Index of drugs

Severe forms of acne (acne nodular acne, 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; capsules contain soybean oil.

Anti-acne drug from the retinoid group. The improvement of the clinical picture in the treatment of severe acne is associated with the suppression of sebaceous glands activity and reduction of their size; in addition, isotretinoin has anti-inflammatory effects on the skin. The bioavailability of isotretinoin is twice as high when administered with food. It is highly bound to plasma proteins (99.9%). Isotretinoin concentrations in the epidermis are half as high as in the blood serum. The main metabolites of isotretinoin are: 4-oxo-isotretinoin, tretinoin (all-trans-retinoic acid) and 4-oxotretinoin. Several CYP isoenzymes participate in the metabolism. Other, less important metabolites include glucuronides. Isotretinoin and tretinoin undergo reciprocal reversal into one another (interconversion). It is estimated that 20% -30% of the isotretinoin dose undergoes isomerization. It is excreted in urine and faeces. T_0,5 isotretinoin is on average 19 hours, and 4-oxo-isotretinoin on average 29 hours.

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 the teratogenic effect of isotretinoin, the use of the drug in women of childbearing potential is contraindicated unless all of the following conditions of the Pregnancy Prevention Program are met: the patient has a severe form of acne (nodular acne or acne or acne with the risk of permanent scars) resistant to adequately conducted standard treatment with general antimicrobials and topical medications; 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 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 described requirements also apply to women who are not currently sexually active, except when the prescribing physician determines that there is no risk of becoming pregnant in a 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. The prescribing doctor should train the patient how to use contraception. During the visit, when the doctor prescribes isotretinoin or within 3 days before this visit, a pregnancy test should also be carried out under the supervision of a doctor, and if the patient has not used effective contraception for at least 1 month, the date of the doctor's appointment should be postponed accordingly. 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 carried out on the day of the visit or within 3 days before the visit. After 5 weeks after the treatment with isotretinoin, patients should undergo a pregnancy test. Isotretinoin for women of childbearing age should be discharged in an 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. The exposure of the partner to the seed of a man taking isotretinoin is not so large that isotretinoin may be teratogenic. Men should be reminded that they are not allowed to share the preparation with another person, especially female, 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. The physician should provide all patients with complete information on the risk of teratogenic effects of isotretinoin and precise explanations on methods of contraception as set out in the Pregnancy Prevention Program. 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. Patients should be advised to use ointments or moisturizing creams and lip balms from the beginning of treatment, as isotretinoin may cause dryness of the skin and lips. Patients should be closely observed for severe skin reactions. If a severe skin reaction or a severe allergic reaction is suspected, treatment with isotretinoin should be discontinued. The symptoms of eye dryness occurring during treatment can be relieved by moisturizing eye Ointment or tears replacing products. Intolerance of contact lenses may occur, which makes it necessary to wear glasses during treatment. Patients with vision disorders should be referred to an ophthalmologist; it may be necessary to stop the use of isotretinoin. 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. In patients with diabetes, obesity, alcoholics or patients with disturbed lipid metabolism, it may be necessary to monitor serum lipids and / or blood Glucose more frequently. Treatment with isotretinoin should be discontinued if plasma triglyceride levels are not achieved 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.

The use of isotretinoin during pregnancy is absolutely contraindicated. If, despite the required precautions taken during the use of isotretinoin, or within one month of discontinuation, the patient becomes pregnant, there is a significant risk of very serious malformations in the fetus. The developmental defects that are associated with isotretinoin exposure include CNS defects (hydrocephalus, cerebellar developmental defects, microcephaly), facial distortions, cleft palate, external ear defects (no external ear, small external or no auditory tubes), eye defects ( little), cardiovascular defects (malformations of the common arterial trunk, such as the Fallot tetralogy, the transmission 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 for the purpose of research and advice. The use of isotretinoin during breastfeeding is contraindicated.

Very common: anemia, increased ESR, thrombocytopenia, thrombocytopenia, blepharitis, conjunctivitis, dry eye, eye irritation, increased aminotranferase activity, red lips inflammation, dermatitis, dry skin, local epidermal exfoliation, pruritus, erythematous rash, hypersensitivity of the skin (risk of injury due to friction), joint pain, muscle pain, back pain (especially in children and adolescents), increase in triglycerides in the blood, reduction in high-density lipoprotein. Common: neutropenia, headache, nosebleeds, dry nose, nasopharyngitis, increased cholesterol in the blood, increased blood Glucose, hematuria, proteinuria. Rare: cutaneous allergic reactions, anaphylactic reactions, hypersensitivity reactions, depression, aggravation of depression symptoms, tendency to aggression, anxiety, mood changes, alopecia. Very rare: infections (skin and mucous membranes) with Gram-positive bacteria, lymphadenopathy, diabetes, hyperuricaemia, behavioral disorders, psychotic disorders, suicidal thoughts, suicide attempts, suicide, benign intracranial hypertension, convulsions, drowsiness, dizziness, blurred vision, cataracts , color blindness (lack of color vision), contact lens intolerance, corneal opacity, decreased vision in the dark, keratitis, congestive disc (a symptom of benign intracranial hypertension), photophobia, visual disturbances, hearing impairment, vasculitis (eg Wegener's granulomatosis, allergic vasculitis), bronchospasm (especially in patients with asthma), hoarseness, colitis, ileitis, dry throat, gastrointestinal haemorrhage, hemorrhagic diarrhea and inflammatory bowel disease, nausea, pancreatitis, hepatitis, fulminant acne, behind sharpening of acne (relapse of acne), erythema (face), rash, hair disorder, hirsutism, dystrophy of the nails,nausea, photosensitivity reactions, pyogenic granuloma, skin discoloration, increased sweating, arthritis, calcification (calcification of ligaments and tendons), premature fusion of the long bone roots, bony growths (hyperostosis), reduction of bone density, tendinitis, rhabdomyolysis, glomerulonephritis kidney, excessive granulation, malaise, increased creatine kinase in the blood. Not known: erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis.

Isotretinoin can only be prescribed by a physician experienced in the use of general retinoids in the treatment of severe forms of acne and full knowledge of the risks associated with the use of isotretinoin and the requirements for patient monitoring. Orally. Adults (including adolescents and elderly patients): initially 0.5 mg / kg per day. It is necessary to adjust the dosage individually. For most patients, the dose is 0.5-1 mg / kg. per day. Long-term remission and the incidence of relapse are more dependent on the total dose given than the duration of treatment or the daily dose. Exceeding the cumulative dose of 120-150 mg / kg does not bring significant additional benefits. The duration of treatment depends on the individual daily dose. Treatment lasting from 16 to 24 weeks is usually sufficient to achieve remission. In the majority of patients, the complete resolution of acne symptoms is achieved after one treatment cycle. In the event of a clear relapse, a repetition of the treatment cycle may be considered using the same daily and cumulative dose. Due to the fact that the further disappearance of acne symptoms may occur up to 8 weeks after the end of treatment, you should not take another treatment cycle before this time.Special groups of patients. In patients with severe renal impairment, treatment should be started with a lower dose (eg 10 mg / day), which should then be increased to not more than 1 mg / kg. daily or up to the maximum dose tolerated by the patient. In patients with severe drug intolerance after the recommended dose, treatment with a lower dose may be continued; this results in prolonged therapy and is associated with a greater risk of relapse; to achieve the maximum possible treatment efficacy in these patients, treatment should be continued with the highest dose tolerated by the patient. Isotretinoin is not indicated for the treatment of acne prior to puberty and is not recommended for use in children under 12 years of age.Way of giving. The capsules should be taken with food once or twice a day.