Nasonex is a glucocorticosteroid nasal spray that has anti-inflammatory and anti-allergic effects. The active ingredient is mometasone.

Synthetic glucocorticosteroid (GCS) for topical application.

It has anti-inflammatory and anti-allergic effects when used in doses that do not cause systemic effects:

• reduces inflammation by reducing the formation of chemotaxis substance (influence on "late" allergy reactions);
• inhibits the development of an immediate allergic reaction;
• exhibits high anti-inflammatory activity both in the early and late stages of an allergic reaction.

In studies with provocative tests with the application of antigens to the nasal mucosa, the high anti-inflammatory activity of Nasonex was demonstrated, both in the early and in the late stages of an allergic reaction.

This was confirmed by a decrease (compared to placebo) in the concentration of histamine and eosinophil activity, as well as a decrease (compared to baseline) in the number of eosinophils, neutrophils and epithelial cell adhesion proteins.

Composition of Nazonex (1 spray dose):

• micronized mometasone furoate (in the form of monohydrate) - 50 mcg;
• auxiliary components: benzalkonium chloride (in the form of a 50% solution), glycerol, dispersed cellulose (microcrystalline cellulose treated with sodium carmellose), polysorbate 80, sodium citrate dihydrate, citric acid monohydrate, purified water.

The systemic bioavailability of mometasone with intranasal administration does not exceed 1% (with a sensitivity of the method of determination of 0.25 pg / ml).

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Price in pharmacies

Information about the price of Magnelis in pharmacies in Moscow and Russia is taken from these online pharmacies and may differ slightly from the price in your region.

You can buy the drug in Moscow pharmacies at the price: Nasonex nasal spray 50 mcg / dose 10 g 60 doses - from 476 to 541 rubles, the cost of a spray of 120 doses - from 806 to 873 rubles, according to 694 pharmacies.

Keep out of reach of children in compliance with temperature regime 2-25 ° C. Avoid freezing. Shelf life is 2 years.

Terms of dispensing from pharmacies - by prescription.

The list of analogs is presented below.

What does Magnelis help from?

Magnelis is prescribed in the following cases:

• seasonal and year-round treatment allergic rhinitis in adults, adolescents and children from 2 years of age;
• exacerbation of chronic sinusitis in adults (including senile) and children from 12 years of age (as an adjunct in complex antibiotic therapy);
• nasal polyposis with impaired nasal breathing and smell in adults;
• prevention of seasonal allergic rhinitis, moderate and severe course(recommended 2-4 weeks before the start of the dusting season).

Instructions for the use of Magnelis, doses and rules

Shake the bottle vigorously before each use.

The spray is intended for intranasal administration (used as inhalation) of the suspension contained in the vial. The procedure is carried out using a dispensing nozzle, which is included in each bottle of Nasonex.

Before the first use of the spray, it is “calibrated” by pressing the dosing device 2-3 times - this makes it possible to establish a stereotyped drug delivery. Each press of the dosing device releases into the nasal cavity 100 mg of the suspension, which contains 50 μg of the active ingredient.

If Nasonex nasal spray has not been used for 14 days or longer, the instruction recommends re-calibration. Shake the bottle vigorously before each use.

If the nozzle is clogged, it is necessary to remove the plastic cap by gently pressing on the white ring, easily remove the nozzle and rinse it with cold running water, dry it and reinstall it.

The standard dosage of the spray, according to the instructions for use of Nasonex, is 2 inhalations (50 mcg each) in each nostril 1 time per day (total daily dose - 200 mcg). Upon reaching therapeutic effect for maintenance therapy, it is possible to reduce the dose to 1 inhalation in each nostril once a day (total daily dose - 100 mcg).

If a decrease in the symptoms of the disease cannot be achieved by using Nasonex at the recommended dose, the daily dosage can be increased to 4 inhalations. After symptom relief, dose reduction is recommended.

The onset of action of the nasal spray is usually noted as early as 12 hours after the first use of the drug.

Children aged 2-11

For the use of the drug in children younger age adult assistance is required.

special instructions

Do not use in ophthalmology.

Cancellation is necessary if a bacterial or fungal infection develops.

When using the drug for a long time (as with any long-term treatment), a periodic examination of the nasal mucosa by an ENT doctor is necessary.

Application features

Before using the drug, read the sections of the instructions for use about contraindications, possible side effects and other important information.

Magnelis side effects

Instructions for use warns of the possibility of development side effects drug Magnelis:

• in adults and adolescents: headache, nosebleeds;
• in children: nosebleeds, headache, nasal irritation, sneezing;
• rarely - bronchospasm, shortness of breath;
• very rarely - anaphylaxis, angioedema, disturbances in taste and smell.

Contraindications

It is contraindicated to use Magnelis for the following diseases or conditions:

• a nasal injury with damage to the nasal mucosa or recent surgery - before the wound heals;
• children under 2 years of age - in the treatment of seasonal and year-round allergic rhinitis, up to 12 years - with acute sinusitis and exacerbation of chronic sinusitis, up to 18 years - with polyposis;
• the presence of individual hypersensitivity to any component in the composition of the drug.

Use with caution:

• active or latent tuberculosis infection of the respiratory tract, untreated local infection with involvement of the nasal mucosa in the process;
• bacterial, fungal, systemic viral infection or Herpes simplex infection involving the eye.

