Locoid crelo, 1 piece, 30 g, 0.1%, emulsion for external use
Locoid® should not be applied to the periorbital area due to the risk of developing glaucoma. In case of systematic contact with the conjunctiva, there is a risk of increasing intraocular pressure.
Lokoid lipokrem® and Lokoid® ointment are not advisable to use on the scalp, as well as in acute inflammation (especially exudative). For the treatment of steroid-sensitive skin lesions localized in the face, folds, genitals, as well as on areas of skin with abundant hair, it is preferable to use Locoid®, cream and Locoid Crelo®.
When the process is localized on the scalp and with exudative inflammation, it is preferable to use Locoid Crelo®.
In cases of resistant disease, for example, when dense psoriatic plaques are localized on the elbows, knees, severe lichenification, infiltration, dryness, hyperkeratosis, it is preferable to use Lokoid®, ointment or Lokoid lipocrem®, if necessary, under occlusive dressings.
It is not advisable to use the drug in the presence of atrophic skin changes.
The risk of local and systemic side effects increases when applied to large areas of the affected area, long-term use, use of occlusive dressings and in childhood.
If there is no effect within 2 weeks of continuous treatment, the diagnosis should be clarified.
As with the use of any GCS, it is advisable to limit the duration of use and the course dose to the minimum sufficient to stop the skin process.
Application in pediatrics.
Can be used in children from 6 months of age. In cases of use of the drug in children, in the face or under occlusive dressings, the duration of treatment should be reduced.
When used in children, the surface area of the skin to which the drug is applied should not exceed 20% of the total.
In childhood, suppression of adrenal function may develop more quickly. In addition, a decrease in growth hormone excretion may occur. When using the drug for a long time, it is necessary to monitor body weight, height, and plasma cortisol levels. In a study in children who received 30–60 g of Lokoid® per week for 4 weeks, in comparison with the use of 1% hydrocortisone ointment, not a single child had dysfunction of the adrenal cortex, i.e. There were no differences between hydrocortisone 17-butyrate and conventional hydrocortisone in this indicator.
Impact on the ability to drive vehicles and operate machinery.
There is no data on the effect of Lokoid® on the ability to drive vehicles and operate machinery.
Lokoid
Lokoid (hydrocortisone 17-butyrate) is a topical synthetic glucocorticosteroid drug for use in dermatological practice. Used to treat eczematous skin lesions, dermatitis, scaly lichen (psoriasis). It has a rapidly developing anti-inflammatory, antiexudative, antipruritic effect. The use of the drug in the doses stated by the manufacturer does not inhibit the hypothalamic-pituitary-adrenal axis. Submaximal and maximum doses of Lokoid when used over a long period (including when using the drug under an airtight bandage) can increase the level of the stress hormone cortisol in the blood, but this does not affect the activity of the pituitary-adrenal system, and after the end of the drug course The secretion of cortisol is normalized as soon as possible. After hydrocortisone is absorbed through the skin, 17-butyrate undergoes a series of metabolic transformations to hydrocortisone and a number of other metabolites. It is excreted from the body by the kidneys and intestines. Lokoid is contraindicated in cases of rosacea, acne, localized on the face, dermatitis in the perioral area, itching in the genital and anal area, dermatitis with concomitant bacterial, viral or fungal infection, individual intolerance to the active or auxiliary components. The use of the drug during pregnancy and breastfeeding is allowed only after assessing the benefit/risk ratio.
Frequency of use: 1-3 times a day. If the clinical situation develops positively, the frequency of dosing is reduced to 1-3 times a week. To improve the absorption of the drug, its application is carried out with repeated massage movements. In case of a pathological process that is resistant to therapeutic effects (for example, in the presence of psoriasis in the elbows and knees), the drug is used under an airtight bandage. The maximum weekly dose is 30-60 g. Adverse effects when using the drug are skin irritation. With prolonged use or application over large areas, Lokoid may provoke the development of systemic side effects characteristic of glucocorticosteroids, however, this drug will have a lower risk than halogenated glucocorticosteroids. Using the drug under a sealed bandage increases the risk of systemic side effects. Lokoid is suitable for use in pediatric practice from the age of six months. If Lokoid is intended to be used on the skin of the face or under an airtight bandage, then the duration of the medication course is recommended to be reduced. When using the drug in pediatric practice, patients may experience inhibition of growth hormone secretion. The use of Lokoid in patients of this age group involves monitoring anthropometric parameters and the level of cortisol in the blood.
