Mometasone furoate - instructions for use, dose, side effects, contraindications

Clinical and pharmacological group: & nbsp

Included in the formulation

АТХ:

S.01.B.A Corticosteroids

Pharmacodynamics:

The drug interacts with the intentricular receptors of glucocorticoids, facilitating the release of the receptor from binding to immunophilin and heat shock proteins 70 and 90. Penetration of the activated receptor into the nucleus, binding to glucocorticoid-sensitive regulatory elements of DNA - a specific effect on gene expression (activation and suppression). Interaction with other protein transcription factors, including NFκB and AP-1, regulating the expression of many proteins of the immune system, which leads to suppression of the expression of genes encoding some cytokines, collagenase and stromelysins.

The anti-inflammatory effect of mometasone is due to several factors.

1. The drug induces the synthesis of lipocortin, which inhibits the activity of phospholipase A2. Inhibition of phospholipase-mediated A2 hydrolysis of membrane phospholipids of damaged tissues prevents the formation of arachidonic acid. The disruption of the formation of arachidonic acid actually means inhibition of the synthesis of prostaglandins, since arachidonic acid is a substrate for further metabolism along the cyclooxygenase pathway, and also along the lipoxygenase pathway, with appropriate inhibition of leukotriene synthesis.

2.The anti-inflammatory effect of glucocorticoids is potentiated by their ability to inhibit the expression of COX-2 genes, which also leads to a decrease in the synthesis of prostaglandins in the inflammatory focus, including pro-inflammatory prostaglandins E₂ and I₂.

3. Mometasone furoate inhibits the expression of molecules of intercellular adhesion in the endothelium of blood vessels, violating the penetration of neutrophils and monocytes into the focus of inflammation. After the introduction of glucocorticoids, an increase in the concentration of neutrophils in the blood (due to their entry from the bone marrow and the restriction of migration from the blood vessels) is noted. This causes a decrease in the number of neutrophils in the site of inflammation.

Mometasone furoate inhibits the transcription of cytokine genes that stimulate the inflammatory and immune response (IL-1, IL-2, IL-6, IL-8), as well as tumor necrosis factor (and some others). Also, a decrease in the transcription rate and an increase in the degradation of the receptor genes for IL-1 and IL-2, inhibition of transcription of the metalloproteinase (collagenase, elastase, etc.) genes involved in the increase permeability of the vascular wall, in the processes of scarring and destruction of cartilaginous tissue in diseases of the joints.

Immunosuppressive action is due to inhibition of transcription of DNA encoding the main histocompatibility complex, pro-inflammatory cytokines and inhibition of proliferation of T lymphocytes. It leads to a decrease in the number of T-lymphocytes and their influence on B-lymphocytes, inhibits the production of immunoglobulins. Reduces the formation and increases the decomposition of components of the complement system.

The antiallergic effect is associated with the inhibition of the synthesis of mediators of allergy, degranulation of mast cells and release of mediators of allergy, and therefore it is effective for allergic reactions of immediate type.

Pharmacokinetics:

With intranasal application, the systemic bioavailability of mometasone furoate is <1%. Mometasone very poorly absorbed from the digestive tract.

A small amount of active substance, which can enter the digestive tract after intranasal administration, undergoes active metabolism during the "first passage" through the liver. It is excreted in urine and bile.

After inhalation, the systemic bioavailability of mometasone is low, in particular, due to low absorption and significant presystemic metabolism when mometasone is ingested.In various studies evaluating the effects of mometasone in the equilibrium state when administered as inhalation, and after a single intravenous injection, absolute bioavailability was approximately 16% in healthy patients and approximately 10% in patients with bronchial asthma. As a consequence, it is impossible to determine either the half-life or the volume of distribution of mometasone after inhalation. It is excreted in urine and bile.

Indications:

Therapy of bronchial asthma of any severity, chronic obstructive pulmonary disease; treatment of seasonal and all-year-round allergic rhinitis in adults, adolescents and children from 2 years; acute sinusitis; chronic sinusitis; acute rhinosinusitis without signs of bacterial infection; prevention of seasonal allergic rhinitis of moderate and severe course in adults and adolescents from the age of 12; polyposis of the nose; to relieve itching in dermatoses.

