Adapalene

When ATH:
D10ad03

Characteristic.

Synthetic analogue of retinoic acid, naphthoic acid derivative. Acne treatment remedy.

White or almost white powder. Soluble in tetrahydrofuran, slightly soluble in ethanol, practically insoluble in water. Molecular weight 412,53.

Existing dosage forms of adapalene: 0,1% and 0,3% water-based gel, 0,1% cream, 0,1% solution. Registered in Russia 0,1% gel and 0,1% cream.

Pharmacological action.
Comedolytic, anti-inflammatory.

Application.

Ordinary (youthful) acne (acne vulgaris).

Contraindications.

Hypersensitivity.

Restrictions apply.

Seborrheic dermatitis, eczema, childhood (safety and efficacy in children under 12 years to be determined).

Pregnancy and breast-feeding.

When pregnancy is possible, if the effect of therapy outweighs the potential risk to the fetus (adequate and well-controlled studies of the safety of use is not carried out).

Teratogenic effects. No teratogenic effect was found in rats when adapalene was administered orally at doses from 0,15 to 5,0 mg / kg / day (to 120 times greater than the MRDH when applied topically).

However, oral administration of doses ≥25 mg/kg/day to animals results in teratogenicity in rats and rabbits..

Teratological studies of cutaneous application of adapalene in animals (rats and rabbits) shown, that when using doses 0,6; 2,0 and 6,0 mg / kg (to 150 times more MRDH when applied topically) fetotoxic effect is not observed, but a minimal increase in the number of ribs was recorded in the offspring of rats.

Category actions result in FDA - C. (The study of reproduction in animals has revealed adverse effects on the fetus, and adequate and well-controlled studies in pregnant women have not held, However, the potential benefits, associated with drugs in pregnant, may justify its use, in spite of the possible risk.)

Breastfeeding women should use caution when using (unknown, Does adapalene pass into breast milk?, but many drugs are excreted in the milk of women).

Side effects.

Cream 0,1%

In controlled clinical trials, 285 patients with acne when applied 0,1% adapalene cream 1 once a day for 12 weeks monitored local skin irritation, assessing the frequency and severity of such effects, like erythema, peeling, xerosis, itch, burning (cm. Table. 2).

Table

The frequency of local skin irritation on the background of the application 0,1% adapalene cream in controlled clinical trials (N=285)

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Other local reactions in patients, applied 1% cream, there was an increase in acne, dermatitis and contact dermatitis, swelling of the eyelids, conjunctivitis, livor, rash, eczema.

Local reactions (10–40%): эritema, dryness and flaking of the skin, itch, burning. Approximately 20% patients itching and burning were noted immediately after application of the gel. In addition, it was noted (≤1%): skin irritation, burning / tingling, sunburn, increased acne. The manifestation of side effects is most likely in the first 2-4 weeks of treatment., then their frequency and severity decrease. All side effects, observed in clinical trials, were reversible and disappeared after cessation of therapy.

Against the background of the use of adapalene, it is possible to use other means for the treatment of acne., incl. benzoyl peroxide, antibiotics in dosage forms for topical use (klindamiцin, Erythromycin). However, it should be remembered, that the simultaneous application on the same areas of the skin and at the same time is not recommended, tk. Physical incompatibility of medicines or a change in PH with joint use can reduce the effectiveness of adapalene. With concomitant use in order to achieve a better clinical effect, it is recommended to use drugs at different times of the day, For example in the morning and evening, To minimize the possible skin irritation.

Since adapalene can cause local skin irritation in some patients, In order to avoid the cumulative effect, simultaneous use with other potentially irritating agents is not recommended (Medical or abrasive soaps and detergents; soap and cosmetics, with a drying effect; perfume, ethanol -containing means, etc.). With particular caution should be used in combination with adaptened agents, sulfur, resorcinol, salicylic acid. If these drugs were used, It is advisable not to start therapy with adapan until then, until the effects of these drugs on the skin will disappear.

Overdose.

Excessive application of gel or cream does not lead to a faster or better result, At the same time, pronounced skin reactions may be noted - redness, peeling, discomfort.

Acute oral toxicity in mice and rats was observed at doses above 10 ml / kg. Chronic swallowing of a substance can cause the same unfavorable effects, that excessive oral use of vitamin A.

Outwardly: gel or cream is evenly applied with a thin layer, without rubbing, on the affected surface of the skin, pre -cleaned and dried, 1 once a day, at least 1 hours before bedtime. If it is necessary to use other products for the treatment of acne, adapalene is used in the evening, And other means - in the morning. The duration of the course of treatment is determined by a dermatologist.

Do not use patients with erythema (incl. caused by weathing, Sunny), damage to the skin until the moment of complete recovery. Use in patients with eczema can cause increased skin irritation.

It will be appreciated, what is in the first 3 Ned therapy is possible to increase acne rash, In this case, the treatment should not be stopped. When a pronounced side effect occurs - irritation and dry skin, etc.. - It is necessary to stop using adapalene (temporarily or completely).

In the case of reactions, testifying to hypersensitivity, the use of adapalene should be discontinued. It is necessary to warn patients, that when receiving a sunburn, adapalen should not be used until a complete recovery.

During the use of adapalen, the effects of direct sunlight and UV radiation should be avoided (possible skin irritation). In the case of a forced long -term stay in the sun, adapalene should not be applicable the day before, On the day of the solar exposition, And also the next day. To minimize UV ​​exposition, as well as a decrease in the influence of weather conditions, it is recommended to use sunscreen and protect the processed areas of the skin with clothing. Adverse weather conditions, incl. wind, cold, can promote skin irritation in patients, Applying adapalene.

Avoid contact with eyes, On the lips, The mucous membrane of the nose, in case of accidental hit - thoroughly rinse them with warm water.

The gel is recommended for oily and normal skin, cream - for dry and sensitive.

If after 8-12 weeks of treatment of improvement did not occur, necessary to consult a doctor.