The problem of atopic dermatitis (AD) does not lose its relevance due to the high prevalence and increasing number of patients with severe disease. In pediatric clinical practice, blood pressure occupies a leading place and is under the close attention of various specialists [1, 2]. Atopic dermatitis is a systemic allergic disease with a complex pathogenesis and characteristic age-related evolution of clinical and morphological manifestations. It is characterized by a persistent course, frequent exacerbations and insufficient effectiveness of existing treatment methods [3].
Over the years, knowledge about the nature of the disease has been improved and deepened, new concepts of pathogenesis have emerged, and terminology has changed. Today, according to modern views, the development of AD is based on immunological mechanisms and a decrease in the barrier function of the skin as a result of a genetically determined deficiency of filaggrin, leading to disruption of the integrity of the water-lipid mantle, which normally provides protection of the body from external pathogenic factors. Violations of the epidermal barrier make it possible for the allergen to penetrate inside and initiate immunopathological processes in the skin. The main pathomorphological changes that occur in AD occur in the epidermis, affecting the dermis in severe chronic disease.
The immunopathogenesis of AD is caused by impaired differentiation of T-helper cells and the profile of cytokines secreted by cells [4, 5]. When directly exposed to an etiologically significant allergen/antigen, antigen-presenting cells (APCs) are activated – Langerhans cells infiltrating the epidermis, which carry antibodies to immunoglobulin E (IgE) on their surface. The binding of IgE antibodies to Langerhans cells occurs through high- and low-affinity (CD23+) receptors. Activated Langerhans cells migrate to the lymph nodes, which in turn activate Th2 lymphocytes, which secrete proinflammatory cytokines that play a major role in maintaining inflammation in the skin. In the acute stage of AD, the Th2 cell response predominates with an increase in the production of interleukin-4 (IL-4), IL-5, IL-13 and a decrease in the level of interferon γ (IFN-γ), as well as an increase in the level of total and allergen-specific IgE antibodies. In the chronic stage of the disease in patients, the activity of the Th1 response predominates, which is characterized by an increase in the synthesis of IL-12 by macrophages and eosinophils, an increase in the level of IL-8 and IFN-γ - markers of chronic inflammation in the skin. In long-term allergic processes, IL-3 and GM-CSF (granulocyte macrophage colony sulating stimulating factor) play an important role. In the mechanisms of development of AD in recent years, the role of cytokines such as IL-10, IL-19, IL-21, IL-17, IL-28, the source of production of which is not only lymphocytes, but also other cells of the immune system, has been discussed [6– 8].
Epidermal keratinocytes are essential in the development of skin inflammation in patients with AD. High production of the chemokine RANTES was established upon stimulation of these cells with tumor necrosis factor α (TNF-α) and IFN-γ [9]. Keratinocytes of patients with AD are an important source of thymic stromal lymphopoietin, which activates dendritic cells to reward naive Th lymphocytes and produce IL-4, IL-13, TNF-α [10]. Activated T lymphocytes from the skin of AD patients can trigger keratinocyte apoptosis via Fas ligand. Normally, proapoptotic markers-Fas ligand receptors (CD95) are weakly expressed on keratinocytes. In patients with AD, under the influence of IFN-γ, the expression of this receptor increases and keratinocytes become sensitive to apoptosis. The interaction of Fas ligand with CD95 is considered as the main mechanism of damage to keratinocytes by T cells with the subsequent development of spongiosis and acanthosis - characteristic clinical and morphological signs of AD.
Penetration ability of topical corticosteroids depending on dosage form
Choosing the basis of the drug depending on the location and characteristics of the skin
Thus, AD is based on genetically determined dysfunction of the epidermal barrier and immune (allergic) inflammation of the skin with the involvement of various immunocompetent cells in the immune response, interacting with the help of cytokines and surface receptors. In this regard, there is a need to use in complex therapy of the disease agents whose action is aimed at restoring the barrier function of the epidermis and external therapy drugs that have an anti-inflammatory effect.
