II. Indications

  1. Allergic Rhinitis or Vasomotor Rhinitis (intranasal Azelastine)
    1. Second-line agent
    2. FDA Approved for age >5 years (seasonal allergies) and >6 years (perennial allergies)
  2. Allergic Conjunctivitis
    1. FDA Approved for age >=3 years

III. Mechanism

  1. See Antihistamine
  2. Second-generation Antihistamine (phthalazinone)

IV. Medications

  1. Azelastine Nasal (Astelin, Astepro): 0.1% and 0.15% (with 200 sprays/bottle)
  2. Azelastine Ophthalmic (Optivar): 0.05% solution (6 ml bottle)
  3. Combination: Fluticasone with Azelastine (Dymista)
    1. Expensive (up to $200/month) and add little to benefit of generic nasal Corticosteroids alone
    2. Alternatively, use OTC Azelastine (Astepro) and a generic generic nasal Corticosteroid
    3. (2022) Presc Lett 29(5): 25-6

V. Dosing

  1. Nasal (age >5-6 years old)
    1. One spray per nostril twice daily
    2. Adults and children age >12 years may increase to 2 sprays per nostril if needed
    3. Shake well before each use
  2. Ocular (age >= 3 years old)
    1. Use 1 drop in each each eye twice daily

VI. Adverse Effects: Nasal

  1. Somnolence (11%)
    1. May affect safety in driving and hazardous activities
  2. Bitter Taste (20%)
  3. Headache (15%)
  4. Nasal burning (4%)
  5. Pharyngitis (4%)

VII. Adverse Effects: Ophthalmic

  1. Eye burning or stinging (30%, transient)
  2. Headaches (15%)
  3. Bitter taste (10%)

VIII. Safety

  1. Pregnancy Category C
  2. Unknown safety in Lactation

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Related Studies

Cost: Medications

azelastine (on 12/21/2022 at Medicaid.Gov Survey of pharmacy drug pricing)
AZELASTINE 0.1% (137 MCG) SPRY Generic $0.29 per ml
AZELASTINE 0.15% NASAL SPRAY Generic $0.92 per ml
AZELASTINE HCL 0.05% DROPS Generic $1.06 per ml

Ontology: azelastine (C0052762)

Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH C020976
SnomedCT 108644000, 372520005
English 4-(p-chlorobenzyl)-2-(N-methylperhydroazepinyl-(4))-1-(2H)-phthalazinone, azelastine, azelastine [Chemical/Ingredient], 4-(p-Chlorobenzyl)-2-(hexahydro-1-methyl-1H-azepin-4-yl)-1-(2H)-phthalazinone, AZELASTINE, Azelastine, Azelastine (product), Azelastine (substance)
Spanish azelastina (producto), azelastina (sustancia), azelastina

Ontology: azelastine nasal (C0717461)

Concepts Clinical Drug (T200)
English azelastine nasal

Ontology: Azelastine hydrochloride (C0771004)

Definition (NCI) The hydrochloride salt form of azelastine, a phthalazinone derivative with antihistaminergic activity. Azelastine hydrochloride competes with histamine for the H1 receptor, thereby diminishing the actions of histamine on effector cells and decreasing the histamine-mediated symptoms of allergic reaction, such as bronchoconstriction, vasodilation, increased capillary permeability and spasmodic contractions of gastrointestinal smooth muscle.
Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH C020976
SnomedCT 331056008, 330538009, 391803007, 108646003
English 1(2H)-Phthalazinone, 4-((4-Chlorophenyl)methyl)-2-(hexahydro-1-methyl-1H-azepin-4-yl)-, Monohydrochloride, azelastine hydrochloride, azelastine hydrochloride (medication), antihistamines azelastine hydrochloride, Azelastine hydrochloride [eye], AZELASTINE HYDROCHLORIDE, azelastine hcl, azelastine HCl, Azelastine hydrochloride [eye] (product), Azelastine hydrochloride - chemical (substance), Azelastine hydrochloride - chemical, Azelastine hydrochloride, Azelastine hydrochloride (substance), 4-((4-chlorophenyl)methyl)-2- (hexahydro-1-methyl-1H-azepin-4-yl)-1(2H)- phthalazinone HCl, Azelastine hydrochloride [dup] (substance), Azelastine hydrochloride [eye] (substance), Azelastine Hydrochloride
Spanish clorhidrato de azelastina (uso oftálmico), clorhidrato de azelastina (uso oftálmico) (producto), clorhidrato de azelastina (ocular) (producto), clorhidrato de azelastina (ocular), clorhidrato de azelastina (sustancia), clorhidrato de azelastina

Ontology: azelastine ophthalmic (C0875909)

Concepts Clinical Drug (T200)
English azelastine ophthalmic