Instruction for use: Nazarel

Active substance Fluticasone

ATX code R01AD08 Fluticasone

Pharmacological group

Glucocorticosteroids

Nosological classification (ICD-10)

J30.1 Allergic rhinitis caused by the pollen

hay fever, Hypersensitivity to pollen, Polypoid allergic rhinosinusitis, Seasonal hay fever, rhinitis

J30.2 Other seasonal allergic rhinitis

Allergic rhinitis seasonal, Seasonal rhinitis of an allergic nature

J30.3 Other allergic rhinitis

Allergic rhinitis all year round, Allergic rhinoconjunctivitis

J30.4 Allergic rhinitis, unspecified

Rninitis chronicles vasumotor neurovegetative

Composition

Spray nasal dosed 1 dose

active substance:

Fluticasone propionate 50 μg

Auxiliary substances: polysorbate 80 - 0,005 mg; MCC + carmellose sodium (dispersive cellulose) - 1.55 mg; Dextrose - 5 mg; Benzalkonium chloride (50% solution) - 0.04 mg; Phenylethanol 0.25 mg; Water - enough

Description of dosage form

Spray: white or almost white opaque, homogeneous suspension.

pharmachologic effect

Pharmacological action - antiallergic, anti-inflammatory local, decongestant local.

Pharmacodynamics

GCS (glucocorticosteroids) for topical application. In recommended doses, it has a pronounced anti-inflammatory, anti-edematous and anti-allergic effect. The anti-inflammatory effect is realized as a result of interaction of the drug with the GCS receptors. Suppresses the proliferation of mast cells, eosinophils, lymphocytes, macrophages, neutrophils, reduces the production and release of mediators of inflammation and other biologically active substances (including histamine, PG (prostaglandins), LT (leukotrienes), cytokines) during the early and late phase Allergic reaction. Antiallergic effect manifests itself in 2-4 hours after the first application. It reduces itching in the nose, sneezing, runny nose, stuffy nose, discomfort in the sinuses and a feeling of pressure around the nose and eyes. It alleviates eye symptoms associated with allergic rhinitis. The effect of the drug is maintained for 24 hours after a single application. When used in therapeutic doses, fluticasone has no systemic effect and has virtually no effect on the hypothalamic-pituitary-adrenal system.

Pharmacokinetics

Absorption

After intranasal administration of fluticasone (200 μg / day) Cmax in blood plasma in most patients below the detection level (<0.01 ng / ml). Direct absorption from the mucous membrane of the nasal cavity is extremely small due to the low solubility of the drug in water, as a result, most of the dose is swallowed. From the gastrointestinal tract, less than 1% of the dose enters the bloodstream due to low absorption and presystemic metabolism. These reasons cause an extremely low total absorption of the drug from the nasal mucosa and gastrointestinal tract.

Distribution

Fluticasone in a stable state has a significant Vd (volume of distribution) - about 318 liters. Binding to plasma proteins is 91%.

Metabolism

Has the effect of first passage through the liver. Metabolised in the liver with the participation of the CYP3A4 isoenzyme (cytochrome P450 isoenzyme) of the cytochrome P450 system to form an inactive carboxyl metabolite.

Excretion

T1 / 2 is 3 hours. It is excreted mainly through the intestine. The renal clearance of fluticasone is less than 0.2%, the renal clearance of a metabolite containing a carboxyl group is less than 5%.

Indications

Prevention and treatment of seasonal and year-round allergic rhinitis.

Contraindications

Hypersensitivity to fluticasone and other components of the drug;

Children under 4 years.

With caution: with concomitant simple herpes, as well as bacterial infections of the upper respiratory tract. In such cases, antibiotics and / or antiviral agents should be additionally prescribed; After surgery in the nasal cavity or injury to the nose, as well as in the presence of ulcerative lesions of the nasal mucosa; Concomitantly with other corticosteroid dosage forms, including tablets, creams, ointments, asthma medications, similar nasal or ophthalmic sprays and nasal drops.

pregnancy and lactation

It is not recommended to prescribe during pregnancy. If necessary, the expected benefit of therapy for the mother and the potential risk to the fetus should be considered.

Penetration of fluticasone into breast milk is unlikely. Nevertheless, it is recommended to stop breastfeeding while the drug is being used.

Side effects

The incidence of adverse events is classified according to WHO recommendations: very often - not less than 10%; Often - not less than 1%, but less than 10%; Infrequently - not less than 0,1%, but less than 1%; Rarely - not less than 0.01%, but less than 0.1%; Very rarely (including isolated cases) - less than 0.01%.

On the part of the immune system: rarely - bronchospasm, anaphylactic reaction; Very rarely - the reaction of skin hypersensitivity, angioedema.

