Fluticasone furoate nasal spray in allergic rhinitis

Fluticasone furoate is a novel glucocorticoid developed for the treatment of allergic rhinitis and other inflammatory diseases. Fluticasone furoate demonstrates high systemic clearance, low oral bioavailability and low absolute bioavailability after intranasal administration (<0.5%). The drug possesses a high receptor affinity. Fluticasone furoate is given once daily at a dose of 110 microg. Clinical studies tested the efficacy of fluticasone furoate in seasonal allergic rhinitis and perennial allergic rhinitis. Patients randomized to the drug experienced significant alleviation in their nasal and ocular symptoms as well as clinically relevant improvement in quality of life. The drug is well tolerated and has a good safety profile owing to reduced systemic exposure. Thus, fluticasone furoate might represent a single treatment option for nasal and ocular symptoms of allergic rhinitis.     

Fluticasone furoate: intranasal use in allergic rhinitis

Fluticasone furoate nasal spray is a new topical intranasal corticosteroid with enhanced affinity for the glucocorticoid receptor and low systemic exposure, which was recently approved in the US for the treatment of seasonal or perennial allergic rhinitis in adults and in children aged >or=2 years. Fluticasone furoate nasal spray employs a novel delivery device with a unique side-actuated design, a short nozzle and a new trigger mechanism designed for ease of use. In well controlled clinical trials, intranasal fluticasone furoate 110microg once daily for 2 weeks in adults and adolescents with seasonal allergic rhinitis reduced nasal and ocular symptoms, and improved health-related quality of life to a significantly greater extent than placebo. Similarly, treatment with intranasal fluticasone furoate 110microg once daily for 4-6 weeks in adults and adolescents with perennial allergic rhinitis was superior to placebo in reducing nasal symptoms and with respect to overall response to therapy. In children aged 6-11 years, fluticasone furoate nasal spray was shown to be effective in reducing the nasal symptoms of seasonal and perennial allergic rhinitis following treatment for 2 and 4 weeks, respectively. Fluticasone furoate nasal spray was well tolerated in adults, adolescents and children aged 2-11 years, with an overall incidence of adverse events similar to that with placebo.     

Intranasal corticosteroids for allergic rhinitis

Intranasal corticosteroids are accepted as safe and effective first-line therapy for allergic rhinitis. Several intranasal corticosteroids are available: beclomethasone dipropionate, budesonide, flunisolide, fluticasone propionate, mometasone furoate, and triamcinolone acetonide. All are efficacious in treating seasonal allergic rhinitis and as prophylaxis for perennial allergic rhinitis. In general, they relieve nasal congestion and itching, rhinorrhea, and sneezing that occur in the early and late phases of allergic response, with studies showing almost complete prevention of late-phase symptoms. The rationale for topical intranasal corticosteroids in the treatment of allergic rhinitis is that adequate drug concentrations can be achieved at receptor sites in the nasal mucosa. This leads to symptom control and reduces the risk of systemic adverse effects. Adverse reactions usually are limited to the nasal mucosa, such as dryness, burning and stinging, and sneezing, together with headache and epistaxis in 5-10% of patients regardless of formulation or compound. Differences among agents are limited to potency, patient preference, dosing regimens, and delivery, device and vehicle.     

A risk-benefit assessment of intranasal triamcinolone acetonide in allergic rhinitis.

