Azelastine Group Research Articles

A Comparative Study of Montelukast and Azelastine add on Therapy in Moderate to Severe Allergic Rhinitis Treatment: A Double-Blind Randomized Clinical Trial.

Allergic Rhinitis (AR) is a prevalent chronic inflammatory nasal condition with significant negative effects on the patients' quality of life. This study aimed to investigate the efficacy of Montelukast and intranasal antihistamine in combination with intranasal corticosteroid (INCS) in moderate to severe allergic rhinitis on the patients' quality of life and AR control. This double-blind randomized clinical trial study was carried out on 66 moderate to severe AR patients referred to Namazi Hospital, Shiraz, Iran from 2020 to 2021, who were randomly divided into 3 groups. Group one received Montelukast add-on therapy and Budesonide nasal spray. The second group received intranasal antihistamine (Azelastine) add-on therapy and Budesonide nasal spray and the third group as the control group received intranasal Budesonide spray with a placebo tablet.To measure the impact of each medication on the patient's quality of life and AR control, we employed the Sino-Nasal Outcome Test-22 questionnaire (SNOT 22). We evaluated the symptoms and compared them at baseline, one and three months after the start of treatments. Spirometry was performed to investigate the possibility of co-morbid asthma at baseline and end of the study. The patients' mean age was 30.13 ± 12.7 years. Most patients experienced perennial AR (65.2%). Reduction of mean scores SNOT22 was statistically different between groups (P-value < 0.001). Three months after treatment, the mean decrease of SNOT-22 in the Azelastine group was statistically significant compared to both Montelukast (P-value < 0.001) and control groups (P-value < 0.001). No significant difference was observed between the Montelukast and control groups (P-value = 0.142). 23 of 66 patients were diagnosed with asthma and asthma treatment was initiated. The amount of FEV1 change after AR treatment was not statistically significant between the groups in asthmatic patients (P-value = 0.351). Based on our findings, we recommend Azelastine in conjunction with an intranasal corticosteroid for the treatment of moderate to severe allergic rhinitis. In moderate to severe AR or even asthma management, Montelukast has no greater impact than INCS.

Comparison of the Effects of Azelastine and Fluticasone Nasal Sprays in the Treatment of Allergic Rhinitis.

Allergic rhinitis is a highly prevalent, allergen-induced disease. Intranasal corticosteroids are currently the first-line therapy for these patients. It is uncertain whether intranasal antihistamines have comparable efficacy. This study compares effects of Azelastine and Fluticasone nasal spray in patients with allergic rhinitis. Prospective comparative study including 240 patients with allergic rhinitis was conducted with 120 each in fluticasone and azelastine group. Nasal sprays were given for period of three months along with an oral antihistamine. Follow up was done after three months. Pre and post treatment symptom assessment were done using Total nasal symptom score. The median TNSS in pre and post treatment of group A (fluticasone) is 10(4) and 1(3) which shows statistical significance with p value < 0.001. Median TNSS in pre and post treatment of group B (azelastine) is 9(4) and 1(2) which shows statistical significance with p value < 0.001. The median TNSS in pre and post treatment value between Group A and B shows no statistically significant difference between two groups with p value 0.56 and 0.06 respectively. Intranasal azelastine and fluticasone had comparable efficacy in symptom control in patients with allergic rhinitis. Azelastine due to its lesser side effects, can be safely used in children, patients with glaucoma and cataract. Azelastine may be considered as a safer replacement to fluticasone for long term use in patients with allergic rhinitis. A larger multicentric study with a bigger sample size may be required to confirm the efficacy and safety profile of azelastine nasal spray.

