Flixonase nasal spray dosed 50mcg/dose 120doz №1

Name:
Flixonase spray 50 mcg dose per vial 120 doses per pack No. 1
Description:
White, opaque suspension, free from foreign particles. The main active ingredient Fluticasone Release form Dosed nasal spray 50 mcg / dose. 60 and 120 doses in Type I or Type III amber glass vials. Each vial is equipped with a dosing device. An adapter for intranasal administration is put on the vial and dosing device. The bottle is additionally equipped with a cap to protect the adapter from dust. Each vial, together with a dosing device, an adapter and a protective cap (in the assembled state) and instructions for medical use, is placed in a cardboard box. Dosage 50 mcg Special instructions Elderly patients Usual adult dose. Children under 12 years old For the prevention and treatment of seasonal and year-round allergic rhinitis in children aged 4-11 years, the drug is prescribed 1 injection (50 mcg) in each nostril 1 time per day, preferably in the morning. In some cases, it may be necessary to prescribe 1 injection in each nostril 2 times a day. The maximum daily dose is 200 mcg (no more than 2 injections in each nostril). The lowest dose should be used to effectively control the symptoms of the disease. Using the inhaler Before use, shake the bottle gently, 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 serviceability of the sprayer: point the tip away from you, make a few clicks until a small cloud appears 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 vial 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. Exhale through your mouth. Repeat the procedure for a second spray in the same nostril, if necessary. Then completely repeat the described procedure by inserting the tip into the other nostril. After use, blot the tip with a clean tissue or handkerchief and close it with a cap. The sprayer should be washed 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 place the tip back into place at the top of the vial. Put on the 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 back on the bottle. Do not clean the tip hole with a pin or other sharp objects. Pharmacological action Mechanism of action After intranasal administration of fluticasone propionate, there is no or slight inhibition of the hypothalamic-pituitary-adrenal system. There was no significant change in the daily area under the pharmacokinetic curve of serum cortisol after intranasal administration of fluticasone propionate at a dose of 200 mcg / day compared with placebo (ratio: 1.01; 90% confidence interval (CI) from 0.9 to 1.14). In a one-year, randomized, double-blind, placebo-controlled growth study in prepubertal children (ages 3-9 years) in parallel groups (56 patients received intranasal fluticasone propionate and 52 patients received placebo), there was no statistically significant difference in growth rate between patients receiving intranasal fluticasone propionate (200 mcg / day), and patients receiving placebo. The estimated growth rate at one year of treatment was 6.20 cm/year (standard error (SD) = 0.23) in the placebo group and 5.99 cm/year (SD = 0.23) in the fluticasone propionate group; the mean difference between groups in growth rate after one year was 0.20 cm/yr (SD = 0.28, 95% CI -0.3’5 to 0.76). There was no evidence of clinically significant changes in the function of the hypothalamic-pituitary-adrenal axis or bone mineral density based on assessment of 12-hour urinary cortisol excretion and dual-energy x-ray absorptiometry, respectively. Pharmacokinetics Absorption After intranasal administration of fluticasone propionate at a dose of 200 mcg / day. maximum equilibrium plasma concentrations are not quantified in most patients (less than 0.01 ng / ml). The highest plasma concentration was recorded at 0.017 ng/mL. Direct absorption from the nasal cavity is unlikely due to low water solubility and ingestion of most 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 first-pass metabolism. The total systemic absorption is thus extremely low. Distribution Fluticasone propionate has a large volume of distribution at steady state (approximately 318 L). Communication with blood plasma proteins is moderately high (91%). Metabolism Fluticasone propionate is excreted rapidly from the systemic circulation, mainly due to metabolism in the liver with the formation of an inactive carboxylic acid through the CYP3A4 isoenzyme of the cytochrome P450 system. The metabolism of the swallowed fraction of fluticasone propionate during the first passage through the liver occurs in the same way. Caution should be exercised when co-administering potent CYP3A4 inhibitors such as ketoconazole and ritonavir as there is a potential for increased systemic exposure to fluticasone propionate. Withdrawal Withdrawal