Consumer medicine information

Nasonex Aqueous Nasal Spray 0.05%

Mometasone furoate

BRAND INFORMATION

Brand name

Nasonex Aqueous Nasal Spray 0.05% Alcohol Free

Active ingredient

Mometasone furoate

Schedule

S4

 

Consumer medicine information (CMI) leaflet

Please read this leaflet carefully before you start using Nasonex Aqueous Nasal Spray 0.05%.

What is in this leaflet

This leaflet answers some common questions about NASONEX. It does not contain all the available information.

It does not take the place of talking to your doctor or pharmacist.

All medicines have risks and benefits. Your doctor has weighed the risks of you using this medicine against the benefits they expect it will have for you.

If you have any concerns about taking this medicine, ask your doctor or pharmacist.

Keep this leaflet with the medicine. You may need to read it again.

What NASONEX is used for

NASONEX contains the active ingredient mometasone furoate. This belongs to a family of medicines called corticosteroids, which are used to help reduce inflammation.

Allergic Rhinitis (hayfever):
NASONEX is sprayed into the nose to help relieve symptoms that may occur with hayfever or other year-round allergies, including stuffiness (congestion) in the nose, discharge, itching and sneezing. Your doctor may also prescribe this medicine to help prevent these symptoms two to four weeks before the beginning of the pollen season.

Nasal Polyps:
Swollen tissue in the nose can cause grape-like swellings called 'polyps'. Polyps can cause nasal stuffiness, discomfort and loss of smell.

NASONEX can be used for the treatment of nasal polyps in patients over 18 years of age.

Acute Rhinosinusitis:
Rhinosinusitis is the swelling of the sinuses resulting in stuffiness of the nose, large quantities of mucus from the nose, cough, face pain and/or fever. These symptoms usually last for less than 4 weeks. NASONEX is used to treat the symptoms of rhinosinusitis in adults and children 12 years of age and older, who do not have the signs or symptoms of a severe bacterial infection.

Your doctor may have prescribed it for another reason. Ask your doctor if you have any questions about why this medicine has been prescribed for you.

There is no evidence that this medicine is addictive.

This medicine is available only with a doctor's prescription.

Before you use NASONEX

When you must not use it

Do not use the medicine if:

  1. You have an allergy to:
  • any medicine containing mometasone furoate
  • any of the ingredients listed at the end of this leaflet.
  1. You have a tendency to bleed or recurrent nose bleeding
  2. You have severe nose infection, especially fungal infection.
  3. You have had recent nose injury or nose surgery; check with your doctor, because you may be told to wait until healing has occurred before using this medicine.

Do not use it after the expiry date (EXP) printed on the pack or if the packaging is torn or shows sign of tampering.

If you are not sure whether you should start taking this medicine, contact your doctor.

Before you start to use it

Tell your doctor or pharmacist if you have or have had any medical conditions, especially the following:

  • a history of tuberculosis, or active tuberculosis
  • infection of the nose, sinus, mouth, throat, lungs or eye
  • sores in the nose
  • recent injury or surgery to your nose
  • open sores in your nose

Tell your doctor or pharmacist if you are taking other corticosteroid medicines, either by mouth, as eye drops, as an asthma inhaler or by injection.

Tell your doctor or pharmacist if you have allergies to:

  • any other medicines
  • any other substances, such as foods, preservatives or dyes

Tell your doctor if you are pregnant or intend to become pregnant Your doctor will discuss the possible risks and benefits of using this medicine during pregnancy.

Tell your doctor if you are breastfeeding or plan to breastfeed. Breastfeeding is not recommended during treatment with this medicine.

If you have not told your doctor about any of the above, tell them before you use this medicine.

Taking other medicines

Tell your doctor if you are taking any other medicines, including any that you buy without a prescription from your pharmacy, supermarket or health food shop.

Some medicines and NASONEX may interfere with each other. These include:

  • Certain antifungals such as ketoconazole and itraconazole
  • Some antibiotics such as clarithromycin
  • Some medicines used to treat HIV infection such as ritonavir and cobcistat-containing products.

How to use NASONEX

Follow all directions given to you by your doctor or pharmacist carefully and do not use more than the recommended dose. These directions may differ from the information contained in this leaflet.

If you do not understand the instructions, ask your doctor or pharmacist for help

How much to use

Hayfever and allergies in adults (including the elderly) and children 12 years of age and older:
Two sprays into each nostril once daily.

Children 3 to 11 years of age:
One spray into each nostril once daily.

Each actuation of the spray pump delivers the equivalent of 50 microgram of mometasone furoate. The volume of the containers are sufficient to deliver the labelled 65 sprays, or 140 sprays.

