Roaccutane capsules 10 mg 30 pcs
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Active ingredients
Isotretinoin
Release form
Uncoated Tablets
Composition
Active ingredient: Isotretinoin (Isotretinoin) Active ingredient concentration (mg): 10
Pharmacological effect
Retinoid for systemic treatment of acne. Isotretinoin is a stereoisomer of all-trans retinoic acid (tretinoin). The exact mechanism of action of Roaccutane has not yet been elucidated, but it has been established that the improvement in the clinical picture of severe acne is due to a decrease in their size histologically. In addition, the isotretinoin anti-inflammatory effect on the skin has been proven. Hyperkeratosis of the epithelium cells of the hair follicle and sebaceous gland leads to desquamation of the corneocytes in the duct of the gland and blockage of the latter with keratin and an excess of sebaceous secretion. This is followed by the formation of comedo and, in some cases, the addition of the inflammatory process. Roaccutane inhibits sebocyte proliferation and acts on acne, restoring the normal process of cell differentiation. Sebum is the main substrate for the growth of Propionibacterium acnes, therefore reducing the formation of sebum suppresses bacterial colonization of the duct.
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 liver enzymes involved in the metabolism of drugs. Absorption The absorption of isotretinoin from the gastrointestinal tract varies. The absolute bioavailability of isotretinoin was not determined, since the release form of the drug for intravenous use is not available in humans. However, extrapolating the data obtained in the experiment on dogs suggests a rather low and variable systemic bioavailability. In patients with acne, the maximum plasma concentration (Cmax) in the equilibrium state after administration of 80 mg of isotretinoin on an empty stomach was 310 ng / ml (range 188-473 ng / ml) and was reached in 2-4 hours. Plasma isotretinoin concentrations are about 1.7 times higher than blood concentrations,due to the poor penetration of isotretinoin into erythrocytes. Taking isotretinoin with food increases the bioavailability by 2 times compared with fasting. DistributionIzotretinoin highly (99.9%) binds to plasma proteins, mainly albumin, therefore in a wide range of therapeutic concentrations of free ( pharmacologically active fraction of the drug is less than 0.1% of its total amount. The volume of distribution of isotretinoin in humans has not been determined, since the dosage form for intravenous This dose does not exist. The equilibrium blood concentrations of isotretinoin (C ss min) in patients with severe acne, who took 40 mg of the drug 2 times a day, ranged from 120 to 200 ng / ml. The concentrations of 4-oxo-isotretinoin in these patients in 2.5 times those of isotretinoin. Data on the penetration of isotretinoin into human tissue is insufficient. The concentration of isotretinoin in the epidermis is two times lower than in serum. Metabolism After oral administration, three major metabolites are found in plasma: 4-oxo-isotretinoin, tretinoin (all-trans-retinoic acid) and 4-oxo-retinoin. The main metabolite is 4-oxo-isotretinoin, the plasma concentrations of which in equilibrium are 2.5 times higher than the concentrations of the original preparation. Found less significant metabolites, including glucuronides, however, the structure is not all metabolites. Metabolites of isotretinoin have biological activity, confirmed in several laboratory tests. Thus, the clinical effects of the drug in patients may be the result of the pharmacological activity of isotretinoin and its metabolites. Since in vivo isotretinoin and tretinoin (fully trans retinoic acid) are reversibly transformed into each other, tretinoin metabolism is associated with isotretinoin metabolism. 20-30% of the dose of isotretinoin is metabolized by isomerization. In the pharmacokinetics of isotretinoin in humans, enterohepatic circulation may play a significant role. In vitro metabolism studies have shown that several CYP enzymes are involved in the conversion of isotretinoin to 4-oxo-isotretinoin and tretinoin. Apparently, none of the isoforms plays a dominant role.Roaccutane and its metabolites do not have a significant effect on the activity of CYP system enzymes. Injection After ingestion of radioactively labeled isotretinoin, approximately the same amount is detected in urine and feces. The half-life of the terminal phase for unchanged drug in patients with acne is, on average, 19 hours. The half-life of the terminal phase for 4-oxo-isotretinoin seems to be longer and equals, on average, 29 hours. Isotretinoin refers to natural (physiological) retinoids. Endogenous retinoid concentrations are restored approximately 2 weeks after Roaccutane is taken. Pharmacokinetics in special clinical situations As isotretinoin is contraindicated in abnormal liver function, data on the pharmacokinetics of the drug in this group of patients are limited. Renal failure does not affect isotretinoin pharmacokinetics.