The efficacy of intranasal triamcinolone acetonide in seasonal and allergic rhinitis has been evaluated in clinical trials and has been compared with antihistamines and other intranasal corticosteroids. Intranasal corticosteroids are either as equally effective as or more effective than comparative drugs. Intranasal corticosteroids are particularly useful as they decrease membrane permeability and inhibit both early and late phase reactions to allergens. They minimise the nasal secretory response and reduce the sensitivity of local nasal irritant receptors. A potential benefit of topical application is the flushing action of the nasal mucosa, which may reduce allergens and secretions. In addition to seasonal and perennial rhinitis, intranasal corticosteroids have additional benefits when used to reduce inflammation in the treatment of sinusitis and may help in decreasing secondary rhinovirus infections. Furthermore, suboptimal control of asthma can be avoided by treatment of allergic rhinitis with intranasal corticosteroids. In clinical trials, common adverse effects for triamcinolone acetonide include sneezing, dry, mucosa, nasal irritation, sinus discomfort, throat discomfort, epistaxis and headache. Posterior subcapsular cataract formation has not been seen with triamcinolone acetonide. Recent literature evaluating systemic absorption of intranasal corticosteroids have shown surprising results where significant absorption has occurred with intranasal budesonide and fluticasone propionate. Growth and hypothalamic pituitary axis (HPA) function studies have been reviewed, with some intranasal corticosteroids showing changes with continual use. A retrospective study in children receiving daily triamcinolone acetonide for 12 months showed no effect on height and bodyweight. Triamcinolone acetonide at standard dosages (110 or 220microg once or twice a day) does not appear to suppress adrenal gland function and is effective in relieving most symptoms of allergic rhinitis. The International Consensus Conference Proceedings on Rhinitis now currently recommends the use of intranasal corticosteroids as first line therapy, since they have been found to be well tolerated and effective with minimal adverse effects and, specifically, no cognitive impairment. The recommended maximum dose of aqueous triamcinolone acetonide in adults and children is 220microg once a day. The aerosol form may be recommended in children between 7 and 12 years old, up to 440microg once a day or in divided doses. Duration of allergy treatment is generally for the length of each allergy season. If symptoms are perennial, then a reduction of dosage is made to the lowest effective dose with monitoring every 3 months for risk and benefit assessment. Complications to watch for include bleeding, and possible septal perforation and nasal candidiasis, although these are rare.     

盐酸氮卓斯汀喷鼻剂与辅舒良在治疗变应性鼻炎中的疗效分析

目的比较盐酸氮卓斯汀喷鼻剂同辅舒良在治疗常年性变应性鼻炎中的疗效。方法在确诊为常年性变应性鼻炎的231例患者,随机分成两组,其中123例患者对其用盐酸氮卓斯汀喷鼻剂进行治疗,另外108例用辅舒良(丙酸氟替卡松鼻喷剂)进行治疗,对比两组的疗效。结果盐酸氮卓斯汀组与辅舒良组治疗效果相当,但盐酸氮卓斯汀起效时间更快。从不良反应看,盐酸氮卓斯汀有个别患者诉有一过性轻微口苦;辅舒良组有10例出现鼻黏膜干燥,有3例出现鼻出血。盐酸氮卓斯汀不良反应更少。结论当常年性变应性鼻炎需要快速、安全和高效减轻症状时盐酸氮卓斯汀喷鼻剂是重要的选择之一。     

A review of the use of fluticasone furoate since its launch

INTRODUCTION: Fluticasone furoate (FF) is the latest glucocorticoid officially approved for the treatment of allergic rhinitis. FF has shown the highest affinity and selectivity for the glucocorticoid receptors as well the longest tissue retention compared with other available intranasal steroids; these new pharmacologic characteristics provide the basis for its potent and prolonged anti-inflammatory activity at the target site. AREAS COVERED: A literature review achieved through PubMed and Medline research methods supports the clinical efficacy of FF versus placebo in reducing ocular and nasal symptoms related to allergic rhinitis (at the recommended starting doses of 110 μg once daily for adults and adolescents and 55 μg once daily for children), with a good safety profile. Moreover, the present review also compares FF with other intranasal steroids: FF represents a molecular evolution of fluticasone propionate (FP), and there is scientific evidence of therapeutic advantages over FP. EXPERT OPINION: Fluticasone furoate is a promising molecule in the treatment of allergic rhinitis as it fits fully all the official guidelines' criteria. It is now being considered as a topical steroid that is quite close to the ideal pharmacological model for glucocorticoids due to its satisfying safety/tolerability profile, both in adults and children, leads FF to be considered as a topical steroid that is quite close to the ideal pharmacologic model for glucocorticoids. More studies should be directed to assess the improvement of quality of life in subjects with allergic rhinitis treated with FF, in comparison with other intranasal steroids and even H1-antihistamines; in addition, it could be also interesting to analyze eventual, additional effects of FF in patients with bronchial asthma, which is frequently associated with allergic rhinitis.     

Flunisolide: a review of its pharmacological properties and therapeutic efficacy in rhinitis

Flunisolide, a derivative of fluocinolone acetonide, is advocated for intranasal inhalation for the treatment of perennial and seasonal allergic rhinitis. It is rapidly absorbed by all routes of administration, but it quickly undergoes extensive first-pass metabolism to a 6 beta-hydroxylated metabolite, which possesses only weak corticosteroid effects. Intranasal flunisolide relieves nasal symptoms (but not eye symptoms) in both perennial and seasonal allergic rhinitis, being most effective in patients who have an allergic component to their rhinitis; and like other corticosteroids it may reduce the need for systemic antihistamines in such patients, expecially during peak pollen periods. A few well designed comparative studies have shown flunisolide to be as effective as intranasal beclomethasone, and (in a single study) more effective than intranasal sodium cromoglycate solution. Only transient side effects have occurred, including nasal stinging and throat irritation. No Candida infections have been clinically apparent in short or longer term trials. Resting morning plasma cortisol levels have not been suppressed by usual therapeutic doses of intranasal flunisolide, but the drug's effects on hypothalamo-pituitary-adrenal (HPA) axis integrity during conditions of stress have not been evaluated.     

