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[PMID]:23796835
[Au] Autor:Aldawsari H; Altaf A; Banjar ZM; Iohara D; Nakabayashi M; Anraku M; Uekama K; Hirayama F
[Ad] Endereço:Faculty of Pharmacy, King Abdulaziz University, 80260, Jeddah 21589, Saudi Arabia.
[Ti] Título:Crystallization of a new polymorph of acetohexamide from 2-hydroxybutyl-ß-cyclodextrin solution: form VI with a high aqueous solubility.
[So] Source:Int J Pharm;453(2):315-21, 2013 Sep 10.
[Is] ISSN:1873-3476
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:A new polymorph of acetohexamide (Form VI) was prepared via the formation of a complex with 2-hydoxybutyl-ß-cyclodextrin (HB-ß-CD) in aqueous solution. An alkaline solution of acetohexamide and HB-ß-CD was adjusted to pH 4.0 by titration with hydrochloric acid. The resulting opaque solution was filtered through paper and allowed to stand at 4°C for 24h. The resulting precipitate was isolated on a filter and analyzed for polymorph content by powder X-ray diffractometry and thermal analysis. The diffraction pattern and thermal behavior of the precipitate was different from those of previously reported acetohexamide polymorphs (Forms I, III, IV and V), indicating that a new polymorph of the drug, i.e. Form VI was produced. This new polymorph was fairly stable against conversion to a stable form even at accelerated storage conditions. Crystalline Form VI was highly soluble in water and dissolved more rapidly than the other known polymorphs. This property was reflected in the blood concentrations of the drug after oral administration to rats.
[Mh] Termos MeSH primário: Acetoexamida/química
Hipoglicemiantes/química
beta-Ciclodextrinas/química
[Mh] Termos MeSH secundário: 2-Hidroxipropil-beta-Ciclodextrina
Acetoexamida/sangue
Acetoexamida/farmacocinética
Animais
Cristalização
Hipoglicemiantes/sangue
Hipoglicemiantes/farmacocinética
Masculino
Difração de Pó
Ratos
Ratos Wistar
Solubilidade
Difração de Raios X
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Hypoglycemic Agents); 0 (beta-Cyclodextrins); 1I96OHX6EK (2-Hydroxypropyl-beta-cyclodextrin); QGC8W08I6I (Acetohexamide)
[Em] Mês de entrada:1402
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:130626
[St] Status:MEDLINE


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[PMID]:23299527
[Au] Autor:Kretschy N; Teichmann M; Kopf S; Atanasov AG; Saiko P; Vonach C; Viola K; Giessrigl B; Huttary N; Raab I; Krieger S; Jäger W; Szekeres T; Nijman SM; Mikulits W; Dirsch VM; Dolznig H; Grusch M; Krupitza G
[Ad] Endereço:Institute of Clinical Pathology, Medical University of Vienna, Waehringer Guertel 18-20, A-1090 Vienna, Austria.
[Ti] Título:In vitro inhibition of breast cancer spheroid-induced lymphendothelial defects resembling intravasation into the lymphatic vasculature by acetohexamide, isoxsuprine, nifedipin and proadifen.
[So] Source:Br J Cancer;108(3):570-8, 2013 Feb 19.
