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