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
Pollinosis, Allergy, Runny nose (rhinitis)
.
Active ingredient
Azelastine
Composition
1 dose contains:
Active ingredient:
azelastine hydrochloride 0.140 mg
Excipients:
hypromellose 0.140 mg;
diethate dihydrate 0.700 mg;
citric acid 0.061 mg;
How to take, the dosage
Intranasal.
Allergic rhinitis and rhinoconjunctivitis:
Interaction
During intranasal administration of azelastine no clinically significant interactions with other drugs were found.
Directions for use
How to use
1. Remove the protective cap
2. Press the nebulizer 2 – 3 times before the first use.
3. Depending on the prescribed dose, inject once or twice in each nostril, keeping your head straight.
4. Put the protective cap back on.
Special Instructions
Impact on the ability to drive vehicles and operate complex machinery.
- In rare cases fatigue, tiredness, dizziness or weakness, which may be a consequence of the disease itself, may develop with azelastine nasal spray. In these cases, driving and operating complex machinery should be avoided.
Special precautions
- In individual cases, fatigue, varying degrees of severity and weakness, which may also be due to the underlying disease, have been identified when using azelastine nasal spray. In these cases, it is not recommended to drive a car and work with dangerous mechanisms. Alcohol consumption may exacerbate these phenomena
.
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
To date, there have been no known cases of overdose from intranasal administration.
Pregnancy use
No evidence of teratogenic effects has been obtained in animal tests of doses many times the therapeutic range, but since there is no experience with azelastine in pregnant and lactating women, the use of azelastine nasal spray during pregnancy and also during lactation is not recommended.
Weight | 0.050 kg |
---|---|
Shelf life | 3 years. Opened vials – 6 months. Do not use after the expiration date. |
Conditions of storage | At 8 – 25 ° C. Keep out of reach of children. |
Manufacturer | Madaus GmbH, Germany |
Medication form | dosed nasal spray |
Brand | Madaus GmbH |
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