Morezon

Morezon

INTERNATIONAL NONPROPRIETARY NAME

Mometasone

DRUG FORM: metered-dose nasal spray.

Description: white or almost white colour suspension.

COMPOSITION:

1 drug dose contains:

Active substance: mometasone furoate – 50 mcg;

Excipients: avicel (microcrystalline cellulose with sodium carmellose), sodium citrate dihydrate, glycerin, citric acid monohydrate, polysorbate 80, benzalkonium chloride (50% solution), purified water.

PHARMACOTHERAPEUTIC GROUP:

Medicines for the treatment of nasal cavity diseases. Corticosteroids.

ATC code: R01AD09

PHARMACOLOGICAL PROPERTIES:

PHARMACODYNAMICS:

Mometasone furoate is a synthetic topical corticosteroid. It possesses strong anti-inflammatory effect. Mometasone furoate local anti-inflammatory effect of is manifested in doses at which systemic effects do not occur.

Mometasone furoate inhibits the release of inflammatory mediators, significantly reduces the synthesis/release of leukotrienes from leukocytes in patients with allergic disorders. In a cell culture Mometasone furoate demonstrated high potential (10 times higher activity than other steroids, including beclomethasone dipropionate, betamethasone, hydrocortisone and dexamethasone) of interleukins and tumor necrosis factor synthesis/release inhibition; it also significantly inhibits interleukins 4 and 5 synthesis by T-helpers: mometasone furoate is 6 times more active in inhibition of IL-5 synthesis than beclomethasone dipropionate and betamethasone.

PHARMACOKINETICS:

Upon the proper intranasal application the drug systemic bioavailability is <1%. In this case, even with the use of high-tech methods the drug is not detected in the blood serum. Mometasone suspension is very poorly absorbed in the gastrointestinal tract providing that very small amount of mometasone suspension which can enter the gastrointestinal tract after nasal inhalation can undergo an active primary metabolism before excretion with the urine or bile.

INDICATIONS FOR USE:

- treatment and prevention of seasonal and perennial allergic rhinitis symptoms in adults and children above 2 years old;

- treatment of acute rhinosinusitis without signs of severe bacterial infection in adults and children above 12 years old;

- treatment of nasal polyps and related symptoms, including nasal congestion and loss of smell in patients over 18 years.

CONTRAINDICATIONS:

- Hypersensitivity to the drug components.

SIDE EFFECTS:

During clinical studies of seasonal and perennial allergic rhinitis the following side effects associated with the use of Morezon have been noted: headache (8%), nosebleeds (i.e. real bleeding, as well as bloody mucus or blood clots) (8%), pharyngitis (4%), burning sensation in the nose (2%), irritation (2%) and ulcerative changes (1%) of the nasal mucosa.

The development of such side effects is typical for any nasal spray contained corticosteroids.

The incidence of side effects in children including nosebleeds (6%), headache (3%), feeling irritation in the nose (2%) and sneezing (2%) was comparable to that with placebo.

Systemic effects can occur with the use of nasal corticosteroids, especially when prescribed at high doses and in prolonged use. These effects are less likely than when using oral corticosteroids and may vary in different patients when using different corticosteroids.

DOSAGE AND ADMINISTRATION

Intranasal administration. Avoid contact with eyes.

Before use the vial should be shaken vigorously.

Before the first use of nasal spray it is necessary to “calibrate” the dosing device (the first 10 actuations) prior to application. Then a stereotypical drug flow rate should be established. If the drug has not been used for 14 days or more the repeated “calibration” is necessary to perform before the next application.

In patients with seasonal allergic rhinitis prevention it is recommended to start in 2-4 weeks before the onset of clinical symptoms.

Treatment and prevention of seasonal and the year round rhinitis in adults and children over 12 years old: 2 injections (100 mcg) into each nostril once a day (daily dose – 200 mcg). Once the therapeutic effect is achieved it is advisable to reduce the dose to 1 actuation into each nostril once a day (daily dose – 100 μg) to maintain the therapy.

Clinical effect is usually observed within 12 hours after the first time drug application.

If the symptoms of the disease cannot be alleviated with the recommended therapeutic drug dose the daily dose can be increased to a maximum of 4 doses into each nostril once a day (daily dose – 400 mcg). Once the symptoms are subsided the dose reduction should be recommended.

