(nasal) ā/zil/as’ tēn

Brand Name: Astelin®, Astepro®

• Generic Available

Common Dosage Forms:

  • Nasal Spray (Astelin): 0.1% azelastine. Each spray delivers 137 mcg of azelastine HCl. 
  • Nasal Spray (Astepro): 0.15% azelastine. Each spray delivers 205.5 mcg of azelastine HCl. 

FDA Indications/Dosages:

  • For the treatment of the symptoms of nonallergic vasomotor rhinitis and seasonal allergic rhinitis such as rhinorrhea, sneezing, and nasal pruritus in adults and children 12 years and older: The recommended dose is two sprays per nostril twice daily. After assembly prime the pump by spraying 4 times. No additional priming is necessary unless more than 3 days lapses between doses.

Pharmacology/Pharmacokinetics:

Azelastine is a histamine H1-receptor antagonist that blocks histamine release in peripheral tissues. Systemic bioavailability after intranasal administration is approximately 40%. Cmax occurs in 2-3 hours. Elimination half-life is 22 hours. Azelastine is metabolized by the cytochrome P450 enzyme system to an active metabolite, desmethylazelastine.

Drug Interactions:

Other CNS depressants may increase drowsiness. Cimetidine may increase effects.

Contraindications/Precautions:

Contraindicated in patients who are hyper- sensitive to any of its components. May cause drowsiness, use caution when performing activities that require alertness. Pregnancy Category C.

Adverse Effects:

Bitter taste in mouth (20%), headache (14%), drowsiness (12%), nasal burning (4%), pharyngitis (4%), dry mouth, sneezing, nausea (3%), rhinitis, fatigue, dizziness, nosebleed, and weight increase (2%).

Patient Consultation:

  • May cause drowsiness. Use care when operating machinery or when mental alertness is required.
  • Carefully read the enclosed patient information sheet before using.
  • Store units upright in a cool place away from sunlight and children. Keep the pump unit tightly closed.
  • Units need to be primed with 4 sprays upon assembly and with 2 sprays if not used for 3 days.
  • If a dose is missed, skip it and return to normal dosing schedule.