Nasonex: relieves allergic rhinitis

Composition and dosage form of the drug

The active component of the drug is mometasone furoate, a hormonal substance with a pronounced antiallergic effect. The therapeutic effect is observed when using microscopically small doses that are unable to influence the body systemically.

Nasonex is available in the form of a nasal spray: in plastic bottles of 18 g each, equipped with a dispenser nozzle. One package of the drug is designed for 140 doses. Nasonex Sinus spray of identical composition is produced in 10 g bottles containing about 60 therapeutic doses.

The solution is a liquid, opaque, whitish suspension with a concentration of 50 mcg of glucocorticosteroid per dose. Spray excipients: citric acid, glycerin, polysorbate, distilled water and others.

The mechanism of action of the drug Nasonex

Mometasone inhibits the release of inflammatory mediators. At the same time, it activates the release of a blocker of the enzyme phospholipase A, which is responsible for the intensity of the immune reaction to antigens. When using a nasal spray, nasal discharge and accompanying other signs of allergy are reduced: conjunctivitis, lacrimation, swelling, itching, hyperemia.

The drug is effective against rapidly developing intolerance and helps prevent delayed allergies. Symptoms as a result of use are reduced at all stages of the pathology. They can be completely eliminated within 1–2 days from the start of treatment.

When applied topically, the drug substances are absorbed into the systemic bloodstream in a negligible concentration, without causing harm to the body.

Nasonex

The drug is used intranasally.

Treatment of seasonal or year-round allergic rhinitis

Adults (including elderly patients) and adolescents from 12 years of age

The recommended preventive and therapeutic dose of the drug is 2 inhalations (50 mcg each) into each nostril 1 time / day (total daily dose - 200 mcg). Upon achieving a therapeutic effect for maintenance therapy, it is possible to reduce the dose to 1 inhalation in each nostril 1 time / day (total daily dose - 100 mcg).

If a reduction in the symptoms of the disease cannot be achieved by using the drug at the recommended therapeutic dose, the daily dose can be increased to 4 inhalations into each nostril 1 time per day (total daily dose - 400 mcg). After the symptoms of the disease decrease, a dose reduction is recommended.

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

Children aged 2 to 11 years

The recommended therapeutic dose is 1 inhalation (50 mcg) into each nostril 1 time / day (total daily dose - 100 mcg).

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

Adjuvant treatment of acute sinusitis or exacerbation of chronic sinusitis

Adults (including elderly patients) and adolescents from 12 years of age

The recommended therapeutic dose is 2 inhalations (50 mcg each) into each nostril 2 times a day (total daily dose - 400 mcg).

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

Treatment of acute rhinosinusitis without signs of severe bacterial infection

The recommended dose for adults and adolescents is 2 inhalations of 50 mcg in each nasal passage 2 times a day (total daily dose 400 mcg). If symptoms worsen during treatment, consultation with a specialist is necessary.

Treatment of nasal polyposis

For adults (including elderly patients) over 18 years of age, the recommended therapeutic dose is 2 inhalations (50 mcg each) into each nostril 2 times a day (total daily dose - 400 mcg).

After the symptoms of the disease have reduced, it is recommended to reduce the dose to 2 inhalations (50 mcg each) into each nostril 1 time / day (total daily dose - 200 mcg).

Rules for using Nasonex®

Inhalation of the suspension contained in the spray bottle is carried out using a special dispensing nozzle on the bottle.

Before using Nasonex® nasal spray for the first time, it is necessary to calibrate by pressing the dispensing device 10 times until splashes appear, indicating that the drug is ready for use.

You should tilt your head and inject the medicine into each nostril as recommended by your doctor.

If the nasal spray has not been used for 14 days or longer, press the dispenser nozzle 2 times until it sprays.

Before each use, shake the bottle vigorously.

Cleaning the dispensing nozzle

It is important to clean the dispensing nozzle regularly to prevent it from malfunctioning. Remove the cap that protects the nozzle from dust, then carefully remove the spray tip. It is necessary to thoroughly rinse the spray tip and dust cap in warm water and rinse under the tap.

Do not attempt to open the nasal applicator with a needle or other sharp object, as This will damage the applicator, which may result in the wrong dose being given.

Dry the cap and tip in a warm place. After this, you need to 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, you must recalibrate by pressing the dispensing nozzle 2 times.

