Tyrozol tablets p/o 5mg №10×5

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Tyrozol tabl p / captivity. about. 5mg in bl. in pack. No. 10×5
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Round biconvex film-coated tablets of light yellow color with a notch for breaking on both sides of the tablet, with a diameter of about 9.1 mm, a thickness of about 3.7 mm The main active ingredient thiamazole Release form Tablets Dosage 5 mg Special instructions Tyrozol® is not recommended for use in patients with hypersensitivity reactions history (eg, allergic rash, itching). Thyrozol® should only be used as short-term therapy and under close supervision of patients with enlarged goiter and the risk of tracheal narrowing due to goiter growth. Agranulocytosis was noted in about 0.3 – 0.6% of cases. Therefore, before starting therapy, patients should be informed about concomitant symptoms (stomatitis, pharyngitis, fever). It usually develops in the first weeks of treatment, but may also occur several months after the start of therapy, as well as when therapy is resumed. Close monitoring of blood counts before and after initiation of therapy is recommended, especially in patients with pre-existing granulocytopenia. If any of these symptoms occur, especially in the first weeks of treatment, patients should be advised to immediately inform their physician for a blood test. In case of confirmation of agranulocytosis, the use of the drug should be suspended. When using the drug in the range of recommended doses, other myelotoxic side effects were occasionally noted. They have often been observed with the use of very high doses of thiamazole (about 120 mg per day). These dosages should be reviewed taking into account special indications (severe course of the disease, thyrotoxic crisis). With the development of bone marrow toxicity during treatment with thiamazole, it is necessary to suspend the use of this drug and, if necessary, switch to the use of an antithyroid drug belonging to another group of drugs. High doses can lead to subclinical or clinical hypothyroidism and goiter growth due to elevated TSH levels. Therefore, the dose of thiamazole should be reduced immediately after reaching the euthyroid state of metabolism, and, if necessary, additional levothyroxine should be prescribed. You should not completely stop the use of thiamazole and continue treatment with levothyroxine alone. Growth of goiter during thiamazole therapy, despite suppression of TSH production, is the result of the underlying disease, and this effect cannot be prevented by additional treatment with levothyroxine. Achieving normal TSH levels is critical to minimizing the risk of developing or worsening endocrine orbitopathy. However, this condition often does not depend on the course of thyroid disease. Such a complication in itself is not a reason to change a sufficient treatment regimen, and it cannot be considered as an adverse reaction to ongoing appropriate therapy. In rare cases, late onset hypothyroidism may develop after antithyroid therapy without any additional ablative measures. It probably represents an adverse reaction associated with the drug, but, at the same time, is considered as an inflammatory and destructive process in the thyroid parenchyma due to the underlying disease. The reduction in pathologically increased energy intake in hyperthyroidism may lead to a possible increase in body weight during treatment with thiamazole. Patients should be informed that their energy intake will return to normal as their general condition improves. Tyrosol contains lactose; therefore, this drug should not be used in patients with rare hereditary disorders of galactose intolerance or lactase deficiency or glucose-galactose malabsorption. Pregnancy and lactation In general, pregnancy has a positive effect on hyperthyroidism. However, it may be necessary to treat hyperthyroidism, especially in the first months of pregnancy. Untreated hyperthyroidism during pregnancy can lead to serious complications such as premature birth and malformations. However, hypothyroidism caused by treatment with inappropriate doses of thiamazole may also be associated with miscarriage. Tyrozol® crosses the placental barrier and in the blood of the fetus can reach concentrations equal to those observed in the mother’s serum. The use of inappropriate dosages of the drug can lead to the formation of goiter and hypothyroidism in the fetus, as well as a decrease in the body weight of the newborn at birth. There have been numerous cases of partial skin aplasia in newborns born to mothers treated with thiamazole. This defect heals spontaneously within a few weeks. In addition to this, a certain pattern of various malformations is associated with high-dose thiamazole therapy in the first weeks of pregnancy – for example, choanalatresia, esophageal atresia, nipple hypoplasia, mental retardation, as well as motor development. In contrast, several case studies of prenatal exposure to thiamazole did not reveal any morphological developmental disorders, nor effects on thyroid development or physical and mental development of children. Since an embryotoxic effect cannot be completely excluded, Tyrozol® can be used during pregnancy only after a careful assessment of the benefits and risks, and only at the lowest effective dose without the additional use of thyroid hormones. Thyrozol passes into breast milk, where it can reach concentrations corresponding to maternal serum levels; therefore, there is a risk of developing hypothyroidism in infants. It is possible to carry out breastfeeding during the period of treatment with thiamazole; however, in this case, only low doses can be used – up to 10 mg per day and without additional use of thyroid hormones. It is necessary to carry out regular monitoring of thyroid function in infants. Features of the effect of the drug on the ability to drive a vehicle or potentially dangerous mechanisms No data are available. The