Indications
Severe acne (nodular / cystic, conglobate acne or acne with the risk of scarring).
Contraindications
Pregnancy, lactation, liver failure, hypervitaminosis A, severe hyperlipidemia, concomitant tetracycline therapy. Hypersensitivity to the drug or its components. Children's age up to 12 years.
Precautionary measures
Do not exceed the recommended doses. With caution: a history of depression, diabetes, obesity, lipid metabolism, alcoholism.
Use during pregnancy and lactation
Pregnancy is an absolute contraindication for Roaccutane therapy. If pregnancy occurs, despite warnings, during treatment or within a month after the end of therapy, there is a very high risk of giving birth to a child with severe developmental disabilities. Isotretinoin is a drug with a strong teratogenic effect. If pregnancy occurs during a period when a woman orally takes isotretinoin (at any dose or even a short time), there is a very high risk of having a child with developmental disabilities. Roaccutane is contraindicated for women of childbearing age unless the condition of the woman meets all of the following criteria: - she must suffer from severe acne,resistant to the usual methods of treatment; - she must surely understand and follow the instructions of the doctor; - she should be informed by the doctor about the dangers of pregnancy during Roaccutane’s treatment, one month after it and urgent consultation if a pregnancy is suspected; warned about the possible ineffectiveness of contraceptives; - she must confirm that she understands the essence of the precautions; - she must understand the need and continuously use effective methods of contraceptives within one month before Roaccutane treatment, during treatment and within a month after its termination (see the section "Interaction with Other Medicines"); It is desirable to use simultaneously 2 different methods of contraception, including the barrier method - a negative result of a reliable pregnancy test must be obtained from it within 11 days before the start of the drug; a pregnancy test is strongly recommended to be carried out monthly during treatment and 5 weeks after the end of therapy; - she should start Roaccutane treatment only on the 2-3 day of the next normal menstrual cycle; - she should understand the need for a mandatory visit to the doctor every month; - during treatment about the recurrence of the disease, she should constantly use the same effective methods of contraception for one month before starting treatment with Roaccutane, during treatment and for one month after completing it They must also fully understand the need for precautions and confirm their understanding and desire to use reliable methods of contraception, which the doctor explained to her. Use of contraceptives according to the above instructions during treatment with isotretinoin should be recommended. women who usually do not use contraception because of infertility (with the exception of patients undergoing hysterectomy), amenorrhea, or who report that they do not sexual zhizn.Vrach must be sure that: - the patient suffers from a severe form of acne (nodular, cystic, conglobata acne or acne with risk of scarring); acnenot amenable to other types of therapy; - a negative result was obtained from a reliable pregnancy test before starting to take 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 1, preferably 2 effective methods of contraception, including a barrier method, within one month before starting treatment with Roaccutane, during treatment and within a month after termination; - the patient is able understand and fulfill all the above requirements for the prevention of pregnancy; - the patient meets all of the above conditions. Pregnancy test According to current practice, test for birch con- cern with a minimum sensitivity of 25 MME / ml should be held in the first 3 days of the menstrual cycle: Prior terapiiDlya exclude the possibility of pregnancy prior to the use of contraceptives and the result of the date of initial pregnancy test should be registered doctor. In patients with irregular menstruation, the time of the pregnancy test depends on sexual activity, it should be carried out 3 weeks after unprotected intercourse. The doctor must inform the patient about the methods of contraception. A pregnancy test is carried out on the day Roakkutan is prescribed or 3 days before the patient's visit to the doctor. The specialist should register the test results. The drug can only be prescribed to patients receiving effective contraception for at least 1 month before starting Roaccutane therapy. During therapy, the patient should visit the doctor every 28 days. The need for monthly pregnancy testing is determined in accordance with local practice and taking into account sexual activity, previous violations of the menstrual cycle. If there is evidence, a pregnancy test is conducted on the day of the visit or three days before the visit to the doctor, test results must be recorded. End of therapy After 5 