Rinetazon^® (Spray) Instructions for Use

Marketing Authorization Holder

Lek d.d. (Slovenia)

ATC Code

R01AD09 (Mometasone)

Active Substance

Mometasone (Rec.INN registered by WHO)

Dosage Form

Rinetazon®

Metered-dose nasal spray 50 mcg/dose: 10 g (60 doses), 17 g (120 doses), or 18 g (140 doses) bottle 1, 2, or 3 pcs.

Dosage Form, Packaging, and Composition

Metered-dose nasal spray as a homogeneous white or almost white suspension.

Excipients: microcrystalline cellulose and carmellose sodium (Avicel RC-591) – 2.0 mg, glycerol (glycerol) – 2.1 mg, citric acid monohydrate – 0.2 mg, sodium citrate dihydrate – 0.28 mg, polysorbate 80 – 0.01 mg, benzalkonium chloride – 0.02 mg, purified water – up to 100.0 mg.

10 g (60 doses) – high-density polyethylene bottles with a dosing device and a protective cap (1) – cardboard packs.
10 g (60 doses) – high-density polyethylene bottles with a dosing device and a protective cap (2) – cardboard packs.
10 g (60 doses) – high-density polyethylene bottles with a dosing device and a protective cap (3) – cardboard packs.
17 g (120 doses) – high-density polyethylene bottles with a dosing device and a protective cap (1) – cardboard packs.
17 g (120 doses) – high-density polyethylene bottles with a dosing device and a protective cap (2) – cardboard packs.
17 g (120 doses) – high-density polyethylene bottles with a dosing device and a protective cap (3) – cardboard packs.
18 g (140 doses) – high-density polyethylene bottles with a dosing device and a protective cap (1) – cardboard packs.
18 g (140 doses) – high-density polyethylene bottles with a dosing device and a protective cap (2) – cardboard packs.
18 g (140 doses) – high-density polyethylene bottles with a dosing device and a protective cap (3) – cardboard packs.

Note: the presence of first-opening control for the cardboard pack (perforation) is allowed.

Clinical-Pharmacological Group

Intranasal corticosteroids

Pharmacotherapeutic Group

Drugs for the treatment of nasal diseases; decongestants and other preparations for topical use; corticosteroids

Pharmacological Action

Intranasal glucocorticosteroid. It has anti-inflammatory and anti-allergic effects.

The mechanism of anti-allergic and anti-inflammatory action is due to the ability to inhibit the release of inflammatory mediators. It increases the production of lipomodulin, which is an inhibitor of phospholipase A, which causes a decrease in the release of arachidonic acid and, accordingly, inhibition of the synthesis of arachidonic acid metabolites – cyclic endoperoxides, prostaglandins. It prevents the marginal accumulation of neutrophils, which reduces inflammatory exudate and the production of lymphokines, inhibits macrophage migration, and leads to a reduction in infiltration and granulation processes.

It reduces inflammation by reducing the formation of chemotaxis substance (effect on late allergic reactions), inhibits the development of an immediate-type allergic reaction (due to inhibition of the production of arachidonic acid metabolites and a decrease in the release of inflammatory mediators from mast cells).

In studies with provocative tests involving antigen application to the nasal mucosa, high anti-inflammatory activity of mometasone was demonstrated, both in the early and late stages of the allergic reaction. This was confirmed by a decrease (compared to placebo) in histamine levels and eosinophil activity, as well as a decrease (compared to baseline) in the number of eosinophils, neutrophils, and epithelial cell adhesion proteins.

Pharmacokinetics

With intranasal use, the systemic bioavailability of mometasone furoate is <1% (with a determination method sensitivity of 0.25 pg/ml). Mometasone is very poorly absorbed from the gastrointestinal tract. The small amount of mometasone that may enter the gastrointestinal tract during intranasal administration undergoes active primary metabolism before being excreted in the urine or bile.

Indications

Treatment of seasonal and perennial allergic rhinitis in adults aged 18 years and older (relief of symptoms such as nasal congestion, runny nose, sneezing, nasal itching, watery eyes).

ICD codes

Dosage Regimen

Administer Rinetazon^® intranasally once daily.

The recommended starting dose for adults (18 years and older) is two sprays (100 mcg) in each nostril.

For maintenance therapy, reduce the dose to one spray (50 mcg) in each nostril upon achieving symptom control.

The maximum total daily dose is four sprays (200 mcg).

Use regularly for optimal effect; symptomatic relief may begin within 12 hours.

Prime the spray pump before first use or if unused for 14 days by releasing several test sprays into the air until a fine mist appears.

Shake the bottle gently before each use.

Blow your nose to clear the nasal passages prior to administration.

