Composition, form of production and packaging
? The cream for external use is white or almost white, homogeneous, soft.
fluticasone propionate micronized 500 Ојg
Auxiliary substances: paraffin liquid 400 mg, isopropyl myristate 50 mg, cetostearyl alcohol 52.5 mg, cetomacrogol 1000 mg 7.5 mg, propylene glycol 100 mg, imidourea 2 mg, sodium phosphate 1.5 mg, citric acid monohydrate 0.5 mg, water purified - up to 1 g.
15 g - aluminum tubes (1) - cardboard packs.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2017.
GCS for external use. It has anti-inflammatory, antipruritic and vasoconstrictive 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, decreased cytokine production by lymphocytes, monocytes, mast cells and eosinophils, and inhibition of arachidonic acid metabolism.
Fluticasone belongs to the SCS with a pronounced local anti-inflammatory effect. When applied to the skin, the probability of oppression of the hypothalamic-pituitary-adrenal system (GGNS) is negligible. In vitro studies have shown that fluticasone is characterized by high selectivity and affinity for glucocorticoid receptors. According to clinical studies, when it enters the systemic circulation, fluticasone is rapidly transformed in the liver to an inactive metabolite (carboxylic acid) followed by rapid elimination from the body. Due to these properties, the KutiveytВ® preparation has a high therapeutic index.
Fluticasone does not cause unforeseen hormonal disorders, does not have a significant effect on the central and peripheral nervous system, gastrointestinal tract, cardiovascular and respiratory systems.
Due to the limited absorption of fluticasone through the skin, the bioavailability of the drug for external use is very low. Bioavailability of fluticasone when taken orally is close to zero due to the very low level of absorption from the gastrointestinal tract and extensive metabolism during the "first passage" through the liver, which provides a low level of systemic exposure to accidental ingestion of the drug.
After entering the systemic circulation, fluticasone quickly enters the bile and is eliminated through the intestine. Fluticasone does not accumulate in the tissues and does not bind to melanin.
According to the results of preclinical and clinical studies, fluticasone has a high metabolic clearance with the subsequent rapid elimination from the body. Thus, the drug that enters the systemic bloodstream through the skin is rapidly inactivated. The main pathway of metabolism is hydrolysis to a carboxylic acid; this metabolite has a very weak glucocorticoid and anti-inflammatory activity.
Fluticasone is excreted within 48 hours mainly through the intestine.
Adults and children aged 1 year and older for relief of inflammation and itching in acute and chronic dermatoses sensitive to glucocorticosteroid therapy, such as:
- atopic dermatitis (including atopic dermatitis in children aged 1 year);
- Numular dermatitis (discoid eczema);
- psoriasis (except for common plaque psoriasis);
- simple chronic lichen;
- Red flat lichen;
- contact or allergic contact dermatitis;
- erythroderma (as an adjunct to systemic GCS therapy);
- inflammatory reactions to insect bites.
Kutiveyt В® is used to reduce the risk of relapse in the chronic form of atopic dermatitis, if a therapeutic effect is observed in the treatment of the acute phase of the disease.
The drug is prescribed for adults, elderly patients, children aged 1 year and older .
The general course of therapy is 4 weeks.
The use of the cream is especially indicated for the treatment of wet or wet surfaces.
Treatment of acute and chronic dermatoses
Apply Coutiveyt В® cream 1 or 2 times / day with a thin layer in an amount not more than necessary to cover the entire affected area, and gently rub. Duration of treatment - up to 4 weeks before the effect, then reduce the frequency of application or switch to treatment with a less active drug. It is necessary to withstand sufficient time to absorb Kutiveyt В® before applying the emollient. If the condition deteriorates or there is no improvement within 2 weeks, a reassessment of treatment and diagnosis should be made.
In the treatment of atopic dermatitis, GCS for external use should be gradually phased out against maintenance therapy with an emollient after the control of the disease is achieved.
Renewal of the initial symptoms of dermatosis can occur when the GSS therapy is suddenly discontinued for external use, especially when using highly active drugs.
Reducing the risk of recurrence of atopic dermatitis
After achieving a therapeutic effect in the acute phase of the disease, the frequency of application of the cream is reduced: it is recommended to apply the drug once or twice a week without applying an occlusive bandage.
