Briefly about the product
It is a nasal spray to relieve symptoms of year-round and seasonal allergic rhinitis. The active substance is fluticasone propionate.
Helps relieve symptoms of allergic rhinitis for 24 hours **. Helps combat the 6 symptoms of allergic rhinitis **, such as:
Sensation of pain and pressure in the sinuses of the nose.
* The first over-the-counter intranasal GCS for the treatment of allergic rhinitis. It has a fundamentally different mechanism of action in comparison with antihistamines.
** Instructions for medical use, RU PN015682 / 01 of 08.04.2009
fluticasone propionate (micronized) 50 mcg;
microcrystalline carboxymethyl cellulose,
solution of benzalkonium chloride,
hydrochloric acid diluted,
No significant changes in the daily AUC of serum cortisol were 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).
The anti-inflammatory effect of fluticasone propionate is realized as a result of its interaction with glucocorticoid receptors. Suppresses the proliferation of mast cells, eosinophils, lymphocytes, macrophages, 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 quick anti-inflammatory effect on the nasal mucosa. The antiallergic effect is manifested already 2-4 hours after the first application. Reduces sneezing, itching in the nose, rhinorrhea, nasal congestion, discomfort in the paranasal sinuses and a feeling of pressure around the nose and eyes.
It also alleviates eye symptoms associated with allergic rhinitis. The decrease 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.
After intranasal administration of fluticasone propionate (200 μg / day), plasma equilibrium Cmax in most patients is not quantified (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 ingestion of most of the drug. When taken orally, the absolute bioavailability is low (less than 1%) as a result of a combination of incomplete absorption from the digestive tract and active metabolism during the "first passage" through the liver. Total systemic absorption is thus extremely low.
In the equilibrium state of fluticasone, propionate has a large Vd of about 318 liters. Plasma protein binding is high - about 91%.
Fluticasone propionate is output rapidly from the systemic circulation mainly due to the hepatic metabolism to form an inactive carboxylic acid by isoenzyme CYP3A4. The metabolism of the swallowed fraction of fluticasone propionate during the "first pass" through the liver occurs in the same way.
Excretion 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).
Cmax in plasma decreases by approximately 98% within 3-4 hours, and only at very low plasma concentrations was a final T1 / 2 of 7.8 hours observed. The
renal clearance of fluticasone propionate is negligible (less than 0.2%), and the inactive metabolite, carboxylic acid, less 5%.
Fluticasone propionate and its metabolites are mainly excreted in the bile through the intestines.
Pregnancy and lactation
Flixonase® 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.
Before using the drug, the patient should consult a doctor in the following cases: taking medications to treat HIV infection, such as ritonavir; taking corticosteroids for the treatment of bronchial asthma, allergies, skin rashes; taking medications to treat fungal infections, such as ketoconazole; taking other powerful inhibitors of the CYP3A isoenzyme, for example, itraconazole; in the presence of glaucoma or cataract.
Use with caution in case of infection 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 Flixonase nasal spray.
Very often, often and infrequently occurring adverse reactions are mainly established on the basis of 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 but attention, since they were generally comparable with the active treatment group.
On the part of the immune system: very rarely - hypersensitivity reactions, incl. bronchospasm, rash, swelling of the face and tongue, anaphylactic reactions, anaphylactoid reactions.
From the nervous system: often - a headache, a feeling of unpleasant taste and smell. The appearance of a headache, a sensation of unpleasant taste and smell was also reported when using other nasal sprays.
From the side of the organ of vision: very rarely - glaucoma, increased intraocular pressure, cataract. 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 cavity and pharynx, irritation of the mucous membrane in the nasal cavity and pharynx (these undesirable reactions, as well as nosebleeds, were also observed when using other intranasal preparations); very rarely - perforation of the nasal septum (reported when taking intranasal corticosteroids).
With the use of certain intranasal corticosteroids, systemic effects may develop, especially when given in high doses for a long time.
As a result of this, a sharp decrease in the concentration of cortisol in serum occurs. The use of fluticasone propionate inhaled or intranasally and ritonavir leads to the development of side effects due to the systemic effect of corticosteroids, including Cushing's syndrome and inhibition of adrenal cortex function. Therefore, the simultaneous use of fluticasone propionate and ritonavir should be avoided, unless the possible benefits outweigh the risk of systemic effects.
With the simultaneous use of fluticasone propionate with other, less powerful inhibitors of the CYP3A4 isoenzyme, such as ketoconazole and itraconazole, it increases the exposure of fluticasone propionate and increases the risk of systemic side effects. It is recommended to be careful and, if possible, to avoid long-term combined use of these drugs.
