levocetirizine and Rhinitis--Allergic--Seasonal

Despite a plethora of published data on levocetirizine, no meta-analyses exist on the effect of study design, and covariates like age, gender, and baseline symptom severity on treatment response. The objective of this study was the efficacy of levocetirizine 5  mg tablets and matching placebo at reducing allergy symptoms in adult subjects with seasonal allergic rhinitis under various pollen exposure study conditions and by age, gender and baseline symptom severity.. This was a meta-analysis of original reports from randomized, double-blind, placebo-controlled studies. Clinical studies without detailed reports, open-label, non-randomized and non-controlled studies, or paediatric studies, were excluded. Study subjects were divided into an environmental exposure (EE) group or a natural exposure (NE) group.. Data from 3640 subjects were analysed (n = 2174 for levocetirizine, n = 1466 for placebo). The overall results confirmed the efficacy of levocetirizine 5  mg, with an approximately 40% symptom score improvement from baseline, in both the EE and NE groups. While levocetirizine showed no gender- or age-related differences in efficacy, female subjects responded better to placebo in the EE, but not in the NE group; younger subjects (<30 years of age) responded less favourably to placebo compared with older subjects (≥ 50 years of age). Levocetirizine was consistently superior to placebo regardless of baseline symptom score levels. The highest significance levels between the active and placebo groups were observed in subjects sensitized to animal dander and grass.. Differences between an oral antihistamine and placebo in clinical studies of allergic rhinitis might be due to a different response to placebo rather than to the active drug. Levocetirizine seems to have consistent efficacy regardless of age, gender, and baseline scores.

Topics: Adult; Aged; Bronchial Provocation Tests; Cetirizine; Double-Blind Method; Environmental Exposure; Female; Histamine H1 Antagonists, Non-Sedating; Humans; Male; Middle Aged; Placebo Effect; Pollen; Randomized Controlled Trials as Topic; Rhinitis, Allergic, Seasonal

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

Nasal congestion is the most troublesome symptom of allergic rhinitis (AR). First-generation and older second-generation antihistamines, while effective against nasal itching, sneezing, and rhinorrhea, have limited efficacy in relieving nasal congestion.. This review included nasal challenge studies and clinical trials that reported the effects on nasal congestion of the newer second-generation antihistamines desloratadine, fexofenadine, and levocetirizine.. MEDLINE and EMBASE were searched for nasal challenge studies and clinical trials published in English between January 1, 1991, and January 31, 2009, using the following terms, alone or in combination: antihistamines, second-generation antihistamines, allergic rhinitis, intermittent allergic rhinitis, perennial allergic rhinitis, persistent allergic rhinitis, seasonal allergic rhinitis, nasal challenge, nasal blockage, and nasal congestion. Studies that were not active or placebo controlled, that did not evaluate change in nasal congestion scores, or that focused on treatments other than desloratadine, fexofenadine, and levocetirizine for nasal congestion associated with AR were excluded.. Twenty-six clinical trials met the criteria for inclusion in the review. In 11 placebo-controlled trials that included objective assessment of nasal congestion, desloratadine, fexofenadine, and levocetirizine were associated with reductions in the severity of nasal congestion through maintenance of nasal airflow. The mean AUC for nasal airflow over 6 hours was significantly greater with desloratadine compared with placebo in 3 studies (P < 0.05); placebo-controlled trials of fexofenadine and levocetirizine had similar results. In 25 placebo- and active-controlled trials that reported subject-rated symptom scores, the 3 newer antihistamines were efficacious in the treatment of nasal congestion associated with AR. In 10 trials that reported objective and/or subjective measures, desloratadine was associated with significant improvements in nasal congestion compared with placebo (P < or = 0.05), beginning as early as the first 2 hours after allergen challenge. Fexofenadine was associated with significantly lower nasal congestion scores compared with placebo in 4 studies (P <- 0.05); nasal congestion scores were significantly reduced with levocetirizine in 3 placebo-controlled trials (P < or = 0.005).. In the studies reviewed, desloratadine, fexofenadine, and levocetirizine were effective in relieving the nasal congestion associated with AR compared with placebo. This effect began as early as day 2 and was consistent and progressive throughout treatment. Desloratadine, fexofenadine, and levocetirizine are appropriate options for the treatment of nasal congestion in patients with AR.

