Base de dados : MEDLINE
Pesquisa : D03.605.687 [Categoria DeCS]
Referências encontradas : 2203 [refinar]
Mostrando: 1 .. 10   no formato [Detalhado]

página 1 de 221 ir para página                         

  1 / 2203 MEDLINE  
              next record last record
seleciona
para imprimir
Fotocópia
Texto completo
[PMID]:29261656
[Au] Autor:Weed MR; Polino J; Signor L; Bookbinder M; Keavy D; Benitex Y; Morgan DG; King D; Macor JE; Zaczek R; Olson R; Bristow LJ
[Ad] Endereço:Genetically Defined Diseases and Genomics, Bristol-Myers Squibb Company, Wallingford, CT, United States of America.
[Ti] Título:Nicotinic alpha 7 receptor agonists EVP-6124 and BMS-933043, attenuate scopolamine-induced deficits in visuo-spatial paired associates learning.
[So] Source:PLoS One;12(12):e0187609, 2017.
[Is] ISSN:1932-6203
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Agonists at the nicotinic acetylcholine alpha 7 receptor (nAChR α7) subtype have the potential to treat cognitive deficits in patients with Alzheimer's disease (AD) or schizophrenia. Visuo-spatial paired associates learning (vsPAL) is a task that has been shown to reliably predict conversion from mild cognitive impairment to AD in humans and can also be performed by nonhuman primates. Reversal of scopolamine-induced impairment of vsPAL performance may represent a translational approach for the development of nAChR α7 agonists. The present study investigated the effect of treatment with the acetylcholinesterase inhibitor, donepezil, or three nAChR α7 agonists, BMS-933043, EVP-6124 and RG3487, on vsPAL performance in scopolamine-treated cynomolgus monkeys. Scopolamine administration impaired vsPAL performance accuracy in a dose- and difficulty- dependent manner. The impairment of eventual accuracy, a measure of visuo-spatial learning during the task, was significantly ameliorated by treatment with donepezil (0.3 mg/kg, i.m.), EVP-6124 (0.01 mg/kg, i.m.) or BMS-933043 (0.03, 0.1 and 0.3 mg/kg, i.m.). Both nAChR α7 agonists showed inverted-U shaped dose-effect relationships with EVP-6124 effective at a single dose only whereas BMS-933043 was effective across at least a 10 fold dose/exposure range. RG3487 was not efficacious in this paradigm at the dose range examined (0.03-1 mg/kg, i.m.). These results are the first demonstration that the nAChR α7 agonists, EVP-6124 and BMS-933043, can ameliorate scopolamine-induced cognitive deficits in nonhuman primates performing the vsPAL task.
[Mh] Termos MeSH primário: Aprendizagem por Associação de Pares/efeitos dos fármacos
Quinuclidinas/farmacologia
Percepção Espacial/classificação
Compostos de Espiro/farmacologia
Tiofenos/farmacologia
Percepção Visual/efeitos dos fármacos
Receptor Nicotínico de Acetilcolina alfa7/agonistas
[Mh] Termos MeSH secundário: Animais
Indanos/farmacologia
Macaca fascicularis
Masculino
Piperidinas/farmacologia
Quinuclidinas/química
Tempo de Reação/efeitos dos fármacos
Hidrobrometo de Escopolamina
Compostos de Espiro/química
Análise e Desempenho de Tarefas
Tiofenos/química
Resultado do Tratamento
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (7-chloro-N-quinuclidin-3-yl-benzo(b)thiophene-2-carboxamide); 0 (BMS-933043); 0 (Indans); 0 (Piperidines); 0 (Quinuclidines); 0 (Spiro Compounds); 0 (Thiophenes); 0 (alpha7 Nicotinic Acetylcholine Receptor); 451IFR0GXB (Scopolamine Hydrobromide); 8SSC91326P (donepezil)
[Em] Mês de entrada:1801
[Cu] Atualização por classe:180108
[Lr] Data última revisão:
180108
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171221
[St] Status:MEDLINE
[do] DOI:10.1371/journal.pone.0187609


