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  1 / 2033 MEDLINE  
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[PMID]:28419164
[Au] Autor:Santamaría E; Estévez JA; Riba J; Izquierdo I; Valle M
[Ad] Endereço:Clinical Development, R&D, J. Uriach y Compañía, S.A., Barcelona, Spain.
[Ti] Título:Population pharmacokinetic modelling of rupatadine solution in 6-11 year olds and optimisation of the experimental design in younger children.
[So] Source:PLoS One;12(4):e0176091, 2017.
[Is] ISSN:1932-6203
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:AIMS: To optimise a pharmacokinetic (PK) study design of rupatadine for 2-5 year olds by using a population PK model developed with data from a study in 6-11 year olds. The design optimisation was driven by the need to avoid children's discomfort in the study. METHODS: PK data from 6-11 year olds with allergic rhinitis available from a previous study were used to construct a population PK model which we used in simulations to assess the dose to administer in a study in 2-5 year olds. In addition, an optimal design approach was used to determine the most appropriate number of sampling groups, sampling days, total samples and sampling times. RESULTS: A two-compartmental model with first-order absorption and elimination, with clearance dependent on weight adequately described the PK of rupatadine for 6-11 year olds. The dose selected for a trial in 2-5 year olds was 2.5 mg, as it provided a Cmax below the 3 ng/ml threshold. The optimal study design consisted of four groups of children (10 children each), a maximum sampling window of 2 hours in two clinic visits for drawing three samples on day 14 and one on day 28 coinciding with the final examination of the study. CONCLUSIONS: A PK study design was optimised in order to prioritise avoidance of discomfort for enrolled 2-5 year olds by taking only four blood samples from each child and minimising the length of hospital stays.
[Mh] Termos MeSH primário: Antialérgicos/farmacocinética
Ciproeptadina/análogos & derivados
Rinite Alérgica/tratamento farmacológico
[Mh] Termos MeSH secundário: Algoritmos
Antialérgicos/administração & dosagem
Antialérgicos/sangue
Antialérgicos/uso terapêutico
Criança
Pré-Escolar
Simulação por Computador
Ciproeptadina/administração & dosagem
Ciproeptadina/sangue
Ciproeptadina/farmacocinética
Ciproeptadina/uso terapêutico
Feminino
Seres Humanos
Masculino
Modelos Biológicos
Projetos de Pesquisa
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Allergic Agents); 2AE8M83G3E (rupatadine); 2YHB6175DO (Cyproheptadine)
[Em] Mês de entrada:1705
[Cu] Atualização por classe:170505
[Lr] Data última revisão:
170505
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170419
[St] Status:MEDLINE
[do] DOI:10.1371/journal.pone.0176091


  2 / 2033 MEDLINE  
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[PMID]:28337893
[Au] Autor:Gelardi M; De Luca C; Taliente S; Fiorella ML; Quaranta N; Russo C; Ciofalo A; Macchi A; Mancini M; Rosso P; Seccia V; Guagnini F; Ciprandi G
[Ad] Endereço:Otolaryngology, Department of Basic Medical Science, Neuroscience and Sensory Organs, University of Bari “Aldo Moro”, Bari, Italy.
[Ti] Título:Adjuvant treatment with a symbiotic in patients with inflammatory non-allergic rhinitis.
[So] Source:J Biol Regul Homeost Agents;31(1):201-206, 2017 Jan-Mar.