Overdose

With long-term use of GCS in high doses or with the simultaneous use of several GCS, suppression of the hypothalamic-pituitary-adrenal system is possible.

Who is Nasonex indicated for?

The use of the drug to prevent the appearance or exacerbation of allergic rhinitis is allowed for adults and children over 2 years of age. Nasonex helps:

with allergic mucus discharge from the nose;
with pathological reactions to pollen during flowering of plants, animal hair, exposure to other antigens.

In complex therapy, the drug is used to eliminate acute and chronic sinusitis. In these cases, its use is indicated for patients over 12 years of age.

Contraindications

Instructions for use of Nasonex require you to refuse treatment with it:

in the presence of viral, bacterial, fungal inflammatory processes of the nasal mucosa, including those not completely cured;
with herpes of the eye mucosa;
with open and closed forms of tuberculosis;
in case of hypersensitivity to the main substance or additional components of the drug.

Relative contraindications to the use of nasal spray: mechanical injuries of the nasal septum, disruption of the integrity of the mucous membrane, postoperative complications accompanied by bleeding. In these cases, it is necessary to wait until the tissues have completely healed.

Special instructions for the use of Nasonex

The use of the drug in young children should be carried out with the help of adults. Nasonex should not be used in the presence of local infection involving the nasal mucosa. Due to the fact that corticosteroids slow down wound healing, the drug should not be prescribed to patients who have recently undergone surgery or nasal trauma until the wounds have completely healed. Nasonex should be prescribed with caution or not at all to patients with active or latent tuberculosis infection, as well as untreated fungal, bacterial, systemic viral infections, and ophthalmic infections caused by the herpes simplex virus. After 12 months of treatment with Nasonex, there was no atrophy of the nasal mucosa; In addition, when using mometasone furoate, there was a tendency towards normalization of the histological picture when examining biopsy samples of the nasal mucosa. However, patients who use Nasonex for several months or longer should undergo periodic examination 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 Nasonex therapy and carry out special therapy. Irritation of the mucous membrane of the nasal cavity and pharynx, which persists for a long time, may also be an indication to discontinue treatment with Nasonex. With long-term treatment with Nasonex, no signs of suppression of the hypothalamic-pituitary-adrenal system were noted. Patients who switch to treatment with Nasonex after prolonged systemic therapy with GCS should be under medical supervision. Withdrawal of systemic corticosteroids in such patients may lead to insufficiency of adrenal cortex function, which may require appropriate measures. During the transition from treatment with systemic corticosteroids to treatment with Nasonex, some patients may experience symptoms of corticosteroid withdrawal (arthralgia, myalgia, fatigue and depression). A change in therapy may also reveal allergic diseases that were previously masked by the use of systemic GCS therapy (allergic conjunctivitis, eczema, etc.). Patients receiving GCS therapy have a potentially reduced immunological reactivity and should be warned about the increased risk of infection in case of contact with patients with certain infectious diseases (for example, chicken pox, measles), as well as the need to consult a doctor if such contact has occurred. Patients should be warned to seek immediate medical attention if signs or symptoms of a severe bacterial infection occur, such as fever, severe unilateral facial or toothache, orbital or periorbital swelling/edema, or worsening after initial improvement. Children. In placebo-controlled clinical studies in children in whom Nasonex was used at a daily dose of 100 mcg for 1 year, no growth retardation was observed. The safety and effectiveness of Nasonex in the treatment of nasal polyps in children and adolescents under 18 years of age, symptoms of rhinosinusitis in children under 12 years of age, and seasonal or year-round allergic rhinitis in children under 2 years of age have not been studied. Use during pregnancy and lactation. Special studies of the effect of the drug during pregnancy have not been conducted. After intranasal administration of the drug at the maximum therapeutic dose, mometasone is not detected in the blood plasma even at the minimum concentration. Therefore, it can be expected that the effect of the drug on the fetus will be insignificant, and the potential toxicity regarding reproductive function will be very low. However, like other corticosteroids for intranasal use, Nasonex should be prescribed during pregnancy or lactation only if the expected benefits of its use justify the potential risk to the mother, fetus or infant. Children whose mothers received corticosteroids during pregnancy should be examined to identify possible adrenal hypofunction.

Adverse reactions when using Nasonex spray

During treatment with the drug, the following are occasionally observed:

headache;
a feeling of dryness, burning and itching of the mucous membrane in the sinuses and larynx;
pharyngitis;
bloody discharge from the nose;
sneezing, coughing;
increased lacrimation, photophobia.

