Mometasone-Akrikhin 0.1% 30 g cream for external use
Description
The ointment for external use is homogeneous, white or almost white.
Compound
1 g
mometasone furoate 1 mg
Excipients: propylene glycol - 120 mg, liquid paraffin (mineral oil) - 120 mg, emulsion wax - 50 mg, glyceryl monostearate 40-55 (glyceryl monostearate) - 20 mg, purified water - 30 mg, concentrated phosphoric acid (phosphoric acid, orthophosphoric acid) - up to pH 4.01.0, soft white paraffin (white petrolatum) - up to 1 g.
Package
5 g - aluminum tubes (1) - cardboard packs.
15 g - aluminum tubes (1) - cardboard packs.
30 g - aluminum tubes (1) - cardboard packs.
pharmachologic effect
GCS for inhalation and intranasal use. Has anti-inflammatory and anti-allergic effects.
The mechanism of antiallergic and anti-inflammatory action is due to the ability to inhibit the release of inflammatory mediators. Increases the production of lipomodulin, which is an inhibitor of phospholipase A, which causes a decrease in the release of arachidonic acid and, accordingly, inhibition of the synthesis of arachidonic acid metabolic products - cyclic endoperoxides, prostaglandins. Prevents the marginal accumulation of neutrophils, which reduces inflammatory exudate and the production of lymphokines, inhibits the migration of macrophages, and leads to a decrease in the processes of infiltration and granulation. Reduces inflammation by reducing the formation of a chemotaxis substance (impact on late allergy reactions), inhibits the development of an immediate allergic reaction (due to inhibition of the production of arachidonic acid metabolites and a decrease in the 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.
When studied in preclinical models, mometasone reduced the accumulation of inflammatory cells (including eosinophils), penetrated into the walls of the upper and lower respiratory tract, and also improved lung function after a challenge test. Mometasone decreased the number of lymphocytes and the concentration of mRNA for the cytokines IL-4 and IL-5.
In studies with provocative tests with the application of antigens to the nasal mucosa, high anti-inflammatory activity of the drug was demonstrated, both in the early and late stages of the allergic reaction. This was confirmed by a decrease (compared to placebo) in histamine levels and eosinophil activity, as well as a decrease (compared to baseline) in the number of eosinophils, neutrophils and epithelial cell adhesion proteins
Pharmacokinetics
After inhalation, the systemic bioavailability of mometasone is low, in part due to the low absorption and significant first-pass metabolism when mometasone is swallowed. In various studies assessing the effects of mometasone at steady state when administered by inhalation, as well as after a single intravenous administration, absolute bioavailability was approximately 16% in healthy patients and approximately 10% in patients with bronchial asthma. When used in recommended doses, the plasma concentration of mometasone is near or below the detection threshold (50 pg/ml). As a result, it is impossible to determine either T1/2 or Vd of mometasone after inhalation. Excreted in urine and bile.
Indications
For inhalation use:
basic therapy for bronchial asthma of any severity; COPD
For intranasal use:
treatment of seasonal and year-round allergic rhinitis in adults, adolescents and children over 2 years of age; acute sinusitis or exacerbation of chronic sinusitis in adults (including the elderly) and adolescents over 12 years of age (as an auxiliary therapeutic agent in antibiotic treatment); acute rhinosinusitis with mild to moderate symptoms without signs of severe bacterial infection in patients aged 12 years and older; prevention of seasonal allergic rhinitis of moderate and severe course in adults and adolescents from 12 years of age; nasal polyposis, accompanied by impaired nasal breathing and sense of smell in adults.
Dosage regimen
The dosage regimen is set individually, depending on the indications, the age of the patient, the route of administration, and the dosage form used.
Side effect
From the respiratory system:
with inhalation use for the treatment of bronchial asthma, the development of bronchospasm and an increase in the amount of wheezing in the lungs may occur immediately after inhalation; with intranasal use, nosebleeds, pharyngitis, a burning sensation in the nose, and sneezing are possible; irritation of the nasal mucosa; very rarely with intranasal use - cases of perforation of the nasal septum.
