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[PMID]:29442035
[Au] Autor:Incecayir T; Ilbasmis-Tamer S; Tirnaksiz F; Degim T
[Ti] Título:Assessment of the potential drug-drug interaction between carvedilol and clopidogrel mediated through intestinal P-glycoprotein.
[So] Source:Pharmazie;71(8):472-477, 2016 08 01.
[Is] ISSN:0031-7144
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:The most widely prescribed oral antiplatelet agent, clopidogrel, shows high interindividual variability resulting in an increased risk of cardiovascular events in the patients with reduced platelet inhibition. The purpose of this study was to investigate the role of the P-glycoprotein (P-gp) efflux pump in limiting the intestinal permeability of clopidogrel and the effect of a ß-blocker, namely, carvedilol, on its intestinal transport. Effective permeabilities (Peff) of clopidogrel and carvedilol were investigated in the proximal jejunum and distal ileum of rats using an in situ intestinal perfusion model. Peff values of clopidogrel and carvedilol were found to be concentration dependent with decreased Peff values at the low perfusate concentrations. Coperfusion with the P-gp inhibitors verapamil (100 µM) and carvedilol (10 µM) significantly increased the Peff of clopidogrel in the jejunum (8.31±0.20 x 10-5 and 6.98±0.75 x 10-5 vs. 3.60±0.51 x 10-5, respectively) and ileum (9.08±2.19 x 10-5 and 8.35±1.58 x 10-5 vs. 3.85±0.15 x 10-5, respectively). However, at the highest concentration tested (30 µM), clopidogrel exhibited 3 and 1.4 times higher Peff than those of metoprolol, an FDA high permeability reference standard, in the jejunum and ileum, respectively. Overall, this study indicates that the efflux function appears not to have a significant impact on the in vivo intestinal absorption of clopidogrel due to the saturation of P-gp, suggesting no clinically relevant interaction between carvedilol and clopidogrel mediated through P-gp at intestinal level.
[Mh] Termos MeSH primário: Membro 1 da Subfamília B de Cassetes de Ligação de ATP/efeitos dos fármacos
Antagonistas Adrenérgicos beta/farmacologia
Carbazóis/farmacologia
Intestino Delgado/efeitos dos fármacos
Inibidores da Agregação de Plaquetas/farmacologia
Propanolaminas/farmacologia
Ticlopidina/análogos & derivados
[Mh] Termos MeSH secundário: Membro 1 da Subfamília B de Cassetes de Ligação de ATP/antagonistas & inibidores
Animais
Interações Medicamentosas
Absorção Intestinal/efeitos dos fármacos
Intestino Delgado/metabolismo
Masculino
Metoprolol/farmacologia
Perfusão
Permeabilidade/efeitos dos fármacos
Ratos
Ratos Wistar
Ticlopidina/farmacologia
Verapamil/farmacologia
[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 (Carbazoles); 0 (Platelet Aggregation Inhibitors); 0 (Propanolamines); 0K47UL67F2 (carvedilol); A74586SNO7 (clopidogrel); CJ0O37KU29 (Verapamil); GEB06NHM23 (Metoprolol); OM90ZUW7M1 (Ticlopidine)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180307
[Lr] Data última revisão:
180307
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180215
[St] Status:MEDLINE
[do] DOI:10.1691/ph.2016.6059


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[PMID]:29189539
[Au] Autor:Joo J; Kim J; Lee J
[Ad] Endereço:Department of Anesthesiology and Pain Medicine, Seoul St. Mary's Hospital, College of Medicine, The Catholic University of Korea, Seoul, Republic of Korea.
[Ti] Título:Effect of Continuous Systemic Administration of Esmolol on Intraocular Pressure During Surgery in a Sustained Steep Trendelenburg Position.
[So] Source:J Glaucoma;26(12):1068-1071, 2017 Dec.