Therapeutic effect of nasal corticosteroids combined with nasal antihistamine on vasomotor rhinitis

Objective: To observe the clinical efficacy of nasal corticosteroids combined with nasal antihistamine in the treatment of vasomotor rhinitis. Method: One hundred and twenty vasomotor rhinitis patients were randomly divided into three groups including budesonide group, azelastine group, and budesonide and azelastine group with 40 cases in each. Nasal spray with nasal corticosteroids and nasal antihistamines was applied for combined treatment group, while the patients in budesonide group and azelastine group were given only nasal corticosteroids and nasal antihistamines, respectively. The course lasted 8 weeks, and the clinical efficacy was evaluated with the visual analogue scale (VAS) score and SF-12v2 score. Result: VAS score of the peripheral nasal symptoms of the three groups was significantly decreased after treatment, and the difference was statistically significant compared with that before treatment (P<0.05). The visual analogue scale of nasal symptoms in the combined treatment group was significantly lower than that in the budesonide group and the azelastine group. There was no statistically significant difference between the budesonide group and the azelastine group after the treatment on the VAS of the three nasal symptoms. However, compared with before treatment, the difference was statistically significant (P<0.05). The visual analogue scale of nasal symptoms in the combined treatment group was higher than that in the budesonide group and the azelastine group, and the difference was statistically significant (P<0.05). After treatment, there was no significant difference between budesonide group and azelastine group (P>0.05). At the same time, the patients in the combined treatment group showed significant efficiency of 47.50% and total efficiency of 90.00%, which were statistically significant compared with budesonide group (30.00%,75.00%) and azelastine group (27.50, 70.00%), respectively (P<0.05). But there was no significant difference between budesonide group and azelastine group (P>0.05). Conclusion: Nasal corticosteroids and nasal antihistamine can effectively relieve the nasal symptoms of vasomotor rhinitis and improve the quality of life of patients. The effect of nasal corticosteroids was better than that of nasal antihistamine. The effect of nasal corticosteroids combined with nasal antihistamine was superior to that of single drug..

A prospective study of efficacy and safety of olopatadine versus azelastine in allergic conjunctivitis at a tertiary care hospital

Background: Allergic conjunctivitis, an ocular surface inflammatory disease with significant social and economic impact affects approximately 25% of the general population. H1 receptor blockers, mast cell stabilizers and drugs that block cytokine and prostaglandin formation form the treatment armamentarium. Olopatadine hydrochloride and Azelastine hydrochloride are dual-acting selective H1 receptor antagonist with mast-cell stabilizing property. This study was undertaken to assess the efficacy and safety of olopatadine hydrochloride 0.1% and Azelastine hydrochloride 0.05% in allergic conjunctivitis amongst Indians.Methods: After obtaining Institutional Ethics Committee approval and written informed consent, 120 patients diagnosed with allergic conjunctivitis fulfilling the inclusion/exclusion criteria were enrolled in the study. Study was done from April 2014 to June 2015 at Minto eye hospital. Study subjects were treated with olopatadine hydrochloride 0.1% and Azelastine hydrochloride 0.05% eye drops BD for 15 days. Ocular symptoms, instead of and signs and adverse events, if any were recorded on the day 8 and day 15 follow up visits.Results: At the end of the study period, the reduction in the ocular itching score from baseline was higher in the olopatadine group compared to the azelastine group (p&lt;0.002). Similarly, the scores of ocular congestion (p&lt;0.008), foreign body sensation (p&lt;0.009), tearing (p&lt;0.001), erythema (p&lt;0.002) and chemosis (p&lt;0.015) also showed larger reduction in the olopatadine treated patients. The common adverse events encountered in both the groups were stinging after instillation, burning, bitter taste and headache.Conclusions: In allergic conjunctivitis, both olopatadine and azelastine were found to be effective in relieving ocular signs and symptoms, but olopatadine was found to be superior in terms of efficacy, safety and tolerability with minimal side effects.

Can curcumin modulate allergic rhinitis in rats?

This study aimed to explore the effects of curcumin on experimental allergic rhinitis in rats. Twenty-eight male Wistar albino rats were randomly divided into four groups: a control group; a group in which allergic rhinitis was induced and no treatment given; a group in which allergic rhinitis was induced followed by treatment with azelastine hydrochloride on days 21-28; and a group in which allergic rhinitis was induced followed by treatment with curcumin on days 21-28. Allergy symptoms and histopathological features of the nasal mucosa were examined. The sneezing and nasal congestion scores were higher in the azelastine and curcumin treatment groups than in the control group. Histopathological examination showed focal goblet cell metaplasia on the epithelial surface in the azelastine group. In the curcumin group, there was a decrease in goblet cell metaplasia in the epithelium, decreased inflammatory cell infiltration and vascular proliferation in the lamina propria. Curcumin is an effective treatment for experimentally induced allergic rhinitis in rats.