Kutiveyt В® is applied to all previously affected areas of the skin or to areas where a relapse of the disease can be expected. This dosing regimen should be combined with daily application of emollients. Regular monitoring of the patient's condition is necessary.
Special patient groups
Children aged 1 year and older
Children are more likely to develop local and systemic side effects when using external GCS, and in general, children are recommended shorter courses of treatment and the appointment of less active drugs than adults. The course of therapy for children should not exceed 4 weeks.
Caution should be exercised when using KutiveytВ® cream, ensuring that the preparation is applied in a minimal amount for the shortest period of time, sufficient for the manifestation of a clinical effect.
In clinical studies, there was no difference in the results between groups of elderly patients and younger patients. The high prevalence of reduced hepatic or renal function in elderly patients can lead to a delay in the removal of the active substance from the body in the event of its systemic absorption. Thus, KutiveytВ® cream should be applied in a minimal amount for the shortest period of time, sufficient for manifesting the clinical effect.
Patients with impaired renal and / or liver function
In the case of systemic absorption (with prolonged application of the cream over a large area), the metabolism and excretion of the active substance slows down in patients with impaired renal and / or liver function, which increases the risk of systemic toxicity. Thus, it is necessary to apply the cream in the minimum amount for the shortest period of time, sufficient for the manifestation of the clinical effect.
The undesirable reactions presented below are listed in accordance with the damage to organs and organ systems and frequency of occurrence. Frequency of occurrence is defined as follows: very often (? 1/10), often (? 1/100 and <1/10), infrequently (? 1/1000 and <1/100), rarely (? 1/10 000 and < 1/1000), very rarely (<1/10 0000, including individual cases). Frequency categories were formed on the basis of post-registration observation.
Infectious and parasitic diseases: very rarely - opportunistic infections.
From the immune system: very rarely - hypersensitivity (itching at the site of application, rashes, swelling).
On the part of the endocrine system: very rarely - inhibition of GGNS (weight gain or obesity, slow weight gain or growth retardation in children, cushingoid traits (eg, lunar face, central obesity), decreased endogenous cortisol, hyperglycemia or glucosuria, hypertension, osteoporosis, cataract, glaucoma.
From the skin and subcutaneous tissues: often - itching at the site of application of the cream; infrequent - burning in the place of application of cream; very rarely - thinning of the skin, atrophy, striae, telangiectasia, hypopigmentation, hypertrichosis, allergic contact dermatitis, exacerbation of the symptoms of the underlying disease, pustular psoriasis, erythema, rash, urticaria.
It should be reported to the doctor about any undesirable reactions noted above. The decision on the further treatment strategy should be made by the doctor.
If any of the unwanted reactions specified in the manual is aggravated or any other undesirable reactions not indicated in the instructions are noted, the patient should inform the physician about it.
- Hypersensitivity to the active substance or any other component included in the preparation;
- Primary skin lesions of bacterial, viral and fungal etiology;
- acne vulgaris;
- perioral dermatitis;
- perianal and genital itching;
- itching without symptoms of inflammation;
- Children's age up to 1 year.
With caution should apply the drug in psoriasis, kidney failure, liver failure, elderly patients, in childhood (from 1 year to 12 years).
PREGNANCY AND LACTATION
There are no available data for assessing the effect of GCS for external application on human fertility.
There is a limited amount of data on the use of fluticasone during pregnancy.
As a result of preclinical studies, it was found that external application of corticosteroids in pregnant animals can cause a deviation of embryonic development, but the significance of this phenomenon for man has not been established.
Kutiveyt В® can be given only if the intended benefit to the mother exceeds any possible risk to the fetus. In this case, the cream should be applied in the minimum amount for the shortest period of time, sufficient for the manifestation of the clinical effect.
The safety of GCS therapy for external use is not established.
There are no available data to confirm the possibility of systemic absorption of GCS for external application in an amount sufficient for their detection in breast milk.
As a result of preclinical studies, it was found that during breastfeeding with a sc administration in quantities sufficient for determination in the plasma, fluticasone was found in milk.
Kutiveyt В® can be given during breastfeeding, only if the intended benefit to the mother exceeds any possible risk to the child.
When applying Kutiveyt В® during breastfeeding, the drug should not be applied to the area of вЂ‹вЂ‹the mammary glands to prevent it from accidentally swallowing the baby.
