====== Cetirizine ====== ===== Classification ===== * Second-Generation H1 Antihistamine * Peripheral H1 receptor inverse agonist * Active metabolite of hydroxyzine Parent class: [[allergy:histamine|Histamine & Antihistamines]] ---- ===== Mechanism of Action ===== Cetirizine selectively blocks peripheral H1 receptors. Effects: * ↓ Histamine-mediated vasodilation * ↓ Capillary permeability * ↓ Pruritus * ↓ Sneezing and rhinorrhea Compared to first-generation antihistamines: * Minimal anticholinergic activity * Limited blood-brain barrier penetration * Low but not zero sedation ---- ===== Pharmacokinetics ===== * Oral administration * Rapid onset (~1 hour) * Duration: ~24 hours * Primarily renally eliminated * Minimal hepatic metabolism Dose adjustment required in renal impairment. ---- ===== Indications ===== * [[allergy:clinical:allergic_rhinitis|Allergic Rhinitis]] * Chronic idiopathic urticaria * Seasonal allergies * Pruritus Effective for: * Sneezing * Itching * Rhinorrhea Less effective for: * Nasal congestion (intranasal steroids superior) ---- ===== Dosing (Adult) ===== * 10 mg PO once daily * Consider 5 mg daily in renal impairment Pediatric dosing based on age. ---- ===== Adverse Effects ===== Generally well tolerated. Possible: * Mild drowsiness (more than loratadine) * Fatigue * Dry mouth (rare) Sedation risk: * Higher than loratadine * Lower than diphenhydramine ---- ===== Contraindications / Cautions ===== * Severe renal impairment (dose adjust) * Hypersensitivity Use caution: * Elderly * Concomitant CNS depressants ---- ===== Drug Interactions ===== * Minimal CYP interaction * Additive sedation with alcohol or CNS depressants ---- ===== Clinical Pearls ===== * Slightly more effective for urticaria than loratadine. * Slightly more sedating than loratadine. * Good balance of potency and tolerability. * Renal clearance makes it safer in hepatic disease. ---- ===== Comparison Within Class ===== ^ Drug ^ Sedation Risk ^ Elimination ^ Notes ^ | [[allergy:drugs:loratadine|Loratadine]] | Very low | Hepatic (CYP3A4) | Active metabolite = desloratadine | | [[allergy:drugs:cetirizine|Cetirizine]] | Low | Renal | Active metabolite of hydroxyzine | | [[allergy:drugs:fexofenadine|Fexofenadine]] | Minimal | Renal | Least sedating | ---- ===== Related Pages ===== * [[allergy:histamine|Histamine & Antihistamines]] * [[allergy:drugs:hydroxyzine|Hydroxyzine]] * [[allergy:drugs:levocetirizine|Levocetirizine]] * [[allergy:clinical:allergic_rhinitis|Allergic Rhinitis – Stepwise Therapy]]