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  1 / 2654 MEDLINE  
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[PMID]:29285947
[Au] Autor:Willems LM; Zöllner JP; Paule E; Schubert-Bast S; Rosenow F; Strzelczyk A
[Ad] Endereço:a Epilepsy Center Frankfurt Rhine-Main and Department of Neurology , Goethe-University , Frankfurt am Main , Germany.
[Ti] Título:Eslicarbazepine acetate in epilepsies with focal and secondary generalised seizures: systematic review of current evidence.
[So] Source:Expert Rev Clin Pharmacol;11(3):309-324, 2018 Mar.
[Is] ISSN:1751-2441
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:INTRODUCTION: Eslicarbazepine acetate (ESL) is a third-generation antiepileptic drug (AED) approved for adjunctive treatment in adults, children, and adolescents with focal-onset seizures. Recently ESL was approved for initial monotherapy in adults. The intention of this article is to review current evidence for ESL and to summarise its pharmacological profile in comparison to other AEDs of the dibenzazepine group. Areas covered: We performed a systematic literature search in electronic databases (MEDLINE database, Cochrane Central Register of Controlled Trials, Excerpta Medica dataBASE) using a combined search strategy including the following keywords: eslicarbazepine, epilepsy and seizure. The search was performed from 2000 until December 2017. Using a standardised assessment form, information on the study design, methodological framework, data sources and efficacy and adverse events attributed to ESL were extracted from each publication and systematically reported. Expert commentary: ESL is an effective, safe and well tolerated third-generation AED for the treatment of focal epilepsies. During therapy, especially serum sodium levels and possible interactions with other substances have to be monitored. As of yet, long-term experience is still needed to make severe late-occurring adverse events unlikely and to obtain data regarding its use in pregnancy.
[Mh] Termos MeSH primário: Anticonvulsivantes/uso terapêutico
Dibenzazepinas/uso terapêutico
Epilepsias Parciais/tratamento farmacológico
[Mh] Termos MeSH secundário: Adolescente
Adulto
Anticonvulsivantes/efeitos adversos
Criança
Dibenzazepinas/efeitos adversos
Interações Medicamentosas
Monitoramento de Medicamentos/métodos
Epilepsia Generalizada/tratamento farmacológico
Seres Humanos
Sódio/sangue
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Anticonvulsants); 0 (Dibenzazepines); 9NEZ333N27 (Sodium); BEA68ZVB2K (eslicarbazepine acetate)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180301
[Lr] Data última revisão:
180301
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171230
[St] Status:MEDLINE
[do] DOI:10.1080/17512433.2018.1421066


  2 / 2654 MEDLINE  
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[PMID]:28745232
[Au] Autor:Khan MA; Javaid K; Wadood A; Jamal A; Batool F; Fazal-Ur-Rehman S; Basha FZ; Choudhary MI
[Ad] Endereço:H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi-75270. Pakistan.
[Ti] Título:In vitro α-Glucosidase Inhibition by Non-sugar based Triazoles of Dibenzoazepine, their Structure-Activity Relationship, and Molecular Docking.
[So] Source:Med Chem;13(7):698-704, 2017.
[Is] ISSN:1875-6638
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: α-Glucosidase inhibitors (AGIs) have been reported for their clinical potential against postprandial hyperglycemia, which is responsible for the risks associated with diabetes mellitus 2 and cardiovascular diseases (CVDs). Besides, a number of compounds have been reported as potent AGIs, several side effects are associated with them. METHODS: The aim of present work is to explore new and potent molecules as AGIs. Therefore, a library of dibenzoazepine linked triazoles (1-15) was studied for their in vitro α-glucosidase inhibitory activity. The binding modes of potent compounds in the active site of α-glucosidase enzyme were also explored through molecular docking studies. RESULTS AND CONCLUSION: Among the reported triazoles, compounds 3-9, 11, and 13 (IC50 = 6.0 ± 0.03 to 19.8 ± 0.28 µM) were found to be several fold more active than the standard drug acarbose (IC50 = 840 ± 1.73 µM). Compound 5 (IC50 = 6.0 ± 0.03 µM) was the most potent AGIs in the series, about 77- fold more active than acarbose. Therefore, dibenzoazepine linked-triazoles described here can serve as leads for further studies as new non-sugar AGIs.
