Flixonase for allergic rhinitis, nasal spray 50 µg/dose, 60 doses

Composition

1 dose:

fluticasone propionate (micronized) 50 mcg

Auxiliary substances:

dextrose-5 mg,

avicel RC591 (microcrystalline cellulose, sodium carmellose) – 1.5 mg,

phenylethanol-0.25 mg,

benzalkonium chloride-0.02 mg,

polysorbate 80-0.005 mg,

hydrochloric acid – up to pH 6.3-6.5,

purified water – up to 100 mg

Pharmacological action

CORTICOSTEROIDS for intranasal use. It has a pronounced anti-inflammatory effect. When administered intranasally, there is no systemic effect, practically does not depress the hypothalamic-pituitary-adrenal system. There was no significant change in the daily AUC of serum cortisol after use of fluticasone propionate at a dose of 200 mcg / day compared to placebo (ratio: 1.01,90% CI-confidence interval from 0.9 to 1.14). The anti-inflammatory effect of fluticasone propionate is realized as a result of its interaction with glucocorticoid receptors. Inhibits the proliferation of mast cells, eosinophils, lymphocytes, macrophages, and neutrophils. Fluticasone propionate reduces the production of inflammatory mediators and a number of biologically active substances (including histamine, prostaglandins, leukotrienes, cytokines) during the early and late phases of an allergic reaction. It has a rapid anti-inflammatory effect on the nasal mucosa. The anti-allergic effect manifests itself within 2-4 hours after the first application. Reduces sneezing, itchy nose, rhinorrhea, nasal congestion, sinus discomfort, and pressure around the nose and eyes. It also relieves eye symptoms associated with allergic rhinitis. A reduction in the severity of symptoms (especially nasal congestion) persists for 24 hours after a single application of the spray at a dose of 200 mcg. Fluticasone propionate improves the quality of life of patients, including physical and social activity.

Clinical pharmacology

Absorption After intranasal use of fluticasone propionate (200 mcg/day), Cmax in blood plasma at steady state is not quantified in most patients (less than 0.01 ng/ml). Cmax in plasma is 0.017 ng / ml. Direct absorption from the nasal mucosa is unlikely due to the low solubility of the drug in water and the ingestion of most of the drug. When taken orally, absolute bioavailability is low (less than 1%) as a result of a combination of incomplete absorption from the gastrointestinal tract and active metabolism during the “first pass” through the liver. The total system suction is thus extremely low. Distribution at steady state, fluticasone propionate has a large Vd of about 318 liters. Binding to plasma proteins is high – about 91%. Metabolism Fluticasone propionate is rapidly eliminated from the systemic circulation mainly due to metabolism in the liver with the formation of inactive carboxylic acid by the CYP3A4 isoenzyme. Metabolism of the ingested fraction of fluticasone propionate during the” first pass” through the liver occurs in the same way. Elimination The elimination of fluticasone propionate is linear in the dose range from 250 to 1000 micrograms and is characterized by a high plasma clearance (1.1 l / min). Plasma Cmax decreases by approximately 98% over 3-4 hours, and only at very low plasma concentrations was a final T1/2 of 7.8 h observed. The renal clearance of fluticasone propionate is insignificant (less than 0.2%), and the inactive metabolite – carboxylic acid – less than 5%. Fluticasone propionate and its metabolites are mainly excreted in the bile through the intestines.

Indications

Treatment of year-round and seasonal allergic rhinitis, including hay fever (hay fever) in adults and children from 4 years of age: pain, pressure in the paranasal sinuses; nasal congestion, sneezing, itching in the nose; lacrimation.

Use during pregnancy and lactation

Before using Flixonase® during pregnancy and lactation, you should consult your doctor. Pregnant and lactating women should only be prescribed Flixonase if the expected benefit to the patient exceeds any possible risk to the fetus or child.

Contraindications

Hypersensitivity to fluticasone propionate and other components of the drug; children under 4 years of age; recently suffered a nasal injury or surgery and the nasal cavity. Before using the drug, the patient should consult a doctor in the following cases: taking medications for the treatment of HIV infection, such as ritonavir; taking CORTICOSTEROIDS for the treatment of bronchial asthma, allergies, skin rashes; taking medications for the treatment of fungal infections, such as ketoconazole; taking other powerful inhibitors of the CYP3A isoenzyme, such as itraconazole; in the presence of glaucoma or cataracts. Use with caution if you have an infection of the nasal cavity or paranasal sinuses. It should be borne in mind that infectious diseases of the nose require appropriate treatment, but they are not a contraindication to the use of Flixonase nasal spray.

