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[PMID]:29223098
[Au] Autor:Figueiredo J; Serrano JL; Cavalheiro E; Keurulainen L; Yli-Kauhaluoma J; Moreira VM; Ferreira S; Domingues FC; Silvestre S; Almeida P
[Ad] Endereço:CICS-UBI - Health Sciences Research Centre, University of Beira Interior, 6200-506 Covilhã, Portugal; Department of Chemistry, University of Beira Interior, 6201-001 Covilhã, Portugal.
[Ti] Título:Trisubstituted barbiturates and thiobarbiturates: Synthesis and biological evaluation as xanthine oxidase inhibitors, antioxidants, antibacterial and anti-proliferative agents.
[So] Source:Eur J Med Chem;143:829-842, 2018 Jan 01.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:Barbituric and thiobarbituric acid derivatives have become progressively attractive to medicinal chemists due to their wide range of biological activities. Herein, different series of 1,3,5-trisubstituted barbiturates and thiobarbiturates were prepared in moderate to excellent yields and their activity as xanthine oxidase inhibitors, antioxidants, antibacterial agents and as anti-proliferative compounds was evaluated in vitro. Interesting bioactive barbiturates were found namely, 1,3-dimethyl-5-[1-(2-phenylhydrazinyl)ethylidene]pyrimidine-2,4,6(1H,3H,5H)-trione (6c) and 1,3-dimethyl-5-[1-[2-(4-nitrophenyl)hydrazinyl]ethylidene]pyrimidine-2,4,6(1H,3H,5H)-trione (6e), which showed concomitant xanthine oxidase inhibitory effect (IC values of 24.3 and 27.9 µM, respectively), and 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activity (IC values of 18.8 and 23.8 µM, respectively). In addition, 5-[1-(2-phenylhydrazinyl)ethylidene]pyrimidine-2,4,6(1H,3H,5H)-trione (6d) also revealed DPPH radical scavenger effect, with an IC value of 20.4 µM. Moreover, relevant cytotoxicity against MCF-7 cells (IC = 13.3 µM) was observed with 5-[[(2-chloro-4-nitrophenyl)amino]methylene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione (7d). Finally, different 5-hydrazinylethylidenepyrimidines revealed antibacterial activity against Acinetobacter baumannii (MIC values between 12.5 and 25.0 µM) which paves the way for developing new treatments for infections caused by this Gram-negative coccobacillus bacterium, known to be an opportunistic pathogen in humans with high relevance in multidrug-resistant nosocomial infections. The most promising bioactive barbiturates were studied in silico with emphasis on compliance with the Lipinski's rule of five as well as several pharmacokinetics and toxicity parameters.
[Mh] Termos MeSH primário: Antibacterianos/farmacologia
Antineoplásicos/farmacologia
Antioxidantes/farmacologia
Bactérias/efeitos dos fármacos
Barbitúricos/farmacologia
Inibidores Enzimáticos/farmacologia
Xantina Oxidase/antagonistas & inibidores
[Mh] Termos MeSH secundário: Antibacterianos/síntese química
Antibacterianos/química
Antineoplásicos/síntese química
Antineoplásicos/química
Antioxidantes/síntese química
Antioxidantes/química
Bactérias/crescimento & desenvolvimento
Barbitúricos/síntese química
Barbitúricos/química
Proliferação Celular/efeitos dos fármacos
Relação Dose-Resposta a Droga
Ensaios de Seleção de Medicamentos Antitumorais
Inibidores Enzimáticos/síntese química
Inibidores Enzimáticos/química
Seres Humanos
Células MCF-7
Testes de Sensibilidade Microbiana
Estrutura Molecular
Relação Estrutura-Atividade
Células Tumorais Cultivadas
Xantina Oxidase/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Bacterial Agents); 0 (Antineoplastic Agents); 0 (Antioxidants); 0 (Barbiturates); 0 (Enzyme Inhibitors); EC 1.17.3.2 (Xanthine Oxidase)
[Em] Mês de entrada:1801
[Cu] Atualização por classe:180101
[Lr] Data última revisão:
180101
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171210
[St] Status:MEDLINE


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[PMID]:28449418
[Au] Autor:Haase VH
[Ad] Endereço:Department of Medicine, Vanderbilt University Medical Center, Nashville, Tennessee, USA.