[Mh] Termos MeSH primário: Dibenzazepinas/farmacologia
Inibidores de Glicosídeo Hidrolases/farmacologia
Triazóis/farmacologia
alfa-Glucosidases/metabolismo
[Mh] Termos MeSH secundário: Acarbose/farmacologia
Domínio Catalítico
Dibenzazepinas/síntese química
Inibidores de Glicosídeo Hidrolases/síntese química
Simulação de Acoplamento Molecular
Saccharomyces cerevisiae/enzimologia
Relação Estrutura-Atividade
Triazóis/síntese química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Dibenzazepines); 0 (Glycoside Hydrolase Inhibitors); 0 (Triazoles); EC 3.2.1.20 (alpha-Glucosidases); T58MSI464G (Acarbose)
[Em] Mês de entrada:1712
[Cu] Atualização por classe:171205
[Lr] Data última revisão:
171205
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170727
[St] Status:MEDLINE
[do] DOI:10.2174/1573406413666170726142949


  3 / 2654 MEDLINE  
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[PMID]:28340402
[Au] Autor:Kay L; Willems LM; Zöllner JP; Reif PS; Klein KM; Rosenow F; Strzelczyk A
[Ad] Endereço:Goethe University Frankfurt, Epilepsy Center Frankfurt Rhine-Main, Frankfurt am Main, Germany; Philipps-University Marburg, Epilepsy Center Hessen, Marburg, Germany.
[Ti] Título:Eslicarbazepine acetate as a therapeutic option in a patient with carbamazepine-induced rash and HLA-A*31:01.
[So] Source:Seizure;47:81-82, 2017 Apr.
[Is] ISSN:1532-2688
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Eslicarbazepine acetate (ESL) is an anticonvulsant drug approved for the treatment of focal epilepsies, and related to oxcarbazepine and carbamazepine (CBZ), which are also derivatives of the dibenzazepine family. ESL is contraindicated in patients with hypersensitivity reactions to CBZ.We report a patient with frontal lobe epilepsy responding to treatment with ESL without any serious adverse effects after developing a severe skin rash following treatment with CBZ. HLA testing revealed an HLA-A*31:01 haplotype, that increases the risk of CBZ-induced cutaneous reactions.This case study shows that, in clinical practice, ESL may be considered in a patient with the HLA-A*31:01 haplotype and a hypersensitivity reaction to CBZ.
[Mh] Termos MeSH primário: Anticonvulsivantes/efeitos adversos
Anticonvulsivantes/uso terapêutico
Carbamazepina/efeitos adversos
Dibenzazepinas/uso terapêutico
Exantema/etiologia
Antígeno HLA-B15/genética
[Mh] Termos MeSH secundário: Adulto
Carbamazepina/uso terapêutico
Epilepsia do Lobo Frontal/tratamento farmacológico
Epilepsia do Lobo Frontal/genética
Exantema/genética
Feminino
Haplótipos
Seres Humanos
Variantes Farmacogenômicos
Bloqueadores do Canal de Sódio Disparado por Voltagem/uso terapêutico
[Pt] Tipo de publicação:CASE REPORTS; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anticonvulsants); 0 (Dibenzazepines); 0 (HLA-B*15:02 antigen); 0 (HLA-B15 Antigen); 0 (Voltage-Gated Sodium Channel Blockers); 33CM23913M (Carbamazepine); BEA68ZVB2K (eslicarbazepine acetate)
[Em] Mês de entrada:1704
[Cu] Atualização por classe:170417
[Lr] Data última revisão:
170417
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170325
[St] Status:MEDLINE


  4 / 2654 MEDLINE  
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[PMID]:28293474
[Au] Autor:Mäkinen J; Rainesalo S; Peltola J
[Ad] Endereço:Department of Neurology Tampere University Hospital Tampere Finland.
