Base de dados : MEDLINE
Pesquisa : D02.092 [Categoria DeCS]
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[PMID]:29486013
[Au] Autor:Wallach JD; Ross JS
[Ad] Endereço:Collaboration for Research Integrity and Transparency, Yale Law School, New Haven, Connecticut.
[Ti] Título:Gabapentin Approvals, Off-Label Use, and Lessons for Postmarketing Evaluation Efforts.
[So] Source:JAMA;319(8):776-778, 2018 02 27.
[Is] ISSN:1538-3598
[Cp] País de publicação:United States
[La] Idioma:eng
[Mh] Termos MeSH primário: Ácidos Cicloexanocarboxílicos
Uso Off-Label
[Mh] Termos MeSH secundário: Aminas
Seres Humanos
Vigilância de Produtos Comercializados
Ácido gama-Aminobutírico
[Pt] Tipo de publicação:EDITORIAL; COMMENT
[Nm] Nome de substância:
0 (Amines); 0 (Cyclohexanecarboxylic Acids); 56-12-2 (gamma-Aminobutyric Acid); 6CW7F3G59X (gabapentin)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180305
[Lr] Data última revisão:
180305
[Sb] Subgrupo de revista:AIM; IM
[Da] Data de entrada para processamento:180228
[St] Status:MEDLINE
[do] DOI:10.1001/jama.2017.21897


  2 / 22854 MEDLINE  
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[PMID]:29407591
[Au] Autor:Zajdel P; Kos T; Marciniec K; Satala G; Canale V; Kaminski K; Holuj M; Lenda T; Koralewski R; Bednarski M; Nowinski L; Wójcikowski J; Daniel WA; Nikiforuk A; Nalepa I; Chmielarz P; Kusmierczyk J; Bojarski AJ; Popik P
[Ad] Endereço:Department of Medicinal Chemistry, Jagiellonian University Medical College, 9 Medyczna Street, 30-688 Kraków, Poland. Electronic address: pawel.zajdel@uj.edu.pl.
[Ti] Título:Novel multi-target azinesulfonamides of cyclic amine derivatives as potential antipsychotics with pro-social and pro-cognitive effects.
[So] Source:Eur J Med Chem;145:790-804, 2018 Feb 10.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:Currently used antipsychotics are characterized by multireceptor mode of action. While antagonism of dopamine D receptors is responsible for the alleviation of "positive" symptoms of schizophrenia and the effects at other, particularly serotonergic receptors are necessary for their additional therapeutic effects, there is no consensus regarding an "ideal" target engagement. Here, a detailed SAR analysis in a series of 45 novel azinesulfonamides of cyclic amine derivatives, involving the aryl-piperazine/piperidine pharmacophore, central alicyclic amine and azinesulfonamide groups has led to the selection of (S)-4-((2-(2-(4-(benzo[b]thiophen-4-yl)piperazin-1-yl)ethyl)pyrrolidin-1-yl)sulfonyl)isoquinoline (62). The polypharmacology profile of 62, characterized by partial 5-HT R agonism, 5-HT /5-HT /D /D R antagonism, and blockade of SERT, reduced the "positive"-like, and "negative"-like symptoms of psychoses. Compound 62 produced no catalepsy, demonstrated a low hyperprolactinemia liability and displayed pro-cognitive effects in the novel object recognition task and attentional set-shifting test. While association of in vitro features with the promising in vivo profile of 62 is still not fully established, its clinical efficacy should be verified in further stages of development.
[Mh] Termos MeSH primário: Aminas/farmacologia
Antipsicóticos/farmacologia
Cognição/efeitos dos fármacos
Receptores de Dopamina D2/metabolismo
Sulfonamidas/farmacologia
[Mh] Termos MeSH secundário: Aminas/síntese química
Aminas/química
Animais
Antipsicóticos/síntese química
Antipsicóticos/química
Relação Dose-Resposta a Droga
Cobaias
Células HEK293
Seres Humanos
Masculino
Estrutura Molecular
Ratos
Ratos Wistar
Relação Estrutura-Atividade
Sulfonamidas/síntese química
Sulfonamidas/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Amines); 0 (Antipsychotic Agents); 0 (Receptors, Dopamine D2); 0 (Sulfonamides)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180302
[Lr] Data última revisão:
180302
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180207
[St] Status:MEDLINE


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[PMID]:29339253
[Au] Autor:Xiao X; Zhang XX; Zhan MM; Cheng K; Li S; Xie Z; Liao C
[Ad] Endereço:School of Biological and Medical Engineering, Hefei University of Technology, Hefei, Anhui 230009, PR China.