Antioxidant activities of curcumin in allergic rhinitis

We investigated the antioxidant effects of curcumin in an experimental rat model of allergic rhinitis (AR). Female Wistar albino rats (n=34) were divided randomly into four groups: healthy rats (control group, n=8), AR with no treatment (AR+NoTr group, n=10), AR with azelastine HCl treatment (AR+Aze group, n=8), and AR with curcumin treatment (AR+Curc group, n=8). On day 28, total blood IgE levels were measured. For measurement of antioxidant activity, the glutathione (GSH) level and catalase (CAT), superoxide dismutase (SOD), and glutathione peroxidase (GSH-Px) activities were measured in both inferior turbinate tissue and serum. Malondialdehyde (MDA) levels were measured only in inferior turbinate tissue, and paraoxonase (PON) and arylesterase (ARE) activities were measured only in serum. Statistically significant differences were found for all antioxidant measurements (GSH levels and CAT, SOD, GSH-Px activities in the serum and tissue, MDA levels in the tissue, and PON and ARE activities in the serum) between the four groups. In the curcumin group, serum SOD, ARE, and PON and tissue GSH values were higher than the control group. Moreover, tissue GSH levels and serum GSH-Px activities in the curcumin group were higher than in the AR+NoTr group. In the azelastine group, except MDA, antioxidant measurement values were lower than in the other groups. Curcumin may help to increase antioxidant enzymes and decrease oxidative stress in allergic rhinitis. We recommend curcumin to decrease oxidative stress in allergic rhinitis.

Efficacy and safety of azelastine 0.15% nasal spray administered once daily in patients with allergy to Texas mountain cedar pollen

A previous study with azelastine nasal spray in patients with seasonal allergic rhinitis (SAR) demonstrated that increasing the azelastine concentration from 0.1% to 0.15% allowed for once-daily dosing without increasing the incidence of adverse effects. This study evaluated the efficacy of azelastine 0.15% nasal spray administered once daily for treating symptoms of SAR. In this 14-day, randomized, double-blind, placebo-controlled study, patients with moderate-to-severe SAR were randomized to azelastine 0.15% (n = 251) or placebo (n = 255), both at a dosage of 2 sprays/nostril once daily. The primary efficacy variable was change from baseline in the 12-hour reflective Total Nasal Symptom Score (TNSS). Key secondary variables were change from baseline in 24-hour instantaneous TNSS, to establish the dosing interval, and change from baseline in the Total Ocular Symptom Score (TOSS). The mean improvement (3.57) and percentage improvement (19.3%) in 12-hour reflective TNSS was significant (p < 0.012) with azelastine 0.15% compared to placebo (2.14 and 11.4%, respectively). The mean improvement in 24-hour instantaneous TNSS was also significant (p < 0.001) for azelastine 0.15% compared to placebo, indicating efficacy with once-daily dosing. The overall improvement and percentage improvement in TOSS was significant (p ≤ 0.012) with azelastine 0.15% (2.21 and 16.7%, respectively) compared to placebo (1.28 and 6.0%, respectively). The overall score for the Rhinoconjunctivitis Quality of Life Questionnaire (RQLQ) was significantly (p < 0.001) improved from baseline in the azelastine group compared with the placebo group. Nasal discomfort (3.6%) and bitter taste (2.4%) were the most common adverse events. There were no reports of somnolence with azelastine. Azelastine 0.15% was effective and well tolerated with once-daily dosing. Azelastine 0.15% nasal spray significantly improved a complex of eye symptoms compared to placebo.

