Asmanex^® Twisthaler (Powder) Instructions for Use

ATC Code

R03BA07 (Mometasone)

Active Substance

Mometasone (Rec.INN registered by WHO)

Clinical-Pharmacological Group

Inhaled corticosteroids

Pharmacotherapeutic Group

Topical glucocorticosteroid

Pharmacological Action

Glucocorticosteroid for inhalation use. It has anti-inflammatory and anti-allergic action.

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 leads to a decrease in the release of arachidonic acid and, consequently, 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 decreasing 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 reduced release of inflammatory mediators from mast cells).

In vitro, mometasone furoate significantly inhibits the release of leukotrienes from leukocytes. In cell cultures, mometasone furoate demonstrated a high ability to inhibit the synthesis and release of IL-1, IL-5, IL-6, as well as TNFα; it is also an inhibitor of leukotriene production, as well as an extremely potent inhibitor of Th₂-cytokines, IL-4 and IL-5, by human CD4+ T-cells.

In preclinical model studies, Mometasone reduced the accumulation of inflammatory cells (including eosinophils), integrated into the walls of the upper and lower respiratory tracts, and improved lung function after a provocation test. Mometasone reduced the number of lymphocytes and the concentration of mRNA of cytokines IL-4 and IL-5.

Pharmacokinetics

After inhalation, the systemic bioavailability of mometasone is low, in particular due to poor absorption and significant presystemic metabolism when mometasone is swallowed. In various studies assessing the effect of mometasone at steady state when administered by inhalation, as well as after a single intravenous administration, the absolute bioavailability was approximately 16% in healthy patients and approximately 10% in patients with bronchial asthma. When used at recommended doses, the plasma concentration of mometasone is at or below the limit of detection (50 pg/ml). Consequently, it is impossible to determine either the T_1/2 or V_d of mometasone after inhalation. It is excreted in urine and bile.

Indications

For inhalation use: basic therapy for bronchial asthma of any severity; COPD.

ICD codes

Dosage Regimen

Determine the dosage individually based on disease severity and prior therapy.

For bronchial asthma in adults and adolescents 12 years and older, the initial recommended dose is one inhalation of 200 mcg or 400 mcg once daily in the evening.

For patients previously receiving bronchodilators alone, initiate with 200 mcg once daily.

For patients previously receiving inhaled corticosteroids, initiate with 200 mcg or 400 mcg once daily.

For patients previously receiving oral corticosteroids, initiate with 400 mcg once daily.

The maximum recommended daily dose is 400 mcg for patients with mild-to-moderate asthma and 800 mcg for patients with severe asthma.

Divide doses exceeding 400 mcg into two administrations, morning and evening.

After achieving asthma stability, titrate to the lowest effective dose to maintain control.

For maintenance therapy, some patients may be adequately controlled with a dose of 100 mcg once daily.

Rinse your mouth with water without swallowing after each inhalation to reduce the risk of oropharyngeal candidiasis.

Adverse Reactions

From the respiratory system: with inhalation use for the treatment of bronchial asthma, the development of bronchospasm and an increase in the number of wheezes in the lungs immediately after inhalation is possible.

Systemic effects (especially when used in high doses and for a prolonged time): with inhalation use – suppression of adrenal cortex function, growth retardation in children and adolescents, bone demineralization, glaucoma, increased intraocular pressure (occurs in isolated cases with intranasal use), development of cataracts.

Allergic reactions in post-marketing use in isolated cases – manifestations of hypersensitivity, such as rash, skin itching, angioedema and anaphylactic reaction. Worsening of asthma has been reported, which may manifest as cough, shortness of breath, wheezing and bronchospasm.

Contraindications

Hypersensitivity to mometasone; children under 12 years of age.

Use in Pregnancy and Lactation

Adequate and well-controlled studies on the use of mometasone during pregnancy have not been conducted. After inhalation use, the plasma concentration of mometasone furoate is very low; the impact on the fetus is likely extremely small, the likelihood of toxic effects on reproduction is very low.

It is not known whether Mometasone is excreted in breast milk.

Inhalation 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 infant.

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

Special Precautions

Mometasone should be used with caution in tuberculosis infection (active or latent) of the respiratory tract, untreated fungal, bacterial, systemic viral infection or infection caused by Herpes simplex with eye involvement (as an exception, the drug may be prescribed for the listed infections as directed by a physician), presence of an untreated local infection involving the nasal mucosa.

Mometasone is not intended for the rapid relief of bronchospasm.

Special caution is required when switching from systemic glucocorticosteroids to inhalation use of mometasone due to the possible risk of developing adrenal insufficiency. After discontinuation of systemic glucocorticosteroids, several months are required to restore the function of the hypothalamic-pituitary-adrenal system.

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 to inhalation use of mometasone, manifestations of concomitant allergic diseases, the symptoms of which were previously suppressed by the use of systemic corticosteroids, may occur. During this period, some patients may experience signs of withdrawal of systemic glucocorticosteroids, including muscle and/or joint pain, depression, feeling tired, despite the fact that 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 withdrawal should be carried out more smoothly in the future.

As with the use of other inhalation drugs, paradoxical bronchospasm may develop after the use of mometasone. In this case, immediate use of inhaled rapid-acting bronchodilators is required, followed by discontinuation of mometasone and the appointment of alternative therapy.

Patients receiving glucocorticosteroids or other immunosuppressants should be advised to avoid contact with patients with certain infections (chickenpox, measles) and be sure to consult a doctor if such contact occurs (especially important when used in adolescents over 12 years of age).

To maintain a low potential for suppression of the hypothalamic-pituitary-adrenal system, 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 use.

Use in pediatrics

It is recommended to regularly monitor the growth of adolescents receiving long-term therapy with mometasone. If growth retardation occurs, the ongoing therapy should be reviewed to reduce the dose of mometasone to the minimum effective dose that allows control of disease symptoms.

Storage Conditions

Store at 8°C (46°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

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.