[Ti] Título:HIF-prolyl hydroxylases as therapeutic targets in erythropoiesis and iron metabolism.
[So] Source:Hemodial Int;21 Suppl 1:S110-S124, 2017 Jun.
[Is] ISSN:1542-4758
[Cp] País de publicação:Canada
[La] Idioma:eng
[Ab] Resumo:A classic response to systemic hypoxia is the increase in red blood cell production. This response is controlled by the prolyl hydroxylase domain/hypoxia-inducible factor (HIF) pathway, which regulates a broad spectrum of cellular functions. The discovery of this pathway as a key regulator of erythropoiesis has led to the development of small molecules that stimulate the production of endogenous erythropoietin and enhance iron metabolism. This review provides a concise overview of the cellular and molecular mechanisms that govern HIF-induced erythropoietic responses and provides an update on clinical experience with compounds that target HIF-prolyl hydroxylases for anemia therapy.
[Mh] Termos MeSH primário: Eritropoese/efeitos dos fármacos
Prolina Dioxigenases do Fator Induzível por Hipóxia/fisiologia
Ferro/metabolismo
Inibidores de Prolil-Hidrolase/uso terapêutico
[Mh] Termos MeSH secundário: Anemia/tratamento farmacológico
Barbitúricos/efeitos adversos
Barbitúricos/uso terapêutico
Ensaios Clínicos como Assunto
Eritropoetina/biossíntese
Glicina/efeitos adversos
Glicina/análogos & derivados
Glicina/uso terapêutico
Seres Humanos
Isoquinolinas/efeitos adversos
Isoquinolinas/uso terapêutico
Ácidos Picolínicos/efeitos adversos
Ácidos Picolínicos/uso terapêutico
Diálise Renal/efeitos adversos
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Barbiturates); 0 (EPO protein, human); 0 (FG-4592); 0 (GSK1278863); 0 (Isoquinolines); 0 (Picolinic Acids); 0 (Prolyl-Hydroxylase Inhibitors); 0 (vadadustat); 11096-26-7 (Erythropoietin); E1UOL152H7 (Iron); EC 1.14.11.29 (Hypoxia-Inducible Factor-Proline Dioxygenases); TE7660XO1C (Glycine)
[Em] Mês de entrada:1712
[Cu] Atualização por classe:171214
[Lr] Data última revisão:
171214
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170428
[St] Status:MEDLINE
[do] DOI:10.1111/hdi.12567


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[PMID]:28881285
[Au] Autor:Yilmaz VT; Icsel C; Batur J; Aydinlik S; Sahinturk P; Aygun M
[Ad] Endereço:Department of Chemistry, Faculty of Arts and Sciences, Uludag University, 16059 Bursa, Turkey. Electronic address: vtyilmaz@uludag.edu.tr.
[Ti] Título:Structures and biochemical evaluation of silver(I) 5,5-diethylbarbiturate complexes with bis(diphenylphosphino)alkanes as potential antimicrobial and anticancer agents.
[So] Source:Eur J Med Chem;139:901-916, 2017 Oct 20.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:New silver(I) 5,5-diethylbarbiturate (barb) complexes with a series of bis(diphenylphosphino)alkanes such as 1,1-bis(diphenylphosphino)methane (dppm), 1,2-bis(diphenylphosphino)ethane (dppe), 1,3-bis(diphenylphosphino)propane (dppp) and 1,4-bis(diphenylphosphino)butane (dppb) were synthesized and characterized. [Ag (barb) (µ-dppm) ] (1), [Ag (barb) (µ-dppe)(DMSO) ] (2) and [Ag (barb) (µ-dppp) ] (3) were binuclear, while [Ag(barb)(µ-dppb)] (4) was a coordination polymer. 1-4 effectively bind to the G/C rich region of the major groove of DNA and interact with BSA via hydrophobic interactions in accordance with molecular docking studies. All complexes displayed significant DNA cleavage in the presence of H O . 1-4 exhibited more specificity against Gram-positive bacteria than Gram-negative bacteria, but 2 targets both bacterial strains, being comparable to AgNO and silver sulfadiazine. Complex 1 has a strong growth inhibitory effect on A549 cells, while 2 and 3 exhibit considerable cytotoxicity against MCF-7 cells. The complexes showed high accumulation in the cytosol fraction of the cells. Mechanistic studies showed that 1 and 2 display effective cell growth inhibition by triggering S and G2/M phase arrest, induce apoptosis via mitochondrial pathways and also damage to DNA due to the overproduction of ROS.