  2 / 2203 MEDLINE  
              first record previous record next record last record
seleciona
para imprimir
Fotocópia
[PMID]:29187483
[Au] Autor:Sento S; Kitamura N; Yamamoto T; Nakashiro K; Hamakawa H; Ibaragi S; Sasaki A; Takamaru N; Miyamoto Y; Kodani I; Ryoke K; Mishima K; Ueyama Y; ORAL CANCER STUDY GROUP OF CHUGOKU-SHIKOKU
[Ad] Endereço:Department of Oral and Maxillofacial Surgery, Kochi Medical School, Kochi University, Nankoku, Japan shinya-sento@kochi-u.ac.jp.
[Ti] Título:Palonosetron Prevents Highly Emetogenic Chemotherapy-induced Nausea and Vomiting in Oral Cancer Patients.
[So] Source:Anticancer Res;37(12):6977-6981, 2017 12.
[Is] ISSN:1791-7530
[Cp] País de publicação:Greece
[La] Idioma:eng
[Ab] Resumo:BACKGROUND/AIM: To evaluate the efficacy of palonosetron in preventing acute and delayed nausea and vomiting in patients receiving highly emetogenic chemotherapy (HEC) in oral cancer patients. PATIENTS AND METHODS: Oral cancer patients receiving HEC were enrolled; among the 40 patients, 87 courses of chemotherapy were administered. On day 1, 0.75 mg palonosetron was intravenously administrated just before chemotherapy. RESULTS: The primary endpoint was the proportion of patients with a complete response (CR) and the secondary endpoint was the proportion of patients with complete control (CC) during the acute and delayed phase. During the acute phase, 86 of 87 courses (98.9%) had CR and 84 of 87 courses (96.6%) had CC. During the delayed phase, 84 of 87 courses (96.6%) had CR and 70 of 87 courses (80.5%) had CC. CONCLUSION: Palonosetron is effective at preventing HEC-induced chemotherapy-induced nausea and vomiting (CINV) in oral cancer chemotherapeutic regimens in the acute and delayed phases.
[Mh] Termos MeSH primário: Antineoplásicos/uso terapêutico
Isoquinolinas/uso terapêutico
Neoplasias Bucais/tratamento farmacológico
Náusea/prevenção & controle
Quinuclidinas/uso terapêutico
Vômito/prevenção & controle
[Mh] Termos MeSH secundário: Administração Intravenosa
Adulto
Idoso
Idoso de 80 Anos ou mais
Antineoplásicos/efeitos adversos
Cisplatino/administração & dosagem
Cisplatino/efeitos adversos
Quimioterapia Combinada
Feminino
Seres Humanos
Isoquinolinas/administração & dosagem
Masculino
Meia-Idade
Náusea/induzido quimicamente
Quinuclidinas/administração & dosagem
Antagonistas da Serotonina/administração & dosagem
Antagonistas da Serotonina/uso terapêutico
Resultado do Tratamento
Vômito/induzido quimicamente
[Pt] Tipo de publicação:CLINICAL TRIAL; JOURNAL ARTICLE; MULTICENTER STUDY
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Isoquinolines); 0 (Quinuclidines); 0 (Serotonin Antagonists); 5D06587D6R (palonosetron); Q20Q21Q62J (Cisplatin)
[Em] Mês de entrada:1712
[Cu] Atualização por classe:171211
[Lr] Data última revisão:
171211
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171201
[St] Status:MEDLINE