weeks of the end of therapy, a test is performed to rule out pregnancy. for 30 days of treatment, the continuation of therapy requires a new prescription of the drug by the doctor.We recommend a pregnancy test, prescription and receipt of the drug in one day. You should take Roakkutan at the pharmacy only for 7 days after the prescription. To help doctors, pharmacists and patients avoid the risk of Roaccutane exposure to the fetus, the manufacturing company created “ Pregnancy Protection Program ”aimed at warning of the teratogenicity of the drug and emphasizing the absolutely obligatory use of reliable contraceptive measures for women of childbearing age. The program contains the following materials: for doctors: - a guide for the doctor on Roakkutan's prescription for women; - an informed consent form for the patient; - a registration form for prescribing the drug for women; for a patient: - an information brochure for the patient, - what you need to know about contraception. - a guide for the pharmaceutical Roakkutana leave. Full information about the teratogenic risk and strict adherence to measures to prevent pregnancy should be provided to both men and women. Male patients Existing data Do not suggest that in women, exposure to the drug that comes from the semen and seminal fluid of men taking Roaccutane is not sufficient for the teratogenic effects of Roaccutane to occur. Men should be excluded from taking the drug by others, especially by women. If, despite precautions taken , during Roaccutane treatment or within a month after its termination, the pregnancy nevertheless occurred, there is a high risk of very severe fetal malformations (in particular, from the central nerve vascular system, heart and large blood vessels). In addition, the risk of miscarriages increases. When a pregnancy occurs, Roaccutane therapy is stopped. The feasibility of its preservation should be discussed with a physician specializing in teratology. Severe congenital malformations of the fetus in humans associated with Roakkutan's appointment, including hydrocephalus, microcephaly, cerebellar malformations, anomalies of the external ear (microtia, narrowing or absence of the external auditory canal, are documented. ), microphthalmia, cardiovascular anomalies (Fallot's tetrad, transposition of the great vessels, defects of the septum), facial developmental defects (cleft palate), thymus gland, patol Gia parathyroid zhelez.Poskolku Isotretinoin is highly lipophilic, it is very likely that it passes into breast milk.Due to possible side effects, Roaccutane should not be given to nursing mothers.
Dosage and administration
Inside, with a meal once or twice a day.
Side effects
Behavioral disorders, depression, headache, increased intracranial pressure, headache, nausea, vomiting, blurred vision, swelling of the optic nerve, seizures, individual cases of visual acuity, photophobia, impaired dark adaptation, color perception, lenticular cataract, keratitis, blepharitis , conjunctivitis, eye irritation, swelling of the optic nerve; hearing loss at certain sound frequencies, nausea, diarrhea, inflammatory bowel disease, bleeding; pancreatitis, anemia, decrease in hematocrit, leukopenia, neutropenia, increase or decrease in the number of platelets, accelerated ESR, bronchospasm, muscle pain with increased serum CK levels or without it, joint pain, hyperostosis, arthritis, calcification of ligaments and tendons, other changes bones, tendinitis, rash, pruritus, erythema of the face / dermatitis, sweating, pyogenic granuloma, paronychia, onychodystrophy, increased proliferation of granulation tissue, persistent hair thinning, reversible hair loss, fulminant forms of acne, hirsutism, hyper pigmentation, photosensitization, photoallergy, slight trauma to the skin, dry skin, mucous membranes, incl. lips (cheilitis), nasal cavity (bleeding), laryngopharynx (hoarseness), eye (conjunctivitis, reversible corneal clouding and intolerance to contact lenses), hypertriglyceridemia, hypercholesterolemia, hyperuricemia, reduction of high-density lipoprotein, hyperglycemia, reduction of high density lipoproteins, hyperglycemia, and hyperglycemia, vasculitis (Wegener's granulomatosis, allergic vasculitis), systemic hypersensitivity reactions, glomerulonephritis.
Overdose
In case of an overdose, signs of hypervitaminosis A may appear. In the first few hours after the overdose, gastric lavage may be necessary.
Interaction with other drugs
Because of the possible increase in symptoms of hypervitaminosis A, the simultaneous administration of Roaccutane and vitamin A should be avoided. Since tetracyclines can also cause an increase in intracranial pressure,their use in combination with Roaccutane is contraindicated. Isotretinoin may weaken the effectiveness of progesterone drugs, so do not use contraceptives containing small doses of progesterone. Combined use with local keratolytic or exfoliative drugs for the treatment of acne is contraindicated because of possible increased local irritation.