[Is] ISSN:0393-974X
[Cp] País de publicação:Italy
[La] Idioma:eng
[Ab] Resumo:Inflammatory non-allergic rhinitis (INAR) is characterized by the presence of an inflammatory infiltrate and a non-IgE-mediated pathogenesis. This retrospective, controlled, multicentre study investigated whether a symbiotic, containing Lactobacillus acidophilus NCFM, Bifidobacterium lactis, and fructo-oligosaccharides (Pollagen®, Allergy Therapeutics, Italy), prescribed as adjunctive therapy to a standard pharmacological treatment, was able to reduce symptom severity, endoscopic features, and nasal cytology in 93 patients (49 males and 44 females, mean age 36.3±7.1 years) with INAR. The patients were treated with nasal corticosteroid, oral antihistamine, and isotonic saline. At randomization, 52 patients were treated also with symbiotic as adjunctive therapy, whereas the remaining 41 patients served as controls. Treatment lasted for 4 weeks. Patients were visited at baseline, after treatment, and after 4-week follow-up. Adjunctive symbiotic treatment significantly reduced the percentages of patients with symptoms and endoscopic signs, and diminished inflammatory cells. In conclusion, the present study demonstrates that a symbiotic was able, as adjuvant treatment, to significantly improve symptoms, endoscopic feature, and cytology in patients with INAR, and its effect may be long lasting.
[Mh] Termos MeSH primário: Adjuvantes Imunológicos/administração & dosagem
Adjuvantes Farmacêuticos/administração & dosagem
Bifidobacterium animalis/imunologia
Lactobacillus acidophilus/imunologia
Probióticos/administração & dosagem
Rinite/terapia
[Mh] Termos MeSH secundário: Administração Intranasal
Administração Oral
Corticosteroides/uso terapêutico
Adulto
Terapia Combinada/métodos
Ciproeptadina/análogos & derivados
Ciproeptadina/uso terapêutico
Feminino
Antagonistas dos Receptores Histamínicos/uso terapêutico
Seres Humanos
Masculino
Furoato de Mometasona/uso terapêutico
Prebióticos/administração & dosagem
Estudos Retrospectivos
Rinite/imunologia
Rinite/fisiopatologia
[Pt] Tipo de publicação:JOURNAL ARTICLE; MULTICENTER STUDY; RANDOMIZED CONTROLLED TRIAL
[Nm] Nome de substância:
0 (Adjuvants, Immunologic); 0 (Adjuvants, Pharmaceutic); 0 (Adrenal Cortex Hormones); 0 (Histamine Antagonists); 0 (Prebiotics); 04201GDN4R (Mometasone Furoate); 2AE8M83G3E (rupatadine); 2YHB6175DO (Cyproheptadine)
[Em] Mês de entrada:1706
[Cu] Atualização por classe:170601
[Lr] Data última revisão:
170601
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170325
[St] Status:MEDLINE


  3 / 2033 MEDLINE  
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[PMID]:28287686
[Au] Autor:Krasaelap A; Madani S
[Ti] Título:Cyproheptadine: A Potentially Effective Treatment for Functional Gastrointestinal Disorders in Children.
[So] Source:Pediatr Ann;46(3):e120-e125, 2017 Mar 01.
[Is] ISSN:1938-2359
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Functional gastrointestinal disorders (FGIDs) negatively affect children's quality of life and health care costs. It has been proposed that alteration of gut serotonin leads to gastrointestinal dysmotility, visceral hypersensitivity, altered gastrointestinal secretions, and brain-gut dysfunction. Cyproheptadine, a serotonin antagonist, has been shown to be a potentially effective and safe treatment option in children who meet the clinical criteria for FGIDs. Well-designed multicenter trials with long-term follow-up are needed to further investigate its efficacy. [Pediatr Ann. 2017;46(3):e120-e125.].
[Mh] Termos MeSH primário: Ciproeptadina/uso terapêutico
Fármacos Gastrointestinais/uso terapêutico
Gastroenteropatias/tratamento farmacológico
[Mh] Termos MeSH secundário: Criança
Gastroenteropatias/fisiopatologia
Seres Humanos
Resultado do Tratamento
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Gastrointestinal Agents); 2YHB6175DO (Cyproheptadine)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171003
[Lr] Data última revisão:
171003
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170314
[St] Status:MEDLINE
[do] DOI:10.3928/19382359-20170213-01


  4 / 2033 MEDLINE  
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[PMID]:28058761
[Au] Autor:Kanthiah S; Kannappan V
[Ad] Endereço:Department of Pharmacy, Faculty of Engineering and Technology, Annamalai University, Annamalai Nagar, Tamil Nadu, India.
