levocetirizine and Rhinitis--Allergic--Perennial

Allergic rhinitis represents a worldwide health problem. The prevalence is increasing. The aim of this study was to analyse the correlation between the severity of allergic rhinitis and an adequate treatment dose of modern oral antihistamines.. From a comprehensive databank containing data from ten different open-label prospective observational studies including raw data of 140,853 patients with allergic rhinitis, symptomatology variables were analysed and scored to study the effects of treatment with four antihistamines (Desloratadine, Ebastine, Fexofenadine, Levocetirizine) alone or in combination with intranasal corticosteroids. The patient data were collected in 23,606 study centres from Germany, mostly medical specialist and some primary care physicians in private practice. The analyses were performed via individual patient data meta-analysis techniques.. Finally 92,900 patient data from nine of ten studies could be analysed. One study with data of 47,953 patients was excluded due to incomplete treatment documentation. Both monotherapy analysis subgroups (Total Symptom Score and Total Nasal Symptom Score) were significantly better than those of their combinations with intranasal steroids. Monotherapy with levocetirizine was determined to be significantly more effective in lowering the Total Symptom Score (p < 0.001) and the Total Nasal Symptom Score (p < 0.05) than the other antihistamines. In the next stage, a greater positive effect of levocetirizine was demonstrated in relation to the severity of the clinical symptoms of allergic rhinitis (Total Nasal Symptom Score in cases with severe symptomatology [effect size = -0.09]).. Levocetirizine asserted itself as the only antihistamine compared with the others as significant in this analysis. The study authors recommend monotherapy with the new-generation antihistamine levocetirizine, especially in severe cases of allergic rhinitis.

Topics: Anti-Allergic Agents; Cetirizine; Histamine Antagonists; Histamine H1 Antagonists, Non-Sedating; Humans; Nasal Obstruction; Prospective Studies; Rhinitis, Allergic; Rhinitis, Allergic, Perennial; Treatment Outcome

Bilastine is an orally administered, second-generation antihistamine used in the symptomatic treatment of seasonal or perennial allergic rhinoconjunctivitis and urticaria. In two well designed phase III trials, 14 days' treatment with bilastine was associated with a significantly lower area under the effect curve (AUEC) for the reflective total symptom score (TSS) than placebo in patients with symptomatic seasonal allergic rhinitis. Additionally, reflective nasal symptom scores were significantly lower in bilastine than placebo recipients in patients with a history of seasonal allergic rhinitis who were challenged with grass pollen allergen in a single-centre, phase II study. Neither bilastine nor cetirizine was effective in the treatment of perennial allergic rhinitis with regard to the mean AUEC for reflective TSS in another well designed phase III trial. However, results may have been altered by differences in some baseline characteristics and placebo responses between study countries. In another well designed phase III trial, compared with placebo, bilastine was associated with a significantly greater change from baseline to day 28 in the mean reflective daily urticaria symptom score in patients with chronic urticaria. There were no significant differences in primary endpoint results between bilastine and any of the active comparators used in these trials (i.e. cetirizine, levocetirizine and desloratadine). Bilastine was generally well tolerated, with a tolerability profile that was generally similar to that of the other second-generation antihistamines included in phase III clinical trials.

Topics: Area Under Curve; Benzimidazoles; Cetirizine; Histamine H1 Antagonists, Non-Sedating; Humans; Loratadine; Piperidines; Randomized Controlled Trials as Topic; Rhinitis, Allergic, Perennial; Urticaria

There have recently been guidelines developed for the diagnosis and treatment of rhinitis and urticaria. For both conditions, second-generation antihistamines remain as the first-line therapy.. The article presents the current pharmacology, chemical properties, pharmacokinetics and metabolism of levocetirizine. The article also reviews the clinical efficacy of levocetirizine for seasonal allergic and perennial rhinitis, as well as chronic urticaria. The article is formed through the review of all the published literature in English retrieved from the PubMed/MEDLINE database between 1966 and March 2011 using the search terms: levocetirizine, allergic rhinitis, chronic urticaria and antihistamine. Furthermore, the article also reviews data provided by the manufacturer in addition to reports from governmental agencies.. Levocetirizine has several pharmacokinetic properties that are desirable for an antihistamine providing a combination of both potency and safety. Its clinical advantages are derived from its rapid and extensive absorption, limited distribution and its very low degree of metabolism. Furthermore, levocetirizine scores very highly in terms of clinical efficacy as well as in patient/physician satisfaction studies. Given the lack of large multi-center studies that compare the treatment options for urticaria, clinicians must rely on potency studies when choosing treatment and levocetirizine does score very highly. However, other potent skin antihistamines, such as desloratadine or fexofenadine, should be preferred for patients who have a strict contraindication to the sedative effects of the drug.

Topics: Cetirizine; Chronic Disease; Drug Evaluation; Histamine H1 Antagonists, Non-Sedating; Humans; Randomized Controlled Trials as Topic; Rhinitis, Allergic, Perennial; Rhinitis, Allergic, Seasonal; Urticaria

Oral antihistamines are considered the gold standard therapy for allergic rhinitis to date. The goal of this investigation is to make an indirect comparison between loratadine, an oral antihistamine available over-the-counter (OTC) in the USA, and the more modern antihistamine levocetirizine. Only double-blind, placebo-controlled (DBPC) studies involving monotherapy with the active substances levocetirizine and loratadine were included in the meta-analysis.. The medical databases EMBASE and Medline were searched systematically for all relevant studies completed by the end of 2009. Only DBPC studies conducted in normal environmental settings were included. Furthermore, the Jadad scale was used to guarantee the quality of the studies involved. The "standardized mean difference" (SMD) method was applied for calculating the study-specific effects to neutralize the variability between studies.. The results of a total of seven published DBPC studies met all criteria for inclusion in meta-analysis. The meta-analysis showed that levocetirizine was significantly more effective than loratadine in improving the total symptom score (TSS) (p < 0.01). The effect sizes were calculated as -0.59 (95% confidence interval -0.89, -0.29) for levocetirizine and -0.21 (95% confidence interval -0.31, -0.1) for loratadine when compared to placebo.. The results of this meta-analysis illustrate greater effectiveness for treatment with the active substance levocetirizine as monotherapy in reducing allergic symptoms when compared to treatment with loratadine.

Topics: Anti-Allergic Agents; Cetirizine; Humans; Loratadine; Rhinitis, Allergic, Perennial; Rhinitis, Allergic, Seasonal; Treatment Outcome

Allergic rhinitis is a common disease of great socio-economic significance. The treatment of this condition is carried out on an individual basis depending on the clinical course of the disease; it includes prevention of contacts with the allergen, medicamental and immunotherapy. The principal pharmaceuticals used to treat the patients include oral and intranasal H1 anti-histaminic preparations, intranasal corticosteroids, intranasal cromones, anti-leukotrien agents, and specific subcutaneous immunotherapy. Glencet (levocetirizine) is one of the modern antihistaminic preparations of the second generation having an advantage over other drugs for the treatment of allergic rhinitis in that it may be prescribed to the patients presenting with concomitant bronchial asthma and cardiac diseases.

Topics: Administration, Oral; Adrenal Cortex Hormones; Cetirizine; Combined Modality Therapy; Histamine H1 Antagonists, Non-Sedating; Humans; Immunotherapy; Rhinitis, Allergic, Perennial; Rhinitis, Allergic, Seasonal; Treatment Outcome

Topics: Cetirizine; Controlled Clinical Trials as Topic; Histamine H1 Antagonists, Non-Sedating; Humans; Rhinitis, Allergic, Perennial

Allergic rhinitis is the most prevalent of the atopic disorders, affecting 25% to 35% of persons, depending on the population studied. Considered by non-sufferers to be a trivial disease, allergic rhinitis delivers a significant personal impact on quality of life. Antihistamines have been successfully used for years in the treatment of seasonal/persistent allergic rhinitis. The new generation antihistaminics are all safe, with negligible sedative effects, excellent tolerability and have no influence on cardiac parameters. Montelukast when used as monotherapy is efficacious and improves quality of life. Combination therapy (montelukast plus levocetirizine) is a more effective strategy than monotherapy in the treatment of persistent allergic rhinitis.

Topics: Acetates; Cetirizine; Cyclopropanes; Drug Therapy, Combination; Histamine H1 Antagonists, Non-Sedating; Humans; Leukotriene Antagonists; Quality of Life; Quinolines; Randomized Controlled Trials as Topic; Rhinitis, Allergic, Perennial; Sulfides

This article reports on a systematic literature review of the costs of allergic rhinitis (AR), the economic value of pharmacotherapy of AR, and the factors affecting costs and economic value of pharmacotherapy. Included studies had carried out a cost-of-illness analysis, cost analysis, cost-effectiveness, cost-utility or cost-benefit analysis. Allergic rhinitis imposes a substantial economic burden on society, with indirect costs of productivity loss being larger than the direct healthcare costs. Cost estimates were biased because of difficulties of diagnosis; exclusion of patients who do not seek healthcare; exclusion of over-the-counter medication; difficulties in estimating productivity loss. There is limited evidence on costs of seasonal/perennial and intermittent/persistent AR. Little is known of the economic value of pharmacotherapy of AR, although levocetirizine appears to be cost-effective as compared with placebo. Economic evaluations suffered limitations from small sample sizes, short trial duration, lack of standardized effectiveness measure, restricted scope of costs. Finally, the economic value of pharmacotherapy of AR is influenced by the perspective of the economic evaluation, relative effectiveness and costs of available drugs, patient compliance with treatment.

