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[PMID]:28591345
[Au] Autor:Lucchetta RC; Riveros BS; Pontarolo R; Radominski RB; Otuki MF; Fernandez-Llimos F; Correr CJ
[Ad] Endereço:Laboratório de Serviços Clínicos e Evidências em Saúde, Departamento de Farmácia, Universidade Federal do Paraná (UFPR), Curitiba, PR, BR.
[Ti] Título:Systematic review and meta-analysis of the efficacy and safety of amfepramone and mazindol as a monotherapy for the treatment of obese or overweight patients.
[So] Source:Clinics (Sao Paulo);72(5):317-324, 2017 May.
[Is] ISSN:1980-5322
[Cp] País de publicação:Brazil
[La] Idioma:eng
[Ab] Resumo:The aim of this study was to evaluate efficacy and safety of amfepramone, fenproporex and mazindol as a monotherapy for the treatment of obese or overweight patients. A systematic review of primary studies was conducted, followed by a direct meta-analysis (random effect) and mixed treatment comparison. Medline and other databases were searched. Heterogeneity was explored through I2 associated with a p-value. Of 739 identified publications, 25 were included in the meta-analysis. The global evaluation of Cochrane resulted in 19 studies with a high level of bias and six with unclear risk. Due to the lack of information in primary studies, direct meta-analyses were conducted only for amfepramone and mazindol. Compared to placebo, amfepramone resulted in higher weight loss in the short-term (<180 days; mean difference (MD) -1.281 kg; p<0.05; I2: 0.0%; p=0.379) and long-term (≥180 days; MD -6.518 kg; p<0.05; I2: 0.0%; p=0.719). Only studies with long-term follow up reported efficacy in terms of abdominal circumference and 5-10% weight reduction. These results corroborated the finding that the efficacy of amfepramone is greater than that of placebo. Treatment with mazindol showed greater short-term weight loss than that with placebo (MD -1.721 kg; p<0.05; I2: 0.9%; p=0.388). However, metabolic outcomes were poorly described, preventing a meta-analysis. A mixed treatment comparison corroborated the direct meta-analysis. Considering the high level of risk of bias and the absence of important published outcomes for anti-obesity therapy assessments, this study found that the evaluated drugs showed poor evidence of efficacy in the treatment of overweight and obese patients. Robust safety data were not identified to suggest changes in their regulatory status.
[Mh] Termos MeSH primário: Depressores do Apetite/uso terapêutico
Dietilpropiona/uso terapêutico
Mazindol/uso terapêutico
Obesidade/tratamento farmacológico
Sobrepeso/tratamento farmacológico
[Mh] Termos MeSH secundário: Depressores do Apetite/metabolismo
Dietilpropiona/metabolismo
Seres Humanos
Mazindol/metabolismo
Obesidade/metabolismo
Sobrepeso/metabolismo
Viés de Publicação
Reprodutibilidade dos Testes
Fatores de Risco
Resultado do Tratamento
Perda de Peso/efeitos dos fármacos
[Pt] Tipo de publicação:JOURNAL ARTICLE; META-ANALYSIS; REVIEW
[Nm] Nome de substância:
0 (Appetite Depressants); C56709M5NH (Mazindol); Q94YYU22B8 (Diethylpropion)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170925
[Lr] Data última revisão:
170925
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170608
[St] Status:MEDLINE


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[PMID]:28489121
[Au] Autor:Lucchetta RC; Riveros BS; Pontarolo R; Radominski RB; Otuki MF; Fernandez-Llimos F; Correr CJ
[Ad] Endereço:Laboratory of Clinical Services and Evidence in Health, Pharmacy Department, Universidade Federal do Paraná (UFPR), Curitiba, PR, Brazil.
[Ti] Título:Diethylpropion and mazindol: An end to the discussion?
[So] Source:Rev Assoc Med Bras (1992);63(3):203-206, 2017 Mar.
