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Pesquisa : D02.886.590.795.204 [Categoria DeCS]
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[PMID]:10709193
[Au] Autor:Mel'nikova OV; Kolesnik IuM
[Ad] Endereço:Department of Pathological Physiology, State Medical University of Zaporozhye.
[Ti] Título:[Neuronal changes in the dorsal motor nucleus of the vagus nerve during intervals of hypoxic exposures in animals with diabetes mellitus].
[Ti] Título:Izmeneniia neironov dorsal'nogo motornogo iadra bluzhdaiushchego nerva pri interval'nykh gipoksicheskikh vozdeistviiakh na zhivotnykh s sakharnym diabetom..
[So] Source:Morfologiia;116(6):19-22, 1999.
[Is] ISSN:1026-3543
[Cp] País de publicação:Russia (Federation)
[La] Idioma:rus
[Ab] Resumo:Changes of neurons of dorsal motor nucleus of nervus vagus were studied in adaptation to hypoxia, experimental diabetes mellitus and its correction by means of interrupted hypoxic effects. It was established previously that interrupted hypoxic training exerted stimulating effect on insulin synthesizing function of pancreas. As a result of the present study the increase of morphofunctional activity of neurons was found in all experimental series although it was greater manifested in animals with experimental diabetes mellitus who were subjected to actions of hypoxia. The changes of morphofunctional activity of dorsal motor nucleus of nervus vagus established allow to conclude on the significant role these structure plays in realization of stimulating effect of interrupted actions of hypoxia on the state of insulin synthesizing function of pancreas and clinical characteristics of the experimental diabetes mellitus.
[Mh] Termos MeSH primário: Diabetes Mellitus Experimental/fisiopatologia
Hipóxia Encefálica/fisiopatologia
Neurônios/patologia
Nervo Vago/fisiopatologia
[Mh] Termos MeSH secundário: Adaptação Fisiológica
Animais
Câmaras de Exposição Atmosférica
Carbutamida
Diabetes Mellitus Experimental/etiologia
Hipoglicemiantes
Masculino
Neurônios/fisiologia
Ratos
Ratos Wistar
Fatores de Tempo
[Pt] Tipo de publicação:COMPARATIVE STUDY; ENGLISH ABSTRACT; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Hypoglycemic Agents); E3K8P4869P (Carbutamide)
[Em] Mês de entrada:0004
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM; S
[Da] Data de entrada para processamento:000310
[St] Status:MEDLINE


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[PMID]:9628248
[Au] Autor:Kleinsorge H
[Ti] Título:Carbutamide--the first oral antidiabetic. A retrospect.
[So] Source:Exp Clin Endocrinol Diabetes;106(2):149-51, 1998.
[Is] ISSN:0947-7349
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:This work describes the history of the first oral antidiabetic in East and West Germany. M. Janbon and A. Loubatières reported experimental and clinical findings about a blood sugar-decreasing effect of a sulphonamide derivate, sulphoisopropyl thiodiazol (1942). These findings, however, did not prove to be useful in the treatment of diabetes. In 1952 the author found a series of hypoglycemic shocks with the sulfonamid-urea derivate carbutamdide during clinical tests of infectious diseases. These were reported to the pharmaceutical company Von Heyden in Dresden. The head chemist E. Haack went with my files from East to West Germany, to Boehringer Mannheim. Without mentioning the synthesis in Dresden, he synthesized carbutamide in Mannheim. The hypoglycemic effect was rediscovered by his friend H. Franke together with J. Fuchs. It took twenty years until the results of the author's research were officially acknowledged.
[Mh] Termos MeSH primário: Carbutamida/história
Hipoglicemiantes/história
[Mh] Termos MeSH secundário: Administração Oral
Carbutamida/uso terapêutico
Diabetes Mellitus/tratamento farmacológico
Alemanha
História do Século XX
Seres Humanos
Hipoglicemiantes/uso terapêutico
[Pt] Tipo de publicação:HISTORICAL ARTICLE; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Hypoglycemic Agents); E3K8P4869P (Carbutamide)
[Em] Mês de entrada:9809
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM; Q
[Da] Data de entrada para processamento:980617
[St] Status:MEDLINE


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PubMed Central Texto completo
[PMID]:9559882
[Au] Autor:Schwanstecher C; Meyer M; Schwanstecher M; Panten U
[Ad] Endereço:Institute of Pharmacology and Toxicology, Technical University of Braunschweig, Germany.