Overdose

The drug has a low (≤ 0.1%) systemic bioavailability, so it is unlikely that in case of an overdose, it will be necessary to take any special measures other than observation and subsequent administration at the recommended dose.

At long-term use GCS in high doses or with the simultaneous use of several GCS may suppress the hypothalamic-pituitary-adrenal system.

List of Magnelis analogues

If necessary, replace the drug, two options are possible - the choice of another medication with the same active ingredient or a drug with a similar effect, but with a different active substance.

Magnelis analogs, a list of drugs:

1. Dezrinit,
2. Risonel,
3. Asmaneks Twistheiler.

Similar in action:

• Flutinex,
• Beclonazal,
• Polydex,
• Nasobek,
• Mometasone.

Most cheap analog, to replace Nazonex - this is the Dezrinit nasal spray, the price of a bottle for 140 doses is from 368 to 439 rubles.

When choosing a replacement, it is important to understand that the price, instructions for use and reviews for Magnelis do not apply to analogues. Before replacing the drug, you must obtain the approval of the attending physician and do not replace the drug yourself.

Nazonex or Avamis - which is better to choose?

The active substance of the Avamis spray is fluticasone furoate (the concentration of the substance in one dose is 27,% 5 μg).

Avamis (fluticasone) and Nazonex (mometasone) - modern drugs characterized by very high degree affinity for GCS-receptors and exceptional topical activity. Both substances have extremely low absolute bioavailability. However, for mometasone, this figure is slightly lower than for fluticasone - 0.1% versus 0.5%.

Mometasone among all existing GCS for intranasal administration has the lowest bioavailability and the most rapid development therapeutic effect.

In addition, its use is allowed from the age of two, while fluticasone furoate in pediatric practice is used only for the treatment of children over 6 years old. Even with prolonged use, Nasonex does not adversely affect the growth of the child.

Compound

Description of the dosage form

Suspension is white or almost white.

pharmachologic effect

Pharmacodynamics

Mometasone is a synthetic topical corticosteroids. It has anti-inflammatory and anti-allergic effects when used in doses that do not cause systemic effects. It inhibits the release of inflammatory mediators, increases the production of lipomodulin, which is an inhibitor of phospholipase A, which leads to a decrease in the release of arachidonic acid and, accordingly, inhibition of the synthesis of metabolic products of arachidonic acid - cyclic endoperoxides, PG. Prevents marginal accumulation of neutrophils, reduces inflammatory exudate and production of lymphokines, inhibits the migration of macrophages, leads to a decrease in the processes of infiltration and granulation. Reduces inflammation by reducing the formation of chemotaxis substance (effect on late allergy reactions), inhibits the development of an immediate type of allergic reaction (due to inhibition of the production of metabolites of arachidonic acid and a decrease in the release of inflammatory mediators from mast cells).

In studies with provocative tests when applying antigens to the nasal mucosa, a high anti-inflammatory activity of mometasone was demonstrated both in the early and in the late stages of an allergic reaction. This was confirmed by a decrease (compared with placebo) in the level of histamine and eosinophil activity, as well as a decrease (compared to the baseline) in the number of eosinophils, neutrophils and adhesion proteins of epithelial cells.

Pharmacokinetics

With intranasal administration, the systemic bioavailability of mometasone furoate is<1% (при чувствительности метода определения 0,25 пг/мл). Суспензия мометазона очень плохо всасывается в ЖКТ , и то небольшое количество суспензии мометазона, которое может попасть в ЖКТ после впрыскивания в носовой ход, еще до экскреции с мочой или желчью подвергается активному первичному метаболизму.

Indications of the drug Nasonex ®

seasonal and year-round allergic rhinitis in adults, adolescents and children from 2 years of age;

acute sinusitis or exacerbation of chronic sinusitis in adults (including the elderly) and adolescents from 12 years old - as an auxiliary therapeutic agent in antibiotic treatment;

acute rhinosinusitis with mild to moderate symptoms without signs of severe bacterial infection in patients from 12 years of age;

preventive treatment of moderate and severe seasonal allergic rhinitis in adults and adolescents from 12 years of age (recommended 2–4 weeks before the expected start of the dusting season);

nasal polyposis, accompanied by impaired nasal breathing and smell, in adults (from 18 years old).

Contraindications

hypersensitivity to any of the substances that make up the drug;

recent surgery or nasal trauma with damage to the nasal mucosa - until the wound heals (due to the inhibitory effect of GCS on the healing process);

children's age (with seasonal and year-round allergic rhinitis - up to 2 years, with acute sinusitis or exacerbation of chronic sinusitis - up to 12 years, with polyposis - up to 18 years) - due to the lack of relevant data.

Carefully: tuberculous infection (active or latent) of the respiratory tract; untreated fungal, bacterial, systemic viral infection or infection caused by Herpes simplex with eye damage (as an exception, it is possible to prescribe the drug for the listed infections as directed by a doctor); the presence of an untreated local infection with the involvement of the nasal mucosa in the process.

Application during pregnancy and lactation

Appropriately designed and well-controlled studies of the drug in pregnant women have not been conducted.

As with the use of other intranasal corticosteroids, Nasonex® should be prescribed to pregnant or breastfeeding women only if the expected benefit from prescribing the drug justifies the potential risk to the fetus or infant.

Infants whose mothers received GCS during pregnancy should be carefully monitored for the possibility of developing adrenal hypofunction.