[Mh] Termos MeSH primário: Antibacterianos/farmacologia
Antineoplásicos/farmacologia
Barbitúricos/farmacologia
Complexos de Coordenação/farmacologia
Bactérias Gram-Negativas/efeitos dos fármacos
Bactérias Gram-Positivas/efeitos dos fármacos
Prata/farmacologia
[Mh] Termos MeSH secundário: Antibacterianos/síntese química
Antibacterianos/química
Antineoplásicos/síntese química
Antineoplásicos/química
Barbitúricos/química
Proliferação Celular/efeitos dos fármacos
Complexos de Coordenação/síntese química
Complexos de Coordenação/química
Relação Dose-Resposta a Droga
Ensaios de Seleção de Medicamentos Antitumorais
Seres Humanos
Testes de Sensibilidade Microbiana
Simulação de Acoplamento Molecular
Estrutura Molecular
Prata/química
Relação Estrutura-Atividade
Células Tumorais Cultivadas
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Bacterial Agents); 0 (Antineoplastic Agents); 0 (Barbiturates); 0 (Coordination Complexes); 3M4G523W1G (Silver)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171016
[Lr] Data última revisão:
171016
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170908
[St] Status:MEDLINE


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[PMID]:28878016
[Au] Autor:Yu Z; Cohen JB
[Ad] Endereço:From the Department of Neurobiology, Harvard Medical School, Boston, Massachusetts 02115.
[Ti] Título:Enantiomeric barbiturates bind distinct inter- and intrasubunit binding sites in a nicotinic acetylcholine receptor (nAChR).
[So] Source:J Biol Chem;292(42):17258-17271, 2017 Oct 20.
[Is] ISSN:1083-351X
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Nicotinic acetylcholine receptors (nAChRs) and γ-aminobutyric acid type A receptors (GABA Rs) are members of the pentameric ligand-gated ion channel superfamily. Drugs acting as positive allosteric modulators of muscle-type α ßγδ nAChRs, of use in treatment of neuromuscular disorders, have been hard to identify. However, identification of nAChR allosteric modulator binding sites has been facilitated by using drugs developed as photoreactive GABA R modulators. Recently, 1-methyl-5-allyl-5-( -trifluoromethyl-diazirinylphenyl) barbituric acid ( TFD-MPAB), an anesthetic and GABA R potentiator, has been shown to inhibit α ßγδ nAChRs, binding in the ion channel and to a γ -α subunit interface site similar to its GABA R intersubunit binding site. In contrast, 1-methyl-5-propyl-5-( -trifluoromethyl-diazirinylphenyl) barbituric acid ( TFD-MPPB) acts as a convulsant and GABA R inhibitor. Photolabeling studies established that TFD-MPPB binds to the same GABA R intersubunit binding site as TFD-MPAB, but with negative rather than positive energetic coupling to GABA binding. We now show that TFD-MPPB binds with the same state (agonist) dependence as TFD-MPAB within the nAChR ion channel, but it does not bind to the intersubunit binding site. Rather, TFD-MPPB binds to intrasubunit sites within the α and δ subunits, photolabeling αVal-218 (αM1), δPhe-232 (δM1), δThr-274 (δM2), and δIle-288 (δM3). Propofol, a general anesthetic that binds to GABA R intersubunit sites, inhibited [ H] TFD-MPPB photolabeling of these nAChR intrasubunit binding sites. These results demonstrate that in an nAChR, the subtle difference in structure between TFD-MPPB and TFD-MPAB (chirality; 5-propyl 5-allyl) determines selectivity for intra- intersubunit sites, in contrast to GABA Rs, where this difference affects state dependence of binding to a common site.
[Mh] Termos MeSH primário: Barbitúricos/química
Proteínas de Peixes/química
Receptores de GABA-A/química
Receptores Nicotínicos/química
[Mh] Termos MeSH secundário: Animais
Sítios de Ligação
Propofol/química
Subunidades Proteicas
Torpedo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Barbiturates); 0 (Fish Proteins); 0 (Protein Subunits); 0 (Receptors, GABA-A); 0 (Receptors, Nicotinic); YI7VU623SF (Propofol)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171028
[Lr] Data última revisão:
171028
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170908
[St] Status:MEDLINE
[do] DOI:10.1074/jbc.M117.808592


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[PMID]:28864149
[Au] Autor:Pianovich NA; Dean M; Lassak A; Reiss K; Jursic BS
[Ad] Endereço:Department of Chemistry, University of New Orleans, New Orleans, LA 70148, USA.