[Ti] Título:Interaction of N-benzoyl-D-phenylalanine and related compounds with the sulphonylurea receptor of beta-cells.
[So] Source:Br J Pharmacol;123(6):1023-30, 1998 Mar.
[Is] ISSN:0007-1188
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:1. The structure activity relationships for the insulin secretagogues N-benzoyl-D-phenylalanine (NBDP) and related compounds were examined at the sulphonylurea receptor level by use of cultured HIT-T15 and mouse pancreatic beta-cells. The affinities of these compounds for the sulphonylurea receptor were compared with their potencies for K(ATP)-channel inhibition. In addition, the effects of cytosolic nucleotides on K(ATP)-channel inhibition by NBDP were investigated. 2. NBDP displayed a dissociation constant for binding to the sulphonylurea receptor (K(D) value) of 11 microM and half-maximally effective concentrations of K(ATP)-channel inhibition (EC50 values) between 2 and 4 microM (in the absence of cytosolic nucleotides or presence of 0.1 mM GDP or 1 mM ADP). 3. In the absence of cytosolic nucleotides or presence of GDP (0.1 mM) maximally effective concentrations of NBDP (0.1-1 mM) reduced K(ATP)-channel activity to 47% and 44% of control, respectively. In the presence of ADP (1 mM), K(ATP)-channel activity was completely suppressed by 0.1 mM NBDP. 4. The L-isomer of N-benzoyl-phenylalanine displayed a 20 fold lower affinity and an 80 fold lower potency than the D-isomer. 5. Introduction of a p-nitro substituent in the D-phenylalanine moiety of NBDP did not decrease lipophilicity but lowered affinity and potency by more than 30 fold. 6. Introduction of a p-amino substituent in the D-phenylalanine moiety of NBDP (N-benzoyl-p-amino-D-phenylalanine, NBADP) reduced lipophilicity and lowered affinity and potency by about 10 fold. This loss of affinity and potency was compensated for by formation of the phenylpropionic acid derivative of NBADP. A similar difference in affinity was observed for the sulphonylurea carbutamide and its phenylpropionic acid derivative. 7. Replacing the benzene ring in the D-phenylalanine moiety of NBDP by a cyclohexyl ring increased lipophilicity, and the K(D) and EC50 values were slightly lower than for NBDP. Exchange of both benzene rings in NBDP by cyclohexyl rings further increased lipophilicity without altering affinity and potency. 8. This study shows that N-acylphenylalanines interact with the sulphonylurea receptor of pancreatic beta-cells in a stereospecific manner. Their potency depends on lipophilic but not aromatic properties of their benzene rings. As observed for sulphonylureas, interaction of N-acylphenylalanines with the sulphonylurea receptor does not induce complete inhibition of K(ATP)-channel activity in the absence of inhibitory cytosolic nucleotides.
[Mh] Termos MeSH primário: Transportadores de Cassetes de Ligação de ATP
Ilhotas Pancreáticas/metabolismo
Fenilalanina/análogos & derivados
Canais de Potássio Corretores do Fluxo de Internalização
Canais de Potássio/metabolismo
Receptores de Droga/metabolismo
[Mh] Termos MeSH secundário: Trifosfato de Adenosina/metabolismo
Animais
Cálcio/metabolismo
Carbutamida/análogos & derivados
Carbutamida/farmacologia
Linhagem Celular Transformada
Cricetinae
Cicloexanos/farmacologia
Glibureto/metabolismo
Guanosina Difosfato/metabolismo
Ilhotas Pancreáticas/citologia
Ilhotas Pancreáticas/efeitos dos fármacos
Masculino
Camundongos
Fenilalanina/metabolismo
Fenilalanina/farmacologia
Canais de Potássio/efeitos dos fármacos
Receptores Sulfonilureia
Trítio
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Cyclohexanes); 0 (Kcnj1 protein, mouse); 0 (Potassium Channels); 0 (Potassium Channels, Inwardly Rectifying); 0 (Receptors, Drug); 0 (Sulfonylurea Receptors); 10028-17-8 (Tritium); 146-91-8 (Guanosine Diphosphate); 41X3PWK4O2 (nateglinide); 47E5O17Y3R (Phenylalanine); 8L70Q75FXE (Adenosine Triphosphate); 9S304JL9M7 (benzoylphenylalanine); E3K8P4869P (Carbutamide); SX6K58TVWC (Glyburide); SY7Q814VUP (Calcium)
[Em] Mês de entrada:9805
[Cu] Atualização por classe:141120
[Lr] Data última revisão:
141120
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:980429
[St] Status:MEDLINE


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[PMID]:9163521
[Au] Autor:Imamura Y; Koga T; Migita T; Ryu A; Otagiri M; Nozawa M; Akita H
[Ad] Endereço:Faculty of Pharmaceutical Sciences, Kumamoto University, Oe-honmachi.
