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NASONEX ALLERGY DEFENCE 0.05% NASAL SPRAY

Active substance(s): MOMETASONE FUROATE MONOHYDRATE

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SUMMARY OF PRODUCT CHARACTERISTICS

1

NAME OF THE MEDICINAL PRODUCT

NASONEX Allergy Control 0.05% Nasal Spray

2

QUALITATIVE AND QUANTITATIVE COMPOSITION

0.05% mometasone furoate (as the monohydrate). Each 100 mg actuation contains 50
micrograms of mometasone furoate.
Excipient with known effect:
This medicinal product contains 0.02 mg of benzalkonium chloride per actuation.
For the full list of excipients, see section 6.1.

3

PHARMACEUTICAL FORM

Nasal Spray, suspension.
White to off-white opaque suspension.

4

CLINICAL PARTICULARS

4.1

Therapeutic indications

NASONEX Nasal Spray is indicated for use in adults to treat the symptoms of seasonal or
perennial allergic rhinitis.

4.2

Posology and method of administration

After initial priming of the NASONEX Nasal Spray pump, each actuation delivers approximately
100 mg of mometasone furoate suspension, containing mometasone furoate monohydrate
equivalent to 50 micrograms mometasone furoate.
Posology
Seasonal or Perennial Allergic Rhinitis
Adults aged 18 years and over (including older patients): The usual recommended dose is two
actuations (50 micrograms/actuation) in each nostril once daily (total dose 200 micrograms).
Once symptoms are controlled, dose reduction to one actuation in each nostril (total dose
100 micrograms) may be effective for maintenance. Dose reduction is recommended following
control of symptoms.

Children under 18 years of age: Should not be used by children and adolescents under 18 years of
age.
NASONEX Nasal Spray demonstrated a clinically significant onset of action within 12 hours
after the first dose in some patients with seasonal allergic rhinitis; however, full benefit of
treatment may not be achieved in the first 48 hours. Therefore, the patient should continue
regular use to achieve full therapeutic benefit.
Treatment with NASONEX Nasal Spray may need to be initiated some days before the expected
start of the pollen season in patients who have a history of moderate to severe symptoms of
seasonal allergic rhinitis.
Method of administration
Prior to administration of the first dose, shake container well and actuate the pump 10 times (until
a uniform spray is obtained). If the pump is not used for 14 days or longer, reprime the pump
with 2 actuations until a uniform spray is observed, before next use.
Shake container well before each use. The bottle should be discarded after the labelled number
of actuations or within 2 months of first use.
If symptoms have not improved after 14 days medical advice must be sought.

4.3

Contraindications

Hypersensitivity to the active substance, mometasone furoate, or to any of the excipients listed in
section 6.1.
NASONEX Nasal Spray should not be used in the presence of untreated localised infection
involving the nasal mucosa, such as herpes simplex.
Because of the inhibitory effect of corticosteroids on wound healing, patients who have
experienced recent nasal surgery or trauma should not use a nasal corticosteroid until healing has
occurred.

4.4

Special warnings and precautions for use

Treatment should be stopped or the advice of a doctor sought if an improvement is not seen
within 14 days. Advice of a doctor or pharmacist should also be sought if symptoms have
improved but are not adequately controlled. This medicines should not be used continuously for
more than 3 months without consulting a doctor.
Immunosuppression
NASONEX Nasal Spray should be used with caution, if at all, in patients with active or quiescent
tuberculous infections of the respiratory tract, or in untreated fungal, bacterial, or systemic viral
infections.
Patients receiving corticosteroids who are potentially immunosuppressed should be warned of the
risk of exposure to certain infections (e.g., chickenpox, measles) and of the importance of
obtaining medical advice if such exposure occurs.

