Mometasone Furoate Ointment Utmost importance in the treatment of dermatoses steroidchuvstvitelnyh has rationally chosen, standards-based outdoor therapy. The problem of treating chronic dermatosis occurring at present is of particular scientific and practical importance in connection with the increasing incidence, especially of allergic skin diseases with inflammatory components, increased severe clinical forms, disability patients, as well as social disadaptation patients.
In 1952, M. Zikegdeg first reported on the successful external application of hydrocortisone acetate. For more than a half century of the use of topical corticosteroids to millions of patients has been greatly improved quality of life, but inappropriate use and self-medication can lead to the implementation of side effects. Today, the dermatologist has several dozens of topical corticosteroids, anti-inflammatory, antiallergic, vasoconstrictor and anti-proliferative effect. The choice of corticosteroid agent in entering the pharmaceutical market of new drugs often becomes a doctor for quite a challenge, since the indications for the use of topical corticosteroids in common chronic dermatosis occurring is not fully standardized.
Under the conditions of entry into the Ukrainian market of new topical corticosteroids pediatricians, internists, family doctors, allergists and often dermatovenerology prescribe them without taking into account the stage of the inflammatory process, shape and activity of the pathological process. Clinical practice shows that there are a number of objective and subjective reasons rather frequent use of topical steroids of high activity. Today one of these main reasons are social and economic problems, not to significantly change the approach to the treatment of patients with dermatoses: most of them can not buy a more expensive modern topical anti-inflammatory external means. Often, patients immediately appoint fluorinated corticosteroids, which cost much less than the cost of safer new generation of hormonal drugs. This leads to the emergence of resistant and complicated forms of various dermatoses, and often – to the irreversible manifestations of side effects of glucocorticosteroids.
Today it is impossible to imagine a treatment for patients with severe dermatoses without external medicines that contain corticosteroids, so the main objective is to maximize the reduction in the risk of side effects while maintaining their effectiveness. The most important processes determining the entire spectrum of biological activity and efficacy of topical steroids include the receptor mechanisms of action of steroids on proteinsintetiche-sky apparatus of complementary cells, the metabolism of steroids in the skin and other organs, transdermal penetration and interaction with steroid transport proteins.
Effectiveness of the drug depends on the speed, strength and duration of steroid binding to receptors, which are determined by the active substance and its dosage forms. Local anti-inflammatory effect of glucocorticoids in the skin is achieved with the participation of different ways, but most important is a mechanism mediated by cytosolic receptors of glucocorticoids. The mechanism consists in the fact that gormonretseptorny complex, penetrating into the core of the target cells of skin, increases the expression of genes coding for the synthesis of lipokortinov that inhibit the activity of lysosomal phospholipase A2. This leads to a decrease in the release of membrane phospholipids of arachidonic acid and the formation of her inflammatory mediators – prostaglandins and leukotrienes.
Glucocorticoids contribute to neutralize the effects of histamine and serotonin in the skin, reduce the sensitivity of nerve endings of neuropeptides and histamine. Drugs in this group inhibit the synthesis of interleukin-1, interleukin-6, tumor necrosis factor and other proinflammatory cytokines, and migration of eosinophils and proliferation of T-lymphocytes may reduce the vascular permeability and exert vasoconstrictor effect potentsiruemy catecholamines. Topical steroids act on the early and late phase allergic reaction and have potent anti-inflammatory and membrane stabilizing effects. Thus, when the local use of ointments and creams that contain steroids, it is possible to achieve the main therapeutic goals – relief of itching, reduction of inflammatory reactions in the skin. Glucocorticoids inhibit the synthesis of glycosaminoglycans, collagen and elastin in the epidermis reduces the number of vnutriepidermalnyh macrophages (Langerhans cells) in the dermis – mast cells, and suppress the irrational use of the functionality of the hypothalamus – pituitary – adrenal glands, the immune reaction, ie have an adverse side effect as systemically and locally.
