Glenspray

INSTRUCTION FOR MEDICAL USE OF THE MEDICINAL PRODUCT GLENSPRAY (GLENSPRAY)

Composition:

Active substance: mometasone furoate;

One dose contains mometasone furoate monohydrate equivalent to 50 mcg of mometasone furoate;

Excipients: microcrystalline cellulose and sodium carboxymethylcellulose; glycerin; citric acid, monohydrate; sodium citrate; polysorbate 80; benzalkonium chloride; water for injections.

Pharmaceutical form. Nasal spray, metered; suspension.

Main physicochemical properties: white or almost white, semi-transparent, viscous suspension.

Pharmacotherapeutic group.
Anti-inflammatory and other drugs for local use in nasal cavity disorders. Corticosteroids. ATC code R01AD09.

Pharmacological Properties

Pharmacodynamics

Mometasone furoate is a synthetic corticosteroid for topical use with pronounced anti-inflammatory activity. Corticosteroids exhibit a broad range of effects on various cells, including mast cells, eosinophils, neutrophils, macrophages, lymphocytes, as well as on inflammatory mediators (histamine, eicosanoids, leukotrienes, and cytokines). The mechanism of the anti-inflammatory and antiallergic action of mometasone furoate is primarily related to its ability to suppress the release of mediators of allergic reactions.

Mometasone furoate significantly inhibits the release of leukotrienes from leukocytes in patients with allergies. In vitro studies have demonstrated that mometasone furoate exhibits strong activity in suppressing the synthesis and release of IL-1, IL-5, IL-6, and TNFα, and it effectively reduces leukotriene production. Furthermore, it potently inhibits the synthesis of Th2 cytokines, IL-4 and IL-5, from human CD4+ T-cells.

Studies have shown that mometasone furoate, administered as a nasal spray at a dose of 50 mcg/dose, reduces, upon local application, the levels of certain mediators involved in both the early and late phases of allergic reactions. It decreases (compared to placebo) the levels of histamine and eosinophilic cationic protein and reduces (compared to baseline values) the number of eosinophils, neutrophils, and epithelial cell adhesion proteins.

Pharmacokinetics

The systemic bioavailability of mometasone furoate following intranasal administration is less than 1% in plasma (based on data obtained using a sensitive quantitative assay method, with a lower limit of quantification of 0.25 pg/mL). Mometasone furoate suspension is poorly absorbed from the gastrointestinal tract. Any small amount that may be swallowed and absorbed undergoes extensive first-pass metabolism prior to excretion, primarily as metabolites in bile and to a lesser extent in urine.

Clinical characteristics.

Indications.

• Treatment of seasonal or perennial allergic rhinitis in adults and children aged 3 years and older. Prophylactic treatment of moderate to severe allergic rhinitis should be initiated 4 weeks before the expected start of the pollen season.
• As an adjunctive therapeutic agent in antibiotic treatment of acute episodes of sinusitis in adults (including elderly patients) and children aged 12 years and older.
• Treatment of symptoms of acute rhinosinusitis without signs of severe bacterial infection in adults and children aged 12 years and older.
• Treatment of nasal polyps and associated symptoms, including nasal congestion and loss of smell, in patients aged 18 years and older.

Contraindications.

Hypersensitivity to mometasone furoate or to any of the excipients of the medicinal product.

Untreated local nasal mucosal infection.

Nasal trauma or recent nasal surgery.

Interaction with other medicinal products and other forms of interaction.

Concomitant therapy with CYP3A inhibitors, including medicinal products containing cobicistat, is expected to increase the risk of systemic adverse effects. Concomitant use should be avoided unless the benefit outweighs the increased risk of systemic corticosteroid adverse effects; in such cases, patients should be monitored for the occurrence of systemic corticosteroid adverse effects.

Mometasone furoate nasal spray has been used concomitantly with loratadine. No effect on plasma concentrations of loratadine or its major metabolite was observed, and mometasone furoate was not detectable in plasma even at minimal concentrations. The combination therapy was well tolerated by patients.

Special precautions for use.

Administration of the drug to younger children should be carried out under adult supervision.

The drug should not be used in the presence of untreated local infection involving the nasal mucosa.

