Lokoid Lipokrem, 0.1%, cream for external use, 30 g, 1 pc.
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.
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.
Pharmacodynamics and pharmacokinetics
Lokoid Lipokrem is a synthetic non-halogenated glucocorticoid agent for external use. When using this drug, a rapid and sustained anti-inflammatory, anti-edematous and antipruritic effect is manifested.
Absorption of the active substance occurs through the epidermis as a result of using the cream in the form of applications. The drug has insignificant systemic absorption.
Metabolism occurs first in the epidermis and then in the liver, with the formation of hydrocortisone and other metabolites . The drug is excreted from the body in metabolites and unchanged form through the kidneys and through the intestines.
Locoid Lipocrem®
If there are signs of hypersensitivity or skin irritation associated with the use of the drug, you should stop treatment and consult a doctor.
With prolonged treatment, when applying the drug to large surfaces of the skin, when using occlusive dressings, as well as in children, systemic absorption of the glucocorticosteroid is possible; it is possible to suppress the function of the hypothalamic-pituitary-adrenal system and develop symptoms of hypercortisolism.
Atrophic changes may appear on the skin of the face more often than on other surfaces of the body after long-term treatment with topical glucocorticosteroids; the course of treatment in this case should not exceed 5 days.
Care must be taken when applying the drug to the face, folds, natural folds, and areas with thin skin.
Avoid getting the drug into your eyes. Do not apply the drug to mucous membranes. It should be borne in mind that glucocorticosteroids can change the manifestations of some skin diseases, which can make diagnosis difficult. In addition, the use of glucocorticosteroids may delay wound healing.
With long-term therapy with glucocorticosteroids, 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 long-term treatment, drug withdrawal should be carried out gradually, for example, by switching to an intermittent treatment regimen before stopping it completely.
Cetostearyl alcohol, which is part of the drug, may cause irritation at the site of application.
Propyl parahydroxybenzoate may cause allergic reactions (possibly delayed). In such cases, you should stop using the drug.
Use in pediatrics
The drug LOCOID LIPOKREM® can be used in children from 6 months. It must be taken into account that in young children, skin folds, diapers, and diapers can have an effect similar to the effect of an occlusive dressing and increase the systemic resorption of glucocorticosteroids.
In addition, in children, a greater degree of systemic resorption is possible due to the relationship between the surface of the skin and body weight, as well as due to insufficient skin maturity.
Long-term treatment of children with glucocorticosteroids can lead to disturbances in their growth and development. Therefore, long-term use of the drug should be carried out under the supervision of a physician. Children should receive the minimum dose of the drug sufficient to achieve an effect.
In children, the course of treatment should not exceed 7 days.
Indications for use
This remedy is prescribed for superficial, non-infected skin diseases that are sensitive to other drugs:
- dermatitis ( atopic , contact and seborrheic );
- eczema;
- psoriasis.
Lokoid Lipokrem, instructions for use (Method and dosage)
For adults and small patients from 6 months of age, it is recommended to apply the cream in a small amount to the affected areas 1-3 times a day. If improvement occurs, the use of the cream is reduced to 1-3 times a week.
Correct application helps increase the effectiveness of treatment - the cream should be applied with massaging movements, and in some diseases - under an occlusive dressing. In this case, 30-60 g are prescribed for use within a week. The therapeutic course is established individually for each specific case, depending on the condition of the patients and the course of the disease.
Side effects
When treated with an external agent, local reactions may occur in the form of skin atrophy , rosacea-like and perioral dermatitis, a rebound effect that makes it difficult to withdraw the corticosteroid, and slower wound healing. It is also possible that there is an increase in intraocular pressure , the development of cataracts , depigmentation, allergic reactions , and so on.
Reviews of Lokoid Lipocream
This drug is rarely discussed online. However, almost everyone who has used this external remedy confirms its high effectiveness. Therefore, reviews of Lokoid Lipokrem are usually positive.
At the same time, patients note that of all the external medications that they had to use, this cream helps the best. However, they use it with extreme caution, as they are afraid that the strong effect may negatively affect their body. For example, according to experts, long-term use of the cream for irritation or allergic reactions on the face can lead to hormonal dermatitis. This means that patients must strictly adhere to the dosage of the drug and the doctor’s prescription. Although none of the users report the development of side effects.
Thus, Lokoid Lipocrem is indeed one of the highly effective remedies used in the treatment of dermatitis, eczema or psoriasis. At the same time, the main thing is not to self-medicate, since an illiterate approach to the treatment of such diseases can significantly aggravate the situation.
Overdose
If you follow the recommended doses when using the cream, you can avoid its suppressive effect on the hypothalamic-pituitary-adrenal system.
Long-term use of the cream in high dosages, especially under occlusive dressings, can increase the content of cortisol in the blood plasma . At the same time, there is no decrease in reactivity in the activity of the pituitary gland and adrenal glands. After discontinuation of the drug, cortisol production quickly normalizes.