Local Nasal Effects
Following 12 months of treatment with NASONEX Nasal Spray in a study of patients with
perennial rhinitis, there was no evidence of atrophy of the nasal mucosa; also, mometasone
furoate tended to reverse the nasal mucosa closer to a normal histologic phenotype. Nevertheless,
patients using NASONEX Nasal Spray over several months or longer should be examined
periodically for possible changes in the nasal mucosa. If localised fungal infection of the nose or
pharynx develops, discontinuance of NASONEX Nasal Spray therapy or appropriate treatment
may be required. Persistence of nasopharyngeal irritation may be an indication for discontinuing
NASONEX Nasal Spray.
Nasonex is not recommended in case of nasal septum perforation (see section 4.8).
In clinical studies, epistaxis occurred at a higher incidence compared to placebo. Epistaxis
was generally self-limiting and mild in severity (see section 4.8).
NASONEX Nasal Spray contains benzalkonium chloride which may cause nasal irritation.
Systemic Effects of Corticosteroids
Systemic effects of nasal corticosteroids may occur, particularly at high doses prescribed for
prolonged periods. These effects are much less likely to occur than with oral corticosteroids
and may vary in individual patients and between different corticosteroid preparations.
Potential systemic effects may include Cushing’s syndrome, Cushingoid features, adrenal
suppression, growth retardation in children and adolescents, cataract, glaucoma and more
rarely, a range of psychological or behavioural effects including psychomotor hyperactivity,
sleep disorders, anxiety, depression or aggression (particularly in children).
Following the use of intranasal corticosteroids, instances of increased intraocular pressure have
been reported (see section 4.8).
Patients who are transferred from long-term administration of systemically active corticosteroids
to NASONEX Nasal Spray require careful attention. Systemic corticosteroid withdrawal in such
patients may result in adrenal insufficiency for a number of months until recovery of HPA axis
function. If these patients exhibit signs and symptoms of adrenal insufficiency or symptoms of
withdrawal (e.g., joint and/or muscular pain, lassitude, and depression initially) despite relief
from nasal symptoms, systemic corticosteroid administration should be resumed and other modes
of therapy and appropriate measures instituted. Such transfer may also unmask pre-existing
allergic conditions, such as allergic conjunctivitis and eczema, previously suppressed by systemic
corticosteroid therapy.
Treatment with higher than recommended doses may result in clinically significant adrenal
suppression. If there is evidence for higher than recommended doses being used, then
additional systemic corticosteroid cover should be considered during periods of stress or
elective surgery.
Non-nasal Symptoms
Although NASONEX Nasal Spray will control the nasal symptoms in most patients, the
concomitant use of appropriate additional therapy may provide additional relief of other
symptoms, particularly ocular symptoms.

4.5

Interaction with other medicinal products and other forms of interaction

(See 4.4 Special warnings and special precautions for use with systemic corticosteroids)

A clinical interaction study was conducted with loratadine. No interactions were observed.

4.6

Fertility, pregnancy and lactation

Pregnancy
There are no or limited amount of data from the use of mometasone furoate in pregnant
women. Studies in animals have shown reproductive toxicity (see section 5.3). As with other
nasal corticosteroid preparations, NASONEX Nasal Spray should not be used in pregnancy
unless the potential benefit to the mother justifies any potential risk to the mother, foetus or
infant. Infants born of mothers who received corticosteroids during pregnancy should be
observed carefully for hypoadrenalism.
Lactation
It is unknown whether mometasone furoate is excreted in human milk. As with other nasal
corticosteroid preparations, a decision must be made whether to discontinue breast-feeding or
to discontinue/abstain from NASONEX Nasal Spray therapy taking into account the benefit
of breast feeding for the child and the benefit of therapy for the woman.
Fertility
There are no clinical data concerning the effect of mometasone furoate on fertility. Animal
studies have shown reproductive toxicity, but no effects on fertility (see section 5.3).
The leaflet and label will include a warning that medical opinion should be sought, before using
this medicine, in the case of pregnancy and breastfeeding.

4.7

Effects on ability to drive and use machines

None known.