[Is] ISSN:1806-9282
[Cp] País de publicação:Brazil
[La] Idioma:eng
[Ab] Resumo:Antiobesity pharmacotherapy remains the main point of disagreement among both scientists and regulators. This is probably due to small sample sizes, high levels of heterogeneity, and low methodological quality. For many years, Brazil was one of the largest consumers of appetite suppressants worldwide, with evidence of irrational use of this drug class. Therefore, the country was the scene of a debate that divided the Brazilian Health Surveillance Agency (Anvisa - Agência Nacional de Vigilância Sanitária) and medical societies over the maintenance record of diethylpropion, mazindol and fenproporex. In this context, this commentary presents new arguments to contribute to the discussion, as well as recommendations for future studies.
[Mh] Termos MeSH primário: Depressores do Apetite/uso terapêutico
Dietilpropiona/uso terapêutico
Mazindol/uso terapêutico
Obesidade/tratamento farmacológico
[Mh] Termos MeSH secundário: Anfetaminas/uso terapêutico
Brasil
Ciclobutanos/uso terapêutico
Aprovação de Drogas
Seres Humanos
Medição de Risco/tendências
Resultado do Tratamento
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Amphetamines); 0 (Appetite Depressants); 0 (Cyclobutanes); C56709M5NH (Mazindol); Q94YYU22B8 (Diethylpropion); W0194S5FOA (fenproporex); WV5EC51866 (sibutramine)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:170829
[Lr] Data última revisão:
170829
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170511
[St] Status:MEDLINE


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[PMID]:26867698
[Au] Autor:Kalyanasundar B; Solorio J; Perez CI; Hoyo-Vadillo C; Simon SA; Gutierrez R
[Ad] Endereço:Laboratory of Neurobiology of Appetite; Department of Pharmacology, CINVESTAV-IPN, 07360 Mexico City, Mexico.
[Ti] Título:The efficacy of the appetite suppressant, diethylpropion, is dependent on both when it is given (day vs. night) and under conditions of high fat dietary restriction.
[So] Source:Appetite;100:152-61, 2016 May 01.
[Is] ISSN:1095-8304
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Obesity is a public health problem caused by excessive consumption of high caloric diets and/or lack of physical activity. Although treatments for obesity include low caloric diets and exercise programs, these activities frequently are supplemented with appetite suppressants. For the short-term treatment of weight loss, diethylpropion (DEP) is a commonly used appetite suppressant. However, little is known with regard to how to improve its weight loss efficacy. We therefore evaluated, in rats, two administration protocols where the animals received daily injections of DEP. First, when these nocturnal animals were normally active (at night) and when they were normally inactive (daytime), and second, with or without high fat dietary restriction (HFDR). We observed that DEP induced a greater weight-loss administered when the animals were in their active phase than in their inactive phase. Moreover, DEP's administration during the inactive phase (and to a lesser degree in the active phase) promotes the consumption of food during normal sleeping time. In addition, we found that DEP-induced weight loss under ad libitum access to a HF diet, but its efficacy significantly improved under conditions of HFDR. In summary, the efficacy of DEP, and presumably other like appetite suppressants, is enhanced by carefully controlling the time it is administered and under dietary restriction of HF diets.
