Allergodil, spray 0.14 ml/0.14 ml 10 ml

Pharmacotherapeutic group: anti-allergic agent – H1 histamine receptor blocker.

Pharmacological action:

Aselastin, a derivative of phthalazinone, is a long-acting anti-allergic agent. Being a selective H1-histamine blocker, it has antihistamine, antiallergic and membrane stabilizing effect, decreases capillary permeability and exudation, stabilizes mast cell membranes and prevents release of bioactive substances (histamine, serotonin, leukotrienes, platelet-activating factor etc.), which cause bronchospasm and contribute to early and late stages of allergic reactions and inflammation. When used topically, the systemic effect is insignificant.

When administered intranasally it reduces itching and nasal congestion, sneezing and rhinorrhea. Relief of symptoms of allergic rhinitis is noted from 15 minutes after application and lasts up to 12 hours and more.

There is no clinically significant effect on the QT (QTc) interval, even with long-term use of high doses of azelastine.

Pharmacokinetics:

Bioavailability after intranasal administration is about 40%.

The maximum concentration (Cmax) in blood after intranasal administration is reached after 2-3 hours. When administered intranasally at a daily dose of 0.56 mg of azelastine hydrochloride (one injection into each nasal passage twice daily), the average equilibrium plasma concentration of azelastine hydrochloride 2 hours after administration is 0.65 ng/ml.

Doubling the total daily dose to 1.12 mg (two injections into each nasal passage twice daily) results in a sustained mean plasma concentration of azelastine equal to 1.09 ng/ml.

However, despite relatively high absorption in patients, systemic exposure after intranasal administration is approximately 8 times lower than after an oral daily dose of 4.4 mg of azelastine hydrochloride, which is the therapeutic oral dose for the treatment of allergic rhinitis.

Intranasal administration in patients with allergic rhinitis causes increased plasma levels of azelastine compared to healthy subjects.

Other pharmacokinetic data have been studied with oral administration.

Binding to blood proteins is 80-90%.

Metabolized in the liver by oxidation involving the cytochrome P450 system to form the active metabolite desmethylazelastine. It is excreted mainly by the kidneys as inactive metabolites.

The elimination half-life (T1/2) of azelastine is about 20 hours, its active metabolite desmethylazelastine about 45 hours.

Indications

Active ingredient

Composition

How to take, the dosage

Interaction

Directions for use

Special Instructions

Impact on the ability to drive vehicles and operate complex machinery.

Special precautions

Contraindications

Side effects

Rarely, mild, transient irritation of the inflamed nasal mucosa, manifested by burning, itching, sneezing, in rare cases, nasal bleeding.

As a result of the incorrect way of administration, when the head is tilted back, a bitter taste in the mouth may occur, which in rare cases may cause nausea.

Very rare – allergic reactions (rash, skin itching, urticaria), weakness, dizziness (may be caused by the disease itself).

Overdose

Pregnancy use