Systemic effects (especially when used in high doses and for a long time):
with inhalation use - suppression of the function of the adrenal cortex, growth retardation in children and adolescents, demineralization of bone tissue, glaucoma, increased intraocular pressure (occurs in some cases with intranasal use), the development of cataracts.
Allergic reactions:
with post-marketing use in isolated cases, manifestations of hypersensitivity such as rash, itching, angioedema and anaphylactic reaction. Worsening of asthma has been reported, which may include cough, shortness of breath, wheezing and bronchospasm
Other:
With intranasal use, headache is possible.
Contraindications for use
Hypersensitivity to mometasone.
For inhalation use:
children's age up to 12 years.
For intranasal use:
recent surgery or trauma to the nose with damage to the mucous membrane of the nasal cavity - before the wound heals (due to the inhibitory effect of GCS on the healing processes); childhood and adolescence up to 18 years with nasal polyposis; children under 12 years of age with acute sinusitis or exacerbation of chronic sinusitis; children under 2 years of age with seasonal and year-round allergic rhinitis.
Use during pregnancy and breastfeeding
There have been no adequate and well-controlled studies of the use of mometasone during pregnancy. After inhalation use, the plasma concentration of mometasone furoate is very low; Fetal exposure is likely to be extremely low and the likelihood of reproductive toxicity is very low.
It is not known whether mometasone is excreted in breast milk.
Inhalation or intranasal use of mometasone during pregnancy and breastfeeding is possible only if the expected benefit to the mother outweighs the potential risk to the fetus or infant.
Newborns whose mothers received corticosteroids during pregnancy should be monitored for possible symptoms of adrenal insufficiency.
special instructions
Carefully
Mometasone should be used for tuberculosis infection (active or latent) of the respiratory tract, untreated fungal, bacterial, systemic viral infection or infection caused by Herpes simplex with eye damage (as an exception, the drug can be prescribed for these infections as directed by a doctor), the presence of untreated local infection involving the nasal mucosa in the process.
Mometasone is not intended for rapid relief of bronchospasm.
With long-term intranasal use of mometasone, periodic examination of the nasal mucosa by an ENT doctor is necessary. If a local bacterial or fungal infection of the nose or throat develops, it is recommended to stop treatment and begin special treatment. Irritation of the mucous membrane of the nasal cavity and pharynx that persists for a long time is an indication for discontinuation of the drug.
When switching from GCS for systemic use to inhaled or intranasal use of mometasone, special caution is required due to the possible risk of developing adrenal insufficiency. After discontinuation of systemic corticosteroids, it takes several months to restore the function of the hypothalamic-pituitary-adrenal axis.
During stressful situations, including trauma, surgery, infectious diseases or a severe attack of bronchial asthma, patients who have previously received corticosteroids for systemic use require an additional prescription of a short course of systemic corticosteroids, which are then gradually withdrawn as symptoms subside.
When switching from systemic corticosteroids to inhaled or intranasal use of mometasone, the manifestation 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 from systemic corticosteroids, including muscle and/or joint pain, depression, and fatigue, despite the fact that pulmonary function tests are stable or even improving. If signs of adrenal insufficiency occur, the dose of GCS for systemic use should be temporarily increased, and subsequently discontinued more gradually.
As with the use of other inhaled drugs, paradoxical bronchospasm may develop after the use of mometasone. In this case, immediate use of inhaled fast-acting bronchodilators is required, followed by discontinuation of mometasone and the appointment of alternative therapy.
Patients receiving corticosteroids or other immunosuppressants should be advised to avoid contact with patients with certain infections (chicken pox, 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 hypothalamic-pituitary-adrenal axis suppression, recommended doses should not be exceeded, and the dose of mometasone should be titrated to the minimum effective dose in each patient.
When using mometasone, it should be taken into account that the effect on cortisol production may vary between patients.
The occurrence of candidiasis may require appropriate antifungal therapy or discontinuation of mometasone.
