Fliksonase® (Flixonase®)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceFluticasoneFluticasone
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    • Dosage form: & nbspnasal dosing spray
    Composition:
    COMPOSITION per 1 dose:
    Component
    Excipients
    Fluticasone propionate (micronized) 0.05 mg
    Dextrose 5.00 mg
    Avicel RC591 (microcrystalline cellulose, carmellose sodium) 1.50 mg
    Phenylethanol 0.25 mg
    Benzalkonium chloride1 0.02 mg
    Polysorbate 80 0.005 mg
    Hydrochloric acid2 to pH 6.3-6.5 mg
    Purified water up to 100.00 mg
    Note:
    1. It is added in the form of an aqueous solution according to the European Pharmacopoeia.
    2. Add to reach pH 6.3-6.5 if the pH of the final suspension is greater than 6.8


    Description:
    White, opaque suspension, free from foreign particles.

    Pharmacotherapeutic group:Glucocorticosteroid for topical application
    ATX: & nbsp

    R.01.A.D.08   Fluticasone

    Pharmacodynamics:
    Mechanism of action
    Fyuticasone propionate is a substance with a strong anti-inflammatory effect. With intranasal administration of ns, there is a marked systemic effect and suppression of the hypothalamic-pituitary-adrenal system.A significant change in the daily area under the pharmacokinetic curve of serum cortisol ns was detected after administration of fluticasone propionate at a dose of 200 mcg / day compared with placebo (ratio: 1.01, 90% CI, confidence interval 0.9 to 1.14).
    Fluticasone propionate has an anti-inflammatory effect due to the interaction of the receptors with glucocorticosteroids. 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 phase of the allergic reaction. Fluticasone propionate has a quick anti-inflammatory effect on the nasal mucosa, and its antiallergic effect is manifested as early as 2-4 hours after the first application. Reduces sneezing, itching in the nose, runny nose, stuffy nose, discomfort in the sinuses and a feeling of pressure around the nose and eyes. In addition, it alleviates eye symptoms associated with allergic rhinitis. Reduction in the severity of symptoms (especially nasal congestion) persists for 24 hours after a single injection of a spray at a dose of 200 μg.Fluticasone propionate improves the quality of life of patients, including physical and social activity.

    Pharmacokinetics:
    Suction
    After intranasal administration of fluticasone propionate at a dose of 200 μg / day, the maximum equilibrium plasma concentrations are not quantitatively determined in the majority of 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 the ingestion of most of the drug. Absolute oral bioavailability is low (less than I%) as a result of a combination of incomplete absorption from the gastrointestinal tract and active metabolism during the first passage through the liver. The overall systemic absorption is, therefore, extremely low.
    Distribution
    Fluticasone propionate has a large volume of distribution in the equilibrium state (approximately 318 L). The association with plasma proteins is high (91%).
    Metabolism
    Fluticasone propionate is excreted rapidly from the systemic blood flow mainly through metabolism in the liver with the formation of an inactive carboxylic acid via the cytochrome P450 cytochrome P450 isoenzyme CYP3A4.Metabolism of the swallowed fraction of fluticasone propionate during the first passage through the liver occurs in the same way.
    Excretion
    Elimination 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 is reduced by approximately 98% within 3-4 hours, and only at very low plasma concentrations was a final half-life of 7.8 hours. The renal clearance of fluticasone propionate is negligible (less than 0.2%), and the inactive metabolite carboxylic acid is less than 5%. Fluticasone propionate and its metabolites are mainly derived from the bile through the intestine.

    Indications:
    Treatment of year-round and seasonal allergic rhinitis, including iollinosis (hay fever) in adults and children from the age of 4 (elimination of symptoms such as pain and sensation of pressure in the paranasal sinuses, nasal congestion, runny nose, sneezing, itching in the nose, lachrymation) .

    Contraindications:
    Hypersensitivity to fluticasone propionate 'or any other component of the drug.
    Children under 4 years.
    Recently suffered nasal trauma or surgery in the nasal cavity.

    Carefully:
    Before using the drug, you should consult your doctor in case you are taking:
    - medicines for the treatment of HIV infection, such as ritonavir;

    - Glucocorticosteroids for the treatment of bronchial asthma, allergies, skin rashes;
    - medicines 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 cataract.
    Take with caution in the presence of 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 nasal Spray Fliksonase.

    Pregnancy and lactation:
    Before using Fliksonase during pregnancy and during lactation it is necessary to consult a doctor.
    Pregnant and lactating women, the preparation Fliksonase can be prescribed only if the expected benefit for the patient exceeds any possible risk to the fetus or child.

