Acnekutan - instructions for use, reviews, analogs and forms of release (capsules or tablets 8 mg and 16 mg) drugs for the treatment of acne or acne, acne in adults, children and pregnancy. Composition and interaction with alcohol

In this article, you can read the instructions for using the drug Acnekutan. Comments of visitors of the site - consumers of this medication, as well as opinions of specialists in the use of Acnecutan in their practice are presented. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Analogues of Acnecutane in the presence of existing structural analogs. Use to treat acne or acne, acne in adults, children, as well as during pregnancy and lactation. Composition and interaction of the drug with alcohol.

Acnekutan - a drug for the treatment of acne. Isotretinoin (active substance of the drug Acnekutan) is a stereoisomer of all-trans-retinoic acid (tretinoin).

The exact mechanism of action of isotretinoin has not yet been revealed, but it has been established that the improvement in the clinical picture of severe forms of acne is associated with suppression of sebaceous gland activity and histologically confirmed decrease in their size.

Skin fat is the main substrate for the growth of Propionibacterium acnes, so reducing the formation of sebum suppresses the bacterial colonization of the duct. Acnekutan suppresses the proliferation of sebocytes and acts on acne, restoring the normal process of cell differentiation, stimulates regeneration processes. In addition, the anti-inflammatory effect of isotretinoin on the skin has been proven.

Composition

Isotretinoin + auxiliary substances.

Pharmacokinetics

Since the kinetics of isotretinoin and its metabolites is linear, its plasma concentrations during therapy can be predicted on the basis of data obtained after a single dose. This property of the drug also suggests that it does not affect the activity of microsomal liver enzymes involved in the metabolism of drugs.High bioavailability of Acnecutane is due to a large proportion of dissolved isotretinoin in the drug, and may increase if the drug is taken with food. The concentration of isotretinoin in the plasma is 1.7 times higher than in the blood, due to the poor penetration of isotretinoin into erythrocytes. Binding to plasma proteins (mainly with albumin) - 99.9%. The concentration of isotretinoin in the epidermis is 2 times lower than in serum.

It is metabolized to form three major active metabolites - 4-oxo-isotretinoin (major metabolite), Tretinoin (all-trans retinoic acid) and 4-oxo-retinoina and less significant metabolites including glucuronides well. Since isotretinoin and tretinoin are reversibly converted into each other, the metabolism of tretinoin is associated with the metabolism of isotretinoin. 20-30% of the dose of isotretinoin is metabolized by isomerization. In the pharmacokinetics of isotretinoin in humans, an important role may be played by enterohepatic circulation.

Studies have shown that several enzymes of cytochrome P450 are involved in the conversion of isotretinoin to 4-oxo-isotretinoin and tretinoin.In this case, none of the isoforms, apparently, does not play a dominant role. Isotretinoin and its metabolites have no significant effect on the activity of cytochrome P450 enzymes.

Isotretinoin is excreted by the kidneys and with bile in approximately equal amounts. Refers to natural (physiological) retinoids. Endogenous concentrations of retinoids are restored approximately 2 weeks after the end of the drug intake.

Since data on the pharmacokinetics of the drug in patients with impaired liver function are limited, isotretinoin is contraindicated in this group of patients.

Renal failure of mild to moderate severity does not affect the pharmacokinetics of isotretinoin.

Indications

• severe acne (nodular-cystic, conglobata, acne with risk of scarring);
• acne or acne, which are not amenable to other types of therapy.

Forms of release

Capsules 8 mg and 16 mg (sometimes mistakenly called tablets).

Other dosage forms, be it ointment or cream, solution or lotion for external use, do not exist.

Instructions for use and reception scheme

Inside, preferably with food, 1-2 times a day.

The therapeutic efficacy of acnecutane and its side effects depend on the dose and vary in different patients. This makes it necessary to select the individual dose in the course of treatment.

The initial dose of Acnecutane is 400 μg / kg per day, in some cases up to 800 μg / kg per day. In severe cases or with acne, a dose of up to 2 mg / kg per day may be required.

