Desrinit, spray 50 mcg/dose 18 g 140 doses

Pharmacotherapeutic group: glucocorticosteroid for topical use

ATX code: R01AD09

Pharmacological properties

Pharmacodynamics

Mometasone is a synthetic glucocorticosteroid (GCS) for topical use. It has anti-inflammatory and anti-allergic effects. The local anti-inflammatory effect of the drug is seen when it is used in doses at which there are no systemic effects.

Inhibits the release of inflammatory mediators. It increases production of lipomodulin, which is an inhibitor of phospholipase A, which causes reduction of release of arachidonic acid and, accordingly, inhibition of synthesis of products of arachidonic acid metabolism – cyclic endoperoxides, prostaglandins. It prevents marginal accumulation of neutrophils, which reduces inflammatory exudate and lymphokine production, inhibits macrophage migration, leads to a decrease in infiltration and granulation processes. It reduces inflammation due to decrease in formation of chemotaxis substance (effect on late allergic reactions), inhibits development of allergic reaction of immediate type (due to inhibition of formation of arachidonic acid metabolites and reduction of release of inflammatory mediators from mast cells).

In studies with provocation tests with application of antigens to the nasal mucosa high anti-inflammatory activity of the drug was demonstrated both in the early and late stages of the allergic reaction. When compared to placebo, a decrease in histamine levels and eosinophil activity as well as a decrease (compared to baseline) in the number of eosinophils, neutrophils and epithelial cell proteins was found.

Pharmacokinetics

In intranasal administration, the systemic bioavailability of mometasone furoate is <1% (with a sensitivity of 0.25 pg/mL detection method). Mometasone suspension is very poorly absorbed in the gastrointestinal (GI) tract, and the small amount of mometasone suspension that may enter the GI tract after nasal aspiration undergoes active primary metabolism before being excreted with urine or bile.

Indications

Active ingredient

Composition

Active ingredient:

mometasone furoate monohydrate (in terms of mometasone furoate) 0.052 mg (0.050 mg);

Associates:

Avicel RC-591 (microcrystalline cellulose, sodium carmellose) – 2 mg,

Glycerol – 2.1 mg,

benzalkonium chloride solution 500 g/l – 40 µg,

polysorbate 80 – 10 µg,

citric acid monohydrate – 200 micrograms,

sodium citrate dihydrate – 280 micrograms,

water d/i – q.s. up to 100 mg.

How to take, the dosage

Intranasally. The suspension contained in the bottle is injected using a special dispensing device on the bottle.

The dosing device must be “calibrated” before the first use of the product.

Do not pierce the nasal applicator (spray tip).

The dispenser must be pressed 10 times or until a homogenous spray appears, indicating that the product is ready to use.

Tilt your head and inject the medication into each nasal passage as instructed by your healthcare provider.

If the medication has not been used for 14 days or longer, you need to press the dispenser 2 times or until a smooth spray appears.

Tilt your head and inject the medication into each nasal passage as recommended by your doctor.

Cleaning the dispensing device

It is important to clean the dispensing device regularly to prevent malfunction. Remove the dust cap to protect the unit, then gently remove the spray tip. Rinse the spray tip and dust cap thoroughly in warm water and rinse under the tap.

Do not try to open the nasal applicator (spray tip) with a needle or other sharp object, as this will damage the applicator and you may take the wrong dose of product.

Dry the cap and tip in a warm place. Then reattach the spray tip to the bottle and screw the cap back onto the bottle to protect it from dust. The first time you use the nasal spray after cleaning, you need to recalibrate by pressing the dispenser 2 times.

Shake the bottle vigorously before each use.

Treatment of seasonal and year-round allergic rhinitis

Healthadults (including the elderly) and adolescents from 12 years of age./u>

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

If reduction of symptoms is not achieved by using the drug in the recommended therapeutic dose, the daily dose can be increased to 4 injections into each nasal passage 1 time daily (total daily dose is 400 mcg).

Dose reduction is recommended once symptoms have decreased.