Topics: Cetirizine; Costs and Cost Analysis; Economics, Pharmaceutical; Humans; Rhinitis, Allergic, Perennial

Levocetirizine (LCZ) is a second-generation antihistamine that was approved in January 2008 for the relief of symptoms of seasonal allergic rhinitis (SAR), perennial allergic rhinitis (PAR), and chronic idiopathic urticaria (CIU) in adults and children aged > or = 6 years.. This article reviews the available literature on the pharmacokinetics and pharmacodynamics, clinical efficacy and tolerability, and effect on quality of life (QoL) of LCZ.. A search of the English-language literature was performed using the following databases: MEDLINE (1966-February 2009), International Pharmaceutical Abstracts (19 70-February 2009), Database of Abstracts of Reviews of Effectiveness, Cochrane Database of Systematic Reviews, EMBASE Drugs & Pharmacology (1991-February 2009), Blackwell Synergy, CINAHL Plus with Full Text, EBSCOhost, ScienceDirect, and Wiley Interscience. The search terms were levocetirizine, allergic rhinitis, chronic idiopathic urticaria, antihistamine, pharmacokinetics, quality of life, drug interactions, case reports, and cost. Publications describing studies of > or = 2 weeks' duration that concerned the efficacy, tolerability, pharmacoeconomics, and/or QoL effects of LCZ were included in the review.. In 4 studies in adult patients with moderate to severe PAR, LCZ 5 mg/d was associated with significant improvements in symptom scores for sneezing, rhinorrhea, and ocular/nasal pruritus at 4 to 6 weeks compared with placebo (P < or = 0.05). In 3 studies, nasal congestion scores were significantly improved within 4 to 6 weeks compared with placebo (P < 0.001). LCZ 5 mg/d was associated with improvements compared with placebo in scores for the ability to do housework, complete work activities, and engage in outdoor activities at 6 months (P < or = 0.011). In a 6-week study in children with moderate to severe SAR, LCZ 5 mg/d was associated with significant improvements compared with placebo in sneezing, rhin-orrhea, and itchy nose (P < 0.004); significant improvements in symptoms from baseline were also seen in a 4-week study in adults with SAR (P < 0.001). One study in patients with SAR reported no significant difference between LCZ and fluticasone compared with fluticasone monotherapy in terms of improvement in QoL, nasal airflow obstruction, sneezing, or pruritus. In a 6-week study in patients with moderate to severe CIU, LCZ 5 mg/d was significantly more effective than placebo in reducing overall CIU symptoms (P < 0.05). In two 4-week studies, one comparing LCZ 5 mg/d with placebo and the other comparing it with desloratadine (DSL), LCZ was significantly more effective than either comparator in terms of improvement in scores for pruritus severity (P < or = 0.001 vs placebo; P < 0.004 vs DSL) and duration (P < or = 0.001 vs placebo; P = 0.009 vs DSL). LCZ was significantly more effective than placebo (but not DSL) in reducing the number and size of wheals (both, P = 0.001). In a 12-week, open-label, crossover study, patients reported significantly longer symptom relief with cetirizine than LCZ (P < 0.005). The most commonly reported adverse events in two 6-month studies in adults with PAR treated with LCZ 5 mg/d included headache (23.8%), pharyngitis (19.4%), influenza (14.6%), fatigue (8.3%), and somnolence (8.3%). There is serious concern about the possibility of febrile seizures in infants treated with LCZ. Three pharmacoeconomic studies of LCZ 5 mg/d were identified, one comparing it with placebo in patients with PAR, one comparing it with placebo in patients with CIU, and another comparing it with second-generation antihistamines and montelukast in patients with PAR. Because of design limitations and differences in comparators in these studies, it wa. In the studies reviewed, LCZ 5 mg/d was effective in reducing symptoms of PAR, SAR, and CIU and improving QoL, with an acceptable tolerabili-ty profile. There is a need for studies of longer durations, head-to-head comparisons against other anti-histamines, drug-interaction studies, safety studies in infants, and cost-effectiveness analyses.

Topics: Adult; Cetirizine; Child; Drug Interactions; Histamine H1 Antagonists, Non-Sedating; Humans; Quality of Life; Rhinitis, Allergic, Perennial; Rhinitis, Allergic, Seasonal; Urticaria

Allergic rhinitis is one of the most common presentations of allergic disorders in the United States, affecting more than 20% of the population. Chronic rhinitis affects patients' quality of life and exacerbates comorbid conditions. Its widespread burden affects society by substantially decreasing worker and scholastic productivity. Allergic rhinitis is typically managed with pharmacotherapy to alleviate symptoms and control comorbid conditions, yet many of these agents carry their own burden due to bothersome and sometimes severe side effects that can compromise patient safety. A new generation of non- or less-sedating antihistamines has recently emerged. These agents offer the promise of enhanced efficacy and tolerability. Of these agents, levocetirizine is the latest antihistamine introduced in the United States. It appears to be safe and effective for the treatment of allergic rhinitis. In addition to covering the above topics, this article reviews the value of levocetirizine for the treatment of allergic rhinitis based on its pharmacologic and pharmacokinetic profile, its efficacy compared with placebo and other new-generation antihistamines, and its safety and tolerability.

Topics: Cetirizine; Histamine H1 Antagonists, Non-Sedating; Humans; Rhinitis, Allergic, Perennial; Rhinitis, Allergic, Seasonal; Treatment Outcome

Second-generation histamine H(1) receptor antagonists were developed to provide efficacious treatment of allergic rhinitis (AR) and chronic idiopathic urticaria (CIU) while decreasing adverse effects associated with first-generation agents. When comparing the efficacy and safety profiles of the newest second-generation antihistamines - desloratadine, fexofenadine and levocetirizine - many pharmacological and clinical criteria must be considered. Most importantly, these elements should not be evaluated separately but, rather, as parts of a puzzle that create a whole picture. As a class, second-generation antihistamines are highly selective for the H(1) receptor. Some bind to it with high affinity, although there is marked heterogeneity among the various compounds. They have a limited effect on the CNS, and clinical studies have noted almost no significant drug-drug interactions in the agents studied. No major cytochrome P450 inhibition has been reported with desloratadine, fexofenadine and levocetirizine, and the bioavailability of desloratadine is minimally affected by drugs interfering with transporter molecules. Of the second-generation antihistamines, desloratadine has the greatest binding affinity for the H(1) receptor. The use of desloratadine, fexofenadine and levocetirizine is not associated with clinically relevant antimuscarinic effects. Desloratadine and fexofenadine do not impair cognitive or psychomotor functioning and are comparable with placebo in terms of somnolence. Based on these pharmacological characteristics, as well as clinical endpoints such as symptom scores, quality-of-life surveys, inflammatory cell counts and investigators' global evaluations, we conclude that desloratadine, fexofenadine and levocetirizine are all efficacious treatments for AR and CIU. However, differences among the antihistamines in relation to a lack of significant interaction with drug transporter molecules and somnolence in excess of placebo may provide some advantages for the overall profile of desloratadine compared with fexofenadine and levocetirizine.

Topics: Cetirizine; Drug Interactions; Histamine H1 Antagonists, Non-Sedating; Humans; Loratadine; Rhinitis, Allergic, Perennial; Rhinitis, Allergic, Seasonal; Terfenadine; Urticaria

Levocetirizine (Xyzal) is a selective, potent, oral histamine H(1) receptor antagonist of the latest generation that is licensed for the symptomatic treatment of allergic rhinitis (including persistent allergic rhinitis [PER]) and chronic idiopathic urticaria (CIU). Large, well designed trials indicate that levocetirizine is effective and generally well tolerated in the treatment of allergic rhinitis and CIU. Its pharmacological profile offers many positive aspects: a rapid onset and long duration of antihistaminic effect; rapid absorption and high bioavailability; a low potential for drug interactions; a low volume of distribution; and a lack of effect on cognition, psychomotor function and the cardiovascular system. Allergen challenge chamber studies suggest that levocetirizine has better efficacy than desloratadine, loratadine or fexofenadine. Well controlled, long-term studies with other later-generation H(1) receptor antagonists are required to fully define its clinical profile relative to other agents in this class. Overall, levocetirizine is a valuable addition to the oral H(1) receptor antagonists available for the treatment of allergic rhinitis and as first-line therapy in patients with CIU.