[Is] ISSN:1532-1827
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: As metastasis is the prime cause of death from malignancies, there is vibrant interest to discover options for the management of the different mechanistic steps of tumour spreading. Some approved pharmaceuticals exhibit activities against diseases they have not been developed for. In order to discover such activities that might attenuate lymph node metastasis, we investigated 225 drugs, which are approved by the US Food and Drug Administration. METHODS: A three-dimensional cell co-culture assay was utilised measuring tumour cell-induced disintegrations of the lymphendothelial wall through which tumour emboli can intravasate as a limiting step in lymph node metastasis of ductal breast cancer. The disintegrated areas in the lymphendothelial cell (LEC) monolayers were induced by 12(S)-HETE, which is secreted by MCF-7 tumour cell spheroids, and are called 'circular chemorepellent induced defects' (CCIDs). The putative mechanisms by which active drugs prevented the formation of entry gates were investigated by western blotting, NF-κB activity assay and by the determination of 12(S)-HETE synthesis. RESULTS: Acetohexamide, nifedipin, isoxsuprine and proadifen dose dependently inhibited the formation of CCIDs in LEC monolayers and inhibited markers of epithelial-to-mesenchymal-transition and migration. The migration of LECs is a prerequisite of CCID formation, and these drugs either repressed paxillin levels or the activities of myosin light chain 2, or myosin-binding subunit of myosin phosphatase. Isoxsuprine inhibited all three migration markers, and isoxsuprine and acetohexamide suppressed the synthesis of 12(S)-HETE, whereas proadifen and nifedipin inhibited NF-κB activation. Both the signalling pathways independently cause CCID formation. CONCLUSION: The targeting of different mechanisms was most likely the reason for synergistic effects of different drug combinations on the inhibition of CCID formation. Furthermore, the treatment with drug combinations allowed also a several-fold reduction in drug concentrations. These results encourage further screening of approved drugs and their in vivo testing.
[Mh] Termos MeSH primário: Acetoexamida/farmacologia
Neoplasias da Mama/tratamento farmacológico
Endotélio Linfático/efeitos dos fármacos
Isoxsuprina/farmacologia
Vasos Linfáticos/efeitos dos fármacos
Nifedipino/farmacologia
Proadifeno/farmacologia
[Mh] Termos MeSH secundário: Ácido 12-Hidroxi-5,8,10,14-Eicosatetraenoico/metabolismo
Protocolos de Quimioterapia Combinada Antineoplásica
Western Blotting
Neoplasias da Mama/metabolismo
Neoplasias da Mama/patologia
Carcinoma Ductal de Mama/tratamento farmacológico
Carcinoma Ductal de Mama/metabolismo
Carcinoma Ductal de Mama/patologia
Adesão Celular/efeitos dos fármacos
Movimento Celular
Quimiotaxia/efeitos dos fármacos
Técnicas de Cocultura
Sinergismo Farmacológico
Endotélio Linfático/citologia
Endotélio Linfático/metabolismo
Inibidores Enzimáticos/farmacologia
Feminino
Seres Humanos
Hipoglicemiantes/farmacologia
Metástase Linfática
Vasos Linfáticos/irrigação sanguínea
Vasos Linfáticos/patologia
NF-kappa B/antagonistas & inibidores
NF-kappa B/genética
NF-kappa B/metabolismo
RNA Mensageiro/genética
Reação em Cadeia da Polimerase em Tempo Real
Reação em Cadeia da Polimerase Via Transcriptase Reversa
Transdução de Sinais/efeitos dos fármacos
Esferoides Celulares/metabolismo
Células Tumorais Cultivadas
Vasodilatadores/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Enzyme Inhibitors); 0 (Hypoglycemic Agents); 0 (NF-kappa B); 0 (RNA, Messenger); 0 (Vasodilator Agents); 59985-28-3 (12-Hydroxy-5,8,10,14-eicosatetraenoic Acid); A510CA4CBT (Proadifen); I9ZF7L6G2L (Nifedipine); QGC8W08I6I (Acetohexamide); R15UI3245N (Isoxsuprine)
[Em] Mês de entrada:1304
[Cu] Atualização por classe:150219
[Lr] Data última revisão:
150219
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:130110
[St] Status:MEDLINE
[do] DOI:10.1038/bjc.2012.580


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[PMID]:21612784
[Au] Autor:Tong Z; Joseph KS; Hage DS
[Ad] Endereço:Chemistry Department, University of Nebraska, Lincoln, NE 68588-0304, USA.
[Ti] Título:Detection of heterogeneous drug-protein binding by frontal analysis and high-performance affinity chromatography.
[So] Source:J Chromatogr A;1218(49):8915-24, 2011 Dec 09.
