Alternative Prescription Allergy Medicines to Levocetirizine (Xyzal)
For patients requiring an alternative to levocetirizine, other second-generation antihistamines including desloratadine, fexofenadine, and loratadine are recommended first-line options due to their efficacy and favorable side effect profiles. 1
Second-Generation Antihistamine Options
Non-Sedating Options
- Fexofenadine - Completely non-sedating even at higher than recommended doses, making it an excellent alternative for patients who need to remain alert 1
- Loratadine - Non-sedating at recommended doses, though may cause sedation at higher doses 1
- Desloratadine - Non-sedating at recommended doses with the longest elimination half-life (27 hours) 1
Mildly Sedating Options
- Cetirizine - May cause mild sedation (13.7% vs 6.3% for placebo), especially at higher doses 1
Clinical Considerations for Selection
Efficacy Comparison
- All second-generation antihistamines have similar overall efficacy profiles for allergic conditions 1
- Some comparative studies suggest levocetirizine may have better efficacy than desloratadine, loratadine, or fexofenadine in allergen challenge studies, but no single agent has been conclusively proven superior in real-world settings 2, 1
Special Populations
Renal Impairment
- Avoid acrivastine in moderate renal impairment 1
- Use loratadine or desloratadine with caution in severe renal impairment 1
- Cetirizine dose should be halved in moderate renal impairment 1
Hepatic Impairment
- Avoid mizolastine in significant hepatic impairment 1
- Avoid chlorphenamine and hydroxyzine in severe liver disease 1
Pregnancy
- All antihistamines should ideally be avoided in pregnancy, especially during the first trimester 1
- If treatment is necessary, chlorphenamine has the longest safety record 1
- Loratadine and cetirizine are classified as FDA Pregnancy Category B drugs 1
Additional Treatment Options
Intranasal Antihistamines
- Azelastine and olopatadine nasal sprays are effective alternatives for allergic rhinitis 1
- These may be considered as first-line treatment for allergic and non-allergic rhinitis 1
- Note that intranasal antihistamines may cause sedation (particularly azelastine) and bitter taste 1
Combination Therapy Options
- Adding an H2 antihistamine to an H1 antihistamine may provide better control of urticaria in some patients 1
- For allergic rhinitis, oral antileukotriene agents (like montelukast) alone or in combination with antihistamines have proven useful 1
Practical Prescribing Algorithm
- First try fexofenadine if alertness is critical (driving, operating machinery, etc.) 1
- Consider loratadine or desloratadine if once-daily dosing is preferred 1
- Try cetirizine if a stronger antihistamine effect is needed and mild sedation is acceptable 1
- Consider intranasal antihistamines for predominant nasal symptoms 1
- For urticaria not responding to single agents, consider increasing the dose of the second-generation antihistamine above the licensed recommendation when benefits outweigh risks 1
Common Pitfalls to Avoid
- Don't assume all second-generation antihistamines have identical side effect profiles - there are important differences in sedation potential 1
- Avoid first-generation antihistamines for daytime use due to significant sedation and performance impairment 1
- Remember that individual response to antihistamines varies - patients should be offered at least two different options if the first is ineffective 1
- Be aware that desloratadine has the longest elimination half-life and should be discontinued 6 days before skin prick testing 1