The optimal course cumulative dose is 100-120 mg / kg. Complete remission is usually achieved in 16-24 weeks. With poor tolerability of the recommended dose, treatment can be continued at a lower dose, but longer. In most patients, acne completely disappears after a single course of treatment.

In case of relapse, it is possible to repeat the course of treatment in the same daily and cumulative dose. Repeated course is prescribed not earlier than 8 weeks after the first, tk. the improvement may be deferred.

In chronic renal failure of a severe degree, the initial dose should be reduced to 8 mg per day.

Side effect

• dry skin, mucous membranes, incl. lips (cheilitis), nasal cavity (bleeding), larynx and pharynx (hoarseness), eye (conjunctivitis, reversible corneal opacity and intolerance of contact lenses);
• peeling of the skin of the palms and soles;
• rash;
• itching;
• face erythema / dermatitis;
• sweating;
• pyogenic granuloma;
• paronychia;
• they are not built;
• increased proliferation of granulation tissue;
• persistent thinning of hair;
• reversible hair loss;
• fulminant forms of acne;
• hirsutism;
• hyperpigmentation;
• photosensitization;
• slight trauma of the skin;
• at the beginning of treatment, there may be exacerbation of acne, which lasts for several weeks;
• pain in the muscles with an increase in the level of CK in serum or without it;
• pain in the joints;
• arthritis;
• calcification of ligaments and tendons;
• tendonitis;
• excessive fatigue;
• headache;
• increased intracranial pressure (pseudotumor brain: headache, nausea, vomiting, impaired vision, edema of the optic nerve);
• convulsive seizures;
• depression;
• psychosis;
• suicidal thoughts;
• xerophthalmia;
• individual cases of visual impairment;
• photophobia;
• disturbance of dark adaptation (reduction of sharpness of twilight vision);
• violation of color perception (passing after withdrawal of the drug);
• lenticular cataract;
• keratitis;
• blepharitis;
• conjunctivitis;
• eye irritation;
• optic neuritis;
• edema of the optic nerve (as a manifestation of intracranial hypertension);
• hearing impairment at certain sound frequencies;
• difficulties with wearing contact lenses;
• dryness of the oral mucosa;
• bleeding from the gums;
• inflammation of the gums;
• nausea;
• diarrhea;
• inflammatory bowel disease (colitis, ileitis);
• bleeding;
• Pancreatitis (especially with concomitant hypertriglyceridemia above 800 mg / dL);
• transient and reversible increase in hepatic transaminase activity;
• hepatitis;
• bronchospasm (more often in patients with bronchial asthma in anamnesis);
• anemia, leukopenia, neutropenia;
• reduction of hematocrit;
• increase or decrease in the number of platelets;
• acceleration of ESR;
• hypertriglyceridemia;
• hypercholesterolemia;
• hyperuricemia;
• decrease in the level of HDL;
• hyperglycemia;
• diabetes;
• local or systemic infections caused by gram-positive pathogens (Staphylococcus aureus (staphylococcus));
• lymphadenopathy;
• hematuria (blood in the urine);
• proteinuria (protein in the urine);
• vasculitis (Wegener's granulomatosis, allergic vasculitis);
• systemic hypersensitivity reactions;
• glomerulonephritis;
• congenital malformations - hydro- and microcephaly, underdevelopment of cranial nerves, microphthalmia,malformations of the cardiovascular system, parathyroid glands, skeletal malformations (hypoplasia of finger phalanges, skull, cervical vertebrae, femur, ankle, forearm bones, facial skull, wolf mouth), low position of the auricles, underdevelopment of the auricles, underdevelopment or complete absence of external auditory meatus, hernia of the brain and spinal cord, bone fusion, fusion of the fingers and toes, disturbance of the development of the thymus gland;
• death of the fetus during the perinatal period;
• premature delivery;
• miscarriages;
• premature closure of epiphyseal growth zones;
• pheochromocytoma.

