Sprays from allergic rhinitis

An effective means of local therapy of allergic sensitization of the body is a spray from allergic rhinitis. Use of this form of drugs can significantly reduce the discharge from the nose (rhinorrhea), reduce itching and sneezing, and also remove the causing chronic nasal obstruction (congestion) of the mucous membranes of the nose with seasonal allergies (hay fever) and during the exacerbation of persistent (all-the-year-round) allergic coryza.

In addition, indications for the use of intrasaline aerosol formulations include IgE-dependent vasomotor rhinitis and pollinosis.

[1], [2], [3], [4], [5], [6], [7]

Names of sprays from allergic rhinitis

To restore the broken permeability of the vascular walls, to reduce the intensity of edema and serous inflammation of the mucous tissues of the nasal cavity and exudate discharge, the following sprays of allergic rhinitis are used :

• Hormonal sprays from allergic rhinitis containing glucocorticosteroids: Nasobek ( Aldetsin, Beklazone, Baconase, Benorin, Clenil, etc.); Nazarel (Flutex, Fliksonase ); Amavis; Nazonex; Budesonide (Rinocort, Tafen nasal).
• Drugs that block peripheral H1 receptors (histamine receptors): Allergodyl (Azelastine); Tizin-Alergi (Levoreakt, Histimet, Reaktin).
• Means stabilizing the membrane of mast cells: kromogeksal (Kromofarm, Kromoglin, Kromosol, Ifiral).
• Sprays-anticongestants (α-adrenomimetics or sympathomimetics): Nazivin (Xymedin, Xylen, Nazol), Otryvin (Pharmazoline Noxprey), Lazolvan Reno, Nazosprey, etc.

Otolaryngologists believe that H1-histamin blockers are safer, but more effective in reducing inflammation of corticosteroids. As for anticongestants - anti-edematous sprays from an allergic rhinitis, for all their unconditional effectiveness in the fight against nasal congestion, these remedies are not recommended for use for longer than a week, as the nasal mucosa ceases to react to them, and the runny nose, as a rule, intensifies.

Hormonal sprays from allergic rhinitis

Pharmacodynamics of aerosol products in this group is the suppression of inflammation with synthetic analogues of adrenal cortex hormones: beclomethasone dipropionate ( Nasobek, Aldetsin, Beklazon, Baconase ), fluticasone propionate ( Nazarel, Fliksonase ), fluticasone furoate ( Amavis ), mometasone furoate ( Nazonex ) and budesonide ( budesonide, Rinocort).

When these substances get into the nasal mucosa, not only the reproduction in the tissues of mast cells and basophils is reduced, but the yield of mediators of allergy and inflammation (leukotriene, cytokines, histamine, etc.) from eosinophilic granulocytes is reduced. Chemotaxis is also slowed down - the promotion of immunocompetent leukocyte cells into the focus of inflammation. As a result, the swelling of the nasal mucosa and the production of mucus are reduced.

The pharmacokinetics of hormonal drugs against an allergic rhinitis is described taking into account their insignificant systemic absorption by binding to plasma proteins (at a level of 0.1-1%). So, the active substances sprays Nasobek, Baconaz, Aldetsin are absorbed by the nasal mucosa, and how much it gets into the stomach and the blood flow with accuracy is difficult to determine. However, two thirds of GCS metabolites are excreted from the body with feces and urine (the half-life period ranges from 3 to 15 hours).

Contraindications to the use of sprays from allergic rhinitis based on GCS:

• hypersensitivity to the main or auxiliary substances of preparations;
• pulmonary tuberculosis;
• viral (HSV) and fungal (Candida albicans) infections in the nasopharynx;
• children's age to 6 years (Nazarel - up to 4 years, Nazonex - up to 2 years).

When assigning these funds, one should take into account the propensity of patients to nosebleeds, nasal septum damage, the presence of glaucoma, thyroid disease, liver and cardiovascular pathologies.

In the instructions for the preparations of this pharmacological group it is indicated that the use of sprays from allergic rhinitis during pregnancy (in the first trimester) is prohibited. Sprays of Nazarel, Fliksonase, Budesonide are contraindicated throughout pregnancy, and the use of Nasobek, Amavis and Nazonex is possible only as a last resort and if the expected health benefits for the mother are higher than the potential threat to fetal development.

Side effects of sprays with corticosteroids often appear in the form of increased dryness in the nose and unpleasant odor, irritation and itching of the mucosa, bleeding, headache, disruption of the integrity (perforation) of the nasal septum.

The way of application of sprays from allergic rhinitis based on GCS: one or two injections into each nasal passage (ie 1-2 pressures on the dispenser-dispenser) - once a day (with exacerbation of allergic rhinitis - twice during the day) .

Overdosing of any sprays with hormones of the adrenal cortex is dangerous by the development of symptoms of hypercorticism, which is manifested by obesity of the face and upper body, increased appetite, appearance of stretch marks on the skin, excessive hair growth in women (above the upper lip and chin), headache, increased blood pressure, pain in bones and their increased fragility, sleep disturbance and depression.

Established interactions with other drugs exclude the simultaneous use of these antiallergic agents with systemic corticosteroids, antituberculosis antibiotics, barbiturates, estrogens, hydantoin antiepileptic drugs and preparations of ephedrine.