  3 / 2203 MEDLINE  
              first record previous record next record last record
seleciona
para imprimir
Fotocópia
Texto completo
[PMID]:28854065
[Au] Autor:Zhang L; Qu X; Teng Y; Shi J; Yu P; Sun T; Wang J; Zhu Z; Zhang X; Zhao M; Liu J; Jin B; Luo Y; Teng Z; Dong Y; Wen F; An Y; Yuan C; Chen T; Zhou L; Chen Y; Zhang J; Wang Z; Qu J; Jin F; Zhang J; Jin X; Xie X; Wang J; Man L; Fu L; Liu Y
[Ad] Endereço:Lingyun Zhang, Xiujuan Qu, Yuee Teng, Jing Shi, Ping Yu, Mingfang Zhao, Jing Liu, Bo Jin, Ying Luo, Zan Teng, Ying Chen, Jinglei Qu, Feng Jin, Lingyu Fu, and Yunpeng Liu, First Hospital of China Medical University, Shenyang; Tao Sun and Jingdong Zhang, Cancer Hospital of China Medical University; Xi
[Ti] Título:Efficacy of Thalidomide in Preventing Delayed Nausea and Vomiting Induced by Highly Emetogenic Chemotherapy: A Randomized, Multicenter, Double-Blind, Placebo-Controlled Phase III Trial (CLOG1302 study).
[So] Source:J Clin Oncol;35(31):3558-3565, 2017 Nov 01.
[Is] ISSN:1527-7755
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Purpose We examined the efficacy and safety of thalidomide (THD) for the prevention of delayed nausea and vomiting in patients who received highly emetogenic chemotherapy (HEC). Patients and Methods In a randomized, double-blind, active-controlled, phase III trial, chemotherapy-naive patients with cancer who were scheduled to receive HEC that contained cisplatin or cyclophosphamide-doxorubicin/epirubincin ≥ 50 mg/m regimens were randomly assigned to a THD group (100 mg twice daily on days 1 to 5) or placebo group, both with palonosetron (0.25 mg on day 1) and dexamethasone (12 mg on day 1; 8 mg on days 2 to 4). Primary end point was complete response to vomiting-no emesis or use of rescue medication-in the delayed phase (25 to 120 h). Nausea and anorexia on days 1 to 5 were evaluated by the 4-point Likert scale (0, no symptoms; 3, severe). Quality of life was assessed by the European Organization for Research and Treatment of Cancer QLQ-C30 version 3 questionnaire on days -1 and 6. Results Of 656 patients, 638 were evaluable: 317 in the THD group and 321 in the control group. Compared with placebo, delayed and overall (0 to 120 h) complete response rates to vomiting were significantly higher with THD: 76.9% versus 61.7% ( P < .001) and 66.1% versus 53.3% ( P = .001), respectively. Rates of no nausea were also higher in the THD group (delayed: 47.3% v 33.3%; P < .001; overall: 41% v 29.6%; P = .003), and mean scores of anorexia were lower overall (0.44 ± 0.717 v 0.64 ± 0.844; P = .003). Adverse effects were mild to moderate. The THD group had increased sedation, dizziness, constipation, and dry mouth, but experienced better quality of life after chemotherapy. Conclusion Thalidomide combined with palonosetron and dexamethasone significantly improved HEC-induced delayed nausea and vomiting prevention in chemotherapy-naive patients.
[Mh] Termos MeSH primário: Protocolos de Quimioterapia Combinada Antineoplásica/efeitos adversos
Náusea/prevenção & controle
Talidomida/uso terapêutico
Vômito/prevenção & controle
[Mh] Termos MeSH secundário: Adulto
Idoso
Protocolos de Quimioterapia Combinada Antineoplásica/administração & dosagem
Cisplatino/administração & dosagem
Cisplatino/efeitos adversos
Ciclofosfamida/administração & dosagem
Ciclofosfamida/efeitos adversos
Dexametasona
Método Duplo-Cego
Doxorrubicina/administração & dosagem
Doxorrubicina/efeitos adversos
Epirubicina/administração & dosagem
Epirubicina/efeitos adversos
Feminino
Seres Humanos
Isoquinolinas/administração & dosagem
Isoquinolinas/efeitos adversos
Masculino
Meia-Idade
Náusea/induzido quimicamente
Neoplasias/tratamento farmacológico
Quinuclidinas/administração & dosagem
Quinuclidinas/efeitos adversos
Vômito/induzido quimicamente
Adulto Jovem
[Pt] Tipo de publicação:CLINICAL TRIAL, PHASE III; JOURNAL ARTICLE; MULTICENTER STUDY; RANDOMIZED CONTROLLED TRIAL
[Nm] Nome de substância:
0 (Isoquinolines); 0 (Quinuclidines); 3Z8479ZZ5X (Epirubicin); 4Z8R6ORS6L (Thalidomide); 5D06587D6R (palonosetron); 7S5I7G3JQL (Dexamethasone); 80168379AG (Doxorubicin); 8N3DW7272P (Cyclophosphamide); Q20Q21Q62J (Cisplatin)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171030
[Lr] Data última revisão:
171030
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170831
[St] Status:MEDLINE
[do] DOI:10.1200/JCO.2017.72.2538