of fluticasone propionate, administered intravenously, is linear in the dose range from 250 to 1000 mcg and is characterized by a high plasma clearance value (1.1 l / min). The maximum plasma concentration decreases by approximately 98% within 3-4 hours, and only at very low plasma concentrations was a terminal half-life of 7.8 hours 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 Prevention and treatment of seasonal allergic rhinitis (including hay fever) and perennial rhinitis. Fluticasone propionate has a powerful anti-inflammatory activity, however, when applied topically to the nasal mucosa, it does not show a systemic effect. Method of application and doses Only intranasally. Avoid contact of the drug with the eyes. To achieve the full therapeutic effect, it must be used regularly. The lack of an immediate effect should be explained to the patient, since the maximum effect can be achieved after 3-4 days of treatment. Adults and children over 12 years of age For the prevention and treatment of seasonal and year-round allergic rhinitis, 2 injections in each nostril 1 time per day, preferably in the morning (200 mcg per day). In some cases, 2 sprays in each nostril 2 times a day (400 micrograms per day) can be used for a short time in order to achieve control of symptoms, after which the dose can be reduced. When symptoms return, the dose may be increased again. The lowest dose should be used to effectively control the symptoms of the disease. The maximum daily dose is 400 mcg (no more than 4 injections in each nostril). Use during pregnancy and lactation There is insufficient evidence for the safety of use in pregnant women. Administration of corticosteroids to animals during pregnancy may result in fetal abnormalities, including cleft palate and intrauterine growth retardation. Therefore, there may be a small risk of developing such effects in the human fetus. However, it is worth noting that fetal changes in animals occurred after relatively high systemic exposure; direct intranasal administration provides minimal systemic exposure. As with other medicines, the use of Flixonase® in pregnant women is possible only in cases where the expected benefit to the patient outweighs the possible risk to the fetus or child. The secretion of fluticasone propionate into breast milk has not been studied. Subcutaneous administration of fluticasone propionate to lactating laboratory rats resulted in measurable plasma levels and fluticasone propionate in milk. However, after intranasal administration to primates, the drug was not detected in plasma and therefore it is unlikely that it will be detected in breast milk. For lactating women, Flixonase® can be prescribed only in cases where the expected benefit to the patient outweighs any possible risk to the child. Precautions Local infections; nasal tract infections should be treated appropriately, but they are not a contraindication for Flixonase® therapy. The full effect of fluticasone propionate nasal spray may take several days of treatment. Caution must be exercised when transferring patients from systemic glucocorticosteroid therapy to treatment with fluticasone propionate nasal spray if there is reason to suspect adrenal dysfunction. 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. Systemic effects of nasal corticosteroids can be observed mainly with the appointment of high doses for a long time. These effects are much less common than with oral corticosteroids and may vary from patient to patient and between different corticosteroid drugs (see Pharmacodynamics and Pharmacokinetics). Potential systemic effects may include Cushing’s syndrome, Cushingoid traits, adrenal suppression, growth retardation in children and adolescents, cataracts, glaucoma, and, less commonly, physiological and behavioral reactions such as psychomotor hyperactivity, sleep disturbances, anxiety, depression, or aggression (especially in children). ). Growth retardation has been reported in children receiving registered doses of certain nasal corticosteroids. It is recommended to regularly monitor the growth of children receiving long-term therapy with nasal corticosteroids. When growth is slowed, therapy should be reviewed, if possible, with the aim of reducing the dose to the minimum that effectively controls the symptoms of the disease. In addition, a visit to the pediatrician is recommended. Therapy with higher than recommended doses of the drug can lead to clinically significant suppression of adrenal function. If higher than recommended doses are used, consideration should be given to the use of additional systemic corticosteroids during periods of stress or elective surgery. Ritonavir can significantly increase the plasma concentration of fluticasone propionate. Therefore, concomitant use of