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[PMID]:27443208
[Au] Autor:Boison JO; Dowling T; Johnson R; Kinar J
[Ad] Endereço:CFIA Saskatoon Laboratory, 116 Veterinary Road, Saskatoon, SK., Canada S7N 2R3.
[Ti] Título:Analysis of phenylbutazone residues in horse tissues with and without enzyme-hydrolysis by LC-MS/MS.
[So] Source:Drug Test Anal;8(5-6):535-8, 2016 May.
[Is] ISSN:1942-7611
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Phenylbutazone (PBZ) is permitted to be used for the treatment of musculoskeletal pain and inflammation in race horses but it is not approved for use in horses destined for human consumption. In a recent study initiated in our laboratory to study the disposition of PBZ and its oxyphenbutazone (OXPBZ) metabolite in equine tissues, we compared the effect of an additional enzymatic hydrolysis step with ß-glucuronidase on the results of the analysis for PBZ without enzymatic hydrolysis. Incurred tissue samples obtained from a female horse dosed with PBZ at 8.8 mg/kg for 3 days and sacrificed 6 days following the last administration were used for this study. Liver, kidney, and muscle tissues were collected, extracted, cleaned up on a silica-based solid-phase extraction (SPE) preceded by a weak-anion exchange SPE and analyzed with our in-house validated liquid chromatography-tandem mass spectrometry (LC-MS/MS) method for PBZ and OXPBZ. Addition of the hydrolysis step resulted in a significant increase in recovery of both PBZ and OXPBZ residues. © 2016 Her Majesty the Queen in Right of Canada. Drug Testing and Analysis © 2016 John Wiley & Sons, Ltd.
[Mh] Termos MeSH primário: Anti-Inflamatórios não Esteroides/análise
Resíduos de Drogas/análise
Cavalos/metabolismo
Oxifenilbutazona/análise
Fenilbutazona/análise
Espectrometria de Massas em Tandem/métodos
[Mh] Termos MeSH secundário: Animais
Anti-Inflamatórios não Esteroides/metabolismo
Anti-Inflamatórios não Esteroides/farmacocinética
Cromatografia Líquida/métodos
Resíduos de Drogas/metabolismo
Resíduos de Drogas/farmacocinética
Feminino
Contaminação de Alimentos/análise
Análise de Perigos e Pontos Críticos de Controle/métodos
Seres Humanos
Hidrólise
Rim/química
Rim/metabolismo
Fígado/química
Fígado/metabolismo
Músculos/química
Músculos/metabolismo
Oxifenilbutazona/metabolismo
Oxifenilbutazona/farmacocinética
Fenilbutazona/metabolismo
Fenilbutazona/farmacocinética
Extração em Fase Sólida/métodos
Distribuição Tecidual
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Inflammatory Agents, Non-Steroidal); GN5P7K3T8S (Phenylbutazone); H806S4B3NS (Oxyphenbutazone)
[Em] Mês de entrada:1702
[Cu] Atualização por classe:170222
[Lr] Data última revisão:
170222
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160723
[St] Status:MEDLINE
[do] DOI:10.1002/dta.2020


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[PMID]:23012453
[Au] Autor:Gold B; Pingle M; Brickner SJ; Shah N; Roberts J; Rundell M; Bracken WC; Warrier T; Somersan S; Venugopal A; Darby C; Jiang X; Warren JD; Fernandez J; Ouerfelli O; Nuermberger EL; Cunningham-Bussel A; Rath P; Chidawanyika T; Deng H; Realubit R; Glickman JF; Nathan CF
[Ad] Endereço:Department of Microbiology, Weill Cornell Medical College, New York, NY 10065, USA.
[Ti] Título:Nonsteroidal anti-inflammatory drug sensitizes Mycobacterium tuberculosis to endogenous and exogenous antimicrobials.
[So] Source:Proc Natl Acad Sci U S A;109(40):16004-11, 2012 Oct 02.