Storage conditions : at t = 15-25 ° C; shelf life Nazarel, Fliksonaze, Amavis

Nazonex, Budesonide -3 years, Nasobek - 4 years.

H1 receptor -blocking sprays

Therapeutic effects of the sprays Allergodil (Azelastin) and Tizin-Alergi (Levoreact) is based on their active substances - azelastine hydrochloride and levocabastine, which bind to the peripheral receptors of histamine H1-key tissue hormone responsible for the development of allergic reactions in the body. As a result, there is an inhibition of histamine release from mast cells and basophils.

Allergodyl penetrates into the blood and 93% binds to plasma proteins, bioavailability - azelastine 40%; metabolites after biotransformation in the liver are excreted in the urine (half-life of about 20 hours).

Levocabastin is absorbed into the blood in a minimal volume (less than 40 μg after a single use); the drug is excreted unchanged through the kidneys with a half-life of about 36-37 hours.

Contraindications to the use of these intranasal drugs include intolerance of substances that make up the drugs, as well as age younger than 6 years. Use allergodyl and Tizin-Alergi sprays during pregnancy is contraindicated.

Their main side effects : headache, dizziness, nausea, irritation of the nasal mucosa, burning and itching in the nasopharynx, nosebleed, rashes on the skin.

The use of intranasal sprays : Allergodyl - 1-2 sprays in both nostrils maximum two times a day; Tizin-Alerdzhi has the same dosage, but it can be used yes 4-times during the day (with absolute obstruction of the nasal passages).

Overdose of these medicines can cause dizziness, falling blood pressure, increased drowsiness.

Store sprays Allergodil (Azelastin) and Tizin-Alergi (Levoreakt, Histimet, Reaktin) are relied at room temperature, their shelf life is 36 months.

Spray from allergic rhinitis with cromoglycic acid

Antiallergic effect of nasal sprays containing cromoglicic acid, as sodium cromoglycate - kromogeksal, Kromofarm, Kromoglin, Kromosol, Ifiral - based on the ability to stabilize cytoplasmic membrane of mast cells, which in the process of occurrence ІgE-mediated allergic reactions are activated and undergo degranulation with subsequent release from the cell structures of inflammatory mediators, in particular histamine H1. Cromoglycate sodium prevents this process by blocking the entry into the cytosol of Ca ²⁺ cells and inhibition of enzymes necessary for the release and chemotaxis of eosinophils, neutrophils, etc.

Pharmacokinetics: after the ingestion of Cromohexal (or drugs-synonyms) on the nasal mucosa, it acts for 4-5 hours; absorbed into the tissue and enters the blood of about 6-7% cromoglicate, which is not biotransformation and is eliminated by the kidneys during the day.

Contraindications to the use of cromoglycic acid drugs are hypersensitivity, as well as age to 6 years and pregnancy (the first three months). The most likely side effects include mucosal irritation, skin rashes and nausea.

It is recommended to apply Cromohexal up to 4 times a day - one injection in each nasal passage. Cases of overdose are not described.

Storage conditions : at a temperature not higher than + 25 ° С; Shelf life is three years.

Sprays-anticongestants against allergic rhinitis

The vasoconstrictor mechanism of the action of Nazivin sprays (Ximedin, Xylen, Nazol), Otrivin ( Pharmazoline, Knoxprey) is caused by imidazole derivatives - oxymetazoline hydrochloride and xylometazoline, whose chemical formulas differ only in the presence of an oxygen atom (in oxymetazoline). Having structural similarity with endogenous α-amino acid histidine (turning into histamine), these substances act on α 1-adrenoreceptors of capillary walls, which leads to their narrowing, increase of impermeability and decrease of blood flow. Due to this, tissue swelling in the nose decreases and the secretion of mucous exudate is reduced.

Pharmacokinetics of α-adrenomimetics Nazivin and Otrivin: it is noted in the instructions that the active substances of these sprays enter the systemic blood stream in small amounts that do not have systemic effects on the body. Imidazole derivatives act 10-15 minutes after the injection of the spray, and this action lasts more than 10 hours after application.

Contraindications to the use of Nazivin, Otrivin and all their synonyms: atrophic rhinitis, glaucoma (closed-angle form), expressed atherosclerosis and hypertension, tachycardia, thyrotoxicosis, history of surgical interventions on the brain, age younger than six years.

During pregnancy, the use of sprays from allergic rhinitis, containing oxymetazoline hydrochloride or xylometazoline, is contraindicated.

Among the side effects of these drugs appear: irritation of the nasal mucosa and its dryness; burning in the nose; loss of sensation and mucosal atrophy; puffiness, sneezing, increased secretion secretion; as well as headache, increased blood pressure, violation of the heart rhythm, excessive mental excitability or depressive state.

Spray from allergic rhinitis Nazivin and Otrivin is recommended to apply no more than 2-3 times a day - one injection into each nostril. According to the instructions, the maximum duration of treatment should not exceed seven consecutive days.

It should be borne in mind that an overdose of these drugs can lead to impaired respiratory function, pulmonary edema, coma, and cardiac arrest.

Nazivin and Otrivin are incompatible with any intranasal drugs, as well as with all systemic antipsychotics.

Storage conditions for these products: at room temperature; Shelf life is three years.