Topics: Cetirizine; Clinical Trials as Topic; Histamine H1 Antagonists, Non-Sedating; Humans; Hypersensitivity; Piperazines; Rhinitis; Rhinitis, Allergic, Perennial; Rhinitis, Allergic, Seasonal; Skin Diseases; Treatment Outcome

Nasal obstruction, also referred to as congestion, blockage or stuffiness, is a crucial symptom in allergic rhinitis (AR) and may affect sleep as well as quality of life. Early- and late-phase-allergic reactions both contribute to nasal obstruction, although it primarily represents a major symptom in the chronic allergic reaction. A complex network of inflammatory and neurogenic phenomena relates to chronic nasal obstruction, including the subepithelial accumulation of inflammatory cells, particularly mast cells and eosinophils, and the release of neuropeptides. Nasal obstruction is a difficult-to-treat symptom. Vasoconstrictors (decongestants) and intranasal corticosteroids, due to their anti-inflammatory properties, have mainly been used for relieving the nasal passages from the congested mucosa. However, there is accumulating evidence recently that the latest-generation potent antihistamines have decongestant properties in AR. This paper aims to review the pathophysiologic background of nasal obstruction and the evidence for an antihistamine, levocetirizine, in relieving nasal congestion. A meta-analysis on the early and late effects of levocetirizine on nasal obstruction under artificial and natural allergen exposure conditions is presented, demonstrating convincingly that levocetirizine shows a consistent effect on nasal obstruction as early as over the first 2 h and sustained over 6 weeks.

Topics: Cetirizine; Eosinophils; Histamine H1 Antagonists, Non-Sedating; Humans; Mast Cells; Nasal Obstruction; Neuropeptides; Piperazines; Rhinitis, Allergic, Perennial; Time Factors; Treatment Outcome

Allergic rhinitis (AR) is now recognised as a global health problem that affects 10-30% of adults and up to 40% of children. Each year, millions of patients seek treatment from their healthcare provider. However, the prevalence of AR maybe significantly underestimated because of misdiagnosis, under diagnosis and failure of patients to seek medical attention. In addition to the classical symptoms such as sneezing, nasal pruritus, congestion and rhinorrhoea, it is now recognised that AR has a significant impact on quality of life (QOL). This condition can lead to sleep disturbance as a result of nasal congestion, which leads to significant impairment in daily activities such as work and school. Traditionally, AR has been subdivided into seasonal AR (SAR) or perennial AR (PAR). SAR symptoms usually appear during a specific season in which aeroallergens are present in the outdoor air such as tree and grass pollen in the spring and summer and weed pollens in the autumn (fall); and PAR symptoms are present year-round and are triggered by dust mite, animal dander, indoor molds and cockroaches. Oral histamine H(1)-receptor antagonists (H(1) antihistamines) are one of the most commonly prescribed medications for the treatment of AR. There are several oral H(1) antihistamines available and it is important to know the pharmacology, such as administration interval, onset of action, metabolism and conditions that require administration adjustments. When prescribing oral H(1) antihistamines, the healthcare provider must take into account the clinical efficacy and weigh this against the risk of adverse effects from the agent. In addition to the clinical efficacy, potential for improvement in QOL with a particular treatment should also be considered.

Topics: Administration, Oral; Cardiovascular System; Central Nervous System; Cetirizine; Drug Interactions; Histamine H1 Antagonists; Histamine H1 Antagonists, Non-Sedating; Humans; Long QT Syndrome; Loratadine; Piperazines; Practice Guidelines as Topic; Quality of Life; Rhinitis, Allergic, Perennial; Rhinitis, Allergic, Seasonal; Terfenadine; Treatment Outcome

Nasal congestion is a common and troublesome symptom of allergic rhinitis. Because it impairs the natural human drive for nasal breathing, it -- in addition -- leads to lower self-esteem and to impaired quality of life. It is a symptom that is difficult to treat. Traditionally, intranasal steroids, because of their potent anti-inflammatory properties, and vasoconstrictors have been utilized for relieving the nasal passages from the inflamed and congested mucosal tissues. Recent studies with the last-generation antihistamines have demonstrated the decongestant properties of these antihistamines in both the more acute seasonal allergic rhinitis and the more chronic and lasting perennial allergic rhinitis. This study aims to review the efficacy of the potent antihistamine, levocetirizine, in relieving nasal congestion as reported in various studies and settings. Comparisons with placebo and with other antihistamines have been presented in order to help general medical practitioners differentiate between the properties of the various available antihistamines.

Topics: Administration, Inhalation; Anti-Allergic Agents; Cetirizine; Histamine H1 Antagonists, Non-Sedating; Humans; Nasal Obstruction; Piperazines; Quality of Life; Rhinitis, Allergic, Perennial

Allergic rhinitis is a significant public health concern in many developed countries. However, despite evidence for a significant impact on patients' quality of life (QoL) including sleep disruption and reduced daytime performance, allergic rhinitis remains under-managed and hence poorly controlled. This is largely owing to lack of knowledge about, and poor adherence to, established treatment guidelines.. The panel considered available evidence and focused on four published studies on the second-generation antihistamine, levocetirizine. Three of these studies explored the clinical impact of levocetirizine in a broad range of different clinical settings.. Levocetirizine demonstrated an increased benefit over other antihistamines in terms of a more durable antihistamine response: levocetirizine provided improved symptom relief at 24 hours compared to desloratadine or fexofenadine, two frequently prescribed second-generation antihistamines. Levocetirizine also maintained relief of the key symptoms of allergic rhinitis and improved patients' QoL over a treatment period of 6 months, in a real-life setting. The variable efficacy and durability of response of different antihistamines arise from differing modulatory effects on the H(1)-receptor. The speed of relief of symptoms with levocetirizine is supported by the pharmacokinetic data, which shows that steady state plasma concentrations are achieved in a shorter period of time than other second-generation histamines (additionally levocetirizine T(max) is reached in 0.9 h).. These findings support both the short-term and long-term use of levocetirizine in the clinical management of allergic rhinitis. The World Health Organization (WHO) ARIA Guidelines (Allergic Rhinitis and its Impact on Asthma), recommend using a combination of a non-sedating antihistamine with a decongestant, or glucocorticosteroids for treating allergic rhinitis - with the order and combination of treatment depending on severity and duration of symptoms.

Topics: Cetirizine; Histamine H1 Antagonists, Non-Sedating; Humans; Piperazines; Practice Guidelines as Topic; Prevalence; Rhinitis, Allergic, Perennial

Levocetirizine and desloratadine are newer antihistamines indicated for the treatment of allergic rhinitis and chronic idiopathic urticaria.. This article discusses the pharmacokinetics and pharmacodynamics of levocetirizine and desloratadine and reviews studies that have directly compared the effects of these 2 drugs in allergic rhinitis and urticaria.. Relevant articles were identified through a search of MEDLINE from 1999 through 2004 using the main search terms levocetirizine and desloratadine.. Levocetirizine is absorbed rapidly and reaches a steady-state plasma concentration more quickly than does desloratadine. It is also metabolized to a lesser extent than desloratadine, has a lower V(d), and has higher specificity for histamine(1) receptors. Eight well-controlled trials were identified that directly compared the effects of levocetirizine and desloratadine in the skin and nose of healthy individuals and patients with allergic rhinitis. Drug activity was measured in terms of wheal, flare, and itch reactions; nasal symptoms or symptom scores; increases in concentrations of inflammatory markers; or facial thermography. In most of these trials, levocetirizine had a faster onset and greater consistency of effect than desloratadine. The differences in the pharmacokinetic and pharmacodynamic profiles of the 2 drugs may partially explain these clinical findings.. Levocetirizine may be preferred to desloratadine as a treatment option for allergic rhinitis because of its faster onset of action and greater consistency of effect. Although comparative studies in chronic idiopathic urticaria are not available, data from histamine-induced wheal and flare studies in healthy volunteers suggest that levocetirizine may be more effective in preventing itching than desloratadine.

Topics: Cetirizine; Histamine Antagonists; Humans; Loratadine; Nose; Piperazines; Quality of Life; Randomized Controlled Trials as Topic; Rhinitis, Allergic, Perennial; Rhinitis, Allergic, Seasonal; Skin; Urticaria

Levocetirizine is the active R-enantiomer of cetirizine and represents a new second-generation histamine H(1) antagonist. It has a high affinity and selectivity for H(1) receptors. Comparative studies have shown evidence of superior H(1) receptor binding affinity over its racemate, cetirizine. Levocetirizine has a favorable pharmacokinetic profile; it is rapidly and extensively absorbed, minimally metabolized, and has a lower volume of distribution (V(d)) than some other second-generation antihistamines. A number of studies using the histamine-induced wheal and flare model have repeatedly demonstrated marked suppressive effects for levocetirizine. Levocetirizine has also been found to be effective in relieving symptoms of seasonal and perennial allergic rhinitis, including nasal congestion, and its side effects are minor.

Topics: Cetirizine; Histamine H1 Antagonists, Non-Sedating; Humans; Nasal Obstruction; Piperazines; Randomized Controlled Trials as Topic; Rhinitis, Allergic, Perennial; Rhinitis, Allergic, Seasonal

The aim of this study was to evaluate the efficacy and safety of a fixed-dose combination of montelukast and levocetirizine in patients with perennial allergic rhinitis with mild to moderate asthma compared with the efficacy and safety of montelukast alone.. The fixed-dose combination of montelukast and levocetirizine was effective and safe in treating perennial allergic rhinitis in patients with asthma compared with montelukast alone. ClinicalTrials.gov identifier: NCT02552667.