[Is] ISSN:1873-3778
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:This study examined the use of frontal analysis and high-performance affinity chromatography for detecting heterogeneous binding in biomolecular interactions, using the binding of acetohexamide with human serum albumin (HSA) as a model. It was found through the use of this model system and chromatographic theory that double-reciprocal plots could be used more easily than traditional isotherms for the initial detection of binding site heterogeneity. The deviations from linearity that were seen in double-reciprocal plots as a result of heterogeneity were a function of the analyte concentration, the relative affinities of the binding sites in the system and the amount of each type of site that was present. The size of these deviations was determined and compared under various conditions. Plots were also generated to show what experimental conditions would be needed to observe these deviations for general heterogeneous systems or for cases in which some preliminary information was available on the extent of binding heterogeneity. The methods developed in this work for the detection of binding heterogeneity are not limited to drug interactions with HSA but could be applied to other types of drug-protein binding or to additional biological systems with heterogeneous binding.
[Mh] Termos MeSH primário: Cromatografia de Afinidade/métodos
Interações Medicamentosas
Proteínas Imobilizadas/metabolismo
Modelos Químicos
[Mh] Termos MeSH secundário: Acetoexamida/química
Acetoexamida/metabolismo
Sítios de Ligação
Seres Humanos
Proteínas Imobilizadas/química
Ligação Proteica
Albumina Sérica/química
Albumina Sérica/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, N.I.H., EXTRAMURAL
[Nm] Nome de substância:
0 (Immobilized Proteins); 0 (Serum Albumin); QGC8W08I6I (Acetohexamide)
[Em] Mês de entrada:1202
[Cu] Atualização por classe:161019
[Lr] Data última revisão:
161019
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:110527
[St] Status:MEDLINE
[do] DOI:10.1016/j.chroma.2011.04.078


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[PMID]:20829128
[Au] Autor:Joseph KS; Anguizola J; Jackson AJ; Hage DS
[Ad] Endereço:Chemistry Department, University of Nebraska, Lincoln, NE 68588-0304, USA.
[Ti] Título:Chromatographic analysis of acetohexamide binding to glycated human serum albumin.
[So] Source:J Chromatogr B Analyt Technol Biomed Life Sci;878(28):2775-81, 2010 Oct 15.
[Is] ISSN:1873-376X
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Acetohexamide is a drug used to treat type II diabetes and is tightly bound to the protein human serum albumin (HSA) in the circulation. It has been proposed that the binding of some drugs with HSA can be affected by the non-enzymatic glycation of this protein. This study used high-performance affinity chromatography to examine the changes in acetohexamide-HSA binding that take place as the glycation of HSA is increased. It was found in frontal analysis experiments that the binding of acetohexamide to glycated HSA could be described by a two-site model involving both strong and weak affinity interactions. The average association equilibrium constant (K(a)) for the high affinity interactions was in the range of 1.2-2.0×10(5)M(-1) and increased in moving from normal HSA to HSA with glycation levels that might be found in advanced diabetes. It was found through competition studies that acetohexamide was binding at both Sudlow sites I and II on the glycated HSA. The K(a) for acetohexamide at Sudlow site I increased by 40% in going from normal HSA to minimally glycated HSA but then decreased back to near-normal values in going to more highly glycated HSA. At Sudlow site II, the K(a) for acetohexamide first decreased by about 40% and then increased in going from normal HSA to minimally glycated HSA and more highly glycated HSA. This information demonstrates the importance of conducting both frontal analysis and site-specific binding studies in examining the effects of glycation on the interactions of a drug with HSA.