[Ti] Título:D-Optimal mixture design optimization of an HPLC method for simultaneous determination of commonly used antihistaminic parent molecules and their active metabolites in human serum and urine.
[So] Source:Biomed Chromatogr;31(8), 2017 Aug.
[Is] ISSN:1099-0801
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:This study describes a specific, precise, sensitive and accurate method for simultaneous determination of hydroxyzine, loratadine, terfenadine, rupatadine and their main active metabolites cetirizine, desloratadine and fexofenadine, in serum and urine using meclizine as an internal standard. Solid-phase extraction method for sample clean-up and preconcentration of analytes was carried out using Phenomenex Strata-X-C and Strata X polymeric cartridges. Chromatographic analysis was performed on a Phenomenex cyano (150 × 4.6 mm i.d., 5 µm) analytical column. A D-optimal mixture design methodology was used to evaluate the effect of changes in mobile phase compositions on dependent variables and optimization of the response of interest. The mixture design experiments were performed and results were analyzed. The region of ideal mobile phase composition consisting of acetonitrile-methanol-ammonium acetate buffer (40 mm; pH 3.8 adjusted with acetic acid): 18:36:46% v/v/v was identified by a graphical optimization technique using an overlay plot. While using this optimized condition all analytes were baseline resolved in <10 min. Solvent mixtures were delivered at 1.5 mL/min flow rate and analytes peaks were detected at 222 nm. The proposed bioanalytical method was validated according to US Food and Drug Administration guidelines. The proposed method was sensitive with detection limits of 0.06-0.15 µg/mL in serum and urine samples. Relative standard deviation for inter- and intra-day precision data was found to be <7%. The proposed method may find application in the determination of selected antihistaminic drugs in biological fluids.
[Mh] Termos MeSH primário: Antialérgicos/sangue
Antialérgicos/urina
Cromatografia Líquida de Alta Pressão/métodos
Antagonistas dos Receptores Histamínicos H1/sangue
Antagonistas dos Receptores Histamínicos H1/urina
[Mh] Termos MeSH secundário: Antialérgicos/metabolismo
Ciproeptadina/análogos & derivados
Ciproeptadina/sangue
Ciproeptadina/metabolismo
Ciproeptadina/urina
Antagonistas dos Receptores Histamínicos H1/metabolismo
Seres Humanos
Hidroxizina/sangue
Hidroxizina/metabolismo
Hidroxizina/urina
Limite de Detecção
Loratadina/sangue
Loratadina/metabolismo
Loratadina/urina
Extração em Fase Sólida/métodos
Terfenadina/sangue
Terfenadina/metabolismo
Terfenadina/urina
[Pt] Tipo de publicação:JOURNAL ARTICLE; VALIDATION STUDIES
[Nm] Nome de substância:
0 (Anti-Allergic Agents); 0 (Histamine H1 Antagonists); 2AE8M83G3E (rupatadine); 2YHB6175DO (Cyproheptadine); 30S50YM8OG (Hydroxyzine); 7AJO3BO7QN (Loratadine); 7BA5G9Y06Q (Terfenadine)
[Em] Mês de entrada:1707
[Cu] Atualização por classe:170726
[Lr] Data última revisão:
170726
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170107
[St] Status:MEDLINE
[do] DOI:10.1002/bmc.3932


  5 / 2033 MEDLINE  
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[PMID]:27955811
[Au] Autor:Lima TC; Lucarini R; Volpe AC; de Andrade CQ; Souza AM; Pauletti PM; Januário AH; Símaro GV; Bastos JK; Cunha WR; Borges A; da Silva Laurentiz R; Conforti VA; Parreira RL; Borges CH; Caramori GF; Andriani KF; E Silva ML
[Ad] Endereço:Núcleo de Pesquisas em Ciências Exatas e Tecnológicas, Universidade de Franca, Av. Dr. Armando Salles Oliveira 201, Franca - SP 14404-600, Brazil.
[Ti] Título:In vivo and in silico anti-inflammatory mechanism of action of the semisynthetic (-)-cubebin derivatives (-)-hinokinin and (-)-O-benzylcubebin.