4.8

Undesirable effects

Summary of the safety profile
Epistaxis was generally self-limiting and mild in severity, and occurred at a higher incidence
compared to placebo (5%), but at a comparable or lower incidence when compared to the active
control nasal corticosteroids studied (up to 15%) as reported in clinical studies for allergic
rhinitis. The incidence of all other adverse events was comparable with that of placebo.
Systemic effects of nasal corticosteroids may occur, particularly when prescribed at high doses
for prolonged periods.
Tabulated list of adverse reactions
Treatment related adverse reactions (≥1%) reported in clinical trials in patients with allergic
rhinitis or nasal polyposis and post-marketing regardless of indication are presented in Table 1.
Adverse reactions are listed according to MedDRA primary system organ class. Within each
system organ class, adverse reactions are ranked by frequency. Frequencies were defined as
follows: Very common (≥1/10); common (≥1/100 to <1/10); uncommon (≥1/1,000 to <1/100).
The frequency of post-marketing adverse events are considered as “not known (cannot be
estimated from the available data)”.

Table 1: Treatment-related adverse reactions reported by system organ class and frequency

Very common
Infections and
infestations

Common
Pharyngitis
Upper respiratory
tract infection†

Immune system
disorders

Hypersensitivity
including
anaphylactic
reactions,
angioedema,
bronchospasm, and
dyspnoea

Nervous system
disorders
Eye disorders

Respiratory, thoracic
and mediastinal
disorders

Gastrointestinal
disorders

Not known

Headache

Epistaxis*

Epistaxis
Nasal burning
Nasal irritation
Nasal ulceration
Throat irritation*

Glaucoma
Increased intraocular
pressure
Cataracts
Nasal septum
perforation

Disturbances of taste
and smell

*recorded for twice daily dosing for nasal polyposis

recorded at uncommon frequency for twice daily dosing for nasal polyposis

Paediatric population
In the paediatric population, the incidence of recorded adverse events in clinical studies, e.g.,
epistaxis (6%), headache (3%), nasal irritation (2%) and sneezing (2%) was comparable to
placebo.
Reporting of suspected adverse reactions
Reporting suspected adverse reactions after authorisation of the medicinal product is
important. It allows continued monitoring of the benefit/risk balance of the medicinal product.
Healthcare professionals are asked to report any suspected adverse reactions via the Yellow
Card Scheme at: www.mhra.gov.uk/yellowcard.

4.9

Overdose

Symptoms
Inhalation or oral administration of excessive doses of corticosteroids may lead to suppression of
HPA axis function.
Management
Because the systemic bioavailability of NASONEX Nasal Spray is <1%, overdose is unlikely to
require any therapy other than observation, followed by initiation of the appropriate prescribed
dosage.

5

PHARMACOLOGICAL PROPERTIES

5.1

Pharmacodynamic properties

Pharmacotherapeutic group: Decongestants and Other Nasal Preparations for Topical UseCorticosteroids, ATC code: R01A D09
Mechanism of action
Mometasone furoate is a topical glucocorticosteroid with local anti-inflammatory properties at
doses that are not systemically active.
It is likely that much of the mechanism for the anti-allergic and anti-inflammatory effects of
mometasone furoate lies in its ability to inhibit the release of mediators of allergic reactions.
Mometasone furoate significantly inhibits the release of leukotrienes from leucocytes of allergic
patients. In cell culture, mometasone furoate demonstrated high potency in inhibition of synthesis
and release of IL-1, IL-5, IL-6 and TNFα; it is also a potent inhibitor of leukotriene production.
In addition, it is an extremely potent inhibitor of the production of the Th2 cytokines, IL-4 and
IL-5, from human CD4+ T-cells.
Pharmacodynamic effects
In studies utilising nasal antigen challenge, NASONEX Nasal Spray has shown antiinflammatory activity in both the early- and late- phase allergic responses. This has been
demonstrated by decreases (vs placebo) in histamine and eosinophil activity and reductions (vs
baseline) in eosinophils, neutrophils, and epithelial cell adhesion proteins.
In 28% of the patients with seasonal allergic rhinitis, NASONEX Nasal Spray demonstrated a
clinically significant onset of action within 12 hours after the first dose. The median (50%) onset
time of relief was 35.9 hours.
Paediatric population
In a placebo-controlled clinical trial in which paediatric patients (n=49/group) were administered
NASONEX Nasal Spray 100 micrograms daily for one year, no reduction in growth velocity
was observed.
There are limited data available on the safety and efficacy of NASONEX Nasal Spray in the
paediatric population aged 3 to 5 years, and an appropriate dosage range cannot be established. In
a study involving 48 children aged 3 to 5 years treated with intranasal mometasone furoate
50, 100 or 200 μg/day for 14 days, there was no significant differences from placebo in the mean
change in plasma cortisol level in response to the tetracosactrin stimulation test.