[Mh] Termos MeSH primário: Depressores do Apetite/uso terapêutico
Regulação do Apetite/efeitos dos fármacos
Dieta com Restrição de Gorduras
Dieta Redutora
Dietilpropiona/uso terapêutico
Sobrepeso/tratamento farmacológico
Perda de Peso/efeitos dos fármacos
[Mh] Termos MeSH secundário: Animais
Depressores do Apetite/administração & dosagem
Depressores do Apetite/efeitos adversos
Depressores do Apetite/farmacocinética
Biotransformação
Ritmo Circadiano/efeitos dos fármacos
Terapia Combinada/efeitos adversos
Dieta Hiperlipídica/efeitos adversos
Dietilpropiona/administração & dosagem
Dietilpropiona/efeitos adversos
Dietilpropiona/análogos & derivados
Dietilpropiona/sangue
Dietilpropiona/farmacocinética
Esquema de Medicação
Ingestão de Energia/efeitos dos fármacos
Meia-Vida
Injeções Intraperitoneais
Masculino
Sobrepeso/sangue
Sobrepeso/dietoterapia
Sobrepeso/etiologia
Fenilpropanolamina/análogos & derivados
Fenilpropanolamina/sangue
Ratos Sprague-Dawley
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Appetite Depressants); 18259-37-5 (N-ethylaminopropiophenone); 33RU150WUN (Phenylpropanolamine); 37025-60-8 (N-diethylnorpseudoephedrine); Q94YYU22B8 (Diethylpropion)
[Em] Mês de entrada:1612
[Cu] Atualização por classe:161217
[Lr] Data última revisão:
161217
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160213
[St] Status:MEDLINE


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[PMID]:26073353
[Au] Autor:Soto-Molina H; Pizarro-Castellanos M; Rosado-Pérez J; Rizzoli-Córdoba A; Lara-Padilla E; del Valle-Laisequilla CF; Reyes-García JG
[Ti] Título:Six-month efficacy and safety of amfepramone in obese Mexican patients: a double-blinded, randomized, controlled trial.
[So] Source:Int J Clin Pharmacol Ther;53(7):541-9, 2015 Jul.
[Is] ISSN:0946-1965
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:Amfepramone, also known as diethylpropion, is an anorectic drug used for the short-term treatment of obesity; however, its efficacy and safety during periods greater than 3 months has been scarcely studied. To evaluate the 6-month efficacy and safety of amfepramone treatment in obese adult Mexican patients resistant to diet and exercise, a double-blinded, randomized, and placebo-controlled clinical trial study was designed on 156 volunteers with a body mass index (BMI) greater than 30 kg/m2 and less than 45 kg/m2. Patients were randomized to receive a 75 mg tablet of amfepramone or placebo daily for 6 months. Primary outcome was the absolute body weight loss, whereas secondary outcomes were the percentage of patients who achieved at least 5% or 10% weight loss, as well as the improvement of anthropometric and metabolic parameters. Amfepramone treatment produced a superior efficacy to decrease body weight than placebo at 3 months (-4.9±0.25 kg vs. -0.7±0.32 kg) and 6 months (-7.7±0.52 kg vs. -1.1±0.7 kg). In addition, 64 and 34 patients achieved at least 5% or 10% weight loss, respectively, with amfepramone at 6 months, compared with 8 and 0 patients on placebo. Amfepramone also significantly improved BMI and waist circumference, but it only showed a favorable tendency in the waist-hip index (WHI), glucose, total cholesterol, low-density lipoproteins (LDL), high-density lipoproteins (HDL), triglycerides, heart rate, systolic blood pressure, and diastolic blood pressure at 3 and 6 months. Amfepramone produced only mild adverse events, and they were presented in a greater number than placebo only at 3 months, dry mouth being the the main adverse event. Data suggest that amfepramone is effective and well tolerated in obese Mexican patients during a 6-month regimen.
