Pharmacological properties Nasonex Nasal Spray:
mometasone furoate – a synthetic corticosteroids for topical use with a pronounced anti-inflammatory action. Local anti-inflammatory effect mometasone furoate has at doses at which there is no use of systemic GCS effects. The mechanism of anti-inflammatory and antiallergic actions mometasone furoate is mainly due to its ability to inhibit the release of mediators of allergic reactions. Mometasone furoate significantly reduces the release of leukotrienes from leukocytes of patients with allergic diseases. Mometasone furoate demonstrated in cell culture the high potential (at least 10-fold higher activity than other steroids including beclomethasone dipropionate, betamethasone, hydrocortisone and dexamethasone) inhibition of synthesis and release of interleukins IL-1, IL-6 and tumor necrosis factor ( TNF-α); he also greatly inhibits the formation of Th2-cytokines, IL-4 and IL-5 CD4 + T cells. Mometasone furoate also at least 6 times more potent to inhibit production of IL-5 than beclomethasone dipropionate and betamethasone. In studies with provocative tests with the application of the antigens on the mucosa of the nasal cavity A high anti-inflammatory activity of water as a nasal spray Nasonex in early and late stage allergic reaction. This was confirmed by reduction (compared with placebo) levels of histamine and activity of eosinophilic granulocytes, as well as a decrease (compared with baseline) the number of eosinophilic and neutrophilic granulocytes and the adhesion proteins of epithelial cells.
Pronounced clinical effect in the first 12 hours after using the nasal spray water Nasonex was observed in 28% of patients with seasonal allergic rhinitis. In 50% of patients improved on average occurred during 35.9 hours
In clinical trials in patients with nasal polyps Nasonex significantly more effective than placebo with respect to nasal congestion, size of polyps, restoration of smell.
Mometasone furoate when administered as an aqueous nasal spray has a low bioavailability (≤ 0,1%), it is almost not detectable in the blood plasma, even when using the method of determining a threshold sensitivity of 50 pg / ml. In this regard, appropriate pharmacokinetic data for this dosage form is not. A small number of mometasone furoate suspension, which can get into the gastrointestinal tract after intranasal administration, prior to excretion in the urine or bile being active primary metabolism.
INDICATIONS Nasonex Nasal Spray:
seasonal or perennial allergic rhinitis in adults and children 2 years of age and older, as well as for use as an auxiliary therapeutic agent in antibiotic therapy of acute episodes of sinusitis in adults (including elderly patients) and in children under the age of 12 and older treated nasal polyps in patients aged 18 years or older, and associated symptoms (including nasal congestion and anosmia).
Application Nasonex Nasal Spray:
before the first use of a nasal spray to hold it Nasonex “calibrated” by 7.6 taps dispensing unit. After the “calibration” set stereotype of drug delivery, in which each press sprayed approximately 50 mcg mometasone furoate chemically pure (1 dose). If the nasal spray was not used for 14 days or longer to re-”calibration”. Before each use, you must shake the bottle.
With seasonal or perennial allergic rhinitis for adults (including elderly) and adolescents aged 12 years and older the recommended preventive and therapeutic dose is two injections (50 mg each) in each nostril once a day (total daily dose – 200 micrograms). After reaching the therapeutic effect of maintenance therapy appropriate dose reduction to 1 injection into each nostril once a day (total daily dose – 100 micrograms). If the use of the drug at the recommended therapeutic dose is not enough effective daily dose can be increased up to 4 injections in each nostril once a day (total daily dose – 400 micrograms). After reducing the severity of symptoms is recommended to reduce the dose. Onset of action of the drug indicated for 12 hours after the first application. For children aged 2-11 years the recommended therapeutic dose is 1 injection (50 mg) in each nostril once a day (total daily dose – 100 micrograms). Patients with seasonal allergic rhinitis is recommended to start prophylactic treatment with nasal spray Nasonex for 2-4 weeks before the season of flowering plants, the alleged allergen.
As adjunctive therapy for acute episodes of sinusitis in adults (including elderly) and children 12 years prescribed in the recommended therapeutic dose – 2 injection (50 mg) in each nostril 2 times a day (total daily dose – 400 micrograms). If reducing the severity of symptoms using the drug at the recommended therapeutic dose can not be reached, the daily dose may be increased up to 4 injections in each nostril 2 times a day (total daily dose – 800 micrograms). After reducing the severity of symptoms is recommended to reduce the dose.