possibility of side effects (headache, dizziness, weakness, etc.) should be taken into account. Pharmacological properties Pharmacodynamics Tyrozol® dose-dependently inhibits the incorporation of iodine into tyrosine and thus the neosynthesis of thyroid hormones. This property allows symptomatic therapy of hyperthyroidism, regardless of its cause. At present, there is no precise data on the further possibility of thiamazole to have an effect on the “natural course” of immunologically induced hyperthyroidism (Graves’ disease), i.e. whether it can suppress the main immunopathogenic process. It does not affect the release of previously synthesized hormones from the thyroid gland. This explains why in different cases there is a different duration of the latent period until normalization of serum thyroxine and triiodothyronine concentrations is achieved, and, thus, until clinical improvement. Hyperthyroidism resulting from the release of hormones after destruction of thyroid cells is not affected, for example, after radioactive iodine therapy or in thyroiditis. Pharmacokinetics Thiamazole is rapidly and almost completely absorbed when taken orally. The maximum plasma concentration is reached within 0.4 – 1.2 hours. It practically does not bind to plasma proteins. Thiamazole accumulates in the thyroid gland, where it is slowly metabolized. Despite changes in serum concentrations, the accumulation of thiamazole in the thyroid gland still leads to stable concentrations. This results in a long lasting effect, about 24 hours after a single dose. The dependence of kinetics on the functional state of the thyroid gland was not revealed. The half-life is about 3-6 hours, with liver failure it increases. Metabolism of thiamazole is carried out in the kidneys and liver; low fecal excretion is observed, indicating enterohepatic circulation. 70% of the substance is excreted through the kidneys within 24 hours. Only a small amount is excreted unchanged. Currently, there are no data on the pharmacological activity of metabolites. Indications for use Treatment of hyperthyroidism, including the following: conservative treatment of hyperthyroidism, especially if there is little or no goiter; preparation for surgery in all forms of hyperthyroidism; preparation for planned treatment with radioactive iodine, in particular in patients with severe forms of hyperthyroidism; intermittent therapy after radioactive iodine treatment. prophylactic treatment in patients with latent (latent) hyperthyroidism, autonomic adenomas, or with a history of hyperthyroidism, for whom iodine treatment is mandatory (for example, when examining using iodine-containing contrast media). Route of administration and doses Dosage in adults Depending on the severity of the disease and iodine intake, treatment usually begins with daily doses of Tyrozol® from 10 to 40 mg. In many cases, suppression of thyroid hormone production can usually be achieved with initial doses of 20 to 30 mg Tyrosol® per day. In less severe cases, a full blocking dose may not be required and a lower starting dose may be considered. In severe cases of hyperthyroidism, an initial dose of 40 mg Tyrosol® may be required. The dose is adjusted individually depending on the metabolic state of the patient – as will be indicated by the development of the status of thyroid hormones. For maintenance therapy, one of the following treatment options is recommended: The daily maintenance dose is 5-20 mg of Thyrozol® in combination with levothyroxine to avoid hypothyroidism. Monotherapy in daily doses of 2.5 – 10 mg Tyrosol®. Iodine-induced hyperthyroidism may require higher dosages. Dosage in children Use in children and adolescents (3 to 17 years of age) The initial dose of treatment in children and adolescents (3 to 17 years of age) should be calculated based on the patient’s body weight. As a rule, treatment is started with a dose of 0.5 mg/kg divided into two or three equal parts. For maintenance therapy, the daily dose may be reduced and given once a day depending on the patient’s response to treatment. Additional treatment with levothyroxine may be required to prevent hypothyroidism. The total daily dose of Thyrozol should not exceed 40 mg/day. Conservative treatment of hyperthyroidism The goal of therapy is to achieve a euthyroid metabolic state and long-term remission after a limited duration of treatment. Depending on the individual patients receiving treatment, remission can be achieved in up to 50% of patients after one year. The frequency of remission varied considerably. Likely factors influencing are the type of hyperthyroidism (immunogenic or non-immunogenic), duration of treatment, dose of thiamazole, and dietary or iatrogenic iodine intake. With conservative treatment of hyperthyroidism, therapy is usually continued for 6 months to 2 years (average 1 year). From a statistical point of view, the likelihood of remission increases with increasing duration of therapy. In cases where it is not possible to achieve remission of the disease by certain therapeutic measures, Tyrozol® can be used as long-term antithyroid therapy at the lowest possible dosage without the addition or combination with low doses of levothyroxine. Patients with enlarged goiter and narrowing of the trachea should, if necessary, undergo only short-term treatment with Tyrozole®, since its long-term use can lead to an increase in goiter. Careful monitoring of therapy ((TSH (thyroid stimulating hormone), tracheal lumen) may be required. Treatment is preferably carried out in combination with the additional use of thyroid hormones. Preoperative therapy Pretreatment can be used to achieve a euthyroid metabolic state in order to reduce the risks associated with surgery.Depending on individual needs, the duration of treatment can be about 3 – 4 weeks or longer.Surgery should be carried out as soon as the patient reaches a euthyroid state, otherwise replenishment of thyroid hormones may be required.Treatment