[So] Source:Bioorg Med Chem Lett;27(2):176-179, 2017 01 15.
[Is] ISSN:1464-3405
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:(-)-Cubebin (CUB), isolated from seeds of Piper cubeba, was used as starting material to obtain the derivatives (-)-hinokinin (HK) and (-)-O-benzyl cubebin (OBZ). Using paw edema as the experimental model and different chemical mediators (prostaglandin and dextran), it was observed that both derivatives were active in comparison with both negative (5% Tween® 80 in saline) and positive (indomethacin) controls. The highest reduction in the prostaglandin-induced edema was achieved by OBZ (66.0%), while HK caused a 59.2% reduction. Nonetheless, the dextran-induced paw edema was not significantly reduced by either of the derivatives (HK or OBZ), which inhibited edema formation by 18.3% and 3.5%, respectively, in contrast with the positive control, cyproheptadine, which reduced the edema by 56.0%. The docking analysis showed that OBZ presented the most stable ligand-receptor (COX-2 - cyclooxygenase-2) interaction in comparison with CUB and HK.
[Mh] Termos MeSH primário: 4-Butirolactona/análogos & derivados
Anti-Inflamatórios não Esteroides/farmacologia
Benzodioxóis/farmacologia
Dioxóis/farmacologia
Furanos/farmacologia
Lignanas/farmacologia
[Mh] Termos MeSH secundário: 4-Butirolactona/administração & dosagem
4-Butirolactona/síntese química
4-Butirolactona/química
4-Butirolactona/farmacologia
Animais
Anti-Inflamatórios não Esteroides/administração & dosagem
Anti-Inflamatórios não Esteroides/síntese química
Anti-Inflamatórios não Esteroides/química
Benzodioxóis/administração & dosagem
Benzodioxóis/síntese química
Benzodioxóis/química
Domínio Catalítico
Simulação por Computador
Ciclo-Oxigenase 2/química
Inibidores de Ciclo-Oxigenase 2/administração & dosagem
Inibidores de Ciclo-Oxigenase 2/síntese química
Inibidores de Ciclo-Oxigenase 2/química
Inibidores de Ciclo-Oxigenase 2/farmacologia
Ciproeptadina/farmacologia
Dextranos/farmacologia
Dinoprostona/farmacologia
Dioxóis/administração & dosagem
Dioxóis/síntese química
Dioxóis/química
Edema/induzido quimicamente
Furanos/administração & dosagem
Furanos/síntese química
Furanos/química
Indometacina/farmacologia
Ligantes
Lignanas/administração & dosagem
Lignanas/síntese química
Lignanas/química
Lignanas/isolamento & purificação
Masculino
Camundongos
Simulação de Acoplamento Molecular
Polissorbatos/farmacologia
Ratos Wistar
Rutaceae/química
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Anti-Inflammatory Agents, Non-Steroidal); 0 (Benzodioxoles); 0 (Cyclooxygenase 2 Inhibitors); 0 (Dextrans); 0 (Dioxoles); 0 (Furans); 0 (Ligands); 0 (Lignans); 0 (Polysorbates); 0 (o-benzyl cubebin); 26543-89-5 (hinokinin); 2YHB6175DO (Cyproheptadine); EC 1.14.99.- (Ptgs2 protein, mouse); EC 1.14.99.1 (Cyclooxygenase 2); J237078S8A (cubebin); K7Q1JQR04M (Dinoprostone); OL659KIY4X (4-Butyrolactone); XXE1CET956 (Indomethacin)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171124
[Lr] Data última revisão:
171124
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161214
[St] Status:MEDLINE


  6 / 2033 MEDLINE  
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[PMID]:27758758
[Au] Autor:Munoz-Cano R; Ainsua-Enrich E; Torres-Atencio I; Martin M; Sánchez-Lopez J; Bartra J; Picado C; Mullol J; Valero A
[Ad] Endereço:Unitat d'Al·lèrgia, Servei de Pneumologia i Al·lèrgia Respiratòria, Hospital Clínic and Universitat de Barcelona, Barcelona, Catalonia, Spain.
