Safety of rupatadine administered over a period of 1 year in the treatment of persistent allergic rhinitis: A multicentre, open-label study in Spain
ABSTRACT Rupatadine (Rupafin), a novel antihistamine approved recently in Europe for the treatment of allergic rhinitis (AR) and chronic idiopathic urticaria in patients aged>or=12 years, has been shown to be highly efficacious, and as safe and well tolerated as other commonly employed antihistamines in the treatment of allergic disease. There are, however, few data on the long-term safety of these antihistamines derived in accordance with the clinical safety recommendations of the European Agency for the Evaluation of Medicinal Products (EMEA) and the International Conference on Harmonisation (ICH) of Technical Requirements for Registration of Pharmaceuticals for Human Use Guideline.
To assess the safety and tolerability of treatment with rupatadine 10 mg/day for 12 months in subjects with persistent AR (PER).
A multicentre, open-label, phase IV study in patients recruited from 33 centres in Spain, from September 2002 to November 2005. The study enrolled 324 male and female patients (aged 12-70 years) with a medical history of PER for at least 12 months and a documented positive skin-prick test to an appropriate allergen. On 4 of the 7 days prior to start of treatment, the patients were required to have a minimum total nasal symptom score (TNSS [for sneezing, rhinorrhoea, nasal obstruction/congestion and nasal itching]) of >or=5. Of the 324 eligible patients starting treatment, 120 needed to be treated for more than 6 months and were followed up until the end of 12 months. All patients received rupatadine 10 mg/day and were allowed to continue their normal concomitant medication for all conditions, other than rhinitis, for up to 6 or 12 months. Safety was assessed by means of adverse events (AEs) reported by patients or detected by investigators, scheduled centralized ECG with special attention to Bazzet corrected QT interval (QTcB) and standard laboratory investigations.
Assessment of treatment compliance rates indicated 90% and 83% of patients to be compliant during the 1-6 months and 1-12 months treatment periods, respectively, with compliance rates>80% being associated with the majority of the study population reporting at least one AE. Overall, 74.1% and 65.8% of the patients reported at least one AE during the 1-6 months and 1-12 months treatment periods, respectively, compared with 20.4% and 10.8% of patients reporting at least one treatment-related AE during these periods. Disorders of the nervous system and respiratory thoracic and mediastinal system, in particular headache, somnolence and catarrh, were the three most common AEs reported by >5% of the patients during both treatment periods. Detailed ECG assessments demonstrated no clinically relevant abnormal ECG findings, nor any QTcB increases >60 msec or QTcB values>470 msec for any patient at any time during treatment. Serious AEs were reported in seven patients, of whom six were considered as unlikely to be related to rupatadine treatment, whereas one involving increased blood enzyme levels was considered as possibly related to rupatadine treatment.
This study confirmed the good long-term safety and tolerability of rupatadine at the therapeutic dose of 10 mg/day in patients with PER.
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ABSTRACT: Allergic rhinitis (AR) is a disease with high prevalence. In AR, exposure to airborne allergens elicits an allergic response which involves epithelial accumulation of effector cells - e.g. mast cells and basophils - and subsequent inflammation. During the early response in AR, histamine has been found to be the most abundant mediator and it is associated with many symptoms of this disease mediated through the histamine H1 receptor. Therefore, anti-histamines have a role to play in the management of AR. However, the available antihistamines have certain well-known side effects like sedation and potential pro-arrythmic effects owing to their interactions with other drugs, as well as having poor or no effect on platelet activating factor (PAF) which also plays an important role in AR. This article is a qualitative systematic literature review on the pharmacological profile of rupatadine in order to evaluate its safety and efficacy in AR as compared to other anti-histamines. Rupatadine is a once-daily non-sedative, selective, long-acting H1 anti-histamine with antagonistic PAF effects through its interaction with specific receptors. Rupatadine significantly improves nasal symptoms in patients with AR. It has a good safety profile and is devoid of arrythmogenic effects. These properties make rupatadine a suitable first line anti-histamine for the treatment of AR.Primary care respiratory journal: journal of the General Practice Airways Group 09/2008; 18(2):57-68. DOI:10.3132/pcrj.2008.00043
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ABSTRACT: The following paper reviews the latest news on antihistamines used in the treatment of allergic rhinitis. It describes the new results of investigations on clinical application of H3 and H4 receptors in therapy of allergic diseases as well as the effect of emedastine on histamine-induced tissue remodeling. Contemporary clinical research of these drugs fulfills the requirements of placebo-controlled trials, including the comparison with a reference drug, usually cetirizine. The paper discusses efficacy and safety of a new drug--bilastine, and the possibility to improve clinical outcome by combining antihistamine drugs with inhaled glucocorticosteroids and antileukotrienes. It also presents the studies on high efficacy of nasal antihistamines, which most probably results from their high concentration in inflamed tissue, as well as describes the latest news on safe use of antihistamines, including studies of fexofenadine enantiomers in drug interactions with P-glycoprotein, safety of a new antihistamine medication--rupatadine, and psychostimulating effect of some other antihistamines. The review shows that antihistamines, the most frequently used class of anti-allergy medications, have been constantly improved, which is of significant importance for progress of allergic diseases treatment.Otolaryngologia polska. The Polish otolaryngology 09/2009; 63(7):5-10.
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ABSTRACT: Allergies are a widespread group of diseases of civilization and most patients are still undertreated. Since histamine is considered to be the most important mediator in allergies such as allergic rhinitis and urticaria, the most commonly used drugs to treat these disorders are antihistamines acting on the histamine 1 (H1) receptor. The currently available antihistamines, however, have significant differences in their effects and safety profiles. Furthermore, the Allergic Rhinitis and its Impact on Asthma initiative calls for additional desirable properties of antihistamines. Here, we review the profile of rupatadine, a new dual platelet-activating factor and H1-receptor antagonist that fulfils these criteria and therefore offers an excellent option for the treatment of allergic diseases.Expert Review of Clinical Immunology 01/2011; 7(1):15-20. DOI:10.1586/eci.10.85 · 3.34 Impact Factor