Fluticasone propionate (50mcg
per actuation) Aqueous Nasal Spray
Qualitative and quantitative
composition
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 degrees
C.
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.
Medicines
classification
Pharmacist Only
Medicine
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