[Ti] Título:Anticancer potential of aminomethylidene-diazinanes I. Synthesis of arylaminomethylidene of diazinetriones and its cytotoxic effects tested in glioblastoma cells.
[So] Source:Bioorg Med Chem;25(19):5068-5076, 2017 Oct 01.
[Is] ISSN:1464-3391
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Diazinane and aryl moieties with vinylamine linkers were synthesized to investigate the importance of their structural variations as potential anti-glioblastoma agents. Structural variations incorporated on to the diazinane moiety included oxa and thio derivatives, each with a variety of nitrogen-bound substituents. The size and shape of the aromatic moiety was varied, with the final variation introducing two carbonyl groups, yielding a substituted anthraquinone. Readily available diazinanes and aryl amines were used asan advantageous foundation. Several parameters were calculated whilst engineering these compounds, including: ClogP, molecular polarizability, polar surface area, minimal molecular projected area, and pK . In addition, a simple and efficient procedure was developed to synthesize these compounds. It was demonstrated that a vinylamine with 1,3-diazinane-2,4,6-trione and 1-anthraquinone moiety is the most promising drug candidate causing almost 70% of LN229 tumor cell death at 1µg/ml. In addition, its molecular polarizability, polar surface area and minimal molecular projected area indicate a possible potential of this molecule for crossing BBB.
[Mh] Termos MeSH primário: Antraquinonas/química
Antraquinonas/farmacologia
Antineoplásicos/química
Antineoplásicos/farmacologia
Barbitúricos/química
Barbitúricos/farmacologia
Glioblastoma/tratamento farmacológico
[Mh] Termos MeSH secundário: Aminação
Antraquinonas/síntese química
Antineoplásicos/síntese química
Barbitúricos/síntese química
Morte Celular/efeitos dos fármacos
Linhagem Celular Tumoral
Ensaios de Seleção de Medicamentos Antitumorais
Seres Humanos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (5-(((9,10-dioxo-9,10-dihydroanthracen-1-yl)amino)methylidene)-1,3-diazinane-2,4,6-trione); 0 (Anthraquinones); 0 (Antineoplastic Agents); 0 (Barbiturates)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171016
[Lr] Data última revisão:
171016
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170903
[St] Status:MEDLINE


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[PMID]:28557718
[Au] Autor:Agulnik A; Kelly DP; Bruccoleri R; Yuskaitis C; Ebrahimi-Fakhari D; Sahin M; Burns MM; Kohane DS
[Ad] Endereço:Department of Global Pediatric Medicine and Division of Critical Care, St. Jude Children's Research Hospital, Memphis, Tennessee; and.
[Ti] Título:Combination Clearance Therapy and Barbiturate Coma for Severe Carbamazepine Overdose.
[So] Source:Pediatrics;139(5), 2017 May.
[Is] ISSN:1098-4275
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:A 15-year-old female subject presented comatose, in respiratory failure and shock, after the intentional ingestion of ∼280 extended-release 200-mg carbamazepine tablets with a peak serum concentration of 138 µg/mL (583.74 µmol/L). The patient developed clinical seizures and an EEG pattern of stimulus-induced rhythmic, periodic, or ictal discharges, suggestive of significant cortical dysfunction. Due to the extremely high drug serum concentration and clinical instability, a combination of therapies was used, including lipid emulsion therapy, plasmapheresis, hemodialysis, continuous venovenous hemodiafiltration, and endoscopic intestinal decontamination. The patient's elevated serum lactate level with a high mixed venous saturation suggested possible mitochondrial dysfunction, prompting treatment with barbiturate coma to reduce cerebral metabolic demand. The serum carbamazepine concentration declined steadily, with resolution of lactic acidosis, no long-term end-organ damage, and return to baseline neurologic function. The patient was eventually discharged in her usual state of health. In the laboratory, we demonstrated in vitro that the active metabolite of carbamazepine hyperpolarized the mitochondrial membrane potential, supporting the hypothesis that the drug caused mitochondrial dysfunction. We thus successfully treated a life-threatening carbamazepine overdose with a combination of modalities. Future studies are required to validate this aggressive approach. The occurrence of mitochondrial dysfunction must be confirmed in patients with carbamazepine toxicity and the need to treat it validated.