[Is] ISSN:1091-6490
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Existing drugs are slow to eradicate Mycobacterium tuberculosis (Mtb) in patients and have failed to control tuberculosis globally. One reason may be that host conditions impair Mtb's replication, reducing its sensitivity to most antiinfectives. We devised a high-throughput screen for compounds that kill Mtb when its replication has been halted by reactive nitrogen intermediates (RNIs), acid, hypoxia, and a fatty acid carbon source. At concentrations routinely achieved in human blood, oxyphenbutazone (OPB), an inexpensive anti-inflammatory drug, was selectively mycobactericidal to nonreplicating (NR) Mtb. Its cidal activity depended on mild acid and was augmented by RNIs and fatty acid. Acid and RNIs fostered OPB's 4-hydroxylation. The resultant 4-butyl-4-hydroxy-1-(4-hydroxyphenyl)-2-phenylpyrazolidine-3,5-dione (4-OH-OPB) killed both replicating and NR Mtb, including Mtb resistant to standard drugs. 4-OH-OPB depleted flavins and formed covalent adducts with N-acetyl-cysteine and mycothiol. 4-OH-OPB killed Mtb synergistically with oxidants and several antituberculosis drugs. Thus, conditions that block Mtb's replication modify OPB and enhance its cidal action. Modified OPB kills both replicating and NR Mtb and sensitizes both to host-derived and medicinal antimycobacterial agents.
[Mh] Termos MeSH primário: Anti-Inflamatórios não Esteroides/farmacologia
Resistência Microbiana a Medicamentos/efeitos dos fármacos
Ensaios de Triagem em Larga Escala/métodos
Mycobacterium tuberculosis/efeitos dos fármacos
Oxifenilbutazona/farmacologia
[Mh] Termos MeSH secundário: Animais
Cromatografia Líquida de Alta Pressão
Resistência Microbiana a Medicamentos/fisiologia
Ácidos Graxos/metabolismo
Feminino
Hidroxilação
Espectroscopia de Ressonância Magnética
Camundongos
Testes de Sensibilidade Microbiana
Mycobacterium tuberculosis/fisiologia
Oxifenilbutazona/metabolismo
Oxifenilbutazona/farmacocinética
Espécies Reativas de Nitrogênio/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Anti-Inflammatory Agents, Non-Steroidal); 0 (Fatty Acids); 0 (Reactive Nitrogen Species); H806S4B3NS (Oxyphenbutazone)
[Em] Mês de entrada:1212
[Cu] Atualização por classe:170220
[Lr] Data última revisão:
170220
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:120927
[St] Status:MEDLINE
[do] DOI:10.1073/pnas.1214188109


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[PMID]:22503874
[Au] Autor:Binil PS; Mary YS; Varghese HT; Panicker CY; Anoop MR; Manojkumar TK
[Ad] Endereço:Department of Chemistry, SN College, Kollam 691001, Kerala, India.
[Ti] Título:Infrared and Raman spectroscopic analyses and theoretical computation of 4-butyl-1-(4-hydroxyphenyl)-2-phenyl-3,5-pyrazolidinedione.
[So] Source:Spectrochim Acta A Mol Biomol Spectrosc;94:101-9, 2012 Aug.
[Is] ISSN:1873-3557
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Infrared and Raman spectroscopic analyses were carried out on 4-butyl-1-(4-hydroxyphenyl)-2-phenyl-3,5-pyrazolidinedione. The interpretation of the spectra was aided by DFT calculation of the molecule. The vibrational wavenumbers were examined theoretically using the Gaussian03 set of quantum chemistry codes and the normal modes were assigned by potential energy distribution calculations. A computation of the first hyperpolarizability of the compound indicates that the compound may be a good candidate as a NLO material. Optimized geometrical parameters are in agreement with the reported XRD results. The RMS error of the observed Raman bands and IR bands are found to be 35.09 and 39.57 for HF method and 14.31 and 17.17 for DFT method. The predicted infrared intensities and Raman activities are reported.