When your symptoms have been controlled, your doctor may recommend one spray into each nostril once daily to keep your symptoms under control.

Your doctor may change this dosage, depending on your response to this medicine.

Nasal Polyps in patients (including the elderly) 18 years of age and older:
Two sprays into each nostril once daily. If your symptoms are not controlled, your doctor may increase your dose to two sprays into each nostril twice daily.

When your symptoms have been controlled, your doctor may reduce your dose.

Acute rhinosinusitis in adults and children 12 years of age and older:
Two sprays in each nostril two times a day.

If symptoms worsen during treatment, see your doctor immediately.

About your nasal spray

Your nasal spray has a dust cap which protects the nozzle and keeps it clean. Remember to take this off before using the spray and to replace it after use.

Do not pierce the nasal applicator.

If you are using the spray for the first time, prime the pump by pumping the spray 10 times until a fine mist is produced. If you have not used the pump for 14 days or more reprime by pumping 2 times.

It is important to clean the nozzle regularly; otherwise, it may not work properly. Remove the dust cap and gently pull off the nozzle. Wash the nozzle and dust cap in warm water and then rinse under a running tap.

Do not try to unblock the nasal applicator by inserting a pin or other sharp object as this will damage the applicator and cause you not to get the right dose of medicine.

Allow the nozzle to dry. Push the nozzle back onto the bottle and replace the dust cap. The pump will need to be reprimed when first used after cleaning.

How to use it

  1. Shake the bottle gently and remove the dust cap.
  2. Gently blow your nose.
  3. Close one nostril and put the nozzle into the other nostril.
  4. Tilt your head forward slightly, keeping the bottle upright.
  5. Start to breathe in gently or slowly through your nose and whilst you are breathing in squirt a spray of fine mist into your nose by pressing down ONCE with your fingers.
  6. Breathe out through your mouth. Repeat step 5 to inhale a second spray in the same nostril.
  7. Remove the nozzle from this nostril and breathe out through the mouth.
  8. Repeat steps 3 to 7 for the other nostril. After using the spray, wipe the nozzle carefully with a clean tissue and replace the dust cap.

When to use it

As instructed by your doctor. Do not use more frequently than instructed.

How long to use it

Your doctor will determine the length of treatment.

If you forget to use it

If it is almost time for your next dose, skip the dose you missed and use your next dose when you are meant to.

Otherwise, use it as soon as you remember, and then go back to use your medicines as you would normally.

Do not use a double dose to make up for the dose you missed.

If you are not sure what to do, ask your doctor or pharmacist.

If you take too much (overdose)

Immediately telephone your doctor or the Australian Poisons Information Centre on 13 11 26 if you think you or anyone else may have used too much of this medicine. Do this even if there are no signs of discomfort or poisoning.

Keep telephone numbers for these places handy.

While you are using NASONEX

Things you must do

If you become pregnant while you are using this medicine tell your doctor.

Tell any other doctors, dentists and pharmacists who are treating you that you are using this medicine.

If you are about to be started on any new medicine, tell your doctor, dentist or pharmacist that you are using this medicine.

If you are going to have surgery, tell the surgeon or anaesthetist that you are using this medicine.

See your doctor immediately if you notice the symptoms of severe bacterial infection. These symptoms may include fever, persistent face/tooth pain on one side of the face, swelling around the eye area, or worsening of symptoms after an initial improvement.

Things you must not do

Do not give this medicine to anyone else, even if they have the same condition as you.

Do not use it to treat any other complaints unless your doctor tells you to.

Things to be careful of

This medicine generally does not cause any problems with your ability to drive a car or operate machinery.

If you have a lower resistance to infection, avoid coming into contact with anyone who has measles or chickenpox especially while you are using cortisone-type medicines. Tell your doctor if you do.

Side effects

Tell your doctor or pharmacist as soon as possible if you do not feel well while you are using this medicine. The doctor will decide whether any change in your treatment is needed.

This medicine helps most people, but it may have unwanted side effects in a few people.

All medicines can have side effects. Sometimes they are serious, most of the time they are not. You may need medical treatment if you get some of the side effects. If you are over 65 years of age, you may have an increased chance of getting side effects.

Ask your doctor or pharmacist to answer any questions you may have.

Most people do not have any problems after using the nasal spray. However, a few people may find that they suffer from one or more of the following:

  • headache
  • sneezing
  • nosebleeds or blood-tinged mucus
  • sore throat or burning or irritation inside the nose after using this medicine. These symptoms are consistent with the use of corticosteroid nasal sprays.
  • visual disturbances or blurred vision
  • cataracts have been reported with the use of corticosteroid nasal sprays

If you develop a rash, wheezing or breathlessness, stop using the nasal spray, as you may be allergic to it and contact your doctor immediately.