[Mh] Termos MeSH primário: Barbitúricos/envenenamento
Carbamazepina/envenenamento
Coma/induzido quimicamente
Terapia Combinada/métodos
Overdose de Drogas/terapia
[Mh] Termos MeSH secundário: Adolescente
Barbitúricos/sangue
Carbamazepina/sangue
Coma/terapia
Descontaminação/métodos
Feminino
Hemodiafiltração/métodos
Seres Humanos
Plasmaferese/métodos
Diálise Renal/métodos
[Pt] Tipo de publicação:CASE REPORTS; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Barbiturates); 33CM23913M (Carbamazepine)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:170803
[Lr] Data última revisão:
170803
[Sb] Subgrupo de revista:AIM; IM
[Da] Data de entrada para processamento:170531
[St] Status:MEDLINE


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[PMID]:28407198
[Au] Autor:Dudley K; Liu X; De Haan S
[Ad] Endereço:Institute of Mental Health, University of Nottingham, Nottingham, UK.
[Ti] Título:Chlorpromazine dose for people with schizophrenia.
[So] Source:Cochrane Database Syst Rev;4:CD007778, 2017 04 13.
[Is] ISSN:1469-493X
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: The World Health Organization (WHO) Model Lists of Essential Medicines lists chlorpromazine as one of its five medicines used in psychotic disorders. OBJECTIVES: To determine chlorpromazine dose response and dose side-effect relationships for schizophrenia and schizophrenia-like psychoses. SEARCH METHODS: We searched the Cochrane Schizophrenia Group's Study-Based Register of Trials (December 2008; 2 October 2014; 19 December 2016). SELECTION CRITERIA: All relevant randomised controlled trials (RCTs) comparing low doses of chlorpromazine (≤ 400 mg/day), medium dose (401 mg/day to 800 mg/day) or higher doses (> 800 mg/day) for people with schizophrenia, and which reported clinical outcomes. DATA COLLECTION AND ANALYSIS: We included studies meeting review criteria and providing useable data. Review authors extracted data independently. For dichotomous data, we calculated fixed-effect risk ratios (RR) and their 95% confidence intervals (CIs). For continuous data, we calculated mean differences (MD) and their 95% CIs based on a fixed-effect model. We assessed risk of bias for included studies and graded trial quality using GRADE (Grading of Recommendations Assessment, Development and Evaluation). MAIN RESULTS: As a result of searches undertaken in 2014, we found one new study and in 2016 more data for already included studies. Five relevant studies with 1132 participants (585 are relevant to this review) are now included. All are hospital-based trials and, despite over 60 years of chlorpromazine use, have durations of less than six months and all are at least at moderate risk of bias. We found only data on low-dose (≤ 400 mg/day) versus medium-dose chlorpromazine (401 mg/day to 800 mg/day) and low-dose versus high-dose chlorpromazine (> 800 mg/day).When low-dose chlorpromazine (≤ 400 mg/day) was compared to medium-dose chlorpromazine (401 mg/day to 800 mg/day), there was no clear benefit of one dose over the other for both global and mental state outcomes (low-quality and very low-quality evidence). There was also no clear evidence for people in one dosage group being more likely to leave the study early, over the other dosage group (moderate-quality evidence). Similar numbers of participants from each group experienced agitation and restlessness (very low-quality evidence). However, significantly more people in the medium-dose group (401 mg/day to 800 mg/day) experienced extrapyramidal symptoms in the short term (2 RCTS, n = 108, RR 0.47, 95% CI 0.30 to 0.74, moderate-quality evidence). No data for death were available.When low-dose chlorpromazine (≤ 400 mg/day) was compared to high-dose chlorpromazine (> 800 mg/day), data from one study with 416 patients were available. Clear evidence of a benefit of the high dose was found with regards to global state. The low-dose group had significantly fewer people improving (RR 1.13, 95% CI 1.01 to 1.25, moderate-quality evidence). There was also a marked difference between the number of people leaving the study from each group for any reason, with significantly more