Since corticosteroids may impair wound healing, nasal corticosteroids should not be administered to patients who have recently undergone nasal surgery or have sustained nasal trauma until healing has occurred.

Glenpray should be used with caution or not used at all in patients with active or latent tuberculosis of the respiratory tract, as well as in patients with untreated fungal, bacterial, systemic viral infections, or herpes simplex infection involving the eyes.

After 12 months of treatment with mometasone furoate nasal spray, no signs of atrophy of the nasal mucosa were observed; moreover, mometasone furoate contributed to normalization of the histological picture of the nasal mucosa. As with any prolonged treatment, patients using the drug for several months or longer should undergo periodic examinations to detect possible changes in the nasal mucosa. If local fungal infection of the nose and/or pharynx develops, discontinuation of treatment with the drug or appropriate antifungal therapy may be necessary. Persistent irritation of the nasal and pharyngeal mucosa may also be an indication for discontinuation of therapy.

Although the drug controls nasal symptoms in most patients, concomitant use of appropriate additional therapy may provide further relief of other symptoms, particularly ocular symptoms.

No evidence of suppression of hypothalamic-pituitary-adrenal (HPA) axis function has been observed during long-term treatment with mometasone furoate nasal spray. However, prolonged use of intranasal corticosteroids (including Glenpray) may affect adrenal cortex function and may cause hypercorticism in corticosteroid-sensitive patients and in certain cases. Patients who are switched to nasal spray treatment after prolonged systemic corticosteroid therapy should be closely monitored. Discontinuation of systemic corticosteroids in such patients may lead to adrenal insufficiency, which may require resumption of systemic corticosteroid therapy and other appropriate treatment.

The safety and efficacy of the drug in the treatment of unilateral nasal polyps, polyps associated with cystic fibrosis, or polyps completely obstructing the nasal cavity have not been studied.

Unilateral polyps that are atypical, especially those associated with ulcers or bleeding, require additional evaluation.

During transition from systemic corticosteroid therapy to treatment with Glenpray, some patients may experience corticosteroid withdrawal symptoms (e.g., joint and/or muscle pain, fatigue, depression) despite improvement in nasal symptoms. Such patients should be specifically reassured about the importance of continuing spray therapy. The change in therapy may also unmask previously suppressed allergic conditions (such as allergic conjunctivitis, eczema) that had been masked by systemic corticosteroid therapy.

Patients receiving corticosteroids may have potentially reduced immune responsiveness and should be warned about the increased risk of infection when exposed to certain infectious diseases (such as varicella, measles), as well as the need to consult a physician if such exposure occurs.

The potential risk of Cushing's syndrome may occur with prolonged use of the drug at high doses.

Very rare cases of nasal septum perforation or increased intraocular pressure have been reported after use of intranasal corticosteroids.

High-dose or prolonged use of glucocorticosteroids may result in systemic effects such as growth suppression in children. The long-term effects of intranasal/inhaled steroids in children are not fully understood. Physicians should carefully monitor the growth of children receiving long-term glucocorticosteroid therapy.

If growth retardation occurs, therapy should be re-evaluated with the aim of reducing the dose of the nasal corticosteroid to the lowest possible dose at which effective symptom control is maintained.

In placebo-controlled clinical trials in children treated with mometasone furoate nasal spray at a daily dose of 100 mcg for 1 year, no growth retardation was observed.

Patients should be advised to seek immediate medical attention if signs or symptoms of severe bacterial infection occur, such as elevated body temperature, severe unilateral facial pain or toothache, orbital or periorbital swelling/edema, or worsening condition after initial improvement.

Visual disturbances

Visual disturbances may occur with systemic and local use of corticosteroids (including intranasal, inhaled, and intraocular administration). If symptoms such as blurred vision or other visual disturbances occur, the patient should undergo ophthalmological examination to evaluate possible causes, including cataract, glaucoma, or rare conditions such as central serous chorioretinopathy, which has been reported after use of systemic and locally administered corticosteroids.

Use during pregnancy or breastfeeding

Specific studies on the effects of the drug in pregnant women have not been conducted.

