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https://www.readbyqxmd.com/read/29723372/suppression-of-wheal-and-flare-in-histamine-test-by-the-main-h1-antihistamines-commercialized-in-brazil
#1
Helena Maciel-Guerra, Mariana Álvares Penha, Marília Formentini Scotton Jorge, Ricardo da Silva Libório, Ana Cláudia Nazareno Dos Anjos Carrijo, Maria Rita Parise-Fortes, Hélio Amante Miot
BACKGROUND: Several dermatoses are mediated by histamine, such as urticaria, angioedema, and papular urticaria. There are no Brazilian studies comparing the potency of antihistamines. OBJECTIVES: To evaluate the tolerability and efficacy of the main commercial brand and generic H1 antihistamines, regarding the suppression of the wheal and flare to the histamine test. METHODS: A quasi-experimental, open study with 10 healthy adults submitted to the histamine test on the ventral aspect of the forearms...
March 2018: Anais Brasileiros de Dermatologia
https://www.readbyqxmd.com/read/29644705/a-fully-validated-method-for-the-simultaneous-determination-of-11-antihistamines-in-breast-milk-by-gas-chromatography-mass-spectrometry
#2
Maria Katselou, Sotiris Athanaselis, Panagiota Nikolaou, Samir Qammaz, Artemisia Dona, Chara Spiliopoulou, Ioannis Papoutsis
Antihistamines are excreted into breast milk in small amounts; however, there are no adequate published studies or data concerning their effects on newborns and safety during breastfeeding. Thus, the development of sensitive and specific methodologies for the determination of antihistamines in breast milk is critical. A simple and sensitive GC-MS method for the simultaneous determination of eleven antihistamines (diphenhydramine, orphenadrine, chlorpheniramine, dimethindene, meclozine, hydroxyzine, loratadine, desloratadine, cetirizine, rupatadine and ebastine) in breast milk was developed and validated...
April 12, 2018: Biomedical Chromatography: BMC
https://www.readbyqxmd.com/read/29497121/a-preliminary-study-on-efficacy-of-rupatadine-for-the-treatment-of-acute-dengue-infection
#3
Gathsaurie Neelika Malavige, Ananda Wijewickrama, Samitha Fernando, Chandima Jeewandara, Anushka Ginneliya, Supun Samarasekara, Praveen Madushanka, Chameera Punchihewa, Shiran Paranavitane, Damayanthi Idampitiya, Chandanie Wanigatunga, Harsha Dissanayake, Shamini Prathapan, Laksiri Gomes, Siti A B Aman, Ashley St John, Graham S Ogg
Currently there are no specific treatments available for acute dengue infection. We considered that rupatadine, a platelet-activating factor receptor inhibitor, might modulate dengue-associated vascular leak. The effects of rupatadine were assessed in vitro, and in a dengue model, which showed that rupatadine significantly reduced endothelial permeability by dengue sera in vitro, and significantly inhibited the increased haematocrit in dengue-infected mice with dose-dependency. We conducted a randomised, placebo-controlled trial in 183 adult patients in Sri Lanka with acute dengue, which showed that rupatadine up to 40 mg daily appeared safe and well-tolerated with similar proportions of adverse events with rupatadine and placebo...
March 1, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29392757/chronic-spontaneous-urticaria-in-children-a-systematic-review-on-interventions-and-comorbidities
#4
Hélène Cornillier, Bruno Giraudeau, Stéphane Munck, Florence Hacard, Annie-Pierre Jonville-Bera, Gwenaëlle d'Acremont, Bach-Nga Pham, Annabel Maruani
BACKGROUND: Chronic spontaneous urticaria (CSU) is not frequent in children. Management guidelines have been developed for adults and randomized controlled trials (RCTs) included teenagers aged 12-18, but data for children under age 12 are limited. We performed a systematic review to assess comorbidities in children <12 years old with CSU and the efficacy and safety of treatments. METHODS: We searched for original articles of epidemiologic and treatment data in children <12 years old with CSU that were published from 2005 to July 2016 in MEDLINE, EMBASE, CENTRAL, and LILACS...