Other side effects not listed above may also occur in some patients. Tell your doctor if you notice anything that is making you feel unwell.

Long-term use of corticosteroid sprays may be associated with other side effects. Your doctor will monitor your health if you are using NASONEX for extended periods of time.

Do not be alarmed by this list of possible side effects. You may not experience any of them.

After using NASONEX

Storage

Keep the nasal spray in a cool dry place where the temperature stays below 25°C. Do not freeze. Store it away from heat.

Do not store it or any other medicine in the bathroom or near a sink. Do not leave it in the car or on windowsills. Heat and dampness can destroy some medicines.

Keep it where children cannot reach.

Disposal

If your doctor tells you to stop using this medicine or it has passed the expiry date, ask your pharmacist what to do with any that is left over.

Further information

Drug testing for sport events:
This product is a corticosteroid for intranasal administration; it is not a restricted drug for sports.

Corticosteroid may be detected in blood and in the urine during drug testing; thus prior written permission for its use may be required by some sport agencies.

Product description

What it looks like

The nasal spray is a white to off-white suspension contained in a plastic bottle with a metered-dose, manual spray pump for intranasal administration.

Ingredients

Active ingredient:
Mometasone furoate monohydrate

Inactive ingredients:
Dispersible cellulose, glycerol, citric acid monohydrate (or anhydrous citric acid), sodium citrate, polysorbate 80 and purified water

Preservatives:
Benzalkonium chloride

Sponsor

Organon Pharma Pty Ltd
Building A, 26 Talavera Road
Macquarie Park NSW 2113
AUSTRALIA

Australian Registration Number

2 x 140 metered dose bottles per pack

140 metered doses per pack

65 metered doses per pack (Junior Pack)

NASONEX: AUST R 77112

Date of Preparation

16 February 2021

S-CCDS-MK0887-NS-082017

Published by MIMS April 2021

BRAND INFORMATION

Brand name

Nasonex Aqueous Nasal Spray 0.05% Alcohol Free

Active ingredient

Mometasone furoate

Schedule

S4

 

1 Name of Medicine

Mometasone furoate (as monohydrate).

2 Qualitative and Quantitative Composition

Nasonex Aqueous Nasal Spray 0.05% is a metered-dose, manual pump spray unit containing a suspension of mometasone furoate. Each actuation delivers approximately 100 mg of mometasone furoate monohydrate suspension, containing mometasone furoate monohydrate equivalent to mometasone furoate 50 micrograms.
Nasonex Aqueous Nasal Spray 0.05% contains mometasone furoate 0.5 mg/g (as the monohydrate).
For the full list of excipients, see Section 6.1 List of Excipients.

3 Pharmaceutical Form

Nasal Spray, suspension.
Nasonex Aqueous Nasal Spray 0.05% does not contain fluorocarbon propellants.

4 Clinical Particulars

4.1 Therapeutic Indications

Nasonex Aqueous Nasal Spray 0.05% is indicated for the treatment of symptoms associated with seasonal allergic rhinitis and perennial allergic rhinitis and the prophylaxis of seasonal allergic rhinitis in adults, adolescents and children between the ages of 3 and 11 years.
Nasonex Aqueous Nasal Spray 0.05% is also indicated for the treatment of nasal polyps in adult patients 18 years of age and older.
Nasonex Aqueous Nasal Spray 0.05% is indicated for the treatment of symptoms associated with acute rhinosinusitis in patients 12 years of age and older without signs or symptoms of severe bacterial infection.

4.2 Dose and Method of Administration

Do not exceed the recommended dosage.
The effect of Nasonex Aqueous Nasal Spray 0.05% is not immediate. Full therapeutic benefit takes a few days to develop. Dosage should be administered as directed and not be taken by the patients at will for symptomatic relief.
Administration to young children should be aided by an adult.

Allergic rhinitis.

In patients who have a history of moderate to severe symptoms of seasonal allergic rhinitis, prophylactic treatment with Nasonex Aqueous Nasal Spray 0.05% is recommended two to four weeks prior to the anticipated start of the pollen season.

Adults (including geriatric patients) and children 12 years of age and over.

The usual recommended dose for prophylaxis and treatment is two sprays (50 microgram/spray) in each nostril once daily (total daily dose 200 microgram). Once symptoms are controlled, reducing the dose to one spray in each nostril (total daily dose 100 microgram) may be effective for maintenance.
After the first dose of Nasonex Aqueous Nasal Spray 0.05%, clinically significant improvement of symptoms was achieved within 12 hours in 28% of a group of patients (n = 190) with seasonal allergic rhinitis (median = 36 hours). However, the 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.

