FeniVate cream for external use 0.05%, 15g

Eczema (atopic, discoid, in children); nodular pruritus; psoriasis (excluding common plaque); neurodermatosis (including lichen simplex, lichen planus, seborrheic dermatitis); discoid lupus erythematosus; red prickly heat; generalized erythroderma (as an adjunct to systemic therapy); insect bites, allergic contact reactions, itching.

Locally.

Treatment of acute and chronic dermatoses. Ointment or cream is applied in a thin layer to the affected skin 1-2 times a day. The course of treatment is 2 weeks.

Reducing the risk of developing relapses of the disease. After achieving a therapeutic effect in the acute phase of the disease, the frequency of using the ointment or cream is reduced: it is recommended to apply the drug once 2 times a week without applying an occlusive dressing. Kutiveit is applied to all previously affected areas of the skin or to areas where a relapse of the disease can be expected.

1 g of cream contains:

fluticasone propionate 0.05 mg;

excipients: liquid paraffin; isopropyl myristate; cetostearyl alcohol; ketomacrogol 1000; propylene glycol; imidourea; sodium phosphate; citric acid monohydrate; purified water

Hypersensitivity, acne rosacea and vulgaris, perioral dermatitis, primary viral, fungal and bacterial skin infections, itching of the anogenital area.

Active ingredient: Fluticasone

Dosage form: cream for external use

Composition:

1 g of cream contains:

fluticasone propionate 0.05 mg;

excipients: liquid paraffin; isopropyl myristate; cetostearyl alcohol; ketomacrogol 1000; propylene glycol; imidourea; sodium phosphate; citric acid monohydrate; purified water

Pharmacotherapeutic group:

Topical glucocorticosteroid

Pharmacodynamics:

Mechanism of action

Topical glucocorticosteroids have anti-inflammatory properties. Anti-inflammatory properties are due to numerous mechanisms of inhibition of the late phase of allergic reactions, including a decrease in the number of mast cells, weakening of chemotaxis and activation of eosinophils, a decrease in the production of cytokines by lymphocytes, monocytes, mast cells and eosinophils, as well as inhibition of arachidonic acid metabolism.

Fluticasone refers to glucocorticosteroids (GCS) with a pronounced local anti-inflammatory effect. Fluticasone propionate is highly lipophilic, which allows it to penetrate the double lipid layer of the target cell and bind to glucocorticoid receptors in the cytoplasm. Studies in vitroshowed that fluticasone is characterized by high selectivity and affinity for glucocorticosteroid receptors. The fluticasone propionate receptor complex stimulates or inhibits mRNA transcription and subsequent protein synthesis. The production of enzymes responsible for the anti-inflammatory effect is increased while the production of inflammatory mediators is reduced. The production of enzymes responsible for the anti-inflammatory effect is increased while the production of inflammatory mediators is reduced. When applied to the skin, the likelihood of suppression of the function of the hypothalamic-pituitary-adrenal system (HPA) is negligible. According to clinical studies, when it enters the systemic circulation, fluticasone is rapidly transformed in the liver to an inactive metabolite (17?-carboxylic acid), followed by rapid excretion from the body.Due to these properties, FeniVate has a high therapeutic index.

Pharmacodynamic effects

Fluticasone does not cause unexpected hormonal disturbances, does not significantly affect the central and peripheral nervous systems, gastrointestinal tract, cardiovascular and respiratory systems.

Pharmacokinetics:

Due to the limited absorption of fluticasone through the skin, the bioavailability of the drug when applied externally is very low. Oral bioavailability of fluticasone is close to zero due to very low absorption in the gastrointestinal tract and extensive metabolism during the 'first pass' through the liver, which provides a low level of systemic exposure if the drug is accidentally swallowed.

Distribution

After entering the systemic circulation, fluticasone quickly enters the bile and is excreted through the intestines. The degree of binding to blood plasma proteins is quite high (91%). Fluticasone does not accumulate in tissues and does not bind to melanin.