盐酸氮卓斯汀与丙酸氟替卡松喷鼻剂治疗变应性鼻炎临床对比观察

目的观察并比较盐酸氮卓斯汀与丙酸氟替卡松喷鼻剂在治疗变应性鼻炎中的效果。方法 146例变应性鼻炎患者,随机分为观察组和对照组,观察组应用盐酸氮卓斯汀喷鼻剂,对照组应用丙酸氟替卡松喷鼻剂(辅舒良),比较两组疗效及不良反应。结果两组治疗效果比较差异无统计学意义。但观察组起效快、不良反应明显少于对照组。结论对于常年性变应性鼻炎的治疗,应首选盐酸氮卓斯汀,该药起效快、安全有效,值得临床推广应用。     

Mometasone furoate nasal spray: a review of safety and systemic effects.

The development of corticosteroids that are delivered directly to the nasal mucosa has alleviated much of the concern about the systemic adverse effects associated with oral corticosteroid therapy. However, given the high potency of these drugs and their widespread use in the treatment of allergic rhinitis, it is important to ensure that intranasal corticosteroids have a favourable benefit-risk ratio. One agent that typifies the systemic safety found in the majority of intranasal corticosteroids is mometasone furoate nasal spray, a potent and effective treatment for seasonal and perennial allergic rhinitis and nasal polyposis. Mometasone furoate does not reach high systemic concentrations or cause clinically significant adverse effects. Results from pharmacokinetic studies in adults and children suggest that systemic exposure to mometasone furoate after intranasal administration is negligible. This is probably because of the inherently low aqueous solubility of mometasone furoate, which allows only a small fraction of the drug to cross the nasal mucosa and enter the bloodstream, and because a large amount of the administered drug is swallowed and undergoes extensive first-pass metabolism. There is no clinical evidence that mometasone furoate nasal spray suppresses the function of the hypothalamus-pituitary-adrenal axis when the drug is administered at clinically relevant doses (100-200 microg/day); consequently, mometasone furoate nasal spray has not been associated with growth inhibition in children. The safety and tolerability of mometasone furoate nasal spray have been rigorously assessed in clinical trials involving approximately 4,500 patients, with epistaxis, headache and pharyngitis being the most common adverse effects associated with treatment in adolescents and adults.The clinical effectiveness of mometasone furoate nasal spray, coupled with its agreeable safety and tolerability profile, confirms its favourable benefit-risk ratio.     

Effect of fluticasone propionate nasal spray on bioavailability of intranasal hydromorphone hydrochloride in patients with allergic rhinitis

STUDY OBJECTIVE: To investigate the effect of the nasal corticosteroid fluticasone propionate on the bioavailability and pharmacokinetics of single-dose intranasal hydromorphone hydrochloride in patients with allergic rhinitis. DESIGN: Randomized, three-way, crossover pharmacokinetic study. SETTING: University clinical research unit. PATIENTS: Twelve patients with allergic rhinitis. INTERVENTION: Hydromorphone hydrochloride 2.0 mg was administered by intravenous infusion (treatment A), intranasal spray without allergic rhinitis treatment (treatment B), and intranasal spray after 6 days of fluticasone propionate (treatment C). Blood samples were collected serially from 0-16 hours. MEASUREMENTS AND MAIN RESULTS: Pharmacokinetic parameters were determined by noncompartmental methods. An analysis of variance (ANOVA) model was used for statistical analysis. Mean (% coefficient of variation) absolute bioavailability of intranasal hydromorphone was 51.9% (28.2) and 46.9% (30.3) in patients with allergic rhinitis with and without treatment with fluticasone propionate, respectively. Mean maximum concentration (Cmax) values were 3.02 and 3.56 ng/ml, respectively. No statistical differences in Cmax and area under the concentration versus time curve were detected between intranasal treatments. Bioavailability values for both intranasal treatments were lower than those in healthy volunteers (57%). Median time to Cmax (Tmax) values were significantly different (p=0.02) for treatments B and C (15 and 30 min, respectively) using rank-transformed Tmax for ANOVA. Adverse effects were consistent with known effects of hydromorphone administered by other routes, with the exception of bad taste after intranasal administration. CONCLUSION: Hydromorphone was rapidly absorbed after nasal administration, with maximum concentrations occurring for most subjects within 30 minutes. Allergic rhinitis may affect pain management strategies for intranasal hydromorphone, with a delay in onset of action for patients treated with fluticasone propionate.     