Topics: Adolescent; Adult; Aged; Aged, 80 and over; Cetirizine; Child; Clinical Trials as Topic; Female; Histamine H1 Antagonists, Non-Sedating; Humans; Loratadine; Male; Middle Aged; Nasal Obstruction; Rhinitis, Allergic, Seasonal; Terfenadine; Treatment Outcome; Young Adult

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

Topics: Cetirizine; Histamine H1 Antagonists, Non-Sedating; Humans; Loratadine; Piperazines; Retrospective Studies; Rhinitis, Allergic, Seasonal; Treatment Outcome

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

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

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

No comparative study of antihistamines that differ in structural system has been conducted in allergic rhinitis.. This was a randomized, double-blind, crossover comparative study to verify the efficacy of antihistamines that differ in structural system.. A total of 50 patients with moderate or more severe Japanese cedar pollen-induced allergic rhinitis were randomized to receive either placebo, desloratadine 5 mg (a tricyclic), or levocetirizine 5 mg (a piperazine). One dose of the study drug was orally administered at 9 pm on the day before a pollen exposure test, which was performed for 3 h (9 a.m. to 12 p.m.) to assess symptoms in an environmental challenge chamber (ECC). Nasal and ocular symptoms were compared at an airborne pollen level of 8,000 grains/m3. The primary endpoint was mean total nasal symptom score (TNSS) from 120 to 180 min in the ECC. Subjects with a difference of ≥1 in TNSS between 2 drugs were extracted to the relevant drug-responsive group.. The difference in TNSS from placebo was -2.42 (p < 0.0001) with levocetirizine and -1.66 (p < 0.01) with desloratadine, showing that both drugs were significantly more effective than placebo in controlling symptoms, but with no statistically significant difference between the 2 drugs. There were 12 subjects in the desloratadine-responsive group and 24 subjects in the levocetirizine-responsive group, with no contributor to response was detected.. Levocetirizine tended to control nasal symptoms more effectively than desloratadine. However, the response to each antihistamine varied among individuals and the predictors to the response are unknown.. UMIN ID: UMIN000029653.

Topics: Adult; Cedrus; Cetirizine; Cross-Over Studies; Double-Blind Method; Female; Histamine H1 Antagonists, Non-Sedating; Humans; Loratadine; Male; Placebos; Pollen; Rhinitis, Allergic, Seasonal

The efficacy of prophylactic treatment before the start of pollen dispersal for prevention of aggravation of symptoms is unclear. The aim of the present study was to examine the efficacy of prophylactic treatment with an antihistamine for seasonal allergic rhinitis (SAR) using an environmental challenge chamber (ECC).. The study was performed in a randomized double-blind manner with a 3-way crossover design. The subjects were 50 patients with SAR caused by Japanese cedar pollen who were randomized for treatment with levocetirizine hydrochloride 5 mg (Xyzal®) or placebo as follows: administration of placebo for 8 days (treatment A), single administration of levocetirizine on day 8 after placebo for 7 days (treatment B) or administration of levocetirizine for 8 days (treatment C). Efficacy in each treatment arm was evaluated based on cedar pollen exposure for 3 h on day 9 in an ECC, following 1-hour exposure on day 8. The primary endpoint was the total nasal symptom score for 12 h on day 9. Other nasal and ocular symptoms were secondary endpoints.. The evaluation was performed in 45 subjects. The total nasal symptom score on day 9 was significantly lower with treatment B compared with treatment A. Treatment C did not show superior efficacy compared with treatment B.. Our results suggest that early intervention with levocetirizine soon after onset of symptoms may attenuate these symptoms as effectively as prophylactic treatment before pollen dispersal. These results are important from the perspective of patient convenience and reduction of medical costs.

Topics: Cetirizine; Double-Blind Method; Histamine Antagonists; Humans; Rhinitis, Allergic, Seasonal; Treatment Outcome

Persistent allergic rhinitis (PER) has a moderate impact on the sense of smell, but no controlled study has reported the effect of antihistamines on the loss of smell in patients with PER.. Patients with PER and subjective loss of the sense of smell (n = 27) were included in this pilot randomised, double-blind, placebo-controlled study. Nasal symptoms, nasal endoscopy, skin prick test, acoustic rhinometry, peak nasal inspiratory flow, nasal nitric oxide (nNO), and olfactometry (Barcelona Smell Test-24; BAST-24) were performed and evaluated in all PER patients at baseline and after 7 and 30 days of treatment with levocetirizine 5 mg or placebo.. The study population was randomized into two homogeneous groups: levocetirizine (n = 14) and placebo groups (n = 13). The evolution of symptoms reflected the therapeutic effect of levocetirizine treatment on rhinorrhea, nasal itching, eye itching, sneezing, and the total symptoms score after 7 and 30 days. Significant improvement in loss of smell by a visual analog scale (VAS) was observed after 7 days of levocetirizine treatment (7.2 ± 4.3; p < 0.05) compared to placebo (-9.4 ± 6.2). Improvement in smell identification by BAST-24 was strongly correlated (r = 0.72; p < 0.05) with smell improvement by VAS after 30 days. After 7 days of treatment with levocetirizine, the nNO values decreased (-494 ± 188) compared to placebo (155 ± 284 ppb; p < 0.05).. The CIRANO study suggests that levocetirizine is effective on PER symptoms, including a transient improvement in loss of smell, and that this improvement concurs more with reduction of nasal inflammation than of nasal patency.