Side effects

Application medicinal product v clinical research

Adverse events associated with the use of the drug (> 1%), identified during clinical studies in patients with allergic rhinitis or nasal polyposis and during the post-registration period of drug use, regardless of the indication for use, are presented in the table. Adverse reactions are listed according to the classification of system organ classes. MedDRA... Within each system-organ class, adverse reactions are classified by frequency of occurrence.

Nasal bleeding, as a rule, was moderate and stopped on its own, the frequency of their occurrence was slightly higher than with placebo (5%), but equal or less than with the appointment of other intranasal corticosteroids, which were used as active control (in some of the the incidence of nosebleeds was up to 15%).

The incidence of all other adverse events was comparable to that with placebo. The overall incidence of adverse events in patients treated for nasal polyposis was comparable to that in patients with allergic rhinitis.

The overall incidence of adverse events in patients treated for acute rhinosinusitis was comparable to that in patients with allergic rhinitis and placebo. With the use of intranasal corticosteroids, systemic side effects may develop, especially with prolonged use of intranasal corticosteroids in high doses (see "Special instructions").

The frequency of adverse reactions is set as follows: very often (≥1 / 10); often (≥1 / 100,<1/10); редко (≥1/1000, <1/100). Для нежелательных реакций в период пострегистрационного наблюдения частота не установлена (не может быть определена на основании имеющихся данных).

* Revealed with a frequency of "rare" when using the drug 2 times a day with nasal polyposis.

** Revealed when using the drug 2 times a day with nasal polyposis.

Children

From the respiratory system, chest and mediastinal organs: nosebleeds (6%), irritation of the nasal mucosa (2%), sneezing (2%).

From the nervous system: headache (3%).

The incidence of these adverse events in children was comparable to the incidence with placebo.

Post-registration use of a medicinal product

During the post-registration use of the drug Nasonex ®, additional undesirable reactions were detected: blurred vision.

Interaction

The combination therapy with loratadine was well tolerated by the patients. At the same time, no effect of the drug on the concentration of loratadine or its main metabolite in blood plasma was noted. In these studies, mometasone furoate was not detected in blood plasma (with a sensitivity of the method of determination of 50 pg / ml).

Mometasone furoate is metabolized by CYP3A4. Concomitant use with strong inhibitors of CYP3A4 (for example, ketoconazole, itraconazole, clarithromycin, ritonavir, drugs containing cobicistat) can lead to an increase in the concentration of GCS in the blood plasma and, possibly, to an increase in the risk of systemic side effects of GCS therapy. The advantages of co-administration of mometasone furoate with strong inhibitors of CYP3A4 and the potential risk of developing systemic side effects of GCS should be evaluated. In the case of joint use of drugs, monitoring of the patient's condition is required for the development of systemic side effects of GCS therapy.

Method of administration and dosage

Intranasally. Injection of the suspension contained in the vial is carried out using a special dispensing nozzle on the vial.

Before using Nasonex ® nasal spray for the first time, it must be calibrated. Do not pierce the nasal applicator.

To calibrate, press the dispensing nozzle 10 times or until a homogeneous spray appears. The applicator is ready for use. Tilt your head and inject drugs into each nasal passage as recommended by the attending physician.

If the drug has not been used for 14 days or more, press the dispensing nozzle 2 times or until a homogeneous spray appears. Tilt your head and inject drugs into each nasal passage as recommended by the attending physician.

Cleaning the dispensing nozzle. It is important to clean the dispensing tip regularly to avoid malfunctioning. Remove the dust cap, then carefully remove the spray tip. Thoroughly rinse spray tip and dust cap in warm water and rinse under tap.

Do not try to open the nasal applicator with a needle or other sharp object. this will damage the applicator and may result in the patient taking the wrong dose of the drug.

Dry the cap and tip in a warm place. Then attach the spray tip to the bottle and screw the dust cap back onto the bottle. When using the nasal spray for the first time after cleaning, recalibrate by pressing the dispensing tip 2 times.

Shake the bottle vigorously before each use.

Treating seasonal or perennial allergic rhinitis

The recommended prophylactic and therapeutic dose of the drug is 2 injections (50 mcg of mometasone furoate each) into each nasal passage once a day (total daily dose - 200 mcg). Upon reaching the therapeutic effect for maintenance therapy, it is possible to reduce the dose to 1 injection into each nasal passage once a day (total daily dose - 100 mcg).

If a decrease in the symptoms of the disease cannot be achieved by using the drug in the recommended therapeutic dose, the daily dose can be increased to 4 injections into each nasal passage once a day (total daily dose - 400 mcg). After symptom relief, dose reduction is recommended. The onset of action of the drug is usually noted clinically within 12 hours after the first use of the drug.

Children 2-11 years old. The recommended therapeutic dose for the treatment of seasonal or year-round allergic rhinitis is 1 injection (50 μg of mometasone furoate) into each nasal passage once a day (total daily dose - 100 μg).

For the use of the drug in young children, adult assistance is required.

Adjunctive treatment of acute sinusitis or exacerbation of chronic sinusitis

Adults (including the elderly) and adolescents from 12 years old. The recommended therapeutic dose is 2 injections (50 mcg of mometasone furoate each) into each nasal passage 2 times a day (total daily dose - 400 mcg).

If a decrease in the symptoms of the disease cannot be achieved by using the drug in the recommended therapeutic dose, the daily dose can be increased to 4 injections into each nasal passage 2 times a day (total daily dose - 800 mcg). After symptom relief, dose reduction is recommended.