[Mh] Termos MeSH primário: Acetoexamida/química
Cromatografia de Afinidade/métodos
Cromatografia Líquida de Alta Pressão/métodos
Albumina Sérica/química
[Mh] Termos MeSH secundário: Acetoexamida/metabolismo
Diabetes Mellitus/tratamento farmacológico
Diabetes Mellitus/metabolismo
Seres Humanos
Hipoglicemiantes/química
Hipoglicemiantes/metabolismo
Ligação Proteica
Análise de Regressão
Albumina Sérica/metabolismo
Triptofano/química
Triptofano/metabolismo
Varfarina/química
Varfarina/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, N.I.H., EXTRAMURAL
[Nm] Nome de substância:
0 (Hypoglycemic Agents); 0 (Serum Albumin); 0 (glycosylated serum albumin); 5Q7ZVV76EI (Warfarin); 8DUH1N11BX (Tryptophan); QGC8W08I6I (Acetohexamide)
[Em] Mês de entrada:1101
[Cu] Atualização por classe:161019
[Lr] Data última revisão:
161019
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:100911
[St] Status:MEDLINE
[do] DOI:10.1016/j.jchromb.2010.08.021


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[PMID]:20435530
[Au] Autor:Joseph KS; Hage DS
[Ad] Endereço:Chemistry Department, University of Nebraska-Lincoln, Lincoln, NE 68588-0304, USA.
[Ti] Título:Characterization of the binding of sulfonylurea drugs to HSA by high-performance affinity chromatography.
[So] Source:J Chromatogr B Analyt Technol Biomed Life Sci;878(19):1590-8, 2010 Jun 01.
[Is] ISSN:1873-376X
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Sulfonylurea drugs are often prescribed as a treatment for type II diabetes to help lower blood sugar levels by stimulating insulin secretion. These drugs are believed to primarily bind in blood to human serum albumin (HSA). This study used high-performance affinity chromatography (HPAC) to examine the binding of sulfonylureas to HSA. Frontal analysis with an immobilized HSA column was used to determine the association equilibrium constants (Ka) and number of binding sites on HSA for the sulfonylurea drugs acetohexamide and tolbutamide. The results from frontal analysis indicated HSA had a group of relatively high-affinity binding regions and weaker binding sites for each drug, with average Ka values of 1.3 (+/-0.2) x 10(5) and 3.5 (+/-3.0) x 10(2) M(-1) for acetohexamide and values of 8.7 (+/-0.6) x 10(4) and 8.1 (+/-1.7) x 10(3) M(-1) for tolbutamide. Zonal elution and competition studies with site-specific probes were used to further examine the relatively high-affinity interactions of these drugs by looking directly at the interactions that were occurring at Sudlow sites I and II of HSA (i.e., the major drug-binding sites on this protein). It was found that acetohexamide was able to bind at both Sudlow sites I and II, with Ka values of 1.3 (+/-0.1) x 10(5) and 4.3 (+/-0.3) x 10(4) M(-1), respectively, at 37 degrees C. Tolbutamide also appeared to interact with both Sudlow sites I and II, with Ka values of 5.5 (+/-0.2) x 10(4) and 5.3 (+/-0.2) x 10(4) M(-1), respectively. The results provide a more quantitative picture of how these drugs bind with HSA and illustrate how HPAC and related tools can be used to examine relatively complex drug-protein interactions.
[Mh] Termos MeSH primário: Acetoexamida/análise
Cromatografia de Afinidade/métodos
Proteínas Imobilizadas/metabolismo
Albumina Sérica/metabolismo
Tolbutamida/análise
[Mh] Termos MeSH secundário: Acetoexamida/metabolismo
Seres Humanos
Hipoglicemiantes/análise
Hipoglicemiantes/metabolismo
Cinética
Modelos Químicos
Dinâmica não Linear
Ligação Proteica
Tolbutamida/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, N.I.H., EXTRAMURAL
[Nm] Nome de substância:
0 (Hypoglycemic Agents); 0 (Immobilized Proteins); 0 (Serum Albumin); 982XCM1FOI (Tolbutamide); QGC8W08I6I (Acetohexamide)
[Em] Mês de entrada:1008
[Cu] Atualização por classe:161019
[Lr] Data última revisão:
161019
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:100504
[St] Status:MEDLINE
[do] DOI:10.1016/j.jchromb.2010.04.019


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[PMID]:16541746
[Au] Autor:Tokunaga H; Uchino T
[Ad] Endereço:tokunaga@nihs.go.jp
[Ti] Título:[Studies for analyzing the prohibited ingredients such as acetohexamide in cosmetics].
