 144O8QL0L1 (Diclofenac); RP4A60D26L (Pentazocine)
[Em] Mês de entrada:1608
[Cu] Atualização por classe:160706
[Lr] Data última revisão:
160706
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160708
[St] Status:MEDLINE



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