Azelastine Hydrochloride

Azelastine Hydrochloride is a phthalazinone derivative classified as a potent long-acting anti-allergic compound with selective H1 antagonist properties. It blocks histamine H1-receptor activity and inhibits the release of inflammatory mediators from mast cells.

Azelastine nasal spray is used for seasonal allergic rhinitis (in patients 5 years and older) and vasomotor rhinitis (in patients 12 years and older). As an eye drop, it is used for seasonal allergic conjunctivitis (4 years and older) and non-seasonal (perennial) allergic conjunctivitis (12 years and older).

Common side effects include headache, dizziness, somnolence, nosebleeds, nausea, and bitter taste.

• Seasonal allergic rhinitis - adults and pediatric patients 5 years and older
• Vasomotor rhinitis - adults and adolescent patients 12 years and older
• Seasonal allergic conjunctivitis - adults and children 4 years and older
• Non-seasonal (perennial) allergic conjunctivitis - adults and children 12 years and older

Azelastine, a phthalazinone derivative, is classified as a potent long-acting anti-allergic compound with selective H1 antagonist properties. An additional anti-inflammatory effect could be detected after topical ocular administration.

Data from in vivo (pre-clinical) and in vitro studies show that Azelastine inhibits the synthesis or release of the chemical mediators known to be involved in early and late stage allergic reactions (e.g., leukotriene, histamine, PAF and serotonin).

Azelastine blocks histamine H1 receptors, reducing allergy symptoms (sneezing, itching, runny nose, watery eyes). It also inhibits the release of histamine, leukotrienes, and other inflammatory mediators from mast cells, which play a role in both early and late stages of allergic reactions.

Nasal Spray:

• Seasonal Allergic Rhinitis (Adults & 12+ years): 1-2 sprays per nostril twice daily
• Seasonal Allergic Rhinitis (5-11 years): 1 spray per nostril twice daily
• Vasomotor Rhinitis (Adults & 12+ years): 2 sprays per nostril twice daily

Eye Drop:

• Seasonal Allergic Conjunctivitis (Adults & 4+ years): 1 drop in each eye twice daily (up to 4 times daily if needed)
• Non-seasonal Allergic Conjunctivitis (Adults & 12+ years): 1 drop in each eye twice daily (up to 4 times daily if needed)
• Duration: Maximum 6 weeks; consult doctor if no improvement in 48 hours

Nasal Spray: Shake the bottle gently before use. Clear nostrils by gently blowing nose. Close one nostril and insert the applicator into the other. Tilt head slightly forward and spray while breathing in gently. Breathe out through mouth. Repeat for the other nostril. Clean the applicator at least once weekly.

Eye Drop: Do not touch the dropper tip to the eye.

If you miss a dose, take it as soon as you remember. If it is almost time for your next dose, skip the missed dose. Do not double the dose.

• Dysgeusia (bitter taste)
• Headache
• Dizziness
• Somnolence
• Epistaxis (nosebleeds)
• Nasal stinging or itching
• Dry mouth
• Sore throat
• Nausea

• Caution when driving or operating machinery (may cause somnolence or dizziness)
• Avoid alcohol or other CNS depressants
• Avoid use in patients with recent nasal ulcers, nasal surgery, or nasal trauma
• Avoid spraying into the eyes
• Do not share the bottle with others
• Consult your doctor during pregnancy and breastfeeding

• Known hypersensitivity to Azelastine or any component

• Alcohol and CNS Depressants: Additive effects (increased drowsiness and CNS impairment)
• Cimetidine and Ketoconazole: May interact with Azelastine

No food interactions known.

[CONSULT YOUR DOCTOR] The effects of Azelastine during pregnancy have not been adequately studied. Use only if potential benefit justifies the potential risk to the fetus.

[CONSULT YOUR DOCTOR] It is not known whether Azelastine is excreted in human milk. Caution is advised when administered to nursing mothers. To reduce the amount reaching breast milk, remove excess solution with an absorbent tissue.

Nasal Spray: Safety and efficacy in patients below 5 years have not been established. Eye Drop: Safety and efficacy in patients below 4 years have not been established.

No specific dose adjustment needed for elderly patients, but caution is advised.

Systemic absorption with topical application (nasal or ocular) is minimal, so no dose adjustment is needed for renal or hepatic impairment.

Azelastine overdose may cause increased somnolence. Supportive therapy is recommended.

Keep out of reach of children. Store below 30°C, in a cool and dry place, protected from light. Do not freeze.

Azelastine Hydrochloride (C₂₂H₂₄ClN₃O·HCl)