[Mh] Termos MeSH primário: Depressores do Apetite/uso terapêutico
Dietilpropiona/uso terapêutico
Obesidade/tratamento farmacológico
Perda de Peso/efeitos dos fármacos
[Mh] Termos MeSH secundário: Adulto
Depressores do Apetite/efeitos adversos
Biomarcadores/sangue
Glicemia/efeitos dos fármacos
Glicemia/metabolismo
Pressão Sanguínea/efeitos dos fármacos
Índice de Massa Corporal
Dietilpropiona/efeitos adversos
Método Duplo-Cego
Feminino
Frequência Cardíaca/efeitos dos fármacos
Seres Humanos
Lipídeos/sangue
Masculino
México/epidemiologia
Obesidade/sangue
Obesidade/diagnóstico
Obesidade/epidemiologia
Obesidade/fisiopatologia
Fatores de Tempo
Resultado do Tratamento
Circunferência da Cintura
Relação Cintura-Quadril
[Pt] Tipo de publicação:CLINICAL TRIAL, PHASE III; JOURNAL ARTICLE; RANDOMIZED CONTROLLED TRIAL
[Nm] Nome de substância:
0 (Appetite Depressants); 0 (Biomarkers); 0 (Blood Glucose); 0 (Lipids); Q94YYU22B8 (Diethylpropion)
[Em] Mês de entrada:1510
[Cu] Atualização por classe:151119
[Lr] Data última revisão:
151119
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:150616
[St] Status:MEDLINE
[do] DOI:10.5414/CP202135


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[PMID]:25972577
[Au] Autor:Kalyanasundar B; Perez CI; Luna A; Solorio J; Moreno MG; Elias D; Simon SA; Gutierrez R
[Ad] Endereço:Laboratory of Neurobiology of Appetite, Department of Pharmacology, Centro de Investigación y de Estudios Avanzados (CINVESTAV), Mexico City, Mexico;
[Ti] Título:D1 and D2 antagonists reverse the effects of appetite suppressants on weight loss, food intake, locomotion, and rebalance spiking inhibition in the rat NAc shell.
[So] Source:J Neurophysiol;114(1):585-607, 2015 Jul.
[Is] ISSN:1522-1598
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Obesity is a worldwide health problem that has reached epidemic proportions. To ameliorate this problem, one approach is the use of appetite suppressants. These compounds are frequently amphetamine congeners such as diethylpropion (DEP), phentermine (PHEN), and bupropion (BUP), whose effects are mediated through serotonin, norepinephrine, and dopaminergic pathways. The nucleus accumbens (NAc) shell receives dopaminergic inputs and is involved in feeding and motor activity. However, little is known about how appetite suppressants modulate its activity. Therefore, we characterized behavioral and neuronal NAc shell responses to short-term treatments of DEP, PHEN, and BUP. These compounds caused a transient decrease in weight and food intake while increasing locomotion, stereotypy, and insomnia. They evoked a large inhibitory imbalance in NAc shell spiking activity that correlated with the onset of locomotion and stereotypy. Analysis of the local field potentials (LFPs) showed that all three drugs modulated beta, theta, and delta oscillations. These oscillations do not reflect an aversive-malaise brain state, as ascertained from taste aversion experiments, but tracked both the initial decrease in weight and food intake and the subsequent tolerance to these drugs. Importantly, the appetite suppressant-induced weight loss and locomotion were markedly reduced by intragastric (and intra-NAc shell) infusions of dopamine antagonists SCH-23390 (D1 receptor) or raclopride (D2 receptor). Furthermore, both antagonists attenuated appetite suppressant-induced LFP oscillations and partially restored the imbalance in NAc shell activity. These data reveal that appetite suppressant-induced behavioral and neuronal activity recorded in the NAc shell depend, to various extents, on dopaminergic activation and thus point to an important role for D1/D2-like receptors (in the NAc shell) in the mechanism of action for these anorexic compounds.