Penetration into the skin of glucocorticosteroid carried out in three main ways: through the stratum corneum of the epidermis, hair follicles and sebaceous and sweat glands. Transepidermal penetration – the main route of penetration of topical glucocorticoids. Penetration of corticosteroids through the skin is determined by the following factors: the site of application of the drug, patient’s age, the properties of the active components, the basis of preparation, method of application, stage of the pathological process in the skin.
The depth and rate of penetration of the drug depends on the lipophilicity of the compound and the dosage form (ointment or cream). The more lipophilic a corticosteroid, to a greater concentration accumulates in the cells of the skin and the more slowly out into the blood. The greatest degree of penetration of steroids provides ointment bases, moderate – cream. Total resorption of corticosteroids through the skin in most anatomical regions is 3-10%. Systemic effects of glucocorticoids depend on the degree of binding molecules of the drug in contact with the blood transport protein transkortinom (stronger bond, the weaker the effect of the system) and the rate of metabolism of steroids (the higher the speed, the less systemic effect).
To date, adopted worldwide classification of local corticosteroids does not exist. We adhere to the European classification of topical steroids, according to which anti-inflammatory activity can be identified 4 classes.
Preparations of hydrocortisone acetate, related to generation, and I have the most reasonable act, now in dermatological practice almost do not apply. Much more frequently used topical drugs II generation, which have average severity of effect. III generation represented a significant number of topical corticosteroids, preferably halogenated, a moderate, strong or very strong anti-inflammatory action. Drugs in this group are appointed often clinicians of all specialties, which are sometimes ignored by certain features of the mechanism of action of fluorinated steroids, which often leads to unwanted local side effects (skin atrophy, telangiectasia, perioral dermatitis, steroid acne, and hypertrichosis, the activation of viral, fungal or bacterial infection, etc.). In this regard, the safer natural corticosteroids and synthetic fluorinated analogues, which are balanced influence on gene expression and did not cause the death of sensitized cells of the hypothalamus and the thymus.
Stage, the localization of the lesions and the severity of the pathological process in the skin determine the choice of topical glucocorticosteroids. The most rational is to use the least active among the effective means. However, the application at the beginning of therapy is too weak drug can lead to worsening or persistent flow of dermatosis and violations of the therapy. At the same time, if the patient initially appoint a highly active corticosteroid short course with no side effects, and among its advantages should be noted the high lipophilicity, rapid penetration through the epidermis and a good local effect. Issue Mometasone in the form of ointments and creams significantly expands the possibilities of its application. Cream Mometasone “gives the best effect in the presence of exudate, soak and large erosive surfaces. Ointment “mometasone” more effective when allergodermatosis with marked lichenification, scaling, and dryness of the skin. To achieve the clinical effect of only one application of the drug on the lesion. Compared with other topical steroids mometasone has a similar group of high local activity that allows us to assign it to class 3 in potency, has a low systemic effect and uroplanovogo reduce the amount of therapy, it also may develop a withdrawal syndrome in the form of exacerbation. Much better enforced regimen with the possibility of single daily application of topical corticosteroid. Some researchers believe that treatment with highly active drug short-course (3 days) may not yield the clinical effectiveness of therapies, involving frequent and prolonged use of low-level glucocorticosteroid.
To date, we can use a topical glucocorticosteroid drug, which has strong anti-inflammatory effect of low systemic bioavailability, rapid onset and is characterized by minimal local and systemic side effects. This drug is mometasone, produced by “Pharmak. Mometasone successfully combines the positive features of its predecessors: It has a high activity, comparable to the potency of fluorinated steroids and minimalven security, similar to a weak corticosteroids.
A high clinical activity Mometasone in the treatment of chronic inflammatory skin diseases like atopic dermatitis, psoriasis, eczema and dermatitis. In the study of therapeutic activity Mometasone under our supervision there were 65 patients aged 5 to 62 years (36 women and 29 men). On nosological forms the patients were divided into groups: Group 1 – atopic dermatitis (25 patients), Group 2 – psoriasis (19 patients), Group 3 – eczema (12 patients), 4 – dermatitis (9 patients).