Topics: Acetates; Adult; Anti-Allergic Agents; Anti-Asthmatic Agents; Asthma; Cetirizine; Cyclopropanes; Double-Blind Method; Drug Therapy, Combination; Female; Humans; Male; Quinolines; Republic of Korea; Respiratory Function Tests; Rhinitis, Allergic, Perennial; Sulfides; Treatment Outcome

Dietary supplementation with probiotics alters intestinal microflora of children and may have immunomodulatory effects in prevention of allergic diseases. The aim of this study was to evaluate the effects of Lactobacillus paracasei (LP), strain HF.A00232, as a supplementary agent to levocetirizine in treating children with perennial allergic rhinitis (AR).. This study was a 12-week, double-blind, randomized, placebo-controlled trial. Sixty children with AR aged 6-13 years with nasal total symptoms score (NTSS) ≥5 who fulfilled the inclusion criteria were enrolled. Patients were randomized into two groups with 28 participants receiving levocetirizine plus placebo and 32 participants receiving regular levocetirizine plus LP (HF.A00232) for the first 8 weeks, with a shift to levocetirizine as rescue treatment during the following 4 weeks. Parameters evaluated, including nasal, throat, and eye TSS (NTSS, TTSS, and ETSS, respectively), TSS and levocetirizine use, were recorded daily. Physical examinations and Pediatric Rhinoconjunctivitis Quality of Life Questionnaires (PRQLQs) were administered at each visit. In addition, blood samples were obtained for evaluation of cytokines including interleukin-4, interferon-γ, interleukin-10, and transforming growth factor-β at baseline, Week 8, and Week 12.. The LP (HF.A00232) group had significantly lower PRQLQ scores even after discontinuing regular levocetirizine from Week 9 to Week 12 (p < 0.01). There was more improvement in individual parameters in the PRQLQ, including sneezing (p = 0.005), itchy nose (p = 0.040), and swollen puffy eyes (p = 0.038), in the LP (HF.A00232) group. No significant differences in TSS, NTSS, TTSS, ETSS, or cytokine levels were found between the two groups.. Dietary supplementation with LP (HF.A00232) provided no additional benefit when used with regular levocetirizine in treating AR in the initial 8 weeks of our study, but there was a continuing decrease in PRQLQ scores, as well as a significant improvement in individual symptoms of sneezing, itchy nose, and swollen eyes, after discontinuing regular levocetirizine treatment.

Topics: Adolescent; Cetirizine; Child; Double-Blind Method; Female; Health Surveys; Histamine H1 Antagonists, Non-Sedating; Humans; Interleukin-10; Interleukin-4; Lactobacillus; Male; Probiotics; Quality of Life; Rhinitis, Allergic, Perennial; Surveys and Questionnaires; Treatment Outcome

Supplementary consumption of probiotics may temporarily alter the intestinal microflora of infants and children, thereby preventing and treating allergic disorders.. To compare the clinical efficacy of levocetirizine with that of levocetirizine plus Lactobacillus johnsonii EM1 (Lj EM1) for treating perennial allergic rhinitis (PAR) in children.. Sixty-three children aged 7-12 years fulfilled the entry criteria for the study and had moderate to severe PAR of at least 1 year's duration. The treatment followed a randomized, open-label crossover design: all subjects were randomized to 2 crossover treatment regimens of levocetirizine with Lj EM1 (group 1) or levocetirizine alone (group 2) for 12 weeks; subsequently, treatments were reversed for a further 12 weeks. The effects of the 2 regimens were compared using the Pediatric Rhinoconjunctivitis Quality of Life Questionnaire (PRQLQ) and the total symptom score (TSS) from diary cards. The parameters evaluated were nasal peak expiratory flow rate (nPEFR), FVC, FEV1, serum immunoglobulin E (IgE), mite-specific IgE, eosinophilic cationic protein (ECP), resistin, blood eosinophils, eosinophil percentage in nasal smears, IL-4, IL-10, interferon-γ (IFN-γ), and transforming growth factor-β (TGF-β).. After the first 12 weeks of treatment, TSS in both groups had improved progressively compared with that in the run-in period. Both groups had improved TSS at weeks 4, 8, and 12 (P<0.05), and group 1 was more efficacious than group 2 at week 4 (P=0.014), week 8 (P=0.011), and week 12 (P<0.009). During the second 12-week period, group 2 showed continual and progressive improvement, while group 1 did not. The PRQLQ scores were significantly decreased in both groups (P<0.05), but there was no statistically significant difference between the 2 groups (P=0.446). The eosinophil percentage in nasal smears decreased in both groups compared with that in the run-in period, and significant differences were detected in groups 2 and 1at 16 and 24 weeks of treatment, respectively (P<0.05). Both groups showed significant improvement in nPEFR at weeks 4, 8, 12, 16, and 24 (P<0.01), and the treatment for group 1 appeared to be more efficacious than that for group 2 at weeks 12, 16, and 20 (P<0.05). FVC and FEV1 were improved in both groups at weeks 8 through 24 (P<0.05), but there was no significant difference between the 2 groups. In cytokine measurements, IFN-γ and IL-10 increased significantly and IL-4 decreased significantly in both groups, while elevation of TGF-β was seen only in group 1 at 12 weeks (P<0.001). However, the difference in TGF-β disappeared after 24 weeks treatment. There was no difference in serum resistin levels. No serious adverse events were recorded in either treatment group.. The 24-week, 2-phase, crossover treatment program showed that levocetirizine plus Lj EM1 was more effective for PAR than levocetirizine and that this difference persisted for at least 3 months after discontinuation of Lj EM1.

Topics: Cetirizine; Child; Cross-Over Studies; Histamine H1 Antagonists, Non-Sedating; Humans; Lactobacillus; Probiotics; Rhinitis, Allergic, Perennial

The non-sedating third generation antihistamine levocetirizine has ample evidence of efficacy in allergic rhinitis. In vitro studies suggested that levocetirizine has anti-inflammatory properties not simply related to the antihistamine activity but also to regulation of eosinophils. We performed a double-blind placebo-controlled study in 40 children allergic to house dust mites with persistent rhinitis with the primary aim to evaluate the anti-inflammatory efficacy of levocetirizine measuring eosinophil-related parameters and exhaled nitric oxide (eNO). After one month of treatment, a significant improvement in nasal symptom-medication scores was observed in actively but not in placebo treated patients. After 3 months of treatment, a significant effect was detected on eosinophilic cationic protein (ECP) in nasal mucosa and on nasal eNO in active treated patients. This suggests that during treatment of mite-allergic children with levocetirizine the early improvement in nasal symptoms is due to the antihistamine activity, while more time is needed to achieve an effect on allergic inflammation.

Topics: Animals; Anti-Inflammatory Agents; Asthma; Bronchi; Bronchoconstriction; Cetirizine; Child; Double-Blind Method; Drug Administration Schedule; Eosinophil Cationic Protein; Female; Histamine H1 Antagonists, Non-Sedating; Humans; Italy; Male; Nasal Mucosa; Nitric Oxide; Pyroglyphidae; Rhinitis, Allergic, Perennial; Time Factors; Treatment Outcome

Compared with placebo, levocetirizine has been found to be less sedating than cetirizine in separate trials. However, whether levocetirizine is less sedating than its parent drug cetirizine has not yet been studied in a randomized trial.. To determine whether levocetirizine is less sedating than cetirizine.. We conducted a randomized, double-blind, crossover, placebo-controlled trial examining sedation and allergy symptoms in patients with perennial allergic rhinitis who had previously reported significant sedation with cetirizine. Enrollment ran from January 28, 2009, to February 25, 2009. All patients completed the study by April 17, 2009. Thirty patients enrolled, and 29 patients completed the study (1 patient did not return her questionnaire). In a double-blind fashion, the 29 study participants received levocetirizine, 5 mg daily for 1 week, cetirizine, 10 mg daily for 1 week, and an equivalent placebo pill for 1 week in randomized order with washout periods before each treatment arm. At the end of each washout period and each treatment period, participants completed a 1-page questionnaire. This questionnaire included questions about sedation or sleepiness in the form of a modified Epworth Sleepiness Scale, a Likert scale measuring general or global sedation, and allergy symptoms as measured by the total rhinitis symptom score.. Sedation as measured by both the modified Epworth Sleepiness Scale and the Likert scale was not significantly different between the levocetirizine and cetirizine treatments.. In patients with a perceived history of sedation with cetirizine, most were able to tolerate levocetirizine. However, this controlled trial also suggests that many of these patients would tolerate cetirizine if given in a masked manner. Therefore, patients with a history of mild to moderate sedation with cetirizine are unlikely to experience a different sedation profile with levocetirizine.