  4 / 2203 MEDLINE  
              first record previous record next record last record
seleciona
para imprimir
Fotocópia
Texto completo
[PMID]:28756138
[Au] Autor:Duffy MJ; Synnott NC; Crown J
[Ad] Endereço:UCD School of Medicine, Conway Institute of Biomolecular and Biomedical Research, University College Dublin, Dublin 4, Ireland; UCD Clinical Research Centre, St. Vincent's University Hospital, Dublin 4, Ireland. Electronic address: MICHAEL.J.DUFFY@UCD.IE.
[Ti] Título:Mutant p53 as a target for cancer treatment.
[So] Source:Eur J Cancer;83:258-265, 2017 Sep.
[Is] ISSN:1879-0852
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:TP53 (p53) is the single most frequently altered gene in human cancers, with mutations being present in approximately 50% of all invasive tumours. However, in some of the most difficult-to-treat cancers such as high-grade serous ovarian cancers, triple-negative breast cancers, oesophageal cancers, small-cell lung cancers and squamous cell lung cancers, p53 is mutated in at least 80% of samples. Clearly, therefore, mutant p53 protein is an important candidate target against which new anticancer treatments could be developed. Although traditionally regarded as undruggable, several compounds such as p53 reactivation and induction of massive apoptosis-1 (PRIMA-1), a methylated derivative and structural analogue of PRIMA-1, i.e. APR-246, 2-sulfonylpyrimidines such as PK11007, pyrazoles such as PK7088, zinc metallochaperone-1 (ZMC1), a third generation thiosemicarbazone developed by Critical Outcome Techonologies Inc. (COTI-2) as well as specific peptides have recently been reported to reactive mutant p53 protein by converting it to a form exhibiting wild-type properties. Consistent with the reactivation of mutant p53, these compounds have been shown to exhibit anticancer activity in preclinical models expressing mutant p53. To date, two of these compounds, i.e. APR-246 and COTI-2 have progressed to clinical trials. A phase I/IIa clinical trial with APR-246 reported no major adverse effect. Currently, APR-246 is undergoing a phase Ib/II trial in patients with advanced serous ovarian cancer, while COTI-2 is being evaluated in a phase I trial in patients with advanced gynaecological cancers. It remains to be shown however, whether any mutant p53 reactivating compound has efficacy for the treatment of human cancer.
[Mh] Termos MeSH primário: Antineoplásicos/uso terapêutico
Genes p53
Terapia de Alvo Molecular/métodos
Neoplasias/genética
Proteína Supressora de Tumor p53/genética
[Mh] Termos MeSH secundário: Linhagem Celular Tumoral
Terapia Genética/métodos
Seres Humanos
Mutação
Neoplasias/tratamento farmacológico
Quinuclidinas/uso terapêutico
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (2-hydroxymethyl-2-methoxymethylazabicyclo(2.2.2)octan-3-one); 0 (Antineoplastic Agents); 0 (Quinuclidines); 0 (Tumor Suppressor Protein p53)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170911
[Lr] Data última revisão:
170911
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170731
[St] Status:MEDLINE


  5 / 2203 MEDLINE  
              first record previous record next record last record
seleciona
para imprimir
Fotocópia
Texto completo
[PMID]:28732594
[Au] Autor:Guo X; Liu Q; Hu S; Guo W; Yang Z; Zhang Y
[Ad] Endereço:School of Chemical Engineering & Pharmaceutics, Henan University of Science and Technology, Luoyang 471023, China.
[Ti] Título:Thermodynamic models to elucidate the enantioseparation of drugs with two stereogenic centers by micellar electrokinetic chromatography.
[So] Source:J Chromatogr A;1512:133-142, 2017 Aug 25.
[Is] ISSN:1873-3778
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:An equilibrium model depicting the simultaneous protonation of chiral drugs and partitioning of protonated ions and neutral molecules into chiral micelles in micellar electrokinetic chromatography (MEKC) has been introduced. It was used for the prediction and elucidation of complex changes in migration order patterns with experimental conditions in the enantioseparation of drugs with two stereogenic centers. Palonosetron hydrochloride (PALO), a weakly basic drug with two stereogenic centers, was selected as a model drug. Its four stereoisomers were separated by MEKC using sodium cholate (SC) as chiral selector and surfactant. Based on the equilibrium model, equations were derived for a calculation of the effective mobility and migration time of each stereoisomer at a certain pH. The migration times of four stereoisomers at different pHs were calculated and then the migration order patterns were constructed with derived equations. The results were in accord with the experiment. And the contribution of each mechanism to the separation and its influence on the migration order pattern was analyzed separately by introducing virtual isomers, i.e., hypothetical stereoisomers with only one parameter changed relative to a real PALO stereoisomer. A thermodynamic model for a judgment of the correlation of interactions between two stereogenic centers of stereoisomers and chiral selector was also proposed. According to this model, the interactions of two stereogenic centers of PALO stereoisomers in both neutral molecules and protonated ions with chiral selector are not independent, so the chiral recognition in each pair of enantiomers as well as the recognition for diastereomers is not simply the algebraic sum of the contributions of two stereogenic centers due to their correlation.
[Mh] Termos MeSH primário: Cromatografia Capilar Eletrocinética Micelar/métodos
Isoquinolinas/química
Quinuclidinas/química
[Mh] Termos MeSH secundário: Cromatografia Capilar Eletrocinética Micelar/instrumentação
Micelas
Modelos Químicos
Colato de Sódio/química
Estereoisomerismo
Tensoativos/química
Termodinâmica
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Isoquinolines); 0 (Micelles); 0 (Quinuclidines); 0 (Surface-Active Agents); 5D06587D6R (palonosetron); NU3Y4CCH8Z (Sodium Cholate)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171016
[Lr] Data última revisão:
171016
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170723
[St] Status:MEDLINE