[So] Source:Kokuritsu Iyakuhin Shokuhin Eisei Kenkyusho Hokoku;(123):19-22, 2005.
[Is] ISSN:1343-4292
[Cp] País de publicação:Japan
[La] Idioma:jpn
[Ab] Resumo:Acetohexamide (AH) is nominated as the prohibited ingredients in cosmetics in Japanese Pharmaceutical Affairs Act. So the analytical method for AH was investigated by HPLC. The lotion or milky lotion of 0.5g was put into a 10-ml volumetric flask. After adding 1.0ml of AH solution at 50 microg/ml into the volumetric flask, the mixture was made up to 10ml with methanol as the testing solution. Creams were procedured as follows; 0.5 g of cream was put into a 10-ml volumetric flask. After adding 1.0ml of tetrahydrofuran into the volumetric flask, the mixture was stirred for several minutes and the ingredients of the creams were dissolved. After adding 1.0ml of AH solution at 50 microg/ml into the volumetric flask, the mixture was made up to 10ml with methanol. One milliliter of the mixture including AH at 5 microg/ml was exactly put into a test tube with a cap and then 1 ml of water and 1 ml of hexane were added. After shaking vigorously, stand for several minutes. After centrifuging, the hexane layer was eliminated and the residual mixture was used as the test solution. The testing solution of 20 microl was analyzed by HPLC using the ODS column (CAPCELL PAK C18 column, 4.6 x 250mm), the mixture of acetonitrile and 50 mmol/l phosphate buffer(pH 5.3)(3:1) and the detection wavelength of 247 nm. The working curve from 0.5 to 6.0 microg/ml showed a linear line between the concentrations of AH and the peak areas. There was no interference of peak of AH with the ingredients such as methylparaben, ethylparaben in the lotions, milky lotion and creams.
[Mh] Termos MeSH primário: Acetoexamida/análise
Cromatografia Líquida de Alta Pressão/métodos
Cosméticos/análise
Hipoglicemiantes/análise
[Mh] Termos MeSH secundário: Japão
Legislação de Medicamentos
[Pt] Tipo de publicação:ENGLISH ABSTRACT; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Cosmetics); 0 (Hypoglycemic Agents); QGC8W08I6I (Acetohexamide)
[Em] Mês de entrada:0604
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:060318
[St] Status:MEDLINE


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[PMID]:15635190
[Au] Autor:Imamura Y; Shimada H
[Ad] Endereço:Graduate School of Pharmaceutical Sciences, Kumamoto University, Japan. yorishig@gpo.kumamoto-u.ac.jp
[Ti] Título:Differential pharmacokinetics of acetohexamide in male Wistar-Imamichi and Sprague-Dawley rats: role of microsomal carbonyl reductase.
[So] Source:Biol Pharm Bull;28(1):185-7, 2005 Jan.
[Is] ISSN:0918-6158
[Cp] País de publicação:Japan
[La] Idioma:eng
[Ab] Resumo:Acetohexamide (AH) is reduced to its alcohol metabolite by carbonyl reductase. We have previously shown that carbonyl reductase present in the liver microsomes of rats is a male-specific and androgen-dependent enzyme. In the present study, the role of microsomal carbonyl reductase in the pharmacokinetics of AH was examined in male Wistar-Imamichi (WI) and Sprague-Dawley (SD) rats after its intravenous administration. AH was eliminated more slowly from plasma in the WI strain, which lacks most of the microsomal carbonyl reductase, than in the SD strain. Furthermore, several pharmacokinetic parameters were derived from the data for the plasma concentrations of AH. The plasma clearance (CL(p)) of AH (72.8+/-11.2 ml/h/kg) in male WI rats was significantly smaller than that (105.5+/-11.1 ml/h/kg) in male SD rats. Testectomy caused a marked decrease, from 105.5+/-11.1 to 44.3+/-11.8 ml/h/kg, in the CL(p) of AH in male SD rats. These results indicate that microsomal carbonyl reductase plays a critical role in the differential pharmacokinetics of AH in male WI and SD rats.