Children between the ages of 3 and 11 years.

The usual recommended dose is one spray (50 microgram/spray) in each nostril once daily (total daily dose 100 microgram).

Nasal polyposis.

Adults (including geriatric patients) and adolescents 18 years of age and older.

The usual recommended dose for polyposis is two sprays (50 microgram/spray) in each nostril once daily (total daily dose of 200 microgram). If symptoms are inadequately controlled, the dose may be increased to a daily dose of two sprays in each nostril twice daily (total daily dose of 400 microgram). Dose reduction is recommended following control of symptoms.

Acute rhinosinusitis.

The usual recommended dose for acute rhinosinusitis is two sprays (50 micrograms/spray) in each nostril twice daily (total daily dose of 400 micrograms). If no improvement is seen after 15 days of twice daily administration, alternative therapies should be considered. If symptoms worsen during treatment, the patients should be advised to consult their physician.

Instructions to patients.

Shake container well before each use. Do not pierce the nasal applicator. After the initial priming of the Nasonex Aqueous Nasal Spray 0.05% pump (10 actuations, until a uniform spray is observed), each actuation delivers approximately 100 mg of mometasone furoate suspension, containing mometasone furoate monohydrate equivalent to 50 microgram of mometasone furoate. If the spray pump has not been used for 14 days or longer, it should be reprimed with 2 actuations, until a uniform spray is observed, before the next use.

Cleaning your nasal spray.

It is important to clean your nasal spray regularly, otherwise it may not work properly. Remove the dust cap and gently pull off the nozzle. Wash the nozzle and dust cap in warm water and then rinse under a running tap. Do not try to unblock the nasal applicator by inserting a pin or other sharp object as this will damage the applicator and cause you not to get the right dose of medicine. Allow to dry in a warm place. Push the nozzle back onto the bottle and replace the dust cap. The spray will need to be re-primed with 2 sprays when first used after cleaning.

4.3 Contraindications

Patients with known hypersensitivity to mometasone furoate or any of the excipients.
Severe nasal infection, especially candidiasis.
Persons with haemorrhagic diathesis or with a history of recurrent nasal bleeding.

4.4 Special Warnings and Precautions for Use

Local nasal effects.

Nasonex Aqueous Nasal Spray 0.05% should not be used in the presence of untreated localised infection involving the nasal mucosa.
Following 12 months of treatment with Nasonex Aqueous Nasal Spray 0.05%, there was no evidence of atrophy of the nasal mucosa. Mometasone furoate tended to reverse the nasal mucosa closer to a normal histological phenotype. As with any long-term treatment, patients using Nasonex Aqueous Nasal Spray 0.05% 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 Aqueous Nasal Spray 0.05% therapy or appropriate treatment may be required. Persistence of nasopharyngeal irritation may be an indication for discontinuing Nasonex Aqueous Nasal Spray 0.05%.
Following the use of intranasal aerosolised corticosteroids, instances of nasal septum perforation have been reported very rarely.

Recent surgery or trauma.

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.

Immunosuppression.

Nasonex Aqueous Nasal Spray 0.05% 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, systemic viral infections or ocular herpes simplex.
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.

Systemic effects of corticosteroids.

Topical corticosteroids may be absorbed in amounts that can have systemic effects. Use of excessive doses may suppress hypothalamic-pituitary-adrenal (HPA) function. Physicians should be alert for evidence of systemic effects, especially in chronically treated patients.
However, there is no evidence of HPA axis suppression following prolonged treatment with Nasonex Aqueous Nasal Spray 0.05%. Patients who are transferred from long-term administration of systemically active corticosteroids to Nasonex Aqueous Nasal Spray 0.05% 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, systemic corticosteroid administration should be resumed and other modes of therapy and appropriate measures instituted.
Following the use of intranasal aerosolised corticosteroids, increased intraocular pressure has been reported very rarely.
During transfer from systemic corticosteroids to Nasonex Aqueous Nasal Spray 0.05%, some patients may experience symptoms of withdrawal from systemically active corticosteroids (e.g. joint and/or muscular pain, lassitude, and depression initially) despite relief from nasal symptoms and will require encouragement to continue Nasonex Aqueous Nasal Spray 0.05% therapy. Such transfer may also unmask pre-existing allergic conditions such as allergic conjunctivitis and eczema, previously suppressed by systemic corticosteroid therapy.

Visual disturbance.