  6 / 2203 MEDLINE  
              first record previous record next record last record
seleciona
para imprimir
Fotocópia
Texto completo
Texto completo
[PMID]:28631387
[Au] Autor:Ni H; Htet A; Moe S
[Ad] Endereço:Internal Medicine, Faculty of Medicine, SEGi University, Hospital Sibu, Jalan Ulu Oya, Sibu, Sarawak, Malaysia, 96000.
[Ti] Título:Umeclidinium bromide versus placebo for people with chronic obstructive pulmonary disease (COPD).
[So] Source:Cochrane Database Syst Rev;6:CD011897, 2017 Jun 20.
[Is] ISSN:1469-493X
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: People with chronic obstructive pulmonary disease (COPD) have poor quality of life, reduced survival, and accelerated decline in lung function, especially associated with acute exacerbations, leading to high healthcare costs. Long-acting bronchodilators are the mainstay of treatment for symptomatic improvement, and umeclidinium is one of the new long-acting muscarinic antagonists approved for treatment of patients with stable COPD. OBJECTIVES: To assess the efficacy and safety of umeclidinium bromide versus placebo for people with stable COPD. SEARCH METHODS: We searched the Cochrane Airways Group Specialised Register (CAGR), ClinicalTrials.gov, the World Health Organization (WHO) trials portal, and the GlaxoSmithKline (GSK) Clinical Study Register, using prespecified terms, as well as the reference lists of all identified studies. Searches are current to April 2017. SELECTION CRITERIA: We included randomised controlled trials (RCTs) of parallel design comparing umeclidinium bromide versus placebo in people with COPD, for at least 12 weeks. DATA COLLECTION AND ANALYSIS: We used standard Cochrane methodological procedures. If we noted significant heterogeneity in the meta-analyses, we subgrouped studies by umeclidinium dose. MAIN RESULTS: We included four studies of 12 to 52 weeks' duration, involving 3798 participants with COPD. Mean age of participants ranged from 60.1 to 64.6 years; most were males with baseline mean smoking pack-years of 39.2 to 52.3. They had moderate to severe COPD and baseline mean post-bronchodilator forced expiratory volume in one second (FEV ) ranging from 44.5% to 55.1% of predicted normal. As all studies were systematically conducted according to prespecified protocols, we assessed risk of selection, performance, detection, attrition, and reporting biases as low.Compared with those given placebo, participants in the umeclidinium group had a lesser likelihood of developing moderate exacerbations requiring a short course of steroids, antibiotics, or both (odds ratio (OR) 0.61, 95% confidence interval (CI) 0.46 to 0.80; four studies, N = 1922; GRADE: high), but not specifically requiring hospitalisations due to severe exacerbations (OR 0.86, 95% CI 0.25 to 2.92; four studies, N = 1922, GRADE: low). The number needed to treat for an additional beneficial outcome (NNTB) to prevent an acute exacerbation requiring steroids, antibiotics, or both was 18 (95% CI 13 to 37). Quality of life was better in the umeclidinium group (mean difference (MD) -4.79, 95% CI -8.84 to -0.75; three studies, N = 1119), and these participants had a significantly higher chance of achieving a minimal clinically important difference of at least four units in St George's Respiratory Questionnaire (SGRQ) total score compared with those in the placebo group (OR 1.45, 95% CI 1.16 to 1.82; three studies, N = 1397; GRADE: moderate). The NNTB to achieve one person with a clinically meaningful improvement was 11 (95% CI 7 to 29). The likelihood of all-cause mortality, non-fatal serious adverse events (OR 1.33; 95% CI 0.89 to 2.00; four studies, N = 1922, GRADE: moderate), and adverse events (OR 1.06, 95% CI 0.85 to 1.31; four studies, N = 1922; GRADE: moderate) did not differ between umeclidinium and placebo groups. The umeclidinium group demonstrated significantly greater improvement in change from baseline in trough FEV compared with the placebo group (MD 0.14, 95% CI 0.12 to 0.17; four studies, N = 1381; GRADE: high). Symptomatic improvement was more likely in the umeclidinium group than in the placebo group, as determined by Transitional Dyspnoea Index (TDI) focal score (MD 0.76, 95% CI 0.43 to 1.09; three studies, N = 1193), and the chance of achieving a minimal clinically important difference of at least one unit improvement was significantly higher with umeclidinium than with placebo (OR 1.71, 95% CI 1.37 to 2.15; three studies, N = 1141; GRADE: high). The NNTB to attain one person with clinically important symptomatic improvement was 8 (95% CI 5 to 14). The likelihood of rescue medication usage (change from baseline in the number of puffs per day) was significantly less for the umeclidinium group than for the placebo group (MD -0.45, 95% CI -0.76 to -0.14; four studies, N = 1531). AUTHORS' CONCLUSIONS: Umeclidinium reduced acute exacerbations requiring steroids, antibiotics, or both, although no evidence suggests that it decreased the risk of hospital admission due to exacerbations. Moreover, umeclidinium demonstrated significant improvement in quality of life, lung function, and symptoms, along with lesser use of rescue medications. Studies reported no differences in adverse events, non-fatal serious adverse events, or mortality between umeclidinium and placebo groups; however, larger studies would yield a more precise estimate for these outcomes.
[Mh] Termos MeSH primário: Brometos/uso terapêutico
Doença Pulmonar Obstrutiva Crônica/tratamento farmacológico
Quinuclidinas/uso terapêutico
[Mh] Termos MeSH secundário: Antibacterianos/uso terapêutico
Brometos/efeitos adversos
Progressão da Doença
Feminino
Volume Expiratório Forçado
Hospitalização/estatística & dados numéricos
Seres Humanos
Masculino
Meia-Idade
Números Necessários para Tratar
Placebos/uso terapêutico
Qualidade de Vida
Quinuclidinas/efeitos adversos
Ensaios Clínicos Controlados Aleatórios como Assunto
Fumar/epidemiologia
Esteroides/uso terapêutico
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Anti-Bacterial Agents); 0 (Bromides); 0 (GSK573719); 0 (Placebos); 0 (Quinuclidines); 0 (Steroids)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170901
[Lr] Data última revisão:
170901
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170621
[St] Status:MEDLINE
[do] DOI:10.1002/14651858.CD011897.pub2