Effects of Ototopical Antihistamine on Otitis Media in an Allergic Rat

A reliable model of allergy has been created in the Brown Norway rat. In this model, allergen presentation to the middle ear causes functional disruption of the eustachian tube, predisposing to the development of otitis media with effusion. The purpose of this study was to study the effects of ototopical antihistamine on lipopolysaccharide (LPS)-induced otitis media in the allergic rat model. Prospective animal-based research study. Fifteen (n = 15) rats were made allergic via sensitization to ovalbumin (OVA) by subcutaneous injection and randomized into three groups: saline (SAL) + LPS, olopatadine (OLO) + LPS, and azelastine (AZE) + LPS. Allergic rats were transtympanically injected with OVA 24 hours prior to challenge, creating a subclinical inflammatory response in which there is no visible middle ear effusion. Thirty-five microliters of test substance (SAL + LPS, OLO + LPS, or AZE + LPS) were injected into the middle ear at 0, 2, and 4 hours. Effusion was collected at 2, 4, and 6 hours. Statistical analysis was performed on effusion volume and albumin concentration. Significant increase in effusion volume with respect to time was noted for the SAL + LPS group, whereas the AZE + LPS group demonstrated a decrease. Intergroup comparison revealed a significant decrease in effusion volume at hour 6, with both AZE and OLO less than LPS alone. A significant decrease in albumin concentration over time was noted in the AZE group. Intergroup comparison revealed a significant difference inalbumin concentration at hour 6, with OLO significantly lower than LPS. Ototopical antihistamines are effective in reducing effusion volume and albumin concentration in LPS-induced otitis media in an allergic rat model. This finding supports the hypothesis that ototopic antihistamines may prove effective in treating patients with allergy-induced eustachian tube dysfunction.

Azelastine Nasal Spray and Fluticasone Nasal Spray in the Treatment of Geriatric Patients with Rhinitis

Treatment of Geriatric Patients with Rhinitis V. B. Behncke1, G. Alemar2, D. A. Kaufman1, F. J. Eidelman1; 1Allergy and Immunology, Cleveland Clinic Florida, Weston, FL, 2Otorhinolaryngology, Cleveland Clinic Florida, Weston, FL. RATIONALE: The prevalence and differential diagnosis of rhinitis changes over time, with nonallergic rhinitis increasingly prevalent in the fifth decade of life. This study was conducted to evaluate the effect of an antihistamine nasal spray (azelastine hydrochloride) and a corticosteroid nasal spray (fluticasone propionate) in treating geriatric patients with allergic or nonallergic rhinitis. METHODS: This was an open-label trial in 18 patients 65 years and older with a history of moderate-to-severe rhinitis. Eligible patients were randomized to treatment with either azelastine nasal spray 2 sprays per nostril bid (1.1 mg) or fluticasone 2 sprays per nostril qd (200 mcg) for a 6-week study period. The primary outcome variable was quality of life as assessed by the Rhinitis Quality of Life Questionnaire (RQLQ). Patients completed the RQLQ at baseline and at week 3 and week 6. Patients also recorded symptoms and side effects each day in a diary. RESULTS: Three patients had positive allergen skin tests and 15 had negative skin tests. Both treatments led to significant improvement from baseline in the RQLQ score after 3 and 6 weeks of treatment and there were no significant differences between treatment groups. Both treatments improved symptom scores compared to baseline, with statistically significant improvement at week 2 through 6 in the fluticasone group and at week 4 in the azelastine group. There were no significant differences between azelastine and fluticasone at week 6. CONCLUSIONS: Azelastine nasal spray and fluticasone nasal spray improved RQLQ scores and rhinitis symptom scores in geriatric patients with either allergic or nonallergic rhinitis.

