====== Fexofenadine ====== ===== Classification ===== * Second-Generation H1 Antihistamine * Selective peripheral H1 receptor inverse agonist * Active metabolite of terfenadine Parent class: [[allergy:histamine|Histamine & Antihistamines]] ---- ===== Mechanism of Action ===== Fexofenadine selectively blocks peripheral H1 receptors. Effects: * ↓ Histamine-mediated vasodilation * ↓ Capillary permeability * ↓ Pruritus * ↓ Sneezing and rhinorrhea Key Feature: * Minimal penetration of the blood-brain barrier * Essentially non-sedating at therapeutic doses ---- ===== Pharmacologic Background ===== Fexofenadine is the active metabolite of terfenadine. Terfenadine was removed from the market due to QT prolongation and torsades risk (CYP3A4 inhibition interactions). Fexofenadine: * Does not significantly prolong QT interval * Does not rely on hepatic metabolism for activation ---- ===== Pharmacokinetics ===== * Oral administration * Onset: ~1 hour * Duration: ~24 hours * Primarily eliminated unchanged in feces and urine * Minimal hepatic metabolism Absorption reduced by: * Aluminum/magnesium antacids * Fruit juices (apple, orange, grapefruit) Separate dosing from antacids by at least 2 hours. ---- ===== Indications ===== * [[allergy:clinical:allergic_rhinitis|Allergic Rhinitis]] * Chronic idiopathic urticaria * Seasonal allergies Effective for: * Sneezing * Itching * Rhinorrhea Less effective for: * Nasal congestion (intranasal steroids preferred) ---- ===== Dosing (Adult) ===== * 60 mg PO twice daily * OR 180 mg PO once daily Dose adjustment in renal impairment. ---- ===== Adverse Effects ===== Generally very well tolerated. Possible: * Headache * Mild nausea * Rare dizziness Sedation: * Minimal to none * Lowest sedation risk among common 2nd-generation H1 blockers ---- ===== Contraindications / Cautions ===== * Renal impairment (dose adjust) * Hypersensitivity Caution: * Avoid coadministration with fruit juice * Separate from antacids ---- ===== Drug Interactions ===== * Aluminum/magnesium antacids ↓ absorption * Fruit juice ↓ bioavailability * Minimal CYP interaction * No meaningful QT risk at therapeutic doses ---- ===== Clinical Pearls ===== * Least sedating of the second-generation H1 blockers. * Preferred in patients requiring full daytime alertness. * Safe cardiovascular profile compared to its predecessor (terfenadine). * Does not significantly impair cognition or psychomotor function. * Not effective for nasal congestion as monotherapy. ---- ===== Comparison Within Class ===== ^ Drug ^ Sedation Risk ^ Elimination ^ Unique Feature ^ | [[allergy:drugs:loratadine|Loratadine]] | Very low | Hepatic | Active metabolite = desloratadine | | [[allergy:drugs:cetirizine|Cetirizine]] | Low | Renal | Slightly more sedating | | [[allergy:drugs:levocetirizine|Levocetirizine]] | Low | Renal | R-enantiomer refinement | | [[allergy:drugs:fexofenadine|Fexofenadine]] | Minimal | Renal/Fecal | Least sedating; safe QT profile | ---- ===== Related Pages ===== * [[allergy:histamine|Histamine & Antihistamines]] * [[allergy:drugs:loratadine|Loratadine]] * [[allergy:drugs:cetirizine|Cetirizine]] * [[allergy:clinical:allergic_rhinitis|Allergic Rhinitis – Stepwise Therapy]]