[Is] ISSN:1536-481X
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:PURPOSE: To investigate the effects of continuous systemic administration of esmolol on intraocular pressure (IOP) during laparoscopic and robotic surgeries for recto-sigmoid cancer in a steep Trendelenburg position. MATERIALS AND METHODS: A total of 50 patients undergoing laparoscopic surgery in a steep Trendelenburg position were included. Patients in the esmolol (E) group received a 0.25 mg/kg IV loading dose of esmolol before anesthesia, followed by an infusion of 15 µg/kg/min throughout the operation. Patients in the saline (S) group were infused with the same volume of normal saline. IOP and ocular perfusion pressure were measured 16 times: before anesthetic induction (T1), before administration of the study drug (T2), after administration of anesthetic induction agents (T3), after tracheal intubation (T4), 1, 3, 5, and 10 minutes after tracheal intubation (T5-T8), immediately after intraperitoneal CO2 insufflation (T9), immediately after the steep Trendelenburg position (T10), 1, 2, and 4 hours after the steep Trendelenburg position (T11-T13), just before the supine position (T14), and 10 and 30 minutes after the supine position (T15, T16). RESULTS: The IOP increased markedly after adopting the steep Trendelenburg position, reaching 28.8±4.4 mm Hg in group S. The IOP at T13 in group S was ∼5.7 mm Hg higher than in group E. The IOP at T13 was ∼10.6 mm Hg higher than in T1 in group S, but only ∼4.4 mm Hg higher than in group E. CONCLUSIONS: Continuous systemic administration of esmolol can alleviate the increase in IOP during a sustained steep Trendelenburg position without adverse cardiovascular effects.
[Mh] Termos MeSH primário: Neoplasias Colorretais/cirurgia
Decúbito Inclinado com Rebaixamento da Cabeça
Pressão Intraocular/efeitos dos fármacos
Laparoscopia/métodos
Propanolaminas/administração & dosagem
Procedimentos Cirúrgicos Robóticos
[Mh] Termos MeSH secundário: Antagonistas de Receptores Adrenérgicos beta 1/administração & dosagem
Relação Dose-Resposta a Droga
Feminino
Seguimentos
Seres Humanos
Infusões Intravenosas
Masculino
Meia-Idade
Estudos Prospectivos
Tonometria Ocular
Resultado do Tratamento
[Pt] Tipo de publicação:JOURNAL ARTICLE; RANDOMIZED CONTROLLED TRIAL
[Nm] Nome de substância:
0 (Adrenergic beta-1 Receptor Antagonists); 0 (Propanolamines); MDY902UXSR (esmolol)
[Em] Mês de entrada:1712
[Cu] Atualização por classe:171226
[Lr] Data última revisão:
171226
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171201
[St] Status:MEDLINE
[do] DOI:10.1097/IJG.0000000000000746


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[PMID]:29049251
[Au] Autor:Kao MC; Tzeng IS; Chan HL
[Ad] Endereço:aDepartment of Anesthesiology, Taipei Tzu Chi Hospital, Buddhist Tzu Chi Medical Foundation, New Taipei City bSchool of Medicine, Tzu Chi University, Hualien cDepartment of Research, Taipei Tzu Chi Hospital, Buddhist Tzu Chi Medical Foundation, New Taipei City dDepartment of Electrical Engineering, Chang Gung University, Taoyuan eNeuroscience Research Center, Chang Gung Memorial Hospital, Linkou, Taiwan.
[Ti] Título:Esmolol pretreatment attenuates heart rate increase and parasympathetic inhibition during rapid increases in desflurane concentration: A preliminary randomized study.
[So] Source:Medicine (Baltimore);96(42):e8340, 2017 Oct.