[Ti] Título:Design, synthesis and bioevalucation of novel 2,3-dihydro-1H-inden-1-amine derivatives as potent and selective human monoamine oxidase B inhibitors based on rasagiline.
[So] Source:Eur J Med Chem;145:588-593, 2018 Feb 10.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:Parkinson's disease (PD) is associated with elevated levels of hMAO-B in the brain, and MAO-B has been recognized a successful target for developing anti-PD drugs. Herein we report rasagiline derivatives as novel potent and selective hMAO-B inhibitors. They were designed by employing fragment-based drug design strategy to link rasagiline and hydrophobic fragments, which may target a hydrophobic pocket in the entrance cavity of hMAO-B. Different linkers such as -OCH -, -SCH -, -OCH CH -, -OCH CH O-, -OCH CH CH O- were tried. A promising selective hMAO-B inhibitor D14 with similar inhibitory activity as rasagiline and improved isoform selectivity was yielded. The selectivity profile of compounds reported herein suggests that we can further develop more potent hMAO-B inhibitors with high isoform selectivity through this strategy.
[Mh] Termos MeSH primário: Aminas/farmacologia
Desenho de Drogas
Indanos/farmacologia
Indenos/farmacologia
Inibidores da Monoaminoxidase/farmacologia
Monoaminoxidase/metabolismo
[Mh] Termos MeSH secundário: Aminas/síntese química
Aminas/química
Cristalografia por Raios X
Relação Dose-Resposta a Droga
Seres Humanos
Indanos/química
Indenos/síntese química
Indenos/química
Modelos Moleculares
Estrutura Molecular
Inibidores da Monoaminoxidase/síntese química
Inibidores da Monoaminoxidase/química
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Amines); 0 (Indans); 0 (Indenes); 0 (Monoamine Oxidase Inhibitors); 003N66TS6T (rasagiline); EC 1.4.3.4 (Monoamine Oxidase)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180302
[Lr] Data última revisão:
180302
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180118
[St] Status:MEDLINE


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[PMID]:29248767
[Au] Autor:G AG; Kamalanathan AS; Vijayalakshmi MA; Venkataraman K
[Ad] Endereço:Centre for Bioseparation Technology, VIT University, Vellore- 632014, Tamil Nadu, India.
[Ti] Título:Efficient purification of Apolipoprotein A1 (ApoA1) from plasma by HEA HyperCel™: An alternative approach.
[So] Source:J Chromatogr B Analyt Technol Biomed Life Sci;1073:104-109, 2018 Jan 15.
[Is] ISSN:1873-376X
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:HDL-ApoA1 plays a pivotal role in the prevention of atherosclerosis and cardiovascular diseases. ApoA1 purification from blood plasma has always remained tedious, involving multiple steps, large volumes of plasma and substantial loss in the final yield of pure ApoA1. In this study, a two-step method has been developed and optimized for the purification of ApoA1 from plasma. Plasma was first subjected to 60% ammonium sulphate (NH ) SO precipitation and subsequently, ApoA1 was recovered using mixed mode chromatographic sorbent, HEA HyperCel™. ApoA1 was found to be enriched in 60% (NH ) SO supernatant that was dialyzed and injected onto HEA sorbent with 50 mM phosphate buffer pH 7.4. The bound proteins were eluted by decreasing the pH in step-gradient from pH 7.4 to pH 4.0 and subsequently to pH 3.5 using 50 mM sodium acetate buffer. Gel electrophoresis showed elution of homogeneous apoA1 at pH 3.5, with purity and yield of 63%. An interesting feature of this approach is that the purified ApoA1 was monomeric with a mass of 28,079.30 Da as confirmed by MS analysis. This simple and efficient method of purification of apoA1 serves as an alternative method which can be combined with traditional approaches and has a great potential for biochemical and clinical studies.