people leaving from the high-dose group (RR 0.60, 95% CI 0.40 to 0.89, moderate-quality evidence). More people in the low-dose group had to leave the study due to deterioration in behaviour (RR 2.70, 95% CI 1.34 to 5.44, low-quality evidence). There was clear evidence of a greater risk of people experiencing extrapyramidal symptoms in general in the high-dose group (RR 0.43, 95% CI 0.32 to 0.59, moderate-quality evidence). One death was reported in the high-dose group yet no effect was shown between the two dosage groups (RR 0.33, 95% CI 0.01 to 8.14, moderate-quality evidence). No data for mental state were available. AUTHORS' CONCLUSIONS: The dosage of chlorpromazine has changed drastically over the past 50 years with lower doses now being the preferred of choice. However, this change was gradual and arose not due to trial-based evidence, but due to clinical experience and consensus. Chlorpromazine is one of the most widely used antipsychotic drugs yet appropriate use of lower levels has come about after many years of trial and error with much higher doses. In the absence of high-grade evaluative studies, clinicians have had no alternative but to learn from experience. However, such an approach can lack scientific rigor and does not allow for proper dissemination of information that would assist clinicians find the optimum treatment dosage for their patients. In the future, data for recently released medication should be available from high-quality trials and studies to provide optimum treatment to patients in the shortest amount of time.
[Mh] Termos MeSH primário: Antipsicóticos/administração & dosagem
Clorpromazina/administração & dosagem
Esquizofrenia/tratamento farmacológico
[Mh] Termos MeSH secundário: Antipsicóticos/efeitos adversos
Barbitúricos/administração & dosagem
Hidrato de Cloral/administração & dosagem
Clorpromazina/efeitos adversos
Esquema de Medicação
Seres Humanos
Hipnóticos e Sedativos/administração & dosagem
Pacientes Desistentes do Tratamento/estatística & dados numéricos
Ensaios Clínicos Controlados Aleatórios como Assunto
[Pt] Tipo de publicação:JOURNAL ARTICLE; META-ANALYSIS; REVIEW
[Nm] Nome de substância:
0 (Antipsychotic Agents); 0 (Barbiturates); 0 (Hypnotics and Sedatives); 418M5916WG (Chloral Hydrate); U42B7VYA4P (Chlorpromazine)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:170802
[Lr] Data última revisão:
170802
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170414
[St] Status:MEDLINE
[do] DOI:10.1002/14651858.CD007778.pub2


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[PMID]:28399085
[Au] Autor:Slustovskaya YV; Krys'ko MV; Strelova OY
[Ad] Endereço:Saint-Petersburg State Chemical and Pharmaceutical Academy, Saint-Petersburg, Russia, 197376.
[Ti] Título:[The development of the method for enzymatic hydrolysis for the extraction of toxic substances from the hair samples].
[Ti] Título:Razrabotka metodiki fermentativnogo gidroliza dlia izolirovaniia toksichnykh veshchestv iz obraztsov volos..
[So] Source:Sud Med Ekspert;60(2):36-40, 2017.
[Is] ISSN:0039-4521
[Cp] País de publicação:Russia (Federation)
[La] Idioma:rus
[Ab] Resumo:The objective of the present study was to develop and validate the method for the extraction of toxic substances from the hair samples as exemplified by enzymatic hydrolysis of barbituric acid derivatives. The experiments were carried out with the use of laboratory animals (white female rats and albino guinea pigs) that had been daily given a phenobarbital solution per os during 4 months preceding the study. The hairs obtained from the experimental animals were subjected to acid hydrolysis with a 6 mole hydrochloric acid and enzymatic hydrolysis with the use of chymopsin, trypsin, chymotrypsin, and papain solutions. The analysis of the extracted materials was performed by means of gas chromatography with mass-selective detection. The application of the proposed method for enzymatic hydrolysis produced the better results than acid hydrolysis. This technique was validated. The results of the study made possible the comparative characteristic of the effectiveness of acid and enzymatic hydrolysis.
