Index of drugs

Severe forms of acne (such as nodular acne or acne or acne with the risk of permanent scarring), resistant to adequately conducted standard treatment with general antimicrobials and topical medications.

1 capsule contains 10 mg or 20 mg of isotretinoin. The product contains: purified soya oil, partially hydrogenated soybean oil, sorbitol, cochineal red A.

Anti-acne preparation from the group of retinoids. The improvement of the clinical picture in the course of severe acne is associated with inhibition of sebaceous glands activity and histologically confirmed reduction of sebaceous glands. In addition, isotretinoin has anti-inflammatory effects on the skin. Isotretinoin inhibits sebaceous cell proliferation and in the course of acne restores the normal process of differentiation of these cells. The reduction of sebaceous secretion inhibits the multiplication of bacteria (Propionibacterium acnes) within the canal that leads out the sebaceous gland. Absorption of the drug from the gastrointestinal tract is variable and linearly dose-dependent within the therapeutic range; food increases absorption (when taken with food, the bioavailability is increased by 2-fold compared to the administration on an empty stomach). The drug is largely bound to plasma proteins, mainly albumin (99.9%). Isotretinoin concentrations in the epidermis are half that of serum concentrations. After oral administration, 3 major metabolites were isolated: 4-oxo-isotretinoin, tretinoin (all-trans-retinoic acid) and 4-oxotretinoin (metabolites are active). Metabolic studiesin vitro indicate that a number of CYP enzymes are involved in the metabolism of isotretinoin to 4-oxo-isotretinoin and tretinoin. Following oral administration, similar parts of the dose were detected in urine and faeces. T_0,5 isotretinoin (unchanged form) at the final phase of elimination is on average 19 h, and its metabolite (4-oxo-isotretinoin) - an average of 29 h. Isotretinoin is a physiologically occurant retinoid. Two weeks after the end of treatment, specific concentrations for endogenous retinoids are obtained.

Pregnancy and breastfeeding, isotretinoin is contraindicated in women of childbearing age, unless the requirements of the Pregnancy Prevention Program are met. Hypersensitivity to isotretinoin, soybean oil (peanuts or soy) or to any of the excipients. Liver failure. Significantly increased blood lipids. Hypervitaminosis A. Simultaneous use of tetracyclines.