[Mh] Termos MeSH primário: Aminas/química
Apolipoproteína A-I/sangue
Apolipoproteína A-I/isolamento & purificação
Cromatografia Líquida/métodos
[Mh] Termos MeSH secundário: Sulfato de Amônio
Apolipoproteína A-I/química
Eletroforese em Gel de Poliacrilamida
Seres Humanos
Espectrometria de Massas por Ionização e Dessorção a Laser Assistida por Matriz
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (APOA1 protein, human); 0 (Amines); 0 (Apolipoprotein A-I); CI4E002ZV8 (hexylamine); SU46BAM238 (Ammonium Sulfate)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180302
[Lr] Data última revisão:
180302
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171218
[St] Status:MEDLINE


  5 / 22854 MEDLINE  
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[PMID]:29311461
[Au] Autor:Nambu H
[Ad] Endereço:Graduate School of Medicine and Pharmaceutical Sciences, University of Toyama.
[Ti] Título:[Novel Methods for the Synthesis of Heterocycles Using Highly Reactive Spirocyclopropanes].
[So] Source:Yakugaku Zasshi;138(1):19-25, 2018.
[Is] ISSN:1347-5231
[Cp] País de publicação:Japan
[La] Idioma:jpn
[Ab] Resumo:This review describes our recent efforts to develop efficient methods for the synthesis of heterocyclic compounds, such as indoles and benzofurans, employing ring-opening cyclization of cyclohexane-1,3-dione-2-spirocyclopropanes, which were prepared by the reaction of 1,3-cyclohexanediones with sulfonium salts. Ring-opening cyclization of cyclohexane-1,3-dione-2-spirocyclopropanes with primary amines proceeded at room temperature to provide 2-substituted tetrahydroindol-4(5H)-ones in good to excellent yield. The obtained product was readily converted into a 2-substituted 4-hydroxyindole derivative. Furthermore, acid-catalyzed ring-opening cyclization of cyclohexane-1,3-dione-2-spirocyclopropanes proceeded smoothly at room temperature to provide 2-substituted tetrahydrobenzofuran-4(2H)-ones in excellent yield. The obtained product was converted into a 2-substituted 4-hydroxybenzofuran derivative. The synthetic utility of this catalytic protocol was demonstrated by the total synthesis of cuspidan B.
[Mh] Termos MeSH primário: Química Orgânica/métodos
Compostos Heterocíclicos/síntese química
[Mh] Termos MeSH secundário: Aminas/química
Benzofuranos/síntese química
Catálise
Ciclização
Cicloexanos/síntese química
Cicloexanonas/química
Ciclopropanos/síntese química
Indóis/síntese química
Fenômenos de Química Orgânica
Alimentos de Soja
Estilbenos/síntese química
Compostos de Sulfônio/química
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Amines); 0 (Benzofurans); 0 (Cyclohexanes); 0 (Cyclohexanones); 0 (Cyclopropanes); 0 (Heterocyclic Compounds); 0 (Indoles); 0 (Stilbenes); 0 (Sulfonium Compounds); 0 (cuspidan B); 6UK3D2BXJT (1,3-cyclohexanedione)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180226
[Lr] Data última revisão:
180226
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180110
[St] Status:MEDLINE
[do] DOI:10.1248/yakushi.17-00188


  6 / 22854 MEDLINE  
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[PMID]:29279555
[Au] Autor:Masuda R; Ajimi J; Murata T
[Ad] Endereço:Department of Anesthesiology, Tokai University Hachioji Hospital.
[Ti] Título:Pharmacotherapy for Neuropathic Pain in Japan.
[So] Source:J Nippon Med Sch;84(6):258-267, 2017.
[Is] ISSN:1347-3409
[Cp] País de publicação:Japan
[La] Idioma:eng
[Ab] Resumo:Neuropathic pain (NeP) results from injury to, or disease of, the peripheral or central components of the neural systems involved in pain. In contrast to inflammatory pain, NeP can persist after healing from the initial injury has resolved. Antipyretic agents, such as non-steroidal anti-inflammatory drugs, steroids, and acetaminophen are ineffective, while specific agents such as gabapentinoids, antidepressants, antiepileptics, and opioids are effective in treating NeP. In this review, we address the definition of NeP, pharmacotherapy for NeP in Japan, pain classification, setting goals for successful NeP medication, and the Japanese algorithm for the pharmacotherapy of NeP with specific prescription guidance.