[Ti] Título:Effects of Rupatadine on Platelet- Activating Factor-Induced Human Mast Cell Degranulation Compared With Desloratadine and Levocetirizine (The MASPAF Study).
[So] Source:J Investig Allergol Clin Immunol;27(3):161-168, 2017.
[Is] ISSN:1018-9068
[Cp] País de publicação:Spain
[La] Idioma:eng
[Ab] Resumo:BACKGROUND AND OBJECTIVE: Platelet-activating factor (PAF) is a lipid mediator involved in the pathophysiology of several allergic diseases, for example, in the amplification of mast cell (MC) activation in anaphylaxis. Rupatadine is an antihistamine with a demonstrated anti-PAF effect, although its capacity to inhibit PAF-induced MC degranulation has not been fully evaluated. Objectives: To compare the ability of rupatadine to inhibit PAF-induced MC degranulation with that of desloratadine and levocetirizine and to confirm the dual anti-H1 and anti-PAF activity of rupatadine. METHODS: The human MC line LAD2 and primary MCs (human lung tissue MCs [hLMCs]) were used. MC mediator release was evaluated using the b-hexosaminidase and histamine release assay. The effects of rupatadine (H1 antagonist + PAF receptor antagonist), desloratadine, and levocetirizine (H1 antagonists) on LAD2 and hLMCs were compared. The PAF receptor antagonists WEB2086, BN52021, and CV6209 were also tested. PAF receptor protein expression was evaluated in both LAD2 and hLMCs. RESULTS: CV6209 and rupatadine inhibited PAF-induced MC degranulation in both LAD2 and hLMCs. In LAD2, rupatadine (5 and 10 µM) and levocetirizine (5 µM), but not desloratadine, inhibited PAF-induced b-hexosaminidase release. Rupatadine (1-10 µM), levocetirizine (1-10 µM), and desloratadine (10 µM) inhibited PAF-induced histamine release. Rupatadine at 10 µM had an inhibitory effect on hLMC degranulation, but levocetirizine and desloratadine did not. CONCLUSIONS: This study shows that rupatadine and, to a lesser extent, levocetirizine, but not desloratadine, inhibit PAF-induced degranulation in both LAD2 and hLMCs. These findings support the dual antihistamine and anti-PAF effect of rupatadine in allergic disorders.
[Mh] Termos MeSH primário: Degranulação Celular/efeitos dos fármacos
Cetirizina/farmacologia
Ciproeptadina/análogos & derivados
Antagonistas dos Receptores Histamínicos H1 não Sedativos/farmacologia
Loratadina/análogos & derivados
Mastócitos/efeitos dos fármacos
[Mh] Termos MeSH secundário: Azepinas/farmacologia
Linhagem Celular
Ciproeptadina/farmacologia
Fibrinolíticos/farmacologia
Ginkgolídeos/farmacologia
Antagonistas dos Receptores Histamínicos H1/farmacologia
Seres Humanos
Lactonas/farmacologia
Loratadina/farmacologia
Fator de Ativação de Plaquetas/farmacologia
Inibidores da Agregação de Plaquetas/farmacologia
Glicoproteínas da Membrana de Plaquetas/antagonistas & inibidores
Compostos de Piridínio/farmacologia
Receptores Acoplados a Proteínas-G/antagonistas & inibidores
Triazóis/farmacologia
beta-N-Acetil-Hexosaminidases/efeitos dos fármacos
beta-N-Acetil-Hexosaminidases/secreção
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Azepines); 0 (Fibrinolytic Agents); 0 (Ginkgolides); 0 (Histamine H1 Antagonists); 0 (Histamine H1 Antagonists, Non-Sedating); 0 (Lactones); 0 (Platelet Activating Factor); 0 (Platelet Aggregation Inhibitors); 0 (Platelet Membrane Glycoproteins); 0 (Pyridinium Compounds); 0 (Receptors, G-Protein-Coupled); 0 (Triazoles); 0 (platelet activating factor receptor); 100488-87-7 (CV 6209); 105219-56-5 (WEB 2086); 2AE8M83G3E (rupatadine); 2YHB6175DO (Cyproheptadine); 6U5EA9RT2O (levocetirizine); 7AJO3BO7QN (Loratadine); DF149B9460 (ginkgolide B); EC 3.2.1.52 (beta-N-Acetylhexosaminidases); FVF865388R (desloratadine); YO7261ME24 (Cetirizine)
[Em] Mês de entrada:1711
[Cu] Atualização por classe:171103
[Lr] Data última revisão:
171103
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161021
[St] Status:MEDLINE
[do] DOI:10.18176/jiaci.0117


  7 / 2033 MEDLINE  
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[PMID]:27659218
[Au] Autor:Antonijoan R; Coimbra J; García-Gea C; Puntes M; Gich I; Campo C; Valiente R; Labeaga L
[Ad] Endereço:a Drug Research Center (CIM), Biomedical Research Institute Sant Pau (IIB Sant Pau) , Barcelona , Spain.