Like other intranasal corticosteroids, Glenpray should be used during pregnancy and breastfeeding only if the expected benefit justifies the potential risk to the mother, fetus, or infant. Infants born to mothers who used corticosteroids during pregnancy should be carefully monitored for possible adrenal insufficiency.

Ability to affect reaction speed when driving or operating machinery

Unknown.

Administration and Dosage

The product is intended for intranasal use only.

Treatment of seasonal or perennial allergic rhinitis: The recommended prophylactic and therapeutic dose for adults (including elderly patients) and adolescents aged 12 years and older is 2 sprays (50 mcg each) in each nostril once daily (total daily dose – 200 mcg). After achieving the therapeutic effect, a reduction in dose to 1 spray in each nostril once daily (total daily dose – 100 mcg) is advisable for maintenance therapy.

If symptoms are not adequately controlled with the recommended therapeutic dose, the daily dose may be increased to the maximum: 4 sprays in each nostril once daily (total daily dose – 400 mcg). After symptom relief, dose reduction is recommended.

The product has demonstrated a clinically significant onset of action within 12 hours after the first dose in some patients with seasonal allergic rhinitis. However, full therapeutic benefit may not be achieved within the first 48 hours; therefore, patients should continue regular use to achieve optimal therapeutic effect.

For children aged 3 to 11 years, the recommended therapeutic dose is 1 spray (50 mcg) in each nostril once daily (total daily dose – 100 mcg).

Adjunctive treatment of acute episodes of sinusitis. For adults (including elderly patients) and adolescents aged 12 years and older, the recommended therapeutic dose is 2 sprays (50 mcg each) in each nostril twice daily (total daily dose – 400 mcg).

If symptoms are not adequately controlled with the recommended therapeutic dose, the daily dose may be increased to 4 sprays in each nostril twice daily (total daily dose – 800 mcg). After symptom relief, dose reduction is recommended.

Acute rhinosinusitis. For adults and adolescents aged 12 years and older, the recommended therapeutic dose is 2 sprays (50 mcg each) in each nostril twice daily (total daily dose – 400 mcg).

Nasal polyps. For patients aged 18 years and older (including elderly patients), the recommended dose is 2 sprays (50 mcg each) in each nostril twice daily (total daily dose – 400 mcg). After achieving clinical response, the dose should be reduced to 2 sprays in each nostril once daily (total daily dose – 200 mcg). If no clinical response is observed after 5–6 weeks of treatment with the recommended doses, alternative therapy should be considered.

Use of the nasal spray

Shake the bottle vigorously before each use. Then remove the protective cap. Before first use, the bottle must be primed. Priming is performed by pressing the pump approximately 10 times until a consistent spray is produced, ensuring that each spray delivers approximately 100 mg of suspension containing 50 mcg of mometasone (one dose). If the nasal spray has not been used for 14 days or longer, it must be re-primed by spraying 2 times until a full spray is observed. Do not pierce the nozzle before use.

Before each administration, clear the nasal passages thoroughly of mucus. After cleaning the nose, administer the suspension into each nostril while keeping the head slightly tilted forward. After use, wipe the spray nozzle and replace the protective cap.

If the nozzle becomes blocked, clean the spray device according to the following instructions. Do not attempt to unblock the pump with a needle or other sharp object, as this may damage the device and affect accurate dosing.

To clean the nasal spray device, remove the plastic cap (Figure 1).

(Figure 1)

Gently pull upward on the white nasal spray nozzle to remove it (Figure 2).

(Figure 2)

Soak the nozzle and dust cap in warm water for several minutes, then thoroughly rinse the spray nozzle and dust cap under warm water, and finally rinse with clean running water.

(Figure 3)

After the spray device has dried, reattach the nasal spray nozzle, ensuring that the pump stem is properly reinserted into the central opening of the applicator (Figure 4).

(Figure 4)

Prepare the pump for further use by pressing the sides of the upper part of the white nasal spray nozzle with the index and middle fingers while holding the base of the bottle with the thumb. Press and release the pump twice, or continue pressing until a fine mist is produced (repeat the rinsing procedure described above if no mist appears). Do not spray into the eyes. The pump is now ready for use. The pump may be stored without use for up to 1 week without the need for re-priming. If the pump has not been used for more than 1 week, prepare it for use by spraying into the air twice, or until a fine mist appears (Figure 5).