    Dosing and Administration:
    Only intranasal.
    To achieve the full therapeutic effect, it is necessary to apply the drug regularly. The maximum therapeutic effect can be achieved after 3-4 days of therapy.
    Adults and children over 12 years of age
    Week 1: 2 injections per nostril once a day (200 μg per day).
    From the 2nd week - up to 3 months: but 1 or 2 injections into each nostril 1 time per day (100-200 mkg per day).
    The maximum daily dose is 200 mcg per day (no more than 2 injections per each nostril).
    Special patient groups
    Elderly patients Usual Adult Dose.
    Children from 4 to 12 years old
    For 1 injection into each nostril 1 time per day (100 mcg per day). Do not exceed the recommended dose (100 μg per day). Children between the ages of 4 and 12 must use the drug for the shortest period of time necessary to control the symptoms of the disease. It is necessary to consult a doctor if the child needs to use the drug for a period of more than 2 months per year.
    The maximum daily dose is 100 μg (not more than 1 injection into each nostril).
    In the absence of effect from the use of the drug in all age groups of patients it is necessary to consult a doctor.
    Instructions for use
    Before the use should be carefully shake the bottle, take it by placing your index and middle fingers on either side of the tip, and the thumb under the bedplate.
    For the first use of the drug or a break in its use more weeks I should check the serviceability of the atomizer: forward tip of itself, produce few taps until the tip of the small cloud does not appear. 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, continuing to hold the bottle upright. Then you should start breathing in through your nose and, continuing to inhale, press once with your fingers to spray the drug. Exhale through the mouth. Repeat the procedure for the second spray in the same nostril if necessary. Then repeat the above procedure completely by inserting the tip into the other nostril. 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 1 time per week. To do this, gently shine the tip and rinse it in warm water.Shake off excess water and leave to dry in a warm place. Avoid overheating. Then gently place the tip on the same place in the top of the vial. Put the protective cap on.
    If the tip of the tip is clogged, the tip should be removed as described above and left for some time in warm water. Then rinse under a stream of cold water, dry and re-put on the bottle. Do not clean the tip of the tip with a pin or other sharp objects.

    Side effects:
    The undesirable reactions presented below are listed in accordance with the damage to organs and organ systems and frequency of occurrence. Frequency of occurrence is defined as follows: very parts (> 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 individual cases). Very often, often and infrequently, unwanted reactions are mainly established based on clinical trials. Reactions that occur rarely and very rarely are mainly determined from spontaneous reports. When forming the frequency of occurrence of undesired reactions, background indices in the placebo group were not taken into account, since they were generally comparable to the active treatment group.
    Immune system disorders
    Rarely: hypersensitivity reactions, including bronchospasm, rash, swelling
    face and tongue, anaphylactic reactions, anaphylactoid reactions. Disturbances from the nervous system
    Often: headache, a sense of unpleasant taste and smell.
    The appearance of a headache, a sense of unpleasant taste and smell was also reported when using other nasal sprays. Disturbances on the part of the organ of sight
    Rarely: glaucoma, increased intraocular pressure, cataract.
    A small number of spontaneous reports were associated with prolonged therapy with the drug.
    Disturbances from the respiratory system, chest and mediastinal organs
    Often: nose bleed.
    Often: dryness of the mucous membrane in the nasal cavity and pharynx,
    irritation of the mucous membrane in the nasal cavity and pharynx.
    These adverse reactions, as well as nasal bleeding, were observed with other intranasal drugs. Rarely: perforation of the nasal septum (reported on admission
    intranasal glucocorticosteroids).
    With some intranasal corticosteroids may develop systemic effects, particularly when administered at high doses for a long period of time (see. Also see "Cautions"),

    Overdose:
    There is no evidence of acute or chronic overdose of fluticasop propionate.
    In healthy volunteers, the administration of 2 mg intranazalnos flutikazopa propionate twice a day for 7 days had no effect on the function of the hypothalamic-pituitary-adrsnalovoy system (dose 20 times higher therapeutic). The use of the drug in doses higher than those recommended for a long period of time can lead to a temporary suppression of the function of the adrenal glands.
    In case of overdose, see a doctor.

    Interaction:
    Ritonavir (highly potent inhibitor of CYP3A4 isoenzyme cytochrome P450 enzyme system) is able to significantly increase the concentration of fluticasone propionate in blood plasma, resulting in dramatically reduced cortisol concentration in serum. Use of fluticasone propionate by inhalation or nntranazalno and ritonavir results in the development of systemic glucocorticoid effects including pituitary Kushiiga syndrome and depression of adrenocortical function.Therefore, simultaneous use of fluticasone propionate and ritonavir should be avoided, unless the possible benefit exceeds the risks of systemic effects. The concomitant use of fluticasone propionate for inhalation and the use of less potent inhibitors of the CYP3A isoenzyme, such as kstoconazole and itraconazole leads to an increased exposure of fluticasone propionate and an increased risk of systemic side effects. It is advisable to use caution and, if possible, avoid long-term joint use of these drugs. Inhibitors of the isoenzyme CYP3A4 of the cytochrome P450 enzyme system cause negligible (erythromycin) or insignificant (kstokonazol) increase in concentrations of fluticasone propionate in plasma, which does not entail any noticeable decrease in serum cortisol concentrations. Nevertheless, caution should be exercised when using the inhibitors of the CYP3A4 isoenzyme inhibitor of the cytochrome P450 enzyme system (eg, kstoconazole) and fluticasone propionate in view of a possible increase in plasma concentration of the latter.

