From the Guidelines
Second-generation antihistamines are the best type of antihistamine for allergic rhinitis.
Key Characteristics
- They have less or no tendency to cause sedation, performance impairment, and anticholinergic effects compared to first-generation antihistamines 1.
- Examples of second-generation antihistamines include fexofenadine, loratadine, and desloratadine, which do not cause sedation at recommended doses 1.
- Cetirizine and intranasal azelastine may cause sedation at recommended doses, but the effect is generally milder than that observed with first-generation antihistamines 1.
Therapeutic Considerations
- Second-generation antihistamines are generally preferred over first-generation antihistamines due to their lower risk of adverse effects 1.
- They are effective in reducing rhinorrhea, sneezing, and itching associated with allergic rhinitis, but have little objective effect on nasal congestion 1.
- Intranasal antihistamines, such as azelastine, may be useful alternatives to oral antihistamines, but may cause sedation in some patients and/or have a bitter taste 1.
Clinical Guidelines
- The use of first-generation antihistamines should be approached with caution, especially in older adults, due to their potential to cause sedation, performance impairment, and anticholinergic effects 1.
- Second-generation antihistamines are generally recommended as the first-line treatment for allergic rhinitis, due to their efficacy and safety profile 1.
From the Research
Types of Antihistamines
- Second-generation antihistamines, such as fexofenadine and bilastine, are recommended for first-line therapy of allergic rhinitis due to their non-sedating properties 2.
- Bilastine has a more potent binding affinity to the H₁ receptor and its action tends to last longer compared to fexofenadine 2.
- Chlorpheniramine is considered a reasonable initial antihistaminic agent, but a nonsedating antihistamine should be used initially if a patient is involved in activities where drowsiness is dangerous 3.
Administration Routes
- Both oral and intranasal antihistamines are approved for the first-line treatment of allergic rhinitis and result in a reduction in symptoms and an improvement in quality of life 4.
- Intranasal agents may be preferred in patients with nasal congestion or when a more rapid onset of action is desired, while oral agents may be better suited for young children or patients with poor medication compliance 4.
Treatment Guidelines
- For mild intermittent or mild persistent allergic rhinitis, first-line treatment may include a second-generation H₁ antihistamine (e.g., cetirizine, fexofenadine, desloratadine, loratadine) or an intranasal antihistamine (e.g., azelastine, olopatadine) 5.
- For persistent moderate to severe allergic rhinitis, initial treatment should be an intranasal corticosteroid, either alone or in combination with an intranasal antihistamine 5.
Mechanism of Action
- Intranasal antihistamines have broad anti-inflammatory effects, involving multiple pathways and mediators, including histamine, leukotrienes, and cytokines 6.
- These anti-inflammatory actions may contribute to the effectiveness of intranasal antihistamines in relieving symptoms of nonallergic rhinitis, where histamine has a lesser role 6.