ICD-10

X.J00-J06.J01 Acute Sinusitis

X.J30-J39.J30.1 Allergic rhinitis caused by pollen of plants

X.J30-J39.J30.2 Other seasonal allergic rhinitis

X.J30-J39.J30.3 Other allergic rhinitis

X.J30-J39.J32 Chronic Sinusitis

X.J40-J47.J44.9 Chronic obstructive pulmonary disease, unspecified

X.J40-J47.J45 Asthma

XII.L20-L30.L20 Atopic dermatitis

XII.L20-L30.L21 Seborrheic dermatitis

XII.L20-L30.L30.9 Dermatitis, unspecified

XII.L40-L45.L40 Psoriasis

Contraindications:

· Hypersensitivity.

· Age under 12 years with inhalation.

· Trauma or recent nasal surgery - until the wound is healed (in connection with the inhibitory effect of glucocorticosteroids on healing processes).

· Age under 18 years with polyposis of the nose.

· Age under 12 years with acute and chronic sinusitis,

· Age to 2 years with seasonal rhinitis.

Carefully:

With intranasal application - hypersensitivity, infectious diseases of the nasal mucosa, recent surgery or trauma of the nose (until the wounds heal completely), children's age (up to 12 years).

With intranasal application - tuberculosis (active or latent), fungal, bacterial, systemic viral infection, Herpes simplex with eye damage, long-term therapy with glucocorticoid systemic effects, pregnancy, breast-feeding.

With external application - pregnancy, tuberculosis (active and latent forms), fungal, bacterial and systemic viral infections, infections caused by Herpes simplex with eye damage. Long-term therapy with glucocorticoid systemic action.

Applying to the face skin and intertriginoznuyu surface of the skin, the use of occlusive dressings, as well as the treatment of large areas of the skin and / or long-term treatment (especially in children).

Pregnancy and lactation:

Action category for the fetus by FDA - C. Adequate studies on the effect of the drug on the fetus or on the baby (with breastfeeding) were not conducted. Do not apply.

Inhalational or intranasal application of mometasone during pregnancy and during breastfeeding is possible only if the intended benefit to the mother exceeds the potential risk to the fetus or infant.

Newborns whose mothers received glucocorticosteroids during pregnancy should be observed to identify possible symptoms of adrenocortical insufficiency.

Dosing and Administration:

The dosage regimen is set individually for each patient in accordance with his diagnosis, clinical indices and individual characteristics.

Locally, intranasally, inhalation. The dosage regimen is set individually, depending on the mode of administration, diagnosis of the patient, his age and dosage form.

Cream and ointment applied to the affected skin with a thin layer once a day. Lotion in the amount of a few drops applied to the affected areas (including the scalp) and rub softly until completely absorbed. Outer adults and children from 2 years.

Allergic rhinitis (seasonal^B6 or year-round). Prophylactic and therapeutic dose of 2 inhalations of 50 micrograms per each nasal passage 1 time per day; daily dose of 200 mcg. If necessary, up to 4 inhalations in each nasal passage; daily dose of 400 mcg. After the disappearance of symptoms of the disease - reduced dose. A maintenance dose of 50 mcg in each nasal passage; daily dose of 100 mcg.

- Chronic sinusitis (exacerbation, as part of complex therapy). By 2 inhalations (100 mcg) in each nasal passage 2 times a day. Children from 3 to 12 years of age for 1 inhalation (50 mcg) in each nasal passage per day.

Side effects:

Systemic effects: growth retardation in children, cataract, suppression of adrenal cortex function and Itenko-Cushing syndrome, demineralization of bone tissue, increased intraocular pressure, glaucoma.

On the part of the respiratory system: bronchospasm, pharyngitis, nosebleeds, perforation of the nasal septum, sneezing, burning in the nose, irritation of the nasal mucosa.

Other: allergic reactions, headache.

Overdose:

Development of symptoms of hypercortisy (Isenko-Cushing syndrome). With intranasal application, bleeding from the nose is possible.

Itching and burning of the skin at the site of application, hyperglycemia, glucosuria,

Treatment is symptomatic on the background of a gradual discontinuation of the drug.

With prolonged use of mometasone in high doses or with the simultaneous use of several glucocorticosteroids, oppression of the hypothalamic-pituitary-adrenal system is possible.

Interaction:

With simultaneous administration with immunosuppressants, the risk of infections is increased.

Special instructions:

With prolonged use, it is necessary to monitor the function of the adrenal glands.

Not intended for use in ophthalmology.

Impact on the ability to drive vehicles and manage mechanisms

Studies to study the effect on the ability to drive vehicles and mechanisms were not conducted.

Instructions

Mometasone furoate (Mometasoni furoas)