  7 / 2203 MEDLINE  
              first record previous record next record last record
seleciona
para imprimir
Fotocópia
Texto completo
[PMID]:28612633
[Au] Autor:Doggrell SA
[Ad] Endereço:a Faculty of Health , Queensland University of Technology , Brisbane , Australia.
[Ti] Título:Granisetron in the treatment of chemotherapy-induced nausea and vomiting (CINV) - is there still a role after comparison with palonosetron?
[So] Source:Expert Opin Pharmacother;18(10):1019-1026, 2017 Jul.
[Is] ISSN:1744-7666
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:INTRODUCTION: Chemotherapy-induced nausea and vomiting (CINV) has a negative impact on the lives of subjects receiving chemotherapy. In 2009, the second generation 5-HT -receptor antagonist, palonosetron, which is longer-acting than granisetron, was shown, as part of dual therapy with dexamethasone, to be superior to intravenous granisetron in the delayed phase of CINV. Area covered: In an attempt to maintain plasma levels of granisetron during the delayed phase of CINV, longer-acting preparations of granisetron have been manufactured. In addition to comparing intravenous/oral granisetron with palonosetron, this review considers the new longer-acting preparations of granisetron (transdermal and subcutanous) with emphasis on whether they are effective in the delayed phase of CINV. Expert opinion: Comparison of intravenous/oral granisetron and palonosetron, as part of triple therapy against the delayed phase of CINV, do not give clear-cut results as to non-inferiority or superiority of either agent. Subcutaneous granisetron is more convenient to use than transdermal granisetron, and has been shown to be non-inferior to palonosetron, as part of dual therapy, in the treatment of the acute and delayed phases of CINV. At present, it seems likely that there will be ongoing roles for intravenous and subcutaneous granisetron in CINV, but further data is required to ascertain the future of transdermal granisetron.
[Mh] Termos MeSH primário: Antieméticos/uso terapêutico
Antineoplásicos/efeitos adversos
Náusea/tratamento farmacológico
Vômito/induzido quimicamente
Vômito/tratamento farmacológico
[Mh] Termos MeSH secundário: Administração Cutânea
Antieméticos/farmacocinética
Antieméticos/farmacologia
Ensaios Clínicos como Assunto
Dexametasona/farmacocinética
Dexametasona/farmacologia
Dexametasona/uso terapêutico
Granisetron/farmacocinética
Granisetron/farmacologia
Granisetron/uso terapêutico
Seres Humanos
Isoquinolinas/farmacocinética
Isoquinolinas/farmacologia
Isoquinolinas/uso terapêutico
Náusea/induzido quimicamente
Quinuclidinas/farmacocinética
Quinuclidinas/farmacologia
Quinuclidinas/uso terapêutico
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Antiemetics); 0 (Antineoplastic Agents); 0 (Isoquinolines); 0 (Quinuclidines); 5D06587D6R (palonosetron); 7S5I7G3JQL (Dexamethasone); WZG3J2MCOL (Granisetron)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:170822
[Lr] Data última revisão:
170822
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170615
[St] Status:MEDLINE
[do] DOI:10.1080/14656566.2017.1342809