The effects of ototopical antihistamine on allergic induced otitis media

Problem: A reliable model of allergic otitis media has been created in the Brown-Norway (BN) rat. In the presensitized rat, allergen presentation to the middle ear causes functional disruption of the eustacian tube predisposing to the development of otitis media with effusion. The purpose of this study was to determine the effects of ototopical antihistamine on lipopolysaccharide (LPS) induced otitis media in the sensitized BN rat. Methods: Fifteen rats were randomized into 3 groups: LPS, olopatadine+LPS, and azelastine+LPS. The rats were sensitized to ovalbumin (OVA) by subcutaneous injection mixed with aluminum hydroxide. Sensitized rats were transtympanically injected with ovalbumin 24 hours prior to challenge creating a subclinical inflammatory response. 35 μL of test substance was injected into the middle ear at 0, 2, and 4 hours. Effusion was collected at 2, 4, and 6 hours. Statistical analysis was performed on effusion volume and albumin concentration. Results: Significant increase in effusion volume with respect to time was noted for the LPS group while the azelastine group demonstrated a decrease. Intergroup comparision revealed a significant decrease in effusion volume at hour 6, with both azelastine and olopatidine less than LPS alone. A significant decrease in albumin concentration over time was noted in the azelastine group. Intergroup comparison revealed significant difference in albumin concentration at hour 6, with patanol significantly lower than LPS. Conclusion: Ototopical antihistamines seem effective in reducing effusion volume and albumin concentration in allergic otitis media. The Brown-Norway rat is an excellent model for assessing the effects of allergy on the dynamic function of the eustacian tube. Significance: Topical antihistamine is commonplace as current clinical indications include both nasal ond ocular application. Ototopical antihistamine, through a patent pressure equalization tube, may have a future role as allergy has been hypothesized to significantly contribute to approximately 15% of otitis media with effusion. Support: None reported.

Vasomotor Rhinitis: Clinical Efficacy of Azelastine Nasal Spray in Comparison with Placebo

The H₁ antagonist azelastine is used in nasal sprays for the treatment of allergic rhinitis, but its therapeutic efficacy in vasomotor rhinitis is unknown. We performed a multicenter randomized double-blind placebo-controlled study of the efficacy and tolerance of azelastine nasal spray in 89 adult patients with vasomotor rhinitis (confirmed by negative Phadiatop). Following a washout period, patients were treated for 15 days with one puff three times daily per nostril of azelastine (n = 44) or placebo (n = 45) nasal spray. Efficacy was evaluated by the reduction in symptomatology and by rhinoscopy. Intent-to-treat analysis revealed better results in the azelastine group for all assessed symptoms; the significance level was reached for nasal obstruction on day 15 (p = 0.042). Using per protocol analysis (in 85 patients complying with the protocol), the significance level was reached for nasal obstruction on day 15 (p = 0.017) and for the percentage of success in rhinorrhea (p = 0.023). In the azelastine group, rhinoscopy examination showed a significantly higher reduction in the inflammatory level and edema of the nasal mucosa (p = 0.03 and 0.02 for VAS on day 15 respectively, per protocol analysis). General efficacy assessment by the physician and the patient was in favor of azelastine (with significance levels <0.01). No drowsiness or serious adverse event was reported, and the frequency of mouth dryness and headaches was similar in the two treatment groups. The present study demonstrates the efficacy of azelastine nasal spray in the treatment of vasomotor rhinitis. The best achieved results were a decrease in nasal obstruction and mucosal edema. Further studies are required to investigate if this therapeutic benefit results from H₁ antagonism or from another, not well-characterized pharmacological action of azelastine.

Efficacy of azelastine nasal spray in the treatment of vasomotor (perennial nonallergic) rhinitis

Azelastine hydrochloride is an antihistamine with anti-inflammatory properties that is available in the United States in a nasal spray formulation for the treatment of seasonal allergic rhinitis. Vasomotor (perennial nonallergic) rhinitis (VMR) is a noninfectious, chronic rhinitis usually not associated with inflammatory cell infiltration. Two multicenter, randomized, double-blind, placebo-controlled, parallel-group clinical trials were conducted to determine whether patients with symptoms of VMR (rhinorrhea, sneezing, postnasal drip, and nasal congestion) could be effectively treated with azelastine nasal spray. All of the patients who participated in the trials had a diagnosis of VMR, symptoms for at least 1 year, negative skin tests for a mixed panel of seasonal and perennial allergens, and a nasal cytology examination negative for eosinophils. After a 1-week, single-blind, placebo lead-in period, patients who met the symptom severity qualification criteria were randomized to receive either azelastine nasal spray (two sprays per nostril twice daily, 1.1 mg/day) or placebo nasal spray for 21 days. Patients recorded the severity of their VMR symptoms on diary cards each morning and evening of the trial using a four-point symptom rating scale (0 = none to 3 = severe). The primary efficacy variable was the overall reduction from baseline in the total vasomotor rhinitis symptom score (TVRSS) over the 21-day, double-blind treatment period. In both studies, azelastine nasal spray significantly (study 1, P = .002; study 2, P = .005) reduced the TVRSS from baseline when compared with placebo. Significant improvement was observed within the first week and improvement in all symptoms favored treatment with azelastine nasal spray. No serious or unexpected adverse events were reported in either study. Bitter taste (19% vs 2%) was the only adverse experience that occurred with a statistically significantly greater incidence in the azelastine group than in the placebo group. This is the first demonstration of the efficacy of an antihistamine in the therapy of VMR in two double-blind, placebo-controlled clinical trials.