ritonavir and fluticasone propionate should be avoided unless the potential benefit to the patient outweighs the potential risk of systemic side effects of corticosteroids. There is an increased risk of systemic side effects when fluticasone propionate is used in combination with other potent CYP3A inhibitors. Interaction with other drugs Under normal conditions, intranasal use of fluticasone propionate leads to very low plasma concentrations of fluticasone propionate due to significant first-pass metabolism in the liver and high systemic clearance through cytochrome P450 3A4 in the intestine and liver. Therefore, clinically significant interactions with fluticasone propionate are unlikely. As shown in an interaction study in healthy volunteers, ritonavir (a strong inhibitor of the coenzyme CYP3A4 of the cytochrome P450 enzyme system) at a dose of 100 mg 2 times a day is able to significantly (several hundred times) increase plasma concentrations of fluticasone propionate, resulting in a sharp decrease in levels serum cortisol and systemic side effects have been noted, including Cushing’s syndrome and adrenal suppression. Such a combination should be avoided until the benefit of the appointment outweighs the possible risk of developing systemic glucocorticoid adverse reactions. In a small study of inhaled fluticasone propionate in healthy volunteers, the slightly less potent CYP3A4 inhibitor ketoconazole was shown to increase fluticasone propionate exposure by 150% after a single inhalation. This results in a greater reduction in plasma cortisol compared to fluticasone propionate alone. It is expected that the co-administration of other strong inhibitors of the CYP3A4 coenzyme of the cytochrome P450 enzyme system, such as itraconazole, will also lead to an increase in the systemic exposure of fluticasone propionate and the risk of developing systemic side effects. It is recommended to be careful and avoid, if possible, long-term therapy with such drugs. I__ Studies have shown that other inhibitors of the CYP3A4 isoenzyme of the cytochrome P450 system cause a negligible (erythromycin) or insignificant (ketoconazole) increase in plasma fluticasone propionate concentration, which does not entail any noticeable decrease in serum cortisol concentration. However, caution should be exercised in the combined use of inhibitors of the CYP3A4 isoenzyme of the cytochrome P450 enzyme system (for example, ketoconazole) and fluticasone propionate due to a possible increase in the plasma concentration of the latter. Contraindications Hypersensitivity to fluticasone propionate or any other component of the drug. Composition Active ingredient: fluticasone propionate (micronized) 50.0 mcg / dose. Excipients: dextrose (anhydrous), Avicel RC591 (microcrystalline cellulose, sodium carboxymethylcellulose), phenylethanol, benzalkonium chloride (in the form of benzalkonium chloride solution), polysorbate 80, diluted hydrochloric acid, purified water. Overdose There is no evidence of acute or chronic overdose of fluticasone propionate. In healthy volunteers, intranasal administration of 2 mg of fluticasone propionate twice a day for 7 days had no effect on the function of the hypothalamic-pituitary-adrenal system. The use of high doses of corticosteroids orally or inhaled for a long period of time can lead to depression of the function of the hypothalamic-pituitary-adrenal system. The use of the drug in doses higher than recommended for a long period of time can lead to temporary inhibition of adrenal function. In such patients, treatment with fluticasone propionate should be continued at doses required to control symptoms. Side effects The undesirable effects presented below are listed depending on the anatomical and physiological classification and frequency of occurrence. The frequency of occurrence is defined as follows: very often (? 1/10), often (> 1/100 and < 1/10), infrequently (? 1/1 OOO and < 1/100), rarely (? 1/10,000 and < 1/1,000), very rare (< 1/10,000, including isolated cases). Frequency categories very often, often and infrequently were formed on the basis of clinical studies of the drug, categories rarely and very rarely were determined during post-registration observation. As with other nasal sprays, there have been reports of unpleasant taste and odor sensations, as well as headaches. As with other nasal sprays, cases of dryness and irritation of the nose and throat, as well as nosebleeds, have been reported. Also, after the use of intranasal corticosteroids, perforation of the nasal septum has been reported. Systemic effects of some intranasal corticosteroids may be observed; in particular, when used in high doses for a long period of time. Storage conditions Store at a temperature not exceeding 30 °C. Keep out of the reach of children.