Treating acute rhinosinusitis without evidence of severe bacterial infection

The recommended dose for adults and adolescents is 2 injections (50 mcg of mometasone furoate each) into each nasal passage 2 times a day (total daily dose - 400 mcg). If symptoms worsen during treatment, consult a specialist.

Treatment of nasal polyposis

Adults (including the elderly) from 18 years old. The recommended therapeutic dose is 2 injections (50 mcg of mometasone furoate each) into each nasal passage 2 times a day (total daily dose - 400 mcg). After reducing the symptoms of the disease, it is recommended to reduce the dose to 2 injections (50 mcg of mometasone furoate each) in each nasal passage once a day (total daily dose - 200 mcg).

Overdose

Symptoms: with prolonged use of corticosteroids in high doses, as well as with the simultaneous use of several corticosteroids, it is possible to suppress the function of the HPA.

Treatment: due to small (<1%, при чувствительности метода определения 0,25 пг/мл) системной биодоступности маловероятно, что при случайной или намеренной передозировке потребуется принятие каких-либо мер, помимо наблюдения с возможным последующим возобновлением приема препарата в рекомендованной дозе.

special instructions

As with any long-term treatment, patients who have been using Nasonex ® nasal spray for several months or longer should periodically be examined by a doctor for possible changes in the nasal mucosa. It is necessary to monitor patients receiving intranasal corticosteroids for a long time.

Development of growth retardation in children is possible. In case of detection of growth retardation in children, it is necessary to reduce the dose of intranasal corticosteroids to the lowest that allows effective control of symptoms. In addition, the patient should be referred to a pediatrician for consultation.

If a local fungal infection of the nose or throat develops, it may be necessary to discontinue therapy with Nasonex® nasal spray and conduct special treatment... Persistent irritation of the nasal and pharyngeal mucosa for a long time may also serve as a reason for discontinuing treatment with Nasonex ® nasal spray.

When conducting placebo-controlled clinical studies in children, when Nasonex ® nasal spray was used in daily dose 100 μg for a year, growth retardation was not observed in children.

With prolonged treatment with Nasonex ® nasal spray, no signs of suppression of the HPA function were observed. Patients who switch to treatment with Nasonex ® nasal spray after prolonged therapy with systemic corticosteroids require special attention. Cancellation of systemic corticosteroids in such patients can lead to insufficiency of adrenal function, the subsequent recovery of which can take up to several months. If signs of adrenal insufficiency appear, you should resume taking systemic corticosteroids and take other necessary measures.

With the use of intranasal corticosteroids, systemic side effects may develop, especially with prolonged use in high doses. The likelihood of developing these effects is much less than with the use of oral corticosteroids. Systemic side effects may differ both in individual patients and depending on the GCS drug used. Potential systemic effects include Cushing's syndrome, characteristic features of Cushingoid, adrenal suppression, growth retardation in children and adolescents, cataracts, glaucoma, and, less commonly, a range of psychological or behavioral effects, including psychomotor hyperactivity, sleep disturbance, anxiety, depression, or aggression (especially in children).

During the transition from treatment with systemic corticosteroids to treatment with nasal spray Nasonex ®, some patients may experience initial symptoms of cancellation of systemic corticosteroids (for example, pain in joints and / or muscles, fatigue and depression), despite a decrease in the severity of symptoms associated with damage nasal mucosa. Such patients need to be specially convinced of the advisability of continuing treatment with Nasonex ® nasal spray. The transition from systemic to local corticosteroids can also reveal already existing, but masked by therapy, corticosteroids of systemic action allergic diseases such as allergic conjunctivitis and eczema.

Patients who are treated with GCS have a potentially reduced immune reactivity and should be warned about the increased risk of infection for them in case of contact with some patients. infectious diseases(For example, chickenpox, measles), as well as the need for medical advice if such contact has occurred. If signs of severe bacterial infection appear (for example, fever, persistent and sharp pain on one side of the face or toothache, swelling in the orbital or periorbital region), immediate medical advice is required.

When using the nasal spray Nasonex ® for 12 months, there were no signs of atrophy of the nasal mucosa. In addition, mometasone furoate tended to contribute to the normalization of the histological picture in the study of biopsies of the nasal mucosa.

With systemic and local (including intranasal, inhalation and intraocular) use of GCS, visual impairment may occur. If the patient has symptoms such as blurred vision or other visual impairments, the patient should be advised to see an ophthalmologist to identify possible causes of visual impairment, including cataract, glaucoma, or rare diseases, for example, central serous chorioretinopathy, which have been observed in some cases with systemic and local application of GCS.

The efficacy and safety of mometasone has not been studied in the treatment of unilateral polyps, polyps associated with cystic fibrosis, and polyps that completely obstruct the nasal cavity. If unilateral polyps of an unusual or irregular shape are detected, especially ulcerated or bleeding polyps, additional medical examination is necessary.

Influence on the ability to drive vehicles and work with mechanisms. There is no data on the effect of the drug Nasonex ® on the ability to drive vehicles or moving mechanisms.

Release form

Hormonal drugs have a number of side effects that can be caused by overuse or inappropriate use. Therefore, Nasonex, like other glucocorticoids, must be used strictly in accordance with the prescribed dosages and treatment periods. They are determined by the doctor. In case of non-compliance with the doctor's prescriptions, the drug can cause hormonal disorders in the body.