[Ti] Título:Transition from oxcarbazepine to eslicarbazepine acetate: A single center study.
[So] Source:Brain Behav;7(3):e00634, 2017 Mar.
[Is] ISSN:2162-3279
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:OBJECTIVES: There is limited clinical evidence for comparison between oxcarbazepine (OXC) and eslicarbazepine acetate (ESL) in terms of tolerability, or how to execute the change from OXC to ESL. We report the process of transitioning patients with focal epilepsy from previous OXC treatment to ESL due to tolerability problems. The rationale for change from OXC is reported, and the outcome with respective to this rationale is analyzed in terms of tolerability and efficacy. MATERIALS AND METHODS: The subjects were transitioned overnight from OXC to ESL in a hospital inpatient setting. An evaluation of the effects of the transition was made after 1 and 3 months. All adverse events (AEs) were recorded following the transition period. Subjects were classified by outcome in terms of AEs. RESULTS: Twenty-three subjects were transitioned from OXC to ESL. Fifteen patients OXC-related AEs reduced significantly after transition. Particularly, most of (93%) the AEs presented in the morning resolved after transition to ESL. No patient had an increase in seizure frequency following the transition. The incidence of ESL-related AEs was 39% at 1 month and 13% at 3 month follow-up; however, all patients continued ESL throughout the study period. CONCLUSIONS: This study demonstrates that patients suffering from OXC-related AEs improve in terms of tolerability after a switch to ESL with maintaining seizure control. This improvement is more pronounced if the OXC-related AEs are most evident following morning dosing of OXC. Transition can be safely executed in an outpatient setting.
[Mh] Termos MeSH primário: Carbamazepina/análogos & derivados
Dibenzazepinas/farmacologia
Substituição de Medicamentos/métodos
Epilepsia/tratamento farmacológico
Avaliação de Resultados (Cuidados de Saúde)
Sistema de Registros
Bloqueadores do Canal de Sódio Disparado por Voltagem/farmacologia
[Mh] Termos MeSH secundário: Adulto
Idoso
Carbamazepina/administração & dosagem
Carbamazepina/efeitos adversos
Carbamazepina/farmacologia
Dibenzazepinas/administração & dosagem
Dibenzazepinas/efeitos adversos
Substituição de Medicamentos/efeitos adversos
Feminino
Seguimentos
Seres Humanos
Masculino
Meia-Idade
Bloqueadores do Canal de Sódio Disparado por Voltagem/administração & dosagem
Bloqueadores do Canal de Sódio Disparado por Voltagem/efeitos adversos
Adulto Jovem
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Dibenzazepines); 0 (Voltage-Gated Sodium Channel Blockers); 33CM23913M (Carbamazepine); BEA68ZVB2K (eslicarbazepine acetate); VZI5B1W380 (oxcarbazepine)
[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:170316
[St] Status:MEDLINE
[do] DOI:10.1002/brb3.634


  5 / 2654 MEDLINE  
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[PMID]:28236698
[Au] Autor:Velez FF; Bond TC; Anastassopoulos KP; Wang X; Sousa R; Blum D; Cramer JA
[Ad] Endereço:Sunovion Pharmaceuticals Inc., 84 Waterford Drive, Marlborough, MA 01752, United States. Electronic address: Fulton.Velez@sunovion.com.
[Ti] Título:Impact of seizure frequency reduction on health-related quality of life among clinical trial subjects with refractory partial-onset seizures: A pooled analysis of phase III clinical trials of eslicarbazepine acetate.
[So] Source:Epilepsy Behav;68:203-207, 2017 Mar.
