Azelastine 210micrograms/dose nasal spray

Importance: Limited pharmaceutical options exist for preexposure prophylaxis of COVID-19 beyond vaccination. Azelastine, an antihistamine nasal spray used for decades to treat allergic rhinitis, has in vitro antiviral activity against respiratory viruses, including SARS-CoV-2. Objective: To determine the efficacy and safety of azelastine nasal spray for prevention of SARS-CoV-2 infections in healthy adults. Design, Setting, and Participants: A phase 2, double-blind, placebo-controlled, single-center trial was conducted from March 2023 to July 2024. Healthy adults from the general population were enrolled at the Saarland University Hospital in Germany. Interventions: Participants were randomly assigned 1:1 to receive azelastine, 0.1%, nasal spray or placebo 3 times daily for 56 days. SARS-CoV-2 rapid antigen testing (RAT) was conducted twice weekly, with positive results confirmed by polymerase chain reaction (PCR). Symptomatic participants with negative RAT results underwent multiplex PCR testing for respiratory viruses. Main Outcome: The primary end point was the number of PCR-confirmed SARS-CoV-2 infections during the study. Results: A total of 450 participants were randomized, with 227 assigned to azelastine and 223 to placebo; 299 (66.4%) were female, 151 (33.6%) male, with a mean (SD) age of 33.0 (13.3) years. Most were White (417 [92.7%]), with 4 (0.9%) African, 22 (4.9%) Asian, and 7 (1.6%) of other ethnicity. In the intention-to-treat (ITT) population, the incidence of PCR-confirmed SARS-CoV-2 infection was significantly lower in the azelastine group (n = 5 [2.2%]) compared with the placebo group (n = 15 [6.7%]) (OR, 0.31; 95% CI, 0.11-0.87). As secondary end points, azelastine demonstrated an increase in mean (SD) time to SARS-CoV-2 infection among infected participants (31.2 [9.3] vs 19.5 [14.8] days), a reduction of the overall number of PCR-confirmed symptomatic infections (21 of 227 participants vs 49 of 223 participants), and a lower incidence of PCR-confirmed rhinovirus infections (1.8% vs 6.3%). Adverse events were comparable between the groups. Conclusions and Relevance: In this single-center trial, azelastine nasal spray was associated with reduced risk of SARS-CoV-2 respiratory infections. These findings support the potential of azelastine as a safe prophylactic approach warranting confirmation in larger, multicentric trials. Trial registration: EudraCT number: 2022-003756-13.

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Allergic conjunctivitis is a common ocular condition characterized by discomfort, itching, and redness, which significantly impacts quality of life. Its frequent overlap with dry eye disease (DED) complicates diagnosis and management, as both conditions share inflammation and tear film dysfunction as underlying mechanisms. Effective treatments must address both the inflammatory and tear film aspects of these conditions. While traditional therapies include antihistamines and mast cell stabilizers, innovative approaches focus on agents with dual anti-inflammatory and antiallergic properties. N-acetyl-aspartyl-glutamate (NAAGA) has shown potential in alleviating symptoms of both allergic conjunctivitis and DED through mechanisms involving mast cell stabilization, inhibition of inflammatory mediators, and improvement of tear film stability. This study compares the efficacy of NAAGA and azelastine hydrochloride, an established antihistamine, in improving symptoms and clinical markers of tear film dysfunction in patients with allergic conjunctivitis. This randomized, single-blind study included 134 patients with atopy and mild to moderate tear film dysfunction. Participants received either NAAGA (49 mg/ml, four times daily) or azelastine hydrochloride (0.05%, twice daily) for 4 weeks. The primary endpoint was the change in Ocular Surface Disease Index (OSDI) scores. Secondary endpoints included tear osmolarity, Schirmer test results, tear break-up time (TBUT), fluorescein staining, and matrix metalloproteinase-9 (MMP-9) levels. Both treatments improved all parameters significantly over 4 weeks. NAAGA reduced OSDI scores from 26.12 ± 4.70 to 11.84 ± 3.43, compared to azelastine’s improvement from 24.57 ± 4.70 to 15.54 ± 4.36 (p < 0.001). NAAGA showed superior reductions in tear osmolarity (from 320.99 ± 4.35 to 312.33 ± 3.25 mOsm/l) compared to azelastine (from 320.13 ± 3.46 to 318.57 ± 3.46 mOsm/l, p < 0.001), and greater enhancements in Schirmer test results (6.51 ± 1.95 mm to 10.08 ± 1.88 mm) and TBUT (4.10 ± 1.70 to 7.91 ± 1.79 s). NAAGA outperformed azelastine in alleviating symptoms and improving clinical markers of tear film dysfunction in allergic conjunctivitis. Its dual action on inflammation and tear stability highlights its therapeutic potential. Further studies are warranted to confirm these findings and explore additional applications. ClinicalTrials.gov identifier, NCT12345678. Allergic conjunctivitis, a common cause of red and itchy eyes, often overlaps with dry eye disease, making diagnosis and treatment more complicated. Both conditions share inflammation and tear film instability as underlying causes. In this study, we compared two eye drops: N-acetyl-aspartyl-glutamate (NAAGA)—a non-steroidal anti-inflammatory and mast cell stabilizer—and azelastine—an antihistamine. We found that both treatments improved symptoms such as discomfort and tear instability. However, NAAGA provided greater benefits, improving tear production, reducing eye surface inflammation, and stabilizing the tear film more effectively. NAAGA could be a better choice for patients who also suffer from dry eye along with allergies. Further studies are needed to confirm these findings and to investigate NAAGA’s broader potential in treating ocular surface inflammation.