May 2018: Pediatric Allergy and Immunology
https://www.readbyqxmd.com/read/28763575/cardiac-safety-of-rupatadine-in-a-single-ascending-dose-and-multiple-ascending-dose-study-in-healthy-japanese-subjects-using-intensive-electrocardiogram-assessments-comparison-with-the-previous-white-caucasian-thorough-qt-study
#5
J Täubel, G Ferber, S Fernandes, E Santamaría, I Izquierdo
A thorough QT/QTc study in healthy white Caucasian subjects demonstrated that rupatadine has no proarrhythmic potential and raised no cardiac safety concerns. The present phase 1 study aimed to confirm the cardiac safety of rupatadine in healthy Japanese subjects. In this randomized, double-blind, placebo-controlled study, 27 healthy Japanese subjects were administered single and multiple escalating rupatadine doses of 10, 20, and 40 mg or placebo. Triplicate electrocardiogram (ECG) recordings were performed on days -1, 1, and 5 at several points, and time-matched pharmacokinetic samples were also collected...
January 2018: Clinical Pharmacology in Drug Development
https://www.readbyqxmd.com/read/28622592/second-generation-h1-antihistamines-interaction-with-food-and-alcohol-a-systematic-review
#6
REVIEW
Paweł Paśko, Tomasz Rodacki, Renata Domagała-Rodacka, Krzysztof Palimonka, Monika Marcinkowska, Danuta Owczarek
Histamine is a mediator of many physiological processes. It plays an important role in modulating allergy reactions and immune system responses. H1 receptor is a therapeutic target for drugs applied in allergic diseases such as allergic rhinoconjunctivitis, urticarial, or atopic dermatitis. H1-antihistamines display different chemical structures, pharmacokinetics and a potential for drug-drug and drug-food interactions. Drug-food interactions are known to reduce therapeutic effects of the medicine, as well as to induce a potent adverse drug reactions...
September 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28570220/effects-of-rupatadine-on-platelet-activating-factor-induced-human-mast-cell-degranulation-compared-with-desloratadine-and-levocetirizine-the-maspaf-study
#7
R Munoz-Cano, E Ainsua-Enrich, I Torres-Atencio, M Martin, J Sánchez-Lopez, J Bartra, C Picado, J Mullol, A Valero
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...
2017: Journal of Investigational Allergology & Clinical Immunology
https://www.readbyqxmd.com/read/28419164/population-pharmacokinetic-modelling-of-rupatadine-solution-in-6-11-year-olds-and-optimisation-of-the-experimental-design-in-younger-children
#8
Eva Santamaría, Javier Alejandro Estévez, Jordi Riba, Iñaki Izquierdo, Marta Valle
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...
2017: PloS One
https://www.readbyqxmd.com/read/28163538/comparison-of-efficacy-safety-and-cost-effectiveness-of-rupatadine-and-olopatadine-in-patients-of-allergic-rhinitis-a-prospective-randomized-double-blind-parallel-group-study
#9
Ganesh Dakhale, Yogesh Tathod, Seema Patel, Sonali Pimpalkhute, Latesh Raghute, Ajita Khamkar
OBJECTIVE: To compare the efficacy, safety, and cost-effectiveness of rupatadine and olopatadine in patients of allergic rhinitis (AR). MATERIALS AND METHODS: A 2-week, single-centered, randomized, double-blind, parallel group comparative clinical study was conducted on patients with AR. Following inclusion and exclusion criteria, 67 patients were recruited and randomized to two treatment groups and received the respective drugs for 2 weeks. At follow-up, parameters assessed were total nasal symptom score (TNSS), change in total and differential count of eosinophil...