[Is] ISSN:1536-5964
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Rapid increases in desflurane concentration can transiently increase the heart rate (HR). Esmolol possesses a high ß1-adrenoceptor selectivity and a short duration of action. This preliminary study aimed at investigating the effects of esmolol on the HR and autonomic modulation during a desflurane-induced HR increase. METHODS: American Society of Anesthesiologists physical status I female subjects, aged 20 to 50 years, who were undergoing minor breast surgery were randomly assigned to 2 groups. Rapid increases in desflurane concentration were commenced after induction of anesthesia. Each subject received either i.v. saline (control group) or esmolol 0.5 mg/kg (esmolol group) before desflurane inhalation. Using time-frequency spectral analysis of HR variability, the HR indices were studied at baseline, postinduction, posttreatment, as well as at minimal alveolar concentrations of desflurane reaching 1.0, 1.3, and 1.5. The low frequency (LF) power is influenced by both the sympathetic and parasympathetic activity, whereas the high frequency (HF) power reflects the parasympathetic activity. The LF/HF ratio is thought to reflect either sympathovagal balance or sympathetic modulation. RESULTS: Electrocardiograms for data analysis were obtained from 8 subjects in each group. Rapid increases in desflurane concentration after induction caused a HR increase. Both the corresponding LF and HF powers were low and the LF/HF ratio remained unchanged. This indicates that the desflurane-induced HR increase may be attributed to parasympathetic inhibition and may be independent of sympathetic activation. Esmolol pretreatment effectively attenuated desflurane-induced HR increase. Moreover, subjects receiving esmolol pretreatment had increased LF and HF powers, but did not have changes in their LF/HF ratios, as compared to those without esmolol. CONCLUSION: Esmolol pretreatment attenuates HR increase and parasympathetic inhibition during rapid increases in desflurane concentration.
[Mh] Termos MeSH primário: Anestésicos Inalatórios/efeitos adversos
Frequência Cardíaca/efeitos dos fármacos
Isoflurano/análogos & derivados
Sistema Nervoso Parassimpático/efeitos dos fármacos
Propanolaminas/farmacologia
[Mh] Termos MeSH secundário: Adulto
Eletrocardiografia
Feminino
Seres Humanos
Isoflurano/efeitos adversos
Meia-Idade
Estudos Prospectivos
Adulto Jovem
[Pt] Tipo de publicação:JOURNAL ARTICLE; RANDOMIZED CONTROLLED TRIAL
[Nm] Nome de substância:
0 (Anesthetics, Inhalation); 0 (Propanolamines); CRS35BZ94Q (desflurane); CYS9AKD70P (Isoflurane); MDY902UXSR (esmolol)
[Em] Mês de entrada:1711
[Cu] Atualização por classe:171122
[Lr] Data última revisão:
171122
[Sb] Subgrupo de revista:AIM; IM
[Da] Data de entrada para processamento:171020
[St] Status:MEDLINE
[do] DOI:10.1097/MD.0000000000008340


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[PMID]:28965949
[Au] Autor:Pu J; Zhang X; Luo H; Xu L; Lu X; Lu J
[Ad] Endereço:Department of General Surgery, Tangdu Hospital of the Fourth Military Medical University, Xi'an 710038, PR China.
[Ti] Título:Adrenaline promotes epithelial-to-mesenchymal transition via HuR-TGFß regulatory axis in pancreatic cancer cells and the implication in cancer prognosis.
[So] Source:Biochem Biophys Res Commun;493(3):1273-1279, 2017 Nov 25.
[Is] ISSN:1090-2104
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Psychological stress has recently been described as a risk factor in the development of pancreatic cancer. Here, we reported that increased neurotransmitter adrenaline was associated with the poor survival in pancreatic cancer patients. Moreover, in the cell model study, we found adrenaline promoted pancreatic cell PANC-1 migration in a dose dependent manner. Block of the ß2-adrenoreceptor with ICI118,551, significantly reduced cell migration. Further study found that adrenaline induced a cytoplasmic translocation of RNA binding protein HuR, which in turn activated TGFß, as shown by the SBE luciferase assay and phosphorylation of Smad2/3. Either HuR knockdown or TGFß inhibition reduced cell migration induced by adrenaline. Taken together, our study here revealed that adrenaline-HuR-TGFß regulatory axis at least partially contributes to the psychological stress induced metastasis in PANC-1 cells, shedding light on therapeutic targeting psychological stress in improving the prognosis of pancreatic cancer.