special instructions
Roaccutane should be prescribed only by physicians, preferably dermatologists, who are experienced in using systemic retinoids and who are aware of the risk of drug teratogenicity. Patients of both female and male need to issue a copy of a brochure with information for the patient. In order to avoid accidental effects of the drug on the body of other people, patients who receive or shortly before (1 month) received Roaccutane cannot be donated blood. It is recommended to control liver function and liver enzymes before treatment, 1 month after its onset, and then every 3 months or if indicated. A transient and reversible increase in hepatic transaminases is noted, in most cases within normal limits. If the level of liver transaminases exceeds the norm, it is necessary to reduce the dose of the drug or cancel it. You should also determine the level of fasting serum lipids before treatment, 1 month after the start, and then every 3 months or according to indications. Usually, lipid concentrations are normalized after dose reduction or withdrawal of the drug, as well as diet. It is necessary to control the clinically significant increase in triglycerides, since their elevation above 800 mg / dL or 9 mmol / L may be accompanied by the development of acute pancreatitis, possibly with a fatal outcome. If persistent hypertriglyceridemia or symptoms of pancreatitis, Roaccutane should be canceled. In rare cases, patients treated with Roaccutane described depression, psychotic symptoms, and very rarely - suicide attempts. Although their causal relationship with the use of the drug has not been established, special care must be taken in patients with depression in history and all patients should be monitored for depression during treatment with the drug, if necessary, referring them to the appropriate specialist.However, the cancellation of Roaccutane may not lead to the disappearance of symptoms and may require further observation and treatment by a specialist. In rare cases, at the beginning of therapy acne exacerbation is noted, which passes for 7-10 days without dose adjustment of the drug. A few years after Roaccutane has been used for treatment of dyskeratosis with a total course dose and duration of therapy, higher than those recommended for acne therapy, developed bone changes, including premature closure of epiphyseal growth zones, hyperostosis, calcium pecifications ligaments and tendons. Therefore, when prescribing a drug to any patient, you should first carefully evaluate the ratio of possible benefits and risks. Patients receiving Roaccutane are recommended to use moisturizing ointment or body cream, lip balm to reduce dry skin and mucous membranes at the beginning of therapy. During post-marketing follow-up when using Roaccutan has reported cases of severe skin reactions such as erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis. These phenomena can be serious and lead to disability, life-threatening conditions, hospitalization or fatal outcome. Patients receiving Roaccutane need to be carefully monitored to identify severe skin reactions and, if necessary, decide whether to discontinue the drug. Muscle and joint pain, increased serum creatinine phosphokinase, which may be accompanied by a decrease in the tolerance of intense physical activity, may occur. Avoid deep chemical dermaabrasion and laser treatment in patients receiving Roaccutane, as well as for 5-6 months after the end of treatment, because of possible for enhanced scarring in atypical locations and the occurrence of hyperpigmentation and hypopigmentation. During treatment with Roaccutane and for 6 months after it, epilation cannot be performed using wax because of the risk of epidermis detachment, development of scars and dermatitis. Some patients may experience a decrease in visual acuity sometimes should be informed about the possibility of this state, recommending them to be careful when driving a car at night. The state of visual acuity must be carefully monitored. Dryness of the conjunctiva of the eye, corneal opacities, deterioration of night vision and keratitis usually disappear after discontinuation of the drug.In case of dryness of the mucous membrane of the eyes, you can use applications of moisturizing eye ointment or an artificial tear preparation. It is necessary to observe patients with dry conjunctiva for possible development of keratitis. Patients complaining of vision should be referred to an ophthalmologist and consider the appropriateness of canceling Roaccutane. If contact lenses are intolerant, glasses should be used for the duration of therapy. Exposure to sunlight and UV rays should be limited. If necessary, a sunscreen with a high protective factor of at least 15 SPF should be used. Rare cases of the development of benign intracranial hypertension (“brain pseudotumor”), including, are described. when combined with tetracyclines. In such patients, Roaccutane should be discontinued immediately. With Roaccutane therapy, an inflammatory bowel disease may occur. In patients with severe hemorrhagic diarrhea, Roaccutane should be immediately discontinued. Rare cases of anaphylactic reactions, which occurred only after previous external use of retinoids, are described. Severe allergic reactions dictate the need for drug withdrawal and careful monitoring of the patient. Patients in the high-risk group (with diabetes, obesity, chronic alcoholism or impaired metabolism) may need more frequent laboratory monitoring of glucose and lipids in Roaccutane treatment. If it is suspected, more frequent determination of glycemia is recommended.