Side effects

Determining the frequency of side effects: very common (≥1/10), common (≥1/100 and <1/10), uncommon (≥1/1000 and <1/100), rare (≥1/10 000 and <1/1000), very rare (Very frequent, frequent and infrequent adverse reactions are mainly established on the basis of data from clinical studies. Reactions that occur rarely and very rarely are mostly determined from spontaneous messages. Background parameters in the placebo group were not taken into account when determining the frequency of adverse reactions, since they were generally comparable with the active treatment group. From the immune system: very rarely – hypersensitivity reactions, including bronchospasm, rash, swelling of the face and tongue, anaphylactic reactions, anaphylactoid reactions. From the nervous system: often-headache, unpleasant taste and smell. Headaches, unpleasant tastes, and odors have also been reported with other nasal sprays. From the side of the organ of vision: very rarely-glaucoma, increased intraocular pressure, cataracts. A small number of spontaneous reports were associated with long-term drug therapy. From the respiratory system: very often – nosebleeds; often-dryness of the mucous membrane in the nasal and pharyngeal cavity, irritation of the mucous membrane in the nasal and pharyngeal cavity (these adverse reactions, as well as nosebleeds, were observed with the use of other intranasal drugs); very rarely – perforation of the nasal septum (reported when taking intranasal corticosteroids). When using some intranasal corticosteroids, systemic effects may develop, especially when administered in high doses for a long time.

Interaction

When fluticasone propionate is co-administered with ritonavir, which is a strong inhibitor of the CYP3A4 isoenzyme, it is possible to significantly increase the concentration of fluticasone propionate in blood plasma. As a result, there is a sharp decrease in the concentration of cortisol in the serum. The use of fluticasone propionate inhaled or intranasally and ritonavir leads to the development of side effects due to the systemic action of corticosteroids, including Cushing’s syndrome and suppression of the adrenal cortex. Therefore, the concomitant use of fluticasone propionate and ritonavir should be avoided unless the potential benefit outweighs the risk of systemic effects. Concomitant use of fluticasone propionate with other less potent CYP3A4 inhibitors, such as ketoconazole and itraconazole, leads to increased exposure to fluticasone propionate and an increased risk of systemic side effects. It is recommended to exercise caution and, if possible, avoid long-term joint use of these drugs. Inhibitors of the CYP3A4 isoenzyme cause a negligible (erythromycin) or insignificant (ketoconazole) increase in plasma concentrations of fluticasone propionate, which do not entail any noticeable decrease in serum cortisol concentrations. However, caution should be exercised when concomitantly using inhibitors of the CYP3A4 isoenzyme (for example, ketoconazole) and fluticasone propionate due to the possible increase in the plasma concentration of the latter.

How to take, course of use and dosage

of Flixonase® is intended for intranasal use only. To achieve a full therapeutic effect, the drug should be used regularly. The maximum therapeutic effect is manifested after 3-4 days of therapy. Adults and children over 12 years of age%^%Week 1: 2 injections in each nostril 1 time/day (200 mcg/day); from week 2 to 3 months: 1 or 2 injections in each nostril 1 time/day (100-200 mcg/day). The maximum daily dose is 200 mcg/day (no more than 2 injections in each nostril). Elderly patients are prescribed at the usual dose intended for adults. Children aged 4-12 years should be given 1 injection in each nostril 1 time/day (100 mcg / day). Do not exceed the recommended dose (100 mcg/day). In children aged 4 to 12 years, the drug should be used for the shortest possible period of time necessary to achieve control of the symptoms of the disease. You should consult your doctor if your child needs to use the drug for a period of time exceeding 2 months per year. The maximum daily dose is 100 mcg (no more than 1 injection in each nostril). If there is no effect from the use of the drug in all age groups of patients, it is necessary to consult a doctor.Rules for using the drug Before use, you should carefully shake the bottle, take it, placing your index and middle fingers on either side of the tip, and your thumb under the bottom. When using the drug for the first time or after a break in its use for more than 1 week, you should check the functionality of the nebulizer: direct the tip away from you, make several taps until a small cloud appears from the tip. Next, you need to clean your nose (blow your nose). Close one nostril and insert the tip into the other nostril. Tilt your head slightly forward while still holding the bottle vertically. Then you should start inhaling through your nose and, while continuing to inhale, make a single pressure with your fingers to spray the drug. Exhale through your mouth. Repeat the procedure for a second spray into the same nostril, if necessary. Then repeat the procedure completely by inserting the tip into the other nostril. After use, blot the tip with a clean cloth or handkerchief and cover it with a cap. The sprayer should be rinsed at least once a week. To do this, carefully remove the tip and rinse it in warm water. Shake off excess water and leave to dry in a warm place. Avoid overheating. Then carefully replace the tip in its original position at the top of the bottle. Put on a protective cap. If the tip opening is clogged, remove the tip using the method described above and leave it in warm water for a while. Then rinse under cold water, dry and put back on the bottle. Do not clean the tip hole with a pin or other sharp objects.