Visual disturbance may be reported with systemic and topical (including, intranasal, inhaled and intraocular) corticosteroid use. If a patient presents with symptoms such as blurred vision or other visual disturbances, the patient should be considered for referral to an ophthalmologist for evaluation of possible causes of visual disturbances which may include cataract, glaucoma or rare diseases such as central serous chorioretinopathy (CSCR) which have been reported after use of systemic and topical corticosteroids.

Use in acute rhinosinusitis.

If signs or symptoms of severe bacterial infection are observed (such as fever, persistent severe unilateral facial/tooth pain, orbital or peri-orbital facial swelling, or worsening of symptoms after an initial improvement), the patient should be advised to consult their physician immediately. If these signs and symptoms are present at the time of diagnosis, treatment with Nasonex should not be initiated.

Use in the elderly.

None identified.

Paediatric use.

Controlled clinical trials have shown that intranasal corticosteroids may cause a reduction in growth velocity in children. This effect has been observed in the absence of laboratory evidence of HPA axis suppression, suggesting that growth velocity is a more sensitive indicator of systemic corticosteroid exposure in children than some commonly used tests of HPA axis function. The long-term effects of this reduction in growth velocity associated with intranasal corticosteroids, including the impact on final adult height, are unknown. The potential for "catch up" growth following discontinuation of treatment with intranasal corticosteroids has not been adequately studied.
Safety and efficacy of Nasonex Aqueous Nasal Spray 0.05% for the treatment of nasal polyposis in children and adolescents less than 18 years of age have not been studied.
Safety and efficacy of Nasonex Aqueous Nasal Spray 0.05% for the treatment of symptoms of acute rhinosinusitis in children under 12 years of age have not been studied.
The growth of children receiving intranasal corticosteroids should be monitored routinely (e.g. via stadiometry). The potential growth effects of prolonged treatment should be weighed against the clinical benefits and the availability of safe and effective non-corticosteroid alternatives. To minimise the systemic effects of intranasal corticosteroids, each patient should be titrated to his/her lowest effective dose.
However, no reduction in growth velocity was observed in a placebo-controlled clinical trial in which paediatric patients were administered Nasonex Aqueous Nasal Spray 0.05% 100 microgram daily for one year. The effects of treatment for periods of greater than one year have not been studied.

Effects on laboratory tests.

None identified.

4.5 Interactions with Other Medicines and Other Forms of Interactions

In a clinical pharmacokinetic study of mometasone furoate coadministered with loratadine, no clinical interactions between loratadine and mometasone were identified.
Mometasone furoate is metabolised by CYP3A4.
Coadministration with strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, clarithromycin, ritonavir, cobicistat-containing products) may lead to increased plasma concentrations of corticosteroids and potentially increase the risk for systemic corticosteroid side-effects. Consider the benefit of coadministration versus the potential risk of systemic corticosteroid effects, in which case patients should be monitored for systemic corticosteroid side-effects.

4.6 Fertility, Pregnancy and Lactation

Effects on fertility.

As with other corticosteroids, at exposure levels associated with marked signs of systemic corticosteroid toxicity, mometasone furoate had progestogenic effects on the female reproductive tract and mammary glands. However, fertility was unimpaired in a reproductive toxicity study carried out in rats.
(Category B3)
In animal studies, small quantities of mometasone furoate were found to cross the placenta barrier. Like other corticosteroids, at doses associated with signs of systemic toxicity, mometasone furoate reduced fetal growth and was teratogenic in mice, rats and rabbits after subcutaneous or topical application. Higher doses had progestogenic effects in pregnant rats, associated with prolonged gestation, dystocia and reduced pup survival.
There are no adequate or well controlled studies in pregnant women. Low levels of systemic mometasone have been measured following nasal administration of Nasonex Aqueous Nasal Spray 0.05%.
As with other nasal corticosteroid preparations, Nasonex Aqueous Nasal Spray 0.05% should be used in pregnant women only if the potential benefit justifies the potential risk to the mother or fetus. Infants born of mothers who received corticosteroids during pregnancy should be observed carefully for hypoadrenalism.
 After oral administration, small quantities of mometasone furoate and/or its metabolites were transferred into the milk of lactating rats. There are no data on the extent of passage of mometasone furoate and/or its metabolites into the breast milk of women using mometasone furoate nasal spray 0.05%. As with other nasal corticosteroid preparation, Nasonex Aqueous Nasal Spray 0.05% should be used by lactating mother only if the potential benefit justifies any potential risk to the infant.

4.7 Effects on Ability to Drive and Use Machines

The effects of this medicine on a person’s ability to drive and use machines were not assessed as part of its registration.

4.8 Adverse Effects (Undesirable Effects)

Adult population.