[Ti] Título:Characterization of acetohexamide reductases purified from rabbit liver, kidney, and heart: structural requirements for substrates and inhibitors.
[So] Source:J Biochem;121(4):705-10, 1997 Apr.
[Is] ISSN:0021-924X
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:The structural requirements of acetohexamide reductases purified from rabbit liver, kidney, and heart for substrates and inhibitors were examined. Acetohexamide, an oral antidiabetic drug with a ketone group, and analogs of it with various alkyl groups instead of the cyclohexyl group were used as substrates for these three enzymes. The results obtained as to substrate specificity suggested that the nature of the substrate-binding region of the heart enzyme is markedly different from those of the substrate-binding regions of the liver and kidney enzymes. Tolbutamide, which has no ketone group within its chemical structure, strongly inhibited the heart enzyme, whereas it had little ability to inhibit the liver or kidney enzyme. The inhibition of the heart enzyme by tolbutamide was competitive with respect to acetohexamide and uncompetitive with respect to NADPH. Furthermore, tolbutamide analogs with n-pentyl and n-hexyl groups instead of the n-butyl group exhibited very pronounced inhibition of only the heart enzyme. Therefore, it is reasonable to postulate that the heart enzyme, unlike the liver and kidney ones, has a cleft of a strongly hydrophobic nature near its substrate-binding region, and that this hydrophobic cleft plays a critical role in the interaction of the heart enzyme with the cyclohexyl group of acetohexamide.
[Mh] Termos MeSH primário: Oxirredutases do Álcool/antagonistas & inibidores
Oxirredutases do Álcool/metabolismo
Rim/enzimologia
Fígado/enzimologia
Miocárdio/enzimologia
[Mh] Termos MeSH secundário: Acetoexamida/análogos & derivados
Acetoexamida/química
Acetoexamida/metabolismo
Animais
Sítios de Ligação
Carbutamida/química
Carbutamida/farmacologia
Clorpropamida/química
Clorpropamida/farmacologia
Inibidores Enzimáticos/química
Inibidores Enzimáticos/metabolismo
Inibidores Enzimáticos/farmacologia
Hipoglicemiantes/farmacologia
Cinética
Oxirredução
Coelhos
Relação Estrutura-Atividade
Especificidade por Substrato
Tolbutamida/análogos & derivados
Tolbutamida/metabolismo
Tolbutamida/farmacologia
Triazinas/química
Triazinas/metabolismo
Triazinas/farmacologia
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Enzyme Inhibitors); 0 (Hypoglycemic Agents); 0 (Triazines); 5DV0L8V99J (Cibacron Blue F 3GA); 982XCM1FOI (Tolbutamide); E3K8P4869P (Carbutamide); EC 1.1.- (Alcohol Oxidoreductases); EC 1.1.1.- (acetohexamide reductase); QGC8W08I6I (Acetohexamide); WTM2C3IL2X (Chlorpropamide)
[Em] Mês de entrada:9707
[Cu] Atualização por classe:161124
[Lr] Data última revisão:
161124
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:970401
[St] Status:MEDLINE


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[PMID]:9017793
[Au] Autor:Selvaag E
[Ad] Endereço:Department of Dermatology, Ullevaal Hospital, University of Oslo, Norway.
[Ti] Título:Photohemolytic potency of oral antidiabetic drugs in vitro: effects of antioxidants and a nitrogen atmosphere.
[So] Source:Photodermatol Photoimmunol Photomed;12(4):166-70, 1996 Aug.