Metabolism

According to the results of preclinical and clinical studies, fluticasone has a high metabolic clearance with subsequent rapid elimination from the body. Thus, the drug entering the systemic circulation through the skin is rapidly inactivated. The main metabolic pathway is hydrolysis to carboxylic acid; this metabolite has a very weak glucocorticosteroid and anti-inflammatory activity.

Withdrawal

The excretion rate of intravenously administered fluticasone propionate is linear in the dose range from 250 to 1000 ?g and is characterized by high plasma clearance (CL = 1.1 L / min). The maximum plasma concentration decreases by approximately 98% within 3-4 hours, and only low plasma concentrations were associated with a terminal half-life of 7.8 hours. The renal clearance of fluticasone propionate is insignificant (<0.2%), less than 5% of the drug is excreted in the form of a carboxylic acid metabolite. The main route of elimination is the excretion of fluticasone propionate and its metabolites in the bile.

Indications

Eczema (atopic, discoid, in children); nodular pruritus; psoriasis (excluding common plaque); neurodermatosis (including lichen simplex, lichen planus, seborrheic dermatitis); discoid lupus erythematosus; red prickly heat; generalized erythroderma (as an adjunct to systemic therapy); insect bites, allergic contact reactions, itching.

Contraindications

Hypersensitivity, acne rosacea and vulgaris, perioral dermatitis, primary viral, fungal and bacterial skin infections, itching of the anogenital area.

Application during pregnancy and lactation

Perhaps if the expected effect of therapy outweighs the potential risk to the fetus.

Side effects

Allergic contact dermatitis, local allergic reactions: burning and itching (require discontinuation of the drug), secondary infections. With prolonged use in high doses - local atrophic changes in the skin (thinning, striae, dilatation of superficial vessels, hypertrichosis, hypopigmentation), systemic absorption with signs of hypercortisolism, suppression of adrenal cortex function, relapses, tolerance.

Method of administration and dosage

Locally.

Treatment of acute and chronic dermatoses. Ointment or cream is applied in a thin layer to the affected skin 1-2 times a day. The course of treatment is 2 weeks.

Reducing the risk of developing relapses of the disease. After achieving a therapeutic effect in the acute phase of the disease, the frequency of using the ointment or cream is reduced: it is recommended to apply the drug once 2 times a week without applying an occlusive dressing. Kutiveit is applied to all previously affected areas of the skin or to areas where a relapse of the disease can be expected.

Special patient groups

Children 10 years and older

Do not use in children under 10 years of age. Children are more likely to develop local and systemic side effects against the background of the use of external GCS, and, in general, children are recommended shorter courses of treatment and the appointment of less active drugs compared to adults.

Care should be taken when using FeniVate ointment, ensuring that the drug is applied in the minimum amount for the shortest possible period of time, sufficient for the manifestation of a clinical effect.

Elderly patients

In clinical studies, there were no differences in the results between the groups of elderly patients and younger patients.

The high prevalence of reduced hepatic or renal function in elderly patients can lead to a slowdown in the elimination of the active substance from the body in the event of its systemic absorption.

Thus, FeniVate ointment should be applied in a minimum amount for the shortest possible period of time, sufficient for the manifestation of a clinical effect.

Patients with impaired renal and / or liver function

In the case of systemic absorption (with prolonged application of the ointment to a large area), the metabolism and excretion of the active substance slow down in patients with impaired renal and / or liver function, which increases the risk of systemic toxicity. Thus, the ointment should be applied in a minimum amount for the shortest possible period of time, sufficient for the manifestation of a therapeutic effect.

Precautions

Contact with eyes should be avoided (possible local irritation, increased intraocular pressure). Therapy of secondarily infected lesions requires the use of appropriate antibacterial agents, and the appearance of signs of the spread of infection requires the abolition of Kutiveit. It is recommended to thoroughly clean the skin before applying a new dressing.