When nasal polyps in patients aged 18 years and older (including the elderly), the recommended dose is two injections of 50 micrograms in each nostril 2 times a day (total daily dose – 400 micrograms). After achieving clinical response is recommended to reduce the dose to 2 injections in each nostril one time a day (total daily dose – 200 micrograms).
CONTRAINDICATIONS Nasonex Nasal Spray:
Hypersensitivity to the active substance or to other ingredients.
SIDE EFFECTS Nasonex Nasal Spray:
In clinical trials of the drug for seasonal and perennial allergic rhinitis, there were side effects such as headache (8%), bloody mucus from the nose (to 8%), pharyngitis (4%), burning sensation in the nose (2%), irritation (2%) and ulcerative changes (1%) of nasal mucosa. The emergence of such side effects typical of the application of any nasal spray containing corticosteroids. Bloody mucus were not abundant and stopped independently, appeared at a frequency slightly higher than with placebo (5%) but lower than in the appointment of other SCS for intranasal use (some of them the incidence of nasal bleeding up to 15%) . The incidence of all other adverse events was comparable to the frequency of their occurrence in the appointment of a placebo. In children, the incidence of side effects, including nasal bleeding (6%), headache (3%), feelings of irritation in the nose (2%) and sneezing (2%) was comparable with the frequency of their occurrence in the placebo group. It was reported a few cases of violations of taste and smell.
After mometasone furoate nasal administration may rarely occur an allergic reaction of immediate type. Very rarely anaphylaxis and angioedema. When using the nasal spray Nasonex as an aid in the treatment of acute exacerbations of sinusitis were the following side effects, the frequency of occurrence of which was comparable to that in the placebo group: headache (2%), pharyngitis (1%), burning sensation in the nose (1%) and irritation of the nasal cavity (1%). Nasal bleeding was moderate and the frequency of their occurrence in the application of spray Nasonex was also comparable to the frequency of nasal bleeding in the placebo group (5 and 4% respectively).
SPECIAL INSTRUCTIONS Nasonex Nasal Spray:
Nasonex can not be applied in the presence of local infection with involvement in the process of nasal mucosa. Due to the fact that corticosteroids slow the healing of wounds, the drug should not be prescribed for patients who have recently had surgery or trauma of the nose to complete wound healing.
After intranasal drug use to the maximum therapeutic dose of mometasone is not detected in plasma even in minimal concentrations. Consequently, we can expect that the effect of the drug on the fetus will be negligible, and the potential toxicity relative to the reproductive function – very low. However, like other corticosteroids for nasal application, Nasonex should be administered during pregnancy or breast-feeding only if the expected benefits of its use justifies the potential risk to the mother, fetus or infant. Children whose mothers during pregnancy were receiving corticosteroids, should be examined for possible hypoadrenalism.
Nasonex be used with caution or not at all prescribe to patients with active or latent TB infection, as well as in untreated fungal, bacterial, systemic viral infections, ophthalmic infections caused by herpes simplex virus.
After 12 months of treatment did not arise Nasonex atrophy of nasal mucosa, in addition, mometasone furoate in the application of a trend to normalization of histology in the study of biopsies of nasal mucosa. Nevertheless, patients who use Nasonex for several months or longer must undergo periodic inspections to identify possible changes in the nasal mucosa. In the case of a local fungal infection of the nose or throat may require cessation of therapy Nasonex and the special treatment. Irritation of the nasal cavity and pharynx, which persists for a long time, can also be an indication for discontinuation of treatment Nasonex .
In long-term treatment Nasonex signs of depression of the hypothalamic-pituitary-adrenal axis were observed. Patients who go on treatment Nasonex after prolonged systemic treatment with corticosteroids, should be under medical supervision. Cancel systemic corticosteroids in these patients may lead to insufficiency of the adrenal cortex, which may require appropriate action. The transition from treating systemic corticosteroids to treat some patients Nasonex may experience symptoms of withdrawal of GCS (arthralgia, myalgia, fatigue and depression). Change of therapy can also detect allergic diseases, which were previously masked by corticosteroids systemic therapy (allergic conjunctivitis, eczema, etc.) Patients who receive treatment GCS, with potentially reduced immunological reactivity and should be warned about the increased risk of infection in case of contact with sick some infectious diseases (eg chickenpox, measles). Extremely rare in intranasal application of GCS have been cases of perforation of nasal septum, or increased intraocular pressure. When a placebo-controlled clinical studies have noted growth retardation in children, which Nasonex administered a daily dose of 100 mg during the year.
INTERACTION Nasonex Nasal Spray:
not indicated any interaction with concomitant administration of nasal spray Nasonex with loratadine. Data on the interaction with other drugs no.