Composition and form of release

The active ingredient of the drug Nasonex is mometasone furoate. One spray dose contains 50 μg of active compound. In addition, a number of excipients are present in the drug:

• glycerol;
• dispersed cellulose;
• sodium citrate dihydrate;
• citric acid monohydrate;
• polysorbate 80;
• benzalkonium chloride;
• phenylethyl alcohol;
• water.

The dosage form of the drug is a white suspension. Nasonex in the nose is available in the form of a spray, in a bottle for 120 doses. The plastic bottle is equipped with a dispenser. This device virtually eliminates the possibility of drug overdose.

pharmachologic effect

Nasonex is a local remedy. It has a pronounced anti-inflammatory effect. The active ingredient of the drug is a synthetic glucocorticosteroid (GCS). It passes through cell membranes and inhibits the release of inflammatory substances. Nasonex nasal drops are capable of providing an adequate anti-inflammatory effect when used in doses that exclude systemic or general effects on the patient's body.

Nasonex in the form of a nasal spray is effective for both delayed and immediate allergic reactions. Studies were carried out, consisting in the ingress of a foreign agent into the nasal cavity of the subjects. The drug has shown its effectiveness by significantly lowering the level of the biologically active substance histamine and reducing the number of cells participating in the hypersensitivity reaction.

When used as a local agent, the active substance practically does not penetrate into the blood plasma. If the drug enters the gastrointestinal tract, it is eliminated from the body without a trace.

Indications and contraindications

Nasonex drops are prescribed for treatment, regardless of whether it occurs in a certain season or is present all year round. The manifestations of this disease resemble the common cold, therefore, before consulting a specialist, allergic rhinitis is most often not properly treated.

The drug in question is allowed to be taken by adults, as well as adolescents and children from 2 years of age. It is also effective as a means of preventing seasonal allergic rhinitis. In this case, it is recommended to start the course of admission 2-4 weeks before the start of the active flowering season.

The drug is used for exacerbation - inflammation of the mucous membrane of the paranasal sinuses. It can be a complication of allergic rhinitis. The most common type of sinusitis is inflammation of the maxillary or maxillary sinus. Nasonex with sinusitis has an effect if it is used as part of complex therapy, namely in combination with antibacterial agents. Such treatment is prescribed for adults, including patients over 65 years old, as well as children over 12 years old.

There are a number of contraindications to taking the drug:

• children under 2 years of age, since there is no data on the safety of the product;
• the occurrence of an allergic reaction to any component of the drug;
• recent surgery in the nasal cavity;
• recent injury to the nose;
• the presence of a local infection in the mucous membrane of the nasal cavity;
• tuberculosis infection respiratory tract;
• an untreated systemic infection caused by a virus, bacteria, or fungus;
• an infection caused by the herpes virus, proceeding with damage to the eyes (extremely careful use of the drug in these cases is possible as prescribed by a doctor).

Pregnancy and breastfeeding

Thorough studies on the effects of Nasonex drops on the body of a pregnant woman and the fetus have not been conducted. However, it should be assumed that since the active substance practically does not enter the blood plasma, its effect on the fetus will be negligible.

However, due to insufficient data on how exactly the drug works during pregnancy, it must be prescribed if the potential benefit outweighs the possible risk.

Instructions for use

The drug is used in the form of intranasal inhalation (through the nose). The correct dosage is ensured by the nozzle on the bottle. The instruction for use states that it is necessary to calibrate before the initial use of the tool - it is carried out by pressing the device 6-7 times. If inhalations have not been carried out for more than 14 days, the calibration must be repeated. Shake the bottle before use.

Adults and adolescents from 12 years old are recommended to carry out 2 sprays in each nostril. You need to carry out the procedure once a day. The daily dose will be 200 mcg. The daily dose of the drug for children over 2 years of age is 100 mcg - one injection into each nostril.

Nevertheless, the dosage is determined by the doctor, since it depends on the patient's pathology and his individual characteristics. The lack of a pronounced effect may require an increase in the dose. By contrast, a decrease in symptoms is accompanied by a decrease.

Undesirable manifestations

Side effects arising from the use of the drug Nasonex include headaches, nosebleeds, burning sensation in the nose, and pharyngitis - inflammation of the pharynx. Overdose leads to suppression of adrenal function and other hormonal disorders.

Patients using steroid anti-inflammatory drugs (GCS) for treatment should be regularly examined for any changes in the body. The strength of the immune system when using GCS decreases, so patients are more susceptible to infectious diseases.

The drug has a significant therapeutic effect, provided that all the doctor's prescriptions are followed. A careful study of the instructions for the use of nasonex nasal drops can, if possible, exclude side effects.

Useful video about nasal drops

One spray dose contains 50 mcg of anhydrous mometasone furoate and auxiliary components: dispersed cellulose (sodium carboxymethyl cellulose and MCC), glycerin, citric acid, polysorbate-80, sodium citrate dihydrate, benzalkonium chloride solution, purified water.

Release form

• Dosed spray Nasonex Sinus. Polyethylene bottles 10 g, packing No. 1. Each bottle is completed with a protective cap and a spray nozzle. The contents of the bottle are designed for 60 doses, each of which contains 50 μg of the active ingredient.
• Dosed spray Nasonex. Polyethylene bottles 18 g, packing No. 1. Each bottle is completed with a protective cap and a spray nozzle. The contents of the bottle are designed for 140 doses, each of which contains 50 μg of the active ingredient.