The onset of action of the drug is usually seen clinically as early as 12 hours after the first use of the drug.

Children 2-11 years

The recommended therapeutic dose for the treatment of seasonal or year-round allergic rhinitis is 1 injection (50 mcg of mometasone furoate) into each nasal passage once daily (total daily dose is 100 mcg).

In young children, the use of the drug requires the help of adults.

Auxiliary treatment for acute sinusitis or exacerbation of chronic sinusitis

Adultsadults (including the elderly) and adolescents from 12 years of age

The recommended therapeutic dose is 2 injections (50 mcg each) into each nasal passage 2 times daily (total daily dose is 400 mcg).

If reduction of symptoms is not achieved by using the drug in the recommended therapeutic dose, the daily dose of the drug may be increased to 4 injections into each nasal passage 2 times a day (the total daily dose is 800 mcg). Once the symptoms of the disease have decreased, a reduction in the dose is recommended.

Treatment of acute rhinosinusitis without signs of severe bacterial infection

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

Treatment of nasal polyposis

Adults (including the elderly) over 18 years

.p> Recommended therapeutic dose is 2 injections (50 mcg each) into each nasal passage 2 times a day (total daily dose is 400 mcg).

After reduction of symptoms, it is recommended that the dose be reduced to 2 injections (50 mcg each) in each nasal passage once daily (total daily dose is 200 mcg).

Interaction

Special Instructions

As with any treatment, patients using mometasone nasal spray dosage form for several months or longer should periodically be monitored by a physician for possible nasal mucosal changes.

Patients receiving intranasal GCS for a long time should be monitored. Growth retardation in children is possible. If growth retardation in children is detected, the dose of intranasal GCS should be reduced to the lowest dose that effectively controls symptoms. In addition, the patient should be referred to a pediatrician for consultation.

If a local fungal infection of the nose or pharynx develops, it may be necessary to discontinue therapy with mometazone in the dosage form of nasal spray and perform specific treatment. Persistent long-term irritation of the mucous membranes of the nose and pharynx may also serve as a reason for discontinuing treatment with mometazone in dosage form – nasal spray.

In placebo-controlled clinical studies in children when mometasone nasal spray dosage form was used in a daily dose of 100 mcg for one year, no growth retardation was observed in children.

There were no signs of suppression of hypothalamic-pituitary-adrenal function during long-term treatment with mometasone nasal spray.

Patients who switch to treatment with mometazone in dosage form nasal spray after long-term therapy with systemic glucocorticosteroids require special attention. Withdrawal of systemic glucocorticosteroids in such patients may lead to insufficiency of adrenal function, subsequent recovery of which may take up to several months. If signs of adrenal insufficiency appear, systemic glucocorticosteroids should be restarted and other necessary measures taken.

The use of intranasal GCS may result in systemic side effects, especially with prolonged use at high doses. The likelihood of these effects is significantly less than with oral GCS.

Systemic side effects may vary in individual patients and depending on the glucocorticosteroid drug used. Potential systemic effects include Cushing’s syndrome, characteristic cushingoid signs, suppression of adrenal function, growth retardation in children and adolescents, cataracts, glaucoma, and less commonly a number of psychological or behavioral effects, including psychomotor hyperactivity, sleep disturbance, anxiety, depression or aggression (especially in children).

During the transition from systemic glucocorticosteroid treatment to treatment with mometazone nasal spray, some patients may experience initial symptoms of withdrawal from systemic glucocorticosteroids (e.g., joint and/or muscle pain, fatigue and depression) despite a reduction in symptoms associated with nasal mucosal damage. If these symptoms occur, systemic glucocorticosteroids should be restarted and other necessary measures taken. Switching from systemic to topical glucocorticosteroids may also reveal pre-existing but masked systemic glucocorticosteroid therapy for allergic conditions such as allergic conjunctivitis and eczema.

Patients treated with glucocorticosteroids have potentially compromised immune reactivity and should be advised of their increased risk of exposure to certain infectious diseases (e.g., chickenpox, measles) and the need for medical consultation if this occurs.