Contraindications

• pregnancy, established and planned (possibly teratogenic and embryotoxic effect);
• the period of breastfeeding;
• liver failure;
• hypervitaminosis A;
• severe hyperlipidemia;
• concomitant therapy with tetracyclines;
• hypersensitivity to the drug or its components
• children under 12 years.

Application in pregnancy and lactation

Pregnancy is an absolute contraindication for therapy with Acnekutan!

If pregnancy occurs, despite warnings, during treatment or within a month after the end of therapy, there is a very high risk of a child with severe developmental defects.

Isotretinoin is a drug with a strong teratogenic effect. If a pregnancy occurs at a time when a woman is taking orally taking isotretinoin (at any dose and even for a short time), there is a very high risk of a child with developmental defects.

Acnecutane is contraindicated in women of childbearing age, unless the condition of a woman satisfies all of the following criteria:

• severe form of acne, resistant to conventional methods of treatment;
• the patient must understand and follow the doctor's instructions;
• the patient should be informed by the doctor about the danger of pregnancy in the course of treatment with Acnekutan, within one month after it and urgent consultation in case of suspected pregnancy;
• the patient should be warned about the possible ineffectiveness of contraceptives;
• the patient must confirm that she understands the nature of the precautionary measures;
• the patient should understand the need and continuously use effective methods of contraception within one month prior to treatment with Acnecutane, during treatment and for a month after its termination; It is desirable to use at the same time 2 different methods of contraception, including barrier;
• the patient should receive a negative result of a valid pregnancy test within 11 days before the drug is taken; a pregnancy test is strongly recommended to be performed monthly during treatment and 5 weeks after the end of therapy;
• the patient should begin treatment with Acnecutane only on the 2nd-3rd day of the next normal menstrual cycle;
• the patient should understand the need for compulsory medical visits every month;
• when treating for a relapse of the disease, the patient should constantly use the same effective methods of contraception within one month prior to initiation of treatment with Acnecutane, during treatment and within a month after its completion, and also undergo the same reliable pregnancy test;
• the patient should fully understand the need for precautionary measures and confirm her understanding and desire to apply reliable methods of contraception, which the doctor explained to her.

The use of contraceptives in accordance with the above instructions during treatment with isotretinoin should be recommended even to women who usually do not use contraceptive methods due to infertility (except for patients who underwent a hysterectomy), amenorrhea, or who report that they do not have sex.

The doctor should be sure that:

• the patient suffers from severe acne (nodular-cystic, conglobate acne or acne with the risk of scarring); acne, not amenable to other types of therapy;
• a negative result of a valid pregnancy test was obtained prior to taking the drug, during therapy and 5 weeks after the end of therapy; the dates and results of the pregnancy test must be documented;
• the patient uses at least one, preferably two, effective methods of contraception, including the barrier method, within one month prior to initiation of treatment with Acnecutane, during treatment and for a month after its termination;
• the patient is able to understand and fulfill all of the above requirements for protection from pregnancy;
• the patient meets all of the above conditions.

Pregnancy test

In accordance with current practice, a pregnancy test with a minimum sensitivity of 25 mME / ml should be performed in the first 3 days of the menstrual cycle:

Before the start of therapy

To exclude a possible pregnancy before the application of contraception, the result and the date of the initial pregnancy test must be recorded by the doctor. In patients with irregular menstruation, the timing of the pregnancy test depends on sexual activity, it should be performed 3 weeks after unprotected intercourse. The doctor should inform the patient about the methods of contraception.

The pregnancy test is performed on the day of appointment of Acnecutane or 3 days before the patient's visit to the doctor. The specialist should register the test results. The drug can be prescribed only to patients receiving effective contraception at least 1 month before the initiation of therapy with Acnecutane.

During therapy

The patient must visit the doctor every 28 days. The need for monthly pregnancy testing is determined in accordance with local practice and taking into account the sexual activity preceding the menstrual cycle disorders.If there is evidence, a pregnancy test is conducted on the day of the visit or 3 days before the visit to the doctor, the test results must be recorded.