can be completed one day before surgery Tyrozol® increases the risk of thyroid tissue damage and bleeding, which can be compensated by the addition of high doses of iodine to preoperative therapy for ten days before surgery (Plummer iodine therapy). Treatment before radioactive iodine therapy Achieving a state of euthyroid metabolism before starting radioactive iodine therapy is an important factor, in particular in severe hyperthyroidism, since in some cases a post-therapeutic thyrotoxic crisis has been observed after such therapy without prior treatment. Note: Thionamide derivatives may reduce the radiosensitivity of thyroid tissue. In the planned therapy with radioactive iodine, with an autonomous adenoma, it is necessary to avoid activation of the paranodular tissue through preliminary treatment. Intermittent antithyroid therapy after radioactive iodine treatment The duration of treatment and the doses to be used must be determined individually depending on the severity of the clinical picture of the approximate period of time before the onset of the effectiveness of radioactive iodine therapy (approximately 4-6 months). Prophylactic treatment in patients at risk of developing hyperthyroidism as a result of the use of iodine-containing substances for diagnostic purposes In general, daily doses of 10-20 mg of thiamazole and / or 1 g of perchlorate are used for approximately 10 days (for example, for contrast media excreted through the kidneys). The duration of treatment depends on the period of time during which the iodine-containing substance is in the body. Special groups of patients In patients with hepatic insufficiency, a reduced plasma clearance of thiamazole is observed. Therefore, it is necessary to use the lowest possible dose of the drug, and patients must be closely monitored. Due to the lack of pharmacokinetic data on the use of Thyrozol® in patients with renal insufficiency, individual dosage adjustments must be made with caution, and careful monitoring is recommended. The dose should be as low as possible. Although there is no accumulation of the drug in elderly patients, it is still necessary to carefully adjust individual dosing, and careful monitoring is recommended. Method of administration Tablets must be swallowed whole with a sufficient amount of liquid. During initial therapy with high doses for hyperthyroidism, the above single doses can be divided into several doses and taken throughout the day at regular intervals. The maintenance dose can be taken 1 time in the morning – during or after breakfast. Interaction with other drugs Iodine deficiency increases the response of the thyroid gland to thiamazole, and vice versa, an increased content of iodine reduces this reaction. Other types of direct interaction with other drugs are unknown. However, it must be taken into account that the metabolism and elimination of other drugs may be accelerated in hyperthyroidism. They are normalized when normalization of thyroid function is achieved. If necessary, the dosage should be adjusted. Moreover, the appearance of signs indicating an improvement in the state of hyperthyroidism may mean normalization of increased activity of anticoagulants in patients with hyperthyroidism. Contraindications Hypersensitivity to thiamazole, other thionamide derivatives or any of the excipients that make up the drug. agranulocytosis, granulocytopenia; cholestasis before treatment; previously noted bone marrow damage after treatment with thiamazole or carbimazole; combined therapy with thiamazole and thyroid hormones during pregnancy and lactation children under 3 years of age With caution large goiter with narrowing of the trachea , magnesium stearate, hypromellose 2910/15, talc, powdered cellulose, corn starch, lactose monohydrate composition of the film shell: iron oxide yellow (E 172), dimethicone 100, macrogol 400, titanium dioxide (E 171), hypromellose 2910/15 Overdose Symptoms: overdose leads to hypothyroidism with symptoms of low metabolism. Through the feedback effect, there is an activation of the anterior pituitary gland with subsequent growth of the goiter. Treatment: dose reduction as soon as possible after reaching a euthyroid state of metabolism and, if necessary, the addition of levothyroxine to therapy. The negative consequences of accidental use of high doses of thiamazole are unknown. Side effectsCirculatory and lymphatic systems Uncommon: agranulocytosis was observed in 0.3% – 0.6% of cases. Symptoms may appear even weeks and months after the start of treatment and lead to the need to discontinue the drug; Very rare: generalized lymphadenopathy, thrombocytopenia, pancytopenia. Endocrine system Very rare: insulin autoimmune syndrome with hypoglycemia (with a pronounced decrease in blood glucose). Nervous system Rare: reversible change in taste; Very rare: neuritis, polyneuropathy. Gastrointestinal disorders Very rare: salivary gland enlargement, vomiting. Liver and biliary tract disorders Very rare: cholestatic jaundice and toxic hepatitis. Symptoms usually resolved after discontinuation of the drug. A differential diagnosis should be made between clinically silent symptoms of cholestasis during the treatment period and disorders caused by hyperthyroidism – such as increases in GGT (gamma-glutamyltransferase) and alkaline phosphatase or its isoenzyme, specific for bones. Disorders of the skin and subcutaneous tissues Very often: allergic skin reactions (itching, redness, rashes). They are usually mild and often resolve with continued therapy; Very rare: generalized skin rash, hair loss, lupus-like syndrome. Musculoskeletal and connective tissue disorders Common: Gradual development of arthrolgia after several months of treatment Complications of a general nature and reactions at the injection site Rare: fever, weakness, weight gain. Storage conditionsStore in a dry place at a temperature not exceeding 25ºC. Keep out of the reach of children! Buy Tyrozol tablets p/o 5mg No. 10×5