[Is] ISSN:1525-5069
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Subjects who received eslicarbazepine acetate (ESL) as adjunctive therapy experienced significantly greater seizure frequency reduction (SFR) than placebo in three phase III, randomized, double-blind trials. This analysis compared changes in health-related quality of life (HRQOL) between treatment responders and non-responders across the pooled, per-protocol population (N=842) using the validated Quality of Life in Epilepsy Inventory-31 (QOLIE-31). METHODS: QOLIE-31 scores were calculated for Total Score (TS) and seven subscales; higher scores indicate better HRQOL. Mean changes from baseline were calculated. Analysis of covariance examined least square mean (LSM) differences in final scores between responders (≥50% and ≥75% SFR) and non-responders. Clinical significance was based on established minimal clinically important differences (MCIDs). RESULTS: Mean changes were greater among responders for TS (5.2 versus 1.4 for ≥50% SFR; 7.5 versus 1.9 for ≥75% SFR) and all subscales. Additionally, the percentage of subjects with changes meeting or exceeding MCIDs was higher among responders for TS (48.4% versus 33.9% for ≥50% SFR; 56.9% versus 35.8% for ≥75% SFR) and all subscales. Responders had significantly higher final scores for TS (LSM difference=4.0 for ≥50% SFR; LSM difference=5.7 for ≥75% SFR) and all subscales except emotional well-being at ≥50% SFR. LSM differences exceeded MCIDs at ≥75% SFR for TS and five of seven subscales, and two subscales at ≥50% SFR. In a subgroup analysis with placebo removed, LSM differences were larger overall. SIGNIFICANCE: In clinical trials of adjunctive ESL, higher levels of SFR were associated with greater improvements in HRQOL.
[Mh] Termos MeSH primário: Anticonvulsivantes/uso terapêutico
Dibenzazepinas/uso terapêutico
Epilepsias Parciais/tratamento farmacológico
Qualidade de Vida
Convulsões/tratamento farmacológico
[Mh] Termos MeSH secundário: Adulto
Método Duplo-Cego
Feminino
Seres Humanos
Masculino
Saúde Mental
Meia-Idade
Resultado do Tratamento
[Pt] Tipo de publicação:CLINICAL TRIAL, PHASE III; JOURNAL ARTICLE; RANDOMIZED CONTROLLED TRIAL
[Nm] Nome de substância:
0 (Anticonvulsants); 0 (Dibenzazepines); BEA68ZVB2K (eslicarbazepine acetate)
[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:170226
[St] Status:MEDLINE


  6 / 2654 MEDLINE  
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[PMID]:28101651
[Au] Autor:Shorvon SD; Trinka E; Steinhoff BJ; Holtkamp M; Villanueva V; Peltola J; Ben-Menachem E
[Ad] Endereço:UCL Institute of Neurology, Box 5, National Hospital for Neurology and Neurosurgery, Queen Square, London, WC1N 3BG, UK. s.shorvon@ucl.ac.uk.
[Ti] Título:Eslicarbazepine acetate: its effectiveness as adjunctive therapy in clinical trials and open studies.
[So] Source:J Neurol;264(3):421-431, 2017 Mar.
[Is] ISSN:1432-1459
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:Eslicarbazepine acetate (ESL) is a once-daily antiepileptic drug that is approved as adjunctive therapy in adults with focal-onset seizures. Following oral administration, ESL is rapidly metabolized to its active metabolite, eslicarbazepine, which acts primarily by enhancing slow inactivation of voltage-gated sodium channels. The efficacy and safety/tolerability of ESL in the adjunctive setting were established in a comprehensive Phase III program (n = 1702 randomized patients) and this evidence has been supported by several open studies (n = 864). ESL treatment has demonstrated improvements in health-related quality of life, in both randomized clinical trials and open studies. ESL has also been shown to be usually well tolerated and efficacious when used in the adjunctive setting in elderly patients. The effectiveness of ESL as the only add-on to antiepileptic drug monotherapy has been demonstrated in a multinational study (n = 219), subgroup analyses of which have also shown it to be efficacious and generally well tolerated in patients who had previously not responded to carbamazepine therapy. Open studies have also demonstrated improvements in tolerability in patients switched overnight from oxcarbazepine to ESL. Due to differences in pharmacokinetics, pharmacodynamics, and metabolism, there may be clinical situations in which it is appropriate to consider switching patients from oxcarbazepine or carbamazepine to ESL.