Topics: Adult; Aged; Cetirizine; Cross-Over Studies; Double-Blind Method; Female; Histamine H1 Antagonists, Non-Sedating; Humans; Male; Middle Aged; Pilot Projects; Rhinitis, Allergic, Perennial; Statistics, Nonparametric; Surveys and Questionnaires; Young Adult

To compare effectiveness of levocetirizine and budesonide in treatment of persistent allergic rhinitis (PER) in patients with high and low total symptom scores (TSS).. Randomized, parallel-group study. Patients with PER were randomized to receive levocetirizine 5 mg (n = 50) or budesonide 256 microg (n = 50) daily for 4 week and were followed-up for another 4 weeks post-treatment. TSS combining itching, sneezing, rhinorrhea, daytime and nighttime nasal congestion was recorded daily during and after treatment for an entire period of 8 weeks. Efficacy variables included area under curves depicting reduction and increase in TSSs over time relative to baselines and time to response and symptom relapses.. Symptoms were categorized as high and low using a median TSS of 8 as cutoff. Levocetirizine was as effective in control of high and low symptoms except for time to achieve maximum effect (2 days versus 1 week, respectively, p = 0.002) but was more effective in preventing relapses of high symptoms (p = 0.001). Budesonide was more effective against high than low symptoms (p < 0.001) but showed no difference in preventing relapses. Typical response rate of levocetirizine and budesonide were demonstrated in treatment of high symptoms. Levocetirizine achieved its full effectiveness in 2 days while budesonide required 2 weeks. Budesonide at full effect (after 2 weeks) was superior to levocetirizine (p = 0.004) but comparable for the entire treatment of 4 weeks (p =.059) and was inferior to in preventing relapses (p = 0.001). No such difference could be observed between these drugs in control of low symptoms.. The effectiveness of the drug treatment in the present study is dependent of symptom severity. Levocetirizine bases on its rate of response and relapse was superior to budesonide in treatment of the high symptom group and is comparable in the low symptom group.

Topics: Adult; Aged; Anti-Inflammatory Agents; Area Under Curve; Budesonide; Cetirizine; Female; Histamine H1 Antagonists, Non-Sedating; Humans; Male; Middle Aged; Rhinitis, Allergic, Perennial; Severity of Illness Index; Sneezing; Time Factors; Young Adult

Levocetirizine has been shown in observational studies in the west as an effective and satisfactory therapy for patients with allergic respiratory and skin disease. An open-label, multicentre observational study was conducted to investigate the patients' perception of levocetirizine in the treatment of allergic rhinitis (AR) and urticaria in Taiwanese patients. Three hundred and thirty-three patients (236 AR and 97 urticaria patients) attending out-patient clinics of medical centres across Taiwan were included in the study. Patients were treated with levocetirizine 5 mg once daily (AR patients for 2-4 weeks and urticaria patients for 2-6 weeks) and at the end of treatment, they evaluated for symptoms of disease, perception of change in symptoms, global efficacy and tolerability, global preference over previous antiallergic treatment, change in quality of sleep/daily activities, and safety and adverse events (AEs). Levocetirizine markedly improved the symptoms of AR and urticaria; with 70-75% of AR patients and 60-80% of urticaria patients reporting complete or marked improvements in individual symptoms. Asthma symptoms were completely or markedly improved in 44% of patients with AR and concomitant asthma. A majority of the patients was satisfied with levocetirizine therapy and 50-70% indicated preference for levocetirizine over previous therapy. Overall, 50-74% of all patients perceived improvements in quality of sleep/daily activities and 50-65% of the patients rated the onset of action for levocetirizine as very rapid or rapid. Somnolence was the most common AE, reported by 7.4% of AR and 7.0% of urticaria patients. The results of this study indicated that levocetirizine is an effective and satisfactory therapy for the management of allergic respiratory and skin disease in Taiwanese subjects.

Topics: Adolescent; Adult; Aged; Aged, 80 and over; Cetirizine; Child; Female; Histamine H1 Antagonists, Non-Sedating; Humans; Male; Middle Aged; Patient Satisfaction; Rhinitis, Allergic, Perennial; Rhinitis, Allergic, Seasonal; Sleep; Taiwan; Urticaria; Young Adult

Cetirizine (Zyrtec) is a potent and long-acting second-generation histamine H1- receptor antagonist for the treatment of allergic disease, such as allergic rhinitis and chronic idiopathic urticaria, in adult and child. It is a racemic mixture of levocetirizine (Xyzal) and dextrocetirizine. The purpose of this present study was to compare the efficacy of cetirizine, levocetirizine and placebo for the treatment of pediatric perennial allergic rhinitis. 74 perennial allergic rhinitis patients, aged 6 to 12 years old, assigned to 1 of 3 treatment groups for 12 weeks randomly. The effects of the three agents were compared with the Pediatric Rhinoconjunctivitis Quality of Life Questionnaire (PRQLQ) and Total Symptom Score (TSS) by diary. Nasal peak expiratory flow rate (nPEFR) and laboratory examinations including serum immunoglobulin E level, eosinophil cationic protein (ECP), blood eosinophil counts and eosinophil percentage in a nasal smear were evaluated among the three groups. The results revealed that both cetirizine and levocetirizine improved TSS in comparison with the placebo group, and ceterizine appeared to be more efficacious than levocetirizine at week 8 and week 12. The PRQLQ score showed significant decreased both in cetirizine and levocetirizine group, but there was no statistic significant difference between both groups. The eosinophil proportion in a nasal smear significantly decreased among the cetirizine in comparison with the placebo group but there was no statistic significant in levocetirizine groups. Both cetirizine and levocetirizine showed significant improvement in nPEFR in comparison with the placebo group, and ceterizine appeared to be more efficacious than levocetirizine. The 12-week treatment program showed that cetirizine was more effectious than levocetirizine.

Topics: Cetirizine; Child; Female; Histamine H1 Antagonists, Non-Sedating; Humans; Male; Quality of Life; Rhinitis, Allergic, Perennial; Severity of Illness Index; Surveys and Questionnaires; Treatment Outcome

End-organ hyperreactivity is an important feature of the allergic airway. There are no data directly comparing the responsiveness to treatment of different nasal provocation tests (NPT).. We compared the effect of levocetirizine on nasal adenosine 5'-monophosphate (AMP) with specific allergen challenge in patients with intermittent and persistent allergic rhinitis (AR).. Patients with AR were randomized in double-blind cross-over fashion to receive single doses of levocetirizine 5 mg or identical placebo, with nasal challenge performed 12 h after dosing. Sixteen participants completed per protocol. Nasal AMP or allergen challenge was conducted on separate days with 1- and 2-week washout periods in between, respectively. Measurements of peak nasal inspiratory flow (PNIF) were made over 60 min after each challenge. The primary end-point was the provocative concentration of AMP or allergen causing a 20% drop in the PNIF (PC(20)).. The time-profile for PNIF recovery [area under the 60 min time-response curve as % PNIF change (min)] were significantly attenuated for AMP challenge, as mean difference [95% confidence interval (CI)]: 11.57 (3.87, 19.25), P=0.005 and for allergen challenge: 17.82 (0.11, 35.53), P=0.04. A highly significant correlation was shown between methods for the area under the curve: (R=0.86, P<0.001). A statistically significant correlation was also seen for the PC(20): (R=0.94, P<0.001). PC(20) improvement amounted to a 1.26 (95% CI 0.16, 2.35) and 0.16 (95% CI -0.41, 0.73) doubling-dilution shifts for allergen and AMP challenges, respectively. Bland-Altman plots confirmed good agreement between methods.. A high correlation and statistical agreement has been demonstrated between AMP and allergen challenge for all outcome measures. In particular, the recovery profile after NPT is a sensitive and discriminatory measure of anti-allergic treatment.

Topics: Adenosine Monophosphate; Adult; Aged; Allergens; Area Under Curve; Cetirizine; Cross-Over Studies; Double-Blind Method; Female; Humans; Male; Middle Aged; Nasal Provocation Tests; Nose; Rhinitis, Allergic, Perennial; Rhinitis, Allergic, Seasonal; Treatment Outcome; Young Adult

Allergic rhinitis is a high-prevalence disease that affects quality of life (QOL), sleep quality and productivity of patients. According to the ARIA initiative, it is classified as intermittent and persistent, the latter being the most troublesome.. The aim of this randomized, open-label, 6-month, pilot study was to determine whether levocetirizine 5 mg administered continuously once daily in the morning was better than levocetirizine 5 mg on-demand in symptomatic subjects with persistent allergic rhinitis. Total and individual symptom scores were recorded in a diary card throughout the study. QOL, quality of sleep, nasal cytology, rate of drug intake, and safety were also assessed at pre-defined time-points.. In all, adult patients (31 in each group) were enrolled, of whom 22 dropped out. Both treatment regimens considerably decreased the total and individual symptoms scores from baseline and achieved similar levels up to week 14. Continuous treatment was generally better than on-demand from week 15 onwards, reaching statistical significance from weeks 17 to 21 (from week 19 to 21 for nasal pruritus). Both regimens substantially improved QOL and sleep quality. Both treatments were well tolerated, although the on-demand group reported more adverse events.. The present open label study in 62 patients indicates that levocetirizine 5 mg reliably controls persistent rhinitis over a period of 6 months, and shows a trend to be more effective in controlling the symptoms of rhinitis, improving QOL and decreasing nasal inflammation, when administered as long-term continuous therapy rather than as on-demand therapy.