[Mh] Termos MeSH primário: Pirazóis/química
[Mh] Termos MeSH secundário: Conformação Molecular
Oxifenilbutazona
Espectroscopia de Infravermelho com Transformada de Fourier
Análise Espectral Raman
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Pyrazoles); 3QD5KJZ7ZJ (pyrazole); H806S4B3NS (Oxyphenbutazone)
[Em] Mês de entrada:1209
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:120417
[St] Status:MEDLINE
[do] DOI:10.1016/j.saa.2012.03.014


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[PMID]:21428758
[Au] Autor:Murray PI; Bodaghi B; Sharma OP
[Ad] Endereço:University of Birmingham, Birmingham, UK. p.i.murray@bham.ac.uk
[Ti] Título:Systemic treatment of sarcoidosis.
[So] Source:Ocul Immunol Inflamm;19(2):145-50, 2011 Apr.
[Is] ISSN:1744-5078
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:PURPOSE: To compare the evidence base and systemic treatment strategies for sarcoidosis. METHODS: Medline and EMBASE literature search on "sarcoidosis AND treatment", "sarcoidosis AND uveitis AND treatment", and "sarcoidosis AND eye AND treatment". The search was limited to randomized controlled trials (RCTs) and meta-analyses. RESULTS: A total of 19 RCTs for the systemic treatment of extraocular sarcoidosis were identified. The majority were on corticosteroid-oral and inhaled. There were two meta-analyses on corticosteroid, including a Cochrane review. Only two RCTs were indentified for the treatment of intraocular sarcoidosis, one on etanercept, and the other from 1967 on prednisolone or oxyphenbutazone vs. placebo. There were no meta-analyses. Due to the paucity of RCTs other treatment studies were included but these were limited to only a few immunosuppressive agents and on small numbers of patients. CONCLUSION: Limited high-quality evidence exists for the systemic treatment of sarcoidosis, in particular intraocular disease.
[Mh] Termos MeSH primário: Sarcoidose/tratamento farmacológico
[Mh] Termos MeSH secundário: Administração por Inalação
Administração Oral
Corticosteroides/administração & dosagem
Esquema de Medicação
Etanercepte
Medicina Baseada em Evidências/métodos
Oftalmopatias/tratamento farmacológico
Glucocorticoides/uso terapêutico
Seres Humanos
Imunoglobulina G/uso terapêutico
Metanálise como Assunto
Oxifenilbutazona/uso terapêutico
Prednisolona/uso terapêutico
Ensaios Clínicos Controlados Aleatórios como Assunto/estatística & dados numéricos
Receptores do Fator de Necrose Tumoral/uso terapêutico
Sarcoidose Pulmonar/tratamento farmacológico
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Adrenal Cortex Hormones); 0 (Glucocorticoids); 0 (Immunoglobulin G); 0 (Receptors, Tumor Necrosis Factor); 9PHQ9Y1OLM (Prednisolone); H806S4B3NS (Oxyphenbutazone); OP401G7OJC (Etanercept)
[Em] Mês de entrada:1107
[Cu] Atualização por classe:151119
[Lr] Data última revisão:
151119
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:110325
[St] Status:MEDLINE
[do] DOI:10.3109/09273948.2010.542870


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[PMID]:20579495
[Au] Autor:Jedziniak P; Szprengier-Juszkiewicz T; Olejnik M; Zmudzki J
[Ad] Endereço:National Veterinary Research Institute, Department of Pharmacology and Toxicology, Al. Partyzantow 57, 24-100 Pulawy, Poland. jedzi@piwet.pulawy.pl
[Ti] Título:Determination of non-steroidal anti-inflammatory drugs residues in animal muscles by liquid chromatography-tandem mass spectrometry.
[So] Source:Anal Chim Acta;672(1-2):85-92, 2010 Jul 05.
