Pharmacological properties
Mechanism of action. Topical glucocorticosteroids act as anti-inflammatory agents through complex mechanisms to suppress the late phase of an allergic reaction, including reducing mast cell density, reducing chemotaxis and eosinophil activation, decreasing cytokine production by lymphocytes, monocytes, mast cells and eosinophils, and inhibiting arachidonic acid metabolism.
Pharmacodynamic properties.
Topical glucocorticosteroid with anti-inflammatory, antipruritic and vasoconstrictive properties.
Pharmacokinetics
Absorption.
Topical glucocorticosteroids can be systemically absorbed from intact healthy skin. The degree of penetration of topical glucocorticosteroids through the skin is determined by many factors, including transport and the integrity of the epidermal barrier. Occlusion, inflammation, and / or other skin diseases can also increase penetration through the skin.
In a single study, it was found that the average peak plasma concentration of clobetasol propionate (0.63 mg / ml) is reached 8 hours after repeated application (13 hours after the first application) to healthy skin 30 g of clobetasol propionate in the form of 0.05% ointments.
10 hours after the application of the second dose (30 g) of clobetasol propionate in the form of a cream, its average peak plasma concentration slightly exceeds that when using the ointment.
In another study, 3 hours after a single application of 25 g of 0.05% ointment of clobetasol propionate in patients with psoriasis and eczema, the average maximum plasma concentration of the drug is 2.3 mg / ml and 4.6 mg / ml, respectively.
Distribution.
The use of pharmacodynamic endpoints to assess the systemic effects of local glucocorticosteroids is necessary because circulating levels are significantly lower than the detection level.
Metabolism.
After absorption through the skin, topical glucocorticosteroids most likely follow the same metabolic pathway as systemic glucocorticosteroids, which are metabolized mainly in the liver.
Breeding.
Topical glucocorticosteroids are excreted through the kidneys. In addition, some glucocorticosteroids and their metabolites are also excreted in the bile.
Indications for use
MERDirmoviyk is a highly active topical topical glucocorticosteroid for use in adults, the elderly and children over 1 year old to alleviate inflammatory manifestations and itching in dermatoses sensitive to glucocorticosteroid therapy.
Namely:
– psoriasis (excluding common plaque psoriasis);
– eczema (various forms);
– lichen planus;
– discoid lupus erythematosus;
– skin diseases resistant to therapy with less active glucocorticosteroids.
Dosage and administration
The ointment is suitable for dry, lichenized or scaly lesions.
Adults, elderly and children over 1 year old.
Apply a thin layer and carefully rub the required amount of the drug on the affected areas of the skin 1 or 2 times a day until improvement occurs for no more than 4 weeks. Then you should review the frequency of use or switch to therapy with a less powerful drug.
Enough time is needed to absorb after each use of the drug, before using emollient.
In case of exacerbations, repeated short courses of treatment with MERDirmoviyk drugs can be performed.
With more persistent skin lesions, especially with hyperkeratosis, if necessary, you can enhance the effect of MERDirmoviyk by applying a plastic film to the treated surface.
Typically, to obtain a positive result, a hermetic dressing is applied overnight. The achieved effect is supported by simple application of the drug to the skin without applying a bandage.
If the condition worsens or there are no obvious improvements within 2-4 weeks, treatment and diagnosis should be reviewed.
Treatment should not last more than 4 weeks. If it is necessary to continue treatment, it is necessary to switch to therapy with less active drugs.
The maximum weekly dose should not exceed 50 g / week.
Atopic dermatitis (eczema)
Upon reaching control, you should gradually stop therapy with the MERDirmoviyk ointment and switch to maintenance therapy with emollients.
With a sharp cessation of MERDirmoviyk therapy, a resumption of symptoms of previously existing dermatoses may occur.
Persistent dermatoses.
Patients with frequent relapses.
After effective treatment of an acute episode with a long course of the drug,
MERDirmoviyk can be prescribed in an intermittent mode (1 time per day, 2 times a week, without dressing), in order to reduce the frequency of relapses. The drug should be applied to all previously affected areas of the body or to areas of the body of a possible development of relapse. This mode should be used in conjunction with daily intake of emollients.
The patient’s condition, as well as the potential benefits and risks of a long course of treatment should be evaluated on a regular basis.
Children.
MERDirmoviyk is contraindicated in children under the age of one year.
Children are more likely to develop local and systemic adverse reactions as a result of taking topical corticosteroids. Compared with adult patients, in general, children require shorter courses of therapy and less active drugs.
Caution should be exercised when using MERDirmoviyk. The drug must be applied in a minimum effective amount.
Elderly people.
Clinical studies did not reveal differences in responses between elderly patients and young patients. Due to the fact that in elderly patients, decreased liver and kidney function are more common, delayed elimination may occur, with systemic absorption. Therefore, the minimum amount of the drug should be used to achieve the clinical effect in the shortest possible time.
Patients with impaired renal / hepatic function.
In the case of systemic absorption (when applied to a large surface area of the body over a long period), metabolism and elimination processes may be delayed, therefore, the risk of systemic toxicity increases. Therefore, the minimum amount of the drug should be used to achieve the clinical effect in the shortest possible time.
Side effects
The following frequency was used:
Very often: (≥1 / 10),
Often: (≥1 / 100, <1/10),
Sometimes: (≥1 / 1000, <1/100),
Rarely: (≥1 / 10000, <1/1000),
Very rare: (<1/10000), including single cases
Infections and infestations. Very rarely: opportunistic infections;
From the immune system. Very rare: local hypersensitivity reactions
From the endocrine system. Very rare: suppression of the hypothalamic-pituitary adrenal (HPA) axis.