Overdose:

Symptoms

When used externally, fluticasone can be absorbed in sufficient quantities for the manifestation of systemic action. The likelihood of an acute overdose is extremely low, however, with a chronic overdose or improper use of FeniVate, signs of hypercortisolism (Itsenko-Cushing's syndrome) may develop.

Treatment

In case of an overdose of fluticasone, the drug is withdrawn gradually - by reducing the frequency of its application or switching to a less active GCS in order to avoid the risk of developing glucocorticoid insufficiency. With the development of a clinical picture of an overdose of the drug, symptomatic therapy is indicated.

Concomitant therapy with drugs that inhibit the CYP3A4 isoenzyme (for example, ritonavir, itraconazole) can lead to inhibition of GCS metabolism, which is accompanied by an increase in systemic exposure. The degree of clinical significance of such interactions depends on the activity of the inhibitor of the isoenzyme CYP3A4, the dose and route of administration of corticosteroids, however, such an interaction is unlikely with an external route of administration.

Special instructions:

The manifestations of hypercortisolism (Itsenko-Cushing's syndrome) and reversible inhibition of HPA, leading to glucocorticoid insufficiency, in some cases occur due to increased systemic absorption of GCS for external use. In such cases, it is necessary to gradually discontinue treatment, reducing the frequency of applications, or replace FeniVate with a less active GCS. Sudden discontinuation of treatment can lead to glucocorticoid insufficiency (see section 'Side effects').

Risk factors for the development of severe systemic reactions include the following:

- activity and dosage form of GCS for external use;

- duration of treatment;

- application to large areas of the skin;

- increased hydration of the stratum corneum of the dermis;

- application to areas with thin skin, such as the face;

- damaged skin or other conditions, potentially accompanied by damage to the skin barrier;

- Compared to adults, children are likely to absorb more GCS for external use, thus increasing the risk of developing systemic adverse reactions. This is due to the immaturity of the skin barrier and the higher ratio of body surface area to body weight in children compared to adults.

In children from 10 to 12 years old, if possible, long-term continuous therapy with GCS for external use should be avoided, since there is a possibility of suppression of adrenal function.

Cases of visual impairment with the use of systemic and local corticosteroids have been reported, resulting from increased systemic availability and direct eye contact. Therefore, if a patient has symptoms such as blurred vision or other visual impairments, consideration should be given to referring the patient to an ophthalmologist to assess possible causes, which may include cataract, glaucoma, or rare conditions such as central serous chorioretinopathy (CSCHR).

Prolonged application of FeniVate ointment to the face area is undesirable, since the skin in this area is more prone to atrophic changes. When applying FeniVate ointment on the eyelids, it is necessary to ensure that the drug does not get into the eyes, since repeated contact of the drug with the mucous membrane of the eye can lead to the development of cataracts and glaucoma.

In case of secondary infection of skin lesions, appropriate antibiotic therapy should be prescribed. If signs of spread of infection appear, GCS should be canceled for external use and appropriate antibiotic therapy should be prescribed.

Topical corticosteroids are sometimes used to treat dermatitis around chronic leg ulcers. However, this may be associated with a higher frequency of local hypersensitivity reactions and infectious complications. A clear inhibition of the HPA function (the level of cortisol in the blood plasma in the morning is less than 5 ?g / dL) in adults is unlikely when using the FeniVate drug in the recommended doses, except when the drug is applied to more than 50% of the body surface area and in an amount of more than 20 g per day.

Impact on the ability to drive vehicles. Wed and fur .:

Studies assessing the effect of FeniVate on the ability to drive vehicles or mechanisms have not been conducted. Based on the profile of adverse reactions of the drug FeniVate, no adverse effect on the management of vehicles and mechanisms is expected.

Storage conditions

At a temperature not exceeding 30 ? C.

Keep out of the reach of children.

Shelf life

2 years.

Do not use after the expiration date printed on the package.

Terms of dispensing from pharmacies:

On prescription