Properties
What is it?
International Nonproprietary Name - fluticasone propionate ATC Classification Code - R01AD08 Clinical-Pharmacological Group - Anti-inflammatory agents for topical use; Glucocorticosteroids Composition and Dosage Form 50 mcg nasal metered aerosol 14.5g 120 doses in a canister Nasal aqueous metered suspension 1 dose. Fluticasone propionate 50 mcg. Other ingredients: microcrystalline cellulose, sodium carboxymethylcellulose, dextrose, polysorbate 80, benzalkonium chloride, phenylethyl alcohol, disodium hydrogen phosphate, citric acid, purified water. Pharmacological Properties Topical glucocorticosteroid preparation for intranasal use. Exhibits anti-inflammatory and anti-allergic action. Fluticasone is a potent corticosteroid with high affinity for glucocorticoid receptors, used for the prevention and treatment of allergic rhinitis. Fluticasone is characterized by a strong local anti-inflammatory effect and weak systemic action on the body. In studies of allergic rhinitis symptoms, plasma concentration of fluticasone was compared after local and oral administration: 200 mcg nasal spray (plus placebo per os) and 5-10 mg fluticasone per os (plus nasal spray) were used for 14 days. Compared to oral administration, intranasal administration of fluticasone did not result in detectable plasma concentrations. Intranasal spray significantly reduced allergic rhinitis symptoms. The study confirmed its therapeutic superiority with intranasal administration. Flutinex at therapeutic doses does not affect the hypothalamic-pituitary-adrenal system. When fluticasone is sprayed into the nasal mucosa, a portion enters the systemic circulation, and the rest is eliminated by activation of the nasal mucosa and swallowing. Corticosteroids have been shown to have a wide range of effects on various cell types (e.g., eosinophils, basophils, lymphocytes, macrophages, neutrophils) and mediators (histamine, eicosanoids, leukotrienes, and cytokines). Glucocorticoids do not cause unexpected effects on allergy symptoms. Pharmacokinetics The bioavailability of the preparation with intranasal administration is less than 2%. After intranasal treatment in patients with allergic rhinitis for 3 weeks, the plasma concentration level of fluticasone was higher compared to the level of detection (50 mg/ml). Due to low bioavailability with intranasal administration, pharmacokinetic data were obtained by other routes of administration. It was found that a large portion of fluticasone is excreted by plasma, while the absorption rate is low. Fluticasone is characterized by high lipophilicity, and therefore its binding to tissues is quite high. The volume of distribution is 4.2 L/kg. Plasma protein binding is 91%, independent of concentration. A negligible amount of fluticasone binds to human transcortin. Metabolism: Fluticasone is rapidly and completely cleared from the blood (average 1093 ml/min, with renal clearance of 0.02% of the total amount). The only circulating metabolite found in human blood is the 17ß-carboxylic acid derivative of fluticasone, formed with the participation of cytochrome P450 3A4. It exhibits less efficacy than the parent drug. The half-life is 7-8 hours, less than 5% is excreted in urine as metabolites, and the rest is excreted with feces. Indications Prevention and treatment of seasonal allergic rhinitis; prevention and treatment of perennial allergic rhinitis. Dosage and Administration Flutinex is for intranasal use only. For full therapeutic effect, it should be taken regularly. Adults and children over 12 years of age: For the prevention and treatment of seasonal and perennial rhinitis, 100 mcg (2 doses) is administered into each nostril once daily, preferably in the morning. In some cases, 100 mcg (2 doses) into each nostril twice daily is required. The maximum daily dose is 200 mcg/day (4 doses) into each nostril. Elderly patients do not require dose adjustment. Children aged 4-11 years: For the treatment and prevention of seasonal rhinitis, it is recommended to administer 50 mcg (1 dose) into each nostril once daily. The maximum daily dose is 100 mcg (2 doses) into each nostril. Maximum therapeutic effect will be observed after 3-4 days. Before use, the bottle must be shaken carefully. Hold the bottle with the lower part of the spray nozzle between the index and middle fingers, and place the thumb on the bottom of the bottle. When using the preparation for the first time or after a break of 1 week, the spray nozzle must be tested for functionality. After this, the nose should be cleared (gently blown), close one nostril with the index finger of the left hand and spray the preparation into the other, then vice versa. The head should be tilted slightly forward, and the bottle should be held vertically. Inhale through the nose, exhale through the mouth. After use, the spray nozzle should be cleaned with a clean cloth or tissue and the cap should be replaced. Side Effects Local reactions are rare, mainly irritation and dryness of the nasopharynx, unpleasant taste and smell. Contraindications Hypersensitivity to the components of the preparation. Pregnancy and Lactation The safety of Flutinex in pregnant women has not been established to date. Intranasal administration of the preparation minimizes the possibility of systemic effects. Flutinex can be prescribed during pregnancy and lactation only when it is a vital indication for the mother. In experimental studies, fluticasone propionate was not detected in blood plasma after intranasal administration. It is considered that its penetration into breast milk is unlikely. Overdose Acute or chronic symptoms of overdose have not been reported. Upper respiratory tract infections are not a contraindication for the use of Flutinex. Storage Conditions and Expiry Dates Shake before use, store below 25ºC. Store in the original packaging, out of reach of children. Manufacturer, Country: Drogsan İlaç Sanayi. Turkey Turkey