End of therapy

After 5 weeks after the end of therapy, a test is performed to exclude pregnancy.

The recipe for Acnekutan to a woman capable of childbearing can be discharged only for 30 days of treatment, continuation of therapy requires a new prescription of the drug by a doctor. It is recommended that a pregnancy test, a prescription and preparation be conducted on the same day.

If, in spite of the precautionary measures taken, during treatment with Acnecutane or within a month after its termination, pregnancy does occur, there is a high risk of very serious fetal malformations.

If pregnancy occurs, the therapy with Acnecutan is stopped. We should discuss the expediency of maintaining a pregnancy with a doctor specializing in teratology.

Since isotretinoin has a high lipophilicity, it is very likely that it enters the breast milk. Because of possible side effects, Acnecutane should not be given to nursing mothers.

Male Patients

Existing evidence suggests that in women the exposure of the drug from the semen and semen of men taking Acnecutane is not sufficient for the appearance of teratogenic effects of Acnecutane. Men should be excluded from the possibility of taking the drug by other people, especially women.

Use in children

Acnecutane is not indicated in the treatment of acne during puberty and is not recommended for use in children under 12 years of age.

special instructions

It is recommended to monitor liver function and hepatic enzymes before treatment, 1 month after its onset, and then every 3 months or according to indications. There was a transient and reversible increase in hepatic transaminases, in most cases within normal values. If the level of hepatic transaminases exceeds the norm, it is necessary to reduce the dose of the drug or to cancel it.

It is forbidden to use ethanol (alcohol) together with the drug Acnekutan (great risk of toxic liver damage and the development of hepatitis).

The level of serum lipids in the fasting serum should be determined before the treatment, 1 month after the start, and then every 3 months or according to the indications.Usually lipid concentrations are normalized after dose reduction or drug withdrawal, as well as dieting.

It is necessary to monitor a clinically significant increase in triglyceride levels, since their elevation above 800 mg / dl or 9 mmol / l may be accompanied by the development of acute pancreatitis, possibly fatal. With persistent hypertriglyceridemia or symptoms of pancreatitis, Acnecutan should be discontinued.

In rare cases, patients who have received Acnecutan, described depression, psychotic symptoms and very rarely - suicidal attempts. Although their causal relationship with the use of the drug is not established, special care should be taken in patients with a history of depression and observe all patients for depression during treatment with the drug, if necessary referring them to the appropriate specialist. However, the abolition of Acnecutane may not lead to the disappearance of symptoms and further monitoring and treatment by a specialist may be required.

In rare cases, at the beginning of therapy, there is an exacerbation of acne, which occurs within 7-10 days without correction of the dose of the drug.

When prescribing the drug, any patient should first carefully evaluate the ratio of possible benefits and risks.

Patients receiving Acnecutane, it is recommended to use moisturizing ointment or body cream, lip balm to reduce dry skin and mucous membranes at the beginning of therapy.

Against the background of the use of Acnecutane, pain in the muscles and joints, an increase in the serum CK of the blood serum, which may be accompanied by a decrease in the tolerability of intensive physical exertion.

It should avoid deep chemical dermoabrasion and laser treatment in patients receiving Acnecutane, and also within 5-6 months after the end of treatment because of the possibility of increased scarring in atypical sites and the occurrence of hyper and hypopigmentation. During treatment with Acnecutane and within 6 months after it, hair removal with wax applications can not be carried out because of the risk of detachment of the epidermis, development of scarring and dermatitis.

Since some patients may have a decrease in visual acuity, which sometimes persists after the end of therapy, patients should be informed about the possibility of this condition, recommending them to use caution when driving a car at night. The state of visual acuity needs to be carefully monitored.Dryness of the conjunctiva of the eyes, opacity of the cornea, worsening of night vision and keratitis usually pass after drug withdrawal. With dry eye mucosa, you can use moisturizing ointment applications or artificial tears. It is necessary to observe patients with dryness of the conjunctiva for possible development of keratitis. Patients presenting complaints of vision should be referred to an ophthalmologist and consider whether it is advisable to cancel Acnecutane. If intolerance of contact lenses for the duration of therapy should be used glasses.