Topics: Adult; Cetirizine; Double-Blind Method; Female; Histamine H1 Antagonists, Non-Sedating; Humans; Inflammation; Male; Nitric Oxide; Olfaction Disorders; Placebos; Rhinitis, Allergic, Seasonal; Smell

To evaluate the efficacy of levocetirizine 5 mg once daily in reducing seasonal allergic rhinitis (SAR) symptoms in US adults.. This multicenter, randomized, double-blind, placebo-controlled, parallel-group study enrolled adults aged 18 to 65 years with SAR symptoms in the spring in the US. After a single-blind placebo run-in period, subjects received levocetirizine 5 mg or placebo once daily over 14 days. ClinicalTrials.gov registry no.: NCT00621959.. Primary efficacy variable was the Total 5-Symptom Score (T5SS). Secondary variables included Rhinoconjunctivitis Quality of Life Questionnaire (RQLQ), Work Productivity and Activity Impairment-Allergy Specific (WPAI-AS) questionnaire, and Epworth Sleepiness Scale (ESS). Safety assessments were based on adverse events (AEs).. The intent-to-treat population comprised 596 subjects (levocetirizine, n = 301; placebo, n = 295). Comparison of mean T5SS over the total treatment period showed a nonsignificant between-group difference (levocetirizine, 8.90 +/- 0.19; placebo, 9.04 +/- 0.19; adjusted mean difference, -0.14; p = 0.546). Levocetirizine showed numerical (mean RQLQ, WPAI-AS, ESS) and statistically superior differences (two domains within WPAI-AS) compared with placebo upon analysis of secondary efficacy variables. The incidence of treatment-emergent AEs was similar (levocetirizine, 23.9%; placebo, 24.4%). As the lack of efficacy was inconsistent with all previous levocetirizine studies, post hoc analyses were performed to assess the influence of pollen counts, geography, and other factors; however, no conclusive explanation could be identified.. In this study, levocetirizine 5 mg QD was well tolerated but failed to show significant efficacy compared with placebo in a US adult population with SAR. This finding is inconsistent with all previous studies with levocetirizine and in contrast to a concurrently run, similarly designed US study. It reflects the importance of conducting duplicate studies as there is always a small but real risk of false negative results in clinical studies, irrespective of the methodologic quality.

Topics: Adolescent; Adult; Aged; Cetirizine; Double-Blind Method; Female; Histamine H1 Antagonists, Non-Sedating; Humans; Male; Middle Aged; Rhinitis, Allergic, Seasonal; Treatment Outcome; Young Adult

Levocetirizine, a second-generation antihistamine for symptomatic treatment of allergic rhinitis and chronic idiopathic urticaria, has not been previously studied in US patients.. To assess the efficacy and safety of levocetirizine in improving symptoms and health-related quality of life in US adults with seasonal allergic rhinitis (SAR).. This multicenter, double-blind trial randomized adults with SAR, sensitized to at least 1 grass allergen, to receive levocetirizine, 5 mg, or placebo once daily in the evening for 2 weeks. The primary end point was the 24-hour reflective Total 5-Symptom Score (T5SS; sum of rhinorrhea, sneezing, nasal congestion, and nasal and ocular pruritus) during the entire treatment period. Secondary assessments included the Rhinoconjunctivitis Quality of Life Questionnaire (RQLQ), Work Productivity and Activity Impairment-Allergy Specific (WPAI-AS) questionnaire, and Epworth Sleepiness Scale (ESS), each assessed at week 1, week 2, and the end of treatment.. The intent-to-treat population comprised 287 patients taking levocetirizine and 290 taking placebo, with no significant between-group differences at baseline. Levocetirizine resulted in significantly greater improvement from baseline vs placebo in the T5SS (P < .001), overall RQLQ score (P < .001), general and work-related WPAI-AS subscores (P < .05), and ESS score (P < .001). Overall incidence of treatment-emergent adverse events was 14.4% for levocetirizine and 18.4% for placebo. The incidence of somnolence and fatigue was 0.7% and 1.8% with levocetirizine and 1.0% and 0% with placebo, respectively.. Levocetirizine was well tolerated and was significantly more effective than placebo in improving the naso-ocular symptoms and health-related quality of life in US patients with SAR.

