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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
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
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
Selvakumar Kanthiah, Kannappan Valliappan
This present 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 by using meclizine as an internal standard. Solid phase extraction method for sample clean-up and preconcentration of analytes was carried out by using Phenomenex Strata-X-C and Strata X polymeric cartridges. Chromatographic analysis was performed on a Phenomenex cyano (150 mm x 4...
January 6, 2017: Biomedical Chromatography: BMC
R Muñoz-Cano, E Ainsua-Enrich, I Torres-Atencio, M Martin, J Sánchez-Lopez, J Bartra, C Picado, J Mullol, A Valero
RATIONALE: Platelet activating factor (PAF) is a lipid mediator involved in the pathophysiology of several allergic diseases, such as the amplification of mast cell (MC) activation in anaphylaxis. Rupatadine is an antihistamine with demonstrated anti-PAF effect but its capacity to inhibit PAF-induced MC degranulation has not been fully evaluated. OBJECTIVE: To investigate the ability of rupatadine to inhibit PAF-induced MC degranulation compared with desloratadine and levocetirizine, to confirm dual rupatadine anti-H1 and anti-PAF activities...
October 19, 2016: Journal of Investigational Allergology & Clinical Immunology
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
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
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
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
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
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
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
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
Soja Shamizadeh, Knut Brockow, Johannes Ring
Rupatadine is a modern non-sedating H1-antihistamine that also haswith additional antagonist effects on platelet-activating factor (PAF). Under the tradenames Rupafin® and Urtimed®, Rrupatadine is approvedregistered in Germany for the treatment of allergic rhinitis and urticaria infor adults and children aged over 12 years. In this review, the available literature available to date onregarding the pharmacological profile and clinical application of Rrupatadine is reviewed and compared to other conventional histamines...
2014: Allergo Journal International
U B Nurmatov, E Rhatigan, F E R Simons, A Sheikh
BACKGROUND: Primary mast cell activation syndromes (MCAS) are a group of disorders presenting with symptoms of mast cell mediator release. OBJECTIVES: To assess the effectiveness and safety of orally administered H1 -antihistamines in the treatment of primary MCAS compared with placebo and other pharmacologic treatments. METHODS: We systematically searched five databases and three trial repositories and contacted an international panel of experts to identify published and unpublished trials...
September 2015: Allergy
Marina Abajian, Laia Curto-Barredo, Karoline Krause, Eva Santamaria, Iñaki Izquierdo, Martin K Church, Marcus Maurer, Ana Giménez-Arnau
Chronic cold urticaria (ColdU) is a rare disease characterized by mast cell-mediated wheals and angioedema following cold exposure. Second-generation H1-antihistamines, such as rupatadine, are the recommended first-line therapy. As of yet, the effects of rupatadine up-dosing on development of ColdU symptom have only been partially characterized. Two-centre, randomized, double-blind, 3-way crossover, placebo-controlled study in patients with a confirmed ColdU was designed to assess the effects of up-dosing of rupatadine...
January 2016: Acta Dermato-venereologica
Chenglong Sun, Qian Li, Liping Pan, Bing Liu, Pan Gu, Junying Zhang, Li Ding, Chungyong Wu
An easy LC-ESI-MS/MS method was developed and validated for simultaneous determination of rupatadine (RT) and its two active metabolites, namely desloratadine (DT) and 3-hydroxydesloratadine (3-OH-DT), in human plasma. The chromatographic separation was carried out on a C18 column with gradient elution by using methanol and 10mM ammonium acetate containing 0.1% (v/v) formic acid. The lower limit of quantification (LLOQ) was 0.05, 0.035 and 0.035 ng/mL for RT, DT and 3-OH-DT, respectively. The intra- and inter-day precision of analytes were within the range of 1...
2015: Journal of Pharmaceutical and Biomedical Analysis
Elisabetta Poluzzi, Emanuel Raschi, Brian Godman, Ariola Koci, Ugo Moretti, Marija Kalaba, Bjorn Wettermark, Miriam Sturkenboom, Fabrizio De Ponti
BACKGROUND: There is appreciable utilisation of antihistamines (H1) in European countries, either prescribed by physician and purchased by patients for self-medication. Terfenadine and astemizole underwent regulatory restrictions in '90 because of their cardiac toxicity, but only scarce clinical data are available on other antihistamines. AIM: To investigate the pro-arrhythmic potential of antihistamines by combining safety reports of the FDA Adverse Event Reporting System (FAERS) with drug utilization data from 13 European Countries...
2015: PloS One
Madhulika Johnson, Gagandeep Kwatra, Dinesh K Badyal, Emy A Thomas
BACKGROUND: Chronic idiopathic urticaria (CIU) is a common dermatological condition. Its pathogenesis involves mainly histamine and also other mediators, including platelet-activating factor (PAF) and tumor necrosis factor-α (TNF-α). In the absence of an exact etiology, H1 -antihistaminics are the mainstay of treatment. Levocetirizine is widely prescribed for CIU. Rupatadine, a newer antihistaminic, has PAF receptor antagonist activity and has shown anti-TNF-α activity in vitro. These additional anti-inflammatory effects may improve its efficacy...
October 2015: International Journal of Dermatology
J Mullol, J Bousquet, C Bachert, G W Canonica, A Giménez-Arnau, M L Kowalski, F E R Simons, M Maurer, D Ryan, G Scadding
In a review of rupatadine published in 2008, the primary focus was on its role as an antihistamine, with a thorough evaluation of its pharmacology and interaction with histamine H1 -receptors. At the time, however, evidence was already emerging of a broader mechanism of action for rupatadine involving other mediators implicated in the inflammatory cascade. Over the past few years, the role of platelet-activating factor (PAF) as a potent mediator involved in the hypersensitivity-type allergic reaction has gained greater recognition...
January 2015: Allergy
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