[Is] ISSN:0905-4383
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:The sulphonamide-derived oral antidiabetic drugs carbutamide, chlorpropamide, glibenclamide, glibornuride, gliclazide, glipizide, gliquidone, glisoxepide, glymidine, tolazamide and tolbutamide were investigated for photohemolytic properties in vitro. Irradiation with a SOL 3 apparatus (solar simulating irradiation) revealed hemolysis in the presence of chlorpropamide, glipizide, gliquidone, glymidine and tolbutamide (all in the concentration 10(-3) mol/l). Except for glymidine, which exerted photohemolysis in the concentration 10(-4) mol/l, no hemolytic effects were seen in the concentration of 10(-4) mol/l or 10(-5) mol/l. Irradiation with TL 12 light bulbs (UVB), a UVASUN 5000 apparatus (UVA) or an experimental lamp (visible light) did not induce phototoxic hemolysis with either of the test substances. Addition of the antioxidants ascorbic acid, alpha-tocopherol or superoxide dismutase significantly inhibited the phototoxic hemolysis. Investigations carried out in a nitrogen-rich atmosphere reduced the hemolysis as well. These findings indicate an involvement of reactive oxygen species in the mechanism of action of the hemolytic process in the presence of oral antidiabetic drugs.
[Mh] Termos MeSH primário: Antioxidantes/farmacologia
Hemólise/efeitos da radiação
Hipoglicemiantes/efeitos adversos
Nitrogênio/farmacologia
Radiossensibilizantes/efeitos adversos
Sulfonamidas/efeitos adversos
[Mh] Termos MeSH secundário: Antioxidantes/administração & dosagem
Ácido Ascórbico/administração & dosagem
Ácido Ascórbico/farmacologia
Carbutamida/administração & dosagem
Carbutamida/efeitos adversos
Clorpropamida/administração & dosagem
Clorpropamida/efeitos adversos
Relação Dose-Resposta a Droga
Gliclazida/administração & dosagem
Gliclazida/efeitos adversos
Glipizida/administração & dosagem
Glipizida/efeitos adversos
Glibureto/administração & dosagem
Glibureto/efeitos adversos
Hemólise/efeitos dos fármacos
Seres Humanos
Hipoglicemiantes/administração & dosagem
Nitrogênio/administração & dosagem
Radiossensibilizantes/administração & dosagem
Espécies Reativas de Oxigênio/fisiologia
Sulfonamidas/administração & dosagem
Compostos de Sulfonilureia/administração & dosagem
Compostos de Sulfonilureia/efeitos adversos
Superóxido Dismutase/administração & dosagem
Superóxido Dismutase/farmacologia
Tolazamida/administração & dosagem
Tolazamida/efeitos adversos
Tolbutamida/administração & dosagem
Tolbutamida/efeitos adversos
Raios Ultravioleta/efeitos adversos
Vitamina E/administração & dosagem
Vitamina E/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antioxidants); 0 (Hypoglycemic Agents); 0 (Radiation-Sensitizing Agents); 0 (Reactive Oxygen Species); 0 (Sulfonamides); 0 (Sulfonylurea Compounds); 1406-18-4 (Vitamin E); 26944-48-9 (glibornuride); 4C5I4BQZ8F (glymidine); 982XCM1FOI (Tolbutamide); 9LT1BRO48Q (Tolazamide); C7C2QDD75P (gliquidone); E3K8P4869P (Carbutamide); EC 1.15.1.1 (Superoxide Dismutase); G4PX8C4HKV (Gliclazide); H7SC0I332I (glisoxepide); N762921K75 (Nitrogen); PQ6CK8PD0R (Ascorbic Acid); SX6K58TVWC (Glyburide); WTM2C3IL2X (Chlorpropamide); X7WDT95N5C (Glipizide)
[Em] Mês de entrada:9704
[Cu] Atualização por classe:141120
[Lr] Data última revisão:
141120
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:960801
[St] Status:MEDLINE


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[PMID]:7953108
[Au] Autor:Bykova EV; Bykova AA; Iushkova TA
[Ti] Título:[Immunological aspects of insulin therapy of diabetes mellitus and methods of their studies].
[Ti] Título:Nekotorye immunologicheskie aspekty insulinoterapii sakharnogo diabeta i metody ikh izucheniia..