Topics: Adolescent; Adult; Aged; Cetirizine; Double-Blind Method; Female; Histamine H1 Antagonists, Non-Sedating; Humans; Male; Middle Aged; Placebos; Quality of Life; Rhinitis, Allergic, Seasonal; Treatment Outcome; United States

To determine the better agent among rupatadine fumarate and levocetirizine dihydrochloride for seasonal allergic rhinitis. Although treating and ensuring a decent quality of life to patients is challenging, an increasing understanding of pathomechanisms has revealed the potentiality of new-generation antihistamines in the treatment of seasonal allergic rhinitis.. A 2-week, single-center, randomized, open, parallel group comparative clinical study between rupatadine and levocetirizine in patients with seasonal allergic rhinitis.. A tertiary care center.. Following inclusion and exclusion criteria, 60 patients were assigned to either the rupatadine or levocetirizine group.. Two-week treatment with rupatadine or levocetirizine.. After 2 weeks, all postdrug symptoms were listed, baseline laboratory investigations (total and differential leukocyte count and IgE level) were repeated, and clinical improvement was assessed in terms of change in Total Nasal Symptom Score, Rhinoconjunctivitis Quality of Life Questionnaire score, and laboratory parameters.. Differential count (P = .01) and absolute eosinophil count (P = .009) was significantly lowered by both drugs, but rupatadine was found to be superior. In the rupatadine group there was a significantly higher reduction (P = .004) in IgE level and Total Nasal Symptom Score (P < .001) compared with the levocetirizine group. There was a decrease of 18.08% (P = .02) in Rhinoconjunctivitis Quality of Life Questionnaire score in the rupatadine group, which was significantly greater compared with the levocetirizine group. Incidence of adverse effects was less in the rupatadine group compared with the levocetirizine group.. Rupatadine is a better choice for seasonal allergic rhinitis compared with levocetirizine because of its better efficacy and safety profile.

Topics: Adolescent; Adult; Cetirizine; Conjunctivitis, Allergic; Cyproheptadine; Eosinophils; Female; Histamine H1 Antagonists, Non-Sedating; Humans; Immunoglobulin E; Leukocyte Count; Male; Quality of Life; Rhinitis, Allergic, Seasonal; Single-Blind Method; 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

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

To date, no adequate data are available on direct comparison of the efficacy of levocetirizine, a recently approved histamine1-antihistamine, with that of a leukotriene antagonist in the treatment of seasonal allergic rhinitis (SAR) symptoms.. To compare the efficacy of therapeutic doses of 5 mg of levocetirizine and 10 mg of montelukast in ragweed sensitized patients.. A randomized, double-blind, placebo-controlled, parallel-group study was conducted between July and October 2006. Symptomatic patients with SAR were exposed to ragweed pollen under controlled conditions in an environmental exposure chamber for 4 to 5 hours after treatment with 5 mg of levocetirizine, 10 mg of montelukast, or matched placebo on 2 consecutive days. The mean change from baseline in pollen-induced rhinitis symptoms, expressed as a major symptoms complex (MSC) score (sum of scores for rhinorrhea, itchy nose, sniffles, nose blows, sneezes, and watery eyes), in period 1 (first 5 hours after first drug intake) was the primary efficacy outcome.. A total of 611 patients were screened, of whom 403 were randomized to receive treatment (102 placebo, 152 levocetirizine, and 149 montelukast). The MSC score in period 1 was progressively decreased to a significantly greater extent in the levocetirizine group compared with the montelukast and placebo groups (adjusted mean differences, -2.18 [95% confidence interval, -3.35 to -1.01; P < .001] and -2.22 [95% confidence interval, -3.51 to -0.92; P < .001] for levocetirizine vs montelukast and vs placebo, respectively). The effect of 10 mg of montelukast was not significantly different compared with placebo. Levocetirizine also achieved a significantly faster onset of action within 2.5 hours of administration. Both products were well tolerated.. This study in an environmental exposure chamber confirms the therapeutic efficacy of 5 mg of levocetirizine in improving symptoms of SAR, which was superior to 10 mg of montelukast.

