Mometasone furoate (Mometasoni furoas)
The drug interacts with intracellular glucocorticoid receptors, promoting the release of the receptor from connection with 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, which regulate the expression of many immune system proteins, resulting in 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 A2-mediated hydrolysis of membrane phospholipids in damaged tissues prevents the formation of arachidonic acid. Impaired formation of arachidonic acid actually means inhibition of prostaglandin synthesis, since arachidonic acid is a substrate for further metabolism through the cyclooxygenase pathway, as well as through the lipoxygenase pathway with a corresponding 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 at the site of inflammation, including pro-inflammatory prostaglandins E2 and I2.
3. Mometasone furoate inhibits the expression of intercellular adhesion molecules in the endothelium of blood vessels, disrupting the penetration of neutrophils and monocytes into the site of inflammation. After the administration of glucocorticoids, an increase in the concentration of neutrophils in the blood is noted (due to their receipt from the bone marrow and due to the restriction of migration from the blood vessels). This causes a decrease in the number of neutrophils at the site of inflammation.
Mometasone furoate inhibits the transcription of genes for cytokines 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 noted is a decrease in the transcription rate and increased degradation of receptor genes for IL-1 and IL-2, inhibition of transcription of metalloproteinase genes (collagenase, elastase, etc.) involved in increasing the permeability of the vascular wall, in the processes of scarring and destruction of cartilage tissue in joint diseases.
The immunosuppressive effect is due to inhibition of transcription of DNA encoding the major histocompatibility complex, proinflammatory cytokines and inhibition of T-lymphocyte proliferation. 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 breakdown of components of the complement system.
The antiallergic effect is associated with inhibition of the synthesis of allergy mediators, degranulation of mast cells and the release of allergy mediators, and therefore it is effective for immediate allergic reactions.
Mometasone Sandoz 50mcg/dose nasal spray 60doses 10g (Sandoz)
As with any long-term treatment, patients using Mometasone Sandoz® Nasal Spray for several months or longer should be periodically examined by a doctor for possible changes in the nasal mucosa. It is necessary to monitor patients receiving intranasal corticosteroids for a long time.
Possible development of growth retardation in children. If growth retardation is detected in children, it is necessary to reduce the dose of intranasal corticosteroids to the lowest that allows for effective control of symptoms. In addition, the patient should be referred to a pediatrician for consultation.
If a local fungal infection of the nose or throat develops, it may be necessary to discontinue Mometasone Sandoz® nasal spray therapy and undergo special treatment. Irritation of the nasal and pharyngeal mucosa that persists for a long time may also serve as a reason to discontinue treatment with mometasone.
In placebo-controlled clinical trials in children, when a nasal spray containing mometasone was used at a daily dose of 100 mcg for a year, no growth retardation was observed in children. With long-term treatment with a nasal spray containing mometasone, no signs of suppression of the function of the hypothalamic-pituitary-adrenal axis were observed.
Patients who switch to treatment with Mometasone Sandoz® nasal spray after long-term treatment with systemic GCS require special attention. Withdrawal of systemic corticosteroids in such patients can lead to adrenal insufficiency, the subsequent recovery of which may take up to several months. If signs of adrenal insufficiency appear, systemic corticosteroids should be resumed and other necessary measures taken.
When using intranasal corticosteroids, systemic side effects may develop, especially with long-term use in high doses. The likelihood of developing these effects is much less than with the use of oral corticosteroids.
Systemic side effects may vary in individual patients and depending on the glucocorticosteroid drug used. Potential systemic effects include Cushing's syndrome, characteristic Cushingoid signs, adrenal suppression, growth retardation in children and adolescents, cataracts, glaucoma, and less commonly a number of psychological or behavioral effects including psychomotor hyperactivity, sleep disturbance, anxiety, depression, or aggression (especially in children).
During the transition from treatment with systemic corticosteroids to treatment with Mometasone Sandoz® nasal spray, some patients may experience initial withdrawal symptoms of systemic corticosteroids (for example, joint and/or muscle pain, fatigue and depression), despite a decrease in the severity of symptoms associated with damage to the nasal mucosa. Such patients must be specifically reassured of the advisability of continuing treatment with Mometasone Sandoz® nasal spray.
The transition from systemic to local GCS can also reveal allergic diseases such as allergic conjunctivitis and eczema that already existed but were masked by systemic GCS therapy.