[Mh] Termos MeSH primário: Barbitúricos
Toxicologia Forense/métodos
Cabelo/patologia
[Mh] Termos MeSH secundário: Animais
Barbitúricos/análise
Barbitúricos/toxicidade
Feminino
Cromatografia Gasosa-Espectrometria de Massas/métodos
Hidrólise
Hipnóticos e Sedativos/análise
Hipnóticos e Sedativos/toxicidade
Ratos
Reprodutibilidade dos Testes
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Barbiturates); 0 (Hypnotics and Sedatives)
[Em] Mês de entrada:1707
[Cu] Atualização por classe:170713
[Lr] Data última revisão:
170713
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170412
[St] Status:MEDLINE
[do] DOI:10.17116/sudmed201760236-40


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[PMID]:28399083
[Au] Autor:Kirichek AV; Shabalina AE; Rassinskaya LA
[Ad] Endereço:The 111 ,Main State Centre of Forensic Medical and Criminalistic Expertisees, Russian Ministry of Defense, Moscow, Russia, 105229.
[Ti] Título:[The identification of barbituric acid derivatives in the old blood stains on textiles].
[Ti] Título:Issledovanie proizvodnykh barbiturovoi kisloty v zastarelykh piatnakh krovi na tkaniakh..
[So] Source:Sud Med Ekspert;60(2):27-29, 2017.
[Is] ISSN:0039-4521
[Cp] País de publicação:Russia (Federation)
[La] Idioma:rus
[Ab] Resumo:Thus article was designed to report a few cases of the identification of barbituric acid derivatives in the old blood stains on the clothes and other textiles. The data presented give evidence that barbiturates are capable of persisting in dry blood stains during rather a long period. The authors emphasize the necessity of mandatory control investigations to avoid obtaining the false positive results.
[Mh] Termos MeSH primário: Barbitúricos/análise
Manchas de Sangue
[Mh] Termos MeSH secundário: Patologia Legal/métodos
Seres Humanos
Têxteis
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Barbiturates)
[Em] Mês de entrada:1707
[Cu] Atualização por classe:170713
[Lr] Data última revisão:
170713
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170412
[St] Status:MEDLINE
[do] DOI:10.17116/sudmed201760227-29


  10 / 8440 MEDLINE  
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[PMID]:28387807
[Au] Autor:Liu Y; Uboh CE; Li X; Guan F; You Y; Maylin GA; Zhu F; Soma LR
[Ad] Endereço:Department of Clinical Studies, University of Pennsylvania School of Veterinary Medicine, New Bolton Center Campus, 382 West Street Road, Kennett Square, PA 19348, USA.
[Ti] Título:Validated LC-MS-MS Method for Simultaneous Analysis of 17 Barbiturates in Horse Plasma for Doping Control.
[So] Source:J Anal Toxicol;41(5):431-440, 2017 Jun 01.
[Is] ISSN:1945-2403
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:A rapid and sensitive method for simultaneous screening, quantification and confirmation of 17 barbiturates in horse plasma using liquid chromatography-tandem mass spectrometry is described. Analytes were recovered from plasma by liquid-liquid extraction using methyl tert-butyl ether, separated on a C18 column, and analyzed in negative electrospray ionization mode. Multiple-reaction monitoring was employed for screening and quantification. Confirmation for the presence of the analytes was achieved by comparing ion intensity ratio. The ranges for limits of detection, quantification and confirmation were 0.003-1 ng/mL (S/N ≥ 3), 0.01-2.5 ng/mL and 0.02-5 ng/mL, respectively. The linear dynamic range of the method was 0.1-100 ng/mL. The precision and accuracy at 0.5, 5 and 50 ng/mL of all 17 barbiturates during intra-day assay were 1.6-8.6% and 96-106%, respectively. For inter-day assay, precision and accuracy at the same three concentrations were 2.6-8.9% and 96-106%, respectively. Analysis of all 17 analytes was completed within 7 min. Thus, the present method is fast, simple, sensitive and reproducibly reliable.
[Mh] Termos MeSH primário: Barbitúricos/sangue
Doping nos Esportes
Detecção do Abuso de Substâncias/métodos
[Mh] Termos MeSH secundário: Animais
Cavalos
Extração Líquido-Líquido
Éteres Metílicos
Plasma
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Barbiturates); 0 (Methyl Ethers); 29I4YB3S89 (methyl tert-butyl ether)
[Em] Mês de entrada:1707
[Cu] Atualização por classe:170721
[Lr] Data última revisão:
170721
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170408
[St] Status:MEDLINE
[do] DOI:10.1093/jat/bkx025



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