Inhibitors of the CYP3A4 isoenzyme cause a negligible (erythromycin) or insignificant (ketoconazole) increase in plasma fluticasone propionate concentrations that do not entail any noticeable decrease in serum cortisol concentration. Nevertheless, caution should be exercised in the combined use of inhibitors of the CYP3A4 isoenzyme (e.g., ketoconazole) and fluticasone propionate due to a possible increase in the plasma concentration of the latter.
How to take, course of administration and dosage
Adults and children over 12 years old
1st week: 2 injections into each nostril 1 time / day (200 mcg / day);
from the 2nd week to 3 months: 1 or 2 injections into each nostril 1 time / day (100-200 mcg / day).
The maximum daily dose is 200 mcg / day (no more than 2 injections into each nostril).
Elderly patients are prescribed in the usual dose intended for adults.
Children from 4 to 12 years old
1 injection into 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 over the symptoms of the disease. It is necessary to consult your doctor if the child needs to use the drug for a period of time exceeding 2 months per year.
The maximum daily dose is 100 mcg (not more than 1 injection and 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, gently shake the bottle, take it by placing the index and middle fingers on either side 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, you should check the health of the nebulizer: point the tip away from you, press a few times 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 forward a little while continuing to hold the bottle upright. Then you should begin to inhale through the nose and, continuing to inhale, make a single press with your fingers to spray the drug. Breathe out through the mouth. Repeat the procedure for a second spray in the same nostril, if necessary. Next, completely repeat the described procedure by inserting the tip into another nostril. After use, dab the tip with a clean cloth or handkerchief and close it with a cap.
The sprayer should be flushed 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 back to the top of the vial. To put on a protective cap.
If the tip opening is clogged, the tip should be removed as described above and left in warm water for a while. Then rinse under a stream of cold water, dry and put on the bottle again. Do not clean the tip opening with a pin or other sharp objects.
When intranasally administered to healthy volunteers, 2 mg of fluticasone propionate 2 times / day for 7 days did not affect the function of the hypothalamic-pituitary-adrenal system (dose 20 times higher than the therapeutic).
The use of the drug in doses higher than recommended for a long time can lead to temporary inhibition of adrenal function. In case of an overdose, the patient should consult a doctor.
For adults and children from 12 years: do not use Flixonase® Nasal Spray for more than 3 months. If it is necessary to use the drug for more than 3 months, a doctor's consultation is necessary.
For children from 4 to 12 years: do not use Flixonase® Nasal Spray for more than 2 months. If it is necessary to use the drug for more than 2 months, a doctor's consultation is necessary. With prolonged use, regular monitoring of the function of the adrenal cortex is necessary.
There are reports of systemic effects when using nasal GCS, especially in high doses for a long time. These effects are much less likely than when taken orally. Systemic effects when using nasal corticosteroids can occur, in particular, when used in high doses for a long time. The likelihood of these effects is much lower than when taking corticosteroids by mouth, and they may vary in individual patients and between different corticosteroid drugs.
Possible systemic effects may include Itsenko-Cushing's syndrome, characteristic signs of cushingoid, suppression of adrenal function, growth retardation in children and adolescents, cataracts, glaucoma, and less commonly a number of psychological or behavioral effects, including psychomotor hyperactivity, sleep disturbances, anxiety, depression, or aggressiveness (in features in children).
In children receiving therapy with certain intranasal corticosteroids in permitted doses, growth retardation was observed. It is recommended to regularly monitor the growth of children receiving long-term treatment with intranasal GCS. When growth is slowed down, treatment should be reviewed to reduce the dose of intranasal GCS, if possible, to the minimum dose that maintains effective control of symptoms and consult a pediatrician.
The simultaneous use of ritonavir and fluticasone propionate should be avoided unless the potential benefit to the patient exceeds the possible risk of developing systemic side effects of corticosteroids.
It is recommended to stop taking the drug and consult a 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 discharge from the nose, which may indicate infection and are not associated with 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, the fluticasone propionate nasal spray eliminates the symptoms of seasonal allergic rhinitis, but in some cases, with a very high concentration of allergens in the air, additional therapy may be necessary.
Additional treatment may be needed to relieve eye symptoms while treating seasonal allergic rhinitis successfully.
To achieve the maximum therapeutic effect, it is necessary to adhere to a regular regimen.
Caution must be exercised when transferring patients with systemic corticosteroids to treatment with fluticasone propionate in the form of a nasal spray, especially if adrenal dysfunction is observed against the background of regular monitoring.
Flixonase®, a nasal aqueous spray contains benzalkonium chloride, which can cause bronchospasm.
In case of contact with patients with chickenpox, measles and in case of changes from the side of vision, it is recommended to stop treatment and consult a doctor.
Influence on the ability to drive vehicles and mechanisms
In clinical trials, no data were obtained on the effect of the drug on the ability to drive vehicles and other mechanisms, but side effects that the drug may cause should be considered.
120 doses - yellow glass bottles (1) with a metering device, an adapter and a protective cap - plastic cases with a booklet label.