NASONEX NASAL SPRAY 50MCG/DOSE

For medical use of the drug

NAZONEKS®

Trade (proprietary) name of the drug - NAZONEX®

INN - mometasone (mometasone).

Dosage Form - spray nasal dosed.

Composition
1g spray contains:
Active substance: Mometasone furoate (micronized, in the form of monohydrate) in equivalent to mometasone furoate anhydrous - 0.5 mg.
Excipients: dispersed cellulose (microcrystalline cellulose treated with carmellose sodium), glycerol, citric acid monohydrate, sodium chitrate dihydrate, polysorbate 80, benzalkonium chloride (as a 50% solution), phenylethanol, purified water.

Description
Suspension white or almost white.

Pharmacotherapeutic group
Glucocorticosteroid for topical use.

Pharmacology

Pharmacodynamics.
Mometasone is a synthetic glucocorticosteroid (GCS) for topical use. It has anti-inflammatory and anti-allergic effects when used in doses that do not cause systemic effects. Slows down the release of inflammatory mediators. It increases the production of lipomodulin, which is an inhibitor of phospholipase A, which causes a decrease in the release of arachidonic acid and, accordingly, inhibition of the synthesis of products of the metabolism of arachidonic acid - cyclic endoperexia, prostaglandins.It warns the regional accumulation of neutrophils, which 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 the "late" allergy reaction), inhibits the development of an immediate type allergic reaction (due to inhibition of the production of arachidonic acid metabolites and reduced release of inflammatory mediators from mast cells).
In studies with provocative tests with the application of antigens on the mucous membrane of the nasal cavity, high anti-inflammatory activity of mometasone was demonstrated in both the early and late stages of the allergic reaction.
This was confirmed by a decrease (compared to placebo) of histamine level and eosinophil activity, as well as a decrease (compared to baseline) of the number of eosinophils, neutrophils and epithelial cell adhesion proteins.

Pharmacokinetics.
Mometasone is characterized by negligible bioavailability (≤0.1%), and when administered as an inhalation, it is practically not detected in the blood plasma, even when using a sensitive method of determination with a sensitivity threshold of 50 pg / ml. In this regard, the corresponding pharmacokinetic data for this dosage form does not exist; (Mometasone suspension is very poorly absorbed in the gastrointestinal tract.That small amount of mometasone suspension that can enter the gastrointestinal tract after nasal inhalation, even before excretion in urine or bile, is subject to active primary metabolism.

Indications

• Seasonal and perennial 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 of age - as an auxiliary therapeutic agent for treatment with antibiotics.
• Preventive treatment of moderate-to-severe seasonal allergic rhinitis in adults and adolescents from the age of 12 (recommended two to four weeks before the expected start of the dusting season).
• Nasal polyposis, accompanied by a violation of nasal breathing and smell, in adults (from 18 years).

  Contraindications

• Hypersensitivity to any of the substances that make up the drug.
• The presence of an untreated local infection involving the nasal cavity mucosa.
• The recent surgery or injury of the nose with damage to the nasal mucosa - to wound healing (due to the inhibitory effect of the SCS on the healing process).
• Children 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
  NAZONEKS® should be used with caution in tuberculosis 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, the drug may be prescribed for the listed infections as directed by the doctor)

  Use during pregnancy and lactation
  After intranasal use of the drug at a therapeutic dose of 400 mcg per day, 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 negligible, and the potential toxicity regarding reproductive function is very low.
  However, due to the fact that there were no special, well-controlled studies of the effect of the drug in pregnant women, NAZONEKS® should be prescribed to variable or breastfeeding only if the expected benefit from the appointment of the drug justifies the potential risk to the fetus or infant.
  Infants whose mothers received GCS during pregnancy should be carefully examined for possible adrenal hypofunction.

  Dosage and administration
  Intranasal. Inhalation of the suspension contained in the spray vial is carried out using a special dispensing nozzle on the vial.
  Before the first use of the nasal spray NAZONEKS® it is necessary to "calibrate" it by pressing the dosing device 6-7 times.After the “calibration”, a stereotypic drug supply is established, with each press of the metering device emitting approximately 100 mg of the suspension containing mometasone furoate (as a monohydrate) in an amount equivalent to 50 μg of mometasone anhydrous furoate. If the nasal spray has not been used for 14 days or longer, then a new “calibration” is necessary before the new application.
  Before each use, vigorously shake the spray bottle.

  Treatment of seasonal or year-round allergic rhinitis
  Adults (including the elderly) and adolescents from 12 years:
  The recommended prophylactic and therapeutic dose of the drug is 2 inhalations (50 mcg each) in each nostril 1 time per day (total daily dose - 200 mcg). Upon reaching the therapeutic effect for maintenance therapy, it is possible to reduce the dose to 1 inhalation in each nostril 1 time per day (total daily dose - 100 mcg).
  If the reduction of the symptoms of the disease cannot be achieved by using the drug at the recommended therapeutic dose, the daily dose may be increased to 4 inhalations in each nostril 1 time per day (total daily dose of -400 mcg). After reducing the symptoms of the disease, a dose reduction is recommended. The onset of action of the drug is usually marked clinically within 12 hours after the first use of the drug.
  Children 2-11 years old:
  The recommended therapeutic dose is 1 inhalation (50 mcg) in each nostril once a day (total daily dose is 100 mcg).
  To use the drug in young children need help. Adults.