Are intranasal corticosteroids all equally consistent in managing ocular symptoms of seasonal allergic rhinitis?

ABSTRACT

Background: Nasal and ocular symptoms of allergic rhinitis (AR) are reported by >70% of patients and have a profound impact on quality of life while also incurring substantial healthcare costs. It has been suggested that intranasal corticosteroids (INS), in addition to effectively treating the nasal components of AR, are effective in treating the ocular symptoms.

Objective: This review provides a comprehensive, updated assessment of available data in the public domain to determine the consistency of INS efficacy in treating ocular AR symptoms.

Methods: MEDLINE and EMBASE searches, and research of governmental and regulatory institution sources identified 35 randomised, placebo-controlled trials of INS and seasonal AR (SAR) published between 1990 and May 2009 that specifically contained ocular efficacy as part of the study analyses.

Results: Examination of these studies reveals substantial inconsistency of effect of some INS across, and even within, trials, casting doubt on the suggestion that ocular efficacy is a class effect of INS. Conflicting, inconsistent or even negative effects were observed for most INS examined including mometasone furoate and fluticasone propionate. Only fluticasone furoate nasal spray, in addition to established efficacy in treating nasal symptoms, demonstrated a consistent positive effect on ocular symptoms of SAR compared with placebo in a large number of patients across all of its prospective studies. Moreover, these results were consistent across different allergy seasons, including grass, ragweed, and mountain cedar seasons, and different geographical locations throughout Europe and the USA.

Conclusion: While additional prospective head-to-head clinical trials comparing the efficacy of INS in treating ocular symptoms of AR are needed to fully elucidate the benefits of one INS compared with another, data available to date suggest that not all INS are equally consistent in managing ocular symptoms of SAR. Fluticasone furoate is currently the most consistent.     

Review of desloratadine for the treatment of allergic rhinitis,chronic idiopathic urticaria and allergic inflammatory disorders

Desloratadine is a once-daily, non-sedating, non-impairing, selective histamine H₁-receptor antagonist. It relieves the symptoms of seasonal allergic rhinitis (including nasal obstruction and congestion, and morning symptoms), perennial allergic rhinitis and chronic idiopathic urticaria by blocking multiple critical steps in the systemic allergic cascade and downregulating key allergy-induced inflammatory mediators. It also relieves asthma symptoms and decreases rescue medication use in patients with seasonal allergic rhinitis and comorbid asthma. Numerous clinical studies have demonstrated that desloratadine is safe, well tolerated and free of serious cardiac effects. Pharmacokinetic studies have demonstrated a low propensity for drug–drug or drug–food interactions. This review outlines the mechanism of action, efficacy and safety of desloratadine for the treatment of allergic inflammatory disorders.     

Review of desloratadine for the treatment of allergic rhinitis, chronic idiopathic urticaria and allergic inflammatory disorders

Desloratadine is a once-daily, non-sedating, non-impairing, selective histamine H1-receptor antagonist. It relieves the symptoms of seasonal allergic rhinitis (including nasal obstruction and congestion, and morning symptoms), perennial allergic rhinitis and chronic idiopathic urticaria by blocking multiple critical steps in the systemic allergic cascade and downregulating key allergy-induced inflammatory mediators. It also relieves asthma symptoms and decreases rescue medication use in patients with seasonal allergic rhinitis and comorbid asthma. Numerous clinical studies have demonstrated that desloratadine is safe, well tolerated and free of serious cardiac effects. Pharmacokinetic studies have demonstrated a low propensity for drug-drug or drug-food interactions. This review outlines the mechanism of action, efficacy and safety of desloratadine for the treatment of allergic inflammatory disorders.     