Topics: Abdominal Pain; Acetates; Adolescent; Adult; Aged; Ambrosia; Cetirizine; Cyclopropanes; Double-Blind Method; Exanthema; Female; Histamine H1 Antagonists, Non-Sedating; Humans; Leukotriene Antagonists; Male; Middle Aged; Patient Satisfaction; Quinolines; Rhinitis, Allergic, Seasonal; Sulfides; Time Factors; Treatment Outcome

Levocetirizine, a second generation non-sedating antihistamine that blocks the H(1) histamine receptor, may exhibit immunoregulatory properties that augment its primary pharmacological mechanism. To investigate this possibility, 13 Kuwaiti seasonal allergic rhinitis (SAR) patients were treated with levocetirizine for four weeks in comparison with a 7-member placebo-treated control group, followed by clinical evaluation and flow cytometric analysis of peripheral venous blood for inflammatory cell and lymphocyte subpopulation profiles. Relative to the controls, levocetirizine-treated patients exhibited an expected reduction in early phase allergic symptoms, including sneezing (P<0.001), nasal itching (P<0.01), nasal congestion, and running nose (P<0.001); reduced percentages of eosinophils (P<0.05); and three subpopulations of activated T lymphocytes: CD4+CD29+, CD4+CD212+, and CD4+CD54+ (P<0.05). Levocetirizine treatment also correlated with a significant increase in the percentage of CD4+CD25+ T cells (P<0.001). The ability of levocetirizine to reduce percentage representation of cell phenotypes known to contribute to inflammatory tissue damage (eosinophils, CD4+CD29+, CD4+CD212+, and CD4+CD54+) and expand percentages of CD4+CD25+, which may include protective immunoregulatory (Treg) cells, indicates that the drug has pharmacological potential beyond the immediate effects of H(1) histamine-receptor inhibition. Although the present data does not define a therapeutic mechanism, the results reported here establish important trends that may be used to guide future mechanistic examination of immunoregulatory capacity of H(1) inhibitors.

Topics: Adult; Anti-Inflammatory Agents; Cetirizine; Eosinophils; Female; Histamine H1 Antagonists, Non-Sedating; Humans; Immunophenotyping; Lymphocyte Activation; Male; Pruritus; Rhinitis, Allergic, Seasonal; Sneezing; T-Lymphocyte Subsets; Treatment Outcome

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

Addition of H(1) antagonists to intranasal corticosteroid treatment of allergic rhinitis (AR) is common in clinical practice and recommended by guidelines, despite some evidence that the additive benefits are negligible.. To assess additional benefits of 5 mg levocetirizine dihydrochloride in seasonal AR patients using 200 mcg fluticasone propionate nasal spray once daily.. In a double-blind placebo-controlled crossover study of 27 patients, following 2 weeks without treatment, subjects used fluticasone with levocetirizine or identical placebo for 2 weeks each. Assessments were the Juniper mini Rhinoconjunctivitis Quality-of-Life Questionnaire (mini-RQLQ), domiciliary peak nasal inspiratory flow (PNIF), total nasal symptoms (TNS) scores and nasal nitric oxide concentrations. Effects were interpreted and tested against minimal clinically important differences.. Add-on effects for levocetirizine vs. placebo excluded any clinically significant benefits: mean effects (one sided 95% confidence intervals) were mini-RQLQ -0.11 (-0.34), PNIF +0.57 (+5.23), and TNS -0.11 (-0.60). Numbers needed to treat (95% confidence intervals) by outcome were mini-RQLQ 14 (5 to 49), PNIF 4 (3-7), and TNS 3 (2-6). No significant within or between treatment effects were seen for nasal nitric oxide.. Contrary to current practice, the present results demonstrate that for the majority of patients, antihistamine add-on to effective nasal steroid treatment is inappropriate. Further work is required to confirm that this is also true in the most severe cases, and the available evidence needs to be put into guidelines and implemented.

