Over-the-Counter Oral Antihistamines
The following second-generation oral antihistamines are available over-the-counter (OTC) for allergic symptom relief: cetirizine, loratadine, fexofenadine, and levocetirizine. 1, 2, 3
Second-Generation OTC Antihistamines (Preferred)
These are the preferred first-line agents due to superior safety profiles compared to first-generation antihistamines:
Cetirizine (Zyrtec)
- Dosing: Adults and children ≥6 years: 10 mg once daily 1, 2
- Dosing: Children 2-5 years: 5 mg once daily 1
- Available OTC as tablets and liquid formulations 2
- Most potent antihistamine available but may cause sedation in approximately 10% of patients 4
Loratadine (Claritin)
- Dosing: Adults and children ≥6 years: 10 mg once daily 1
- Dosing: Children 2-5 years: 5 mg once daily 1
- Available OTC 1
- Minimal sedation risk 5
Fexofenadine (Allegra)
- Dosing: Adults and children ≥12 years: 60 mg twice daily or 180 mg once daily 1
- Available OTC 1
- Offers best overall balance of effectiveness and safety with essentially no sedation 4
- May require twice-daily dosing for optimal 24-hour coverage 6
Levocetirizine (Xyzal)
- Dosing: Adults and children ≥12 years: 5 mg once daily 1, 3
- Dosing: Children 6-11 years: 2.5 mg once daily 1
- Available OTC as "original prescription strength" 3
- Highly potent but may cause somnolence in susceptible individuals 6
Important Safety Considerations
First-generation antihistamines (diphenhydramine, chlorpheniramine) should be avoided despite OTC availability due to significant sedation, cognitive impairment, anticholinergic effects, and documented fatalities, particularly in children under 6 years. 1, 7, 8
Key Advantages of Second-Generation Agents
- Minimal to no sedation (except cetirizine in ~10% of patients) 4
- Once or twice-daily dosing improves adherence 5
- No anticholinergic effects 8
- Adverse effects similar to placebo overall 4
- Safe for use while driving and working 6
Clinical Pitfalls to Avoid
- Do not use first-generation OTC antihistamines in children under 6 years due to serious safety concerns including 69 documented fatalities (41 in children under 2 years) between 1969-2006 7
- Antihistamines provide limited relief of nasal congestion compared to other symptoms 5
- Second-generation antihistamines are generally more effective for seasonal allergic rhinitis than perennial allergic rhinitis 5
- OTC antihistamines are less effective than intranasal corticosteroids for comprehensive symptom control 1