October 2016: Journal of Pharmacology & Pharmacotherapeutics
https://www.readbyqxmd.com/read/28070872/sedative-effects-of-levocetirizine-a-systematic-review-and-meta-analysis-of-randomized-controlled-studies
#10
REVIEW
Kornkiat Snidvongs, Kachorn Seresirikachorn, Likhit Khattiyawittayakun, Wirach Chitsuthipakorn
INTRODUCTION: As a substrate of P-glycoprotein, levocetirizine should not cause sedative effects. However, while cetirizine, a mixture of levocetirizine and dextrocetirizine, can slightly penetrate the blood brain barrier, the sedative effects of levocetirizine are still under study. OBJECTIVES: The aim of this study was to investigate the sedative effects of levocetirizine. METHODS: An electronic literature search was performed using Medline and EMBASE from January 01, 2001 through August 6, 2015...
February 2017: Drugs
https://www.readbyqxmd.com/read/28058761/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
#11
Selvakumar Kanthiah, Valliappan Kannappan
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...
August 2017: Biomedical Chromatography: BMC
https://www.readbyqxmd.com/read/27758758/effects-of-rupatadine-on-platelet-activating-factor-induced-human-mast-cell-degranulation-compared-with-desloratadine-and-levocetirizine-the-maspaf-study
#12
COMPARATIVE STUDY
R Munoz-Cano, E Ainsua-Enrich, I Torres-Atencio, M Martin, J Sánchez-Lopez, J Bartra, C Picado, J Mullol, A Valero
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...
2017: Journal of Investigational Allergology & Clinical Immunology
https://www.readbyqxmd.com/read/27659218/comparative-efficacy-of-bilastine-desloratadine-and-rupatadine-in-the-suppression-of-wheal-and-flare-response-induced-by-intradermal-histamine-in-healthy-volunteers
#13
RANDOMIZED CONTROLLED TRIAL
Rosa Antonijoan, Jimena Coimbra, Consuelo García-Gea, Montserrat Puntes, Ignasi Gich, Cristina Campo, Román Valiente, Luis Labeaga
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...
January 2017: Current Medical Research and Opinion
https://www.readbyqxmd.com/read/27632557/pharmacokinetics-safety-and-cognitive-function-profile-of-rupatadine-10-20-and-40-mg-in-healthy-japanese-subjects-a-randomised-placebo-controlled-trial
#14
RANDOMIZED CONTROLLED TRIAL
Jörg Täubel, Georg Ferber, Sara Fernandes, Ulrike Lorch, Eva Santamaría, Iñaki Izquierdo
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...
2016: PloS One
https://www.readbyqxmd.com/read/27500993/rupatadine-global-safety-evaluation-in-allergic-rhinitis-and-urticaria
#15
REVIEW
Vanesa González-Núñez, Claus Bachert, Joaquim Mullol
INTRODUCTION: Rupatadine is a second-generation H1-antihistamine with dual affinity for histamine H1 and PAF receptors. Rupatadine is indicated for the treatment of allergic rhinitis and urticaria. AREAS COVERED: A Medline search was conducted to identify preclinical and clinical studies of rupatadine. This was supplemented with additional articles obtained from online sources. The focus of this review is on the safety profile of rupatadine. EXPERT OPINION: The review of these data indicates that rupatadine is highly selective for histamine H1-receptors, exhibits additional PAF antagonism in in vitro and in vivo studies, does not cross the blood-brain barrier, and has similar adverse events comparable with other second-generation antihistamines...
October 2016: Expert Opinion on Drug Safety
https://www.readbyqxmd.com/read/26955097/comparison-of-efficacy-safety-and-cost-effectiveness-of-rupatadine-and-olopatadine-in-patients-of-chronic-spontaneous-urticaria-a-randomized-double-blind-comparative-parallel-group-trial
#16
Ganesh N Dakhale, Sumit S Wankhede, Mohini S Mahatme, Sachin K Hiware, Dharmendra B Mishra, Sujata S Dudhgaonkar
OBJECTIVE: To compare efficacy, safety and cost-effectiveness of rupatadine and olopatadine in patients of chronic spontaneous urticaria. MATERIALS AND METHODS: A 6-week, single-centered, randomized, double blind, parallel group comparative clinical study was conducted on patients with chronic spontaneous urticaria. Following inclusion and exclusion criteria, 60 patients were recruited and were randomized to two treatment groups and received the respective drugs for 6 weeks...