[Is] ISSN:1873-4324
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:A confirmatory method for the determination of residues of nine non-steroidal anti-inflammatory drugs and one metabolite in animal muscles has been developed. After enzymatic hydrolysis samples were extracted with acetonitrile and cleaned up using alumina and C(18) SPE cartridges. Liquid chromatography-tandem mass spectrometry was used for the separation and determination of analytes. The method was validated in bovine muscles, according to the Commission Decision 2002/657/EC criteria. Applicability of the method in the analysis of swine, horse and chicken muscles was checked by precision and recovery experiment. The influence of matrix effect on the quantification of non-steroidal anti-inflammatory drugs residues was investigated. The method was used for the confirmation of phenylbutazone and oxyphenbutazone in horse muscle sample.
[Mh] Termos MeSH primário: Anti-Inflamatórios não Esteroides/análise
Resíduos de Drogas/análise
Músculo Esquelético/química
[Mh] Termos MeSH secundário: Animais
Bovinos
Galinhas
Cromatografia Líquida
Cavalos
Oxifenilbutazona/análise
Fenilbutazona/análise
Suínos
Espectrometria de Massas em Tandem
[Pt] Tipo de publicação:JOURNAL ARTICLE; VALIDATION STUDIES
[Nm] Nome de substância:
0 (Anti-Inflammatory Agents, Non-Steroidal); GN5P7K3T8S (Phenylbutazone); H806S4B3NS (Oxyphenbutazone)
[Em] Mês de entrada:1009
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:100629
[St] Status:MEDLINE
[do] DOI:10.1016/j.aca.2010.04.031


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[PMID]:20299217
[Au] Autor:Kapadia GJ; Azuine MA; Shigeta Y; Suzuki N; Tokuda H
[Ad] Endereço:Department of Pharmaceutical Sciences, School of Pharmacy, Howard University, Washington, DC 20059, USA. gkapadia@howard.edu
[Ti] Título:Chemopreventive activities of etodolac and oxyphenbutazone against mouse skin carcinogenesis.
[So] Source:Bioorg Med Chem Lett;20(8):2546-8, 2010 Apr 15.
[Is] ISSN:1464-3405
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Previous cancer chemoprevention studies have demonstrated that the non-steroidal anti-inflammatory drugs (NSAIDs) can be effective in suppressing the development of various human malignancies. Recently we identified the possible anti-tumor promoting potentials of 14 new NSAIDs in the Epstein-Barr virus early antigen activation assay induced by 12-O-tetradecanoylphorbol-13-acetate (TPA). In this study we report the inhibition of 7,12-dimethylbenz (a) anthracene (DMBA) induced two-stage mouse skin carcinogenesis by etodolac (ETD), one of the most potent NSAIDs identified in our in vitro cancer chemopreventive screening of this group of drugs. Topical administration of ETD at a very low dose of 85 nmol showed a significant decrease in both tumor incidence and burden. This effect is also accompanied by a delay in the tumor latency period. Since ETD showed potent chemopreventive activity in both in vitro and in vivo studies, it warrants prompt consideration for trial in humans as a potential cancer chemopreventive agent. We also investigated oxyphenbutazone (OPB) another commonly used NSAID for its cancer chemopreventive effect on peroxynitrite (PN) induced-TPA promoted skin tumors in the mouse. Following tumor initiation with 390 nmol of PN, the skin tumor promotion with 1.7 nmol of TPA was significantly inhibited by oral administration of 0.0025% OPB. The results demonstrate that OPB is a potent cancer chemopreventive agent in the highly sensitive in vivo mouse test model we used.