[Mh] Termos MeSH primário: Depressores do Apetite/farmacologia
Antagonistas dos Receptores de Dopamina D2/farmacologia
Núcleo Accumbens/efeitos dos fármacos
Receptores de Dopamina D1/antagonistas & inibidores
[Mh] Termos MeSH secundário: Potenciais de Ação/efeitos dos fármacos
Potenciais de Ação/fisiologia
Animais
Depressores do Apetite/efeitos adversos
Benzazepinas/farmacologia
Bupropiona/efeitos adversos
Bupropiona/farmacologia
Dietilpropiona/efeitos adversos
Dietilpropiona/farmacologia
Interações Medicamentosas
Ingestão de Alimentos/efeitos dos fármacos
Ingestão de Alimentos/fisiologia
Locomoção/efeitos dos fármacos
Locomoção/fisiologia
Masculino
Núcleo Accumbens/fisiologia
Fentermina/efeitos adversos
Fentermina/farmacologia
Racloprida/farmacologia
Distribuição Aleatória
Ratos Sprague-Dawley
Receptores de Dopamina D1/metabolismo
Receptores de Dopamina D2/metabolismo
Distúrbios do Início e da Manutenção do Sono/induzido quimicamente
Comportamento Estereotipado/efeitos dos fármacos
Comportamento Estereotipado/fisiologia
Perda de Peso/efeitos dos fármacos
Perda de Peso/fisiologia
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Appetite Depressants); 0 (Benzazepines); 0 (Dopamine D2 Receptor Antagonists); 0 (Receptors, Dopamine D1); 0 (Receptors, Dopamine D2); 0 (SCH 23390); 01ZG3TPX31 (Bupropion); 430K3SOZ7G (Raclopride); C045TQL4WP (Phentermine); Q94YYU22B8 (Diethylpropion)
[Em] Mês de entrada:1603
[Cu] Atualização por classe:170220
[Lr] Data última revisão:
170220
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:150515
[St] Status:MEDLINE
[do] DOI:10.1152/jn.00012.2015


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[PMID]:25831200
[Au] Autor:López-Canales JS; Lozano-Cuenca J; Muãoz-Islas E; Aguilar-Carrasco JC; López-Canales OA; López-Mayorga RM; Castillo-Henkel EF; Valencia-Hernández I; Castillo-Henkel C
[Ad] Endereço:Section of Postgraduate Studies and Investigation, Higher School of Medicine from the National Polytechnic Institute, Mexico City, Mexico.
[Ti] Título:Mechanisms involved in the vasorelaxant effects produced by the acute application of amfepramone in vitro to rat aortic rings.
[So] Source:Braz J Med Biol Res;48(6):537-44, 2015 Jun.
[Is] ISSN:1414-431X
[Cp] País de publicação:Brazil
[La] Idioma:eng
[Ab] Resumo:Amfepramone (diethylpropion) is an appetite-suppressant drug used for the treatment of overweight and obesity. It has been suggested that the systemic and central activity of amfepramone produces cardiovascular effects such as transient ischemic attacks and primary pulmonary hypertension. However, it is not known whether amfepramone produces immediate vascular effects when applied in vitro to rat aortic rings and, if so, what mechanisms may be involved. We analyzed the effect of amfepramone on phenylephrine-precontracted rat aortic rings with or without endothelium and the influence of inhibitors or blockers on this effect. Amfepramone produced a concentration-dependent vasorelaxation in phenylephrine-precontracted rat aortic rings that was not affected by the vehicle, atropine, 4-AP, glibenclamide, indomethacin, clotrimazole, or cycloheximide. The vasorelaxant effect of amfepramone was significantly attenuated by NG-nitro-L-arginine methyl ester (L-NAME) and tetraethylammonium (TEA), and was blocked by removal of the vascular endothelium. These results suggest that amfepramone had a direct vasorelaxant effect on phenylephrine-precontracted rat aortic rings, and that inhibition of endothelial nitric oxide synthase and the opening of Ca2+-activated K+ channels were involved in this effect.
