Each spray delivers: Fluticasone propionate BP 50 mcg (0.05% w/w).
Excipient/Inactive Ingredient: Benzalkonium chloride BP 0.05% w/w q.s.
Fluticasone propionate is a synthetic corticosteroid having the chemical name S-(fluoromethyl) 6α,9-difluoro-11β-17-dihydroxy-16α-methyl-3-oxoandrosta-1,4-diene-17β-carbothioate,17-propionate.
Fluticasone propionate is a white powder with a molecular weight of 500.6, and the empirical formula is C25H31O5S. It is practically insoluble in water, freely soluble in dimethyl sulfoxide and dimethylformamide, and slightly soluble in methanol and 95% ethanol.
Pharmacology: Mechanism of Action: Fluticasone propionate is a synthetic trifluorinated corticosteroid with anti-inflammatory activity. Fluticasone propionate was 3-fold to 5-fold more potent than dexamethasone in assays.
The precise mechanism through which fluticasone propionate affects allergic rhinitis symptoms is not known. Corticosteroids have been shown to have a wide range of effects on multiple cell types (e.g. mast cells, eosinophils, neutrophils, macrophages, and lymphocytes) ad mediators (eg, histamine, eicosanoids, leukotrienes, and cytokines) involved in inflammation. FLUTICASONE PROPIONATE Nasal Spray, like other corticosteroids, is an agent that does not have an immediate effect on allergic symptoms. A decrease in nasal symptoms has been noted in some patients 12 hours after initial treatment with FLUTICASONE PROPIONATE Nasal Spray. Maximum benefit may not be reached for several days. Similarly, when corticosteroids are discontinued, symptoms may not return for several days.
Pharmacokinetics: Absorption: The activity of FLUTICASONE PROPIONATE Nasal Spray is due to the parent drug, fluticasone propionate. Indirect route has an absolute bioavailability averaging less than 2%. After intranasal treatment of patients with allergic rhinitis for 3 weeks, fluticasone propionate plasma concentrations were above the level of detection (50 pg/mL) only when recommended doses were exceeded and then only in occasional samples at low plasma levels. Due to the low bioavailability by the intranasal route, the majority of pharmacokinetic data was obtained via other routes of administration.
Distribution: The volume of distribution averaged 4.2 L/kg following i.v administration. The percentage of fluticasone propionate bound to human plasma proteins averaged 91% with no obvious concentration relationship.
Metabolism: The total blood clearance of fluticasone propionate is high.
Elimination: Following intravenous dosing, fluticasone propionate showed polyexponential kinetics and had a terminal elimination half-life of approximately 7.8 hours.
Special Populations: Fluticasone propionate nasal spray was not studied in any special populations, and no gender-specific pharmacokinetic data have been obtained.
Drug Interactions: Fluticasone propionate is a substrate of cytochrome P450 3A4. Caution should be exercised when other potent cytochrome P450 3A4 inhibitors are coadministered with fluticasone propionate.
Individualization of Dosage: Patients should use FLUTICASONE PROPIONATE Nasal Spray at regular intervals for optimal effect.
FLUTICASONE PROPIONATE (FLUSORT) Nasal Spray is indicated for the management of the nasal symptoms of seasonal and perennial allergic and nonallergic rhinitis in adults and pediatric patients 4 years of age or older.
Safety and effectiveness of FLUSORT Nasal Spray in children below 4 years of age have not been adequately established.
Patients should use FLUTICASONE PROPIONATE Nasal Spray at regular intervals for optimal effect.
Adults: The recommended starting dosage in adults is 2 sprays (50 mcg of fluticasone propionate each) in each nostril once daily (total daily dose, 200 mcg).
The same dosage divided into 100 mcg given twice daily (eg, 8 am and 8 pm) is also effective. After the first few days, patients may be able to reduce their dosage to 100 mcg (1 spray in each nostril) once daily for maintenance therapy. Some patients (12 years of age and older) with seasonal allergic rhinitis may find as needed use of 200 mcg once daily effective for symptom control. Greater symptom control may be achieved with scheduled regular use.