All patients had previously received desensitizing, anti-inflammatory, sedative, enzymes and other symptomatic treatment, depending on the nosology. The use of local corticosteroids in the history indicated 97% of patients. Mometasone was included in the combined therapy according to a particular disease.
Among patients with atopic dermatitis were 16 women and 9 men, the duration of the disease most often corresponded to age, ie dermatosis started on the first year of life. In 14 patients with pathological changes of the skin located on the “favorite” sites – in the elbow and popliteal folds, and in 2 – in the skin of distal upper extremity, 7 patients had a rash around the mouth. In 2 patients in the pathological process was diffusely involved skin of the face, back and side of the neck, upper chest. On the skin lesions were defined erythema, papules, expressed lihenifikatsiya, multiple excoriations and desquamation. Patients worried about the strong attacks of itching. In patients with atopic dermatitis, decrease redness, peeling, itching, marked by 4-6 days of treatment with an ointment or cream “mometasone”. For 10-12 days in 92% of patients achieved clinical cure or significant improvement in the pathological process.
The group of patients with psoriasis included 11 men and 8 women. The disease duration ranged from 6 months to 25 years. In 15 of these patients diagnosed with psoriasis vulgaris (10 cases – an advanced stage, 6 – stationary), in 3 – exudative, and 1 – erythroderma. In 7 patients with cutaneous process has been limited, 12 – circulated. Eruptions were represented by typical psoriatic papules and plaques with severe and / or moderate infiltration of scales silvery-white on the surface, there was a positive psoriatic triad. In patients with advanced disease process was accompanied by disseminated rash, located on the skin of the trunk, upper and lower extremities, the scalp, single plaques were localized on the skin of the neck and face. Subjectively, 10 patients bothered by itchy skin varying degrees of severity.
All patients received combined therapy and externally cream or ointment “mometasone” after peeling treatment. The treatment of patients with psoriasis decrease the color intensity of papules, scaling, and reduction of pruritus was noted by 4-6 days of treatment, but to the 14-18 day process regressed in 58% of patients, a significant improvement in skin process was observed in 32% of patients, ay 10% – clinical improvement.
Group of patients with chronic eczema comprised 12 people (9 women and 3 men) with disease duration from 1 year to 12 years. Pathological process of skin rashes was submitted, which were located mainly on the palms and soles, where there were lesions with the presence of vesicles, get wet, infiltration, scales, crusts, deep fissures, excoriation, only 2 patients process was widespread. Eczema patients receiving combined therapy and Cream Mometasone. Improvement was noted at 2-5 days of treatment. At 7-10 days in 58% of patients in this group, we observed an offensive clinical remission in 42% – a significant improvement.
In 9 patients with dermatitis (in 5 men and 4 women), skin process is localized in different parts of the skin, characterized by limited acute hyperemia, papules, excoriations, and sometimes weeping. 5 patients were diagnosed with a simple contact dermatitis from 4 – atopic dermatitis. Complete recovery observed at 3-6 days of treatment in 78% of patients, while the rest, a significant improvement.
In the treatment of mometasone side effects have not been identified. All participants underwent laboratory tests (complete blood count, general urinalysis, biochemical blood test) before, during and after the prescribed therapy. Significant deviations from the physiological norm in the treatment process have been identified, which indicates high safety of the drug.
Thus, the results of our clinical studies suggest that mometasone, which has anti-inflammatory, antipruritic, vasoconstrictor and antiproliferative effects, a drug of choice in the treatment of chronically occurring steroid-responsive dermatoses. No side effects if used correctly, safety, rapid onset of a positive clinical effect generic dosage forms, almost the exclusion of systemic action, the appointment of children from 2 years of age can be recommended mometasone as a modern local glucocorticosteroid.