Avoid spraying directly onto the nasal septum.

Do not use for more than three consecutive months without medical consultation.

Discontinue use and consult a physician if symptoms persist or worsen, or if local irritation or epistaxis occurs.

Adverse Reactions

Infections and parasitic diseases common – pharyngitis, upper respiratory tract infections.

Immune system disorders frequency not known — hypersensitivity reactions, including anaphylactic reactions, angioedema, bronchospasm, dyspnea.

Nervous system disorders: common – headache.

Eye disorders frequency not known – increased intraocular pressure, glaucoma, cataract, blurred vision.

Respiratory, thoracic and mediastinal disorders very common – epistaxis; common – nosebleeds, burning sensation in the nose, irritation of the nasal mucosa, ulceration of the nasal mucosa; frequency not known – nasal septum perforation.

Gastrointestinal disorders common – pharyngeal irritation (sensation of pharyngeal mucosal irritation); frequency not known – taste and smell disorders.

Contraindications

Hypersensitivity to mometasone; presence of untreated local infection involving the nasal mucosa caused by Herpes simplex; recent surgery or nasal trauma with damage to the nasal mucosa – until the wound has healed (due to the inhibitory effect of glucocorticosteroids on healing processes); children and adolescents under 18 years of age.

With caution

In tuberculosis infection (active or latent) of the respiratory tract, untreated fungal, bacterial, systemic viral infection (as an exception, the drug may be prescribed for the listed infections as directed by a physician).

Use in Pregnancy and Lactation

Adequate and well-controlled studies on the use of mometasone during pregnancy have not been conducted. It is not known whether Mometasone is excreted in breast milk.

Intranasal use of mometasone during pregnancy and breastfeeding is possible only if the intended benefit to the mother outweighs the potential risk to the fetus or breastfed infant.

Newborns whose mothers received glucocorticosteroids during pregnancy should be monitored for possible signs of adrenal insufficiency.

Pediatric Use

Contraindicated for use in children and adolescents under 18 years of age.

Geriatric Use

The drug is approved for use in elderly patients.

Special Precautions

Should not be used for more than 3 consecutive months. If use for more than 3 months is necessary, a doctor’s consultation is required.

With long-term intranasal use of mometasone, periodic examination of the nasal mucosa by an ENT doctor is necessary. If a local bacterial or fungal infection of the nose or pharynx develops, it is recommended to discontinue treatment and initiate specific therapy. Persistent irritation of the nasal and pharyngeal mucosa is an indication for drug withdrawal.

If a patient experiences symptoms such as blurred vision or other visual disturbances, they should be referred to an ophthalmologist to assess possible causes, which may include cataract, glaucoma, or rare conditions such as central serous chorioretinopathy, which have been reported following the use of systemic and topical corticosteroids.

Particular caution is required when switching from systemic glucocorticosteroids to intranasal mometasone due to the possible risk of adrenal insufficiency. After discontinuation of systemic glucocorticosteroids, several months are required for the recovery of the hypothalamic-pituitary-adrenal system function.

During stressful situations, including trauma, surgery, infectious diseases, or a severe asthma attack, patients who previously received systemic glucocorticosteroids require additional prescription of a short course of systemic glucocorticosteroids, which are then gradually withdrawn as symptoms subside.

When switching from systemic glucocorticosteroids, intranasal use of mometasone may reveal concomitant allergic diseases, the symptoms of which were previously suppressed by the use of systemic corticosteroids. During this period, some patients may experience signs of systemic glucocorticosteroid withdrawal, including muscle and/or joint pain, depression, feeling tired, even though lung function indicators are stable or even improving. If signs of adrenal insufficiency occur, the dose of systemic glucocorticosteroids should be temporarily increased, and their subsequent withdrawal should be carried out more gradually.

Patients receiving glucocorticosteroids or other immunosuppressants should be advised to avoid contact with patients with certain infections (chickenpox, measles) and must consult a doctor if such contact occurs.

To maintain a low potential for suppression of the hypothalamic-pituitary-adrenal system, the recommended doses should not be exceeded, and the dose of mometasone should be titrated for each patient to achieve the minimum effective dose.

When using mometasone, it should be taken into account that the effect on cortisol production may vary among different patients.

The occurrence of candidiasis may require appropriate antifungal therapy or discontinuation of mometasone.

Drug Interactions

Concomitant use with CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, clarithromycin, ritonavir, medicinal products containing cobicistat) may increase the risk of systemic side effects. Concomitant administration of these drugs should be avoided, unless the benefits of treatment outweigh the risk of systemic side effects of the corticosteroid. In this case, the patient should be carefully monitored for the occurrence of systemic side effects of corticosteroids.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Over-the-Counter

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.