Azelastine

Benjamin Clanner-Engelshofen is a freelance writer in the medical department. He studied biochemistry and pharmacy in Munich and Cambridge / Boston (USA) and noticed early on that he particularly enjoyed the interface between medicine and science. That is why he went on to study human medicine.

More about the experts All content is checked by medical journalists.

The active ingredient azelastine is an antiallergic agent and is mostly applied locally - either in the form of eye drops or as a nasal spray. In addition to its reliable effect, it is also characterized by its minor side effects. Here you can read everything you need to know about azelastine: nasal spray and eye drop use, mode of action and side effects.

This is how azelastine works

In the case of allergies, for example to grass pollen or animal hair, actually harmless substances trigger an excessive immune reaction in the body. Why this happens in some people has not yet been conclusively clarified among experts. The course of an allergic reaction is now very well understood and enabled the development of antiallergic active ingredients.

Some of them belong to the class of H1 antihistamines.In the event of an allergy, certain immune cells (“mast cells”) release the inflammatory messenger substance histamine in large quantities in the spaces between the tissues. Histamine binds to the specific docking points of the tissue cells (histamine receptors) and tells them that an immune reaction has just been triggered. As a result, for example, the mucous membranes of the nasopharynx and the eyes are better supplied with blood in order to transport further defense cells there. The tissue reddens, swells, itching occurs to remove any foreign bodies that may be present. In addition, tissue fluid escapes to wash away foreign bodies and pathogens - the nose runs and the eyes water.

Active ingredients such as the antihistamine azelastine block the histamine receptors so that the stimulus mediated by histamine no longer leads to said symptoms. This significantly improves the allergic symptoms. In addition, when used locally, only a small part gets into the body's circulation and accordingly only leads to few and weak side effects.

The specialty of azelastine is its "combined effect": In addition to the antihistamine effect, it also stabilizes the mast cells, which means that they release less histamine when irritated. Azelastine also has an anti-inflammatory effect.

Azelastine uptake, breakdown and excretion

When using azelastine nasal spray and eye drops, very little of the active substance enters the body's circulation. When taking azelastine tablets, azelastine is quickly absorbed through the intestines into the blood. It then quickly spreads into many tissues. After about 20 hours, the level of the active substance in the blood has fallen by half. The degradation product desmethyl azelastine, which is also effective and formed in the liver, is half degraded or excreted after about 50 hours. About three quarters of the active ingredient and its breakdown products are excreted in the stool, the rest leaves the body in the urine.

When is azelastine used?

The antiallergic azelastine is approved for the treatment of seasonal and year-round allergic rhinitis (such as hay fever) and allergic conjunctivitis (allergic conjunctivitis).

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

This is how azelastine is used

eye drop

Adults and children over the age of twelve usually use azelastine eye drops twice a day. A drop is placed in each eye. In the case of severe discomfort, it can be used up to four times a day. Strict attention should be paid to the hygienic handling of the eye drops (previous hand washing, do not touch the eye with the opening of the bottle, observe the shelf life after opening - this is usually four weeks).

Nasal spray

Unless otherwise prescribed, adults and children aged twelve and over use the azelastine nasal spray twice a day with one puff per nostril. Before using for the first time, the spray should be actuated several times to fill the pump mechanism. In children, it can be useful to use the nasal spray with the head tilted slightly forward. This means that less of the bitter-tasting solution runs down the throat and is tasted in the mouth.

Tablets

Azelastine tablets should be taken twice a day with a glass of water before or after a meal. Patients over 65 years of age or with impaired liver or kidney function should start treatment with one tablet a day in the evening. According to a doctor's prescription, the tablets are already approved for children from the age of six.

What are the side effects of azelastine?

When using azelastine, the bitter taste can lead to nausea if the nasal spray is used improperly (head tilted back when spraying).

One in a hundred to a thousand people treated complains of slight irritation to the eyes and nasal mucosa, as well as sneezing and nosebleeds.

When taking the tablets, 1 in 10 to 100 people develop tiredness, sleepiness, and dry mouth. These symptoms occur especially at the beginning of treatment and subside as the treatment progresses.

What should be considered when using azelastine?

So far, interactions between azelastine and other active ingredients are only known when taken as a tablet. Nasal spray and eye drops do not interact.

Azelastine is broken down by the liver enzyme cytochrome 2D6. Medicines that inhibit this enzyme can raise the levels of azelastine in the blood. This can increase the rate of side effects. Examples of these are agents for depression (citalopram, fluoxetine, moclobemide, paroxetine, venlafaxine, sertraline), anti-cancer agents (vinblastine, vincristine, doxorubicin, lomustine) and certain anti-HIV agents (delavirdine, ritonavir).

Sedatives and sleeping pills, drugs for psychoses, other allergy medication and alcohol can unexpectedly increase the depressant effect of azelastine.

The use of azelastine in any dosage form is not recommended during pregnancy and breastfeeding as there are insufficient data on safety and efficacy.

The active ingredient can be used by children and adolescents from the age of twelve as well as by adults and the elderly. According to a doctor's prescription, azelastine can be used from the age of six years.

How to get medication with azelastine

Azelastine nasal spray and eye drops do not require a prescription and can be purchased at any pharmacy.

Azelastine tablets or nasal sprays in combination with a glucocorticoid ("cortisone") require a prescription.

Since when is azelastine known?

The allergy drug azelastine belongs to the second generation of H1 antihistamines and is therefore a further development of the first available allergy substances. Compared to its predecessors, it has fewer side effects and is better tolerated. In 1991, azelastine nasal spray and tablets were approved, followed in 1998 by eye drops containing the active ingredient azelastine.

Tags:  foot care hospital womenshealth