[Mh] Termos MeSH primário: Acetoexamida/farmacocinética
Oxirredutases do Álcool/metabolismo
Microssomos/metabolismo
[Mh] Termos MeSH secundário: Acetoexamida/sangue
Aldeído Redutase
Aldo-Ceto Redutases
Animais
Feminino
Masculino
Ratos
Ratos Sprague-Dawley
Ratos Wistar
Especificidade da Espécie
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE
[Nm] Nome de substância:
EC 1.1.- (Alcohol Oxidoreductases); EC 1.1.1.- (Aldo-Keto Reductases); EC 1.1.1.21 (Aldehyde Reductase); QGC8W08I6I (Acetohexamide)
[Em] Mês de entrada:0505
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:050107
[St] Status:MEDLINE


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[PMID]:15558648
[Au] Autor:Imamura Y; Shimada H
[Ad] Endereço:Graduate School of Pharmaceutical Sciences, Kumamoto University, 5-1 Oe-honmachi, Kumamoto 862-0973, Japan. yorishig@gpo.kumamoto-u.ac.jp
[Ti] Título:Strain- and sex-related differences of carbonyl reductase activities in kidney microsomes and cytosol of rats.
[So] Source:J Appl Toxicol;24(6):437-41, 2004 Nov-Dec.
[Is] ISSN:0260-437X
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:This study was designed to elucidate strain- and sex-related differences of carbonyl reductase activity in rat kidney by using the oral antidiabetic drug acetohexamide as substrate. The frequency distribution of carbonyl reductase activities in kidney microsomes of male Fischer 344 (Fischer), Sprague-Dawley, Wistar and Wistar-Imamichi (Wistar-IM) rats exhibited a marked strain-related difference. Furthermore, the enzyme activities in kidney microsomes of Fischer, Sprague-Dawley and Wistar rats were male-specific, resulting insignificant sex-related differences in these strains. There was no sex-related difference of carbonyl reductase activity in kidney microsomes of the Wistar-IM strain, which lacked its activity in both sexes. On the other hand, although carbonyl reductase activities were fully detectable in kidney cytosols from all the strains of male and female rats, no strain- or sex-related difference was observed among the cytosolic enzyme activities. These results provide new information for understanding the influence of internal factors on the renal metabolism of ketone-containing xenobiotics.
[Mh] Termos MeSH primário: Oxirredutases do Álcool/farmacologia
[Mh] Termos MeSH secundário: Acetoexamida/farmacologia
Oxirredutases do Álcool/análise
Animais
Citosol/enzimologia
Feminino
Hipoglicemiantes
Masculino
Microssomos/enzimologia
Ratos
Ratos Endogâmicos F344
Ratos Sprague-Dawley
Ratos Wistar
Reprodutibilidade dos Testes
Fatores Sexuais
Xenobióticos/metabolismo
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Hypoglycemic Agents); 0 (Xenobiotics); EC 1.1.- (Alcohol Oxidoreductases); QGC8W08I6I (Acetohexamide)
[Em] Mês de entrada:0502
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:041124
[St] Status:MEDLINE


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[PMID]:12458186
[Au] Autor:Imamura Y; Kaneko M; Takada H; Otagiri M; Shimada H; Akita H
[Ad] Endereço:Faculty of Pharmaceutical Sciences, Kumamoto University, 5-1, Oe-honmachi, Kumamoto 862-0973, Japan. yorishig@gpo.kumamoto-u.ac.jp
[Ti] Título:Sex-dependent pharmacokinetics of S(-)-hydroxyhexamide, a pharmacologically active metabolite of acetohexamide, in rats.
[So] Source:Comp Biochem Physiol C Toxicol Pharmacol;133(4):587-92, 2002 Dec.