Treatment-related local adverse events reported in clinical studies include headache (8%), epistaxis (i.e. frank bleeding, blood-tinged mucus and blood flecks) (8% vs placebo 5%), nasal burning (2% vs placebo 3%), nasal irritation (2% vs placebo 2%), and nasal ulceration (1%), which are typically observed with the use of a corticosteroid nasal spray. Epistaxis was generally self-limiting and mild in severity, and occurred at a comparable or lower incidence compared to other active control nasal corticoids used in clinical studies (up to 15%). The incidence of all other effects was comparable with that of placebo.

Elderly population.

In the elderly, the more common adverse events were epistaxis (12% vs placebo 5%), headache (9% vs placebo 6%) and pharyngitis (4% vs placebo 2%).

Paediatric population.

In the paediatric population, the most common adverse effects were epistaxis (6% vs placebo 6%), headache (3% vs placebo 4%), nasal irritation (2% vs placebo 1%) and sneezing (2% vs placebo 4%).
Growth suppression has been reported in association with administration of intranasal corticosteroids (see Section 4.4 Special Warnings and Precautions for Use, Paediatric use).

Nasal polyposis.

In patients treated for nasal polyposis, the overall incidence of adverse events was comparable to placebo and similar to that observed for patients with allergic rhinitis.

Acute rhinosinusitis.

In patients treated for acute rhinosinusitis, the overall incidence of adverse events was comparable to placebo and similar to that observed for patients with allergic rhinitis.
Treatment related adverse events reported most frequently in the Nasonex 200 microgram twice daily group include epistaxis (3.7% vs placebo 2.6%), diarrhoea (2.1% vs placebo 0.8%), headache (1.7% vs placebo 2.4%), nausea (1.7% vs placebo 0.6%) and abdominal pain (1.7% vs placebo 1.0%).

Other adverse effects.

Rarely, immediate hypersensitivity reactions (e.g. bronchospasm, dyspnoea) may occur after intranasal administration of mometasone furoate monohydrate. Very rarely, anaphylaxis and angioedema have been reported.
Disturbances of taste and smell have been reported very rarely.
Vision blurred has been reported.
Cataracts have been reported with administration of intranasal corticosteroids (see Section 4.4 Special Warnings and Precautions for Use).

Reporting suspected adverse effects.

Reporting suspected adverse reactions after registration 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 at http://www.tga.gov.au/reporting-problems.

4.9 Overdose

Because the systemic bioavailability of Nasonex Aqueous Nasal Spray 0.05% is low and has been estimated as < 1%, overdose is unlikely to require any therapy other than observation. Treatment can be reinitiated at the usual recommended dose.
Inhalation or oral administration of excessive doses of corticosteroids may lead to suppression of HPA axis function.
For information on the management of overdose, contact the Poison Information Centre on 131126 (Australia).

5 Pharmacological Properties

5.1 Pharmacodynamic Properties

Mechanism of action.

Mometasone furoate is a topical glucocorticosteroid with local anti-inflammatory properties at doses that are not systemically active.
In studies utilising nasal antigen challenge, Nasonex Aqueous Nasal Spray 0.05% has shown anti-inflammatory 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.

Clinical trials.

Adult clinical program.

Allergic rhinitis.

The clinical program evaluated the efficacy and safety of Nasonex Aqueous Nasal Spray 0.05% in the prophylaxis and treatment of seasonal allergic rhinitis and the treatment of perennial allergic rhinitis. Five phase I clinical studies evaluated the systemic safety and local tolerability of Nasonex. Other clinical studies included:
one phase II dose-ranging study conducted to determine the optimum dose for the phase III program;
seven phase III studies designed to assess the safety and efficacy of Nasonex in treating seasonal allergic rhinitis for 28 days (including two studies which evaluated the prophylactic efficacy of Nasonex in preventing the symptoms of seasonal allergic rhinitis, and two which evaluated inflammatory response markers following nasal provocation with allergens); and
five phase III studies designed to assess the safety and efficacy of Nasonex in the treatment of perennial allergic rhinitis for 12 weeks. Four studies investigated the long-term safety and maintenance of therapeutic effect of Nasonex over 52 weeks; one perennial allergic rhinitis study was conducted in the elderly population; and three open-label perennial allergic rhinitis studies included a "variable-dose group" in which the dose of Nasonex varied from 100 to 400 microgram daily depending on symptoms.
During the course of the phase II/III clinical program, 3,120 patients (12 years of age and older) were treated with Nasonex Aqueous Nasal Spray 0.05%. The majority (65%) of patients were treated with 200 microgram once daily. The remainder received Nasonex in a dose ranging from 50 to 800 microgram once daily. A total of 712 patients were treated with Nasonex for at least 6 months and 350 patients were treated for 12 months or longer.
The results of the efficacy studies demonstrated that Nasonex Aqueous Nasal Spray 0.05% 200 microgram/day was consistently superior to placebo in relieving the symptoms of both seasonal allergic rhinitis and perennial allergic rhinitis, and was of comparable efficacy to other commonly used topical corticosteroid sprays. In the case of seasonal allergic rhinitis, it is also superior to placebo in the prophylaxis of symptoms. In the long-term studies in perennial allergic rhinitis there was no evidence of any diminution of its efficacy over time.
After the first dose of Nasonex, clinically significant improvement of symptoms was achieved within 12 hours in 28% of a group of patients (n = 190) with seasonal allergic rhinitis (median = 36 hours). However, the 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.