Topics: Adult; Aged; Cetirizine; Female; Histamine H1 Antagonists, Non-Sedating; Humans; Inflammation; Male; Middle Aged; Pilot Projects; Quality of Life; Rhinitis, Allergic, Perennial; Time Factors

Persistent allergic rhinitis often impairs quality of life.. We assessed the extent to which treating persistent allergic rhinitis with montelukast, desloratadine, and levocetirizine alone or in combination improved quality of life.. A 32-week randomized, double-blind, placebo-controlled, crossover study was performed in 2 arms: 20 patients received montelukast 10 mg/d and/or desloratadine 5 mg/d or placebo; 20 patients received montelukast 10 mg/d and/or levocetirizine 5 mg/d or placebo. The treatment periods were separated by 2-week washout periods. Quality of life was assessed on the day before starting treatment and on the last day of each treatment period using the Rhinoconjunctivitis Quality of Life Questionnaire. Sleep problems were also assessed.. In the desloratadine plus montelukast arm, the mean (SEM) quality of life score before treatment was 3.1 (0.41). After placebo, this score was 2.16 (0.43), after desloratadine it was 1.79 (0.38), after montelukast it was 1.48 (0.37), and after montelukast plus desloratadine it was 1.59 (0.37). In the montelukast plus levocetirizine arm, the mean quality of life score before treatment was 2.58 (0.49). After placebo it was 1.78 (0.46), after levocetirizine it was 1.38 (0.42), after montelukast it was 1.36 (0.37), and after montelukast plus levocetirizine it was 1.26 (0.39).. Placebo, montelukast, desloratadine and levocetirizine significantly improved quality of life. Combining montelukast with either levocetirizine or desloratadine gave additional benefits in comparison to each agent alone and could be considered for patients whose quality of life is impaired by persistent allergic rhinitis.

Topics: Acetates; Adolescent; Adult; Aged; Cetirizine; Chronic Disease; Cross-Over Studies; Cyclopropanes; Double-Blind Method; Drug Interactions; Female; Histamine H1 Antagonists, Non-Sedating; Humans; Leukotriene Antagonists; Loratadine; Male; Middle Aged; Quality of Life; Quinolines; Rhinitis, Allergic, Perennial; Rhinitis, Allergic, Seasonal; Sulfides; Treatment Outcome

Allergic rhinitis is a chronic respiratory disorder with a detrimental impact on health-related quality of life (HRQOL) and health status. Enhancement and maintenance of patient function and well-being are therefore considered as essential.. To determine whether long-term treatment with levocetirizine 5mg improves HRQOL and health status in persistent allergic rhinitis (PER) patients assessed with RQLQ and SF-36 scales over a 6-month period.. The Xyzal in PER Trial (XPERT) was a multi-center, double-blind, parallel-group study. A total of 551 patients were randomized to receive levocetirizine 5mg or placebo once daily for 6 months and assessed for symptoms, HRQOL (Rhinoconjunctivitis Quality of Life Questionnaire: RQLQ) and health status (SF-36). Sensitivity of the RQLQ and SF-36 to disease severity was tested to ensure their suitability for use in PER patients. Treatment effect was assessed by means of repeated measures analyses.. Over the 6-month treatment period, levocetirizine showed statistically significant improvements over placebo in HRQOL (P < 0.001 for all RQLQ domains and overall scores) and health status (P < or = 0.004 for SF-36 physical and mental summary scores; P < 0.05 for all SF-36 scales). The relative improvement of levocetirizine over placebo exceeded the predefined clinically meaningful threshold of 30% for all RQLQ scores and the improvement from baseline was 3 times the established MID for RQLQ.. The RQLQ and SF-36 could be used to measure HRQOL and health status in PER patients. Long-term treatment with levocetirizine provides sustained improvement of HRQOL and reduces disease burden in PER patients.

Topics: Cetirizine; Double-Blind Method; Health Status; Histamine H1 Antagonists, Non-Sedating; Humans; Piperazines; Quality of Life; Rhinitis, Allergic, Perennial; Surveys and Questionnaires; Treatment Outcome

Background Levocetirizine (LCZ) has been shown to be effective in allergic rhinitis. We evaluated its clinical efficacy, antinflammatory actions and its effects on quality of life (QoL) with a specific instrument in the asthma-rhinitis comorbidity. Methods Fifty adult patients with persistent rhinitis with/without asthma were enrolled. After a 1-week run-in for baseline evaluation, they were randomized to LCZ or placebo for 8 weeks. Cromolyn and salbutamol were permitted on demand. Rhinoconjunctivitis and asthma symptoms were evaluated by diary cards. QoL was assessed by the specific Rhinasthma questionnaire and the generic SF-36 at different time-points. Nasal scrapings and lavages were also performed for inflammatory cell count and mediator assessment. Results Ten patients dropped out for unrelated reasons and the remaining completed the study with no side-effect. Symptoms began to decrease in the active group at the second week of treatment when the difference with the placebo group became significant (0.05) and so remained until the end of the trial. Starting from 2 weeks of therapy, there was a significant decrease vs. baseline in all the four components of the Rhinasthma questionnaire only in the active group. The intergroup comparison became significant (P<0.05) at 4 weeks. The SF-36 detected only sporadic differences between groups. Eosinophils and neutrophils in nasal scraping were significantly decreased in the LCZ group vs. baseline at all times. Nasal mediators were under the detection limits and no analysis could be performed. In the active group, only two patients used rescue medications compared with 13 patients in the placebo group. Conclusions LCZ is clinically effective and capable of improving the rhinitis-asthma-related QoL.

Topics: Adolescent; Adult; Asthma; Cetirizine; Conjunctivitis, Allergic; Double-Blind Method; Eosinophils; Female; Histamine H1 Antagonists, Non-Sedating; Humans; Male; Middle Aged; Neutrophils; Piperazines; Quality of Life; Rhinitis, Allergic, Perennial; Tablets; Treatment Outcome

Montelukast sodium is approved as a treatment for intermittent and persistent allergic rhinitis (AR), but it has not been evaluated as combined therapy with antihistamines for persistent AR.. To investigate the effects of 6 weeks of treatment of persistent AR with desloratadine, levocetirizine, or montelukast alone or in combination.. A randomized, double-blind, placebo-controlled crossover study was performed. Patients were assigned to 2 arms: 20 received montelukast, 10 mg/d, desloratadine, 5 mg/d, or both or placebo and 20 received montelukast, levocetirizine, or both, 5 mg/d, or placebo. The treatment periods were separated by 2-week washout periods. Symptom scoring, skin prick tests, spirometry, rhinometry, and nasal lavage were performed the day before and the last days of the treatment periods. Eosinophil cationic protein levels were evaluated by means of nasal lavage.. The mean +/- SD total baseline nasal symptom score was 7.7 +/- 0.49 before treatment, 3.74 +/- 0.54 after desloratadine use, 3.6 +/- 0.48 after montelukast use, and 3.04 +/- 0.4 after montelukast-desloratadine use. The mean +/- SD baseline nasal symptom score was 7.95 +/- 0.68 before treatment, 3.02 +/- 0.64 after levocetirizine use, 3.44 +/- 0.55 after montelukast use, and 2.14 +/- 0.39 after montelukast-levocetirizine use. The greatest improvement in nasal symptoms occurred after combination treatment. Decreases in the level of eosinophil cationic protein were greater after the combined use of montelukast and antihistamine than after each agent given alone.. For persistent AR, the combination of montelukast and either desloratadine or levocetirizine is more effective than monotherapy with these agents.

Topics: Acetates; Adolescent; Adult; Aged; Anti-Asthmatic Agents; Cetirizine; Cross-Over Studies; Cyclopropanes; Double-Blind Method; Drug Therapy, Combination; Eosinophil Cationic Protein; Female; Histamine H1 Antagonists, Non-Sedating; Humans; Loratadine; Male; Middle Aged; Nasal Lavage Fluid; Piperazines; Quinolines; Rhinitis, Allergic, Perennial; Rhinometry, Acoustic; Sulfides; Treatment Outcome

Nasal obstruction is the main symptom in patients with persistent allergic rhinitis. Some antihistamines have been demonstrated to be capable of improving this symptom. The aim of this pilot study was to evaluate nasal symptoms, nasal airflow, and decongestent activity in patients with persistent allergic rhinitis, before and after treatment with levocetirizine or placebo.. Forty patients with persistent allergic rhinitis were evaluated, 35 males and 5 females (mean age 23.3 +/- 5.9 years). All of them received levocetirizine (5 mg/daily) or placebo for 4 weeks. The study was double-blind, parallel-group, placebo-controlled, and randomized. Total symptom score (including: nasal itching, sneezing, rhinorrhea, and nasal obstruction) was assessed before and after treatment. Rhinomanometry and decongestion test were performed in all subjects before and after treatment.. Levocetirizine treatment induced: significant symptom relief (p<0.001), improved nasal airflow (p<0.001), reduction of reversibility percentage (p<0.05), and increase of total airflow after decongestion test (p<0.03). Placebo did not improve nasal symptoms and airflow.. This pilot study demonstrates the effectiveness of levocetirizine in: i) relieving nasal symptoms, including obstruction, ii) improving nasal airflow, and iii) exerting decongestant activity. Thus, these findings are the first evidence of the impact on airflow and the decongestant activity exerted by levocetirizine in persistent allergic rhinitis.