From the central nervous system (central nervous system): often - headache, a violation of taste, a violation of the sense of smell.

From the side of the organ of vision: very rarely - an increase in IOP, glaucoma, cataract.

From the respiratory system, chest and mediastinum: very often - nosebleeds; Often - dryness and irritation of the mucous membrane of the nasopharynx; Very rarely - perforation of the nasal septum.

From the skin and subcutaneous tissues: very rarely - ulceration of the subcutaneous-mucous layer.

Other: very rarely - stunted growth in children, decreased function of the adrenal cortex, osteoporosis.

Interaction

Interaction with other drugs (drug) is unlikely, since in the intranasal route of administration, the concentrations of fluticasone in the plasma are very low. When used simultaneously with strong inhibitors of the CYP3A4 isoenzyme of the cytochrome P450 system (ritonavir), the systemic effect of fluticasone and the development of side effects (Cushing's syndrome, suppression of adrenal cortex function) are possible. With simultaneous use with other inhibitors of the cytochrome P450 system (erythromycin, ketoconazole), a slight increase in the concentration in the blood of fluticasone is observed, which practically does not affect the cortisol content.

Dosing and Administration

Intranasally.

Adults and children 12 years and older: 2 doses (100 mcg) per each nasal passage 1 time per day, preferably in the morning. In some cases it is necessary to administer 2 doses in each nasal passage 2 times a day (the maximum daily dose is 400 mcg). After achieving the therapeutic effect, a maintenance dose of 50 μg / day can be administered to each nasal passage (100 μg). The maximum daily dose should not exceed 400 mcg (4 doses per each nasal passage).

Older patients do not need a dose adjustment.

Children aged 4 to 12 years: one dose (50 mcg) 1 time per day in each nasal passage, preferably in the morning. The maximum daily dose should not exceed 200 mcg in each nasal passage. It is necessary to apply the minimum dosage, which ensures effective elimination of symptoms. To achieve full therapeutic effect, the drug should be used regularly.

Instructions for use

The bottle with a nasal spray is equipped with a protective cap, which protects the tip from getting dust and pollution.

At the first application it is necessary to prepare a bottle: to press on a batcher 6 times. The spraying mechanism is unlocked. If the drug has not been used for more than 1 week, you should again prepare the bottle and unlock the spraying mechanism.

Further it is necessary:

- clean the nose;

- close one nasal passage and insert the tip into the other nasal passage;

- tilt the head slightly forward, continuing to hold the aerosol bottle vertically;

- start breathing in through your nose and, continuing to inhale, make a single tap with your fingers to spray;

Exhale through the mouth.

Then, in the same way, inject the drug into the other nasal passage.

After use, the tip should be soaked with a clean cloth or a handkerchief and cover it with a cap. The sprayer should be washed at least once a week. To do this, remove the tip, rinse it in warm water, dry it and then gently place it in the top of the bottle. Put the protective cap on. If the tip of the tip is clogged, the tip should be removed and left for a while in warm water. Then rinse under the stream, dry and re-put on the bottle. Do not clean the hole with a pin or other sharp objects.

After opening the package, the drug can be used until the expiration date.

Overdose

Symptoms of acute and chronic overdose are not documented. With intranasal administration of 2 mg of fluticasone to volunteers 2 times a day for 7 days, no effect was found on the hypothalamic-pituitary-adrenal system.

special instructions

Simultaneous use with inhibitors of the isoenzyme CYP3A4 (ritonavir, ketoconazole) requires careful monitoring of the patients' condition, as these drugs can cause an increase in the concentration of fluticasone in the plasma (see "Interaction").

When prescribing nasal SCS at high doses for a long period of time, the risk of systemic effects of GCS increases. With prolonged use of the drug Nazarel, regular monitoring of the function of the adrenal cortex is necessary. Since nasal SCS, even when used in approved doses can cause a slowdown in the growth of children with prolonged therapy, it is necessary to regularly monitor the growth of the child and timely adjust the dose of the drug Nazarel. In the treatment of seasonal allergic rhinitis, the drug Nazarel is quite effective, but with an increased concentration of allergens in summer, additional treatment may be required. When Nazarel is prescribed for patients with tuberculosis, infectious process, herpetic keratitis, and also recently undergone operative intervention in the oral cavity and nose, the ratio of possible risk and expected benefit should be carefully estimated.

Form of issue

Spray nasal dosed, 50 mcg / dose. In bottles of dark glass (type 1) with a dispensing device and protective cap, 60, 120 or 150 doses. In a pack of cardboard 1 fl.

Conditions of leave from pharmacies

On prescription.

storage Conditions

At a temperature not higher than 25 ° C.

Keep out of the reach of children.

Shelf life

3 years.

Do not use after the expiry date printed on the package.