[Mh] Termos MeSH primário: Anticonvulsivantes/uso terapêutico
Dibenzazepinas/uso terapêutico
[Mh] Termos MeSH secundário: Anticonvulsivantes/efeitos adversos
Anticonvulsivantes/farmacocinética
Ensaios Clínicos Fase III como Assunto
Dibenzazepinas/efeitos adversos
Dibenzazepinas/farmacocinética
Substituição de Medicamentos
Epilepsias Parciais/tratamento farmacológico
Seres Humanos
Ensaios Clínicos Controlados Aleatórios como Assunto
Convulsões/tratamento farmacológico
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Anticonvulsants); 0 (Dibenzazepines); BEA68ZVB2K (eslicarbazepine acetate)
[Em] Mês de entrada:1704
[Cu] Atualização por classe:170417
[Lr] Data última revisão:
170417
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170120
[St] Status:MEDLINE
[do] DOI:10.1007/s00415-016-8338-2


  7 / 2654 MEDLINE  
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[PMID]:27816990
[Au] Autor:Sakakibara-Konishi J; Ikezawa Y; Oizumi S; Kikuchi J; Kikuchi E; Mizugaki H; Kinoshita I; Dosaka-Akita H; Nishimura M
[Ad] Endereço:First Department of Medicine, Hokkaido University School of Medicine, North 15, West 7, Kita-ku, Sapporo, 060-8638, Japan. konishj@med.hokudai.ac.jp.
[Ti] Título:Combined antitumor effect of γ-secretase inhibitor and ABT-737 in Notch-expressing non-small cell lung cancer.
[So] Source:Int J Clin Oncol;22(2):257-268, 2017 Apr.
[Is] ISSN:1437-7772
[Cp] País de publicação:Japan
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Inhibition of Notch by γ-secretase inhibitor (GSI) has been shown to have an antitumor effect in Notch-expressing non-small cell lung cancer (NSCLC) and to induce apoptosis through modulation of Bcl-2 family proteins. In particular, Bim, a BH3-only member of the Bcl-2 family of proteins, has an important role in the induction of apoptosis in NSCLC when cells are treated with GSI. ABT-737, a BH3-only mimetic, targets the pro-survival Bcl-2 family and also induces apoptosis. METHODS: The Notch-expressing NSCLC cell lines H460, A549, H1793, and HCC2429 were used. The combined antitumor effect of GSI and ABT-737 was evaluated using the MTT proliferation assay in vitro and in xenograft mouse models. The expression of the Notch pathway and Bcl-2 family was analyzed using Western blotting analysis when cells were treated with a single drug treatment or a combination treatment. RESULTS: GSI XX or ABT-737 alone inhibited cell proliferation in a dose-dependent manner, and combination drug treatment showed a synergistic antitumor effect in vitro. In vivo, this drug combination significantly suppressed tumor proliferation compared to the single drug treatment. Phospho-Bcl-2 was downregulated and Bax was upregulated by both the single and combination drug treatments. Bim was induced by a single drug treatment and was enhanced by combination treatment. Combination treatment-induced apoptosis was decreased by Bim inhibition, suggesting that the antitumor effect of the drug combination was dependent on Bim. CONCLUSION: Based on our data, we propose that the combination treatment is a promising strategy for NSCLC therapy.
