Allergodil

General characteristics. Structure:

1 dose contains:
Active agent: azelastina hydrochloride of 0,140 mg

Excipients: gipromelloza of 0,140 mg; dinatrium of an edetat dihydrate of 0,700 mg; citric acid of 0,061 mg; hydrophosphate sodium dodecahydrate of 0,907 mg; sodium chloride of 0,961 mg, the water purified 138,419 mg.

Description: transparent colourless or almost colourless solution.

Pharmacological properties:

Azelastin, derivative a ftalazinona, is antiallergic means of long action. Being the selection H1-gistaminoblokatorom, has antihistaminic, antiallergic and membrane stabilizing effect, reduces permeability of capillaries and exudation, stabilizes membranes of mast cells and interferes with release from them biologically active agents (a histamine, serotonin, leukotrienes, the factor activating thrombocytes, etc.) causing a bronchospasm and promoting development of an early and late stage of allergic reactions and an inflammation. At topical administration systemic action insignificant.
At intranasal introduction reduces an itch and a congestion of a nose, sneezing and a rhinorrhea. Weakening of symptoms of allergic rhinitis is noted since 15 min. after use and continues till 12 o'clock and more.
Clinically significant impact on QT (QTc) an interval is absent even at prolonged use of high doses of an azelastin.

Pharmacokinetics. Bioavailability after intranasal use about 40%.
 The maximum concentration (Cmax) in blood after intranasal use is reached in 2-3 hours. At use intranazalno in a daily dose of 0,56 mg of an azelastin of a hydrochloride (one injection in each nasal course twice a day) average equilibrium concentration of an azelastin of a hydrochloride in plasma in 2 hours after reception makes 0,65 ng/ml.
Doubling of the general daily dose to 1,12 mg (two injections in each nasal course twice a day) results in steady average concentration of an azelastin in the plasma equal 1,09 ng/ml.
However, despite rather high absorption at patients, system influence after intranasal use is about 8 times lower, than after oral administration of the daily dose of 4,4 mg of an azelastin of a hydrochloride which is a therapeutic peroral dose for treatment of allergic rhinitis.
Intranasal use for patients with allergic rhinitis causes increase in level of an azelastin in a blood plasma in comparison with healthy subjects.
Other pharmacokinetic data are studied at use inside.
Communication with blood proteins of 80-90%.
It is metabolized in a liver by oxidation with participation of system of P450 cytochrome with formation of an active metabolite of a dezmetilazelastin. It is removed generally by kidneys in the form of inactive metabolites.
Elimination half-life (T1/2) of an azelastin – about 20 h, its active metabolite of a dezmetilazelastin – about 45 h.

Indications to use:

• Treatment of seasonal and year-round allergic rhinitis (including hay fever) and rinokonjyunktivita.
• Treatment of symptoms vasculomotor (year-round not allergic) rhinitis, such as nose congestion, rhinorrhea, sneezing, post-nasal syndrome.

Route of administration and doses:

Intranazalno.
Allergic rhinitis also rinokonjyunktivit
In the absence of other recommendations adults and children are 6 years old and are more senior - on one dose (140 mkg / 0,14 than ml) in each nasal course twice a day in the morning and in the evening.
If necessary to adults and children 12 years - on two doses (280 mkg / 0,28 ml) in each nasal course twice a day and are more senior in the morning in the evening.
Allergodil is applied before the termination of symptoms and is suitable for long use, but no more than 6 months of continuous treatment.
Vasculomotor rhinitis
To adults and children 12 years - on two doses (280 mkg / 0,28 ml) in each nasal course twice a day and are more senior in the morning in the evening.
Allergodil is applied before the termination of symptoms and is suitable for long use, but no more than 8 weeks of continuous treatment.

The volume of one injection (one dose) makes 0,14 ml and contains 140 mkg of active agent.

Use order
1. Remove a protective cap
2. Before the first use press the sprayer 2 – 3 times.
3. Depending on the appointed dose, inject one time or two times into each nasal course, holding the head directly.
4. Again put on a protective cap.

Features of use:

In some cases at the use of nasal spray the fatigue, various degree of manifestation and weakness which can be caused as well by a basic disease comes to light. In these cases it is not recommended to drive the car and to work with dangerous mechanisms. Alcohol intake can strengthen these phenomena.

Side effects:

Frequency of development of side effects is determined as follows:
Very often:> 1/10;
Often: <1/10> 1/100;
Infrequently: <1/100> 1/1000;
Seldom: <1/1000> 1/10000;
Very seldom: <1/10000.

Often - as a result of the wrong way of introduction when the head is thrown back back, emergence of bitter taste in a mouth is possible that in rare instances can make sick.
Infrequently – the weak, passing irritation of the inflamed mucous membrane of a nose which is shown burning, an itch, sneezing, in rare instances nasal bleeding.
Very seldom – allergic reactions (rash, a skin itch, a small tortoiseshell), weakness, dizziness (it can be caused by a disease).

Interaction with other medicines:

At intranasal use of an azelastin clinically significant interaction with other medicines is not revealed.

Influence on ability to manage vehicles and to work with difficult mechanisms
In rare instances the exhaustion, fatigue, dizziness or weakness which can be a consequence of the disease can develop when using an azelastin of nasal spray. In these cases it is necessary to avoid driving of the car and work with difficult mechanisms.

Contraindications:

• Hypersensitivity to an azelastin and/or other components of drug;
• At allergic rhinitis and a rinokonjyunktivita - children's age up to 6 years; at vasculomotor rhinitis - children's age up to 12 years.

Use during pregnancy and a lactation
When testing the doses which are repeatedly exceeding therapeutic range for animals any certificate on teratogenic action, but as there is no experience of use of an azelastin for pregnant women and feeding is not received, use of nasal spray of an azelastin is not recommended during pregnancy, and also in the period of a lactation.

Overdose:

Currently cases of overdose of drug at intranasal use are unknown.

Storage conditions:

At a temperature of 8 - 25 °C. To store in the place, unavailable to children. Period of validity 3 years. The opened bottles – 6 months. Not to apply after a period of validity.

Issue conditions:

Without recipe

Packaging:

Spray nasal dosed 140 mkg / a dose.
On 10 ml of solution in a glass bottle of brown color with the screwed sprayer doser.
1 bottle together with the application instruction is placed in a cardboard pack.