Ciclesonide nasal spray: in allergic rhinitis

Ciclesonide nasal spray delivers the corticosteroid ciclesonide as a hypotonic spray via a metered-dose manual pump. Systemic exposure to ciclesonide and its active metabolite desisobutyryl-ciclesonide is low after intranasal administration. High protein binding (approximately 99%) and rapid first-pass clearance further reduce systemic exposure to the drug. In well designed trials, intranasal ciclesonide 200 microg once daily for 2-4 weeks was more effective than placebo in terms of improving nasal symptoms in adolescents and adults with moderate to severe seasonal allergic rhinitis. Quality of life measures were statistically significantly improved in ciclesonide relative to placebo recipients during the first 2 weeks of therapy. Similarly, in adolescents and adults with moderately severe perennial allergic rhinitis, ciclesonide 200 microg once daily was more effective than placebo in terms of reducing nasal symptoms in well designed trials of 6 weeks' and 1 year's duration. Improvements relative to placebo in quality of life measures were not considered clinically relevant. Ciclesonide nasal spray was generally well tolerated in these clinical trials; most adverse events were mild to moderate in intensity.     

Safety and tolerability of treatments for allergic rhinitis in children.

Allergic rhinitis is a common condition in adults and children and can have a large impact on patients' health and quality of life. The aim of current allergic rhinitis therapies is to treat the subjective symptoms and to improve objective measures of the disease. Of the available treatment options for paediatric allergic rhinitis, the newer oral antihistamines and intranasal corticosteroids are first-line treatments.First-generation antihistamines are associated with unwanted adverse effects such as cardiotoxicity, sedation and impairment of psychomotor function. Despite results from studies using first-generation antihistamines demonstrating impairment of cognitive and academic function in children, many of these agents are still commonly given to patients. The newer antihistamines, developed with the aim of being more specific for the histamine H(1) receptor and of overcoming these adverse effects, are the medication of choice in patients with mild intermittent allergic rhinitis. For children <12 years of age, three newer oral antihistamines are currently available: cetirizine, loratadine and fexofenadine. A lack of adverse effects with these antihistamines has been demonstrated in children using EEG and psychomotor performance tests, and in clinical studies. However, issues of receptor selectivity and the potential for CNS adverse effects still remain, and further studies are warranted.Intranasal corticosteroids are the most effective anti-inflammatory agents used for the treatment of paediatric allergic rhinitis; however, the safety of these compounds remains controversial. The safety implications associated with corticosteroids are long-term, dose-related systemic effects, such as suppression of adrenocortical function, growth and bone metabolism, and the extent of these effects is influenced by a number of factors including corticosteroid type, pharmacokinetic profile, mode of delivery and delivery device. Topical corticosteroids were introduced to reduce the systemic effects seen with the long-term use of oral agents. The intranasal corticosteroids currently available for the treatment of paediatric allergic rhinitis - beclometasone, budesonide, flunisolide, fluticasone propionate, mometasone and triamcinolone - have short half-lives and rapid first-pass hepatic metabolism; however, their pharmacokinetics vary in terms of systemic absorption, potency, binding affinity, lipophilicity, volume of distribution, and half-life. A number of studies - utilising hypothalamic-pituitary-adrenal axis function tests such as plasma cortisol levels, 24-hour urinary-free cortisol tests; stimulation tests with corticotropin (adrenocorticotropic hormone), lypressin, and corticotropin-releasing hormone; and growth assessment studies using knemometry and stadiometry - have indicated that these intranasal corticosteroids are well-tolerated in paediatric patients and do not significantly affect growth.The wealth of clinical data and the recommendations from evidence-based guidelines suggest that both antihistamines and intranasal corticosteroids have good safety profiles in children. Nevertheless, growth should be regularly monitored in children receiving intranasal corticosteroids. Other treatments such as immunotherapy, local chromones and decongestants can also be beneficial in managing paediatric allergic rhinitis, and therapies should be considered on an individual basis.     

Fluticasone furoate nasal spray consistently and significantly improves both the nasal and ocular symptoms of seasonal allergic rhinitis: a review of the clinical data

Background: Allergic rhinitis (AR) is a highly prevalent disorder, which often manifests as both nasal (congestion, sneezing, itching and rhinorrhoea) and ocular (redness, watery eyes, itching and burning) symptoms. Until recently, efficacy against the ocular symptoms of AR has been inconsistent for any single intranasal corticosteroid (INS). Fluticasone furoate is an enhanced-affinity glucocorticoid with potent anti-inflammatory activity. Objective: To assess better the efficacy of an INS in the treatment of both the nasal and ocular symptoms of seasonal AR (SAR). Methods: Data from all four trials of fluticasone furoate nasal spray (FFNS) in the treatment of SAR are reviewed and critically considered. Results: FFNS consistently and significantly improved the nasal and ocular symptoms of SAR in patients sensitised to several different seasonal allergens (grass, ragweed and mountain cedar pollen) in all trials. An integrated analysis of the results also confirmed improvements in both nasal and ocular symptom scores in previously under-represented adolescent patients treated with FFNS. Conclusion: FFNS is the first INS to show consistent nasal and ocular efficacy across all SAR trials.     