[Mh] Termos MeSH primário: Anticarcinógenos/farmacologia
Transformação Celular Neoplásica/efeitos dos fármacos
Etodolac/farmacologia
Oxifenilbutazona/farmacologia
Neoplasias Cutâneas/prevenção & controle
[Mh] Termos MeSH secundário: 9,10-Dimetil-1,2-benzantraceno/toxicidade
Animais
Carcinógenos/toxicidade
Transformação Celular Neoplásica/induzido quimicamente
Camundongos
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Anticarcinogenic Agents); 0 (Carcinogens); 2M36281008 (Etodolac); 57-97-6 (9,10-Dimethyl-1,2-benzanthracene); H806S4B3NS (Oxyphenbutazone)
[Em] Mês de entrada:1008
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:100320
[St] Status:MEDLINE
[do] DOI:10.1016/j.bmcl.2010.02.093


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[PMID]:19161668
[Au] Autor:You Y; Uboh CE; Soma LR; Guan F; Li X; Rudy JA; Chen J
[Ad] Endereço:University of Pennsylvania, School of Veterinary Medicine, Department of Clinical Studies, New Bolton Center Campus, Kennett Square, Pennsylvania 19348, USA.
[Ti] Título:Screening, quantification, and confirmation of phenylbutazone and oxyphenbutazone in equine plasma by liquid chromatography-tandem mass spectrometry.
[So] Source:J Anal Toxicol;33(1):41-50, 2009 Jan-Feb.
[Is] ISSN:0146-4760
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:A sensitive liquid chromatographic-tandem mass spectrometric method was developed and validated for screening, quantification, and confirmation of phenylbutazone and oxyphenbutazone in equine plasma. Analytes were recovered from plasma by liquid-liquid extraction followed by separation in a reversed-phase column and identification by mass spectrometry with selected reaction monitoring in negative electrospray ionization mode. Extraction recovery for both analytes was >80%. Limits of detection, quantification, and confirmation for both analytes were 0.01 microg/mL (S/N>or= 3), 0.05 microg/mL, and 0.05 microg/mL, respectively. The assay with d9-labeled phenylbutazone as internal standard (IS) was linear over a range of 0.05-20 microg/mL (r2>0.995). Intra- and interday precision in terms of coefficient of variation was less than 15%. Intra- and interday accuracy (bias%) was within 80-120%. Hemolysis of red blood cells decreased analyte signal intensity but did not affect quantification results because an isotope-labeled IS was used. Analytes were stable in plasma for 24 h at room temperature, 9 days at 4 degrees C, and 45 days at -20 degrees C and -70 degrees C. The method was successfully used in screening, quantification, and confirmation of phenylbutazone in post-competition plasma samples obtained from racehorses. The method is simple, rapid, and reliably reproducible.
[Mh] Termos MeSH primário: Anti-Inflamatórios não Esteroides/sangue
Doping nos Esportes
Oxifenilbutazona/sangue
Fenilbutazona/sangue
Espectrometria de Massas por Ionização por Electrospray/métodos
Detecção do Abuso de Substâncias/métodos
Espectrometria de Massas em Tandem/métodos
[Mh] Termos MeSH secundário: Animais
Cromatografia Líquida de Alta Pressão
Hemólise
Cavalos
Reprodutibilidade dos Testes
[Pt] Tipo de publicação:JOURNAL ARTICLE; VALIDATION STUDIES
[Nm] Nome de substância:
0 (Anti-Inflammatory Agents, Non-Steroidal); GN5P7K3T8S (Phenylbutazone); H806S4B3NS (Oxyphenbutazone)
[Em] Mês de entrada:0903
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:090124
[St] Status:MEDLINE


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[PMID]:17979211
[Au] Autor:Kosa T; Nishi K; Maruyama T; Sakai N; Yonemura N; Watanabe H; Suenaga A; Otagiri M
[Ad] Endereço:Department of Biopharmaceutics, Graduate School of Pharmaceutical Sciences, Kumamoto University, 5-1 Oe-honmachi, Kumamoto 862-0973, Japan.
[Ti] Título:Structural and ligand-binding properties of serum albumin species interacting with a biomembrane interface.
[So] Source:J Pharm Sci;96(11):3117-24, 2007 Nov.
