FLIXONASE ​​NASAL SPRAY 50MKG

Fliksonase® / Flixonase®.

International non-proprietary name:

fluticasone / fluticasone.

Dosage Form:

spray nasal dosed.

COMPOSITION on 1 dose:

DESCRIPTION

White, opaque suspension, free from foreign particles.

PHARMACOTHERAPE TREATMENT GROUP

Glucocorticosteroid for topical use.

PHARMACOLOGICAL PROPERTIES

Mechanism of action

Fluticasone Propionate - A substance with a strong anti-inflammatory effect. With intranasal administration, there is no marked systemic effect or suppression of the hypothalamic-pituitary-adrenal system. No significant change in the daily area under the pharmacokinetic curve of serum cortisol was detected after administration of fluticasone propionate at a dose of 200 μg / day compared with placebo (ratio: 1.01, 90% CI - confidence interval from 0.9 to 1.14).
Fluticasone propionate has an anti-inflammatory effect due to interaction with glucocorticosteroid receptors. Suppresses the proliferation of mast cells, eosinophils, lymphocytes, macrophages, neutrophils; reduces the production of inflammatory mediators and other biologically active substances (histamine, prostaglandins, leukotrienes, cytokines) during the early and late phases of an allergic reaction. Fluticasone propionate has a fast anti-inflammatory effect on the nasal mucosa, and its anti-allergic effect is already manifested 2-4 hours after the first use. Reduces sneezing, itching in the nose, runny nose, nasal congestion, discomfort in the region of the paranasal sinuses and the sensation of pressure around the nose and eyes. In addition, it relieves the eye symptoms associated with allergic rhinitis. Reducing the severity of symptoms (especially nasal congestion) persists for 24 hours after a single spray in a dose of 200 mg.
Fluticasone propionate improves the quality of life of patients, including physical and social activity.

Suction

After intranasal administration of fluticasone propionate at a dose of 200 µg / day, maximum equilibrium plasma concentrations are not quantitatively determined in most patients (less than 0.01 ng / ml). The highest plasma concentration was recorded at a level of 0.017 ng / ml.
Direct absorption from the nasal cavity is unlikely due to the low water solubility and swallowing of the majority of the drug. Absolute oral 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 passage through the liver. Overall systemic absorption is thus extremely low.

Distribution

Fluticasone propionate has a large volume of distribution in the equilibrium state (approximately 318 liters). Communication with plasma proteins is high (91%).

Metabolism

Fluticasone propionate is rapidly excreted from the systemic blood flow mainly due to metabolism in the liver with the formation of inactive carboxylic acid by means of the cytochrome P450 system CYP3A4 isoenzyme. The metabolism of the swallowed fraction of fluticasone propionate during the first passage through the liver occurs in the same way.

Removal

The removal of fluticasone propionate is linear in the dose range from 250 to 1000 μg and is characterized by a high plasma clearance (1.1 l / min). The maximum plasma concentration decreases by approximately 98% within 3-4 hours, and only at very low plasma concentrations a final half-life of 7.8 h was 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 FOR USE

Treatment of year-round and seasonal allergic rhinitis, including pollinosis (hay fever) in adults and children from 4 years old (elimination of symptoms such as pain and pressure sensation in the area of ​​the paranasal sinuses, nasal congestion, runny nose, sneezing, itchy nose, watery eyes).

CONTRAINDICATIONS FOR USE

• - Hypersensitivity to fluticasone propionate or any other component of the drug.
• - Children's age up to 4 years.
• - A recent nose injury or surgery in the nasal cavity.

CAREFULLY

Before using the drug should consult a doctor if you are taking:

• - drugs for treating HIV infection, such as ritonavir;
• - glucocorticosteroids for the treatment of bronchial asthma, allergies, skin rashes;
• - drugs for the treatment of fungal infections, such as Ketoconazole;
• - other potent inhibitors of the CYP3A isoenzyme, for example, itraconazole.

Also, consult with your doctor if you have glaucoma or cataracts.
Take with caution if you have infections of the nasal cavity or paranasal sinuses. It should be borne in mind that infectious diseases of the nose require appropriate treatment, but are not a contraindication to the use of the nasal spray Fliksonase ®.

USE IN PREGNANCY AND DURING BREASTFEEDING

Before using Fliksonaze® during pregnancy and lactation, you should consult with your doctor.Fliksonaze ​​® can be prescribed to pregnant and lactating women only when the expected benefit to the patient exceeds any possible risk to the fetus or child.