Topics: Adolescent; Adult; Cetirizine; Double-Blind Method; Female; Histamine H1 Antagonists, Non-Sedating; Humans; Male; Naphazoline; Nasal Obstruction; Pilot Projects; Piperazines; Pruritus; Rhinitis, Allergic, Perennial; Rhinomanometry; Skin Tests

Allergic rhinitis was recently classified by the ARIA guidelines as persistent or intermittent. Levocetirizine was shown to improve symptoms and health-related quality of life of patients with persistent allergic rhinitis in the XPERT study, a 6-month randomized double blind placebo-controlled trial.. To assess the total costs of persistent allergic rhinitis, and the effect of long-term treatment with levocetirizine on these costs from several perspectives (societal, social security system, and employers).. Direct medical cost parameters (medications, physician visits and hospitalizations) and time lost parameters (workdays and Usual Daily Activities (UDA) lost) related to persistent allergic rhinitis and its comorbidities (asthma, sinusitis, otitis and upper respiratory infection) were measured. A cost analysis was performed using 2002 French costing data.. From a societal perspective, the total cost of persistent allergic rhinitis without long-term treatment was estimated at 355.06/patient/month. From a social security perspective, levocetirizine treatment yielded an additional cost of 2.78/patient/month, compared to no-treatment. However, levocetirizine reduced the total cost of persistent allergic rhinitis and its comorbidities by 152.93/patient/month from a societal perspective and by 64.70/patient/month from an employer perspective. Most gains resulted from a decrease in the lost workdays and UDA in the levocetirizine group.. The cost of persistent allergic rhinitis is substantial. Treatment with levocetirizine reduces the cost of persistent allergic rhinitis and its comorbidities to the society by 152.93/patient/month while improving symptoms and health-related quality of life.

Topics: Cetirizine; Cost of Illness; Costs and Cost Analysis; Europe; Histamine H1 Antagonists, Non-Sedating; Humans; Piperazines; Quality of Life; Rhinitis, Allergic, Perennial

This randomized study examined the efficacy and safety of levocetirizine in pediatric patients with perennial allergic rhinitis. Health-related quality of life (HRQL) was also investigated, which is particularly relevant in children because of the effects of rhinitis on learning, social activities, and comorbidity.. To evaluate the effect of levocetirizine on the Total 4 Symptoms Score, the 50% response rate, the Pediatric Rhinitis Quality of Life Questionnaire (PRQLQ), and investigators' global evaluation of symptom improvement.. Double-blind, placebo-controlled, randomized, multicenter trial of levocetirizine, 5 mg once daily for 4 weeks, in 306 children with perennial allergic rhinitis aged 6 to 12 years. There were 154 children in the levocetirizine arm and 152 in the placebo group who completed daily diary cards, and the PRQLQ and investigators' global evaluations were conducted at 3 visits.. The levocetirizine group showed a significant improvement in 2-week and 4-week Total 4 Symptoms Score compared with placebo (P = .001 and P = .008, respectively). The 50% response rate for the first 2 weeks was 12.3% for the levocetirizine group compared with 3.9% for the placebo group (P = .01). The investigators' global evaluation also favored levocetirizine, because 57.1% of the children in the levocetirizine group were considered markedly or moderately improved compared with 44.7% in the placebo group. Levocetirizine also provided a significantly greater HRQL improvement than placebo at 2 weeks (P = .01), and the frequency of adverse events did not differ significantly from those seen in the placebo group.. The study confirmed the efficacy of levocetirizine in relieving symptoms of perennial allergic rhinitis in children between 6 and 12 years of age. A HRQL benefit greater than placebo was shown. The treatment was well tolerated.

Topics: Cetirizine; Child; Double-Blind Method; Female; Histamine H1 Antagonists, Non-Sedating; Humans; Male; Piperazines; Quality of Life; Rhinitis, Allergic, Perennial

Nasal obstruction is the main symptom in patients with perennial allergic rhinitis. Some new antihistamines have been demonstrated to be capable of improving this symptom.. The aim of this pilot study was to evaluate nasal symptoms, nasal airflow, eosinophils, and IL-4 in patients with perennial allergic rhinitis, before and after treatment with two new antihistamines: desloratadine and levocetirizine.. Thirty patients with perennial allergic rhinitis were evaluated, 26 males and 4 females (mean age 26+/-7.1 years). All of them received either desloratadine (5 mg/daily) or levocetirizine (5 mg/daily) or placebo for 4 weeks. The study was double-blind, parallel-group, placebo-controlled, and randomized. Total symptom score (including: rhinorrhea, nasal itching, sneezing, and nasal obstruction) was assessed before and after treatment. Rhinomanometry and decongestion test, nasal lavage, and nasal scraping were performed in all subjects before and after treatment. Eosinophils were counted by conventional staining; IL-4 was measured by immunoassay of fluids recovered from nasal lavage.. Desloratadine and levocetirizine treatment induced significant symptom relief and significant reduction of IL-4. Both antihistamines significantly affected all parameters in comparison with placebo.. This pilot study demonstrates the effectiveness of antihistaminic treatment in: i) relieving nasal symptoms, including obstruction, ii) improving nasal airflow, iii) exerting decongestant activity, iv) reducing eosinophil infiltration, and v) diminishing IL-4 levels.

Topics: Adolescent; Adult; Cetirizine; Double-Blind Method; Eosinophils; Female; Histamine H1 Antagonists, Non-Sedating; Humans; Inflammation; Interleukin-4; Leukocyte Count; Loratadine; Male; Nasal Lavage Fluid; Nasal Mucosa; Nasal Obstruction; Pilot Projects; Piperazines; Rhinitis, Allergic, Perennial; Rhinomanometry

Summary Background There are no data directly comparing the relative efficacy of modern H(1)-antihistamines in allergic rhinitis using nasal provocation challenge. Objective We elected to study the comparative effectiveness of usual clinically recommended doses of desloratadine (DES), fexofenadine (FEX), and levocetirizine (LEV), on nasal adenosine monophosphate (AMP) challenge in patients with perennial allergic rhinitis (PAR). Methods 16 patients with PAR were randomized in double-blind cross-over fashion to receive single doses of DES 5 mg, FEX 180 mg, LEV 5 mg, or placebo (PL), with nasal AMP challenge performed 12 h after dosing. Measurements of peak nasal inspiratory flow (PNIF) were made over 60 min after nasal AMP challenge. Results Pre-challenge values (mean+/-SEM) for PNIF (L/min) were not significantly different comparing all groups; DES (129+/-9), FEX (128+/-11), LEV (128+/-13), and PL (128+/-12). The maximum % PNIF fall from baseline over 60 min after nasal AMP challenge was significantly attenuated (P<0.05) compared to PL (50+/-4), with DES (32+/-5), FEX (36+/-4), and LEV (36+/-4). The area under the 60-min time-response curve (%.min) was also significantly attenuated (P<0.05) compared to PL (2110+/-268), with DES (1126+/-285), FEX (1225+/-255), and LEV (1261+/-194). There were no significant differences between the three H(1)-antihistamines for any outcomes. Conclusion DES, FEX, and LEV were equally effective in attenuating the response to nasal AMP challenge. However, further long-term studies will be required to study their comparative effects on nasal symptoms, quality of life, as well as on nasal inflammatory cells.

Topics: Adenosine Monophosphate; Adult; Aged; Aged, 80 and over; Anti-Allergic Agents; Cetirizine; Cross-Over Studies; Double-Blind Method; Female; Histamine H1 Antagonists; Humans; Loratadine; Male; Middle Aged; Nasal Provocation Tests; Piperazines; Rhinitis, Allergic, Perennial; Terfenadine; Treatment Outcome

The Vienna Challenge Chamber (VCC) is an established method for the controlled exposure of patients to specific allergens, used to make valid comparisons between antihistamines. The aim of the significantly more than loratadine at all time two placebo-controlled, randomised studies reported here was to compare the efficacy and safety of levocetirizine 5 mg od and loratadine 10 mg od in subjects suffering from seasonal allergic rhinitis (SAR) or perennial allergic rhinitis (PAR).. During each study period, SAR and PAR subjects were exposed to grass pollen or house-dust mite allergens, respectively for 6 h on 2 consecutive days in the VCC. Each day, medications were administered 2 h after the start of the challenge; with a washout of at least 5 days between each period. The main criterion for evaluation of efficacy was the major symptom complex (MSC) for SAR and the complex symptom score (CSS) for PAR.. The pattern of patients' response was similar in SAR and PAR. Both levocetirizine and loratadine were superior to placebo in alleviating SAR and PAR symptoms at all time intervals evaluated during the two study days. Levocetirizine decreased the mean MSC score intervals in SAR subjects, with the most marked difference observed on day 2 (p = 0.002). In PAR patients, although with borderline significance (p = 0.08), levocetirizine decreased the mean CSS more than loratadine. Levocetirizine appeared to have a faster onset of action than loratadine in SAR (45 min versus 1 h 15 min) and PAR (1 h versus 1 h 30 min). However, these apparent differences were not tested for statistical significance. Both medications were well tolerated and no treatment-related adverse events were reported. This level of antihistamine efficacy was maintained regardless of whether the subjects' rhinitis was seasonal or perennial.. This study demonstrated that levocetirizine is superior to loratadine in improving symptoms in SAR and that there is a similar trend in PAR.

