Active material: Fluticasone
When ATH: R01AD08
CCF: GCS for intranasal use
ICD-10 codes (testimony): J30.1, J30.3
When CSF: 04.04.01
Manufacturer: GlaxoSmithKline Pharmaceuticals SA (Poland)
PHARMACEUTICAL FORM, COMPOSITION AND PACKAGING
Spray nazalynыy dozirovannыy as a white opaque suspension, free from foreign particles.
|fluticasone propionate (micronized)||50 g|
Excipients: dextrose bezvodnaya, microcrystalline cellulose, carboxymethyl cellulose microcrystalline, phenylethyl alcohol, rr benzalkonium chloride, polysorbate 80, diluted hydrochloric acid, Purified water.
60 doses – vials of dark glass with a dosing device and adapter (1) – packs cardboard.
120 doses – vials of dark glass with a dosing device and adapter (1) – packs cardboard.
GCS for intranasal use. Has a pronounced anti-inflammatory, decongestant and anti-allergic effect.
Anti-inflammatory effect is realized by the interaction of the drug with the receptors glucocorticosteroids. Inhibits proliferation of mast cells, eozinofilov, lymphocytes, macrophages, neutrophil. Fluticasone propionate reduces the production of inflammatory mediators and a number of biologically active substances (incl. gistamina, prostaglandins, leukotrienes, Cytokine) during the early and late phase allergic reactions. It provides rapid anti-inflammatory effect on the nasal mucosa. Allergy effect is already in 2-4 hours after the first application. Reduces sneezing, itchy nose, rhinorrhea, nasal congestion, discomfort in the sinuses and the feeling of pressure around the nose and eyes. Besides, facilitates eye symptoms, associated with allergic rhinitis. The reduction of symptoms (especially nasal congestion) It persists for 24 h after a single spray application of a dose of 200 g.
Fluticasone propionate improves the quality of life of patients, including physical and social activity.
When used in the recommended doses, the drug has no systemic action and practically does not inhibit the hypothalamic-pituitary-adrenal axis.
After intranasal fluticasone propionate (200 mg / day) Cmax plasma levels in most patients not determined (ie. is less than 0.01 ng / ml). The highest value of Cmax is 0.017 ng / ml. Immediate absorption from the mucous membranes of the nasal cavity is very small due to the low solubility of the drug in water, therefore most of the dose, in the end, swallowed. When taken orally, fluticasone propionate absorbed less blood 1% dose due to low absorption and first-pass metabolism. These reasons due to the extremely low total absorption from the nasal cavity and gastrointestinal tract (swallowed drug).
Upon reaching Css plasma fluticasone propionate has a significant Vd – about 318 l.
Plasma protein binding is approximately 91%.
Fluticasone propionate is subjected to the effect “first pass” through the liver, metabolized by CYP3A4 isoenzyme, with the participation with the formation of an inactive metabolite carboxy.
Write mainly with bile in an unchanged form and in the form of metabolites.
- Prevention and treatment of seasonal allergic rhinitis;
- Prevention and treatment of perennial allergic rhinitis.
Fliksonaze is only intended for intranasal use. To achieve the full therapeutic effect of the drug should be used regularly.
Adults and children over 12 years appoint 100 g (2 dose) in each nostril 1 time / day (total dose 200 mg / day), preferably in the morning. After achieving control of symptoms may be nominated by 50 g (1 dose) in each nostril 1 time / day (total dose 100 mg / day).
In some cases, apply for 100 g (2 dose) in each nostril 2 times / day (total dose 400 mg / day) for a short time to achieve control of symptoms, after this dose can be reduced. The maximum daily dose is 400 g (by 4 dose in each nostril).
Elderly patients It does not require correction dosing regimen.
For children 4-12 years It is encouraged to nominate for 50 g (1 dose) in each nostril 1 time / day. The maximum daily dose is 200 g (by 2 dose in each nostril).
The maximum therapeutic effect is manifested through 3-4 day care. To achieve the full therapeutic effect is necessary to regularly use the drug.
Mode of application
Before the use should be carefully Shake, Get him, placing the index and middle fingers on both sides of tip, and the thumb - a bedplate. When first using the drug, or a break in its use of a 1 of the week, check the operation of the spray gun (giving a tip from you, make a few clicks, until the tip of a small cloud appears).