If there are signs of a serious bacterial infection (e.g., fever, persistent or severe pain on one side of the face or toothache, swelling of the orbital or periorbital area), you should get immediate medical advice.

No signs of nasal mucosal atrophy have occurred when using mometasone in the dosage form nasal spray for 12 months. In addition, mometasone furoate tended to promote normalization of the histological picture in nasal mucosal biopsy specimens.

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 cover the nasal cavity.

If unilateral polyps of unusual or irregular shape, particularly ulcerated or bleeding polyps, are detected, further medical evaluation should be performed.

Sight disturbances have been reported with systemic and topical use of corticosteroids. If a patient presents with symptoms such as blurred vision or other visual disturbances, consideration should be given to referring the patient to an ophthalmologist for evaluation of possible causes, which may include cataracts, glaucoma, or rare conditions such as central serous chorioretinopathy (CCP).

Influence on ability to drive or operate machinery

There are no data on the effect of Desrinit drug on the ability to drive or operate moving machinery.

Contraindications

Hypersensitivity to mometazon or any of the drug components; childhood (in seasonal and year-round allergic rhinitis – under 2 years; in acute sinusitis or exacerbations of chronic sinusitis – under 12 years; in nasal polyposis – under 18 years); recent surgery or nasal trauma with damage of the nasal mucosa – until the wound healing (due to the inhibiting effect of GCS on healing processes).

Cautions

Desrinit should be used with caution in cases of tuberculosis infection (active or latent) of the respiratory tract, untreated fungal, bacterial, systemic virus infection or infection caused by Herpes simplex with eye involvement (as an exception, the drug may be prescribed for the above infections as directed by a physician), the presence of untreated local infection with involvement of the nasal mucosa.

Side effects

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

Nasal bleeding was generally moderate and stopped on its own, with a slightly higher incidence than with placebo (5%) but equal to or lower than with other intranasal GCSs used as active controls (some had incidence rates of up to 15%). The incidence of all other adverse events was comparable to that of placebo administration.

The overall incidence of adverse events in patients treated for nasal polyposis was comparable to the incidence in patients with allergic rhinitis.

The overall incidence of adverse events in patients treated for acute rhinosinusitis was comparable to the incidence in patients with allergic rhinitis and when given placebo.

The use of intranasal GCS may cause systemic adverse effects, especially with long-term use of high-dose intranasal GCS (see section “Cautionary Note”).

Table 1

The frequency of adverse reactions is established as follows:

very common (≥1/10); common (≥1/100,< 1/10), rare (≥1/1000,< 1/100).

For adverse reactions during post-registration follow-up, the frequency has not been determined (cannot be determined based on available data).

System-organ class.

very often

Frequently

Rarely

Frequent

Infectious and parasitic diseases

Pharyngitis, upper respiratory tract infections

sup>*

Disorders of the immune system

/p>

Hypersensitivity reactions, including anaphylactic reactions, angioedema, bronchospasm, dyspnea

Nervous system disorders

Headache

Visual disturbances

/td>

Impaired visual clarity (see “Special Indications. Special Indications)

Elevated intraocular pressure, glaucoma, cataracts

Respiratory system, thoracic and mediastinal disorders

Nasal bleeding**

Nasal bleeding (ie.е. obvious bleeding, as well as secretion of blood stained mucus or blood clots), burning sensation in the nose, irritation of the nasal mucosa, ulceration of the nasal mucosa

Nasal septal perforation

Gastrointestinal disorders

Pharyngeal irritation (feeling of irritation of the pharyngeal mucosa)**

/p>

Impairment of taste and smell

* detected with a frequency of “rare” when the drug is used twice daily for nasal polyposis

/p>

** revealed when the drug is used twice daily for nasal polyposis

Children

Disorders of the respiratory system, thoracic and mediastinal organs: nasal bleeding (6%), nasal mucous membrane irritation (2%), sneezing (2%).

Nervous system disorders:headache (3%).

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

Overdose

Pregnancy use

Similarities