Topics: Cetirizine; Cross-Over Studies; Double-Blind Method; Environmental Exposure; Female; Histamine H1 Antagonists, Non-Sedating; Humans; Loratadine; Male; Piperazines; Placebos; Rhinitis, Allergic, Perennial; Rhinitis, Allergic, Seasonal; Seasons; Treatment Outcome

Antihistamines are the cornerstone of treatment for many allergic diseases, such as allergic rhinitis and chronic urticaria. Since the discovery of their beneficial effects in the 1940s, scientists have found molecules with greater selectivity to block specific histamine receptors without some of the detrimental side effects that are seen if antihistamines cross the blood-brain barrier. Levocetirizine is the active enantiomer of cetirizine and a selective H(1)-histamine blocker. It exhibits many favourable characteristics of an ideal antihistamine, both pharmacodynamically and pharmacokinetically, including high bioavailability, rapid onset of action, limited distribution and low degree of metabolism. Furthermore, clinical trials indicate that it is safe and effective for the treatment of allergic rhinitis and chronic urticaria with a minimal amount of untoward effects.

Topics: Allergy and Immunology; Cetirizine; Chronic Disease; Clinical Trials, Phase III as Topic; Double-Blind Method; Histamine H1 Antagonists, Non-Sedating; Humans; Multicenter Studies as Topic; Piperazines; Randomized Controlled Trials as Topic; Rhinitis, Allergic, Perennial; Rhinitis, Allergic, Seasonal; Stereoisomerism; Urticaria

Allergic Rhinitis and its Impact on Asthma in collaboration with the World Health Organization initiative reclassified allergic rhinitis, like asthma, by duration and severity. The Xyzal in Persistent Rhinitis Trial is the first large, long-term clinical trial studying patients with persistent rhinitis as defined by Allergic Rhinitis and its Impact on Asthma.. Two primary objectives were defined: comparison of the Rhinoconjunctivitis Quality of Life Questionnaire overall score and Total 5 Symptoms Score (rhinorrhea, sneezing, nasal congestion, and nasal and ocular pruritus) over a period of 4 weeks between levocetirizine 5 mg and placebo. Secondary endpoints included similar evaluations at 1 week and 3, 4.5, and 6 months, summary scores for a general health status questionnaire (Medical Outcomes Survey Short Form 36), a pharmacoeconomic assessment, comorbidities, and a safety evaluation.. The Xyzal in Persistent Rhinitis Trial was a 6-month double-blind, placebo-controlled, multicenter, multinational trial in 551 patients. Adults with persistent rhinitis sensitized to both grass pollen and house dust mite were randomized to receive levocetirizine 5 mg/d or placebo.. A total of 421 patients completed the full study. Levocetirizine significantly improved both the Rhinoconjunctivitis Quality of Life Questionnaire overall score and the Total 5 Symptoms Score from week 1 to 6 months (all P values <.001). Medical Outcomes Survey Short Form 36 summary scores were also improved in the levocetirizine group compared with the placebo group. Treatment cessation because of lack of effect, comorbidities, and overall costs of disease, and comorbidities per working patient per month (160.27 vs 108.18) were lower in the levocetirizine group.. Levocetirizine was shown to improve quality of life and symptoms and to decrease the overall costs of the disease over the 6-month treatment period.

Topics: Adolescent; Adult; Aged; Cetirizine; Conjunctivitis, Allergic; Costs and Cost Analysis; Double-Blind Method; Europe; Female; Histamine H1 Antagonists, Non-Sedating; Humans; Male; Middle Aged; Piperazines; Quality of Life; Rhinitis, Allergic, Perennial; Rhinitis, Allergic, Seasonal; Treatment Outcome

Allergic rhinitis (AR) and chronic idiopathic urticaria (CIU) are highly burdensome diseases, which are increasing in prevalence, especially in the paediatric population. Despite the availability of a large number of medications for treatment of AR and CIU, their use in children has primarily been based on data obtained from a limited number of clinical trials in children and/or testing in adults. The H(1)-antihistamines have traditionally been used as first-line treatment for the relief of both AR and CIU symptoms in children. The first-generation H(1)-antihistamines are associated with marked adverse effects such as sedation, sleepiness/drowsiness as well as difficulties in learning and cognitive processing; thus, they are recommended for limited or discontinued use in children with AR or CIU. In contrast, second-generation H(1)-antihistamines are more adapted for the use in children with AR and CIU due to better safety profiles. However, only a limited number of trials with these agents have been conducted and generally, data from well-designed trials in children are lacking. Levocetirizine is one of the most extensively investigated H(1)-antihistamines for its pharmacologic properties, safety, efficacy as well as overall global satisfaction in children aged 2-12 years. Levocetirizine is the only H(1)-antihistamine launched in the 21st century shown to lack clinically relevant adverse effects on physical and psychomotor development or routine laboratory tests over a long-term period of 18 months in 1- to 3-year-old children predisposed to development of allergic disease. Available data suggest that levocetirizine is a suitable treatment option for AR and CIU in children aged 6 months to 12 years.

Topics: Adult; Anti-Allergic Agents; Attitude of Health Personnel; Cetirizine; Child; Child, Preschool; Chronic Disease; Histamine H1 Antagonists, Non-Sedating; Humans; Infant; Parents; Physicians; Randomized Controlled Trials as Topic; Rhinitis, Allergic, Perennial; Rhinitis, Allergic, Seasonal; Treatment Outcome; Urticaria

Topics: Adult; Cetirizine; Histamine H1 Antagonists, Non-Sedating; Humans; Iridocyclitis; Male; Rhinitis, Allergic, Perennial

Allergic rhinitis (AR) affects a large percentage of paediatric patients. With the wide array of available agents, it has become a challenge to choose the most appropriate treatment for patients. Second-generation antihistamines have become increasingly popular because of their comparable efficacy and lower incidence of adverse effects relative to their first-generation counterparts, and the safety and efficacy of this drug class are established in the adult population. Data on the use of the second-generation antihistamines oral cetirizine, levocetirizine, loratadine, desloratadine and fexofenadine, and the leukotriene receptor antagonist montelukast as well as azelastine nasal spray in infants and children are evaluated in this review. These agents have been found to be relatively safe and effective in reducing symptoms associated with AR in children. Alternative dosage forms such as liquids or oral disintegrating tablets are available for most agents, allowing ease of administration to most young children and infants; however, limited data are available regarding use in infants for most agents, except desloratadine, cetirizine and montelukast. Unlike their predecessors, such as astemizole and terfenadine, the newer second-generation antihistamines and montelukast appear to be well tolerated, with absence of cardiotoxicities. Comparative studies are limited to cetirizine versus ketotifen, oxatomide and/or montelukast. Although second-generation antihistamines and montelukast are deemed relatively safe for use in paediatric patients, there are some noteworthy drug interactions to consider when selecting an agent. Given the wide variety of available agents for treatment of AR in paediatric patients, the safety and efficacy data available for specific age groups, type of AR, dosage form availability and cost should be considered when selecting treatment for AR in infants and children.

Topics: Acetates; Administration, Oral; Adult; Anti-Allergic Agents; Anti-Asthmatic Agents; Astemizole; Cetirizine; Child; Cyclopropanes; Drug Administration Schedule; Drug Interactions; Histamine H1 Antagonists, Non-Sedating; Humans; Ketotifen; Leukotriene Antagonists; Loratadine; Piperazines; Quinolines; Rhinitis, Allergic, Perennial; Rhinitis, Allergic, Seasonal; Safety; Sulfides; Tablets; Terfenadine; Treatment Outcome

Allergic rhinitis is the most common allergic disease worldwide and affects about 18% to 40% of the general population. Anti-allergic medicines (eg, some antihistamines) can cause adverse events such as somnolence and can have an additional negative impact on quality of life. Combining montelukast with levocetirizine gives additional benefits in comparison with either drug alone and could be considered for patients whose quality of life is impaired by persistent allergic rhinitis. Montelukast sodium is alkaline, stable and levocetirizine dihydrochloride is acid stable, when we prepare a matrix tablet, both the drugs would be in contact and make it unstable during the shelf life of the formulation. Hence it is recommended to prepare bilayer tablet, as it improves and increases the stability of both the drugs in combination. Bilayer tablet of montelukast with levocetirizine is more stable with respect to stability studies, in comparison to matrix tablet.

Topics: Acetates; Cetirizine; Cyclopropanes; Drug Combinations; Histamine H1 Antagonists, Non-Sedating; Humans; Leukotriene Antagonists; Quality of Life; Quinolines; Rhinitis, Allergic, Perennial; Sulfides; Tablets; Treatment Outcome

Topics: Cetirizine; Chronic Disease; Clinical Trials as Topic; Histamine H1 Antagonists, Non-Sedating; Humans; Piperazines; Rhinitis, Allergic, Perennial; Rhinitis, Allergic, Seasonal; Urticaria

Topics: Cetirizine; Histamine H1 Antagonists; Humans; Piperazines; Rhinitis, Allergic, Perennial; Rhinitis, Allergic, Seasonal; Urticaria

Topics: Absenteeism; Cetirizine; Clinical Trials as Topic; Dose-Response Relationship, Drug; Histamine H1 Antagonists, Non-Sedating; Humans; Piperazines; Quality of Life; Rhinitis, Allergic, Perennial; Rhinitis, Allergic, Seasonal; Urticaria

Topics: Cetirizine; Histamine H1 Antagonists, Non-Sedating; Humans; Loratadine; Nasal Obstruction; Nasal Provocation Tests; Piperazines; Rhinitis, Allergic, Perennial