Effect of topical nasal azelastine on the symptoms of rhinitis, sleep, and daytime somnolence in perennial allergic rhinitis

Recent data suggested that daytime somnolence in patients with allergic rhinitis was secondary to disrupted sleep caused by nasal congestion. Medications, which decreased congestion, would be expected to improve sleep and daytime somnolence. Previously, we demonstrated that nasal steroids improved all three symptoms. The effect of topical nasal antihistamines on these symptoms has yet to be studied. The objective of this 8-week, double-blind, placebo-controlled study was to determine whether topical nasal azelastine was effective at decreasing congestion, daytime somnolence, and improving sleep. We recruited 24 subjects with perennial allergic rhinitis and randomized them in a double-blinded, crossover fashion, to receive placebo or azelastine two sprays BID, using Balaam's design. Questionnaires, daily diary, and Epworth Sleepiness Scale were used as tools. The last 2 weeks of each 4-week treatment period were summarized, scored, and compared by PROC MIXED in SAS. The analysis of the Rhinitis Severity Score showed significant improvement only of rhinorrhea in the azelastine group (P = .03). The symptom severity of nasal congestion and daytime somnolence was not significantly different between placebo and azelastine. Subjects considered azelastine effective at improving their sleep (P = .04), but daytime somnolence (P = .06) and congestion (P = .09) were not statistically improved. Azelastine is effective in reducing rhinorrhea and improving sleep quality. We were unable to demonstrate that azelastine can significantly reduce the severity of congestion or daytime somnolence.

The effect of azelastine on acute radiation dermatitis in mice models

In our previous report we described the clinical value of azelastine, an oral antiallergic agent, as an inhibitor of radiation dermatitis. Here we studied the effect of azelastine on normal skin and tumor size after irradiation in a mouse model. The modifying effects of azelastine on both the degree of radiation dermatitis and antitumoral effect of radiation therapy were investigated in the normal skin as well as in SCC VII tumors of C3H/He mice. The right hind legs, with or without tumors, were irradiated with 20-60 Gy at 0.62 Gy/min. Azelastine was administered via the mouse chow, and acute skin reactions and tumor growth curves were compared between the azelastine and control groups. The acute skin reactions of the azelastine group were significantly less prominent than those of the control group (p < 0.01). At a dose of 40 Gy the dose modification factors were 1.19-1.25. The tumor growth curves of the azelastine and control groups were almost identical, indicating that the treatment response of irradiation was not affected by administration of azelastine. Application of azelastine reduces the degree of acute radiation dermatitis without affecting the antitumoral effect of radiation therapy.

A randomized double-blind placebo controlled study of azelastine nasal spray in children with perennial rhinitis

One hundred and twenty five children (median age 8.71 years) suffering from perennial allergic rhinitis were treated in a randomized, double-blind, parallel group study comparing azelastine nasal spray 0.14 mg/nostril twice daily (0.56 mg/day) and placebo nasal spray. Medication was given for a period of 6 weeks which followed a 2 week placebo washout period in all patients. Subjects were aged between 5 and 12 and were skin prick positive to either house dust mites and/or cat or dog dander. Concomitant anti allergic treatment was not permitted during the study. Severity of rhinitis symptoms was scored daily by the child or his/her parents on a diary card using a visual analogue scale (VAS) for each evaluated symptom: 0, absent-100, could not be worse. Mean weekly scores were calculated. Symptoms evaluated were: sneezing, nasal blockage, nasal itch and rhinorrhea. In addition, at each clinic visit the investigator evaluated symptoms using a verbal score of 0, no symptom-3, severe. Compared to the baseline, for each of the six study weeks, the reduction in the VAS scores for all four symptoms was statistically greater for the azelastine group compared to the placebo group. The investigator's assessment at clinic visits bore out these results. Both azelastine nasal spray and placebo were well tolerated, no serious adverse events were reported. During the treatment phase of the study a total of 36 adverse events were reported by 25 patients (azelastine 10, placebo 15). The most frequently occurring events were pharyngitis (azelastine 5, placebo 3), cough (azelastine 3, placebo 1) and bronchitis (azelastine 1, placebo 3). In conclusion, azelastine has been shown to be effective in the treatment of perennial rhinitis in children aged 5–12 years and to be superior to placebo in the relief of all symptoms assessed, namely sneezing, nasal blockage, nasal itch and rhinorrhea.

