Fexofenadine: Primary Indications and Use
Fexofenadine is FDA-approved for treating seasonal allergic rhinitis and chronic idiopathic urticaria in adults and children 6 years and older, with specific advantages in patients requiring a truly non-sedating antihistamine, particularly those with kidney disease, liver disease, or at risk of falls. 1
FDA-Approved Indications
Seasonal Allergic Rhinitis
- Adults and children ≥12 years: 60 mg twice daily or 180 mg once daily 1
- Children 6-11 years: 30 mg twice daily 1
- Effectively treats sneezing, rhinorrhea, itchy nose/palate/throat, and itchy/watery/red eyes 1
- Has limited effect on nasal congestion, similar to other oral antihistamines 2, 3
Chronic Idiopathic Urticaria
- Adults and children ≥12 years: 60 mg twice daily or 180 mg once daily 1
- Children 6-11 years: 30 mg twice daily 1
- Significantly reduces pruritus and number of wheals 1, 4
- Effective for up to 6 weeks of continuous treatment 3
Critical Advantages in Special Populations
Patients with Kidney Disease
- Dose adjustment required: Start with 60 mg once daily (instead of twice daily or 180 mg) in adults with decreased renal function 1
- Pediatric adjustment: 30 mg once daily in children 6-11 years with renal impairment 1
- Unlike cetirizine, which requires 50% dose reduction in moderate renal impairment and should be avoided in severe renal impairment, fexofenadine has a simpler dosing adjustment 2, 5
Patients with Liver Disease
- No hepatic contraindications: Unlike mizolastine (contraindicated in significant hepatic impairment) and alimemazine (hepatotoxic), fexofenadine can be safely used in liver disease 2
- Does not undergo hepatic metabolism via cytochrome P450 CYP 3A4, avoiding drug interactions common with hepatically metabolized antihistamines 6
Patients at Risk of Falls or Requiring Alertness
- Truly non-sedating: Fexofenadine maintains non-sedating properties even at doses exceeding FDA recommendations (up to 240 mg/day), making it the gold standard when sedation must be absolutely avoided 5, 7
- No psychomotor impairment: Does not cross the blood-brain barrier and shows no dose-related increase in sedation 3, 7
- Preferred in elderly: Particularly advantageous for older adults who are more sensitive to psychomotor impairment and fall risk from other antihistamines 5
Comparison with Other Second-Generation Antihistamines
Non-Sedating Profile
- Fexofenadine: Completely non-sedating at all doses 5, 7
- Loratadine/Desloratadine: Non-sedating at recommended doses but may cause sedation at higher doses 2, 5
- Cetirizine/Levocetirizine: May cause mild drowsiness (13.7% vs 6.3% placebo) even at standard doses 5
Clinical Efficacy
- Fexofenadine 120 mg once daily is as effective as cetirizine 10 mg once daily and loratadine 10 mg once daily for overall symptom reduction in seasonal allergic rhinitis 3
- Produces greater improvements in quality of life than loratadine to a clinically meaningful extent 3
- All doses from 60-240 mg twice daily are superior to placebo for chronic urticaria, with 60 mg twice daily being the optimal effective dose 4
Common Pitfalls and Caveats
Drug and Food Interactions
- Avoid with fruit juices: Orange and grapefruit juices significantly reduce fexofenadine bioavailability; always take with water 1, 6
- P-glycoprotein interactions: Although fexofenadine doesn't use CYP 3A4, it interacts at P-glycoprotein and organic anion transporter polypeptides, potentially increasing toxicity risk of other drugs 6
Cardiac Safety
- No cardiotoxicity: Does not inhibit cardiac K+ channels or prolong QT interval, even when combined with erythromycin or ketoconazole 3, 7
- Safe alternative for patients who cannot use terfenadine or astemizole (removed from market for cardiotoxic effects) 2
Limitations
- Nasal congestion: Like all oral antihistamines, fexofenadine has limited effect on nasal congestion; consider adding pseudoephedrine or switching to intranasal corticosteroids for this symptom 2, 3
- Not for anaphylaxis: H1 antihistamines relieve itching and urticaria but do not relieve respiratory symptoms in anaphylaxis 5
Pregnancy Considerations
- Should be avoided in pregnancy, especially during the first trimester, though not shown to be teratogenic in humans 5