[Is] ISSN:1532-0456
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The pharmacokinetic profile of S(-)-hydroxyhexamide (S-HH), a pharmacologically active metabolite of acetohexamide, was examined in male and female rats. S-HH was eliminated more rapidly from plasma in the males than in the females. A significant sex difference was observed in the pharmacokinetic parameters of S-HH in rats. Testectomy caused significant alteration in these parameters of S-HH in male rats, whereas ovariectomy did not in the females. The co-administration of sulfamethazine significantly decreased the plasma clearance (CL(p)) of S-HH in male rats, but had no effect in the females. The plasma concentrations of acetohexamide generated from S-HH showed no sex-related difference. Furthermore, there was no difference in the accumulation of S-HH by renal cortical slices from male and female rats. We propose the possibility that the sex-dependent pharmacokinetics of S-HH in rats is mediated through the male-specific hydroxylation of the cyclohexyl ring catalyzed by a major cytochrome p450 (CYP) isoform (CYP2C11), although the detailed mechanism remains to be elucidated.
[Mh] Termos MeSH primário: Acetoexamida/análogos & derivados
Acetoexamida/metabolismo
Acetoexamida/farmacocinética
Caracteres Sexuais
[Mh] Termos MeSH secundário: Acetoexamida/administração & dosagem
Acetoexamida/sangue
Animais
Feminino
Masculino
Ratos
Ratos Wistar
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
F3F26TZ9HN (hydroxyhexamide); QGC8W08I6I (Acetohexamide)
[Em] Mês de entrada:0307
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:021130
[St] Status:MEDLINE


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[PMID]:11875619
[Au] Autor:Shimada H; Yamaguchi S; Murata H; Otagiri M; Imamura Y
[Ad] Endereço:Faculty of Education, Kumamoto University, 2-40-1, Kurokami, Kumamoto 860-8555, Japan.
[Ti] Título:Cadmium exposure decreases androgen-dependent metabolism of acetohexamide in liver microsomes of male rats through its testicular toxicity.
[So] Source:Arch Toxicol;76(1):8-12, 2002 Feb.
[Is] ISSN:0340-5761
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:Administration of cadmium (Cd) at a dose of 1.23 mg/kg (2.0 mg/kg as CdCl(2)) markedly decreased the activity of an enzyme (acetohexamide reductase) catalysing the ketone-reduction of acetohexamide, an oral antidiabetic drug, in liver microsomes of male rats. However, the decreased enzyme activity was increased by repeated treatment with testosterone propionate (TP). When male rats were castrated and TP was given to the castrated ones, a similar decrease and increase, as described above, were observed in the microsomal enzyme activity. Cd exposure to male rats induced haemorrhage and atrophy of the testes and significantly diminished serum testosterone levels. There was no possibility that Cd accumulated in liver microsomes of male rats causing direct inhibition of the microsomal enzyme activity. We conclude that Cd exposure decreases androgen-dependent metabolism of acetohexamide in liver microsomes of male rats through its testicular toxicity. Cd exposure had no effect on acetohexamide reductase activity in liver cytosol of male rats.
[Mh] Termos MeSH primário: Acetoexamida/metabolismo
Cádmio/toxicidade
Hipoglicemiantes/metabolismo
Microssomos Hepáticos/efeitos dos fármacos
Testículo/efeitos dos fármacos
Testosterona/sangue
[Mh] Termos MeSH secundário: Acetoexamida/administração & dosagem
Oxirredutases do Álcool/efeitos dos fármacos
Oxirredutases do Álcool/metabolismo
Animais
Citosol/efeitos dos fármacos
Citosol/enzimologia
Relação Dose-Resposta a Droga
Sinergismo Farmacológico
Hipoglicemiantes/administração & dosagem
Injeções Intraperitoneais
Injeções Subcutâneas
Masculino
Microssomos Hepáticos/enzimologia
Orquiectomia
Ratos
Ratos Wistar
Testículo/metabolismo
Testosterona/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Hypoglycemic Agents); 00BH33GNGH (Cadmium); 3XMK78S47O (Testosterone); EC 1.1.- (Alcohol Oxidoreductases); EC 1.1.1.- (acetohexamide reductase); QGC8W08I6I (Acetohexamide)
[Em] Mês de entrada:0204
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:020305
[St] Status:MEDLINE



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