The contents of the vial is an almost white or white opaque suspension.

pharmachologic effect

The drug has anti-inflammatory activity and has antiallergic action .

Pharmacodynamics and pharmacokinetics

Is Nasonex hormonal or not?

The active substance of the spray is a synthetic GCS for local (inhalation) use, therefore, the drug Nasonex is hormonal .

Pharmacodynamics

Feature mometasone furoate is its ability to relieve inflammation and inhibit development allergic reaction even when used in doses that do not develop systemic effects.

The substance inhibits the release of inflammatory mediators, stimulates the production of lipomodulin, which is an inhibitor of phospholipase A. Due to this, the release of arachidonic acid is reduced and, accordingly, the synthesis of its metabolic products (Pg and endoperoxides) is suppressed.

Reduces the formation of chemotaxis substance, affecting the "late" (delayed) allergic reactions , and also prevents the development of immediate allergic reaction .

Studies with provocative tests with the application of antigens to the nasal mucosa have shown that Nasonex nasal spray exhibits high anti-inflammatory activity both at an early and late stage of development. allergic reaction .

This (in comparison with placebo) is confirmed by a decrease in activity and level histamine , as well as a decrease (compared to the initial level) in the number neutrophils , eosinophils and adhesion proteins of epithelial tissue cells.

In about a third of patients (28%) with seasonal allergic rhinitis a pronounced clinical effect was achieved within twelve hours after the first inhalation. In half of the patients, improvement occurred on average within 1.5 days (35.9 hours).

In addition, in patients suffering from seasonal rhinitis, the drug has shown significant effectiveness in reducing the severity of eye symptoms (itching, lacrimation, redness).

Pharmacokinetics

Bioavailability mometasone when applied topically, it is negligible (does not exceed 0.1%).

The substance is practically not found in blood plasma. The suspension is very poorly absorbed from the alimentary canal, and the small amount that can be swallowed and has time to be absorbed is actively metabolized even before excretion.

Metabolites are excreted mainly in the bile and, in small quantities, in the urine.

Indications for use

Indications for the use of Nasonex are:

• allergic rhinitis (seasonal or year-round) in children, adolescents and adults;
• exacerbation of chronic (the drug is prescribed as an adjunct to antibiotic therapy) in adolescents and adults;
• prevention of moderate / severe seasonal allergic rhinitis (It is considered optimal to start using the spray no later than 2 weeks before the expected start of the dusting period).

Nasal drops with GCS: Benacap , .

What analogs are cheaper than Nazonex?

The price of Nazonex analogues is from 128 rubles. The most inexpensive substitute for Nazonex is a nasal spray Desrinitis .

Which is better Nasonex or Avamis?

A drug Avamis is available in the form of an aqueous spray for intranasal administration. Its active substance is fluticasone furoate (the concentration of the substance in one dose is 27,% 5 mcg).

Fluticasone and mometasone , - these are the most modern drugs that are characterized by a very high degree of affinity for corticosteroids receptors and exceptional topical activity.

Both substances have extremely low absolute bioavailability. However, in mometasone this figure is slightly lower than that of fluticasone - 0.1% versus 0.5%.

Mometasone among all existing corticosteroids for intranasal administration, it has the lowest bioavailability and the fastest development of a therapeutic effect.

In addition, its use is allowed already from the age of two, while fluticasone furoate in pediatric practice it is used only for the treatment of children over six years old. Even with prolonged use mometasone does not adversely affect the growth of the child.

Nasonex or Fliksonase - which is better?

Fliksonase Is an endonasal aqueous spray based on micronized fluticasone propionate ... The concentration of the active substance in one dose is 50 μg.

The drug has a fast anti-inflammatory action on the nasal mucosa, and his antiallergic effect manifests itself after 2-4 hours after the first inhalation.

The effect (in particular, a decrease in nasal congestion) persists for a day after a single administration of Flixonase at a dose of 200 μg.

When used in therapeutic doses, the agent does not have any pronounced systemic activity and almost does not inhibit hypothalamic-pituitary-adrenal system .

Based on systematic reviews of comparative efficacy and safety fluticasone propionate and mometasone furoate carried out in the framework of the DERP project have shown that the differences in their effectiveness are very small. However, it should be borne in mind that fluticasone propionate characterized by a higher bioavailability than mometasone ... This indicator varies from 0.5 to 2%.

It is essential that Fliksonase in pediatrics it can be used only from the age of four.

FDA studies have shown that reducing the severity of symptoms allergic rhinitis according to the patients in the group fluticasone was more pronounced (45%) in comparison with the group mometasone (36%) and placebo group (11%).

Patients who received fluticasone , less often than patients who received mometasone and placebo, used additional drugs (for example, vasoconstrictor potassium in the nose) to alleviate the condition: frequency of use 42, 47 and 58%, respectively, for fluticasone , mometasone and a placebo.

Side effects when using fluticasone were also recorded less frequently (in particular, pharyngitis and gastrointestinal disorders),

Which is better Nazonex or Nazarel?

The active substance of the spray is fluticasone propionate (50 μg / dose), therefore, comparing the effectiveness of the drug with the effectiveness of Nasonex, we can say that, as is the case with Fliksonase and Avamis , it is comparable.