[Mh] Termos MeSH primário: Proteína Semelhante a ELAV 1/metabolismo
Epinefrina/metabolismo
Neoplasias Pancreáticas/metabolismo
Neoplasias Pancreáticas/patologia
Fator de Crescimento Transformador beta/metabolismo
[Mh] Termos MeSH secundário: Antagonistas Adrenérgicos beta/farmacologia
Idoso
Linhagem Celular Tumoral
Movimento Celular
Proteína Semelhante a ELAV 1/genética
Epinefrina/sangue
Transição Epitelial-Mesenquimal/fisiologia
Feminino
Seres Humanos
Estimativa de Kaplan-Meier
Masculino
Meia-Idade
Neoplasias Pancreáticas/mortalidade
Propanolaminas/farmacologia
Receptores Adrenérgicos beta 2/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Adrenergic beta-Antagonists); 0 (ELAV-Like Protein 1); 0 (ELAVL1 protein, human); 0 (Propanolamines); 0 (Receptors, Adrenergic, beta-2); 0 (Transforming Growth Factor beta); 46OL1UC10R (ICI 118551); YKH834O4BH (Epinephrine)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171027
[Lr] Data última revisão:
171027
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171003
[St] Status:MEDLINE


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[PMID]:28891709
[Au] Autor:Kónyi A
[Ad] Endereço:Klinikai Központ, Szívgyógyászati Klinika, Pécsi Tudományegyetem, Általános Orvostudományi Kar Pécs, Ifjúság u. 13., 7623.
[Ti] Título:[Carvedilol in the everyday interventional cardiology practice].
[Ti] Título:Carvedilol alkalmazása a mindennapi kardiológiai és intervenciós kardiológiai gyakorlatban..
[So] Source:Orv Hetil;158(37):1453-1457, 2017 Sep.
[Is] ISSN:0030-6002
[Cp] País de publicação:Hungary
[La] Idioma:hun
[Ab] Resumo:The treatment of severe coronary stenoses with stent implantation is very effective nevertheless, the underlying problem of atherosclerosis remains unsolved with the implantation of a stent. Therefore, besides lifestyle changes, the adequate medication therapy is of pivotal importance. In the majority of patients scheduled for or acutely undergoing catheterisation, beta-blockers form the basis of medication therapy. Members of the group, however, show significant differences in terms of pharmacodynamics. The third-generation beta-blocker and vasodilator carvedilol possesses complex adrenerg-blocking and Ca-channel blocking effects as well. In the background of the favourable effects, a further positive property is its anti-free-radical effect which most beta-blockers do not have. Therefore, as has been proven by several studies, it provides considerable benefits in hypertension, after myocardial infarction, in diabetes and also in the treatment of patients with cardiac failure. These positive effects have been markedly observed in interventional cardiology practice, as the majority of patients undergoing cardiac catheterisation have hypertension, diabetes or hyperlipidaemia. Its anti-free-radical effect is especially beneficial together with its smooth muscle proliferation-inhibitor effect which may favourably affect in-stent restenosis (ISR) as well. To summarise, due to its vasculoprotective effect, carvedilol is an ideal drug of choice following stent implantation in routine everyday practice. Orv Hetil. 2017; 158(37): 1453-1457.
[Mh] Termos MeSH primário: Carbazóis/uso terapêutico
Doença da Artéria Coronariana/tratamento farmacológico
Propanolaminas/uso terapêutico
Vasodilatadores/uso terapêutico
[Mh] Termos MeSH secundário: Angioplastia Coronária com Balão
Cardiologia
Terapia Combinada
Doença da Artéria Coronariana/terapia
Seres Humanos
Stents
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Carbazoles); 0 (Propanolamines); 0 (Vasodilator Agents); 0K47UL67F2 (carvedilol)
[Em] Mês de entrada:1711
[Cu] Atualização por classe:171109
[Lr] Data última revisão:
171109
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170912
[St] Status:MEDLINE
[do] DOI:10.1556/650.2017.30812


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[PMID]:28882337
[Au] Autor:Li J; Chen Z; Gao X; Zhang H; Xiong W; Ju J; Xu H
[Ad] Endereço:Graduate School, Beijing University of Chinese Medicine, Beijing, China.