  8 / 2203 MEDLINE  
              first record previous record next record last record
seleciona
para imprimir
Fotocópia
Texto completo
[PMID]:28609709
[Au] Autor:Del Bello F; Bonifazi A; Giorgioni G; Petrelli R; Quaglia W; Altomare A; Falcicchio A; Matucci R; Vistoli G; Piergentili A
[Ad] Endereço:Scuola di Scienze del Farmaco e dei Prodotti della Salute, Università di Camerino, Via S. Agostino 1, 62032 Camerino, Italy.
[Ti] Título:Novel muscarinic acetylcholine receptor hybrid ligands embedding quinuclidine and 1,4-dioxane fragments.
[So] Source:Eur J Med Chem;137:327-337, 2017 Sep 08.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:To obtain novel muscarinic acetylcholine receptor (mAChR) antagonists, the enantiomers of the hybrid compounds 3-5, in which the quinuclidin-3-yloxy fragment of solifenacin and the 6,6-diphenyl-1,4-dioxane-2-yl moiety of 2 linked by an ester or ether spacer were embedded in the same chemical entity, were prepared and evaluated for their affinity at the five mAChR subtypes (M -M ). Stereochemistry and the nature of the linker between the quinuclidine moiety and the 1,4-dioxane nucleus play an important role on the affinities of the compounds. The presence of an ether bridge confers higher affinities for all mAChR subtypes to the ligand. Interestingly, the ether enantiomer (R,S)-5 shows the highest affinity at all mAChR subtypes with pK values similar to that of solifenacin at M and higher at the other subtypes. Unlike solifenacin, it shows a preference for M mAChR subtype with respect to the other subtypes. This compound, lacking a permanent positive charge on the nitrogen atom, can be a useful tool for the pharmacological study of mAChRs in the central nervous system.
[Mh] Termos MeSH primário: Dioxanos/farmacologia
Antagonistas Muscarínicos/farmacologia
Quinuclidinas/farmacologia
Receptores Muscarínicos/metabolismo
[Mh] Termos MeSH secundário: Dioxanos/síntese química
Dioxanos/química
Relação Dose-Resposta a Droga
Seres Humanos
Ligantes
Estrutura Molecular
Antagonistas Muscarínicos/síntese química
Antagonistas Muscarínicos/química
Quinuclidinas/síntese química
Quinuclidinas/química
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Dioxanes); 0 (Ligands); 0 (Muscarinic Antagonists); 0 (Quinuclidines); 0 (Receptors, Muscarinic); J8A3S10O7S (1,4-dioxane)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170920
[Lr] Data última revisão:
170920
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170614
[St] Status:MEDLINE


  9 / 2203 MEDLINE  
              first record previous record next record last record
seleciona
para imprimir
Fotocópia
Texto completo
[PMID]:28541001
[Au] Autor:Kim MS; Park JH; Choi YS; Park SH; Shin S
[Ad] Endereço:Department of Anesthesiology and Pain Medicine, Severance Hospital, Seoul, Korea.
[Ti] Título:Efficacy of Palonosetron vs. Ramosetron for the Prevention of Postoperative Nausea and Vomiting: A Meta-Analysis of Randomized Controlled Trials.
[So] Source:Yonsei Med J;58(4):848-858, 2017 Jul.
[Is] ISSN:1976-2437
[Cp] País de publicação:Korea (South)
[La] Idioma:eng
[Ab] Resumo:PURPOSE: This study was designed as a meta-analysis of randomized controlled trials (RCTs) that included the comparison of palonosetron and ramosetron for postoperative nausea and vomiting (PONV) prophylaxis. MATERIALS AND METHODS: A systematic search was conducted for the PubMed, EMBASE, Web of Science, CENTRAL, KoreaMed, and Google Scholar databases (PROSPERO protocol number CRD42015026009). Primary outcomes were the incidences of postoperative nausea (PON) and postoperative vomiting (POV) during the first 48 hrs after surgery. The total 48-hr period was further analyzed in time epochs of 0-6 hrs (early), 6-24 hrs (late), and 24-48 hrs (delayed). Subgroup analyses according to number of risk factors, sex, and type of surgery were also performed. RESULTS: Eleven studies including 1373 patients were analyzed. There was no difference in PON or POV between the two drugs for the total 48-hr period after surgery. However, palonosetron was more effective in preventing POV during the delayed period overall [relative risk (RR), 0.59; 95% confidence interval (CI), 0.39 to 0.89; p=0.013], as well as after subgroup analyses for females and laparoscopies (RR, 0.56; 95% CI, 0.36 to 0.86; p=0.009 and RR, 0.46; 95% CI, 0.23 to 0.94; p=0.033). Subgroup analysis for spine surgery showed that ramosetron was more effective in reducing POV during the total 48-hr (RR, 3.34; 95% CI, 1.46 to 7.63; p=0.004) and early periods (RR, 8.47; 95% CI, 1.57 to 45.72; p=0.013). CONCLUSION: This meta-analysis discovered no definite difference in PONV prevention between the two drugs. The significant findings that were seen in different time epochs and subgroup analyses should be confirmed in future RCTs.
[Mh] Termos MeSH primário: Benzimidazóis/uso terapêutico
Isoquinolinas/uso terapêutico
Náusea e Vômito Pós-Operatório/tratamento farmacológico
Náusea e Vômito Pós-Operatório/prevenção & controle
Quinuclidinas/uso terapêutico
Ensaios Clínicos Controlados Aleatórios como Assunto
[Mh] Termos MeSH secundário: Adulto
Antieméticos/uso terapêutico
Feminino
Seres Humanos
Masculino
Meia-Idade
Náusea e Vômito Pós-Operatório/induzido quimicamente
Viés de Publicação
Fatores de Risco
Resultado do Tratamento
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE; META-ANALYSIS
[Nm] Nome de substância:
0 (Antiemetics); 0 (Benzimidazoles); 0 (Isoquinolines); 0 (Quinuclidines); 5D06587D6R (palonosetron); 7ZRO0SC54Y (ramosetron)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171020
[Lr] Data última revisão:
171020
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170526
[St] Status:MEDLINE
[do] DOI:10.3349/ymj.2017.58.4.848