Patients treated with glucocorticosteroids have a potentially reduced immune responsiveness and should be warned of their increased risk of infection if exposed to patients with certain infectious diseases (eg, chickenpox, measles), as well as the need for medical advice if such exposure occurs .
If signs of a significant bacterial infection appear (for example, fever, persistent or sharp pain on one side of the face or toothache, swelling in the orbital or periorbital area), immediate medical consultation is required.
When using a nasal spray containing mometasone, there are no signs of atrophy of the nasal mucosa for 12 months. In addition, mometasone furoate tends to help normalize the histological picture when examining biopsies of the nasal mucosa.
The effectiveness and safety of mometasone have not been studied in the treatment of unilateral polyps, polyps associated with cystic fibrosis, and polyps that completely occlude the nasal cavity. If unilateral polyps of an unusual or irregular shape are detected, especially those that are ulcerated or bleeding, additional medical examination is necessary.
The development of visual disturbances has been reported with the use of both systemic and local corticosteroids. If the patient experiences blurred vision or other visual disturbances, the patient should be referred to an ophthalmologist to determine possible causes, which may include the development of cataracts, glaucoma, or rarer diseases (eg, central serous chorioretinopathy) that have been reported with the use of systemic and topical corticosteroids .
Special precautions when disposing of unused medicinal product
The bottle must be discarded after the specified number of uses or 2 months from the date of first use.
MOMETASONE (Mometasone)
When applied to large areas of skin for a long time, especially when using occlusive dressings, systemic action of GCS may develop. Given this, patients should be monitored for signs of suppression of the function of the hypothalamic-pituitary-adrenal system and the development of Itsenko-Cushing syndrome.
Avoid contact of MOMETASONE with the eyes.
It should be borne in mind that GCS can change the manifestations of some skin diseases, which can complicate the diagnosis. In addition, the use of GCS may cause a delay in wound healing.
With long-term therapy with GCS, sudden cessation of therapy can lead to the development of rebound syndrome, manifested in the form of dermatitis with intense redness of the skin and a burning sensation. Therefore, after a long course of treatment, the drug should be discontinued gradually, for example, by switching to an intermittent treatment regimen before. how to stop it completely.
With systemic and local (including intranasal, inhalation and intraocular) use of GCS, visual impairment may occur. If a patient has symptoms such as blurred vision or other visual disturbances, the patient should be advised to consult an ophthalmologist to identify possible causes of visual disturbances, including cataracts, glaucoma or rare diseases such as central serous chorioretinopathy (CSC), which have been observed in a number of cases with systemic and local use of GCS.
Any of the side effects described with systemic use of glucocorticosteroids, including suppression of adrenal function, may also occur with topical use, especially in children.
When treating psoriasis, GCS should be used with caution, since in some cases, relapses of the disease, the development of tolerance to the drug, the risk of generalized pustular psoriasis and the development of local or systemic toxic reactions due to impaired skin barrier function have been reported. If a secondary infection occurs, appropriate antibacterial therapy should be carried out. If there are any signs of infection spreading, it is necessary to stop the external use of GCS and carry out appropriate treatment with antibacterial or antifungal drugs. If there are signs of hypersensitivity or skin irritation associated with the use of the drug, you should stop treatment and consult a doctor. On the skin of the face more often than on other surfaces of the body, after long-term treatment with topical corticosteroids, atrophic changes may appear; the course of treatment in this case should not exceed 5 days. Use with caution in persons with existing atrophic skin changes, especially in the elderly. Care must be taken when applying the drug to the face, folds, natural folds, and areas with thin skin.
Use in pediatrics
Due to the fact that in children the ratio of surface area to body weight is greater than in adults, children are at greater risk of suppressing the function of the hypothalamic-pituitary-adrenal system and developing Cushing's syndrome when using any topical corticosteroids. Long-term treatment of children with GCS can lead to disturbances in their growth and development.
Children should receive the minimum dose of the drug sufficient to achieve an effect.
Long-term use of the drug in children should be carried out under the supervision of a physician. In children, the course of treatment should not exceed 5 days. Occlusive dressings should not be used. Propylene glycol may cause skin irritation, propyl parahydroxybenzoate may cause allergic reactions, and stearyl alcohol may cause local skin reactions (eg, contact dermatitis).