[Mh] Termos MeSH primário: Secretases da Proteína Precursora do Amiloide/antagonistas & inibidores
Apoptose/efeitos dos fármacos
Compostos de Bifenilo/farmacologia
Carcinoma Pulmonar de Células não Pequenas/patologia
Dibenzazepinas/farmacologia
Neoplasias Pulmonares/patologia
Nitrofenóis/farmacologia
Sulfonamidas/farmacologia
[Mh] Termos MeSH secundário: Animais
Carcinoma Pulmonar de Células não Pequenas/tratamento farmacológico
Carcinoma Pulmonar de Células não Pequenas/metabolismo
Quimioterapia Combinada
Feminino
Seres Humanos
Neoplasias Pulmonares/tratamento farmacológico
Neoplasias Pulmonares/metabolismo
Camundongos
Camundongos Nus
Piperazinas/farmacologia
Receptores Notch/genética
Receptores Notch/metabolismo
Transdução de Sinais/efeitos dos fármacos
Células Tumorais Cultivadas
Ensaios Antitumorais Modelo de Xenoenxerto
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (ABT-737); 0 (Biphenyl Compounds); 0 (Dibenzazepines); 0 (Nitrophenols); 0 (Piperazines); 0 (Receptors, Notch); 0 (Sulfonamides); EC 3.4.- (Amyloid Precursor Protein Secretases); J411KQJ8C2 (dibenzazepine)
[Em] Mês de entrada:1705
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161107
[St] Status:MEDLINE
[do] DOI:10.1007/s10147-016-1060-3


  8 / 2654 MEDLINE  
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[PMID]:27720602
[Au] Autor:Tagawa Y; Namba K; Nakazono Y; Iwata D; Ishida S
[Ad] Endereço:Department of Ophthalmology, Hokkaido University Graduate School of Medicine, Sapporo, Japan.
[Ti] Título:Evaluating the efficacy of epinastine ophthalmic solution using a conjunctivitis allergen challenge model in patients with birch pollen allergic conjunctivitis.
[So] Source:Allergol Int;66(2):338-343, 2017 Apr.
[Is] ISSN:1440-1592
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: The efficacy of epinastine 0.05% ophthalmic solution for pollen allergic conjunctivitis has already been shown in a conjunctival allergen challenge (CAC) test using cedar pollen as a challenge. The present study investigated the efficacy of this solution against birch pollen conjunctivitis in a CAC test. METHODS: Ten adult subjects (eight males and two females) with asymptomatic birch pollen conjunctivitis were enrolled in this study. The average age of the subjects was 41.1 years. This study was conducted during a period without birch pollen dispersion. In each subject, the epinastine 0.05% ophthalmic solution was instilled in one eye, and an artificial tear fluid was instilled in the fellow eye in a double-blind manner. Five minutes or 4 h after the drug instillation, both eyes were challenged with an optimal concentration of birch pollen, and ocular itching and conjunctival hyperemia were then graded. Tears were collected before the drug instillation and 20 min after the pollen challenge, and the histamine level was measured. RESULTS: The ocular itching scores and palpebral conjunctival hyperemia scores of the epinastine-treated eyes were significantly lower than those of the contralateral control eyes when the eyes were pretreated with the drug 4 h before the CAC. There was a significant correlation between the tear histamine level and mean ocular itching score of three time points (3, 5 and 10 min) following the CAC in the control eyes but not the epinastine-treated eyes. CONCLUSIONS: Epinastine is effective in suppressing ocular itching and conjunctival hyperemia in birch pollen conjunctivitis.