METHOD OF ADMINISTRATION AND DOSES

Only intranasally.
To achieve the full therapeutic effect, it is necessary to use the drug regularly. The maximum therapeutic effect can be achieved after 3-4 days of therapy.

Week 1: 2 injections in each nostril 1 time per day (200 mg per day).
From the 2nd week - up to 3 months: 1 or 2 injections into each nostril 1 time per day (100-200 mcg per day).
The maximum daily dose is 200 mg per day (no more than 2 injections in each nostril).

Elderly patients
The usual dose for adults.
Children from 4 to 12 years
On 1 injection in each nostril 1 time per day (100 mg per day).

Do not exceed the recommended dose (100 mcg per day). Children aged 4 to 12 years should use the drug for the shortest period of time necessary to achieve control over the symptoms of the disease. You should contact your doctor if the child needs to use the drug for a period of time longer than 2 months per year.

The maximum daily dose is 100 mcg (not 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.

Instructions for use

Before use, gently shake the bottle, take it, placing the index and middle fingers on both sides of the tip, and the thumb - under the bottom.

At the first use of the drug or a break in its use for more than 1 week, the condition of the sprayer should be checked: send the tip away from you, make several presses until a small cloud emerges from the tip. Next, you need to clear your nose (blow your nose). Close one nostril and insert the tip into the other nostril. Tilt your head slightly forward while continuing to hold the bottle vertically. Then you should begin to inhale through the nose and, while continuing to inhale, press once with your fingers to dispense the preparation. Exhale through the mouth. Repeat the procedure for the second spray in the same nostril, if necessary. Then completely repeat the procedure described by inserting the tip into the other nostril. After use, blot the tip with a clean cloth or handkerchief and cap it.

Rinse the sprayer at least 1 time per 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 set the tip to its original place at the top of the vial. Wear protective cap.

If the tip hole is clogged, the tip should be removed as described above and left for some time in warm water.Then rinse under running cold water, dry and put on the bottle again. Do not clean the tip opening with a pin or other sharp objects.

SIDE EFFECT

The adverse reactions listed below are listed according to the damage to organs and organ systems and the frequency of occurrence. The frequency of occurrence is determined as follows: very often (≥ 1/10), often (≥ 1/100 and <1/10), infrequently (≥ 1/1000 and <1/100), rarely (≥ 1/10000 and <1 / 1000), very rarely (<1/10000, including isolated cases). Very often, often and infrequently occurring adverse reactions are mainly established on the basis of data from clinical studies. Reactions that occur rarely and very rarely are mainly determined from spontaneous messages. When forming the frequency of occurrence of adverse reactions, background indicators in the placebo group were not taken into account, since they were generally comparable to the active treatment group.

OVERDOSE

No data on acute or chronic overdose of fluticasone propionate.

In healthy volunteers, intranasal administration of 2 mg of fluticasone propionate twice a day for 7 days did not affect the function of the hypothalamic-pituitary-adrenal system (the dose is 20 times higher than the therapeutic one). The use of the drug in doses higher than recommended for a long period of time may lead to a temporary inhibition of adrenal function. In case of overdose, consult a doctor.

INTERACTION WITH OTHER MEDICINES

Ritonavir (a highly active inhibitor of the CYP3A4 isoenzyme of the cytochrome P450 enzyme system) can significantly increase the concentration of fluticasone propionate in the blood plasma, resulting in a sharp decrease in serum cortisol concentration.The use of fluticasone propionate by inhalation or intranasal and ritonavir leads to the development of systemic glucocorticoid effects, including Itsenko-Cushing syndrome and suppression of the function of the adrenal cortex. Therefore, the simultaneous use of fluticasone propionate and ritonavir should be avoided, except for cases where the possible benefits outweigh the risks of systemic effects.

The simultaneous use of fluticasone propionate for inhalation use and less potent inhibitors of the CYP3A isoenzyme, such as ketoconazole and itraconazole, increase the exposure of fluticasone propionate and increase the risk of systemic side effects. It is recommended to be careful and, if possible, to avoid long-term joint use of these drugs.

Inhibitors of the CYP3A4 isoenzyme of the cytochrome P450 enzyme system cause a negligible (erythromycin) or a slight (ketoconazole) increase in plasma concentrations of fluticasone propionate, which do not entail any noticeable decrease in serum cortisol concentrations. However, caution should be exercised in the combined use of CYP3A4 isoenzyme inhibitors of the cytochrome P450 enzyme system (n