[Mh] Termos MeSH primário: Acetilcolina/farmacologia
Aorta Torácica/efeitos dos fármacos
Depressores do Apetite/farmacologia
Dietilpropiona/farmacologia
Vasodilatadores/farmacologia
[Mh] Termos MeSH secundário: Animais
Aorta Torácica/metabolismo
Canais de Cálcio/efeitos dos fármacos
Canais de Cálcio/metabolismo
Endotélio Vascular/efeitos dos fármacos
Masculino
NG-Nitroarginina Metil Éster/metabolismo
Óxido Nítrico Sintase Tipo III/efeitos dos fármacos
Fenilefrina/farmacologia
Canais de Potássio/efeitos dos fármacos
Canais de Potássio/metabolismo
Ratos Wistar
Tetraetilamônio/metabolismo
Vasoconstritores/farmacologia
Vasodilatação/efeitos dos fármacos
[Pt] Tipo de publicação:EVALUATION STUDIES; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Appetite Depressants); 0 (Calcium Channels); 0 (Potassium Channels); 0 (Vasoconstrictor Agents); 0 (Vasodilator Agents); 1WS297W6MV (Phenylephrine); 66-40-0 (Tetraethylammonium); EC 1.14.13.39 (Nitric Oxide Synthase Type III); N9YNS0M02X (Acetylcholine); Q94YYU22B8 (Diethylpropion); V55S2QJN2X (NG-Nitroarginine Methyl Ester)
[Em] Mês de entrada:1512
[Cu] Atualização por classe:170220
[Lr] Data última revisão:
170220
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:150402
[St] Status:MEDLINE


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[PMID]:25633934
[Au] Autor:Guha S; Rajeshkumar V; Kotha SS; Sekar G
[Ad] Endereço:Department of Chemistry, Indian Institute of Technology Madras , Chennai, Tamil Nadu 600036, India.
[Ti] Título:A versatile and one-pot strategy to synthesize α-amino ketones from benzylic secondary alcohols using N-bromosuccinimide.
[So] Source:Org Lett;17(3):406-9, 2015 Feb 06.
[Is] ISSN:1523-7052
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:A metal-free one-pot strategy has been developed for the first time to synthesize pharmaceutically important α-amino ketones from readily available benzylic secondary alcohols and amines using N-bromosuccinimide. This new reaction proceeds via three consecutive steps involving oxidation of alcohols, α-bromination of ketones, and nucleophilic substitution of α-bromo ketones to give α-amino ketones. Importantly, this novel one-pot greener reaction avoids direct usage of toxic and corrosive bromine. This methodology has been employed efficiently to synthesize pharmaceutically important amfepramone and pyrovalerone in a single step.
[Mh] Termos MeSH primário: Álcoois/química
Bromosuccinimida/química
Cetonas/síntese química
[Mh] Termos MeSH secundário: Aminas/química
Catálise
Dietilpropiona/síntese química
Dietilpropiona/química
Halogenação
Cetonas/química
Estrutura Molecular
Oxirredução
Pirrolidinas/síntese química
Pirrolidinas/química
Estereoisomerismo
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Alcohols); 0 (Amines); 0 (Ketones); 0 (Pyrrolidines); K8G1F2UCJF (Bromosuccinimide); Q94YYU22B8 (Diethylpropion); VOU69C02JP (pyrovalerone)
[Em] Mês de entrada:1504
[Cu] Atualização por classe:150206
[Lr] Data última revisão:
150206
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:150131
[St] Status:MEDLINE
[do] DOI:10.1021/ol503683q


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[PMID]:25005806
[Au] Autor:da Silva CJ; Montaldi AP; Dos Santos JE; Takahashi CS
[Ad] Endereço:Federal Institute of Education, Science and Technology of Goiás, City of Goiás, Goiás, Brazil Department of Genetics, Faculty of Medicine of Ribeirão Preto, São Paulo University, São Paulo, Brazil cristianoprofeta@hotmail.com.
[Ti] Título:Evaluation of the toxic activity of anorectic diethylpropion in Chinese hamster ovary cells.
[So] Source:Hum Exp Toxicol;34(3):300-7, 2015 Mar.
[Is] ISSN:1477-0903
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Diethylpropion has been available in the market for treating obesity for over 50 years. Refined studies are lacking to fully elucidate its action spectrum. The aim of our study was to evaluate possible toxic effects of anorectic diethylpropion in Chinese hamster ovary (CHO) cells. Comet assay (detects breaks in the DNA strand), micronucleus test (detects clastogenic/aneugenic damage), and cell survival test (detects cytotoxic damage) were used to evaluate the toxic effects. In comet assay, we found that the damage scores with diethylpropion treatments at the concentrations of 20 and 40 µg/mL were more significant ( p < 0.05) than that of the negative control. When assessing the possible aneugenic and/or clastogenic damage caused by the drug in CHO cells, we found no difference ( p > 0.05) in the values of micronucleated cells when comparing different diethylpropion treatments and the negative control. Regarding the cell viability, for all the diethylpropion concentrations tested, higher values ( p < 0.05) of apoptosis were found compared with those of the negative control. In relation to the number of necrotic cells, no difference ( p > 0.05) was noted between the means of the three concentrations of diethylpropion evaluated and the negative control. In the experimental conditions, we conclude that diethylpropion has weak genotoxic and cytotoxic activities.