[Ti] Título:Meta-Analysis Comparing Metoprolol and Carvedilol on Mortality Benefits in Patients With Acute Myocardial Infarction.
[So] Source:Am J Cardiol;120(9):1479-1486, 2017 Nov 01.
[Is] ISSN:1879-1913
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Although carvedilol, a nonselective beta-blocker with alpha-adrenergic blocking and multiple ancillary activities, has been demonstrated to be superior to metoprolol in chronic heart failure, it remains unclear whether the superiority of carvedilol still exists in myocardial infarction (MI). Therefore, we performed a network meta-analysis of randomized controlled trials (RCTs) to compare the 2 drugs in patients with MI. All RCTs that compared either 2 of the following interventions, carvedilol, metoprolol, and placebo, for the treatment of MI were included. The Cochrane Collaboration Central Register of Controlled Trials, Embase, and PubMed were searched thoroughly for potential eligible studies. Finally, 12 RCTs involving 61,081 patients were included. Pooled results showed that compared with placebo, carvedilol and metoprolol significantly reduced composite cardiovascular events (risk ratio [RR] 0.63; 95% credible interval [CrI] 0.41, 0.85 for carvedilol; RR 0.78; 95% CrI 0.65, 0.93 for metoprolol) and re-infarction (RR 0.57; 95% CrI 0.37, 0.84 for carvedilol; RR 0.77; 95% CrI 0.62, 0.91 for metoprolol) in patients with MI. However, neither carvedilol nor metoprolol showed significant benefits on all-cause death, cardiovascular death, revascularization, and rehospitalization. Also, no obvious difference was found when comparing carvedilol and metoprolol on primary or secondary outcomes. In conclusion, there is insufficient evidence supporting the superiority of carvedilol over metoprolol for the treatment of MI. Further studies are needed to confirm our findings.
[Mh] Termos MeSH primário: Antagonistas de Receptores Adrenérgicos alfa 1/uso terapêutico
Antagonistas de Receptores Adrenérgicos beta 1/uso terapêutico
Carbazóis/uso terapêutico
Metoprolol/uso terapêutico
Infarto do Miocárdio/mortalidade
Propanolaminas/uso terapêutico
[Mh] Termos MeSH secundário: Idoso
Feminino
Seres Humanos
Masculino
Meia-Idade
Infarto do Miocárdio/tratamento farmacológico
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE; META-ANALYSIS
[Nm] Nome de substância:
0 (Adrenergic alpha-1 Receptor Antagonists); 0 (Adrenergic beta-1 Receptor Antagonists); 0 (Carbazoles); 0 (Propanolamines); 0K47UL67F2 (carvedilol); GEB06NHM23 (Metoprolol)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171020
[Lr] Data última revisão:
171020
[Sb] Subgrupo de revista:AIM; IM
[Da] Data de entrada para processamento:170909
[St] Status:MEDLINE


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[PMID]:28843854
[Au] Autor:Ensho T; Maruyama K; Mori K; Miyazato M; Kangawa K; Nakahara K; Murakami N
[Ad] Endereço:Department of Veterinary Physiology, Faculty of Agriculture, University of Miyazaki, Miyazaki 889-2192, Japan.
[Ti] Título:Neuromedin U precursor-related peptide (NURP) exerts neuromedin U-like sympathetic nerve action in the rat.
[So] Source:Biochem Biophys Res Commun;492(3):412-418, 2017 Oct 21.