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Nasal spray treatments that inhibit the Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2) entry into nose and nasopharynx at early stages can be an appropriate approach to stop or delay the progression of the disease. We performed a prospective, randomized, double-blind, placebo-controlled, parallel-group, multicentric, phase II clinical trial comparing the rate of hospitalization due to COVID-19 infection between azelastine 0.1% nasal spray and placebo nasal spray treatment groups. The study furthermore assessed the reduction in virus load in SARS-CoV-2-infected subjects estimated via quantitative reverse transcriptase polymerase chain reaction (RT-PCR) using nasopharyngeal swabs in both groups during the treatment period. A total of 294 subjects with mild COVID-19 infection were screened and randomized in a 1:1 ratio. There was no incidence of COVID-19-related hospitalization in either treatment group. Mean virus load was significantly reduced in both groups during the 11 treatment days as compared with baseline viral load values. The reduction in virus load in the azelastine 0.1% nasal spray group was significantly higher than the reduction in the placebo group at day 11 (log10 5.93 vs. log10 5.85 copies/mL, respectively, p = 0.0041). A total of 39 (32.0%) subjects in the azelastine 0.1% treatment group and 40 (31.0%) subjects in the placebo group reported 48 and 51 adverse events, respectively. It is therefore concluded that azelastine 0.1% nasal spray is an efficacious, safe, and well-tolerated treatment of mild COVID-19 infection.

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Background Prophylactic treatment for pollinosis is advantageous for managing nasal symptoms in patients with seasonal allergic rhinitis. Inadequate control of rhinitis symptoms increases the risk of acute asthma attacks. Nevertheless, there is limited research on the use of nasal glucocorticoids and antihistamines for the preventive treatment of pollinosis. Objective This study aimed to assess the efficacy of prophylactic treatment for nasal symptoms and acute asthma attacks by enrolling patients with Artemisia pollinosis to use a combined device of azelastine hydrochloride and fluticasone nasal spray prior to the pollen season. Methods The study was registered at Chictr.org.cn (ChiCTR2300073758). A total of 120 patients with Artemisia pollinosis were randomly assigned to either a prophylactic treatment group or a control group at a 1:1 ratio. In the prophylactic treatment group, the nasal spray was initiated approximately two weeks before the onset of the pollen season. Results During both the pollen season and the concurrent medication period, the prophylactic treatment group presented significantly lower total nasal symptom scores (TNSS) (means of 5.97 and 5.94) than the control group (means of 7.86 and 7.80) ( P = 0.015 and 0.016). Although the prophylactic treatment group had a lower asthma attack rate than the control group, the difference was not statistically significant ( P = 0.284). Conclusions Prophylactic treatment with azelastine hydrochloride and fluticasone propionate nasal sprays can alleviate nasal symptoms and may reduce acute asthma attacks during the pollen season. Clinical Trial Registration [ Chictr.org.cn ], identifier (ChiCTR2300073758).

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Allergic rhinitis (AR) is a common chronic respiratory disease that significantly impairs the life of children. While a combination intranasal spray of azelastine hydrochloride and fluticasone propionate (Aze-Flu) is an established effective treatment for adults with moderate-to-severe AR, the clinical evidence available in the pediatric population is limited. This review summarizes the current evidence on the efficacy, safety, and impact on Quality of Life (QoL) of Aze-Flu in children. Clinical trials have demonstrated that Aze-Flu provides faster and greater symptom relief in children with AR compared to fluticasone propionate (FP) monotherapy. One randomized controlled trial demonstrated that, although the overall change in the reflective Total Nasal Symptom Score (rTNSS) was not statistically different from the placebo, this was possibly due to rater assessment bias. Children's symptoms self-assessment showed considerable ameliorations in both nasal and ocular scores. Furthermore, treatment with Aze-Flu has been shown to produce clinically relevant and statistically significant improvements in QoL compared to placebo in children with moderate-to-severe seasonal AR. The safety profile is favorable; a 3-month study confirmed that Aze-Flu is well-tolerated, with an incidence of treatment-related adverse events comparable to that of FP monotherapy. Beyond AR, emerging evidence suggests potential benefits of Aze-Flu in children with adenoid hypertrophy. The available evidence supports Aze-Flu as an effective and well-tolerated therapeutic option for children with moderate-to-severe AR, offering superior and faster symptom control than monotherapy and leading to meaningful improvements in quality of life. Future pediatric trials should incorporate validated, child-specific assessment tools to better capture treatment efficacy.