Modern emollients - softening and moisturizing agents used for this purpose, often contain essential lipids of the human epidermis (ceramides, cholesterol and free fatty acids), which make it possible to more successfully restore the epidermal lipid barrier.
As an example of a modern emollient, we can cite the Locobase Ripea cream, which contains all three categories of essential lipids in a physiological ratio, as well as solid paraffin nanoparticles, which ensure deeper transport of essential lipids into the epidermis and give the cream matting properties. A special feature of this cream is that it lasts for 24 hours. The ability of this product to effectively restore the epidermal barrier in atopic dermatitis and other dermatoses accompanied by dryness has been proven in a number of clinical studies.
The choice of external anti-inflammatory therapy is determined by the activity of inflammation and its symptoms. Glucocorticosteroid drugs (GCS) are most widely used in the external treatment of AD. The most important effects of GCS are inhibition of the synthesis of IL-4, IL-5, IL-13, IFN-γ and other cytokines, inhibition of eosinophil migration and T-lymphocyte proliferation, reduction of vascular permeability and microcirculation disorders. GCS increase the binding of histamine and serotonin in the skin, reduce the sensitivity of nerve endings to neuropeptides and histamine, reduce the activity of phospholipase A2 and the production of eicosanoids, and also reduce the expression of cell adhesion molecules and the sensitivity of the endothelium to allergy mediators. Having a pronounced anti-inflammatory effect, GCS act on all inflammatory cells.
Corticosteroid drugs are presented in a wide range of external forms: creams, ointments, lotions, etc. The correct choice of external corticosteroids depends on the clinical manifestations of blood pressure, the activity of the inflammatory process and the location of the lesion. In this case, it is necessary to take into account the chemical structure of external corticosteroids, the mechanism of action, the rate of absorption, the characteristics of excretion, effectiveness and safety. For external therapy, the influence of the base and the amount of absorption of the active component is very important, since the amount of intradermal absorption when using different forms of the same drug can vary by 15–20 times (Fig. 1).
The choice of dosage form is largely determined by the location of the lesions (Table 1). One of the promising external corticosteroids in the arsenal of practicing doctors is hydrocortisone 17-butyrate (Lokoid), presented in the following dosage forms: cream, ointment, Lipocrem, Crelo. They differ in the amount of water contained in the medicinal base, and, accordingly, in the occlusive ability, the degree of skin hydration, and the intensity of penetration of the active substance.
Dynamics of clinical symptoms during therapy
Dynamics of the SCORAD index against the background of external therapy
Features of dosage forms of hydrocortisone 17-butyrate (locoid)
Lokoid® ointment:
• Has an anhydrous petroleum jelly-polyethylene base (95% petroleum jelly and 5% polyethylene, patented Plastibase base).
• Provides a pronounced occlusive effect, moisturizing and softening effect, deeper penetration of the active substance.
• Highly effective for severe dryness, lichenification, infiltration, hyperkeratosis.
• The absence of water in the ointment makes it possible not to add preservatives to the dosage form, which can cause skin irritation.
Lokoid Lipocrem ® :
• Unique dosage form (contains 70% fat and 30% water). Occupies an intermediate position between ointment and cream and combines the advantages of both forms.
• Lokoid Lipokrem® is easily applied to the skin, quickly absorbed, does not stain clothes, and can be washed off with water.
• Has pronounced anti-inflammatory, softening and moisturizing effects comparable to ointment. These properties of the base of Lokoid Lipokrem served as the basis for the creation of an emollient based on it (a softening and moisturizing cosmetic product for the care of dry skin) - Lokobase Lipocream, which is the basis of Lokoid Lipokrem without an active hormonal component
Lokoid ® cream :
• Oil-in-water cream with a light texture (contains 30% fat and 70% water). Intended for use in acute and subacute processes without exudation, including those localized on sensitive areas of the skin (face, folds).
• Locoid cream has a weak occlusive effect, which avoids aggravation during an acute process, and has very good cosmetic properties.
• Has a softening and cooling effect.