[Mh] Termos MeSH primário: Aminas/administração & dosagem
Analgésicos Opioides/administração & dosagem
Anticonvulsivantes/administração & dosagem
Antidepressivos/administração & dosagem
Ácidos Cicloexanocarboxílicos/administração & dosagem
Cloridrato de Duloxetina/administração & dosagem
Neuralgia/tratamento farmacológico
Pregabalina/administração & dosagem
Ácido gama-Aminobutírico/administração & dosagem
[Mh] Termos MeSH secundário: Idoso
Algoritmos
Aminas/efeitos adversos
Analgésicos Opioides/efeitos adversos
Anticonvulsivantes/efeitos adversos
Antidepressivos/efeitos adversos
Ácidos Cicloexanocarboxílicos/efeitos adversos
Esquema de Medicação
Cloridrato de Duloxetina/efeitos adversos
Feminino
Seres Humanos
Japão
Neuralgia/classificação
Manejo da Dor
Pregabalina/efeitos adversos
Ácido gama-Aminobutírico/efeitos adversos
[Pt] Tipo de publicação:CASE REPORTS; JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Amines); 0 (Analgesics, Opioid); 0 (Anticonvulsants); 0 (Antidepressive Agents); 0 (Cyclohexanecarboxylic Acids); 55JG375S6M (Pregabalin); 56-12-2 (gamma-Aminobutyric Acid); 6CW7F3G59X (gabapentin); 9044SC542W (Duloxetine Hydrochloride)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180222
[Lr] Data última revisão:
180222
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171228
[St] Status:MEDLINE
[do] DOI:10.1272/jnms.84.258


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[PMID]:29241365
[Au] Autor:Mason BJ; Quello S; Shadan F
[Ad] Endereço:a Pearson Center for Alcoholism and Addiction Research , The Scripps Research Institute , La Jolla , CA , USA.
[Ti] Título:Gabapentin for the treatment of alcohol use disorder.
[So] Source:Expert Opin Investig Drugs;27(1):113-124, 2018 Jan.
[Is] ISSN:1744-7658
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:INTRODUCTION: Alcohol misuse is the fifth leading risk factor for premature death and disability worldwide. Fewer than 10% of afflicted Americans receive pharmacological treatment for alcohol use disorder. Gabapentin is a calcium channel GABAergic modulator that is widely used for pain. Studies showing reduced drinking and decreased craving and alcohol-related disturbances in sleep and affect in the months following alcohol cessation suggest therapeutic potential for alcohol use disorder. Areas covered: Human laboratory and clinical studies assessing gabapentin for alcohol use disorder are reviewed. Data were obtained by searching for English peer-reviewed articles on PubMed, reference lists of identified articles, and trials registered on clinicaltrials.gov. Additionally, the mechanism of action of gabapentin specific to alcohol use disorder, and studies of gabapentin for alcohol withdrawal and non-alcohol substance use disorders are summarized. Expert opinion: Alcohol use disorder represents a challenge and large, unmet medical need. Evidence from single-site studies lend support to the safety and efficacy of gabapentin as a novel treatment for alcohol use disorder, with unique benefits for alcohol-related insomnia and negative affect, relative to available treatments. Proprietary gabapentin delivery systems may open a path to pivotal trials and registration of gabapentin as a novel treatment for alcohol use disorder.
[Mh] Termos MeSH primário: Consumo de Bebidas Alcoólicas/prevenção & controle
Alcoolismo/tratamento farmacológico
Aminas/uso terapêutico
Ácidos Cicloexanocarboxílicos/uso terapêutico
Ácido gama-Aminobutírico/uso terapêutico
[Mh] Termos MeSH secundário: Alcoolismo/fisiopatologia
Aminas/efeitos adversos
Aminas/farmacologia
Animais
Bloqueadores dos Canais de Cálcio/efeitos adversos
Bloqueadores dos Canais de Cálcio/farmacologia
Bloqueadores dos Canais de Cálcio/uso terapêutico
Ácidos Cicloexanocarboxílicos/efeitos adversos
Ácidos Cicloexanocarboxílicos/farmacologia
Seres Humanos
Distúrbios do Início e da Manutenção do Sono/tratamento farmacológico
Distúrbios do Início e da Manutenção do Sono/etiologia
Síndrome de Abstinência a Substâncias/tratamento farmacológico
Ácido gama-Aminobutírico/efeitos adversos
Ácido gama-Aminobutírico/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Amines); 0 (Calcium Channel Blockers); 0 (Cyclohexanecarboxylic Acids); 56-12-2 (gamma-Aminobutyric Acid); 6CW7F3G59X (gabapentin)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180222
[Lr] Data última revisão:
180222
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171216
[St] Status:MEDLINE
[do] DOI:10.1080/13543784.2018.1417383


  8 / 22854 MEDLINE  
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[PMID]:29447012
[Au] Autor:Gao X; Tang J; Liu H; Liu L; Kang L; Chen W
[Ad] Endereço:a Key Laboratory Breeding Base of Hu'nan Oriented Fundamental and Applied Research of Innovative Pharmaceutics, College of Pharmacy , Changsha Medical University , Changsha , China.