[Is] ISSN:1090-2104
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:It has been suggested that novel peptide that is produced from the neuromedin U (NMU) precursor may exist, as this precursor contains multiple consensus sequences for proteolytic processing. Recently, we identified two mature novel peptides comprising 33 and 36 residues in the rat brain, which were designated neuromedin U precursor-related peptide (NURP) 33 and 36. In the present study, we compared the roles of NURP33 and 36 with that of NMU, as neither activates the NMU receptors. Immunoreactivity for NMU and NURPs was widely present in the central nervous system and showed a similar distribution. Intracerebroventricular (icv) injection of NURP33 in rats increased locomotor activity, energy expenditure, heart rate and back surface temperature (BS-T), similarly to NMU or NURP36. NMU treatment reduced food intake, but NURP33 did not. Pretreatment with the ß3 blocker, SR59230A, and the cyclooxygenase blocker, indomethacin, inhibited the NURP33- or NMU-induced increase of BS-T. In addition, icv injection of NURP33 or NMU increased the expression of mRNA for cyclooxygenase 2 in the hypothalamus and for uncoupling protein 1 in the brown adipose tissue. These results suggest that although NURP33 and 36 do not activate the NMU receptors, they might exert NMU-like sympathetic nerve action in the brain.
[Mh] Termos MeSH primário: Neuropeptídeos/química
Neuropeptídeos/metabolismo
Fragmentos de Peptídeos/química
Fragmentos de Peptídeos/farmacologia
Sistema Nervoso Simpático/efeitos dos fármacos
[Mh] Termos MeSH secundário: Animais
Ingestão de Alimentos/efeitos dos fármacos
Indometacina/farmacologia
Infusões Intraventriculares
Masculino
Propanolaminas/farmacologia
Ratos
Ratos Wistar
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (3-(2-ethylphenoxy)-1-(1,2,3,4-tetrahydronaphth-1-ylamino)-2-propanol oxalate); 0 (Neuropeptides); 0 (Peptide Fragments); 0 (Propanolamines); 117505-80-3 (neuromedin U); XXE1CET956 (Indomethacin)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171024
[Lr] Data última revisão:
171024
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170828
[St] Status:MEDLINE


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[PMID]:28827152
[Au] Autor:Kawai S; Yamada T; Matsuura T; Funao T; Nishikawa K
[Ad] Endereço:Department of Anesthesiology, Osaka City University Graduate School of Medicine, Japan.
[Ti] Título:Neuropathic pain attenuates ischemia reperfusion injury through ß2-adrenergic pathway.
[So] Source:Life Sci;187:9-16, 2017 Oct 15.
[Is] ISSN:1879-0631
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:AIMS: The relationship between neuropathic pain and myocardial infarction (MI) was uncertain because of some medication or underlying diseases. This study investigated the impact of neuropathic pain on ischemia reperfusion injury using isolated rat hearts and cardiomyocytes. MAIN METHODS: Male Sprague-Dawley rats were assigned to the control and allodynia (AL) groups, with the latter subjected to the fifth lumbar spinal-nerve ligation. First, isolated hearts underwent 25-min ischemia and 90-min reperfusion to assess hemodynamic changes and MI area. Second, isolated cardiomyocytes underwent 10-min laser illumination to assess the opening of mitochondrial permeability transition pore (mPTP) and cellular hypercontraction. Lastly, expression of pro-survival kinases was measured in another cardiomyocytes using flow cytometry. AL-treated hearts were concomitantly examined regarding the involvement of ß-adrenergic pathways by esmolol (ESM), ß1-blocker (100µM, AL+ESM), and ICI118551 (ICI), ß2-blocker (50nM, AL+ICI). KEY FINDINGS: All hemodynamic variables did not change significantly in between-group comparisons except at 30min of reperfusion. MI area decreased remarkably in the AL and AL+ESM groups after 90-min reperfusion. The AL+ICI group significantly increased it as compared with the AL and AL+ESM groups. Similarly, the AL and AL+ESM groups significantly inhibited mPTP opening and cellular hypercontraction, whereas the AL+ICI group reversed these effects. Enhanced expression of pro-survival kinases was observed in the AL and AL+ESM groups, but the AL+ICI group abolished this enhancement. SIGNIFICANCE: Our findings suggested that neuropathic pain possessed cardioprotective effects through inhibiting mPTP opening. The underlying mechanisms were possibly regulated by ß2-adrenergic activation and pro-survival kinase expression in cardiomyocytes.