Nasal polyps.

Three studies were conducted to assess the safety and efficacy of Nasonex Aqueous Nasal Spray 0.05% in the treatment of nasal polyps for four months. These included two pivotal trials evaluating doses of 200 microgram once or twice daily and a supportive trial evaluating a dose of 200 microgram once daily. A total of 594 adult patients (ages 18 to 86 years) received Nasonex Aqueous Nasal Spray 0.05%. The co-primary efficacy endpoints in the pivotal trials were 1) change from baseline in nasal congestion/obstruction averaged over the first month of treatment; and 2) change from baseline to last assessment in bilateral polyp grade during the entire 4 months of treatment as assessed by endoscopy. Efficacy was demonstrated in both studies at a dose of 200 microgram twice daily and in one study at a dose of 200 microgram once a day. Improvement in other symptoms of nasal polyps (loss of smell, rhinorrhoea and postnasal drip) was also observed after a 1 month treatment with the 200 microgram, twice daily dose compared to placebo in both studies and in one study after once daily treatment. In the supportive study, patients demonstrated a statistically significant improvement with Nasonex Aqueous Nasal Spray 0.05% at a dose of 200 microgram once a day in relief of nasal congestion and reduction of polyp size with 4 months of treatment compared to placebo.

Acute rhinosinusitis.

In two trials with 1954 patients 12 years of age and older with signs and symptoms of acute rhinosinusitis for 7 to 28 days prior to baseline, Nasonex Aqueous Nasal Spray 0.05% 200 microgram twice daily was effective in significantly improving symptoms of rhinosinusitis compared to placebo as evaluated by the Major Symptom Score (MSS) composite of symptoms (facial pain/pressure/tenderness, sinus headache, rhinorrhoea, postnasal drip and nasal congestion/stuffiness) during the 15 day treatment period (P02683 p < 0.001; P02692 p = 0.038). In P02683, Nasonex Aqueous Nasal Spray 0.05% 200 microgram twice daily reduced the MSS score (averaged across the 15 day treatment period) by 55.6% from baseline, whereas placebo treatment reduced the MSS by 45.6%. In P02692, Nasonex Aqueous Nasal Spray 0.05% 200 microgram twice daily reduced the MSS score by 48.4% from baseline, whereas placebo treatment reduced the MSS by 41.5% (Table 1).
Patients were eligible for study entry only if all signs and symptoms suggestive of bacterial rhinosinusitis were absent. These signs and symptoms were: fever > 38.3°C; persistent severe unilateral facial pain or tooth pain; orbital or periorbital facial swelling; dental involvement; and worsening of symptoms after initial improvement. In addition, patients with severe symptoms (on a scale of mild, moderate or severe) in more than three of the five MSS symptom groups were not eligible for study participation. Thus, study subjects generally had mild or moderate rhinosinusitis, likely of non-bacterial origin. Consistent with this, a 500 mg three times a day amoxicillin arm was not significantly different from placebo in reducing the symptoms of rhinosinusitis as evaluated by the MSS. Overall, fewer subjects treated with Nasonex Aqueous Nasal Spray 0.05% 200 microgram twice daily were considered by the treating physician to be treatment failures than those with placebo (p = 0.0074). In addition, during the post-treatment follow-up period, the number of recurrences seen with Nasonex was low and comparable to the amoxicillin and placebo treatment groups. Treatment duration beyond 15 days was not evaluated in acute rhinosinusitis.

Paediatric clinical program.