[Ti] Título:Structure-activity relationship investigation of tertiary amine derivatives of cinnamic acid as acetylcholinesterase and butyrylcholinesterase inhibitors: compared with that of phenylpropionic acid, sorbic acid and hexanoic acid.
[So] Source:J Enzyme Inhib Med Chem;33(1):519-524, 2018 Dec.
[Is] ISSN:1475-6374
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:In the present investigation, 48 new tertiary amine derivatives of cinnamic acid, phenylpropionic acid, sorbic acid and hexanoic acid (4d-6g, 10d-12g, 16d-18g and 22d-24g) were designed, synthesized and evaluated for the effect on AChE and BChE in vitro. The results revealed that the alteration of aminoalkyl types and substituted positions markedly influences the effects in inhibiting AChE. Almost of all cinnamic acid derivatives had the most potent inhibitory activity than that of other acid derivatives with the same aminoalkyl side chain. Unsaturated bond and benzene ring in cinnamic acid scaffold seems important for the inhibitory activity against AChE. Among them, compound 6g revealed the most potent AChE inhibitory activity (IC value: 3.64 µmol/L) and highest selectivity over BChE (ratio: 28.6). Enzyme kinetic study showed that it present a mixed-type inhibition against AChE. The molecular docking study suggested that it can bind with the catalytic site and peripheral site of AChE.
[Mh] Termos MeSH primário: Aminas/farmacologia
Caproatos/farmacologia
Inibidores da Colinesterase/farmacologia
Cinamatos/farmacologia
Fenilpropionatos/farmacologia
Ácido Sórbico/farmacologia
[Mh] Termos MeSH secundário: Acetilcolinesterase/metabolismo
Aminas/síntese química
Aminas/química
Animais
Butirilcolinesterase/metabolismo
Caproatos/química
Inibidores da Colinesterase/síntese química
Inibidores da Colinesterase/química
Cinamatos/química
Relação Dose-Resposta a Droga
Simulação de Acoplamento Molecular
Estrutura Molecular
Fenilpropionatos/química
Ratos
Ratos Sprague-Dawley
Ácido Sórbico/química
Relação Estrutura-Atividade
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Amines); 0 (Caproates); 0 (Cholinesterase Inhibitors); 0 (Cinnamates); 0 (Phenylpropionates); 1F8SN134MX (hexanoic acid); 5Q445IN5CU (3-phenylpropionic acid); EC 3.1.1.7 (Acetylcholinesterase); EC 3.1.1.8 (Butyrylcholinesterase); U14A832J8D (cinnamic acid); X045WJ989B (Sorbic Acid)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180219
[Lr] Data última revisão:
180219
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180216
[St] Status:MEDLINE
[do] DOI:10.1080/14756366.2018.1436053


  9 / 22854 MEDLINE  
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[PMID]:29198904
[Au] Autor:Fatima N; Reddy BVS; Gowravaram S; Yadav JS; Kadari S; Putta CS
[Ad] Endereço:Center for Semiochemicals Natural Products Chemistry Division, CSIR-Indian Institute of Chemical Technology, Hyderabad 500007, India. Electronic address: dr.narjisiict@yahoo.com.
[Ti] Título:Synthesis and biological evaluation of 1-amino isochromans from 2-bromoethyl benzaldehyde and amines in acid medium.
[So] Source:Bioorg Med Chem Lett;28(2):196-201, 2018 01 15.
[Is] ISSN:1464-3405
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:We have developed a facile and efficient synthetic route to substituted isochromans for the first time by reacting 2-(2-bromoethyl)benzaldehyde with a variety of aryl, heteroaryl amines in AcOH. The reaction is catalyst/additive free and takes place at reflux conditions with short reaction time to furnish products in good to excellent yields. All the compounds have been characterized by spectral techniques such as IR, H NMR and Mass etc. Synthesized compounds were evaluated for antimicrobial activity against specific bacterial like 1) Staphylococcus strains aureus 2) Bacillus subtilis 3) Escherichia coli 4) Pseudomonas aeruginosa. Compounds 3e, 3n, 3 m, 3 l, 3 k, 3j and 3b showed most potent in vitro activity against bacterial strains.