    Special instructions:
    The drug is indicated only for intranasal administration.
    For adults and children from the age of 12: Fliksonase Nasal Spray should not be used for more than 3 months. If you need to use the drug for more than 3 months, you need a doctor's consultation
    For children from 4 to 12 years: Fliksonase nasal spray should not be used for more than 2 months. If it is necessary to use the drug for more than 2 months, it is necessary to consult a doctor. With prolonged use, regular monitoring of the function of the adrenal cortex is necessary.
    There have been reports of systemic effects when using nasal glucocorticosteroids, especially at high doses for a long time. These effects are much less likely than with oral administration. Systemic effects when using nasal corticosteroids can occur, in particular, when high doses are used for a long time. The likelihood of these effects is much lower than when taking corticosteroids by mouth, and they can vary in individual patients and between different corticosteroid drugs. Possible systemic effects may include Itenko-Cushing syndrome, characteristic features of the Cushingoid,inhibition of adrenal function, growth retardation in children and adolescents, cataracts, glaucoma and, rarely, a number of psychological or behavioral effects, including psychomotor hyperactivity, sleep disorders, anxiety, depression, or aggression (especially in children).
    In children receiving therapy with some intranasal glucocorticosteroids at permitted doses, a decrease in the growth rate was observed. It is recommended to regularly monitor the growth of children receiving long-term treatment with intranasal glucocorticosteroids. If the growth is slowed, treatment should be reviewed to reduce the dose of the intranasal glucocorticosteroid, but the possibility, up to the minimum dose, to maintain effective control over the symptoms and contact the pediatrician.
    The simultaneous use of ritonavra and fluticasone propionate should be avoided unless the potential benefit to the patient exceeds the possible risk of developing side effects of corticosteroids (see "Interactions with Other Drugs").
    The full effect of fluticasone propionate in the form of a nasal spray may appear only after 3-4 days of treatment.
    It is recommended to stop taking the drug and consult a doctor if there is no improvement within 4 days. Consultation with your doctor is also necessary if you have 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 ns are a contraindication to the use of the nasal spray Fliksonase.
    In most patients, the nasal spray of fluticasone propionate eliminates the symptoms of seasonal allergic rhinitis, in some cases, with a very high concentration of allergens in the air, additional therapy may be needed.
    To relieve the symptoms from the eyes on the background of the successful therapy of seasonal allergic rhinitis, additional therapy may be required.
    To achieve the maximum therapeutic effect, you must adhere to a regular scheme of application.
    Care should be taken when transferring patients with systemic glucocorticosteroid therapy to nasal spray fluticasone propionate,especially if there is a violation of adrenal function against a background of regular monitoring.
    Fliksonase, nasal aqueous spray contains benzalkonium chloride, which can cause bronchospasm.
    In case of contact with patients with chickenpox, measles and in case of changes in vision it is recommended to stop treatment and consult a doctor).

    Effect on the ability to drive transp. cf. and fur:
    In clinical trials, no evidence of the effect of the drug on the ability to drive vehicles and other mechanisms has been obtained, but side effects that the drug may cause should be considered.

    Form release / dosage:Spray nasal dosed, 50 mcg / dose.
    Packaging:

    For 60 and 120 doses in a vial of yellow glass type I or type III. Each vial is equipped with a dosing device. The vial and dosing device are fitted with an adapter for intranasal administration. The bottle is additionally equipped with a cap to protect the adapter from dust.
    One bottle together with the dosing device, adapter and protective cap (in the assembled state) and instructions for use in a cardboard bundle.
    For 120 doses in a polypropylene bottle. Each vial is equipped with a dosing device.The vial and dosing device are fitted with an adapter for intranasal administration. The bottle is additionally equipped with a cap to protect the adapter from dust.
    One bottle together with the dosing device, adapter and protective cap (in the assembled state) and instructions for use in a cardboard bundle.

    Storage conditions:
    Store at a temperature of no higher than 30 ° C. Keep out of the reach of children.

    Shelf life:
    3 years.
    Do not use after the expiry date printed on the package.

    Terms of leave from pharmacies:Without recipe
    Registration number:П N015682 / 01
    Date of registration:08.04.2009
    The owner of the registration certificate:GlaxoSmithKline Trading, ZAO GlaxoSmithKline Trading, ZAO Russia
    Manufacturer: & nbsp
    Representation: & nbspGlaxoSmithKline Trading, ZAOGlaxoSmithKline Trading, ZAO
    Information update date: & nbsp24.10.2015
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