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Composition:


active ingredients: adapalene, benzoyl peroxide;


1 g of gel contains adapalene 1 mg and benzoyl peroxide 25 mg;


excipients: Simulgel 600 PHA (copolymer of acrylamide and sodium acryloyldimethyltaurate, isohexadecane, polysorbate 80, sorbitanoleate), sodium docusate, disodium edetate, glycerin, poloxamer 124, propylene glycol, purified water.


Dosage form. Gel.


Basic physical and chemical properties: opaque gel from white to light yellow color.


Pharmacotherapeutic group. Medications for topical acne treatment. Retinoids for topical acne treatment. ATX code D10A D53.


Pharmacological properties.


Pharmacodynamics.


The composition of the drug includes two active substances with different, but complementary mechanisms of action.


Adapalene is a chemically stable naphthoic acid derivative with a retinoid-like effect. Studies of the biochemical and pharmacological profile have shown the effect of adapalene in the disease caused by Acne vulgaris: it is a powerful modulator of cell differentiation and keratinization, and also has anti-inflammatory properties. The mechanism of action of adapalene is based on The Binding of the compound to specific retinoic acid nuclear receptors. Current data suggest that when applied topically, adapalene normalizes the differentiation of follicular epithelial cells, thereby reducing the formation of microcomedones. In vitro models, adapalene inhibits the chemotactic (directed) and chemokinetic (random) responses of human polymorphonuclear leukocytes; it also inhibits the conversion of arachidonic acid to inflammatory mediators. According to in vitro studies, adapalene inhibits AP-1 factors, as well as the expression of toll-like receptors 2. This profile indicates that adapalene reduces the inflammatory component of acne mediated by cells.


Benzoyl peroxide has an antimicrobial effect, in particular against P. aspes, which are present in excessive amounts in the affected sebaceous-hair complex. In addition, benzoyl peroxide has exfoliating and keratolytic properties, and also has a sebostatic effect, preventing excessive sebum production, which is accompanied by acne.


Pharmacokinetics.


The pharmacokinetic properties of Effezel are similar to the pharmacokinetic profile of the gel, which contains only adapalene at a concentration of 0.1 %.


In a 30-day clinical pharmacokinetic study involving acne patients who used a gel with a combination of fixed doses or a drug of the appropriate composition with 0.1% adapalene in maximum doses (applying 2 g of gel per day), adapalene concentrations in most blood plasma samples were not quantified (the threshold for quantitative determination was 0.1 ng/mL). Low concentrations of adapalene (Cmax 0.1 to 0.2 ng/mL) were determined in two blood samples of participants using Effezel and in three blood samples of participants using Adapalene Gel 0.1 %. The highest value of adapalene AUC0-24h determined in the fixed-dose combination group was 1.99 ng·H/ML.


These results are similar to those obtained in previous clinical studies of the pharmacokinetics of various adapalene 0.1% preparations, according to which systemic exposure to adapalene was consistently low.


The penetration of benzoyl peroxide through the skin is low; when applied to the skin, it is completely converted to benzoic acid, which is quickly eliminated.


Preclinical safety data.


The results of standard preclinical pharmacological safety studies, studies of drug toxicity with repeated use, genotoxicity, phototoxicity or carcinogenicity do not indicate the presence of special threats to humans.


The toxic effect of adapalene on reproductive function was studied in animals that were administered orally and applied to the skin. At high systemic exposures (oral administration at doses starting from 25 mg/kg/day), a teratogenic effect was observed. At lower exposures (applied to the skin at a dose of 6 mg/kg/day), changes in the number of ribs or vertebrae were noted.


Animal studies of Effezel included studies of local tolerability and skin toxicity with repeated use of the drug in animals for a period of up to 13 weeks; the drug had a local irritant effect and showed the ability to cause sensitization, as expected from a combination containing benzoyl peroxide. Systemic exposures of adapalene after repeated application to the skin of a combination of fixed doses in animals are very low, which is consistent with clinical pharmacokinetic data. Benzoyl peroxide is rapidly and completely converted to benzoic acid in the skin and is excreted in the urine after absorption; its systemic exposure is limited.