Overdose

Data on acute and chronic overdose of the drug are not available. Intranasal use of 2 mg fluticasone propionate twice daily for 7 days to healthy volunteers did not affect the function of the hypothalamic-pituitary-adrenal system (doses 20 times higher than therapeutic). The use of the drug in doses higher than recommended for a long time can lead to temporary suppression of adrenal function. In case of overdose, the patient should consult a doctor.

Description

Nasal spray dosed in the form of an opaque suspension of white color, free of foreign particles.

Special instructions

The drug is indicated only for intranasal use. For adults and children over 12 years of age: do not use Flixonase nasal spray for more than 3 months. If you need to use the drug for more than 3 months, you should consult a doctor. For children from 4 to 12 years of age: do not use Flixonase nasal spray for more than 2 months. If you need to use the drug for more than 2 months, you should consult a doctor. With prolonged use, regular monitoring of the function of the adrenal cortex is necessary. There are reports of systemic effects when using nasal corticosteroids, especially in high doses for a long time. These effects are much less likely than when taken orally. Systemic effects of nasal corticosteroids may occur, in particular, when they are used in high doses for a long time. These effects are much less likely to occur than with oral corticosteroids, and they may vary between individual patients and between different corticosteroid medications. Possible systemic effects may include Itsenko-Cushing syndrome, characteristic features of cushing’s disease, adrenal suppression, growth retardation in children and adolescents, cataracts, glaucoma, and more rarely a number of psychological or behavioral effects, including psychomotor hyperactivity, sleep disorders, anxiety, depression, or aggressiveness (especially in children). Growth retardation was observed in children treated with certain intranasal corticosteroids at the permitted doses. It is recommended to regularly monitor the growth of children receiving long-term treatment with intranasal corticosteroids. If growth slows down, you should review treatment to reduce the dose of intranasal corticosteroids, if possible, to the minimum dose that ensures effective control of symptoms, and consult a pediatrician. Concomitant use of ritonavir and fluticasone propionate should be avoided unless the potential benefit to the patient outweighs the potential risk of systemic corticosteroid side effects. It is recommended to stop taking the drug and consult your doctor if there is no improvement within 4 days. Consultation with a doctor is also necessary if the patient has new symptoms, such as severe facial pain, thick nasal discharge, which may indicate infection and are not related to allergies. Infections of the nasal cavity or paranasal sinuses require appropriate treatment, but are not a contraindication to the use of Flixonase nasal spray. In most patients, fluticasone propionate nasal spray eliminates the symptoms of seasonal allergic rhinitis, but in some cases, with very high concentrations of allergens in the air, additional therapy may be necessary. Additional therapy may be required to relieve eye symptoms during successful treatment of seasonal allergic rhinitis. To achieve the maximum therapeutic effect, it is necessary to adhere to a regular application schedule. Caution should be exercised when transferring patients from systemic corticosteroid therapy to fluticasone propionate b formenasal spray, especially if there is a violation of adrenal function against the background of regular monitoring. Flixonase ® nasal water spray contains benzalkonium chloride, which can cause bronchospasm. In case of contact with patients with chickenpox, measles and changes in vision, it is recommended to stop treatment and consult a doctor. Effects on the ability to drive vehicles and mechanicsin clinical studies, no data have been obtained on the effect of the drug on the ability to drive vehicles and other mechanisms, but it is necessary to take into account the side effects that the drug can cause.

Product form

60 doses-yellow glass vials (1) with dosing device, adapter and protective cap-plastic cases with booklet label.

Storage conditions

The drug should be stored out of the reach of children at a temperature not exceeding 30°C.

Shelf life

3 years

Active ingredient

of Fluticasone furoate

Dosage Form

Spray nasal