(Figure 5)

Replace the plastic cap (Figure 6).

(Figure 6)

Children

In placebo-controlled clinical studies in children who received mometasone furoate nasal spray at a daily dose of 100 mcg for one year, no growth suppression was observed.

The safety and efficacy of the product in the treatment of nasal polyps in children and adolescents under 18 years of age, symptoms of rhinosinusitis in children under 12 years of age, and seasonal or perennial allergic rhinitis in children under 3 years of age have not been established.

Overdose

Due to the low systemic bioavailability of the product (less than 1%, based on sensitive quantitative methods with a lower limit of quantification of 0.25 pg/mL), it is unlikely that any measures other than patient monitoring and subsequent use of the recommended dose will be required in case of overdose.

Prolonged inhalation or oral administration of high doses of corticosteroids may lead to suppression of the hypothalamic-pituitary-adrenal (HPA) axis.

Adverse reactions.

During clinical studies on seasonal and perennial allergic rhinitis, adverse events associated with intranasal administration of mometasone furoate are presented in Table 1.

Nasal bleeding stopped spontaneously and was mild, occurring somewhat more frequently than with placebo (5%), but less frequently than with other investigational intranasal corticosteroids used as active control (in some of these, the incidence of nasal bleeding reached up to 15%). The incidence of other adverse events was comparable to that observed with placebo.

In children, the incidence of adverse events was comparable to that with placebo, for example, epistaxis (6%), headache (3%), nasal irritation (2%), and sneezing (2%).

In patients with nasal polyps, the overall number of adverse events was comparable to that with placebo and similar to that observed in patients with allergic rhinitis.

Intranasal mometasone furoate-related adverse reactions observed in clinical trials in more than 1% of patients are listed in Table 2.

After intranasal administration of mometasone furoate, hypersensitivity reactions, including bronchospasm and dyspnea, may occasionally occur. Very rarely, anaphylactic reactions, angioedema, or disturbances of smell and taste have been reported.

In patients with acute rhinosinusitis, the overall number of adverse events was comparable to that observed with placebo and similar to the number observed in patients with other indications. Treatment-related adverse reactions observed in clinical trials in more than 2% of patients are listed in Table 3.

The most common adverse reaction, nasal bleeding, occurred at approximately the same frequency in the placebo group (2.6%) and in the mometasone furoate groups (2.9% and 3.7%, respectively).

Systemic effects of nasal corticosteroids are possible, especially with prolonged use of high doses.

Very rarely, cases of nasal septum perforation and increased intraocular pressure have been reported with intranasal corticosteroids.

Rare cases of glaucoma, cataract, and central serous chorioretinopathy have been reported with the use of intranasal corticosteroids.

Blurred vision has been reported.

Children. In children, the frequency of reported adverse reactions during clinical trials, such as nasal bleeding (6%), headache (3%), nasal mucosal irritation (2%), and sneezing (2%), was comparable to that observed with placebo.

Reporting of suspected adverse reactions

Reporting of suspected adverse reactions after medicinal product registration is important. It allows continuous monitoring of the benefit-risk balance of the medicinal product. Healthcare and pharmacy professionals, as well as patients or their legal representatives, should report all suspected adverse reactions and lack of efficacy through the automated pharmacovigilance information system at: https://aisf.dec.gov.ua.

Shelf life.

2 years.

Storage conditions.

Store in a place protected from light, at a temperature not exceeding 30 °C. Do not freeze. Keep out of reach of children.

Packaging.

60 or 120 doses in a polyethylene bottle. One bottle with a metered dose pump-spray, closed with a cap, in a cardboard box.

Prescription status.

Prescription only.

Manufacturer.

Glenmark Pharmaceuticals Ltd./Glenmark Pharmaceuticals Ltd.

Manufacturer's address and location of its business operations.

Unit III, Village Kishanpura, Baddi-Nalagarh Road, Tehsil Baddi, Distt. Solan (H.P.) 173 205, India/
Unit III, Village Kishanpura, Baddi-Nalagarh Road, Tehsil Baddi, Distt. Solan (H.P.) 173 205, India.