[So] Source:Klin Lab Diagn;(4):29-33, 1994.
[Is] ISSN:0869-2084
[Cp] País de publicação:Russia (Federation)
[La] Idioma:rus
[Mh] Termos MeSH primário: Diabetes Mellitus/imunologia
Diabetes Mellitus/terapia
Insulina/uso terapêutico
[Mh] Termos MeSH secundário: Animais
Autoanticorpos/análise
Carbutamida/uso terapêutico
Seres Humanos
Imunização Passiva
Anticorpos Anti-Insulina/análise
Resistência à Insulina
Ratos
Receptor de Insulina/imunologia
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Autoantibodies); 0 (Insulin); 0 (Insulin Antibodies); E3K8P4869P (Carbutamide); EC 2.7.10.1 (Receptor, Insulin)
[Em] Mês de entrada:9411
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:940101
[St] Status:MEDLINE


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[PMID]:2106423
[Au] Autor:Ballagi-Pordány G; Köszeghy A; Koltai MZ; Aranyi Z; Pogátsa G
[Ad] Endereço:National Institute of Cardiology, Research Department, Budapest, Hungary.
[Ti] Título:Divergent cardiac effects of the first and second generation hypoglycemic sulfonylurea compounds.
[So] Source:Diabetes Res Clin Pract;8(2):109-14, 1990 Jan.
[Is] ISSN:0168-8227
[Cp] País de publicação:Ireland
[La] Idioma:eng
[Ab] Resumo:The effects of first and second generation hypoglycemic sulfonylureas on the incidence of ventricular ectopic beats and on the duration of transitional ventricular fibrillation in the ischemic rat heart were investigated. First generation sulfonylurea compounds (tolbutamide, carbutamide and gliclazide) in 105 preparations increased, while second generation sulfonylurea compounds (glibenclamide and glipizide) in 50 preparations decreased in a dose-dependent manner both the number of ventricular ectopic beats and the duration of transitional ventricular fibrillation during the first 30 min after ligation of the left anterior descending coronary artery. Therefore, second generation sulfonylureas should be preferred in the treatment of type 2 diabetics with ischemic heart diseases, if satisfactory metabolic control cannot be achieved by a treatment regimen and diet alone.
[Mh] Termos MeSH primário: Eletrocardiografia/efeitos dos fármacos
Hipoglicemiantes/farmacologia
[Mh] Termos MeSH secundário: Animais
Arritmias Cardíacas/fisiopatologia
Glicemia/metabolismo
Carbutamida/farmacologia
Relação Dose-Resposta a Droga
Gliclazida/farmacologia
Glipizida/farmacologia
Glibureto/farmacologia
Masculino
Infarto do Miocárdio/fisiopatologia
Potássio/sangue
Ratos
Ratos Endogâmicos
Valores de Referência
Relação Estrutura-Atividade
Tolbutamida/farmacologia
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Blood Glucose); 0 (Hypoglycemic Agents); 982XCM1FOI (Tolbutamide); E3K8P4869P (Carbutamide); G4PX8C4HKV (Gliclazide); RWP5GA015D (Potassium); SX6K58TVWC (Glyburide); X7WDT95N5C (Glipizide)
[Em] Mês de entrada:9004
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:900101
[St] Status:MEDLINE


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[PMID]:3826740
[Au] Autor:Belokurov MIu; Kozlova AS; Andreev AM; Larionov SV; Preobrazhenskaia VI
[Ti] Título:[Hyperbaric oxygenation and hemosorption in the treatment of allergotoxic hepatic insufficiency].
[Ti] Título:Giperbaricheskaia oksigenatsiia i gemosorbtsiia v lechenii allergotoksicheskoi pechenochnoi nedostatochnosti..
[So] Source:Anesteziol Reanimatol;(6):52-3, 1986 Nov-Dec.
[Is] ISSN:0201-7563
[Cp] País de publicação:Russia (Federation)
[La] Idioma:rus
[Mh] Termos MeSH primário: Carbutamida/efeitos adversos
Hemoperfusão
Encefalopatia Hepática/induzido quimicamente
Oxigenação Hiperbárica
Hipoglicemiantes/efeitos adversos
[Mh] Termos MeSH secundário: Adulto
Feminino
Seres Humanos
[Pt] Tipo de publicação:CASE REPORTS; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Hypoglycemic Agents); E3K8P4869P (Carbutamide)
[Em] Mês de entrada:8704
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:861101
[St] Status:MEDLINE


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[PMID]:3823115
[Au] Autor:Lippold BH; Lichey JF
[Ti] Título:[The effect of the hydrogen ion concentration on membrane transport of dissociated drugs from saturated solutions].