[Mh] Termos MeSH primário: Depressores do Apetite/toxicidade
Citotoxinas/toxicidade
Dietilpropiona/toxicidade
Mutagênicos/toxicidade
[Mh] Termos MeSH secundário: Animais
Células CHO
Sobrevivência Celular/efeitos dos fármacos
Ensaio Cometa
Cricetinae
Cricetulus
Dano ao DNA
Testes para Micronúcleos
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Appetite Depressants); 0 (Cytotoxins); 0 (Mutagens); Q94YYU22B8 (Diethylpropion)
[Em] Mês de entrada:1511
[Cu] Atualização por classe:150220
[Lr] Data última revisão:
150220
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:140710
[St] Status:MEDLINE
[do] DOI:10.1177/0960327114542884


  9 / 251 MEDLINE  
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[PMID]:25038769
[Au] Autor:Mariotti Kde C; Schuh RS; Ferranti P; Ortiz RS; Souza DZ; Pechansky F; Froehlich PE; Limberger RP
[Ad] Endereço:Programa de Pós-Graduação em Ciências Farmacêuticas, Faculdade de Farmácia, Laboratório de Análises e Pesquisas Toxicológicas, Universidade Federal do Rio Grande do Sul, 2752 Ipiranga Avenue, Santana, Porto Alegre, Rio Grande do Sul 90610-000, Brazil krismariotti@gmail.com.
[Ti] Título:Simultaneous analysis of amphetamine-type stimulants in plasma by solid-phase microextraction and gas chromatography-mass spectrometry.
[So] Source:J Anal Toxicol;38(7):432-7, 2014 Sep.
[Is] ISSN:1945-2403
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Brazil is considered one of the countries with the highest number of amphetamine-type stimulant (ATS) users worldwide, mainly diethylpropion (DIE) and fenproporex (FEN). The use of ATS is mostly linked to diverted prescription stimulants and this misuse is widely associated with (ab)use by drivers. A validated method was developed for the simultaneous analysis of amphetamine (AMP), DIE and FEN in plasma samples employing direct immersion-solid-phase microextraction, and gas chromatographic/mass spectrometric analysis. Trichloroacetic acid 10% was used for plasma deproteinization. In situ derivatization with propylchloroformate was employed. The linear range of the method covered from 5.0 to 100 ng/mL. The detection limits were 1.0 (AMP), 1.5 (DIE) and 2.0 ng/mL (FEN). The accuracy assessment of the control samples was within 85.58-108.33% of the target plasma concentrations. Recoveries ranged from 46.35 to 84.46% and precision was <15% of the value of relative standard deviation. This method is appropriate for screening and confirmation in plasma forensic toxicology analyses of these basic drugs.
[Mh] Termos MeSH primário: Anfetaminas/sangue
Estimulantes do Sistema Nervoso Central/sangue
Dietilpropiona/sangue
Detecção do Abuso de Substâncias/métodos
[Mh] Termos MeSH secundário: Adulto
Anfetamina/sangue
Brasil
Cromatografia Gasosa-Espectrometria de Massas
Seres Humanos
Limite de Detecção
Masculino
Reprodutibilidade dos Testes
Microextração em Fase Sólida
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Amphetamines); 0 (Central Nervous System Stimulants); CK833KGX7E (Amphetamine); Q94YYU22B8 (Diethylpropion); W0194S5FOA (fenproporex)
[Em] Mês de entrada:1504
[Cu] Atualização por classe:140809
[Lr] Data última revisão:
140809
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:140721
[St] Status:MEDLINE
[do] DOI:10.1093/jat/bku063


  10 / 251 MEDLINE  
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[PMID]:24795175
[Au] Autor:Opacka-Juffry J; Pinnell T; Patel N; Bevan M; Meintel M; Davidson C
[Ad] Endereço:Department of Life Sciences, University of Roehampton, London SW15 4JD.