[Ti] Título:Comparative efficacy of bilastine, desloratadine and rupatadine in the suppression of wheal and flare response induced by intradermal histamine in healthy volunteers.
[So] Source:Curr Med Res Opin;33(1):129-136, 2017 Jan.
[Is] ISSN:1473-4877
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:OBJECTIVE: To compare the peripheral antihistaminic activity of bilastine, rupatadine and desloratadine in inhibiting the histamine-induced wheal and flare (W&F) response. RESEARCH DESIGN AND METHODS: Twenty-four healthy volunteers aged 18-40 years participated in this crossover, randomized, double-blind, placebo-controlled clinical study. Subjects received single doses of bilastine 20 mg, desloratadine 5 mg, rupatadine 10 mg and placebo. W&F responses induced by intradermal injection of histamine 5 µg were evaluated before treatment (basal value) and at 0.5, 1, 2, 4, 6, 9, 12 and 24 hours after treatment. Fifteen minutes after histamine injection, W&F surface areas (cm ) were quantified using the Visitrak System. Itching sensation was evaluated using a 100 mm visual analog scale. EudraCT number: 2015-000790-13. MAIN OUTCOME MEASURES: The primary outcome measure was the percentage reduction in W&F areas after each active treatment compared with corresponding basal values. RESULTS: Bilastine induced the greatest inhibition in wheal area and was significantly superior to desloratadine and rupatadine from 1 to 12 hours (both p < .001). Rupatadine and desloratadine were better than placebo without differences between them. Maximum wheal inhibition occurred at 6 hours (bilastine 83%, desloratadine 38%, rupatadine 37%). Onset of action was 1 hour for bilastine and 4 hours for desloratadine and rupatadine. Bilastine was significantly superior to desloratadine and rupatadine for flare inhibition from 1-24 hours (both p < .001) with an onset of action at 30 minutes. Bilastine was significantly better than desloratadine (2-12 hours; at least p < .05) and rupatadine (2-9 hours; at least p < .01) for reducing itching sensation. Neither desloratadine nor rupatadine significantly reduced itching compared to placebo. All active treatments were well tolerated. CONCLUSIONS: Bilastine 20 mg induced significantly greater inhibition of the W&F response compared with desloratadine 5 mg and rupatadine 10 mg throughout the 24 hour study period, and had the fastest onset of action. Only bilastine significantly reduced itching sensation versus placebo.
