Astelin (Azelastine) Uses

Active Ingredient: Azelastine

Pharmacological action

Antiallergic, antihistamine, membrane stabilizing.

Selectively blocking histamine H1-receptor, reduces capillary permeability and exudation. Inhibits mast cell degranulation suppresses or prevents liberatiou synthesis of biologically active substances (histamine, serotonin, leukotrienes, platelet activating factor, etc.) That cause bronchospasm and contributing to the development of early and late phase allergic reactions and inflammation. When administered intranasally reduces itching and stuffy nose, sneezing, mucus. Easing the symptoms of allergic rhinitis develops within 3 hours. The maximum effect is achieved in 4-5 hours and lasts 12 hours. The local application in the form of eye drops is accompanied by a decrease in symptoms of allergic eye inflammation (redness, pain, itching, watery eyes, swelling of the eyelids). Ophthalmic effect appears in 10 minutes and maintained for 12 hours.



Easily absorbed by the mucous membranes of the respiratory tract, it produces blood concentrations proportional to dose. After intranasal administration the systemic bioavailability is 40%, the volume of distribution – 14.5 l / kg. Associated with the blood by 80-90%. Passes gistogematicalkie barriers, including the placenta, and the liquid penetrates the fabric. In multiple application of eye drops almost not determined in the blood. Repeated application in a dose of 0.56 mg / day in patients with allergic rhinitis, creates a higher blood concentration (0.65 ng / ml) than in healthy volunteers (0.27 ng / ml).


Allergic rhinitis and conjunctivitis (seasonal, year-round).


Hypersensitivity, pregnancy, lactation, infancy (eye drops – up to 4 years, nasal spray – up to 6 years).

Side effects Astelin

Allergic reactions: skin rash, hives, itching.

  1. From the respiratory system: attacks of sneezing, sore throat, cough, shortness of breath, feeling of tightness in the chest, shortness of breath, bronchospasm.
  2. From the nervous system: headache, dizziness, fatigue.
  3. From the digestive tract: a bitter taste in the mouth (19.7%), change in taste, dry mouth, nausea, gastralgia.

Other: tachycardia, hematuria, myalgia, weight gain; using nasal spray: drowsiness (11.5%), dryness, irritation, burning or itching of the nasal mucosa; rarely – nosebleeds; when applied eye drops: conjunctival irritation; rarely – dry eyes, tearing, foreign body sensation or pain in the eye, swelling, chemosis, bleeding in the anterior chamber of the eye, corneal erosion or excoriation eyes, blurred vision, blepharitis.


Increase (mutually) sedative effect of alcohol and other CNS depressants. Ketoconazole inhibits determining the concentration of Astelin in the blood plasma, and cimetidine, inhibiting cytochrome P450, it increases.


Symptoms: chance of hypersomnia.

The treatment is symptomatic.

Dosing and Administration

Nasal Spray: intranasal (pre-clearing the nasal passages): 1 spraying (0.14 mg / 0.14 ml) in each nostril 2 times a day until symptoms disappear. The course of treatment is not more than 6 months.

Eye drops: conjunctively 1 drop in each eye in the morning and evening until disappearance of symptoms. If necessary, the dose is increased to four times a day by one drop to each eye.

Safety measures

With care prescribe a nasal spray in patients with impaired renal function. When using the spray you should not throw back your head back. During the treatment should be avoided alcohol and the use of CNS depressants. Keep in mind the possibility of dizziness and drowsiness.

Special instructions

When using an eye drop it is not recommended wearing contact lenses.

Astelin (eye drops) can be used for treatment of infectious diseases of the eye in the treatment only on doctor’s advice.