The Nasonex paediatric clinical program consisted of three phase I pharmacology/pharmacodynamic studies, one phase II dose ranging study and three phase III studies. A total of 1084 paediatric patients received Nasonex. The paediatric program was designed to address all relevant safety issues in paediatric patients aged 3 to 11 years. Additionally, the goal of this program was to establish the lowest effective dose and to confirm efficacy in both seasonal allergic rhinitis and perennial allergic rhinitis.
Two of the phase I studies conducted in children with allergic rhinitis demonstrated no detectable HPA-axis suppression at multiple doses of 50 to 200 microgram/day for 7 days or 14 days. The third phase I study, a knemometry study, showed no evidence of a reduction in short-term lower leg growth velocity in Nasonex treated subjects (100 or 200 microgram/day).
The phase II dose-ranging study confirmed the lowest effective dose to be 100 microgram/day in the treatment of seasonal allergic rhinitis. The three phase III studies were designed to assess efficacy and safety in perennial allergic rhinitis as well as long-term safety, including an assessment of possible long-term effects on growth.
Compared with placebo, Nasonex 100 microgram once daily significantly reduced the symptoms of seasonal allergic rhinitis and perennial allergic rhinitis in paediatric patients aged between 3 and 11 years. In addition, Nasonex 100 microgram once daily was not associated with any reduction in growth velocity when administered for one year.

5.2 Pharmacokinetic Properties

Absorption.

Systemic bioavailability of mometasone furoate was investigated in 24 healthy volunteers following intranasal administration of 400 microgram of the suspension. Mometasone was detectable in plasma (at sporadic time points) in only 4 of the 24 subjects, despite the use of a sensitive assay with a limit of quantitation of 50 picogram/mL. Thus, there were no relevant pharmacokinetic data for this dosage form.
Systemic absorption of mometasone furoate suspension administered as aqueous nasal spray, 200 microgram single dose, was measured using a sensitive assay with a lower quantitation limit of 0.25 picogram/mL. Mean Cmax was 5.77 picogram/mL (CV% 32) and mean AUC (0-12hr) 29.6 picogram.hr/mL (CV% 37). When compared with dose adjusted PK data for IV mometasone administration from earlier studies with a quantitation limit of 50 picogram/mL and longer sampling duration, the estimated relative systemic (or absolute) bioavailability is < 1%. The bioavailability of mometasone following intranasal administration is low.
Systemic effects were not detected in adults, adolescents or children following the administration of mometasone furoate aqueous nasal spray.
Mometasone furoate suspension is very poorly absorbed from the gastrointestinal tract, and the small amount that may be swallowed and absorbed undergoes extensive first-pass metabolism prior to excretion in urine and bile.

5.3 Preclinical Safety Data

Genotoxicity.

Mometasone furoate is not considered to be genotoxic. There was no evidence of mutagenicity in in vitro tests which included tests for reverse mutation in Salmonella typhimurium and Escherichia coli and forward gene mutation in a mouse lymphoma cell line. Limited evidence of clastogenicity was obtained in Chinese hamster ovary cells, although this finding was not confirmed in a second assay in Chinese hamster lung cells in vitro, nor in vivo assays including a chromosomal aberration assay in mouse spermatogonia, a mouse micronucleus assay or in a rat bone marrow clastogenicity assay. Mometasone furoate did not cause DNA damage in rat liver cells.

Carcinogenicity.

No data available.

6 Pharmaceutical Particulars

6.1 List of Excipients

Benzalkonium chloride (as preservative), citric acid monohydrate, dispersible cellulose, glycerol, polysorbate 80, purified water, sodium citrate dihydrate.

6.2 Incompatibilities

Incompatibilities were either not assessed or not identified as part of the registration of this medicine.

6.3 Shelf Life

3 years.

6.4 Special Precautions for Storage

Store Nasonex Aqueous Nasal Spray 0.05% below 25°C. Do not freeze.

6.5 Nature and Contents of Container

Nasonex Aqueous Nasal Spray 0.05% is supplied in a HDPE Pump Actuated Metered Dose Aerosol containing mometasone furoate (as the monohydrate) 50 micrograms/actuation; 1 x 40* metered doses, 1 x 65 metered doses (junior pack), 1 x 140 metered doses, and 2 x 140 metered doses.
* Not currently marketed in Australia.

6.6 Special Precautions for Disposal

In Australia, any unused medicine or waste material should be disposed of by taking to your local pharmacy.

6.7 Physicochemical Properties

Chemical structure.


Mometasone furoate monohydrate is 9,21-Dichloro-11β,17-dihydroxy-16α-methylpregna-1,4-diene-3,20-dione 17-(2-furoate) monohydrate. The empirical formula is C27H30Cl2O6.H2O.
MW = 539.45 g/mol.
Mometasone furoate is a white to off white powder and it is practically insoluble in water; slightly soluble in methanol, ethanol and isopropanol; soluble in acetone.

CAS number.

CAS Registry number: 83919-23-7 (mometasone furoate anhydrous).

7 Medicine Schedule (Poisons Standard)

Prescription Only Medicine (Schedule 4).

Summary Table of Changes