The effects of solar insolation and UV therapy should be limited. If necessary, use a sunscreen with a high protective factor of at least 15 SPF.

Rare cases of development of benign intracranial hypertension (pseudotumour of the brain), including when combined with tetracyclines. Such patients should immediately discontinue Acnecatan.

With therapy with Acnekutan, inflammatory bowel disease may occur. In patients with severe hemorrhagic diarrhea, it is necessary to immediately cancel Acnecutane.

Rare cases of anaphylactic reactions, which occurred only after the previous external application of retinoids, are described. Severe allergic reactions dictate the need to discontinue the drug and carefully monitor the patient.

With caution should prescribe the drug in diabetes mellitus, a history of depression, obesity, a violation of lipid metabolism, alcoholism.

Patients in the high-risk group (with diabetes, obesity, chronic alcoholism, or disorders of fat metabolism) may need more frequent laboratory monitoring of glucose and lipid levels when using Acnecutane. In the presence of diabetes or suspected of it, a more frequent definition of glycemia is recommended. Patients with diabetes are encouraged to conduct more frequent monitoring of blood glucose.

During the treatment period and within 30 days after its termination, it is necessary to completely exclude blood sampling from potential donors to completely exclude the possibility of getting this blood to pregnant patients (high risk of teratogenic and embryotoxic action).

Impact on the ability to drive vehicles and manage mechanisms

During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities requiring increased concentration of attention and speed of psychomotor reactions (when taking the first dose).

Drug Interactions

Antibiotics of the Tetracycline series, glucocorticosteroids (SCS) reduce the effectiveness of Acnecutane.

Simultaneous use with drugs that increase photosensitivity (including sulfonamides, tetracyclines, thiazide diuretics) increases the risk of sunburn.

Simultaneous use with other retinoids (including acitretin, tretinoin, retinol, tazarotene, adapalen) increases the risk of hypervitaminosis A.

Isotretinoin may impair the effectiveness of Progesterone preparations, so do not use contraceptives containing small doses of progesterone.

Combined use with local keratolytic drugs for the treatment of acne is not recommended because of the possible increase in local irritation.

Since tetracyclines increase the risk of increased intracranial pressure, simultaneous use with isotretinoin is contraindicated.

Analogues of medicinal product

Structural analogs for the active substance:

• Verocutan;
• Retasol;
• Roaccutane;
• Wipe off.

Analogues on the curative effect (remedies for the treatment of acne or acne):

• Aquazan;
• Androkur;
• Arthromax;
• Basiron AC;
• Bassado;
• Bellune 35;
• Betaspan Depot;
• Betula Charm;
• Betusil;
• Biseptol;
• Bonade;
• Wilprafen;
• Wilprafen solute;
• Delex Acne gel from acne;
• Deleks Acne cleansing lotion;
• Desquam;
• Jess;
• Jess Plus;
• Diane 35;
• Dimephosphone;
• Doxal;
• Doxycycline;
• Dr. Theiss Acne Cream for acne;
• Dr. Theiss Acne Acne Lotion;
• Yeast beer;
• Genetten;
• Mirror;
• Zinerit;
• Zitrolid forte;
• Clenzite;
• Cylinder C;
• Curious;
• Kutis compositum;
• Lei;
• Purge of Puree;
• Metronidazole;
• Microfolline;
• Monoclin;
• Piolizin;
• Proderm;
• Retinoic ointment 0.05 and 0.1%;
• Roaccutane;
• Rosamet;
• Roxithromycin Lek;
• Silhouettes;
• Skinoren;
• Streptonitol;
• Sudokrem;
• Chloe;
• Zinctal;
• Cytale;
• Eplan;
• Erica 35;
• Unidox Solutab;
• Yarina Plus.

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