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Last Updated on September 7, 2021

Azelastine 0.1% is a highly effective and fast-acting anti-histamine. It works by blocking the histamine receptor in the body and has a unique mechanism of action and a short half-life. It is indicated for the relief of pruritus and seasonal allergic rhinitis. Azelastine is also effective in the management of symptoms associated with perennial allergic rhinitis.

Azelastine (azelastine hydrochloride) is a new-generation, first-generation H1-receptor histamine antagonist for the treatment of allergic rhinitis and pruritus associated with exanthems. As a first-generation H1-receptor antagonist, azelastine works by blocking histamine receptors in the upper airways to relieve nasal and ocular symptoms of hay fever.

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What is Azelastine

The active ingredient Azelastine is a remedy for allergies (anti-allergic) and is usually applied locally – either in the form of eye drops or as a nasal spray. In addition to its reliable effect it is also distinguished by its minor side effects. Here you can read everything you need to Azelastine: nasal spray and eye drops application, mode of action and side effects

How Azelastine works?

With allergies, such as to grass pollen or animal hair, normally harmless substances trigger an excessive immune response in the body. How is it in some people this is not fully understood by experts. The expiry of an allergic reaction but is now well understood and allowed for the development of anti-allergic agents.

Some of them belong to the class of H1 antihistamines. When an allergy specific defense cells release (“mast cells”) into tissue spaces in large quantities the inflammation messenger histamine from. Histamine binds to the specific docking sites of the tissue cells (histamine receptors), and mediates this that just has been triggered an immune response. Then, for example, the mucous membranes of the nasopharyngeal space and the eyes are better supplied with blood to carry more immune cells there. The tissue reddens, swells, occurs to possibly remove any foreign objects. In addition, tissue fluid exits to wash away debris and pathogens -. Runny nose and watering eyes

as the antihistamine Azelastine drugs block the histamine receptors, so that the mediated by histamine stimulus no longer causes said symptoms. Thus, the allergic symptoms improve significantly. In addition, with the local application only a small part reaches the systemic circulation and, accordingly, leads only to a few and weak side-effects.

The peculiarity of Azelastine is its “combined effect”: In addition to the antihistamine effect it stabilizes also the mast cells, which secrete these less histamine in irritation. Moreover, Azelastine has an anti-inflammatory.


When using Azelastine nasal spray and eye drops very little drug reaches the systemic circulation. When taking Azelastine tablets Azelastine is rapidly absorbed through the intestine into the blood. Then it spread rapidly in many tissues. After about 20 hours of drug levels in the blood has dropped to half. This also effective, formed in the liver metabolite desmethyl Azelastine is degraded or excreted after about 50 hours in half. Approximately three quarters of the active substance and its degradation products are excreted in the stool, the rest leaves the body through urine.

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When to use Azelastine?

The antiallergic agent Azelastine is for the treatment of seasonal and perennial allergic rhinitis (such as (allergic conjunctivitis) authorized.

The application of the active ingredient in the form of tablets or as a nasal spray is also possible long term. The eye drops should be used a maximum of six weeks.

How to take Azelastine?

Eye Drops

Adults and children from the age of twelve contact Azelastine eye drops usually twice daily. In this case, one drop is introduced in the eye. With severe symptoms, the application can be carried out up to four times a day. On the hygienic handling of the eye drops should be strictly respected (first doing hand washing, do not touch the eye with the opening of the vial, observe the shelf life after opening – this is usually four weeks)

Nasal Spray

Unless otherwise prescribed, contact adults and children over twelve years, the Azelastine nasal spray twice daily with a spray per nostril at. Before the first use, the spray should be repeatedly actuated to fill the pumping mechanism. In children, it can be useful to apply the nasal spray with slightly sloping forward head. So runs less of the bitter-tasting solution down the throat and is tasted in the mouth.


Azelastine tablets should be taken twice a day with a glass of water before or after eating. Patients older than 65 years or with a hepatic or renal impairment should begin treatment with one tablet daily in the evening. Following doctor’s prescription, the tablets have already been authorized in children aged six and over.

What are the side effects of Azelastine?

In the application of Azelastine the bitter taste in case of improper use of the nasal spray may lead (reclined head while spraying) to nausea.

One of hundred to a thousand patients treated complained of slight irritation to the eye and to the nasal mucosa, as well as sneezing and nosebleeds.

When taking the tablets evolve at a ten to one hundred patients fatigue, drowsiness and dry mouth. These symptoms occur particularly at the start of treatment and usually resolve in the course.

What should be considered when applying Azelastine?

Interactions between Azelastine and other active compounds are only known when taking a tablet. Nasal spray and eye drops show no interactions.

Azelastine is broken down by the liver enzyme cytochrome 2D6. Medicinal products that inhibit this enzyme may lead to high blood levels of Azelastine. This can increase the rate of side effects. Examples include antidepressants (Sertraline), anticancer agents (vinblastine, vincristine, doxorubicin, lomustine) and certain HIV agent (delavirdine, ritonavir).

sedatives and sleeping agents, anti-psychosis, other allergy medication and alcohol may the damping effect of Azelastine increase unexpectedly.

During pregnancy and lactation The use of Azelastine is recommended in any dosage form, due to insufficient data on safety and efficacy.

The active ingredient can be used by children and adolescents from the age of twelve, and of adults and older people. According to medical prescription Azelastine may only be applied from the age of six years.

How to get Azelastine online?

Azelastine nasal spray and eye drops are available without a prescription and can be purchased at any drug store.
Azelastine nasal spray 10 ml in UK: This product is classified as a drug or prescription-only medicine. It may cause drowsiness or impair coordination. Read the facts before you take Azelastine.
Azelastine tablets or nasal sprays in combination with a glucocorticoid (“cortisone”) are only available on prescription.

When did azesteline appear?

The allergy agents Azelastine already belongs to the second generation of H1 antihistamines and is thus a development of the first available allergy drugs. Compared to its predecessors, it has fewer side effects and is better tolerated. In 1991, Azelastine nasal spray and tablets have been approved, in 1998, followed by eye drops containing the active substance Azelastine.