[Is] ISSN:0022-3549
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:In the process of drug development, preclinical testing using experimental animals is an important aspect, for verification of the efficacy and safety of a drug. Serum albumin is a major binding protein for endogenous and exogenous ligands and regulates their distribution in various tissues. In this study, the structural and drug-binding properties of albumins on a biomembrane surface were investigated using reverse micelles as a model membrane. In reverse micelles, the secondary structures of all albumins were found, to varying degrees, to be intermediate between the native and denatured states. The tertiary structures of human and bovine albumin were similar to those of the native and intermediate states, respectively, whereas those of the dog, rabbit, and rat were in a denatured state. Thus, bovine albumin is an appropriate model for studying structural changes in human albumin in a membrane-water phase. Binding studies also showed the presence of species difference in the change in binding capacity of albumins during their interaction with reverse micelles. Among the albumins, rat albumin appears to be a good model for the protein-mediated drug uptake of human albumin in a biomembrane environment. These findings are significant in terms of the appropriate extrapolation of pharmacokinetics and pharmacodynamics data in various animals to humans.
[Mh] Termos MeSH primário: Micelas
Albumina Sérica/química
Albumina Sérica/metabolismo
[Mh] Termos MeSH secundário: Animais
Dicroísmo Circular
Compostos de Dansil/química
Compostos de Dansil/metabolismo
Cães
Seres Humanos
Ligantes
Membranas/química
Membranas/metabolismo
Oxifenilbutazona/química
Oxifenilbutazona/metabolismo
Ligação Proteica
Coelhos
Ratos
Sarcosina/análogos & derivados
Sarcosina/química
Sarcosina/metabolismo
Especificidade da Espécie
Espectrometria de Fluorescência
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Dansyl Compounds); 0 (Ligands); 0 (Micelles); 0 (Serum Albumin); 1093-96-5 (dansylsarcosine); H806S4B3NS (Oxyphenbutazone); Z711V88R5F (Sarcosine)
[Em] Mês de entrada:0712
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:071106
[St] Status:MEDLINE


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[PMID]:15941686
[Au] Autor:Ten Brinke A; Dekkers DW; Notten SM; Karsten ML; de Groot ER; Aarden LA
[Ad] Endereço:Department of Immunopathology, Sanquin Research at CLB, PO.BOX 9190, 1006 AD Amsterdam, The Netherlands. a.tenbrinke@sanquin.nl
[Ti] Título:4-Hydroxy-oxyphenbutazone is a potent inhibitor of cytokine production.
[So] Source:Eur Cytokine Netw;16(2):144-51, 2005 Jun.
[Is] ISSN:1148-5493
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:4-Hydroxy-oxyphenbutazone (4OH-OPB), is currently in phase II trials for its immunosuppressive effect in patients with rheumatoid arthritis. 4OH-OPB and other compounds related to phenylbutazone were tested for their effect on in vitro cytokine production by monocytes and lymphocytes present in peripheral mononuclear cells (PBMC) or whole blood (WB) cultures, and compared against phenylbutazone and oxyphenbutazone, two known anti-inflammatory drugs. In PBMC cultures, 4OH-OPB was by far the most potent inhibitor, and both monokines and Th1 and Th2 lymphokines were efficiently inhibited at low concentrations. In WB cultures, 4OH-OPB was less effective than in PBMC cultures, but was still the best inhibitor of lymphokine production and, furthermore, was the only inhibitor of monokine production. The increase in 4OH-OPB concentration needed to induce the same inhibition of cytokine production in WB as in PBMC culture could be mimicked by the addition of erythrocytes to the PBMC cultures. Experiments with radioactively-labeled 4OH-OPB suggest that 4OH-OPB is taken up very rapidly into erythrocytes and is secreted by the erythrocytes with much slower kinetics via a multidrug-resistance-associated protein. The secreted compound is most likely structurally different from 4OH-OPB, as in PBMC and WB cultures, the inhibition of cytokine production seems to be caused by a different mechanism. In PBMC cultures, the inhibition of cytokine production is accompanied by a loss of cell viability, while this is not the case when 4OH-OPB inhibits cytokine production in WB. Our data suggest that 4OH-OPB may be useful as an immunosuppressive drug for patients with inflammatory diseases.