January 2016: Indian Journal of Dermatology
https://www.readbyqxmd.com/read/26591001/rupatadine-in-established-treatment-schemes-improves-chronic-spontaneous-urticaria-symptoms-and-patients-quality-of-life-a-prospective-non-interventional-trial
#17
Martin Metz, Karsten Weller, Claudia Neumeister, Iñaki Izquierdo, Rolf-Hasso Bödeker, Ulrich Schwantes, Marcus Maurer
INTRODUCTION: Chronic spontaneous urticaria (CSU) is a common and hard to treat condition associated with a substantial negative impact on patients' quality of life (QoL). Clinical studies have shown that rupatadine is effective and safe in the treatment of CSU, but data from routine clinical care are scarce. Therefore, we assessed the effectiveness and tolerability of rupatadine in established dosages on CSU activity and patients' QoL in a routine daily practice setting. METHODS: This was an open, prospective, non-interventional study performed in 146 dermatological practices in Germany...
December 2015: Dermatology and Therapy
https://www.readbyqxmd.com/read/26513942/rupatadine-relieves-allergic-rhinitis-a-prospective-observational-study
#18
MULTICENTER STUDY
Ph Eloy, L Tobback, J Imschoot
BACKGROUND: Allergic rhinitis has reached epidemic levels for years in Belgium and substantially impacts the quality of life of patients. Observational, non-interventional studies can provide valuable data, supplementing findings from double-blind trials, on the true value of a drug therapy in daily practice. Rupatadine is a new, second-generation, selective oral H1-antihistamine. The primary objective of.this study was to evaluate the evolution of quality of life in patients treated with rupatadine in clinical practice...
2015: B-ENT
https://www.readbyqxmd.com/read/26267219/rupatadine-is-effective-in-the-treatment-of-chronic-spontaneous-urticaria-in-children-aged-2-11-years
#19
RANDOMIZED CONTROLLED TRIAL
Paul Potter, Essack Mitha, László Barkai, Györgyi Mezei, Eva Santamaría, Iñaki Izquierdo, Marcus Maurer
BACKGROUND: Recommendations in current guidelines for the treatment of chronic spontaneous urticaria (CSU) in infants and children are mostly based on extrapolation of data obtained in adults. This study reports the efficacy and safety of rupatadine, a modern H1 and PAF antagonist recently authorized in Europe for children with allergic rhinitis and CSU. METHODS: A double-blind, randomized, parallel-group, multicentre, placebo-controlled compared study to desloratadine was carried out in children aged 2-11 years with CSU, with or without angio-oedema...
February 2016: Pediatric Allergy and Immunology
https://www.readbyqxmd.com/read/26239325/-antihistamines-for-the-treatment-of-urticaria-in-mexico
#20
Désirée Larenas-Linnemann, Mario Sánchez-Borges, Blanca Estela Del Río-Navarro, María De Lourdes Alonzo-Romero Pareyón, César Alfonso Maldonado-García, Enrique Mendoza-López, José Antonio Ortega-Martell, Juan José Luis Sienra-Monge, Miguel Alejandro Medina-Ávalos, María Isabel Rojo-Gutiérrez, Angélica María Beirana-Palencia, Jorge Bernardo Vargas-Correa, Carlos Báez-Loyola, Ruth Ivonne Mireya Ramírez-Segura, María Graciela Guzmán-Perea
There are four types of histamine receptors. Allergic symptoms, especially those in rhinoconjunctivitis and urticaria, are mainly caused by activation of histamine receptor 1 (H1). Consequently, oral H1-antihistamines form and integral part of the treatment of these diseases. Antihistamines are inverse agonists that stabilize the non-active configuration of the histamine receptor. First generation H1-antihistamines cause a variety of adverse effects via several mechanisms: sedation (accumulation in the central nervous system), dry mouth, urinary retention, weight gain (low selectivity: stimulation of serotonin/muscarinic/alpha-adrenergic receptors) and drug interactions (substrate of CYP450-3A4)...
July 2015: Revista Alergia Mexico: Organo Oficial de la Sociedad Mexicana de Alergia e Inmunología, A.C
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