Use in pediatrics
It is recommended to regularly monitor the growth of adolescents receiving long-term therapy with mometasone. If growth slows, therapy should be reconsidered in order to reduce the dose of mometasone to the minimum effective dose to control the symptoms of the disease.
In placebo-controlled clinical studies in children with intranasal use of mometasone at a dose of 100 mcg/day for a year, no growth retardation was observed.
Mometasone-Akrikhin cream for external use 0.1% 15g
Compound
Active substance: mometasone furoate - 1 mg. Excipients: hexylene glycol, glyceryl monostearate 40-55, cetostearyl alcohol, macrogol 20 cetyl stearate, white wax, titanium dioxide, aluminum starch octenyl succinate, diluted phosphoric acid, white petrolatum, purified water.
Pharmacokinetics
Absorption of the drug when applied externally is negligible. 8 hours after application to intact skin (without an occlusive dressing), 0.7% mometasone is detected in the systemic circulation.
Indications for use
Inflammatory phenomena and itching in dermatoses amenable to glucocorticosteroid therapy.
Contraindications
Hypersensitivity to mometasone;
rosacea; perioral dermatitis; bacterial, viral (Herpes simplex, Herpes zoster, chicken pox), fungal skin infection; tuberculosis; syphilis; post-vaccination reactions; pregnancy (use on large areas of skin, long-term treatment); lactation period (use in high doses and/or for a long time); children under 2 years of age. Use with caution on the face and intertriginous skin, use occlusive dressings, and use over large areas of skin and/or for long periods of time (especially in children).
Directions for use and doses
Apply externally. The dosage regimen is set individually, depending on the indications, the age of the patient, and the dosage form used.
Storage conditions
Store out of the reach of children at a temperature of 15°C to 25°C.
Best before date
2 years. Do not use after expiration date
special instructions
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 Cushing's syndrome. Avoid getting the cream into your eyes.
Propylene glycol, which is part of the drug, may cause irritation at the site of application. In such cases, you should stop using the cream and prescribe appropriate treatment.
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 stopping it completely.
Use in pediatrics
The safety and effectiveness of the cream when applied topically to children for periods greater than 6 weeks have not been studied.
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 axis 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. In children from 6 months to 2 years, the course of treatment should not exceed 5 days.
Description
Glucocorticosteroid for local use.
Pharmacodynamics
Mometasone is a synthetic glucocorticosteroid (GCS) with anti-inflammatory, antipruritic and antiexudative effects. GCS induces the release of phospholipase A2 inhibitory proteins, collectively known as lipocortins, which control the biosynthesis of inflammatory mediators such as prostaglandins and leukotrienes by inhibiting the release of their common precursor, arachidonic acid.
Side effects
Infections and infestations: rarely - folliculitis, secondary infection.
From the skin and subcutaneous tissues: rarely - irritation and dryness of the skin, burning sensation, itching, hypertrichosis, acne, hypopigmentation, perioral dermatitis, allergic contact dermatitis, secondary infection, skin maceration, signs of skin atrophy, stretch marks, prickly heat, formation papules, pustules.
From the nervous system: frequency has not been established - paresthesia.
When using external forms of GCS for a long time and/or to treat large areas of skin, or using occlusive dressings, especially in children and adolescents, side effects characteristic of systemic GCS may occur, including adrenal insufficiency and Cushing's syndrome.
Use during pregnancy and breastfeeding
The safety of using the cream during pregnancy and lactation has not been studied. Glucocorticosteroids penetrate the placental barrier. Long-term treatment and the use of large doses during pregnancy should be avoided due to the risk of negative effects on fetal development. Glucocorticosteroids are excreted in breast milk. In cases where GCS is intended to be used in large doses and/or for a long time, breastfeeding should be stopped.
Overdose
Symptoms: inhibition of the function of the hypothalamic-pituitary-adrenal system, including secondary adrenal insufficiency.
Treatment: symptomatic, if necessary - correction of electrolyte imbalance, drug withdrawal (with long-term therapy - gradual withdrawal).
