Last Updated on May 23, 2023
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 an anti-allergic and is usually used locally – either as eye drops or as a nasal spray. In addition to its reliable action, it has very few side effects. Here you can read everything you need to know about azelastine: nasal spray and eye drops, how it works and side effects.
How does azelastine work?
In allergies, such as to grass pollen or animal dander, normally harmless substances trigger an excessive immune response in the body. Why this happens in some people is not fully understood by experts. However, it is now well understood and has led to the development of anti-allergic drugs.
Some of these belong to the class of H1 antihistamines. When an allergy occurs, specific defence cells (“mast cells”) release large amounts of the inflammatory messenger histamine into tissue spaces. Histamine binds to the specific docking sites on tissue cells (histamine receptors) and mediates the immune response that has just been triggered. For example, the mucous membranes of the nasopharynx and the eyes are then better supplied with blood to carry more immune cells there. The tissues become red and swollen, possibly to remove foreign bodies. Tissue fluid also leaks out to wash away debris and germs. Runny nose and watery eyes
Azelastine antihistamines block the histamine receptors so that the histamine-mediated stimulus no longer causes these symptoms. This significantly improves the allergic symptoms. In addition, only a small proportion of azelastine enters the systemic circulation when it is used locally, so side effects are few and mild.
The special feature of azelastine is its “combined effect”: In addition to its antihistamine effect, it also stabilises mast cells, which secrete less histamine when irritated. Azelastine also has an anti-inflammatory effect.
When azelastine nasal spray and eye drops are used, very little drug enters the systemic circulation. When you take azelastine tablets, azelastine is quickly absorbed into the blood through the intestines. It then spreads quickly to many tissues. After about 20 hours, the level of the drug in the blood is reduced by half. The active metabolite desmethyl azelastine is formed in the liver and is metabolized or excreted in about 50 hours. About three-quarters of the active ingredient and its breakdown products are excreted in the stool, with the remainder leaving the body in the urine.
When should you use Azelastine?
The antiallergic agent azelastine is approved for the treatment of seasonal and perennial allergic rhinitis (e.g. allergic conjunctivitis).
It can also be used as a tablet or nasal spray for long-term use. The eye drops should be used for a maximum of six weeks.
How to take Azelastine?
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)
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 possible side effects of azelastine?
With azelastine, the bitter taste may cause nausea if the nasal spray is used improperly (tilting the head while spraying).
One in a hundred treated patients complained of mild irritation of the mucous membranes of the eyes and nose, as well as sneezing and nasal bleeding.
One in ten patients experienced fatigue, drowsiness and dry mouth when taking the pills. These symptoms are more common at the beginning of treatment and usually disappear over time.
What should I watch for while using azelastine?
Interactions between azelastine and other drugs are only known when taken as a tablet. There are no known interactions with nasal spray or eye drops.
Azelastine is metabolized by the liver enzyme cytochrome 2D6. Medications that inhibit this enzyme may result in high blood levels of azelastine. This may increase the rate of side effects. Examples include antidepressants (sertraline), cancer drugs (vinblastine, vincristine, doxorubicin, lomustine), and certain HIV drugs (delavirdine, ritonavir).
Sedatives and sleeping pills, antipsychotics, other allergy medications and alcohol may unexpectedly increase the depressant effect of azelastine.
During pregnancy and lactation The use of azelastine in any dosage form is not recommended due to insufficient data on safety and efficacy.
The drug can be used by children and adolescents from twelve years of age and by adults and elderly people. According to medical prescription, azelastine may be used only 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 drugstore.
Azelastine nasal spray 10 ml in UK: This product is classified as a medicine or prescription drug. It may cause drowsiness or impaired coordination.
Azelastine tablets or nasal sprays in combination with a glucocorticoid (“cortisone”) are only available on prescription.
When was azelastine first introduced?
Azelastine belongs to the second generation of H1 antihistamines and is therefore a further development of the first available allergy medicines. Compared with its predecessors, it has fewer side effects and is better tolerated. Azelastine nasal spray and tablets were approved in 1991, followed by eye drops containing the active ingredient azelastine in 1998.