Lokoid Krelo®:
• The dosage form of Locoid Crelo® combines the properties of a cream and lotion.
• Can be used on large areas of exudative skin lesions and areas with hair.
• The lotion has a cooling and “soothing” effect, but does not cause dry skin.
• Contains propylene glycol and borage oil, which provide moisturizing and reparative effects.
• Due to its properties, Lokoid Crelo® is intended for use primarily in acute, including exudative, processes, as well as for application to skin areas with abundant hair.
• At the same time, unlike lotions, it does not dry out the skin (due to the absence of alcohol and the presence of a lipid phase), moreover, it helps to moisturize it and accelerate reparative processes.
Material and methods
Lokoid Lipokrem® and Lokoid Crelo® were used in 22 children aged 6 months to 2 years who were treated in the allergology department of the Clinic of the Research Institute of Nutrition of the Russian Academy of Medical Sciences. Of these, 12 children received Lokoid Lipocrem® and 10 children received Lokoid Crelo®. All children had confirmed blood pressure in a state of exacerbation of a skin process of moderate (group 1) or severe (group 2) severity of the disease (SCORAD index - scoring of atopic dermatiti - 23.8 ± 1.6 and 44.5 ± 3.4 respectively).
Distribution of sick children by severity of atopic dermatitis
The distribution of children according to the severity of the disease is presented in table. 2.
According to the localization of the skin process: in 5 children there were rashes on the skin of the face, in 9 children - on the limbs and torso, in 2 - in the groin area, in 6 - the process was widespread with localization on the face, elbow bends, extensor and flexor surfaces of the radius. wrist joints, popliteal fossae. With a moderate course of the disease, the observed children had moderate itching of the skin and sleep disturbance, moderately severe erythema and swelling, papular elements, foci of exudation, crusts, excoriations, severe dry skin and peeling on both affected and unaffected skin. In patients with severe AD, significant swelling of the skin and erythema, numerous papular and vesicular elements, excoriations, fissures, severe itching and sleep disturbance were observed. The duration of the disease was 4.7 ± 2.7 months.
External agents were applied to the affected areas 2 times a day. The duration of treatment was 10 days. The children also received diet therapy and antihistamines. To shade the scratches, a 1% solution of methylene blue was used.
The effectiveness of the therapy in the observed patients was assessed based on the results of a daily examination and an individual card, which recorded the dynamics of the skin process according to the SCORAD index in points. This index took into account the area of skin lesions, the severity of clinical symptoms (erythema, papules/vesicles, exudation, excoriation, dry skin, itchy skin and sleep disturbance). At the same time, the SCORAD index from 0 to 20 points characterized a mild course of the disease, from 20 to 40 - moderate course, from 40 and above - severe course of the disease.
Research results
Studies conducted to evaluate the clinical effectiveness and safety of Lokoid Lipokrem and Lokoid Crelo® for children with AD showed their high effectiveness and good tolerability. There were no adverse reactions to these external therapy agents in the observed children. All children showed positive dynamics, which was expressed in a gradual decrease in itching of the skin, acute inflammatory phenomena, peeling and dry skin. By the end of treatment, a pronounced positive dynamics of the main objective and subjective (itching) symptoms and the prevalence of the skin process was noted.
The most pronounced effect was obtained in moderate cases of AD - a significant reduction in erythema and other symptoms by the 5th day and complete relief by the end of the 10th day of therapy (Fig. 2).
The dynamics of the SCORAD index in the observed children are presented in Fig. 3. In children with a moderate course, the index values decreased to 11.2 ± 2.8, and in children with a severe course – to 18.1 ± 3.3 (p < 0.05).
In children with severe AD, mild erythema and dry skin remained at the end of treatment. The effectiveness of treatment averaged 86.4%. Excellent results were obtained in 45.5% of cases, good – in 36.4%, moderate – in 18.1%.
Thus, in the course of the study, the high efficiency and good tolerability of Lokoid Lipokrem and Lokoid Crelo were demonstrated for moderate and severe AD in young children. The use of these medications is comfortable for patients, as they have good cosmetic properties, are well absorbed and do not leave greasy marks, which entails an increase in the quality of life and adherence to treatment.