Research results and subjective feelings of patients taking different endonasal corticosteroids confirm that both drugs are effective and safe. However, the advantage Nazarela is its significantly lower cost (about 330-350 rubles for 120 doses).

Nazonex during pregnancy

After the introduction of the drug into the nasal cavity at the maximum permissible therapeutic dose, its active substance is not detected in the blood even at the minimum concentration.

Thus, its potential reproductive toxicity (including the effect on male / female fertility and the effect on the developing organism) is negligible.

However, due to the fact that well-controlled studies of the effect of mometasone furoata on the body in the case of its use during pregnancy and lactation was not carried out, the spray should be prescribed to pregnant women, mothers who breastfeed, and women of childbearing age only in cases where the expected effect of therapy justifies the potential risk to the fetus / newborn.

Newborn babies whose mothers received GCS during pregnancy should be examined for possible hypofunction of the adrenal cortex .

• Instructions for the use of Nasonex ®
• The composition of the drug Nasonex ®
• Indications of the drug Nasonex ®
• Storage conditions of the drug Nasonex ®
• Shelf life of the drug Nasonex ®

ATX code: Respiratory system (R)> Nasal medicines (R01)> Decongestants and other topical preparations (R01A)> Corticosteroids (R01AD)> Triamcinolone (R01AD11)

Release form, composition and packaging

Nasal spray (suspension) metered in the form of an opaque liquid of white or close to white color.

Excipients: dispersed cellulose, glycerol (glycerin), sodium citrate dihydrate, citric acid monohydrate, polysorbate 80, benzalkonium chloride, phenylethyl alcohol, purified water.

120 doses - polyethylene bottles (1) - cardboard boxes.

Description of the medicinal product NAZONEX ® based on the officially approved instructions for use of the drug and made in 2011. Updated date: 04.03.2011

pharmachologic effect

GCS for local use. It has a pronounced anti-inflammatory effect, which is manifested in doses that do not cause systemic effects.

The mechanism of anti-inflammatory and anti-allergic action of mometasone furoate is mainly associated with its ability to reduce the release of mediators of allergic reactions. Mometasone furoate significantly reduces the synthesis / release of leukotrienes from leukocytes in patients with allergic diseases. Mometasone furoate has shown a high potential in cell culture (at least 10 times more active than other steroids, including beclomethasone dipropionate, betamethasone, hydrocortisone and dexamethasone) in inhibiting the synthesis / release of IL-1, IL-6 and TNF-α. It also significantly inhibits the production of Th 2 cytokines, IL-4 and IL-5 from human CD4 + T cells. Mometasone furoate is also at least 6 times more active than beclomethasone dipropionate and betamethasone in inhibiting IL-5 production. In studies with provocative tests, with the application of antigens to the nasal mucosa, a high anti-inflammatory activity of the aqueous nasal spray Nasonex ® was shown both in the early and in the late stages of an allergic reaction. This was confirmed by a decrease (compared with placebo) in the level of histamine and eosinophil activity, as well as a decrease (compared to the baseline) in the number of eosinophils, neutrophils and adhesion proteins of epithelial cells.

A pronounced clinical effect was achieved in 28% of patients with seasonal allergic rhinitis in the first 12 hours of application of the water nasal spray Nasonex ®. On average (50%), relief occurred within 35.9 hours.

In clinical studies in patients with nasal polyps, a pronounced clinical efficacy of Nasonex ® was observed in relation to nasal congestion, polyp size, and restoration of the sense of smell, compared with placebo.

Pharmacokinetics

Suction

Mometasone furoate, when administered as a nasal spray, has a very low bioavailability (≤ 0.1%), and it is practically not detected in blood plasma, even when using a sensitive detection method with a sensitivity threshold of 50 pg / ml. In this regard, the relevant pharmacokinetic data for this dosage form does not exist. Mometasone furoate is very poorly absorbed from the gastrointestinal tract.

Metabolism

That small amount of a suspension of mometasone furoate that can penetrate into the gastrointestinal tract after intranasal inhalation, even before excretion in the urine or bile, undergoes active primary metabolism.

Indications for use

• treatment of seasonal or perennial allergic rhinitis in adults and children 2 years of age and older;
• as an auxiliary therapeutic agent in antibiotic treatment of exacerbations of sinusitis in adults (including senile age) and adolescents from 12 years old;
• treating nasal polyps and related symptoms, including nasal congestion and loss of smell in patients 18 years of age and older;
• prevention of moderate and severe seasonal allergic rhinitis (recommended 2-4 weeks before the expected start of the flowering season).

Dosage regimen

For treatment of seasonal and perennial rhinitis the recommended prophylactic and therapeutic dose is 2 injections (50 mcg each) into each nostril 1 time / day (total daily dose - 200 mcg). After achieving a therapeutic effect for maintenance therapy, it is advisable to reduce the dose to 1 injection in each nostril 1 time / day (total daily dose - 100 mcg). If it is not possible to achieve a clinical effect in the recommended therapeutic dose, then the daily dose can be increased to 4 injections into each nostril (total daily dose - 400 mcg). After symptom relief, dose reduction is recommended.

The onset of action of the drug is clinically manifested within the first 12 hours after the first use of the drug.

For sinusitis treatmentadults (including seniors) and adolescents from 12 years old the recommended therapeutic dose is 2 injections (50 mcg) into each nostril 2 times / day. The total daily dose is 400 mcg. If it is not possible to achieve a clinical effect in the recommended therapeutic dose, then the daily dose can be increased to 4 injections into each nostril 2 times / day (total daily dose - 800 mcg). After symptom relief, dose reduction is recommended.