[Mh] Termos MeSH primário: Fator Estimulador de Colônias de Granulócitos e Macrófagos/antagonistas & inibidores
Interleucina-6/antagonistas & inibidores
Oxifenilbutazona/análogos & derivados
[Mh] Termos MeSH secundário: Sobrevivência Celular/efeitos dos fármacos
Células Cultivadas
Eritrócitos/efeitos dos fármacos
Eritrócitos/metabolismo
Fator Estimulador de Colônias de Granulócitos e Macrófagos/biossíntese
Seres Humanos
Técnicas In Vitro
Interleucina-6/biossíntese
Monócitos/efeitos dos fármacos
Monócitos/metabolismo
Oxifenilbutazona/farmacologia
Linfócitos T/efeitos dos fármacos
Linfócitos T/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (4-hydroxy-oxyphenbutazone); 0 (Interleukin-6); 83869-56-1 (Granulocyte-Macrophage Colony-Stimulating Factor); H806S4B3NS (Oxyphenbutazone)
[Em] Mês de entrada:0511
[Cu] Atualização por classe:141120
[Lr] Data última revisão:
141120
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:050609
[St] Status:MEDLINE


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Fotocópia
[PMID]:17564304
[Au] Autor:Pesce E; Struma E; Giri SN; Margolin SB
[Ad] Endereço:Local Health Unit of Parma, Bassa Est, N4, 43100 Parma, Italy.
[Ti] Título:Antirheumatic effect of pirfenidone in a double blind clinical pilot trial in humans.
[So] Source:Res Commun Mol Pathol Pharmacol;115-116:39-48, 2004.
[Is] ISSN:1078-0297
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The antirheumatic effect of pirfenidone was compared with a positive control drug, oxyphenbutazone which is used in patients suffering from rheumatoid arthritis, in a double blind clinical trial in humans. The data collected in this pilot project revealed that pirfenidone was more effective (p < 0.025) than oxyphenbutazone in providing relief from arthritic pain. In addition, a greater number (p < 0.025) of patients reported favorable response to oral pirfenidone than oral oxyphenbutazone. However, there were no significant differences in the number of patients who dropped out from the trial and the number of patients who tolerated the drugs for 21 days of the trial between the pirfenidone and oxyphenbutazone groups. It was concluded from this pilot study that pirfenidone potentially offers a novel therapeutic modality for the management of rheumatoid arthritis with little or no adverse effects unlike steroidal and non-steroidal anti-inflammatory drugs which are frequently used for this chronic debilitating disease.
[Mh] Termos MeSH primário: Antirreumáticos/uso terapêutico
Artrite Reumatoide/tratamento farmacológico
Piridonas/uso terapêutico
[Mh] Termos MeSH secundário: Adulto
Antirreumáticos/administração & dosagem
Antirreumáticos/efeitos adversos
Artrite Reumatoide/fisiopatologia
Distribuição de Qui-Quadrado
Método Duplo-Cego
Feminino
Seres Humanos
Masculino
Meia-Idade
Oxifenilbutazona/administração & dosagem
Oxifenilbutazona/uso terapêutico
Pacientes Desistentes do Tratamento
Projetos Piloto
Piridonas/administração & dosagem
Piridonas/efeitos adversos
Resultado do Tratamento
[Pt] Tipo de publicação:CLINICAL TRIAL; COMPARATIVE STUDY; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antirheumatic Agents); 0 (Pyridones); D7NLD2JX7U (pirfenidone); H806S4B3NS (Oxyphenbutazone)
[Em] Mês de entrada:0707
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:070615
[St] Status:MEDLINE



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