Instruction for use: Acitretin (Acitretinum)

Pharmacological group

dermotropic means

Nosological classification (ICD-10)

L30.8 Other specified dermatitis

Angiokeratoma, Angiokeratoma diffuse trunk, Darya's follicular dyskeratosis, Follicular dyskeratosis, Darya's disease, Enteropathic acrodermatitis, Skin aurantiases, Ochrodermatosis, Chronic dermatitis of the hand

L40 Psoriasis

Chronic psoriasis with diffuse plaques, Generalized psoriasis, Psoriasis of the scalp, Psoriasis of the scalp, Generalized form of psoriasis, Psoriasis dermatitis, Psoriasis complicated by erythroderma, Invalidative psoriasis, Isolated psoriatic plaque, Exfoliative psoriasis, Psoriatic Erythroderma, Psoriasis with eczematosis, Hyperkeratosis in psoriasis,Inverse psoriasis,Psoriasis eczematous, Dermatosis of psoriasis, Psoriasis of the genitals, Psoriasis with lesions of hairy areas of skin, Erythrodermal psoriasis, Chronic psoriasis of the scalp, Chronic psoriasis, Ordinary psoriasis, Refractory psoriasis, Kebner phenomenon, Scaly lichen

L40.1 Generalized pustular psoriasis

Pustular psoriasis

L40.3 Palmar and plantar pustulosis

Pustular psoriasis

L43 Red Leaf Flat

Lishay Wilson, Erosive-ulcerative form of red flat lichen, Warty forms of red lichen, Red lichen, Flat lichen, Kebner phenomenon

L44.9 Papulovosvamous changes, unspecified

Darya's follicular dyskeratosis, Follicular dyskeratosis, Asbestos Liver, Darya's disease, Dyskeratosis, Papula (nodule)

Q80 Congenital ichthyosis

Ichthyosis is hereditary4

CAS 55079-83-9

Characteristics of Acitretin

Yellow or greenish-yellow powder. Molecular weight 326.44.

Pharmacology

The pharmacological action is antipsoriatic.

Normalizes the processes of renewal, differentiation and keratinization of skin cells, incl. with psoriasis.

Quickly and fairly completely absorbed from the gastrointestinal tract, Cmax is reached after 1-4 hours. Bioavailability - about 60% (increases with appointment during or after meals). It binds to plasma proteins by 99%. Easily penetrates into tissues (has high lipophilicity), diffuses through the placental barrier and into breast milk. Biotransformation is carried out, mainly, by isomerization (with the formation of 13-cis-isomer) and glucuronidation. T1 / 2 Acitretinum - 50 h, and its main metabolite - 60 h. Within 36 days after discontinuation 99% is excreted as metabolites with urine and bile in equal amounts. In some cases, the body produces etretinate, T1 / 2 which is about 4 months. Acitretin and all products of its biotransformation are completely removed within 2 years after the end of treatment.

The therapy continues until the disappearance of psoriatic lesions. When keratinization is disrupted, minimal effective doses are maintained for a long time (up to 50 mg / day).

Application of Acitretin

Psoriatic erythroderma, pustular psoriasis (localized or generalized), congenital ichthyosis, lichen planus, Darya disease.

Contraindications

Hypersensitivity (including vitamin A and other retinoids), severe renal and hepatic dysfunction, tetracycline, vitamin A and other retinoid therapy, methotrexate, pregnancy, breastfeeding.

Restrictions for use

Diabetes mellitus, pancreatitis in the anamnesis.

pregnancy and lactation

The action category for the fetus by FDA is X.

Side effects

Symptoms of hypervitaminosis A: dry mucous membranes, cheilitis, cracks in the corners of the mouth, conjunctivitis; thinning and peeling of the skin, alopecia, fragility of the nails, paronychia, photosensitivity, headache, impaired vision, reversible increase in the activity of transaminases and AP in the blood plasma, hypercalcemia, increased concentration of triglycerides and cholesterol of the blood plasma, bone and muscle pain, hyperostosis and calcification fabrics incl. vertebral ligaments with subsequent compression of the spinal cord.

Interaction

Incompatible with tetracyclines, methotrexate, vitamin A and other retinoids. Displaces phenytoin from binding to proteins. Ethanol-containing preparations and beverages promote the formation of etretinate.

Update of information

Additional information about the drug interaction of acitretin

The simultaneous use of vitamin A and / or other retinoids with acitretin should be avoided because of the risk of hypervitaminosis A. Since both acitretin and tetracyclines can cause an increase in intracranial pressure, their simultaneous use is contraindicated.

There are reports of an increased risk of hepatitis with combined use of methotrexate and etretinate (retinoid with a longer T1 / 2 than in acitretin), so the appointment of methotrexate simultaneously with acitretin is also contraindicated.

Acitretin can reduce the contraceptive effect of mini-pili with progesterone, so during treatment with acitretin should not use them for contraception.

Overdose

Symptoms: headache, dizziness.

Treatment: symptomatic with the mandatory cancellation of the drug.

Precautions for Acitretin

It is necessary to monitor the function of the liver (before the beginning and every 1-2 weeks of therapy for 2 months, and then every 3 months and after it stops, with pathological changes performed every week, and if the liver function does not return to normal or worsens, the drug is canceled), to determine the concentration of cholesterol and triglycerides in the blood serum on an empty stomach, especially in case of violations of lipid metabolism, diabetes, obesity, chronic alcoholism, during long-term treatment. Patients with diabetes should carefully monitor blood glucose levels, in children - for indicators of growth and development of bones. Therapy of women of childbearing age begins on the 2nd or 3rd day of the menstrual cycle; they should use contraceptives for 4 weeks before the start of treatment, during the course and, at least, for 2 years after it. Additional tests for pregnancy are compulsory.