[Mh] Termos MeSH primário: Proteínas de Transporte da Membrana Mitocondrial/efeitos dos fármacos
Infarto do Miocárdio/patologia
Neuralgia/metabolismo
Propanolaminas/farmacologia
Traumatismo por Reperfusão/prevenção & controle
[Mh] Termos MeSH secundário: Antagonistas de Receptores Adrenérgicos beta 1/farmacologia
Antagonistas de Receptores Adrenérgicos beta 2/farmacologia
Animais
Hemodinâmica/efeitos dos fármacos
Hemodinâmica/fisiologia
Hiperalgesia/patologia
Hiperalgesia/prevenção & controle
Preparação de Coração Isolado
Ligadura
Masculino
Proteínas de Transporte da Membrana Mitocondrial/metabolismo
Infarto do Miocárdio/fisiopatologia
Miócitos Cardíacos/metabolismo
Neuralgia/complicações
Fosfotransferases/efeitos dos fármacos
Fosfotransferases/metabolismo
Fatores de Proteção
Ratos
Medula Espinal
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Adrenergic beta-1 Receptor Antagonists); 0 (Adrenergic beta-2 Receptor Antagonists); 0 (Mitochondrial Membrane Transport Proteins); 0 (Propanolamines); 0 (mitochondrial permeability transition pore); 46OL1UC10R (ICI 118551); EC 2.7.- (Phosphotransferases); MDY902UXSR (esmolol)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170921
[Lr] Data última revisão:
170921
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170823
[St] Status:MEDLINE


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[PMID]:28803116
[Au] Autor:da Silva ATM; de Oliveira HL; Silva CF; Fonseca MC; Pereira TFD; Nascimento CS; de Figueiredo EC; Borges KB
[Ad] Endereço:Departamento de Ciências Naturais, Universidade Federal de São João del-Rei (UFSJ), Campus Dom Bosco, Praça Dom Helvécio 74, Fábricas, 36301-160, São João del-Rei, Minas Gerais, Brazil.
[Ti] Título:Efficient molecularly imprinted polymer as a pipette-tip solid-phase sorbent for determination of carvedilol enantiomers in human urine.
[So] Source:J Chromatogr B Analyt Technol Biomed Life Sci;1061-1062:399-410, 2017 Sep 01.
[Is] ISSN:1873-376X
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:In this work, an efficient pipette tip based on molecularly imprinted polymers solid-phase extraction (PT-MIP-SPE) method was developed for carvedilol (CAR) analysis. This compound is available in clinical practice as a racemic mixture, in which (-)-(S)-CAR is a ß- and α -adrenergic antagonist, while (+)-(R)-CAR only acts as an α -adrenergic antagonist. Enantioseparation of CAR presented satisfactory retention times (5.85 and 14.84min), acceptable theoretical plates (N=2048 and 2018) and good resolution (Rs=9.27). The separation was performed using a Chiralpak IA column (100mm×4.6mm, 3µm), a mixture of methanol:ethanol:water (64:15:21, v/v/v) plus 0.3% diethylamine as mobile phase, temperature of 35°C and flow rate of 1.5mLmin . After density functional theory calculations based on prepolymerization complexes, the best protocol for the MIP synthesis was chosen. Then, some parameters that affect the PT-MIP-SPE technique were investigated. After optimization, the best conditions were 300µL of water as washing solvent, 500µL of acetonitrile:acetic acid (7:3, v/v) as eluting solvent, 20mg of MIP, 500µL of urine sample (pH 12.5) and no addition of NaCl. Recoveries±relative standard deviation (RSD%) for (+)-(R)-CAR and (-)-(S)-CAR were 101.9±4.8% and 104.6±2.1%, respectively. The method was linear over the concentration range from 20 to 1280ngmL for each enantiomer, with correlation coefficients larger than 0.99 for both enantiomers. The method was applied successfully in a preliminary study of urinary excretion after administration of CAR racemate to a healthy volunteer.
