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allergy:drugs:loratadine

Loratadine

Classification

  • Second-Generation H1 Antihistamine
  • Peripheral H1 receptor inverse agonist

Parent class: 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

  • 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
Loratadine Very low 24 hr Active metabolite (desloratadine)
Cetirizine Low 24 hr Slightly more sedating
Fexofenadine Minimal 24 hr Least sedating

allergy/drugs/loratadine.txt · Last modified: by andrew2393cns