Pharmacology of Azelastine (Astelin) ; Mechanism of action, Pharmacokinetics, Uses, Effects

1 Views • 08/17/25

Side Effects

Subscribers

Azelastine is a potent antihistamine used primarily in the management of allergic rhinitis and allergic conjunctivitis. Here’s a detailed look at its pharmacology:

Mechanism of Action
Histamine H1 Receptor Antagonist: Azelastine works by selectively antagonizing histamine H1 receptors, which helps to inhibit the action of histamine and relieve allergic symptoms.

Anti-Inflammatory Properties: It also stabilizes mast cells, preventing the release of histamine and other inflammatory mediators. This reduces nasal congestion, sneezing, itching, and watery eyes.

Pharmacokinetics
Absorption: When administered intranasally, azelastine has a bioavailability of around 40%. It is absorbed rapidly with an onset of action within 15 minutes3.

Metabolism: Metabolized mainly in the liver by the enzyme CYP3A4.

Half-life: The elimination half-life is approximately 22 hours.

Excretion: Primarily excreted via the urine as metabolites.

Clinical Uses
Allergic Rhinitis: Both seasonal and perennial allergic rhinitis. It is effective in reducing symptoms such as sneezing, runny nose, and nasal itching.

Vasomotor Rhinitis: Provides symptomatic relief for vasomotor rhinitis.

Allergic Conjunctivitis: Azelastine ophthalmic solution is used to treat itchy eyes associated with allergic conjunctivitis.

Side Effects
Common: Bitter taste, headache, somnolence (drowsiness), nasal burning, and rhinitis.

Serious: Rare cases of severe side effects, including hypersensitivity reactions and anaphylaxis, have been reported.

Dosage and Administration
Nasal Spray: Typically, 1-2 sprays per nostril twice daily for allergy management.

Ophthalmic Solution: 1 drop in each affected eye twice daily.

Safety and Precautions
CNS Effects: Azelastine can cause drowsiness, so caution is advised while driving or operating machinery.

Alcohol and CNS Depressants: Concomitant use can enhance CNS depressive effects, so it is best to avoid alcohol and other CNS depressants while using azelastine

#Azelastine #Astelin

Up next

Pharmacology of Azelastine (Astelin) ; Mechanism of action, Pharmacokinetics, Uses, Effects

Up next

Please note that if you are under 18, you won't be able to access this site.

Up next

Pharmacology of Azelastine (Astelin) ; Mechanism of action, Pharmacokinetics, Uses, Effects

Up next

Language