Signs of Cushing’s syndrome: (for example, a moon-shaped face, central obesity), delayed weight gain / growth retardation in children, osteoporosis, glaucoma, hyperglycemia / glucosuria, cataracts, arterial hypertension, weight gain / obesity, decreased endogenous cortisol, allopecia, brittle hair .
From the part of the skin and subcutaneous cells. Often: itching, burning. Sometimes: atrophy of the skin, striae, telangiectasia.
Contraindications
The use of MERDirmoviyk is contraindicated under the following conditions:
– untreated skin infections;
– rosacea (rosacea);
– vulgar acne;
– itching without inflammation.
– perianal and genital itching;
– near-mouth dermatitis;
The use of MERDirmoviyk is contraindicated in dermatoses in children under one year of age, including dermatitis.
Drug interactions
Simultaneous administration of drugs that can inhibit CYP3A4 (for example, ritonavir and itraconazole) inhibit the metabolism of glucocorticosteroids, which leads to an increase in systemic exposure. The degree of interaction depends on the dose and method of administration of glucocorticosteroids and the activity of the CYP3A4 inhibitor.
Compatibility with other drugs. There is no data.
Special instructions
MERDirmoviyk should be used with caution in patients with local hypersensitivity to glucocorticosteroids or to any of the excipients of the drug in history. Local hypersensitivity reactions may resemble conditional symptoms during treatment.
Abrupt withdrawal of treatment can lead to glucocorticosteroid failure.
Risk factors for increased systemic effects:
- Efficacy and dosage form of topical glucocorticosteroids
- Duration of exposure
- Use over a large surface area•
Use on clogged areas of the skin (e.g. diaper rash or under occlusive dressings (in infants, diapers can act as occlusive dressings)
- Increased hydration of the stratum corneum
- Use on thin areas of the skin such as the face
- Use on damaged skin areas or areas with a weakened skin barrier
- Compared with adults, children and infants can absorb a proportionally larger amount of topical glucocorticosteroids, and therefore are more susceptible to the development of systemic side effects. This is due to the fact that in children the skin barrier is not sufficiently developed, and the ratio of skin surface area to weight is much greater than in adults.
Children
In infants and children under 12 years of age, if possible, long-term continuous treatment with topical glucocorticosteroids should be avoided, as this can lead to suppression of adrenal function. Children are more susceptible to the development of atrophic changes due to the use of topical glucocorticosteroids. If it is necessary to use MR Dirmoviyk in children, one should limit the intake to several days, the doctor’s supervision is also required at least once a week.
Infection risk in occlusions
Warm, moist conditions created by applying an occlusive dressing contribute to the occurrence of bacterial infection, so be sure to clean the skin before applying a new dressing.
Use for Psoriasis
Topical glucocorticosteroids should be used with caution in patients with psoriasis, as there have been cases of relapse, drug resistance, generalized pustular form of the disease, local or systemic toxic reactions due to impaired skin barrier function.
During treatment, such patients should be under the constant supervision of a physician.
Associated infections
When attaching a secondary infection, appropriate antibacterial therapy should be carried out. With any signs of generalization of the infection, it is necessary to stop therapy with topical glucocorticosteroids and conduct appropriate treatment with antibacterial drugs.
Chronic foot ulcer
Topical glucocorticosteroids are sometimes used to treat dermatitis around chronic leg ulcers. However, such use may be associated with a higher incidence of local hypersensitivity reactions and an increased risk of local infection.
Face application
Applying on the face is undesirable, since this area is more susceptible to atrophic changes. When taking the drug on the face, treatment should be limited to a few days.
Eyelids applications
If it is necessary to apply MERDirmoviyk on the skin of the eyelids, the product should be avoided in the eyes, as in some cases this can provoke the development of glaucoma and cataracts.
Use during pregnancy and lactation
Fertility There are no data on the impact of topical glucocorticosteroids on fertility in humans. Clobetasol, administered subcutaneously to rats, did not affect mating, however, fertility decreased with the highest dose.
Pregnancy
Data on the use of MERDirmoviyk in pregnant women are limited.
Topical use of topical glucocorticosteroids in animals during pregnancy can cause fetal abnormalities. The clinical significance of this phenomenon for humans has not been established. The use of MERDirmoviyk during pregnancy should be considered only if the expected benefit to the mother outweighs the risk to the fetus. A minimum dosage and a minimum duration should be prescribed.
Lactation. The safety of the use of MERDirmoviyk during lactation is not established.
There is no evidence that the use of topical glucocorticosteroids can lead to systemic absorption sufficient to produce a detectable amount in breast milk. Reception MERDirmoviyk in the period of a lactation should be considered only if the expected benefit for mother exceeds risk for the child.
If MERDirmoviyk is used during lactation, the drug should not be used in the chest area to avoid accidental ingestion in the baby’s mouth.
Influence on the ability to drive a car and work with mechanisms:
Not a single study has been conducted to study the effect of MERDirmoviyk on the ability to drive vehicles and other mechanisms. In accordance with the safety profile MERDirmoviyk, there is no likelihood of a negative impact on the ability to drive vehicles and other mechanisms.
The drug should not be used after the expiration date and should be stored out of the reach of children.
Overdose
Symptoms and signs: when applied topically, MERDirmoviyk is absorbed in amounts sufficient to develop systemic effects. The development of acute overdose is unlikely, however, in case of chronic overdose or improper use, symptoms of hypercorticism may develop.
Treatment: in case of an overdose, a gradual withdrawal of the MERDirmoviyk is necessary by reducing the frequency of use or replacing it with a less active glucocorticosteroid, due to the risk of developing glucocorticosteroid insufficiency.
Release form
Ointment 15 g, 20 g and 25 g in tubes.
Storage conditions
In a dry, dark place at a temperature of no higher than 25°C.
Shelf life
2 years.
Pharmacy sales terms
On prescription.