An evaluation of the efficacy and safety of azelastine in patients with chronic asthma

BACKGROUND: Azelastine, an oral nonsteroidal, antiinflammatory drug with a good safety profile, has demonstrated relief of symptoms in patients with asthma. OBJECTIVE: The study was designed to evaluate the efficacy and safety of azelastine, a novel antiallergy compound, in patients with asthma who required maintenance therapy. METHODS: During this 16-week, double-blind, randomized, parallel-group study, patients received orally administered azelastine (4 mg twice daily), albuterol sulfate (4 mg twice daily), or placebo. RESULTS: Overall, patients in the azelastine group used 2.5 times less backup medication (p = 0.024) for relief of their asthma symptoms than patients in the placebo group. Reductions in asthma symptoms in the azelastine group were also noted throughout the double-blind treatment period. Moreover, the azelastine group had statistically significant improvements in FEV1 after the first dose of medication. The only notable adverse experiences in the azelastine group were alterations in taste perception and a small mean increase in body weight. CONCLUSION: Oral administration of azelastine to patients with asthma resulted in overall improvement in airway function while reducing the requirement for adjunctive antiasthma medications. (J ALLERGY CLIN IMMUNOL 1996;97:1218-24.)

Corticosteroid-sparing effect of azelastine in the management of bronchial asthma.

The objective of this double-blind trial was to evaluate the corticosteroid-sparing effect of azelastine in patients with chronic bronchial asthma. A total of 193 subjects received either 6 mg of azelastine twice per day or placebo (in a 2:1 ratio) in combination with beclomethasone dipropionate (6 to 16 inhalations per day). The number of daily inhalations of the corticosteroid was reduced until maximum reduction or elimination was achieved. Patients then entered a 12-wk maintenance period, during which patients were maintained on their lowest possible dose of inhaled corticosteroid. Compared with placebo, the azelastine group had a statistically significantly greater overall median reduction in inhaled corticosteroids (4.9 puffs/day for azelastine versus 3.1 puffs/day for placebo; p < or = 0.010) during the maintenance period. The azelastine group also had a statistically significantly higher percentage of patients with reductions of > or = 50% and > or = 75% from the baseline level (53 and 31%, respectively, for azelastine versus 34 and 14%, respectively, for placebo; p < or = 0.028). The results demonstrated that azelastine, 6 mg twice per day, can reduce the need for inhaled corticosteroids in patients with chronic bronchial asthma and not lead to a deterioration in pulmonary function.

Effect of intranasal azelastine and beclomethasone dipropionate on nasal symptoms, nasal cytology, and bronchial responsiveness to methacholine in allergic rhinitis in response to grass pollens