Side effects in most cases are observed in the first 1–2 days of using the medication. Subsequently, unwanted reactions decrease and disappear on their own. If negative symptoms increase, additional consultation with an otolaryngologist and discontinuation of the drug are required.

Instructions for use of Nasonex spray

Before first use, the bottle nozzle must be calibrated by checking its functionality: press several times. The spray is sprayed intranasally, carefully inserting the tip of the dispenser into each nostril. In this case, the head must be slightly moved back.

For allergic rhinitis in adults and adolescents, the product is sprayed twice a day: 2 pumps in each nostril. When symptoms decrease, reduce the daily dose by half.
If signs of allergy persist, it is permissible to increase the number of injections to 4 once. In case of severe pathology, repeat the procedure twice a day.
Children under 12 years of age are allowed to administer the medicine once a day, one injection into each nostril.

No negative health consequences have been recorded with a single overdose of the drug. Regularly exceeding the volume of the spray can provoke disturbances in the functioning of the pituitary gland and hypothalamus.

During the treatment period, it is important to stay as little as possible in places where allergens accumulate, to avoid dusty rooms, abundantly flowering parks and gardens.

Pharmacological properties of the drug Nasonex

Pharmacodynamics. Mometasone furoate is a synthetic corticosteroid for topical use with a pronounced anti-inflammatory effect. Mometasone furoate has a local anti-inflammatory effect in doses, the use of which does not cause systemic GCS effects. The mechanism of anti-inflammatory and antiallergic action of mometasone furoate is mainly associated with its ability to inhibit 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 demonstrated in cell culture a high potential (at least 10 times higher activity than other steroids, including beclomethasone dipropionate, betamethasone, hydrocortisone and dexamethasone) to inhibit the synthesis/release of interleukins (IL-1, IL-6) and necrosis factor tumors (TNF-α); it also significantly inhibits the production of Th2 cytokines, IL-4 and IL-5 by CD4+ T cells. Mometasone furoate is also at least 6 times more potent in inhibiting IL-5 production than beclomethasone dipropionate and betamethasone. In studies with provocative tests with the application of antigens to the mucous membrane of the nasal cavity, the high anti-inflammatory activity of the Nasonex aqueous nasal spray was established in both the early and late stages of the allergic reaction. This was confirmed by a decrease (compared to placebo) in histamine levels and eosinophilic granulocyte activity, as well as a decrease (compared to baseline) in the number of eosinophilic and neutrophilic granulocytes and epithelial cell adhesion proteins. A pronounced clinical effect in the first 12 hours after using Nasonex aqueous nasal spray was observed in 28% of patients with seasonal allergic rhinitis. In 50% of patients, improvement occurred on average within 35.9 hours. In addition, when using Nasonex, significant effectiveness was noted in reducing the severity of visual symptoms (redness, lacrimation, itching) in patients with seasonal allergic rhinitis. In clinical studies in patients with nasal polyps, Nasonex was significantly effective compared to placebo in reducing nasal congestion, polyp size, and restoring the sense of smell. In clinical studies involving patients aged 12 years, the use of Nasonex 200 mcg 2 times a day demonstrated high effectiveness in reducing the symptoms of rhinosinusitis compared to placebo. During 15 days of treatment, symptoms of rhinosinusitis were assessed using the Major Symptom Score (MSS - pain in the face, sensation of pressure and pain when pressing in the area and projection of the paranasal sinuses, rhinorrhea, mucus flow down the back of the throat and nasal congestion) . The effectiveness of amoxicillin 500 mg 3 times a day was not significantly different from placebo in reducing symptoms of rhinosinusitis according to the MSS scale. During the follow-up period after completion of treatment, the number of relapses in the Nasonex group was lower and comparable to the amoxicillin and placebo groups. The duration of treatment for acute rhinosinusitis beyond 15 days has not been assessed. Pharmacokinetics. Mometasone furoate, when administered as an aqueous nasal spray, has low bioavailability (≤0.1%), it is practically undetectable in blood plasma, even when using a detection method with a sensitivity threshold of 50 pg/ml. Therefore, there are no relevant pharmacokinetic data for this dosage form. A small amount of mometasone furoate suspension, which can enter the gastrointestinal tract after intranasal administration, undergoes active primary metabolism even before excretion in urine or bile.