Topics: Administration, Intranasal; Adolescent; Adult; Aged; Androstadienes; Anti-Allergic Agents; Cetirizine; Cross-Over Studies; Double-Blind Method; Drug Therapy, Combination; Eosinophils; Female; Fluticasone; Histamine H1 Antagonists, Non-Sedating; Humans; Inhalation; Male; Middle Aged; Nitric Oxide; Nose; Piperazines; Pollen; Quality of Life; Rhinitis, Allergic, Seasonal; Treatment Outcome

The aim of this study was to assess the effectiveness and safety of levocetirizine in the treatment of the symptoms of seasonal allergic rhinitis (SAR) in patients consulting their primary care doctor.. Open-label uncontrolled and non-randomised multi-centre study including patients presenting symptoms of SAR and treated with levocetirizine tablets, 5 mg OD, for 4 weeks.. patients with nasal symptoms who were not on treatment or not responsive to treatment, or affected by excessive adverse events due to the antihistamines used previously. There were two visits (initial and after four weeks). Primary end point: efficacy as measured by T4SS (combined score of sneezing, rhinorrhoea, nasal and ocular pruritus, ranging from 0 to 12 recorded by the patient); change in Clinical Global Impression (CGI-c) as rated by the general practitioner, subjective satisfaction with and preference for levocetirizine. Secondary end points: treatment-related adverse events.. 1290 patients were evaluated. Before the start of the study, 61.2% did not use any medication, 36.4% took anti-histamines which were not effective, and 27.0% of those previously treated patients experienced excessive adverse events. Statistically significant decreases (p < 0.01) compared to baseline were observed for each individual symptom of the itemised T4SS as well as for the global T4SS. The CGI-c improved in 91.1% of the patients who had received treatment previously and 96.8% of those who had not. Of the patients who had received treatment previously, 91.7% (p < 0.01) were satisfied with the study treatment and 84.5% of these patients reported they would prefer levocetirizine in future. All adverse events (somnolence, fatigue, headache, dry mouth) decreased by comparison with previous treatments after levocetirizine was used.. Levocetirizine showed an improvement in symptom control for SAR and was preferred by patients compared to the antihistamines they had taken previously. Levocetirizine was well tolerated.

Topics: Adolescent; Adult; Aged; Cetirizine; Histamine H1 Antagonists; Histamine H1 Antagonists, Non-Sedating; Humans; Middle Aged; Patient Satisfaction; Piperazines; Rhinitis, Allergic, Seasonal

Topics: Adolescent; Bacillus; Cetirizine; Double-Blind Method; Eosinophils; Female; Histamine H1 Antagonists, Non-Sedating; Humans; Male; Nasal Cavity; Pilot Projects; Piperazines; Probiotics; Rhinitis, Allergic, Seasonal; Treatment Outcome

Studies evaluating newer antihistamines in children are few. Levocetirizine is a potent and highly selective H1-antihistamine with a proven efficacy in adults. Primary objective was to assess the efficacy of levocetirizine 5 mg once-daily in reducing seasonal allergic rhinitis (SAR) symptoms, as measured by Total Four Symptom Score (T4SS = sum of sneezing, rhinorrhea, nasal and ocular pruritus), over the first 2 wk of treatment. Efficacy over 4 and 6 wk of treatment, effect on nasal congestion and on health-related quality of life as measured by PRQLQ (Paediatric Rhinoconjunctivitis Quality of Life Questionnaire) were among the major secondary objectives. A double-blind, randomized, placebo-controlled study including 177 children with a documented SAR (to grass and/or weed) for at least a year and having a mean baseline T4SS > or = 6 (out of 12). Children evaluated daily the severity of T4SS and nasal congestion on a scale from 0 (absent) to 3 (severe). PRQLQ responses were assessed on a scale from 0 (not bothered) to 6 (extremely bothered) and analysed descriptively. Global evaluation of disease evolution judged by investigators, parents and children was made on a scale from 1 (marked worsening) to 7 (marked improvement). For the primary objective, levocetirizine was statistically highly superior to placebo with a difference in adjusted means of 1.29 (95% CI: 0.66-1.92) in favour of levocetirizine (p < 0.001). The effect of levocetirizine was almost twice that of placebo (94.1% relative improvement over placebo). Nasal congestion was improved with levocetirizine reaching maximum difference to placebo of 0.31 (p < 0.05), a relative improvement over placebo of 77.5%. PRQLQ scores at week 2 improved with levocetirizine more than with placebo (0.85 vs. 0.51, respectively) remaining larger after 4 and 6 wk of treatment. In the study, 84.3%, 80.9%, 80.9% of children had their disease evolution rated as slightly-to-markedly improved by, respectively, the investigators, the parents and children themselves. Incidence of treatment-emergent adverse events was similar in both groups (33.7% with levocetirizine; 30.7% with placebo). No child in the levocetirizine group discontinued treatment because of adverse events. The 6-wk duration of this study was longer than the usual 2-4-wk duration for similar studies and shows that levocetirizine controls SAR symptoms in children over the entire pollen season.