Medical management of noninfectious rhinitis

Noninfectious rhinitis and the clinical pharmacology of drugs used in its treatment, including specific treatment recommendations, are reviewed. Characterized by hyperreactivity of the nasal mucosa to a variety of stimuli, noninfectious rhinitis can be classified either as seasonal or perennial allergic rhinitis (when antigens can be identified) or as vasomotor or nonallergic rhinitis (when antigens are not identifiable). However, noninfectious rhinitis is probably better viewed as a continuum between these extremes rather than as definitive categories. Treatment measures include removal of offending agents when possible, and injection of allergenic extracts to decrease sensitivity to inhalant allergens. Among the pharmacologic alternatives, the classical H1 antihistamines competitively inhibit the action of mast-cell histamine at its receptor sites and thus decrease sneezing, nasal pruritus, rhinorrhea, and conjunctivitis. Orally bioavailable alpha-adrenergic agents such as pseudoephedrine and phenylpropanolamine decrease nasal congestion that responds poorly to antihistamines. Topical vasoconstrictors are contraindicated in chronic rhinitis because of the complications of rebound congestion. Systemic corticosteroids are effective but rarely appropriate for chronic rhinitis. Potent topical corticosteroids such as intranasal beclomethasone dipropionate are useful for severe nasal congestion. Cromolyn sodium, an inhibitor of histamine release from mast cells, appears to have some efficacy in suppressing symptoms of allergic rhinitis and conjunctivitis when used topically. Anticholinergics have occasionally been recommended to reduce rhinorrhea, but little data on their efficacy are available.     

丙酸氟替卡松鼻喷雾剂对儿童哮喘控制及过敏性鼻炎症状改善的作用

目的 比探讨丙酸氟替卡松鼻喷雾剂在改善儿童过敏性鼻炎症状以及控制哮喘反复发作方面的作用.方法 将100例过敏性鼻炎合并哮喘综合征患儿按照随机数字表法分为对照组和观察组.对照组应用氯雷他定及经口腔吸人糖皮质激素,观察组在此基础上使用丙酸氟替卡松鼻喷雾剂治疗,观察两组疗效.结果 观察组总有效率（94％）明显优于对照组（76％）（x2=6.35,P＜0.05）.10 ～ 12周以后,观察组与对照组鼻炎症状评分及哮喘症状评分差异均有统计学意义（t=2.47、2.64、3.41;2.30、3.17、2.47,均P＜0.05）.不良反应方面两组鼻腔干燥、鼻出血发生率差异均有统计学意义（x2 =7.11、7.53,均P＜0.05）.结论 丙酸氟替卡松鼻喷雾剂在改善儿童过敏性鼻炎和哮喘症状复发方面有很好疗效,值得临床大力推广.     

Effect of mometasone furoate by topical application on allergic rhinitis model in rats

The effects of mometasone furoate on experimental allergic rhinitis in rats were studied in comparison with that of fluticasone propionate. Topical application of both drugs inhibited dose-dependently the increase of nasal symptoms (sneezing and nasal rubbing) after antigen challenge to the nasal cavity of actively sensitized rats. Mometasone furoate and fluticasone propionate at concentrations of 0.01 or 0.1% significantly inhibited both nasal rubbing and sneezing 1 h after topical application of both drugs. The relative potencies of mometasone furoate in nasal rubbing and sneezing compared to fluticasone propionate were 5.01 and 6.87, respectively. Mometasone furoate (0.02%) and fluticasone propionate (0.1%) significantly inhibited the increase of antigen-induced nasal rubbing even 6 h after topical application, indicating that both drugs have a long-lasting effect.     

新型鼻用皮质类固醇糠酸氟替卡松

鼻用皮质类固醇具有全面强效的抗炎作用,是目前治疗变应性鼻炎最有效的药物之一。文中介绍了新型鼻用皮质类固醇糠酸氟替卡松的分子机制、药效学、药动学、临床疗效、安全性和装置等特点,并与现有其他鼻用皮质类固醇进行比较。