Fluticasone propionate (50mcg per actuation) Aqueous Nasal Spray
Flixonase 24 hour (0.05% w/w) is a white, opaque, aqueous suspension of microfine fluticasone propionate for topical administration to the nasal mucosa by means of a metering, atomising spray pump. Each 100mg of spray delivered by the nasal actuator contains 50 micrograms of fluticasone propionate.
Pharmaceutical form
Nasal spray, suspension
Clinical particulars
Therapeutic Indications
Flixonase 24 hour is indicated for the short term (3-6 months) prevention and treatment of seasonal allergic rhinitis including hayfever. Fluticasone propionate has potent anti-inflammatory activity but when used topically on the nasal mucosa has no detectable systemic activity.
Administration
Flixonase 24 hour is for administration by the intranasal route only.
Adults and children over 12 years of age for the prevention and treatment of seasonal allergic rhinitis including hayfever
Two sprays into each nostril once a day, preferably in the morning. The maximum daily dose should not exceed two sprays into each nostril.
Elderly
The normal adult dosage is applicable.
For full therapeutic benefit regular usage is essential. The absence of an immediate effect should be explained to the patient as maximum relief may not be obtained until after 3 to 4 days of treatment.
Do not use continuously for more than 6 months without consulting your doctor.
Contra-indications
Flixonase 24 hour is contra-indicated in patients with a hypersensitivity to any of its ingredients.
Special warnings and special precautions for use
Local infection: Infections of the nasal airways should be appropriately treated but do not constitute a specific contra-indication to treatment with Flixonase 24 hour.
The full benefit of Flixonase 24 hour may not be achieved until treatment has been administered for several days.
Care must be taken while transferring patients from systemic steroid treatment to Flixonase 24 hour if there is any reason to suppose that their adrenal function is impaired.
Although Flixonase 24 hour will control seasonal allergic rhinitis in most cases, an abnormally heavy challenge of summer allergens may in certain instances necessitate appropriate additional therapy, particularly to control eye symptoms.
Pregnancy and lactation
Pregnancy
There is inadequate evidence of safety in human pregnancy. In animal reproduction studies adverse effects typical of potent corticosteroids are only seen at high systemic exposure levels; direct intranasal application ensures minimal systemic exposure.
However, as with other medicines the use of Flixonase 24 hour during human pregnancy requires that the benefits be weighed against the possible risks associated with the product or with any alternative therapy.
Lactation
The excretion of fluticasone propionate into human breast milk has not been investigated. When measurable plasma levels were obtained in lactating laboratory rats following subcutaneous administration there was evidence of fluticasone propionate in the breast milk. However plasma levels in patients following intranasal application of fluticasone propionate at recommended doses are likely to be low.
Effects on ability to drive and use machines
None reported.
Interaction with other medicaments and other forms of interaction
Care should be taken when co-administering known strong CYP3A4 inhibitors (eg. ketoconazole, ritonavir) as there is a potential for increased systemic exposure to fluticasone propionate.
Undesirable effects
As with other nasal sprays, dryness and irritation of the nose and throat, unpleasant taste and smell, headache and epistaxis have been reported.
Hypersensitivity reactions including skin rash and oedema of the face or tongue have been reported. There have also been rare reports of anaphylaxis/anaphylactic reactions and bronchospasm.
Extremely rare cases of nasal septal perforation have been reported following the use of intranasal corticosteroids.
Overdosage
There are no data available on the effects of acute or chronic overdosage with Flixonase 24 hour. Intranasal administration of 2mg fluticasone propionate twice daily for seven days to healthy human volunteers had no effect on hypothalamic-pituitary-adrenal axis function.
Pharmacological properties
Pharmacodynamic properties
Fluticasone propionate causes little or no hypothalamic-pituitary-adrenal axis suppression following intranasal or topical (dermal) administration, and only causes overt HPA axis suppression after very high oral doses (10mg four times a day - i.e. 40mg daily and above). Plasma fluticasone propionate levels after intranasal doses of up to and including 1mg are low, around the limit of quantitation of the assay (0.05 nanograms/mL).
Pharmacokinetic properties
Following oral administration 87-100% of the dose is excreted in the faeces, up to 75% as unabsorbed parent compound depending on the dose.
After a 6mg oral dose 64% is excreted as the parent substance. There is a non active major metabolite. Following intravenous administration there is high plasma clearance suggestive of extensive hepatic extraction. From limited early data the terminal plasma half-life was estimated at 3 hours and the associated volume of distribution, over 3 times body weight. This is consistent with rapid elimination and extensive tissue distribution.
Pre-clinical safety data
Toxicology has shown only those class effects typical of a potent corticosteroid, and these only at doses greatly in excess of those proposed for therapeutic use. No novel effects were identified in repeat dose toxicity tests, reproductive toxicology studies or teratology studies.
Fluticasone propionate is devoid of mutagenic activity in vitro and in vivo and showed no tumorigenic potential in rodents. It is both non irritant and non sensitising in animal models.
Pharmaceutical particulars
Shake gently before use.
Shelf life
24 months
Storage conditions
Store below 25°C (77°F).
Package quantities
Flixonase 24 hour is supplied in an amber glass bottle fitted with a metering, atomising pump, nasal adaptor and a dust cover. Each bottle provides approximately 120 metered sprays, when used as recommended.
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