====== Desloratadine ====== ===== Classification ===== * Second-Generation H1 Antihistamine * Selective peripheral H1 receptor inverse agonist * Active metabolite of [[allergy:drugs:loratadine|Loratadine]] Parent class: [[allergy:histamine|Histamine & Antihistamines]] ---- ===== Mechanism of Action ===== Desloratadine selectively blocks peripheral H1 receptors. Effects: * ↓ Histamine-mediated vasodilation * ↓ Capillary permeability * ↓ Pruritus * ↓ Sneezing and rhinorrhea Characteristics: * Minimal blood-brain barrier penetration * Very low sedation risk * Long duration of action ---- ===== Pharmacologic Background ===== Loratadine is metabolized in the liver (CYP3A4, CYP2D6) to desloratadine. Desloratadine: * Is the active metabolite * Does not require hepatic activation * Has longer half-life * Provides consistent 24-hour symptom control Clinically: * Similar efficacy to loratadine * Slightly more predictable pharmacokinetics ---- ===== Pharmacokinetics ===== * Oral administration * Rapid absorption * Duration: ~24 hours * Primarily hepatic metabolism * Eliminated via urine and feces Minimal clinically significant CYP interactions at standard doses. ---- ===== Indications ===== * [[allergy:clinical:allergic_rhinitis|Allergic Rhinitis]] * Chronic idiopathic urticaria * Seasonal allergic symptoms Effective for: * Sneezing * Itching * Rhinorrhea Less effective for: * Nasal congestion (intranasal corticosteroids superior) ---- ===== Dosing (Adult) ===== * 5 mg PO once daily Pediatric dosing based on age. ---- ===== Adverse Effects ===== Generally well tolerated. Possible: * Headache * Dry mouth * Fatigue (rare) Sedation: * Very low * Comparable to loratadine ---- ===== Contraindications / Cautions ===== * Severe hepatic impairment (monitor) * Hypersensitivity ---- ===== Drug Interactions ===== * Minimal clinically significant CYP interaction * Low risk of QT prolongation ---- ===== Clinical Pearls ===== * Active metabolite of loratadine. * Similar efficacy and safety profile to loratadine. * Once-daily dosing. * Low sedation risk. * Marketing distinction more than major clinical difference from loratadine. ---- ===== Comparison Within Class ===== ^ Drug ^ Sedation Risk ^ Elimination ^ Unique Feature ^ | [[allergy:drugs:loratadine|Loratadine]] | Very low | Hepatic (CYP3A4) | Prodrug | | [[allergy:drugs:desloratadine|Desloratadine]] | Very low | Hepatic | Active metabolite | | [[allergy:drugs:cetirizine|Cetirizine]] | Low | Renal | Racemic mixture | | [[allergy:drugs:levocetirizine|Levocetirizine]] | Low | Renal | R-enantiomer | | [[allergy:drugs:fexofenadine|Fexofenadine]] | Minimal | Renal/Fecal | Least sedating | ---- ===== Related Pages ===== * [[allergy:histamine|Histamine & Antihistamines]] * [[allergy:drugs:loratadine|Loratadine]] * [[allergy:clinical:allergic_rhinitis|Allergic Rhinitis – Stepwise Therapy]]