====== Second-Generation H1 Antihistamines ====== These agents are selective peripheral H1 receptor inverse agonists with minimal central nervous system penetration. Primary use: * [[allergy:clinical:allergic_rhinitis|Allergic Rhinitis]] * Chronic urticaria * Pruritus ---- ===== Side-by-Side Comparison ===== ^ Drug ^ Usual Adult Dose ^ Sedation Risk ^ Elimination ^ Unique Feature ^ | [[allergy:drugs:loratadine|Loratadine]] | 10 mg daily | Very low | Hepatic (CYP3A4) | Prodrug | | [[allergy:drugs:desloratadine|Desloratadine]] | 5 mg daily | Very low | Hepatic | Active metabolite | | [[allergy:drugs:cetirizine|Cetirizine]] | 10 mg daily | Low | Renal | Active metabolite of hydroxyzine | | [[allergy:drugs:levocetirizine|Levocetirizine]] | 5 mg daily | Low | Renal | R-enantiomer refinement | | [[allergy:drugs:fexofenadine|Fexofenadine]] | 180 mg daily | Minimal | Renal/Fecal | Least sedating | ---- ===== Sedation Spectrum (Low → Higher) ===== * [[allergy:drugs:fexofenadine|Fexofenadine]] * [[allergy:drugs:loratadine|Loratadine]] * [[allergy:drugs:desloratadine|Desloratadine]] * [[allergy:drugs:cetirizine|Cetirizine]] * [[allergy:drugs:levocetirizine|Levocetirizine]] (Note: All far less sedating than first-generation agents.) ---- ===== Clinical Selection Guide ===== If daytime alertness is critical: [[allergy:drugs:fexofenadine|Fexofenadine]] If patient has hepatic impairment: [[allergy:drugs:cetirizine|Cetirizine]] or [[allergy:drugs:levocetirizine|Levocetirizine]] If patient has renal impairment: [[allergy:drugs:loratadine|Loratadine]] or [[allergy:drugs:desloratadine|Desloratadine]] If chronic urticaria: [[allergy:drugs:cetirizine|Cetirizine]] commonly effective ---- ===== Key Board Pearls ===== * Second-generation agents have minimal anticholinergic effects. * Intranasal corticosteroids are superior for nasal congestion. * Sedation varies within the class. * Fexofenadine has the cleanest CNS profile. * Cetirizine and levocetirizine require renal dose adjustment.