Topics: Adolescent; Cetirizine; Child; Double-Blind Method; Female; Histamine H1 Antagonists, Non-Sedating; Humans; Male; Piperazines; Quality of Life; Rhinitis, Allergic, Seasonal; Surveys and Questionnaires; Treatment Outcome

The Environmental Exposure Unit, an indoor pollen challenge system to test anti-allergic medications, was used to compare the onset and duration of action and the efficacy of levocetirizine and desloratadine, two recently developed H1-antagonists. In this double-blind, placebo-controlled, parallel-group study, qualified subjects were randomised to once-daily levocetirizine 5 mg (n = 141), desloratadine 5 mg (n = 140) or placebo (n = 92) and exposed to ragweed pollen on two consecutive days (7 h and 6 h). Symptoms were self-rated every 30 min. On both days, levocetirizine produced a greater improvement in the major symptom complex score (primary efficacy variable) than desloratadine (p = 0.015); both were better than placebo (p < 0.001). Levocetirizine acted earlier (1 h vs. 3 h) and produced greater symptom relief at 24 h than desloratadine (p = 0.003). Levocetirizine also alleviated nasal obstruction better than desloratadine (p = 0.007) on day 1; and better than placebo (p = 0.014) after the second dose on day 2, which was not observed with desloratadine. Levocetirizine and desloratadine were safe and well tolerated.

Topics: Adolescent; Adult; Cetirizine; Cohort Studies; Double-Blind Method; Female; Histamine H1 Antagonists, Non-Sedating; Humans; Loratadine; Male; Piperazines; Rhinitis, Allergic, Seasonal; Severity of Illness Index; Treatment Outcome

Allergic rhinitis is characterized by an IgE-dependent inflammation. Nasal obstruction is related to allergic inflammation. Some antihistamines have been demonstrated to be capable of improving this nasal symptom.. The aim of this pilot study was to evaluate nasal symptoms, nasal airflow, inflammatory cells, and cytokine pattern in patients with seasonal allergic rhinitis (SAR), before and after treatment with levocetirizine, desloratadine, or placebo.. Thirty patients with SAR were evaluated, 27 males and three females (mean age 26.9+/-5.4 years). All of them received levocetirizine (5 mg/day), desloratadine (5 mg/day), or placebo for 2 weeks. The study was double-blind, parallel-group, placebo-controlled, and randomized. Total symptom score (TSS) (including: rhinorrhea, nasal itching, sneezing, and nasal obstruction) was assessed before and after treatment. Rhinomanometry, nasal lavage, and nasal scraping were performed in all subjects before and after treatment. Inflammatory cells were counted by conventional staining; IL-4 and IL-8 were measured by immunoassay on fluids recovered from nasal lavage.. Levocetirizine treatment induced significant symptom relief (P=0.0009) and improved nasal airflow (P=0.038). Desloratadine also relieved TSS (P=0.01), but did not affect nasal airflow. Levocetirizine significantly reduced eosinophils (P=0.029), neutrophils (P=0.005), IL-4 (P=0.041), and IL-8 (P=0.02), whereas desloratadine diminished IL-4 only (P=0.044). Placebo treatment did not significantly affect any evaluated parameters.. This pilot study demonstrates the effectiveness of levocetirizine in: (i) relieving nasal symptoms, (ii) improving nasal airflow, (iii) reducing leucocyte infiltration, and (iv) diminishing cytokine levels. These findings are the first evidence of the effectiveness of levocetirizine in SAR.

Topics: Adult; Cetirizine; Double-Blind Method; Eosinophils; Female; Histamine H1 Antagonists; Humans; Interleukin-4; Interleukin-8; Leukocyte Count; Loratadine; Male; Nasal Lavage Fluid; Nasal Obstruction; Pilot Projects; Piperazines; Rhinitis, Allergic, Seasonal; Statistics, Nonparametric

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; Conjunctivitis, Allergic; Desensitization, Immunologic; Female; Histamine H1 Antagonists, Non-Sedating; Humans; Plants; Pollen; Rhinitis, Allergic, Seasonal; Time Factors