Background:We compared the effect of nasal azelastine (0.56 mg/day), nasal beclomethasone dipropionate (BDP, 200 μg/day) and matched placebo on seasonal symptoms, nasal cytology, and the increase in bronchial responsiveness occurring during pollen season in a group of subjects with history of allergic rhinitis to grass pollens only. Methods: The study was completed by nine subjects in the azelastine group, 13 subjects in the BDP group, and 13 subjects in the placebo group. Treatments were randomly administered for 6 weeks. Each subject recorded daily nasal, eye and chest symptoms and additional treatment requirement for the entire pollen season. Each subject performed nasal lavage 4 weeks into the pollen season. Bronchial responsiveness to methacholine was measured before and 4 weeks into the pollen season. Response was expressed as provocative dose causing a 20% fall in forced expiratory volume in 1 second in micromoles. Results:Azelastine-treated subjects had significantly fewer nasal symptoms during week 4 (p < 0.05), and BDP-treated subjects had fewer nasal symptoms during week 4 (p < 0.05) and week 5 (p < 0.05) compared with subjects given placebo. Both treatments significantly reduced the need for additional medications. BDP, but not azelastine, treatment significantly reduced the percent of eosinophils recovered in nasal lavage (p < 0.05). Neither azelastine nor BDP protected against the increase in bronchial responsiveness to methacholine occurring during the pollen season. Conclusion:We demonstrated that both azelastine and BDP are effective treatments for nasal symptoms of seasonal allergic rhinitis after 4 weeks of therapy. However, we were not able to demonstrate an antiinflammatory activity of nasally administered azelastine. Nasal therapy with azelastine and BDP did not block the increase in bronchial responsiveness to methacholine caused by seasonal allergen exposure. (J ALLERGY CLIN IMMUNOL 1995;95:515-23.)

A double-blind, controlled trial to assess the safety and efficacy of azelastine nasal spray in seasonal allergic rhinitis

Background: Azelastine solution is a topically (nasal) administered antiallergy drug with a preclinical profile suggestive of efficacy in patients with allergic rhinitis. Objectives: The study was designed to compare the effectiveness and safety of two dosages of azelastine nasal spray (2 sprays per nostril once daily and twice daily) with that of placebo in the treatment of patients with symptomatic seasonal allergic rhinitis. Methods: Two hundred fifty-one patients (12 years of age or older) were randomized to treatment in this 2-week, double-blind, parallel-group study. Primary efficacy variables were Major Symptom Complex (nose blows, sneezes, runny nose, itchy nose, watery eyes) and Total Symptoms Complex (Major Symptom Complex plus itchy eyes/ears/throat/palate, cough, postnasal drip). Results: Patients treated with azelastine had mean percent improvements in Total and Major Symptom Complex scores that were consistently superior to placebo at each evaluation point. Overall, improvements were statistically significant ( p ⩽ 0.05) in the Total Symptoms Complex for both azelastine groups and in the Major Symptom Complex for the twice daily group with a trend toward statistical significance for the once daily group. Azelastine was superior to placebo in improving all individual rhinitis symptoms. Adverse experiences in the azelastine groups were minor and infrequent. Conclusion: The results support the efficacy and safety of azelastine nasal spray in the treatment of seasonal allergic rhinitis.

The Effectiveness of Oral Azelastine in the Management of Perennial Allergic Rhinitis

Azelastine, a phthalazinone derivative, is a chemically novel antiallergy compound that inhibits inflammatory responses in the upper and lower airway. Previous clinical trials demonstrated the effectiveness of azelastine in the treatment of allergic rhinitis. The objective of this double-blind trial was to further evaluate the efficacy and safety of oral azelastine compared with placebo in patients with perennial allergic rhinitis. A total of 192 patients (between 13 and 60 years of age) who satisfied a minimum symptom score during a single-blind placebo evaluation period were randomized to receive one of three treatments: 2 mg of azelastine b.i.d., 1.34 mg of clemastine fumarate b.i.d., or placebo b.i.d. for a 4-week double-blind treatment period. In the primary efficacy analysis, rhinitis symptoms were analyzed as a Total Symptom Complex severity score (nose blows, runny nose, sneezes, stuffy nose, itchy nose, and itchy eyes/ears/throat). After 2 and 4 weeks of therapy, the azelastine group had greater mean percent improvements than the placebo group in the Total Symptom Complex severity scores. The overall and endpoint improvements for the azelastine group were statistically significant (P ≤ .026) versus placebo. Improvements in individual rhinitis symptoms for the azelastine group were superior to placebo for nose blows, runny nose, sneezes, itchy nose, and itchy eyes/ears/throat. Azelastine was well tolerated. Clemastine was also significantly more effective than placebo and was well tolerated. The results support oral azelastine's safety and effectiveness in the treatment of perennial allergic rhinitis.