[Mh] Termos MeSH primário: Carbazóis/química
Carbazóis/urina
Impressão Molecular/métodos
Propanolaminas/química
Propanolaminas/urina
Extração em Fase Sólida/métodos
[Mh] Termos MeSH secundário: Cromatografia Líquida de Alta Pressão
Seres Humanos
Limite de Detecção
Modelos Lineares
Reprodutibilidade dos Testes
Estereoisomerismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Carbazoles); 0 (Propanolamines); 0K47UL67F2 (carvedilol)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170906
[Lr] Data última revisão:
170906
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170814
[St] Status:MEDLINE


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[PMID]:28763358
[Au] Autor:Ander F; Magnuson A; Berggren L; Ahlstrand R; de Leon A
[Ad] Endereço:From the *Department of Anesthesiology and Intensive Care and †Clinical Epidemiology and Biostatistics, School of Medical Sciences, Örebro University, Örebro, Sweden.
[Ti] Título:Effects of Esmolol on the Esophagogastric Junction: A Double-Blind, Randomized, Crossover Study on 14 Healthy Volunteers.
[So] Source:Anesth Analg;125(4):1184-1190, 2017 Oct.
[Is] ISSN:1526-7598
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Passive regurgitation may occur throughout the perioperative period, increasing the risk for pulmonary aspiration and postoperative pulmonary complications. Hypnotics and opioids, especially remifentanil, that are used during anesthesia have been shown to decrease the pressure in the esophagogastric junction (EGJ), that otherwise acts as a barrier against passive regurgitation of gastric contents. Esmolol, usually used to counteract tachycardia and hypertension, has been shown to possess properties useful during general anesthesia. Like remifentanil, the ß-1-adrenoreceptor antagonist may be used to attenuate the stress reaction to tracheal intubation and to modify perioperative anesthetic requirements. It may also reduce the need for opioids in the postoperative period. Its action on the EGJ is however unknown.The aim of this trial was to compare the effects of esmolol and remifentanil on EGJ pressures in healthy volunteers, when administrated as single drugs. METHODS: Measurements of EGJ pressures were made in 14 healthy volunteers using high-resolution solid-state manometry. Interventions were administered in a randomized sequence and consisted of esmolol that was given IV as a bolus dose of 1 mg/kg followed by an infusion of 10 µg·kg·minute over 15 minutes, and remifentanil with target-controlled infusion of 4 ng/mL over 15 minutes. Interventions were separated by a 20-minute washout period. Analyses of EGJ pressures were performed at baseline, and during drug administration at 2 (T2) and 15 minutes (T15). The primary outcome was the inspiratory EGJ augmentation, while the inspiratory and expiratory EGJ pressures were secondary outcomes. RESULTS: There was no effect on inspiratory EGJ augmentation when comparing remifentanil and esmolol (mean difference -4.0 mm Hg [-9.7 to 1.7]; P= .15). In contrast, remifentanil significantly decreased both inspiratory and expiratory pressures compared to esmolol (-12.2 [-18.6 to -5.7]; P= .003 and -8.0 [-13.3 to -2.8]; P= .006). CONCLUSIONS: Esmolol, compared with remifentanil, does not affect EGJ function. This may be an advantage regarding passive regurgitation and esmolol may thus have a role to play in anesthesia where maintenance of EGJ barrier function is of outmost importance.
[Mh] Termos MeSH primário: Antagonistas de Receptores Adrenérgicos beta 1/farmacologia
Junção Esofagogástrica/efeitos dos fármacos
Junção Esofagogástrica/fisiologia
Propanolaminas/farmacologia
[Mh] Termos MeSH secundário: Adolescente
Adulto
Estudos Cross-Over
Método Duplo-Cego
Feminino
Seres Humanos
Masculino
Resultado do Tratamento
Adulto Jovem
[Pt] Tipo de publicação:JOURNAL ARTICLE; RANDOMIZED CONTROLLED TRIAL
[Nm] Nome de substância:
0 (Adrenergic beta-1 Receptor Antagonists); 0 (Propanolamines); MDY902UXSR (esmolol)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171004
[Lr] Data última revisão:
171004
[Sb] Subgrupo de revista:AIM; IM
[Da] Data de entrada para processamento:170802
[St] Status:MEDLINE
[do] DOI:10.1213/ANE.0000000000002339



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