FLUTICON
Each spray delivers:
Fluticasone Propionate IP 50 mcg
COMPOSITION
Fluticasone Propionate IP 0.05% w/v
Benzalkonium Chloride Solution BP 0.02 % v/v (as preservative)
DESCRIPTION
A white to off-white colored homogenous re-dispersible suspension.
PHARMACODYNAMIC
Pharmacotherapeutic group: Decongestants and Other Nasal Preparations for Topical Use-Corticosteroids.
ATC code: R01AD08
Mechanism of action
Fluticasone propionate causes little or no hypothalamic-pituitary-adrenal axis suppression following intranasal administration.
Following intranasal dosing of fluticasone propionate, (200mcg/day) no significant change in 24h serum cortisol AUC was found compared to placebo (ratio1.01, 90%CI 0.9-1.14).
In a 1-year randomized, double-blind, placebo-controlled, parallel group growth study in pre-pubescent children aged 3 to 9 years (56 patients receiving intranasal fluticasone propionate and 52 receiving placebo) no statistically significant difference in growth velocity was observed in patients receiving intranasal fluticasone propionate (200 micrograms per day nasal spray) compared to placebo. The estimated growth velocity over one year of treatment was 6.20 cm/year (SE=0.23) in the placebo group and 5.99 cm/year (SE=0.23) in the fluticasone propionate group; the mean difference between treatments in growth velocity after one year was 0.20 cm/year (SE=0.28, 95% CI= -0.35, 0.76). No evidence of clinically relevant changes in HPA axis function or bone mineral density was observed as assessed by 12-hour urinary cortisol excretion and dual-energy x-ray absorptiometry, respectively.
PHARMACOKINETICS
Absorption
Following intranasal dosing of fluticasone propionate, (200mcg/day) steady-state maximum plasma concentrations were not quantifiable in most subjects (<0.01ng/mL). The highest Cmax observed was 0.017ng/mL. Direct absorption in the nose is negligible due to the low aqueous solubility with the majority of the dose being eventually swallowed. When administered orally the systemic exposure is <1% due to poor absorption and pre-systemic metabolism. The total systemic absorption arising from both nasal and oral absorption of the swallowed dose is therefore negligible.
Distribution
Fluticasone propionate has a large volume of distribution at steady-state (approximately 318L). Plasma protein binding is moderately high (91%).
Biotransformation
Fluticasone propionate is cleared rapidly from the systemic circulation, principally by hepatic metabolism to an inactive carboxylic acid metabolite, by the cytochrome P450 enzyme CYP3A4. Swallowed fluticasone propionate is also subject to extensive first pass metabolism. Care should be taken when co-administering potent CYP3A4 inhibitors such as ketoconazole and ritonavir as there is potential for increased systemic exposure to fluticasone propionate.
Elimination
The elimination rate of intravenous administered fluticasone propionate is linear over the 250-1000mcg dose range and are characterized by a high plasma clearance (CL=1.1L/min). Peak plasma concentrations are reduced by approximately 98% within 3-4 hours and only low plasma concentrations were associated with the 7.8h terminal half-life. The renal clearance of fluticasone propionate is negligible (<0.2%) and less than 5% as the carboxylic acid metabolite. The major route of elimination is the excretion of fluticasone propionate and its metabolites in the bile.
THERAPEUTIC INDICATION
Fluticasone Nasal Spray is indicated for the management of the nasal symptoms of seasonal perennial allergic and non-allergic rhinitis patients aged 4 years and older.
DOSAGE AND ADMINISTRATION
Adults and Adolescents (>12 years)
Initially, two sprays in each nostril once daily or one spray in each nostril twice daily. Once the symptom has been controlled reducing the dosage to one spray in each nostril once daily may be effective. Some patients with seasonal allergic rhinitis may find as-needed use of Fluticasone Propionate nasal spray (not to exceed 200 mcg daily) effective for symptom control. However, greater symptom control may be achieved with scheduled regular use.
Children (4-11 years)
Initially, treatment should be started with one spray in each nostril once daily. If the desired effects are not observed the dosage may be increased to two sprays in each nostril once daily. It is not recommended for use in children bellow 4 years.
INSTRUCTION FOR USE
Apply FLUTICON Nasal Spray in the following way:
- Shake the bottle well before using the nasal spray.
- Blow your nose gently.
- Remove the dust cap of the bottle and keep its tip between your index finger and middle finger with thumb at the bottom.
- If you are using this nasal spray for the first time or have not used it for a week or more, then examine it by spraying it, away from you in the air, few times until a fine mist appears.
- To use the spray, tilt your head forward slightly while breathing out.
- Carefully insert the nozzle tip into one of the nostrils.
- Remember to point the nozzle tip towards the corner of your eye or ear and not towards the center of your nose.
- Press down with your fingers once to release a spray.
- Pull out the nozzle tip from the nostril.
- Close the other nostril with your finger and breathe slowly through your nose and exhale slowly through mouth.
- If you have been prescribed the second dose in the same nostril, wait a minute or two and repeat the process.
- Repeat STEPS 5 through 10 for the other nostril.
- After use, wipe the nozzle with a clean handkerchief or tissue and replace the dust cap.
- Do not blow your nose for few minutes after using the spray.
- Use the nasal spray as per your doctor’s recommendation and do not exceed the dose.
CONTRAINDICATION
FLUTICON aqueous nasal spray is contradicted in patients with a hypersensitivity to any of its ingredients.
WARNING AND PRECAUTIONS
In 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 replacement of a systemic corticosteroid with a topical corticosteroid can be accompanied by signs of adrenal insufficiency and, in addition, some patients any experience symptoms of withdrawal, e.g. joint and/ or muscular pain, lassitude, and depression. Avoid spraying into eye.
DRUG INTERACTION
Fluticasone propionate is a substrate of cytochrome P450 3A4. Co-administration of fluticasone propionate and the highly potent cytochrome P450 3A4 inhibitor, ritonavir, is not recommended. The concomitant use of intranasal corticosteroids with other inhaled corticosteroids with another inhaled corticosteroid could increase the risk of signs or symptoms of hypercorticism and/or suppression of the HPA axis.
PREGNANCY, LACTATION & PAEDIATRIC
Pregnancy
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 the foetus.
Lactation
It is not known whether fluticasone propionate is excreted in human breast milk. Since there are no data from controlled trials on the use of intranasal fluticasone propionate by nursing mothers, caution should be exercised when administered to a nursing mother.
Paediatric Use
Intranasal corticosteroids may cause a reduction in growth velocity when administered to paediatric patients in higher dose.
UNDESIRABLE EFFECTS
The most commonly reported side effects are headache, pharyngitis, epistaxis, nasal burning/irritation. Other adverse events include alteration or loss of sense of taste and/ or smell and, rarely, nasal ulcer, cough, hoarseness, and voice changes.
If you experience any side effect, talk to your doctor or pharmacist.
PRESENTATION
FLUTICON Nasal Spray are supplied in 10 ml sterilized container containing 100 metered doses.
STORAGE AND OTHER INFORMATION
Store at temperature below 30 °C. Keep this medicine out of the sight and reach of children. Do not touch the spray tip or other dispensing tip to any surface since this may contaminate the solution.