APPLICATION FOR FUNCTIONS OF THE LIVER
Caution should be used in cases of kidney failure.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
With caution , use the drug for liver failure.
APPLICATION FOR CHILDREN
Contraindicated in children under 1 year.
With caution should be used in childhood (from 1 year to 12 years).
APPLICATION IN ELDERLY PATIENTS
Caution should be applied to elderly patients.
Carewith В® should be used with caution in patients with a history of local reactions of hypersensitivity to other GCS. Local reactions of hypersensitivity can resemble the symptoms of the underlying disease.
Manifestations of hypercorticism (Itenko-Cushing syndrome) and reversible inhibition of HHHC leading to glucocorticoid insufficiency, in some cases arise as a result of increased systemic absorption of GCS for external application. In such cases, it is necessary to gradually stop treatment, reducing the frequency of application, or replace the drug Kutiveyt В® with a less active SCS. A sudden cessation of treatment can lead to glucocorticoid insufficiency.
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;
- application to the closed areas of the skin, for example, in diaper rash or under occlusive dressings (children may have a diaper as an occlusive dressing);
- increased hydration of the horny layer of the dermis;
- application to areas with thin skin, such as face;
- damaged skin or other conditions, potentially accompanied by damage to the skin barrier;
- compared with adults in children, there is a possibility of absorption of more GCS for external use, thus increasing the risk of systemic unwanted reactions. This is due to the immaturity of the skin barrier and a higher ratio of body surface area to body weight in children compared to adults.
In children from 1 to 12 years of age, prolonged continuous therapy with GCS for external use should be avoided whenever possible. there is a possibility of suppression of adrenal function.
Caution should be exercised when prescribing GCS for external use in the treatment of psoriasis. there are reports of early relapses, development of addiction, the risk of generalized pustular psoriasis, and local or systemic toxicity due to a violation of the barrier function of the skin. The use of psoriasis requires careful monitoring of the course of the disease in the patient.
Long-term application of the cream of Kutiveyt В® on the face is undesirable. the skin in this area is more prone to atrophic changes.
When applying the cream of Quitveit В® 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.
When secondary infection of the skin lesions should be prescribed appropriate antibiotic therapy. In case of signs of spread of infection, it is necessary to abolish GCS for external use and prescribe appropriate antibiotic therapy.
Bacterial infections are easier to develop in warm and humid conditions in natural folds of the skin or under occlusive dressings, therefore, the skin should be thoroughly cleaned before applying a new bandage.
SCS therapy for external use is sometimes used to treat dermatitis developing around chronic ulcers of the lower limbs. However, this may be associated with a higher incidence of local hypersensitivity reactions and infectious complications.
The apparent inhibition of the function of the GGNS (the level of cortisol in the blood plasma in the morning is less than 5 Ојg / dL) in adults is unlikely with the use of Kutiveyt В® in recommended doses, except for the application of the preparation more than 50% of the body surface area and in excess of 20 g / day .
Kutiveyt В® contains imidourea as an adjuvant, which is metabolized to form trace amounts of formaldehyde. Formaldehyde can cause allergic reactions or irritation in contact with the skin.
Impact on the ability to drive vehicles and manage mechanisms
Studies to assess the effect of the drug Kutiveyt В® on the ability to drive vehicles or mechanisms have not been carried out. Based on the profile of undesirable reactions of the drug KutiveytВ®, no adverse effect on the management of vehicles and mechanisms is expected.
Symptoms: with external application fluticasone can be absorbed in sufficient quantity to manifest systemic action. The likelihood of an acute overdose is extremely low, but chronic overdose or misuse of Kutiveyt В® may develop signs of hypercorticism (Itenko-Cushing syndrome).
Treatment: with an overdose of fluticasone, the withdrawal of the drug is carried out 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 have an inhibitory effect on the isoenzyme CYP3A4 (eg, ritonavir, intraconazole), may lead to inhibition of GCS metabolism, which is accompanied by an increased systemic effect. The degree of clinical significance of this interaction depends on the activity of the inhibitor of the isoenzyme CYP3A4, the dose and method of administration of GCS, however, such interaction is unlikely with an external application.
TERMS OF RELEASE FROM PHARMACY
The drug is dispensed without a prescription.
TERMS AND CONDITIONS OF STORAGE
The drug should be stored out of reach of children at a temperature of no higher than 30 В° C. Shelf life - 2 years.