Children aged 2 to 12 years: 1 dose (50 mcg) into each nostril once a day (daily dose – 100 mcg).

Treatment of acute rhinosinusitis without signs of severe bacterial infection in adults and children over 12 years: 2 doses (100 mcg) into each nostril 2 times a day (daily dose – 400 mcg).

Treatment of nasal polyps and related symptoms including nasal congestion and loss of smell in patients older 18 years: 2 injections (100 mcg) into each nostril 2 times a day (daily dose – 400 μg). Once the symptoms of the disease have alleviated, it is recommended to reduce the dose to 2 injections (100 mcg) into each nostril once a day (daily dose – 200 μg).

In case of no improvement with the symptoms of the disease in 5-6 weeks, an alternative treatment should be considered.

If the drug dose was missed, the dose should be taken as soon as possible.

Elderly patients: dose adjustment not required.

PRECAUTIONARY MEASURES:

Morezon should not be used in case of current untreated local infection involved the nasal mucosa.

Due to the fact that corticosteroids slow down wound healing these drugs should not be prescribed intranasal to patients who have recently undergone surgery or had nasal trauma until the wounds have completely healed.

Morezon should be used with caution or not used at all in case of respiratory tuberculosis (including latent), untreated fungal, bacterial, systemic viral infections (including those caused by Herpes simplex with eye disorders).

The drug safety and efficacy in treatment of unilateral polyps associated with cystic fibrosis or in treatment of polyps that completely block the nasal tract have not been established.

In prolonged treatment with Morezon the signs of hypothalamic-pituitary-adrenal system inhibition have not been observed. Patients on treatment with Morezon nasal spray after prolonged treatment with systemic corticosteroids should be closely monitored. Discontinuation of systemic corticosteroids therapy in these patients may lead to adrenal cortex insufficiency which may require the resumption of therapy with systemic corticosteroids and another appropriate treatment mode.

When switching from systemic corticosteroid to Morezon treatment some patients may experience relief of nasal symptoms along with symptoms of corticosteroid withdrawal (for example, pain in joints and/or muscles, tiredness and depression). Such patients should be specifically convinced to continue the treatment with Morezon. Therapy replacement may also induce allergic diseases (allergic conjunctiva, eczema, etc.) that developed earlier and had been masked by systemic corticosteroid therapy.

Patients should be warned to immediately consult the doctor if signs or symptoms of severe bacterial infection occurred, e.g. fever, severe unilateral pain in the face or toothache, orbital or periorbital swelling/edema or deterioration after preliminary improvement.

PEDIATRIC USE:

In placebo-controlled clinical studies with Morezon therapy in children with a daily dose of 100 mcg round the year growth retardation was not observed. However long-term effects on intranasal /inhaled route of steroid administration have not been studied conclusively. The doctor should carefully monitor the growth and development in children on long-term therapy with glucocorticosteroids.

The drug administration in small children should be carried out by adults.

PREGNANCY AND LACTATION:

Special studies of the drug effect in pregnant women have not been conducted. The drug should be prescribed only when the expected benefit to the mother outweighs the potential risk to the fetus or child. Infants whose mothers have used corticosteroids during pregnancy period should be carefully examined for possible adrenal glands hypofunction.

EFFECT ON ABILITY TO DRIVE AND OPERATE MACHINERY:

The drug does not effect on ability to drive and operate machinery.

PREGNANCY AND LACTATION:

The drug should be prescribed only if the expected benefit to the mother outweighs the potential risk to the fetus or child.

Infants whose mothers have used corticosteroids during pregnancy should be carefully examined for possible adrenal glands hypofunction.

INTERACTION WITH OTHER DRUGS:

Combination therapy with loratadine was well tolerated by patients. In this case no any drug effect on loratadine or its main metabolite plasma concentration was observed.

STORAGE CONDITIONS:

Store at a temperature not above 25°С.

Keep out of reach of children!

SHELF LIFE:

Shelf life is 3 years. Do not use after the expiration date specified on the package.

PRESCRIPTION STATUS

By prescription

Manufacturer Information

Foreign production and trade unitary enterprise “Reb-Pharma”, 223216, Republic of Belarus, Minsk region, Chervensky district, Smilovichi, Sadovaya st., 1, tel./fax: (+375) 17 240 26 35,

e-mail: rebpharma@rebpharma.by, http://www.rebpharma.by