====== Loratadine ====== ===== Classification ===== * Second-Generation H1 Antihistamine * Peripheral H1 receptor inverse agonist Parent class: [[allergy:histamine|Histamine & Antihistamines]] ---- ===== Mechanism of Action ===== Loratadine selectively blocks peripheral H1 receptors. * Inhibits histamine-mediated vasodilation * Decreases capillary permeability * Reduces pruritus and sneezing * Minimal blood-brain barrier penetration Result: * ↓ rhinorrhea * ↓ itching * ↓ sneezing * Minimal sedation Unlike first-generation agents, loratadine has minimal central anticholinergic effects. ---- ===== Pharmacokinetics ===== * Oral administration * Hepatic metabolism (CYP3A4, CYP2D6) * Active metabolite: desloratadine * Duration: ~24 hours * Once-daily dosing Avoid strong CYP3A4 inhibitors in high-risk patients. ---- ===== Indications ===== * [[allergy:clinical:allergic_rhinitis|Allergic Rhinitis]] * Chronic idiopathic urticaria * Seasonal allergies * Mild allergic symptoms Not first-line for nasal congestion (intranasal steroids preferred). ---- ===== Dosing (Adult) ===== * 10 mg PO once daily Pediatric dosing varies by age and weight. ---- ===== Adverse Effects ===== Generally well tolerated. Possible: * Mild headache * Dry mouth * Fatigue (rare) Minimal sedation compared to first-generation antihistamines. ---- ===== Contraindications / Cautions ===== * Severe hepatic impairment (dose adjustment may be needed) * Hypersensitivity to drug ---- ===== Drug Interactions ===== * Strong CYP3A4 inhibitors may increase levels * Rare QT prolongation risk (much lower than older agents) ---- ===== Clinical Pearls ===== * Preferred over first-generation antihistamines for daytime use. * Poor for nasal congestion as monotherapy. * Does not significantly impair cognition or psychomotor function. * Once-daily dosing improves adherence. ---- ===== Comparison Within Class ===== ^ Drug ^ Sedation Risk ^ Duration ^ Notes ^ | [[allergy:drugs:loratadine|Loratadine]] | Very low | 24 hr | Active metabolite (desloratadine) | | [[allergy:drugs:cetirizine|Cetirizine]] | Low | 24 hr | Slightly more sedating | | [[allergy:drugs:fexofenadine|Fexofenadine]] | Minimal | 24 hr | Least sedating | ---- ===== Related Pages ===== * [[allergy:histamine|Histamine & Antihistamines]] * [[allergy:clinical:allergic_rhinitis|Allergic Rhinitis – Stepwise Therapy]] * [[allergy:clinical:urticaria_angioedema|Urticaria & Angioedema]]