Acitretin Brand And Generic Names

Pharmacology

Pharmacological action - antipsoriatic. Acitretin is a drug belonging to the group of systemic retinoids. The agent normalizes the process of renewal, differentiation and keratinization of the skin cells, including in psoriasis. Acitretin slows down the process of cell division of the surface layer of the skin (epidermis) and accelerates cell maturation. Currently Acitretin is considered one of the best medicines for the treatment of psoriasis in people who have symptoms quickly returned after the termination of other types of treatment. Respecting the principle of gradually increasing doses, Acitretin is well tolerated and can be used for a long time.

Acitretin is quickly and adequately absorbed from the gastrointestinal tract, Cmax is achieved within 1-4 hours. Bioavailability is about 60% (increases in the appointment during or after a meal). Bound to plasma proteins is 99%. The agent easily penetrates the tissues (highly lipophilic) and diffuses through the placenta and breast milk. Within 36 days after discontinuation, 99% of the drug components are excreted as metabolites in urine and bile in equal amounts. Acitretin and all of its biotransformation products are completely removed within 2 years after treatment.

Treatment should be continued until the disappearance of psoriatic lesions. In keratinization, minimum maintaining effective doses are appointed (50 mg/day).

Acitretin administration

Erythrodermic psoriasis, pustular psoriasis (localized or generalized), congenital ichthyosis, lichen planus, Darier's disease.

Dermatologists recommend Acitretin agents to treat moderate to severe psoriasis, as well as for the treatment of pustular psoriasis and psoriasis of the feet and palms. Acitretin studies demonstrate that low dose of the drug (30-40 mg per day for 12 weeks) causes the complete or almost complete disappearance of lesions of psoriasis in no more than 30% of patients receiving therapy. Larger doses of this medication may be more effective; however, Acitretin should not be used for a long time because of the serious side effects that it might cause.

Contraindications

Hypersensitivity (including vitamin A and other retinoids), pronounced renal and liver dysfunction, therapy with tetracyclines, vitamin A and other retinoids, therapy with methotrexate, pregnancy, breastfeeding.

Restrictions

Diabetes, a history of pancreatitis.

Pregnancy and breast-feeding

Animal studies have shown that Acitretin is excreted in breast milk. Since Acitretin theoretically can cause serious side effects in infants, breast-feeding women should not take this medicine.
If you are forced to undergo treatment with Acitretin - you should stop breastfeeding.

Acitretin side effects

Symptoms of hypervitaminosis A: dryness of mucous membranes, cheilitis, cracks in the corners of the mouth, conjunctivitis, thinning and peeling of the skin, alopecia, brittle nails, paronychia, photosensitivity, headache, night blindness, reversible elevation of transaminases and alkaline phosphatase in blood plasma, hypercalcemia, increased concentration of plasma triglycerides and cholesterol blood, pain in bones and muscles, hyperostosis and calcification including vertebral ligaments with subsequent compression of the spinal cord.

Acitretin interaction

Acitretin is incompatible with tetracyclines, methotrexate and other retinoids. The drug displaces phenytoin from its bound with proteins. During treatment with Acitretin, do not take vitamin supplements containing vitamin A (they may increase the risk of side effects associated with Acitretin). Simultaneous use of Acitretin and a small amount of alcohol is harmless. However, during the treatment period and for at least another 2 months after treatment, it is prohibited to drink alcoholic beverages, take drugs or food with alcohol content. This is extremely important, since alcohol intake violates Acitretin metabolism, turning it into etretinate having a very pronounced teratogenic effect. During treatment with Acitretin, avoid using herbal preparations containing St. John's wort. This plant can reduce the effectiveness of certain contraceptives.

While receiving Acitretin, do not take any other medicines without advice from your doctor. The simultaneous use of Acitretin and certain drugs can cause serious side effects.

Special notes

Before starting treatment, your doctor will have to assign you a number of tests and analyzes that will help establish that you do not belong to the group of people who may suffer from the development of serious side effects when taking Acitretin.

Avoid simultaneous use of vitamin A and/or other retinoids with Acitretin because of the risk of hypervitaminosis A. Since both Acitretin and tetracyclines can cause increased intracranial pressure, their simultaneous use is contraindicated.

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

Overdose

Symptoms: headache, dizziness.

Treatment: symptomatic treatment, mandatory drug discontinuation.

Dosing and administration

Orally, 1 time a day, during meals or with milk.

Adults - 25-30 mg per day for 2-4 weeks, then - 25-50 mg for 6-8 weeks. Maximum daily dose may be increased up to 75 mg.

Children - 500 mcg/kg/day with possible increase to 1 mg/kg/day (not exceeding 35 mg/day); maintenance dose - possibly lower.

Acitretin is produced in the form of capsules containing 10 or 25 mg of active substance. Absorption of Acitretin and the body's sensitivity to the drug is different for different people, so treatment should always start with small doses. Side effects associated with taking Acitretin can appear within 15 days after starting treatment or increasing the dose. After dose reduction, side effects disappear within the next 15 days.

If you missed a dose of Acitretin - no need to take 2 doses of medication at once. Continue to take Acitretin in the former regime.

Acitretin precautions

It is necessary to monitor liver function (before treatment and every 1-2 weeks of therapy for 2 months, and then - every 3 months and after its termination. In pathological changes, analyzes are performed every week, and if liver function does not return to normal, the drug is discontinued). Determine the concentration of cholesterol and triglycerides in the blood serum on an empty stomach, especially in lipid disorders, diabetes, obesity, alcoholism, during prolonged treatment. Patients with diabetes should carefully monitor blood glucose levels. Monitor the growth and development of bones in children. Therapy in women of childbearing age should be started on the 2 or 3 day of the menstrual cycle; they should use contraceptives for 4 weeks prior to treatment, during the course and at least within 2 years after. Additional studies are required for pregnancy.