[Mh] Termos MeSH primário: Benzimidazóis/farmacologia
Ciproeptadina/análogos & derivados
Antagonistas dos Receptores Histamínicos/farmacologia
Loratadina/análogos & derivados
Piperidinas/farmacologia
Pele/efeitos dos fármacos
[Mh] Termos MeSH secundário: Adulto
Estudos Cross-Over
Ciproeptadina/farmacologia
Método Duplo-Cego
Feminino
Voluntários Saudáveis
Histamina/farmacologia
Seres Humanos
Injeções Intradérmicas
Loratadina/farmacologia
Masculino
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE; RANDOMIZED CONTROLLED TRIAL
[Nm] Nome de substância:
0 (Benzimidazoles); 0 (Histamine Antagonists); 0 (Piperidines); 2AE8M83G3E (rupatadine); 2YHB6175DO (Cyproheptadine); 7AJO3BO7QN (Loratadine); 820484N8I3 (Histamine); FVF865388R (desloratadine); PA1123N395 (bilastine)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170928
[Lr] Data última revisão:
170928
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160924
[St] Status:MEDLINE


  8 / 2033 MEDLINE  
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[PMID]:27335428
[Au] Autor:De Bruyne P; Christiaens T; Boussery K; Mehuys E; Van Winckel M
[Ad] Endereço:Department of Paediatrics and Medical Genetics, Faculty of Medicine and Health Sciences, Ghent University, Ghent, Belgium.
[Ti] Título:Are antihistamines effective in children? A review of the evidence.
[So] Source:Arch Dis Child;102(1):56-60, 2017 Jan.
[Is] ISSN:1468-2044
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:BACKGROUND AND AIMS: During the last decades, much attention has been paid to off-label and unlicensed prescriptions in paediatrics. However, on-label prescribing can also cause health issues. In this paper, the case of first-generation H -antihistamines is investigated, notably the range of indications for which products are licensed in different European countries and the evidence base (or lack thereof) for each indication, as well as reported adverse drug reactions. METHODS: Review of the Summary of Product Characteristics of first-generation H -antihistamines with a focus on paediatric use. This is plotted against the evidence available in the literature. RESULTS: This investigation shows a large variability in labelled indications and licensing ages when compared in five different European countries. Moreover, most of the indications are not based on clinical trials evaluating efficacy and safety of these drugs in children. CONCLUSIONS: Many of the licensed indications of first-generation antihistamines do not appear to be evidence based.
[Mh] Termos MeSH primário: Antagonistas dos Receptores Histamínicos/uso terapêutico
[Mh] Termos MeSH secundário: Criança
Ciproeptadina/uso terapêutico
Dimetideno/uso terapêutico
Aprovação de Drogas
Rotulagem de Medicamentos
Medicina Baseada em Evidências
Seres Humanos
Uso Off-Label
Resultado do Tratamento
Trimeprazina/uso terapêutico
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Histamine Antagonists); 2YHB6175DO (Cyproheptadine); 661FH77Z3P (Dimethindene); 76H78MJJ52 (Trimeprazine)
[Em] Mês de entrada:1706
[Cu] Atualização por classe:170605
[Lr] Data última revisão:
170605
[Sb] Subgrupo de revista:AIM; IM
[Da] Data de entrada para processamento:160624
[St] Status:MEDLINE
[do] DOI:10.1136/archdischild-2015-310416


  9 / 2033 MEDLINE  
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[PMID]:27828700
[Au] Autor:Deardorff OG; Khan T; Kulkarni G; Doisy R; Loehr C
[Ad] Endereço:Fulton State Hospital, 600 East 5th St, Fulton, MO 65251. Greg.Deardorff@dmh.mo.gov.
[Ti] Título:Serotonin Syndrome: Prophylactic Treatment With Cyproheptadine.
[So] Source:Prim Care Companion CNS Disord;18(4), 2016 Aug 25.
[Is] ISSN:2155-7780
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Despite the numerous advantages of linezolid therapy, one disadvantage continuing to hinder its use is the risk of serotonin syndrome when coadministered with other serotonergic agents. Developing a better understanding of serotonin syndrome is essential for the prevention and management of this potentially life-threatening condition. This report describes a patient with schizophrenia, depression, and severe, acute osteomyelitis. The patient was taking multiple serotonergic agents and required the use of linezolid without the possibility of a sufficient washout period. The severity of the patient's condition in conjunction with increased risk for serotonin syndrome warranted prophylactic treatment with cyproheptadine. The complex pathophysiology of prophylactic treatment of serotonin syndrome with cyproheptadine is worthy of discussion.