Due to teratogenic effects, the use of the drug in women of childbearing potential is contraindicated unless all the conditions listed below of the Pregnancy Prevention Program are met: the patient has a severe form of acne (acne nodular or acne or acne with the risk of permanent scars) refractory to appropriate standard treatment with general antimicrobials and topical drugs; the patient is aware of the risk of teratogenic effects of the drug; the patient understands the need for regular medical checks every month; the patient understands and accepts the need to continuously use effective contraception, starting 1 month before the start of treatment, during the entire treatment period and for 1 month after the end of therapy (the patient should use at least one, preferably two complementary methods of contraception, in the mechanical method); even if the patient does not have menses, she must follow all recommendations for effective contraception; the patient is able to use effective methods of contraception; the patient has been informed about the potential consequences of pregnancy, is aware of them and understands the need to immediately report to a doctor if she thinks she has become pregnant; the patient understands and accepts the need to carry out pregnancy tests before, during therapy and after 5 weeks after its completion; the patient confirmed that she knows and understands the risks of treatment with isotretinoin and the need for precautions related to isotretinoin treatment.The requirements described also apply to women who are not currently sexually active, except when the prescribing physician stated that there is no risk of becoming pregnant in the given case. It is recommended to perform - under the doctor's supervision - pregnancy tests with a sensitivity of at least 25 m. m./ml, in the first 3 days of the menstrual cycle, as described below. Before starting the use of contraceptives, an initial pregnancy test should be carried out under the supervision of a physician, and the date and test result should be recorded in the documentation. The date of the pregnancy test in patients with irregular menstruation should be determined taking into account the sexual activity of patients and should be carried out after about 3 weeks after the last sexual intercourse without contraceptive protection. During the visit, during which the doctor prescribes isotretinoin, or within 3 days before this visit, a pregnancy test should also be carried out under the supervision of medical staff, and if the patient has not used effective contraception for at least 1 month, the date of the doctor's appointment should be . This test should ensure that the patient is not pregnant when starting treatment with isotretinoin. Control visits should be carried out every 28 days. The doctor decides about the necessity of monthly pregnancy testing, taking into account the sexual activity of the patient and the history of the last menstrual cycles (abnormal menstrual bleeding, lack of the menstrual cycle or total absence of menstruation). If necessary, further pregnancy tests should be performed on the day of the visit or within 3 days before the appointment with the prescribing doctor. After 5 weeks after completing treatment with isotretinoin, the patients should undergo a final pregnancy test. Isotretinoin for women of childbearing age should be discharged in a limited amount - sufficient for 30 days of treatment. It is best if the pregnancy test, prescription and dispensing take place on the same day. The prescription should be completed no later than within 7 days after the doctor has prescribed isotretinoin. Exposing a woman to contact with isotretinoin contained in the semen of a man treated with isotretinoin is too small to cause isotretinoin to cause fetal damage. Patients should be instructed not to share the product with any other person, especially women, and unused capsules should be returned to the pharmacy after the end of treatment. During and for 1 month after treatment, patients should not be blood donors because of the potential risk of fetal damage if their blood is transfused to a pregnant woman. Particular caution should be exercised when isotretinoin is used in patients with a history of depression. All patients should be monitored for symptoms of depression and referred for treatment if necessary. Discontinuation of treatment with isotretinoin may not be sufficient to alleviate symptoms, so it may be necessary to evaluate the psychiatrist or psychologist. At the beginning of therapy, acne symptoms are sometimes exacerbated, but it disappears with continuation of therapy, usually within 7-10 days and usually there is no need to change the dosage of isotretinoin. Avoid exposure to intense solar radiation or ultraviolet light. If necessary, products containing UV filters of at least SPF 15 should be used. Patients taking isotretinoin and up to 5-6 months after the end of therapy should avoid aggressive chemical dermabrasion and laser treatment of the skin due to the risk of scarring with atypical location and, more rarely, post-inflammatory discolorations or discolorations in the treated areas of the skin. At least 6 months after stopping treatment with isotretinoin, waxing should be discontinued due to the risk of rupture of the epidermis. The concomitant use of isotretinoin with topically administered keratolytic agents or exfoliating preparations used to treat acne should be avoided as excessive skin irritation may occur. Careful observation of patients for severe skin reactions should be made; if severe skin reaction is suspected, treatment with isotretinoin should be discontinued. Patients with vision disorders should be referred to an ophthalmologist; it may be necessary to stop the use of isotretinoin. After several years of using the drug in very large doses (much larger than those used in the treatment of acne), bone lesions were observed, including premature obliteration of epiphyseal cartilage, hypertrophy of the bones and calcifications in tendons and ligaments. In case of mild intracranial hypertension, the drug should be discontinued. The liver enzymes should be monitored before treatment, after 1 month after the start of treatment, and then every 3 months, unless there are clinical indications for more frequent monitoring.If persistent and clinically significant elevations in transaminases occur, dose reduction or discontinuation of isotretinoin therapy should be considered. Serum lipids should be monitored (fasted) before treatment, after 1 month after the start of treatment, and then every 3 months, unless there is a clinical indication to check them more frequently. Treatment with isotretinoin should be discontinued if hypertriglyceridemia can not be stabilized until the triglycerides in the plasma are adequate or when symptoms of pancreatitis are present. Triglyceride concentrations above 800 mg / dl or 9 mmol / l may occur in the course of acute pancreatitis, which can lead to death. Due to the risk of inflammatory bowel diseases, in case of severe diarrhea (haemorrhagic), treatment with isotretinoin should be stopped immediately. In case of severe allergic reactions, the treatment should be discontinued and the patient carefully observed. In patients with diabetes, obesity, alcoholics or patients with lipid metabolism disorders treated with isotretinoin, more frequent monitoring of serum lipids and / or blood Glucose may be necessary. Increased fasting blood glucose has been reported and new cases of diabetes have been diagnosed during treatment with isotretinoin. Isotretinoin is not indicated for the treatment of pre-pubescent acne and is not recommended for use in children under 12 years of age. The preparation contains soybean oil - it should not be used in case of allergy to peanut or soya. The cochineal red contained in the preparation may cause allergic reactions, including asthma attacks (allergy is more common in patients allergic to acetylsalicylic acid). The preparation contains sorbitol - do not use in patients with rare hereditary fructose intolerance.