  Auxiliary treatment of acute sinusitis or exacerbation of chronic sinusitis
  Adults (including the elderly) and adolescents from 12 years:
  The recommended therapeutic dose is 2 inhalations (50 mcg each) in the nostril two times a day (total daily dose is 400 mcg).
  In the case, if the reduction of 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 in each nostril 2 times a day (total daily dose -800 mcg). After reducing the symptoms of the disease, a dose reduction is recommended.

  Nose polyposis treatment
  Adults (including the elderly) from 18 years:
  The recommended therapeutic dose is 2 inhalations (50 mcgch each) in each nostril 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 inhalations (50 mcg each) in each nostril 1 time per day (total daily dose - 200 mcg).

  Side effect
  In adults and adolescents: headache, nasal bleeding (i.e. obvious bleeding, as well as the discharge of blood-stained mucus or blood clots), pharyngitis, burning sensation in the nose, irritation of the nasal mucosa, ulceration of the nasal mucosa. Nosebleeds, as a rule, were moderate and stopped on their own, the frequency of their occurrence was slightly higher than when using placebo (5%), but equal to or less than when other nasal GCSs were used as active controls (some of their incidence of nosebleeds (left up to 15%).The incidence of all other adverse events was comparable to the frequency of their occurrence when placebo was prescribed.
  In children: nasal bleeding, headache, sensation of irritation in the nose, sneezing. The incidence of these adverse events in children was comparable to the frequency of their occurrence with placebo.
  Rarely observed hypersensitivity reactions of the immediate type ([eg, bronchospasm, shortness of breath).
  Very rarely, anaphylaxis, angioedema, taste and smell disturbances. Also very rarely with intranasal application of GCS were cases of perforation of the nasal septum and an increase in intraocular pressure.

  Overdose
  With prolonged use of GCS in high doses, as well as with the simultaneous use of several GCS, it is possible to suppress the function of the hypothalamic-pituitary-adrenal system. Due to the low systemic bioavailability of the drug (<0.1%), it is unlikely that in case of an accidental or deliberate overdose, it will be necessary to take any measures other than observation with possible subsequent resumption of the drug at the recommended dose.

  Interaction with other drugs
  Combination therapy with loratadine was well tolerated by patients. However, no effect of the drug on the plasma concentration of loratadine or its main metabolite was noted.

  special instructions
  As with any long-term treatment, patientsnasal spray nazonex® for several months and longer, should be periodically examined by a doctor for possible changes in the nasal mucosa.
  In case of a local nasal or pharynx fungal infection, it may be necessary to discontinue the nasal spray therapy. NAZONEKS® and conducting special treatment. Persistent irritation of the mucous membranes of the nose and pharynx can also serve as a basis for stopping the treatment with a nasal spray. NAZONEKS®.
  When conducting placebo-controlled clinical trials in children, when NAZONEKS nasal spray was used in a daily dose of 100 μg for a year, growth was not observed in children.
  With long-term treatment with nasal spray NAZONEKS® signs of suppression of the hypothalamic-pituitary-adrenal system was not observed.
  Patients who are moving on to nasal spray treatment NAZONEKS® after long-term therapy with glucocorticosteroids of systemic action, they require special attention. Cancellation of glucocorticosteroids of a systemic effect in such patients may lead to insufficiency of the adrenal function, the subsequent recovery of which may take up to several months. In case of signs of adrenal insufficiency, you should resume taking systemic corticosteroids and take other necessary measures.During the transition from treatment with glucocorticosteroids of systemic action to treatment with a nasal spray, NAZONEKS® some patients may experience initial withdrawal symptoms of systemic glucocorticosteroids (for example, pain in the joints and / or muscles, fatigue and depression), despite a reduction in the severity of symptoms associated with lesions of the nasal mucosa; such patients need to be specifically convinced of the feasibility of continuing treatment with a nasal spray. NAZONEKS®. The transition from systemic to local glucocorticosteroids can also reveal pre-existing, but masked therapy with glucocorticosteroids of systemic action, allergic diseases such as allergic conjunctivitis and eczema.
  Patients who are treated with glucocorticosteroids have potentially reduced immune reactivity and should be warned about the increased risk of infection in case of contact with patients with certain infectious diseases (eg, chicken pox, measles), and the need for medical advice, if such contact occurs. 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 area), immediate medical consultation is required.
  When applying the nasal spray NAZONEKS® for 12 months there were no signs of atrophy of the nasal mucosa; in addition, mometasone furoate showed a tendency to contribute to the normalization of the histological pattern in the study of nasal mucosa biopsy specimens.

  Release form
  Spray nasal dosage 50 mcg / dose.
  On 18 g (120 doses) suspensions in the polyethylene bottles of white color supplied with the dosing device and closed with a cap. On 1 bottle together with the application instruction in a cardboard pack.

  Storage conditions
  In the reach of children; at a temperature of from 2 to 25 ° C.
  Do not freeze.