[Mh] Termos MeSH primário: Antibacterianos/efeitos adversos
Ciproeptadina/uso terapêutico
Linezolida/efeitos adversos
Antagonistas da Serotonina/uso terapêutico
Síndrome da Serotonina/prevenção & controle
[Mh] Termos MeSH secundário: Adulto
Interações Medicamentosas
Seres Humanos
Masculino
Osteomielite/tratamento farmacológico
[Pt] Tipo de publicação:CASE REPORTS; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Bacterial Agents); 0 (Serotonin Antagonists); 2YHB6175DO (Cyproheptadine); ISQ9I6J12J (Linezolid)
[Em] Mês de entrada:1703
[Cu] Atualização por classe:170307
[Lr] Data última revisão:
170307
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161110
[St] Status:MEDLINE
[do] DOI:10.4088/PCC.16br01966


  10 / 2033 MEDLINE  
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[PMID]:27632557
[Au] Autor:Täubel J; Ferber G; Fernandes S; Lorch U; Santamaría E; Izquierdo I
[Ad] Endereço:Richmond Pharmacology Ltd, St George's University of London, Cranmer Terrace, London, United Kingdom.
[Ti] Título:Pharmacokinetics, Safety and Cognitive Function Profile of Rupatadine 10, 20 and 40 mg in Healthy Japanese Subjects: A Randomised Placebo-Controlled Trial.
[So] Source:PLoS One;11(9):e0163020, 2016.
[Is] ISSN:1932-6203
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:INTRODUCTION: Rupatadine is a marketed second generation antihistamine, with anti-PAF activity, indicated for symptomatic treatment of allergic rhinitis and urticaria. This study was conducted to evaluate the pharmacokinetics (PK), pharmacodynamics (PD), safety and tolerability of rupatadine in healthy Japanese subjects after single and multiple oral doses. METHODS: In this randomised, double-blind, placebo-controlled study, 27 male and female healthy Japanese subjects were administered single and multiple escalating rupatadine dose of 10, 20 and 40 mg or placebo. Blood samples were collected at different time points for PK measurements and subjects were assessed for safety and tolerability. The effect of rupatadine on cognitive functioning was evaluated by means of computerized cognitive tests: rapid visual information processing (RVP), reaction time (RT), spatial working memory (SWM) and visual analogue scales (VAS). RESULTS: Exposure to rupatadine as measured by Cmax and AUC was found to increase in a dose dependent manner over the dose range of 10-40 mg for both single and multiple dose administration. The safety assessments showed that all treatment related side effects were of mild intensity and there were no serious adverse events (SAEs) or withdrawals due to treatment-emergent adverse events (TEAEs) in this study. The therapeutic dose of rupatadine did not show any CNS impairment in any of the cognitive tests. CONCLUSIONS: This study demonstrated that rupatadine is safe and well tolerated by Japanese healthy subjects. The PK-PD profile confirmed previous experience with rupatadine.
[Mh] Termos MeSH primário: Cognição/efeitos dos fármacos
Ciproeptadina/análogos & derivados
Antagonistas dos Receptores Histamínicos/administração & dosagem
[Mh] Termos MeSH secundário: Adulto
Área Sob a Curva
Ciproeptadina/administração & dosagem
Ciproeptadina/efeitos adversos
Ciproeptadina/farmacocinética
Relação Dose-Resposta a Droga
Método Duplo-Cego
Feminino
Voluntários Saudáveis
Antagonistas dos Receptores Histamínicos/efeitos adversos
Antagonistas dos Receptores Histamínicos/farmacocinética
Seres Humanos
Japão
Masculino
Placebos
Fator de Ativação de Plaquetas/antagonistas & inibidores
[Pt] Tipo de publicação:JOURNAL ARTICLE; RANDOMIZED CONTROLLED TRIAL
[Nm] Nome de substância:
0 (Histamine Antagonists); 0 (Placebos); 0 (Platelet Activating Factor); 2AE8M83G3E (rupatadine); 2YHB6175DO (Cyproheptadine)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:170802
[Lr] Data última revisão:
170802
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160916
[St] Status:MEDLINE
[do] DOI:10.1371/journal.pone.0163020



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