The use of isotretinoin during pregnancy is absolutely contraindicated. If, despite the required precautions taken during the use of isotretinoin, or if the patient becomes pregnant within one month of discontinuation, there is a high risk of very serious malformations in the fetus. Defects in development that are associated with isotretinoin exposure include: disadvantages o.u.n. (hydrocephalus, developmental defects, cerebellar deformities, microcephaly), facial distortions, cleft palate, external ear defects (lack of external ear, small external auditory tubes or lack thereof), eye defects (minor), cardiovascular defects (cone defects and arterial trunk, such as the Fallot tetralogy, the translation of large vessels, defects of the septum), thymic and parathyroid defects. In addition, spontaneous abortions are more common. If a woman becomes pregnant during treatment with isotretinoin, treatment must be discontinued. The patient should be referred to a doctor who specializes or has experience in the field of teratology in order to conduct research and seek advice. The use of isotretinoin during breastfeeding is contraindicated.

Very common: anemia, accelerated red blood cell (OB), thrombocytopenia, thrombocytopenia, blepharitis, conjunctivitis, dry eye syndrome, eye irritation, transaminase elevation, inflammation of the lips, dermatitis, dry skin, local exfoliation, pruritus, erythematosus skin rash, skin sensitivity to damage (risk of injury due to friction), joint pain, muscle pain, back pain (especially in adolescents), increase in serum triglycerides, reduction in high-density lipoprotein. Common: neutropenia, headache, nosebleeds, dry nose, nasopharyngitis, increased serum cholesterol, increased blood Glucose, hematuria, proteinuria. Rare: cutaneous allergic reactions, anaphylactic reactions, hypersensitivity, depression, worsening of depression symptoms, tendency to aggression, anxiety, mood changes, alopecia. Very rare: infections (skin and mucous membranes) caused by Gram-positive bacteria, lymphadenopathy, diabetes, hyperuricaemia, behavioral disorders, psychotic disorders, suicidal thoughts, suicide attempts, suicide, benign intracranial hypertension, convulsions, drowsiness, blurred vision, cataracts, color blindness (color vision limitations), contact lens intolerance, corneal opacity, decreased vision in the dark, keratitis, optic nerve edema (as a sign of benign intracranial hypertension), photophobia, impaired hearing, vasculitis (e.g.Wegener's granulomatosis, allergic vasculitis), bronchospasm (especially in patients with asthma), hoarseness, colitis, ileitis, dry mucous pharynx, gastrointestinal haemorrhages, haemorrhagic diarrhea and inflammatory bowel disease, nausea, pancreatitis, inflammation liver, acne fulminant, exacerbation of acne (acne relapse), erythema (on the face), efflorescence, hair disorder, hirsutism, dystrophy of the nails, skin eruption, hypersensitivity reaction to the light, pyogenic granuloma, skin discoloration, increased sweating, arthritis, calcifica (calcification of ligaments and tendons), premature bone epiphyseal growth, bone growth, bone hypertrophy, reduction in bone density, tendinitis, glomerulonephritis, excessive formation of granulomatous tissue, malaise, increased creatine phosphokinase in the blood. Not known: erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis.

Orally. Isotretinoin can only be prescribed by a dermatologist who has experience in the use of general retinoids in the course of severe forms of acne and full knowledge of the risks associated with the use of isotretinoin and the requirements for monitoring the patient during the use of the drug. Adults, including the elderly and adolescents (from 12 years, not before puberty): treatment should start with a dose of 0.5 mg / kg. per day. Response to treatment and some adverse reactions depend on dose and vary in individual patients. Therefore, individual adjustment of the dose is required during therapy. For most patients, the appropriate dose is 0.5 - 1 mg / kg. per day. Long-term remission and the rate of relapse depend more on the total dose administered than on the treatment or daily dose. It has been demonstrated that exceeding the cumulative dose of the drug 120 mg / kg -150 mg / kg does not bring significant additional benefits. The duration of treatment depends on the individual daily dose. Usually, treatment for 16-24 weeks is sufficient for remission. In most patients, the symptoms of acne disappear completely after one treatment cycle. In the event of a clear relapse, a repetition of the isotretinoin treatment cycle may be considered using the same daily dose and cumulative drug. Due to the fact that the further disappearance of acne symptoms may occur up to 8 weeks after the end of treatment, the recurrence of the treatment should not be taken into consideration before this time. In patients with severe renal impairment, treatment should be started with a lower dose (eg 10 mg daily). The dose should then be increased to 1 mg / kg. daily or up to the maximum dose tolerated by the patient. In patients with severe intolerance, the recommended dose may be continued with a lower dose, which is associated with an increase in the duration of treatment and a greater risk of relapse. In order to obtain the highest possible treatment effectiveness, the highest dose tolerated by the patient should be continued.
Kaps. should be taken with food, once or twice a day.