- Clean the nose (gently blow your nose);
- Close one nostril and put the tip into the other nostril;
- Tilt your head slightly forward, continuing to hold the spray bottle upright;
- Start to breathe in through your nose and, Continuing to inhale, to produce a single touch of a finger to spray the drug;
- Exhale through the mouth.
Repeat this procedure for the second spray into the same nostril, if necessary. Next, repeat the full procedure, insert the tip into the other nostril.
After use wet the tip with a clean cloth or handkerchief and close the cap.
The sprayer should be washed at least 1 times a week. To this end, carefully remove the tip, rinse it in warm water. Shake off excess water and leave to dry in a warm place. Avoid overheating. Then gently install the tip into place on top of the brown bottle. Wear protective cap. If the hole is clogged tip, the tip should be removed as described above and leave for a while in hot water. Then rinse under cold running water, dried and then put in the bottle. You can not clean the tip orifice with a pin or other sharp objects.
Local reactions: dryness and irritation of the nose, unpleasant taste and smell, nosebleeds, burning sensation, nasal congestion; rarely (less 1/10 000 cases) – perforation of the nasal septum (especially in surgical interventions in the nasal cavity history).
Allergic reactions: possible skin rash, swelling of the face and tongue; rarely (less 1/10 000 cases) – anaphylactic reactions and bronchospasm.
It has been reported very rare cases of glaucoma, increased intraocular pressure and cataracts on a background of long-term use of fluticasone propionate, However, causation in clinical trials lasting up to 1 It had not been identified.
- Children up to age 4 years;
- Hypersensitivity to fluticasone propionate and other components of the drug.
FROM caution should use the drug in the presence of herpes, as well as infections of the nasal cavity or paranasal sinuses. When infectious diseases of the nose requires appropriate treatment. Infectious diseases of the nose are not a contraindication for use Fliksonaze.
FROM caution It should be prescribed the drug after recent nasal trauma or surgery in the nasal cavity, as well as the presence of ulcerative lesions of the nasal mucosa.
FROM caution should be given simultaneously with Fliksonaze inhibitors of CYP3A4 (incl. with ritonavir, ketoconazole), because these drugs can cause an increase in the concentration of fluticasone propionate in plasma.
FROM caution the drug should be administered concurrently with other dosage forms of corticosteroids, including tablets, Creams, ointment, for the treatment of asthma, similar nasal sprays and eye drops or nasal.
Pregnancy and lactation
Do not appoint Fliksonaze during pregnancy. If necessary, use of the drug in these patients must take into account the expected benefits of therapy for the mother and the potential risk to the fetus.
Care must be taken when transferring patients from systemic corticosteroid therapy to treatment with Flixonase, if there is reason to believe a violation of the adrenal glands.
With long-term use of the drug requires regular monitoring of adrenocortical function.
Patients should be warned about, that if through 7 days of constant improvement of the drug does not occur, you should seek medical advice.
With continued use of the drug more 6 months requires medical supervision of the patient.
In most cases, the use of Fliksonaze can successfully control the symptoms of seasonal allergic rhinitis, but in some cases, At very high concentrations of allergens in the air in the summer, may require additional therapy.
For relief of ocular manifestations with successful treatment of seasonal allergic rhinitis may require additional treatment.
Symptoms of acute and chronic overdose is not registered. When administered intranasally to healthy volunteers by 2 mg Valium 2 times / day for 7 days did not show any effect on the function of the hypothalamic-pituitary-adrenal axis.
Because of the very low concentrations of fluticasone propionate in plasma after application Fliksonaze clinically significant interaction unlikely.
In an application with ritonavir Fliksonaze, which is a potent inhibitor of CYP3A4, may be a significant increase in the concentration of fluticasone propionate in plasma. The result is a dramatic decrease in the serum cortisol concentration, and develop side effects, due to systemic effects of corticosteroids, including Cushing's syndrome and suppression of adrenocortical function.
In an application Fliksonaze with other inhibitors of CYP3A4 been negligible (erythromycin) or minor (ketoconazole) increasing concentrations of fluticasone propionate in plasma, causing no significant decrease in serum cortisol concentrations.
Conditions of supply of pharmacies
The drug is released under the prescription.
Conditions and terms
List B. The drug should be stored at a temperature no higher than 30 ° C. Shelf life - 2 year.