Adolescents and Children (4 Years of Age and Older): Patients should be started with 100 mcg (1 spray in each nostril once daily). Patients not adequately responding to 100 mcg may use 200 mcg (2 sprays in each nostril). Once adequate control is achieved, the dosage should be decreased to 100 mcg (1 spray in each nostril) daily.
The maximum total daily dosage should not exceed 2 sprays in each nostril (200 mcg/day).
FLUTICASONE PROPIONATE Nasal Spray is not recommended for children under 4 years of age.
Shake gently before use.
Route of Administration: Nasal.
FLUTICASONE PROPIONATE (FLUSORT) Nasal Spray is contraindicated in patients with a hypersensitivity to any of its ingredients.
The replacement of a systemic corticosteroid with a topical corticosteroid can be accompanied by signs of adrenal insufficiency, and in addition, some patients may experience symptoms of withdrawal, eg, joint ad/or muscular pain, lassitude, and depression. Patients previously treated for prolonged periods with systemic corticosteroids and transferred to topical corticosteroids should be carefully monitored for acute adrenal insufficiency in response to stress. In those patients who have asthma or other clinical conditions requiring long-term systemic corticosteroid treatment, too rapid a decrease in systemic corticosteroids may cause a severe exacerbation of their symptoms.
The concomitant use of intranasal corticosteroids with other inhaled corticosteroids could increase the risk of signs or symptoms of hypercorticism and/or suppression of the HPA axis.
Avoid spraying in eyes.
General: Intranasal corticosteroids may cause a reduction in growth velocity when administered to pediatric patients.
Use of excessive doses of corticosteroids may lead to signs or symptoms of hypercorticism and/or suppression of HPA function.
Although systemic effects have been minimal with recommended doses of FLUTICASONE PROPIONATE Nasal Spray, potential risk increases with larger doses. Therefore, larger than recommended doses of FLUTICASONE PROPIONATE Nasal Spray should be avoided.
Carcinogenesis, Mutagenesis, Impairment of Fertility: Fluticasone propionate demonstrated no tumorigenic potential in mice. Fluticasone propionate did not induce gene mutation in prokaryotic or eukaryotic cells in vitro. No significant clastogenic effect was seen in cultured human peripheral lymphocytes in vitro or in the mouse micronucleus test.
No evidence of impairment of fertility was observed in reproductive studies conducted in male and female.
Use in pregnancy: Teratogenic Effects: Pregnancy Category C.
There are no adequate and well-controlled studies in pregnant women.
Fluticasone propionate should be used during pregnancy only if the potential benefit justifies the potential risk to fetus.
Use in lactation: It is not known whether fluticasone propionate is excreted in human breastmilk.
Use in children: The potential for FLUTICASONE PROPIONATE Nasal Spray to cause growth suppression in susceptible patients or when given at higher doses cannot be ruled out.
In general, adverse reactions in clinical studies have been primarily associated with irritation of the nasal mucous membranes.
Hypersensitivity reactions, including angioedema, skin rash, edema of the face and tongue, pruritus, urticaria, bronchospasm, wheezing, dyspnea and anaphylaxis/anaphylactoid reactions, which in rare instances were severe.
Ear, Nose, and Throat:
Alteration or loss of sense of taste and/or smell and, rarely, nasal septal perforation, nasal ulcer, sore throat, throat irritation and dryness, cough, hoarseness, and voice changes.
Dryness and irritation, conjunctivitis, blurred vision, glaucoma, increased intraocular pressure, and cataracts.
Store at temperatures not exceeding 30°C. Do not freeze.
R01AD08 - fluticasone ; Belongs to the class of topical corticosteroids used for prophylaxis and treatment of allergic rhinitis.
Nasal spray 50 mcg/actuation x 120 actuations.