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

The drug interacts with the intracellular 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 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 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 note the reduction in velocity and increased transcription of genes degradation receptors to IL-1 and IL-2, inhibition of gene transcription metalloproteinases (collagenases, elastase and others) 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:

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. When used in recommended doses, the concentration of mometasone in the plasma is about or below the detection threshold (50 pg / ml).As a consequence, it is impossible to determine either the half-life or the volume of distribution of mometasone after inhalation. The drug is absorbed from the skin surface by 0.4%, with mucous by inhalation - less than 0.1%. The connection with plasma proteins is 98-99%, metabolized in the liver, excreted by the kidneys. The half-life is 5.8 hours.

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 Other chronic obstructive pulmonary disease

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 up to 12 years with inhalation, trauma or recent nasal surgery - until the wound is healed (in connection with inhibitory action glucocorticosteroids on healing processes), age under 18 years with polyposis of the nose, age up to 12 years with acute and chronic sinusitis, age up 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 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 glucocorticosteroids of systemic action.

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

Pregnancy and lactation:

Category FDA - C. Adequate and well-controlled studies of mometasone in pregnancy have not been conducted. After inhalation, the concentration of mometasone furoate in the blood plasma is very low; the impact on the fetus is probably extremely small, the likelihood of toxic effects on reproductive efficiency is very low.

It is not known whether mometasone with breast milk.

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:

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 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:

On the part of the respiratory system: bronchospasm, nosebleeds, burning in the nose, irritation of the nasal mucosa, sneezing, pharyngitis, perforation of the nasal septum, oppression of the adrenal cortex, bone marrow dimineralization, glaucoma, rash, skin itching, worsening asthma, headache, delay growth in children and adolescents, the development of cataracts, increased intraocular pressure.

For external use:

Burning, itching, steroid acne, striae, dry skin, folliculitis.

With long-term use - skin atrophy, local hirsutism, hypertrichosis, telangiectasia, purpura, skin pigmentation disorders, alopecia, especially in women.

Secondary immunodeficiency (exacerbation of chronic infectious diseases, generalization of the infectious process, development of opportunistic infections).

When applied to large surfaces - systemic manifestations gastritis, "steroid" stomach ulcer, adrenal insufficiency, Itenko-Cushing syndrome, "steroid" diabetes, slowing of reparative processes, and others).

With intranasal application:

More often - mild and transient burning, dryness or other irritation in the nasal cavity and pharynx, sneezing attacks, headache.

Less common is the formation of scabs in the nasal cavity, nosebleeds, lingering rhinorrhea and nasal congestion, lacrimation, sore throat, hoarseness, coughing, lethargy, dizziness, nausea or vomiting, stomach pain, loss of taste or smell.

Rarely - candidiasis of the nasal cavity and pharynx, atrophic rhinitis, ulceration of the nasal mucosa, perforation of the nasal septum,conjunctivitis, increased intraocular pressure, glaucoma, cataracts, muscle pains, shortness of breath, allergic reactions, tinnitus.

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 GCS, oppression of the hypothalamic-pituitary-adrenal system is possible.

Interaction:

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

Special instructions:

The drug is not intended for arresting bronchospasm. With prolonged use of the drug intranasal, regular visits to the ENT doctor are necessary to monitor the condition of the nasal mucosa.

Not intended for use in ophthalmology. You should regularly monitor the function of the adrenal glands (so as not to miss the symptoms of hypercorticism). Newborns, whose mothers used GK during pregnancy,should be carefully examined to identify possible hypofunction of the adrenal glands.

In case of development of local infections of the nose or pharynx, mometasone gradually cancel. Treatment of children is carried out under strict indications and under medical supervision, as it is possible to develop systemic side effects.

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 (Mometasonum)