  10 / 2203 MEDLINE  
              first record previous record
seleciona
para imprimir
Fotocópia
Texto completo
[PMID]:28494140
[Au] Autor:Quadri M; Matera C; Silnovic A; Pismataro MC; Horenstein NA; Stokes C; Papke RL; Dallanoce C
[Ad] Endereço:Dipartimento di Scienze Farmaceutiche, Sezione di Chimica Farmaceutica "Pietro Pratesi", Università degli Studi di Milano, Via Mangiagalli 25, 20133, Milano, Italy.
[Ti] Título:Identification of α7 Nicotinic Acetylcholine Receptor Silent Agonists Based on the Spirocyclic Quinuclidine-Δ -Isoxazoline Scaffold: Synthesis and Electrophysiological Evaluation.
[So] Source:ChemMedChem;12(16):1335-1348, 2017 Aug 22.
[Is] ISSN:1860-7187
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:Compound 11 (3-(benzyloxy)-1'-methyl-1'-azonia-4H-1'-azaspiro[isoxazole-5,3'-bicyclo[2.2.2]octane] iodide) was selected from a previous set of nicotinic ligands as a suitable model compound for the design of new silent agonists of α7 nicotinic acetylcholine receptors (nAChRs). Silent agonists evoke little or no channel activation but can induce the α7 desensitized D state, which is sensitive to a type II positive allosteric modulator, such as PNU-120596. Introduction of meta substituents into the benzyloxy moiety of 11 led to two sets of tertiary amines and quaternary ammonium salts based on the spirocyclic quinuclidinyl-Δ -isoxazoline scaffold. Electrophysiological assays performed on Xenopus laevis oocytes expressing human α7 nAChRs highlighted four compounds that are endowed with a significant silent-agonism profile. Structure-activity relationships of this group of analogues provided evidence of the crucial role of the positive charge at the quaternary quinuclidine nitrogen atom. Moreover, the present study indicates that meta substituents, in particular halogens, on the benzyloxy substructure direct specific interactions that stabilize a desensitized conformational state of the receptor and induce silent activity.
[Mh] Termos MeSH primário: Isoxazóis/química
Agonistas Nicotínicos/síntese química
Quinuclidinas/química
Receptor Nicotínico de Acetilcolina alfa7/metabolismo
[Mh] Termos MeSH secundário: Animais
Desenho de Drogas
Seres Humanos
Isoxazóis/síntese química
Isoxazóis/farmacologia
Agonistas Nicotínicos/química
Agonistas Nicotínicos/farmacologia
Oócitos/efeitos dos fármacos
Oócitos/fisiologia
Quinuclidinas/síntese química
Quinuclidinas/farmacologia
Compostos de Espiro/química
Relação Estrutura-Atividade
Xenopus laevis/crescimento & desenvolvimento
Xenopus laevis/fisiologia
Receptor Nicotínico de Acetilcolina alfa7/agonistas
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Isoxazoles); 0 (Nicotinic Agonists); 0 (Quinuclidines); 0 (Spiro Compounds); 0 (alpha7 Nicotinic Acetylcholine Receptor)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171009
[Lr] Data última revisão:
171009
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170512
[St] Status:MEDLINE
[do] DOI:10.1002/cmdc.201700162



página 1 de 221 ir para página                         
   


Refinar a pesquisa
  Base de dados : MEDLINE Formulário avançado   

    Pesquisar no campo  
1  
2
3
 
           



Search engine: iAH v2.6 powered by WWWISIS

BIREME/OPAS/OMS - Centro Latino-Americano e do Caribe de Informação em Ciências da Saúde