[Mh] Termos MeSH primário: Ácido Acético/química
Aminas/química
Antibacterianos/farmacologia
Benzaldeídos/química
Cromanos/farmacologia
[Mh] Termos MeSH secundário: Antibacterianos/síntese química
Antibacterianos/química
Bacillus subtilis/efeitos dos fármacos
Benzaldeídos/síntese química
Cromanos/síntese química
Cromanos/química
Relação Dose-Resposta a Droga
Escherichia coli/efeitos dos fármacos
Testes de Sensibilidade Microbiana
Estrutura Molecular
Pseudomonas aeruginosa/efeitos dos fármacos
Staphylococcus aureus/efeitos dos fármacos
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Amines); 0 (Anti-Bacterial Agents); 0 (Benzaldehydes); 0 (Chromans); Q40Q9N063P (Acetic Acid)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180216
[Lr] Data última revisão:
180216
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171205
[St] Status:MEDLINE


  10 / 22854 MEDLINE  
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[PMID]:28451875
[Au] Autor:Peckham AM; Fairman KA; Sclar DA
[Ad] Endereço:Department of Pharmacy Practice, College of Pharmacy-Glendale, Midwestern University, 19555 N. 59th Avenue, Glendale, AZ, 85308, USA. apeckh@midwestern.edu.
[Ti] Título:Prevalence of Gabapentin Abuse: Comparison with Agents with Known Abuse Potential in a Commercially Insured US Population.
[So] Source:Clin Drug Investig;37(8):763-773, 2017 Aug.
[Is] ISSN:1179-1918
[Cp] País de publicação:New Zealand
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Despite international calls to make gabapentin a controlled substance, studies of gabapentin use/abuse patterns are limited to small/high-risk samples and adverse event reports. OBJECTIVE: The aim of this study was to conduct a systematic assessment of the abuse potential/prevalence of gabapentin in a large sample. DATA SOURCE: Truven Health MarketScan Commercial Claims and Encounters database, years 2013-2015. ELIGIBILITY CRITERIA: Patients with two or more claims for one or more abusable drugs and ≥12 months' continuous enrollment were sampled for Lorenz curve analysis. Prevalence analysis was limited to those with ≥120 days of therapy. METHODS: Abuse potential was measured as Lorenz-1 (consumption of drug supply by top 1% of users) of ≥15%. Dose thresholds were morphine milligram equivalent (MME) standards for opioids, and maximum labeled doses in milligrams (mg) for other drugs. RESULTS: Lorenz-1 values were 37% opioids, 19% gabapentin, 15% pregabalin, 14% alprazolam, and 13% zolpidem. The top 1% gabapentin users filled prescriptions for a mean (median) 11,274 (9534) mg/day, more than three times the recommended maximum (3600 mg). Of these, one-quarter used or diverted ≥12,822 mg/day. The top 1% opioid and pregabalin users filled prescriptions for a mean (median) 180 (127) MMEs and 2474 (2219) mg/day, respectively. Of patients using opioids + gabapentin simultaneously, 24% had three or more claims exceeding the dose threshold within 12 months. LIMITATIONS: Established threshold criteria for gabapentinoid abuse are uncertain. Indications for gabapentinoid use (e.g. hot flashes, restless legs syndrome) were not measured. CONCLUSION: Gabapentin use patterns are similar to those of other abusable medications. High daily doses pose safety and/or diversion concerns, and investigation of the medical consequences of gabapentin abuse is needed.
[Mh] Termos MeSH primário: Aminas
Ácidos Cicloexanocarboxílicos
Transtornos Relacionados ao Uso de Substâncias/epidemiologia
Ácido gama-Aminobutírico
[Mh] Termos MeSH secundário: Adolescente
Adulto
Feminino
Seres Humanos
Masculino
Meia-Idade
Prevalência
Adulto Jovem
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Amines); 0 (Cyclohexanecarboxylic Acids); 56-12-2 (gamma-Aminobutyric Acid); 6CW7F3G59X (gabapentin)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180216
[Lr] Data última revisão:
180216
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170429
[St] Status:MEDLINE
[do] DOI:10.1007/s40261-017-0530-3



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