At nasal polyps for adults (including elderly patients) and adolescents aged 18 years and older the recommended dose is 2 injections (50 mcg) into each nostril 2 times / day (total daily dose is 400 mcg). After achieving the clinical effect, it is recommended to reduce the dose to 2 injections into each nostril 1 time / day (total daily dose - 200 mcg).

Before the first use of Nasonex ® nasal spray, 6-7 "calibration" presses of the dosing device must be performed. After "calibration", a stereotyped delivery is established medicinal substance which releases approximately 100 mg of a suspension of mometasone furoate containing 50 μg of mometasone (one dose) with each press of a button. If the nasal spray has not been used for 14 days or longer, a recalibration is required before using it again.

Shake the bottle vigorously before each use.

If the nozzle is clogged, then remove the plastic cap by gently pressing on the white ring, easily remove the nozzle, rinse it with cold running water, dry it and reinstall it.

Side effects

Side effects reported in clinical trials in the treatment of seasonal and perennial allergic rhinitis: headache (8%);

In children, the incidence of side effects, incl. the incidence of nosebleeds (6%), headache (3%), nasal irritation (2%) and sneezing (2%) was comparable to the incidence with placebo.

Rarely - allergic reaction immediate type (eg, bronchospasm, dyspnea); very rarely - anaphylactic reaction and angioedema.

In isolated cases - violations of taste and smell.

Use as an adjuvant in the treatment of acute episodes of sinusitis: the incidence of side effects was comparable to that with placebo - headache (2%), pharyngitis (1%), burning sensation in the nose (1%) and irritation of the nasal mucosa (1%). Nosebleeds were moderately pronounced, and the frequency of their occurrence when using Nasonex was also comparable to the frequency of nosebleeds when using placebo (5% and 4%, respectively).

When treating nasal polyps the total number of the above side effects was comparable to those with placebo and similar to those observed in patients with allergic rhinitis.

Rarely with intranasal use of corticosteroids, there have been cases of perforation of the nasal septum or increased intraocular pressure.

Application during pregnancy and lactation

Special, strictly controlled studies of the use of Nasonex during pregnancy have not been conducted. After intranasal administration of the drug at the maximum therapeutic dose, mometasone is not detected in blood plasma even at a minimum concentration; therefore, the effect of the drug on the fetus can be expected to be very small and the potential toxicity to reproduction very low.

Prescribing the drug during pregnancy and lactation, as well as women of childbearing age, is possible only if the intended benefit to the mother outweighs the potential risk to the fetus or infant.

Newborns whose mothers received GCS during pregnancy should be carefully examined to identify possible adrenal hypofunction.

special instructions

The use of the drug for the treatment of young children should be with the help of adults.

The drug should not be used in the presence of untreated local infection with involvement of the nasal mucosa in the process. Due to the fact that corticosteroids inhibit wound healing, such drugs should not be prescribed for local intranasal use in patients who have recently undergone surgery or nasal trauma until the wounds are completely healed.

Nasonex ® should be prescribed with caution (or not at all) to patients with active or latent tuberculosis infection of the respiratory tract, as well as untreated fungal, bacterial, systemic viral infection or for an infection caused by Herpes simplex with eye damage.

After 12 months of treatment with Nasonex®, no symptoms of atrophy of the nasal mucosa were observed. In addition, under the influence of mometasone furoate, there was a tendency to normalize the histological picture in the study of biopsies of the nasal mucosa. As with any long-term treatment, patients who have been using Nasonex ® nasal spray for several months or more should be examined periodically to identify possible changes in the nasal mucosa. If a local fungal infection of the nose or pharynx develops, it may be necessary to discontinue the drug Nasonex ® or to carry out special treatment. Irritation of the nasal and pharyngeal mucosa, which persists for a long time, may also be an indication to discontinue treatment with this drug.

With prolonged treatment with Nasonex, no signs of suppression of the function of the hypothalamic-pituitary-adrenal system were observed. When switching to treatment with Nasonex® nasal spray after long-term therapy with systemic GCS, patients need special control. Cancellation of systemic GCS in such patients can lead to adrenal insufficiency, which may require appropriate measures. During the transition from treatment with systemic corticosteroids to treatment with Nasonex, some patients may experience symptoms of corticosteroids withdrawal (for example, joint and / or muscle pain, fatigue and depression). Such patients need to be specially convinced of the advisability of continuing treatment with Nasonex. When changing therapy, previously developed allergic diseases, such as allergic conjunctivitis and eczema, which were previously masked by systemic GCS therapy, may also appear.

Patients receiving GCS have a potentially reduced immune reactivity and should be warned of the increased risk of infection in case of contact with certain infectious diseases (for example, chickenpox, measles), as well as the need to consult a doctor if such contact occurs.

Use in pediatrics

When conducting placebo-controlled clinical trials in children, when Nasonex® was used in a daily dose of 100 μg for a year, no growth retardation was observed in children.

The safety and efficacy of Nasonex in the treatment of nasal polyps in children and adolescents under 18 years of age.

Overdose

The drug has a low (≤0.1%) systemic bioavailability, so it is unlikely that in case of an overdose, any special measures will be required, other than observation and subsequent administration at the recommended dose.