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Background: Symptom control in patients with moderate-to-severe persistent allergic rhinitis (PAR) who remain inadequately controlled on intranasal corticosteroid monotherapy remains challenging, highlighting the urgent need for more effective treatments. This study aimed to determine whether the addition of nasal saline irrigation to a regimen of intranasal corticosteroids and antihistamines can further improve symptoms in patients with moderate-to-severe PAR. Methods: A multicenter, randomized, open-label, controlled trial was conducted, enrolling 248 eligible patients aged 12 years and above from six clinical centers. They were randomized 1:1 into two groups. The experimental group received nasal saline irrigation combined with azelastine-fluticasone (Aze-Flu) nasal spray, and the control group was treated with azelastine nasal spray and fluticasone nasal spray. The primary outcome was the least-squares-mean (LSmean) change in total nasal symptom score (TNSS) from baseline to four weeks, with secondary outcomes including LSmean change in TNSS from baseline to two weeks, subscores, rhinoscopic scores, visual analogue scale (VAS), and rhinoconjunctivitis quality of life questionnaire (RQLQ) scores. Results: < 0.001 at both time points). The experimental group presented more favorable changes in rhinoscopy scores, VAS scores, and RQLQ scores. Both groups showed no substantial differences in adverse events, indicating a comparable safety profile. Conclusion: Nasal saline irrigation combined with Aze-Flu nasal spray provides additional benefits in managing moderate-to-severe PAR, with good safety and tolerability. This combination therapy could be a valuable option in primary care settings. Clinical Trial Registration: http://www.medicalresearch.org.cn, identifier (MR-32-23-044661).

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The incidence of allergic rhinitis (AR) in Asia and the world is steadily rising. Patients experience incomplete symptom relief despite existing treatment options, which warrants the need for new therapeutic regimes. Azelastine hydrochloride/fluticasone propionate (MP-AzeFlu), a novel intranasal formulation of azelastine hydrochloride and fluticasone propionate has been indicated in the treatment of AR. The current review discusses the effects of MP-AzeFlu versus conventional therapies in achieving superior clinical improvement with a very rapid onset of action (5 minutes). The superiority of MP-AzeFlu in offering complete symptom control with sustained relief in patients with AR compared to the existing therapeutic options is also discussed. MP-AzeFlu has been shown to improve the quality of life for patients with AR, thereby enhancing patient adherence to therapy and establishing its preference for the treatment of AR. Currently, the Allergic Rhinitis and its Impact on Asthma (ARIA) guidelines recommend the use of a combination of intranasal corticosteroids and intranasal antihistamines as first-line treatment in patients with persistent AR with visual analog scores ≥5 or when prior treatment with single agents has been ineffective. Widely published data on the efficacy and safety of its prolonged use in adults and children have validated that effective treatment of AR can be achieved with MP-AzeFlu.

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This study provides the first evidence that azelastine may be novel therapeutics for CRC treatment. ARF1 promotes colon tumorigenesis, representing a promising biomarker and therapeutic target in CRC.

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In order to increase bioavailability and intranasal absorbance, the current work set out to create azelastine nasal spray based on nanosuspension. Chondroitin was utilized as a polymer to prepare azelastine nanosuspension through the precipitation procedure. A size of 500 nm and a polydispersity index of 0.276 with a negative potential (-20 mV) were achieved. X-ray diffraction, scanning electron microscopy, Fourier transform infrared spectroscopy, thermal analysis including differential scanning calorimetry and thermogravimetric analysis, in vitro release, and diffusion studies were used to characterize the optimized nanosuspension. MTT assay was used to assess the viability of the cells, and hemolysis assay was used to assess the blood compatibility. Using RNA extraction and reverse transcription polymerase chain reaction, the levels of the anti-inflammatory cytokine IL-4, which is most closely related to cytokines in allergic rhinitis, were measured in mouse lungs. The drug dissolution and diffusion study indicated 2.0-fold increase compared to pure reference sample. Therefore, the azelastine nanosuspension could be suggested as a practical and simple nanosystem for intranasal delivery with improved permeability and bioavailability. The outcome obtained in this study indicated that azelastine nanosuspension has great potential to treat allergic rhinitis as intranasal treatment.

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