[Ti] Título:Einfluss der Wasserstoffionenkonzentration auf den Membrantransport dissoziierender Arzneistoffe aus gesättigten Lösungen..
[So] Source:Pharmazie;41(10):717-9, 1986 Oct.
[Is] ISSN:0031-7144
[Cp] País de publicação:Germany
[La] Idioma:ger
[Ab] Resumo:Dissociating drugs diffuse from saturated solutions with suspended drug particles across lipophilic membranes according to zero order kinetics. The highest rate is maintained even if large fractions of the drug are dissociated due to the pH-conditions of the solution. The pH range of the highest and pH-independent membrane transport corresponds with drug solubility/pH-profiles, showing the solubility of the undissociated drug.
[Mh] Termos MeSH primário: Preparações Farmacêuticas/análise
[Mh] Termos MeSH secundário: Carbutamida/análise
Química Farmacêutica
Difusão
Dimetideno/análise
Concentração de Íons de Hidrogênio
Cinética
Membranas Artificiais
Solubilidade
Soluções
[Pt] Tipo de publicação:ENGLISH ABSTRACT; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Membranes, Artificial); 0 (Pharmaceutical Preparations); 0 (Solutions); 661FH77Z3P (Dimethindene); E3K8P4869P (Carbutamide)
[Em] Mês de entrada:8704
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:861001
[St] Status:MEDLINE


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[PMID]:3486236
[Au] Autor:Hughes WT; Smith-McCain BL
[Ti] Título:Effects of sulfonylurea compounds on Pneumocystis carinii.
[So] Source:J Infect Dis;153(5):944-7, 1986 May.
[Is] ISSN:0022-1899
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Two sulfonylurea compounds, carbutamide and tolbutamide, were studied for efficacy against Pneumocystis carinii pneumonitis in the corticosteroid-treated rat model and compared with trimethoprim-sulfamethoxazole (TMP-SMZ). The chemical structures of these sulfonylureas are identical except that an amino group in carbutamide is replaced with a methyl group in tolbutamide. Carbutamide was totally effective in the prevention and treatment of P. carinii pneumonitis in dosages of 100 and 200 mg/kg per day. The carbutamide dosage of 50 mg/kg per day prevented the infection in 90% of animals, whereas tolbutamide in the same dosage permitted infection in 100% of animals. This study shows that carbutamide is at least as effective as TMP-SMZ in the treatment and prevention of murine P. carinii pneumonitis. The presence of an amino group in the para position on the benezene ring is a determinant for this activity.
[Mh] Termos MeSH primário: Carbutamida/uso terapêutico
Pneumonia por Pneumocystis/tratamento farmacológico
Tolbutamida/uso terapêutico
[Mh] Termos MeSH secundário: Administração Oral
Animais
Anti-Infecciosos/uso terapêutico
Carbutamida/administração & dosagem
Fenômenos Químicos
Química
Combinação de Medicamentos/uso terapêutico
Tolerância Imunológica
Pneumonia por Pneumocystis/prevenção & controle
Ratos
Sulfametoxazol/uso terapêutico
Tolbutamida/administração & dosagem
Trimetoprima/uso terapêutico
Combinação Trimetoprima e Sulfametoxazol
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE; RESEARCH SUPPORT, U.S. GOV'T, P.H.S.
[Nm] Nome de substância:
0 (Anti-Infective Agents); 0 (Drug Combinations); 8064-90-2 (Trimethoprim, Sulfamethoxazole Drug Combination); 982XCM1FOI (Tolbutamide); AN164J8Y0X (Trimethoprim); E3K8P4869P (Carbutamide); JE42381TNV (Sulfamethoxazole)
[Em] Mês de entrada:8606
[Cu] Atualização por classe:151119
[Lr] Data última revisão:
151119
[Sb] Subgrupo de revista:AIM; IM
[Da] Data de entrada para processamento:860501
[St] Status:MEDLINE



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