[Ti] Título:Stimulant mechanisms of cathinones - effects of mephedrone and other cathinones on basal and electrically evoked dopamine efflux in rat accumbens brain slices.
[So] Source:Prog Neuropsychopharmacol Biol Psychiatry;54:122-30, 2014 Oct 03.
[Is] ISSN:1878-4216
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Mephedrone, an erstwhile "legal high", and some non-abused cathinones (ethcathinone, diethylpropion and bupropion) were tested for stimulant effects in vitro, through assessing their abilities to increase basal and electrically evoked dopamine efflux in rat accumbens brain slices, and compared with cocaine and amphetamine. We also tested mephedrone against cocaine in a dopamine transporter binding study. Dopamine efflux was electrically evoked and recorded using voltammetry in the rat accumbens core. We constructed concentration response curves for these cathinones for effects on basal dopamine levels; peak efflux after local electrical stimulation and the time-constant of the dopamine decay phase, an index of dopamine reuptake. We also examined competition between mephedrone or cocaine and [(125)I]RTI121 at the dopamine transporter. Mephedrone was less potent than cocaine at displacing [(125)I]RTI121. Mephedrone and amphetamine increased basal levels of dopamine in the absence of electrical stimulation. Cocaine, bupropion, diethylpropion and ethcathinone all increased the peak dopamine efflux after electrical stimulation and slowed dopamine reuptake. Cocaine was more potent than bupropion and ethcathinone, while diethylpropion was least potent. Notably, cocaine had the fastest onset of action. These data suggest that, with respect to dopamine efflux, mephedrone is more similar to amphetamine than cocaine. These findings also show that cocaine was more potent than bupropion and ethcathinone while diethylpropion was least potent. Mephedrone's binding to the dopamine transporter is consistent with stimulant effects but its potency was lower than that of cocaine. These findings confirm and further characterize stimulant properties of mephedrone and other cathinones in adolescent rat brain.
[Mh] Termos MeSH primário: Estimulantes do Sistema Nervoso Central/farmacologia
Dopamina/metabolismo
Metanfetamina/análogos & derivados
Núcleo Accumbens/efeitos dos fármacos
[Mh] Termos MeSH secundário: Anfetamina/farmacologia
Anfetaminas/farmacologia
Animais
Bupropiona/farmacologia
Cocaína/análogos & derivados
Cocaína/farmacologia
Dietilpropiona/farmacologia
Proteínas da Membrana Plasmática de Transporte de Dopamina/metabolismo
Relação Dose-Resposta a Droga
Estimulação Elétrica
Radioisótopos do Iodo
Masculino
Metanfetamina/farmacologia
Microeletrodos
Núcleo Accumbens/fisiologia
Propiofenonas/farmacologia
Ensaio Radioligante
Ratos Wistar
Técnicas de Cultura de Tecidos
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (2-ethylamino-1-phenyl-propan-1-one); 0 (Amphetamines); 0 (Central Nervous System Stimulants); 0 (Dopamine Plasma Membrane Transport Proteins); 0 (Iodine Radioisotopes); 0 (Propiophenones); 01ZG3TPX31 (Bupropion); 146145-21-3 (RTI 121); 44RAL3456C (Methamphetamine); 8BA8T27317 (mephedrone); CK833KGX7E (Amphetamine); I5Y540LHVR (Cocaine); Q94YYU22B8 (Diethylpropion); VTD58H1Z2X (Dopamine)
[Em] Mês de entrada:1505
[Cu] Atualização por classe:140816
[Lr] Data última revisão:
140816
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:140506
[St] Status:MEDLINE



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