5.2

Pharmacokinetic properties

Absorption
Mometasone furoate, administered as an aqueous nasal spray, has a systemic bioavailability of
<1% in plasma, using a sensitive assay with a lower quantitation limit of 0.25 pg/ml.

Distribution
Not applicable as mometasone is poorly absorbed via the nasal route.
Biotransformation
The small amount that may be swallowed and absorbed undergoes extensive first-pass hepatic
metabolism.
Elimination
Absorbed mometasone furoate is extensively metabolized and the metabolites are excretedin
urine and bile.

5.3

Preclinical safety data

No toxicological effects unique to mometasone furoate exposure were demonstrated. All
observed effects are typical of this class of compounds and are related to exaggerated
pharmacologic effects of glucocorticoids.
Preclinical studies demonstrate that mometasone furoate is devoid of androgenic, antiandrogenic,
estrogenic or antiestrogenic activity but, like other glucocorticoids, it exhibits some
antiuterotrophic activity and delays vaginal opening in animal models at high oral doses of
56 mg/kg/day and 280 mg/kg/day.
Like other glucocorticoids, mometasone furoate showed a clastogenic potential in-vitro at high
concentrations. However, no mutagenic effects can be expected at therapeutically relevant doses.
In studies of reproductive function, subcutaneous mometasone furoate, at 15 micrograms/kg
prolonged gestation and prolonged and difficult labour occurred with a reduction in offspring
survival and body weight or body weight gain. There was no effect on fertility.
Like other glucocorticoids, mometasone furoate is a teratogen in rodents and rabbits. Effects
noted were umbilical hernia in rats, cleft palate in mice and gallbladder agenesis, umbilical
hernia, and flexed front paws in rabbits. There were also reductions in maternal body weight
gains, effects on foetal growth (lower foetal body weight and/or delayed ossification) in rats,
rabbits and mice, and reduced offspring survival in mice.
The carcinogenicity potential of inhaled mometasone furoate (aerosol with CFC propellant and
surfactant) at concentrations of 0.25 to 2.0 micrograms/l was investigated in 24-month studies in
mice and rats. Typical glucocorticoid-related effects, including several non-neoplastic lesions,
were observed. No statistically significant dose-response relationship was detected for any of the
tumour types.

6

PHARMACEUTICAL PARTICULARS

6.1

List of excipients

Dispersable cellulose (microcrystalline cellulose and carmellose sodium)
Glycerol
Sodium citrate
Citric acid monohydrate
Polysorbate 80
Benzalkonium chloride
Purified water

6.2

Incompatibilities

Not applicable

6.3

Shelf life

3 years
Use within 2 months of first use.

6.4

Special precautions for storage

Do not store above 25°C. Do not freeze.

6.5

Nature and contents of container

NASONEX Nasal Spray is contained in a white, high density polyethylene bottle, that
contains 10 g (60 actuations) or 18 g (140 actuations) of product formulation, supplied with a
metered dose, manual polypropylene spray pump actuator.
Pack sizes:

10g, 1 bottle
18g, 1 bottle

Not all pack sizes may be marketed.

6.6

Special precautions for disposal

Any unused medicinal product or waste material should be disposed of in accordance with
local requirements.

7

MARKETING AUTHORISATION HOLDER

Bayer plc
Bayer House
Strawberry Hill
Newbury, Berkshire
RG14 1JA
Trading as Bayer plc, Consumer Care Division

8

MARKETING AUTHORISATION NUMBER(S)

PL 00010/0663

9

DATE OF FIRST AUTHORISATION/RENEWAL OF THE
AUTHORISATION
10/07/2017

10

DATE OF REVISION OF THE TEXT
10/07/2017

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