[Mh] Termos MeSH primário: Alérgenos/imunologia
Antialérgicos/uso terapêutico
Betula/efeitos adversos
Conjuntivite Alérgica/tratamento farmacológico
Conjuntivite Alérgica/imunologia
Dibenzazepinas/uso terapêutico
Imidazóis/uso terapêutico
Pólen/imunologia
[Mh] Termos MeSH secundário: Adulto
Antialérgicos/administração & dosagem
Biomarcadores
Conjuntivite Alérgica/diagnóstico
Dibenzazepinas/administração & dosagem
Feminino
Histamina/biossíntese
Seres Humanos
Imidazóis/administração & dosagem
Masculino
Meia-Idade
Soluções Oftálmicas
Fenótipo
Lágrimas
Resultado do Tratamento
[Pt] Tipo de publicação:CLINICAL TRIAL; JOURNAL ARTICLE; RANDOMIZED CONTROLLED TRIAL
[Nm] Nome de substância:
0 (Allergens); 0 (Anti-Allergic Agents); 0 (Biomarkers); 0 (Dibenzazepines); 0 (Imidazoles); 0 (Ophthalmic Solutions); 820484N8I3 (Histamine); Q13WX941EF (epinastine)
[Em] Mês de entrada:1704
[Cu] Atualização por classe:170411
[Lr] Data última revisão:
170411
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161011
[St] Status:MEDLINE


  9 / 2654 MEDLINE  
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[PMID]:27444636
[Au] Autor:Schmid E; Kuchukhidze G; Kirschner M; Leitinger M; Höfler J; Rohracher A; Kalss G; Wendling AS; Steinhoff BJ; Trinka E
[Ad] Endereço:Department of Neurology, Christian Doppler Klinik, Paracelsus Medical University, and Centre for Cognitive Neuroscience, Salzburg, Austria.
[Ti] Título:Overnight switching from oxcarbazepine to eslicarbazepine acetate: an observational study.
[So] Source:Acta Neurol Scand;135(4):449-453, 2017 Apr.
[Is] ISSN:1600-0404
[Cp] País de publicação:Denmark
[La] Idioma:eng
[Ab] Resumo:OBJECTIVES: There are clinical situations where it might be appropriate to switch patients from immediate-release oxcarbazepine (OXC) to eslicarbazepine acetate (ESL). We investigated the effects of transitioning patients overnight from OXC to ESL. MATERIALS AND METHODS: A retrospective, single-center study was conducted in which patients with drug-resistant focal epilepsy on a stable dose of immediate-release OXC for at least 4 weeks were switched overnight to ESL. Patients were switched because they experienced persistent seizures with OXC but were unable to tolerate increased OXC dosing due to adverse events. Tolerability was assessed using the Adverse Events Profile (AEP), quality of life was assessed using the Quality of Life in Epilepsy Inventory 10 (QOLIE-10), and alertness was assessed as reaction time using a subtest of the Test Battery for Attention Performance version 2.3. Assessments were performed immediately prior to and 5 days after switching from OXC to ESL (days 0 and 5, respectively). RESULTS: The analysis included 21 patients (12 women, 9 men; mean age 36 years). After switching from OXC to ESL, there were significant improvements in mean scores for AEP (P<.001), QOLIE-10 (P=.001), and alertness (P<.05). Adverse Events Profile total scores improved for 21/21 (100.0%) patients, QOLIE-10 total scores improved for 17/21 (81.0%) patients, and alertness scores improved for 16/21 (76.2%) patients. CONCLUSIONS: In this short-term, single-center study, an overnight switch from twice-daily OXC to once-daily ESL in patients with drug-resistant focal epilepsies resulted in improvements in side effects, quality of life, and alertness.
[Mh] Termos MeSH primário: Anticonvulsivantes/uso terapêutico
Carbamazepina/análogos & derivados
Dibenzazepinas/uso terapêutico
Epilepsia Resistente a Medicamentos/tratamento farmacológico
Substituição de Medicamentos/efeitos adversos
[Mh] Termos MeSH secundário: Adulto
Idoso
Anticonvulsivantes/administração & dosagem
Anticonvulsivantes/efeitos adversos
Carbamazepina/administração & dosagem
Carbamazepina/efeitos adversos
Carbamazepina/uso terapêutico
Dibenzazepinas/administração & dosagem
Dibenzazepinas/efeitos adversos
Feminino
Seres Humanos
Masculino
Meia-Idade
[Pt] Tipo de publicação:JOURNAL ARTICLE; OBSERVATIONAL STUDY
[Nm] Nome de substância:
0 (Anticonvulsants); 0 (Dibenzazepines); 33CM23913M (Carbamazepine); BEA68ZVB2K (eslicarbazepine acetate); VZI5B1W380 (oxcarbazepine)
[Em] Mês de entrada:1705
[Cu] Atualização por classe:170508
[Lr] Data última revisão:
170508
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160723
[St] Status:MEDLINE
[do] DOI:10.1111/ane.12645


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[PMID]:26933171
[Au] Autor:Gifford GB; Demitrack ES; Keeley TM; Tam A; La Cunza N; Dedhia PH; Spence JR; Simeone DM; Saotome I; Louvi A; Siebel CW; Samuelson LC
[Ad] Endereço:Department of Molecular & Integrative Physiology, The University of Michigan School of Medicine, Ann Arbor, Michigan, USA.