Children with allergic rhinitis (AR) are reported to have disturbed sleep and daytime fatigue due to nasal obstruction.. To evaluate sleep impairment in children with AR using actigraphic evaluation.. Fourteen children aged 7 to 16 years with grass pollen-sensitized seasonal AR were enrolled. They completed the Total 4-Symptom Score (T4SS) scoring system for AR symptom score and the Pittsburgh Sleep Quality Index (PSQI) questionnaire for sleep quality, and they underwent actigraphy for 3 days in the pretreatment period. After topical corticosteroid and antihistaminic treatment for 8 weeks, actigraphy, the T4SS, and the PSQI were repeated. Fourteen healthy children aged 8 to 16 years underwent actigraphy and completed the PSQI questionnaire as controls.. There were no significant age or sex differences between the AR and control groups. Pretreatment PSQI and actigraphy scores were worse in the AR group vs the control group. After treatment, sleep quality improved, and there were no differences in actigraphy and PSQI scores between the 2 groups. Before treatment, the T4SS was significantly correlated with the sleep efficiency, daytime napping episodes, and total nap duration variables of actigraphy (r = -0.53, P = .004; r = 0.43, P = .02; and r = 0.39, P = .04, respectively). The T4SS was correlated with the total PSQI score (r = 0.67, P < .001).. Sleep can be compromised in children with AR. There is a significant correlation of clinical symptom score with the actigraphic and PSQI variables. Therefore, actigraphy may be used as an objective tool to evaluate sleep disturbance in children with AR.

Topics: Actigraphy; Adolescent; Androstadienes; Anti-Allergic Agents; Cetirizine; Child; Female; Fluticasone; Humans; Male; Rhinitis, Allergic, Seasonal; Sleep Wake Disorders

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 and urticaria are common allergic disorders that may affect approximately 15% of people at some time in their lives. Antihistamines are the most widely used therapeutic interventions for these disorders but the newer generation agents have differing pharmacokinetic characteristics that may result in different patient satisfaction and preferences. The objective of this study was to investigate patients' and physicians' satisfaction with their current antihistamine treatment for allergic disease.. In an observational study, physicians in nine European countries completed questionnaires evaluating 7,274 patients treated with an oral antihistamine. The satisfaction of patients and physicians with the efficacy and tolerability of treatment was rated on a visual analogue scale. In addition, the proportion of patients satisfied with treatment (overall satisfaction) and willing to continue treatment with the same antihistamine were assessed. Safety and tolerability data were also gathered.. The results of this study indicate that modern antihistamines are generally considered effective and well tolerated by patients. In general, levocetirizine scored significantly higher in terms of perception of efficacy, tolerability and overall satisfaction. In terms of tolerability, three-quarters of patients were 'very satisfied' and a further fifth were moderately satisfied with levocetirizine and almost all (95%) were happy to continue treatment. Overall, the most commonly reported adverse event in this study was somnolence, a well known effect of antihistamines. The rate of somnolence in the levocetirizine group (3.8%) was similar to that for fexofenadine (both doses) and desloratadine, two products which are considered to be nonsedating antihistamines, and significantly less than half the rate for cetirizine.. Levocetirizine is considered an effective and well tolerated option for treating allergic disease by patients and physicians alike, particularly when the best available effectiveness and tolerability are required.

Topics: Activities of Daily Living; Administration, Oral; Adult; Aged; Aged, 80 and over; Cetirizine; Child; Child, Preschool; Data Collection; Disorders of Excessive Somnolence; Dose-Response Relationship, Drug; Europe; Female; Histamine H1 Antagonists; Humans; Infant; Male; Middle Aged; Patient Satisfaction; Piperazines; Prevalence; Rhinitis, Allergic, Seasonal; Terfenadine; Treatment Outcome; Urticaria

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

The long QT syndrome is a rare disease. The prevalence is estimated at 1/5 000 to 1/20,000. Numerous drugs are contra-indicated because they can lengthen the QT interval. A case of pollen allergy in an adolescent with LQTS is described. The possibility to prescribe anti-H1 drugs is reviewed since cases of torsades de pointe and even deaths have been reported for terfenadine and astemizole. Diphenhydramine, orphenadrine and hydroxyzine are contra-indicated. No accidents and no effects on the QT interval have been published for ebastine, fexofenadine, desloratadine and levocetirizine. These anti-H1 drugs could be used with great care, without any association with drugs resulting in low serum potassium level. Azelastine eye drops have been authorized and a routine protection by inhaled corticosteroids during the pollinic period has been advised in this adolescent treated by betablockers.

Topics: Adolescent; Adrenergic beta-Antagonists; Anti-Asthmatic Agents; Butyrophenones; Cetirizine; Conjunctivitis, Allergic; Cromolyn Sodium; Diabetes Mellitus, Type 1; Heart; Histamine H1 Antagonists; Humans; Long QT Syndrome; Male; Piperazines; Piperidines; Rhinitis, Allergic, Seasonal; Terfenadine

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