Clinical characteristics.


Indications.


Treatment of common acne (acne vulgaris) with comedones, papules and pustules.


Contraindications.


* Pregnancy.


* Women planning pregnancy.


* Hypersensitivity to active substances or to any of the excipients.


Interactions with other drugs and other types of interactions.


Drug interaction studies of Effezel have not been conducted.


Based on previous experience with adapalene and benzoyl peroxide, no interactions with other drugs that can be applied to the skin simultaneously with Effezel were detected. However, other retinoids or benzoyl peroxide, or drugs with a similar mechanism of action, should not be used simultaneously. Caution should be exercised when using cosmetics that exhibit exfoliating, irritating or drying properties, as this may cause an additive irritating effect when using Effezel.


Adapalene absorption through human skin is low, so interaction with systemic drugs is unlikely.


The penetration of benzoyl peroxide through the skin is low, it is completely metabolized to benzoic acid, which is quickly eliminated from the body. Thus, the interaction of benzoic acid with systemic drugs is unlikely.


Application features.


Effezel Gel should not be applied to damaged, injured (cuts or abrasions) or eczematous skin.


Avoid contact of the gel with the eyes, mouth, nostrils or mucous membranes. If the drug gets into the eyes, they should be immediately rinsed with warm water.


The product contains propylene glycol (E1520), which can cause skin irritation.


If a reaction develops that indicates sensitivity to any component of the drug, the use of Effezel Gel should be discontinued.


Excessive exposure to sunlight or UV radiation should be avoided.


Avoid contact of the product with any colored material, including hair and colored fabrics, as this may lead to discoloration or discoloration.


Use during pregnancy or lactation.


Oral administration of retinoids is associated with the occurrence of congenital anomalies. As a general rule, it is considered that when applied topically in accordance with approved indications, retinoids can cause minor systemic effects due to minimal absorption through the skin. However, there are individual factors (such as skin damage, overuse) that can contribute to increased systemic exposure.


Pregnancy


Effezel is contraindicated during pregnancy or in women planning pregnancy.


The amount of data on topical application of adapalene in pregnant women is limited or there are no data.


In studies on animals that received the drug orally, a toxic effect on reproductive function was found at high systemic exposures.


Clinical experience with topical application of adapalene and benzoyl peroxide in pregnant women is limited.


If the drug is used during pregnancy or if the patient becomes pregnant while taking this medicine, treatment should be discontinued.


Breast-feeding


Studies on the penetration of the drug into breast milk of animals or humans after applying Effezel gel (adapalene and benzoyl peroxide) to the skin have not been conducted.


The effect on a breastfed child is not expected, since the systemic effect of the drug on a breastfed woman is insignificant. Effezel can be used during breast-feeding.


To prevent contact effects on infants, avoid applying Effezel gel to the breast during breast-feeding.


Fertility


No studies of human fertility using Effezel gel have been conducted.


However, in animal reproductive studies, no effect of adapalene or benzoyl peroxide on fertility was found .


Ability to influence the reaction rate when driving vehicles or other mechanisms.


It doesn't affect you.


Dosage and administration.


Effezel gel is applied to the entire acne-affected surface once a day in the evening on clean and dry skin. The drug is applied in a thin layer with your fingertips, avoiding contact with the eyes and lips (see the section "application features").


In case of irritation, it is recommended to apply non-comedogenic moisturizers, reduce the frequency of use of the drug (for example, every other day), temporarily interrupt or completely stop its use.


The duration of treatment should be determined by the doctor, taking into account the patient's clinical condition. The first signs of clinical improvement usually appear after 1-4 weeks of treatment.


Children.


The safety and efficacy of Effezel in children under 9 years of age have not been studied.


Overdose.


The drug is intended only for application to the skin once a day.


In case of unintentional ingestion, appropriate symptomatic therapy should be resorted to.

Tags: Effezel® [Adapalene, Benzoyl Peroxide]