The Pharmacotherapy of Rhinitis and Asthma
Pudupakkam K Vedanthan, Harold S Nelson, Shripad N Agashe, PA Mahesh, Rohit Katial in Textbook of Allergy for the Clinician, 2021
Two intranasal antihistamines preparations are available (azelastine and olopatadine). Their onset of action is within 15 to 30 minutes. In comparison studies they have proven of equal or occasionally slightly superior efficacy to the second-generation oral antihistamines (Wallace and Dykewicz 2008). Intranasal antihistamines are equally effective but faster in onset of action as compared with intranasal corticosteroids (Kaliner et al. 2009). In one study comparing intranasal azelastine to intranasal fluticasone, intranasal fluticasone was superior to reducing rhinorrhea, but intranasal azelastine showed comparable efficacy for all other nasal and ocular symptoms. Additionally, compared to baseline ocular symptoms, there was a larger percentage (53.0%) of patients on intranasal azelastine as opposed to intranasal fluticasone (39.6%) that exhibited a 50% reduction in reflective total ocular symptom score by day 14 of treatment (Carr et al. 2012b). The use of intranasal antihistamines in combination with intranasal corticosteroids demonstrates additional symptom reduction and improved quality of life as compared to intranasal antihistamine monotherapy (Brozek et al. 2017). Intranasal antihistamines may have greater efficacy for nasal congestion than oral antihistamines (Brozek et al. 2017). Azelastine is associated with taste perversion and somnolence in some patients (Bousquet et al. 2008), while these symptoms are less frequent with olopatadine (Lieberman et al. 2011).
United Airways
Jonathan A. Bernstein, Mark L. Levy in Clinical Asthma, 2014
Antihistamines are useful for mild symptoms, either intermittent or persistent. In the latter case, regular daily use is advisable because when they are withdrawn the histamine receptor becomes more active and the symptoms can increase. Antihistamines are active against sneezing, rhinorrhea, and nasal itch, but are inferior to nasal corticosteroids in reducing nasal congestion. Most second-generation oral antihistamines (loratidine, cetirizine, fexofenadine, desloratidine, levocetirizine, misolastine, rupatadine) reduce symptoms within 1 hour and are used once daily. Acrivastine is an exception to this rule; it has a rapid onset of action, but lasts only 8 hours. Topical nasal antihistamines are available as azelastine and olopatadine, which have a 15-minute onset of action.
Nasal problems in the athlete
John W. Dickinson, James H. Hull in Complete Guide to Respiratory Care in Athletes, 2020
A number of useful guidelines exist concerning the pharmacological management of allergic rhinitis. The ARIA (Allergic Rhinitis and its Impact on Asthma) document provides a simple system for classification and treatment; the BSACI (British Society of Allergy and Clinical Immunology) has recently published updated detailed guidelines and associated algorithm. In brief, mild symptoms can be treated with an as-required non-sedating anti-histamine, but anything more persistent or troublesome should be treated with an intranasal corticosteroid (see Table 8.1). Nasal corticosteroids are more effective than anti-histamines and the combination of anti-histamine and anti-leukotriene (e.g. montelukast). Many preparations are available, but newer drugs with lower systemic bioavailability (mometasone furoate, fluticasone propionate, fluticasone furoate) are preferable. Regular use and correct application are essential for optimal benefit (Figure 8.5). Failure to respond to an intranasal steroid alone should prompt consideration of a combined corticosteroid plus topical anti-histamine preparation. Anti-cholinergic sprays (ipratropium bromide) can help reduce watery rhinorrhoea. Intranasal steroids also have a beneficial effect on allergic conjunctivitis, but more troublesome symptoms warrant treatment with topical sodium cromoglicate, nedocromil sodium or topical antihistamine (azelastine, olopatadine). Athletes should be treated along the same lines.