[Ti] Título:Notch1 and Notch2 receptors regulate mouse and human gastric antral epithelial cell homoeostasis.
[So] Source:Gut;66(6):1001-1011, 2017 Jun.
[Is] ISSN:1468-3288
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:OBJECTIVE: We tested the ability of Notch pathway receptors Notch1 and Notch2 to regulate stem and epithelial cell homoeostasis in mouse and human gastric antral tissue. DESIGN: Mice were treated with the pan-Notch inhibitor dibenzazepine (DBZ) or inhibitory antibodies targeting Notch1 and/or Notch2. Epithelial proliferation, apoptosis and cellular differentiation were measured by histological and molecular approaches. Organoids were established from mouse and human antral glands; growth and differentiation were measured after treatment with Notch inhibitors. RESULTS: Notch1 and Notch2 are the predominant Notch receptors expressed in mouse and human antral tissue and organoid cultures. Combined inhibition of Notch1 and Notch2 in adult mice led to decreased epithelial cell proliferation, including reduced proliferation of LGR5 stem cells, and increased apoptosis, similar to the response to global Notch inhibition with DBZ. Less pronounced effects were observed after inhibition of individual receptors. Notch pathway inhibition with DBZ or combined inhibition of Notch1 and Notch2 led to increased differentiation of all gastric antral lineages, with remodelling of cells to express secretory products normally associated with other regions of the GI tract, including intestine. Analysis of mouse and human organoids showed that Notch signalling through Notch1 and Notch2 is intrinsic to the epithelium and required for organoid growth. CONCLUSIONS: Notch signalling is required to maintain gastric antral stem cells. Notch1 and Notch2 are the primary Notch receptors regulating epithelial cell homoeostasis in mouse and human stomach.
[Mh] Termos MeSH primário: Células Epiteliais/fisiologia
Homeostase
Organoides/crescimento & desenvolvimento
Receptor Notch1/metabolismo
Receptor Notch2/metabolismo
Células-Tronco/fisiologia
[Mh] Termos MeSH secundário: Animais
Anticorpos Monoclonais Humanizados/farmacologia
Apoptose
Diferenciação Celular
Proliferação Celular
Células Cultivadas
Dibenzazepinas/farmacologia
Células Epiteliais/efeitos dos fármacos
Feminino
Mucosa Gástrica/citologia
Expressão Gênica
Seres Humanos
Masculino
Camundongos
Camundongos Endogâmicos C57BL
Camundongos Transgênicos
Organoides/efeitos dos fármacos
Antro Pilórico
Receptor Notch1/antagonistas & inibidores
Receptor Notch1/genética
Receptor Notch2/antagonistas & inibidores
Receptor Notch2/genética
Receptores Acoplados a Proteínas-G/genética
Receptores Acoplados a Proteínas-G/metabolismo
Transdução de Sinais
Células-Tronco/efeitos dos fármacos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antibodies, Monoclonal, Humanized); 0 (Dibenzazepines); 0 (Lgr5 protein, mouse); 0 (Receptor, Notch1); 0 (Receptor, Notch2); 0 (Receptors, G-Protein-Coupled); J411KQJ8C2 (dibenzazepine)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:AIM; IM
[Da] Data de entrada para processamento:160303
[St] Status:MEDLINE
[do] DOI:10.1136/gutjnl-2015-310811



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