Alcaftadine 0.25% versus Olopatadine 0.1% in Preventing Cedar Pollen Allergic Conjunctivitis in Japan: A Randomized Study
Published in Ocular Immunology and Inflammation, 2019
Hiroshi Nakatani, Paul Gomes, Ron Bradford, Qiang Guo, Eleonora Safyan, David A. Hollander
Topical ophthalmic antihistamines remain the primary therapy option for treating allergic conjunctivitis. In the United States, alcaftadine 0.25%11 and olopatadine 0.2%12 are approved once-daily ophthalmic solutions, and olopatadine 0.1%13 is an approved twice-daily ophthalmic solution for allergic conjunctivitis. In Japan, olopatadine 0.1% ophthalmic solution is approved for the treatment of allergic conjunctivitis in a four-times-daily dose, whereas alcaftadine 0.25% ophthalmic solution has yet to be approved. Alcaftadine and olopatadine are classified as dual-action anti-allergic agents, directly inhibiting histamine receptor activation and indirectly preventing allergic responses by stabilizing mast cells.14 Antihistamines have different affinities toward histamine receptors, and thus may potentially have varying effects on mast cell stabilization and anti-inflammatory properties.14,15
Revisiting Ocular Allergy: Evaluating Symptoms, Benzalkonium Chloride and Efficacy of Topical Ketotifen 0.025%
Published in Ocular Immunology and Inflammation, 2020
Kostas G. Boboridis, Nikolaos Kozeis, Anastasios GP. Konstas
The development of newer topical compounds enhanced our treatment options over the last few years. Olopatadine hydrochloride 0.1% was introduced as a promising new dual action anti-allergy ocular medication, showing in clinical trials superior efficacy than Ketotifen 0.025%.4 The presence of BAK in both preparations has undoubtedly influenced their clinical efficacy.3 The release of preservative-free ketotifen 0.025% formulation (Zaditen Oftabak, Thea, France) gained acceptance as an effective unpreserved dual action anti allergic eyedrop in Europe. It exhibited faster resolution of conjunctival hyperemia, favorable reduction of ICAM-1 expression and greater tolerability compared with preserved Olopatadine in a clinical trial on SAC.5 Also, anecdotal data from clinical practice suggests a slight trend in favor of the specific ketotifen preparation over other similar unpreserved compounds of ketotifen possibly due to the presence of excipients or differences in manufacturing process.
Efficacy of Alcaftadine 0.25% (AGN-229666) for Once-daily Prevention of Cedar-Pollen Allergic Conjunctivitis: A Phase 3 Randomized Study
Published in Ocular Immunology and Inflammation, 2021
Hiroshi Fujishima, Tomoko Hasunuma, Tetsuya Kawakita, Takuro Sekiya, Paul Gomes, David A. Hollander
Topical antihistamines represent the primary therapy option for treating AC.10 Alcaftadine 0.25% is approved for once-daily use in the United States11 but is not approved for use in Japan. Olopatadine is approved in once-daily (0.7%, 0.2%) and twice-daily (0.1%) dosing formulations in the US and is also approved as a four-times-daily formulation (Olopatadine 0.1%) in Japan.12–14 Both Alcaftadine and Olopatadine are classified as dual-action anti-allergic agents as they are competitive inhibitors of histamine receptor activation and also mediate a stabilization of mast cells that inhibits IgE-mediated degranulation.15 Alcaftadine is known to protect epithelial tight junction protein markers from allergic inflammation-based degradation while Olopatadine, in contrast, failed to prevent tight junction protein degradation.16 Differences in antihistamine efficacy in relief of AC are potentially due to differences in the relative potency in mediating histamine receptor activation and in the ability of Alcaftadine to prevent epithelial gap junction degradation.15,17
Related Knowledge Centers
- Allergic Conjunctivitis
- Allergic Rhinitis
- Hyperaemia
- Mast Cell Stabilizer
- Pregnancy
- Ophthalmic Drug Administration
- Nasal Administration
- Breastfeeding
- Antihistamine
- Generic Drug