Mercazolil-Health tablets 5mg in plastic containers No. 100 No. 1

NameMerkazolil-Zdorovye tabl 5mg in plastic container. No. 100 in pack No. 1 Physical and chemical properties Tablets of white or white color with a yellowish tint, with a flat surface and a bevel. Active ingredient: 1 tablet contains thiamazole 5 mg; excipients: potato starch, calcium stearate, sucrose, talc. Pharmacotherapeutic group Antithyroid drugs. Sulfur-containing imidazole derivatives. ATS code: H03B B02. Pharmacological properties Pharmacodynamics. Antithyroid agent. The mechanism of thyreostatic action is due to the inhibition of the activity of the peroxidase enzyme involved in the iodination of thyroid hormones of the thyroid gland, which leads to a violation of the synthesis of thyroxine and triiodothyronine. This property allows symptomatic treatment of thyrotoxicosis, regardless of its etiology. Thiamazole does not affect the secretion of pre-synthesized thyroid hormones, which explains the duration of the latent period until the concentration of thyroxine and triiodothyronine in the blood serum normalizes, resulting in an improvement in the clinical picture of the disease. Does not affect thyrotoxicosis, which has developed due to the release of hormones after the destruction of thyroid cells (after treatment with radioactive iodine or with thyroiditis). Pharmacokinetics. After ingestion, it is quickly and completely absorbed from the digestive tract. Cmax in blood plasma is reached in 40-80 minutes. It practically does not bind to plasma proteins. Thiamazole accumulates in the thyroid gland and is metabolized very slowly, and therefore a concentration plateau is formed on the kinetic curve, which persists for 24 hours after taking a single dose of the drug. The pharmacological activity of the metabolites is currently unknown. The kinetics of metabolism does not depend on the function of the thyroid gland. T? is 3 hours; in patients with hepatic insufficiency it is longer. Excreted with urine and bile, to a small extent – with faeces. It is excreted in the urine as metabolites (70% within 24 hours) and unchanged substance. There are limited data on the pharmacokinetics of thiamazole in patients with renal and hepatic insufficiency. There are no pharmacokinetic data after repeated dosing. Indications Treatment of thyrotoxicosis. Conservative treatment of thyrotoxicosis, especially with absent or small goiter. Preparation for surgical treatment in all forms of thyrotoxicosis. Preparation for the treatment of thyrotoxicosis with radioactive iodine. Therapy during the latent period of radioactive iodine. thyrotoxicosis in history. Contraindications Hypersensitivity to the components of the drug / other derivatives of thionamides, moderate and severe disorders of the quantitative composition of the blood (granulocytopenia), cholestasis before treatment, bone marrow damage during previous therapy with thiamazole or carbimazole, combined therapy with the drug and thyroid hormones during pregnancy contraindicated (see section “Use during pregnancy or lactation”). Dosage and administration Use the daily dose once or divide into several doses during the day. At the beginning of treatment, single doses should be taken throughout the day, at regular intervals. Maintenance dose taken at one time, during or after breakfast. Take the tablets without chewing, drinking plenty of liquid. General recommendations for dosing. Adults. Depending on the severity of the disease and the intake of iodine in the body, the recommended dose for adults is 10-40 mg per day. In many cases, inhibition of thyroid hormone production is provided by taking 20-30 mg of the drug per day. In the case of a mild disease, prescribe the drug at a lower dosage, with a severe degree of the disease, it is necessary to use the drug at an initial dose of 40 mg per day. Dose adjustment should be carried out individually, taking into account the activity of metabolic processes due to the level of thyroid hormone production. For maintenance therapy, the following dosing is recommended: a maintenance dose of the drug, 5-20 mg per day in combination with levothyroxine, for the prevention of hypothyroidism; in the form of monotherapy, 2.5-10 mg of the drug per day. In the case of thyrotoxicosis due to high iodine content, it is possible to use the drug in higher doses. Children. Use in children and adolescents from 3 to 17 years. The initial dose for children over 3 years of age and adolescents should be adjusted according to the patient’s body weight. Usually, treatment is initiated at a dose of 0.5 mg/kg divided into 2 or 3 equal single doses. For further treatment, the maintenance dose may be reduced depending on the patient’s response to therapy and administered once a day. Additional treatment with levothyroxine may be required to avoid hypothyroidism. The total daily dose should not exceed 40 mg of thiamazole. Use in children (2 years of age and younger) The safety and efficacy of thiamazole in children aged 2 years and younger has not been studied. Therefore, the use of thiamazole in children aged 2 years and younger is not recommended. Conservative treatment of thyrotoxicosis. The duration of therapy with the drug ranges from 6 months to 2 years (average – within 1 year). The possibility of extending the period of remission depends on the duration of therapy. In cases where it is not possible to ensure remission, and other therapeutic measures are not possible, the drug can be used for long-term therapy at the lowest effective doses or in combination with a low dose of levothyroxine. In patients with narrowing of the trachea and a very large goiter, the drug should be used for a short period. Prolonged therapy may lead to the growth of goiter. The therapy is preferably carried out in combination with thyroid hormones. Preparation for surgical treatment in all forms of thyrotoxicosis. Short-term preparatory therapy (within 3-4 weeks, in some cases the drug can be used longer) helps to restore the euthyroid state, thereby reducing the risks associated with surgery. Surgical intervention is performed immediately after reaching the euthyroid state. Therapy with the drug can be completed the day before the operation. During the last 10 days before surgery, the surgeon may additionally prescribe high doses of iodine to strengthen the thyroid tissue. Preparation for the treatment of thyrotoxicosis with radioactive iodine. The drug should be used to achieve a euthyroid state before starting therapy with radioactive iodine. Especially, previous therapy with the drug is necessary for patients with severe thyrotoxicosis, since isolated cases of thyrotoxic crisis have been observed after iodine treatment without previous thiamazole therapy. It should be borne in mind that thiourea derivatives can reduce the sensitivity of thyroid tissue to radiation therapy. When carrying out planned therapy with the use of radioactive iodine in connection with autonomic adenomas, it is necessary to carry out preliminary therapy with the drug to prevent activation of the paranodular tissue. Therapy in the latent period of action of radioactive iodine. The duration and dose of the drug are selected individually depending on the severity of the disease, as well as taking into account the period before the onset of action of radioactive iodine (approximately 4-6 months). Prevention of thyrotoxicosis with the appointment of iodine preparations, with the existence of latent thyrotoxicosis, autonomic adenomas or thyrotoxicosis in history. Usually the recommended dose is 10-20 mg of the drug per day and / or 1 g of perchlorate daily for 10 days (for example, if it is necessary to administer a radiopaque agent that is excreted by the kidneys). The duration of prophylactic treatment is determined taking into account the duration of the period during which iodine preparations are in the body. Special groups of patients. In patients with impaired liver function, the rate of elimination of thiamazole decreases. In this regard, the drug is recommended to be used in the lowest possible effective doses; during the period of drug therapy, it is necessary to monitor the patient’s condition. In patients with renal insufficiency, individual dose adjustment and constant monitoring are recommended, since there is insufficient data on the pharmacokinetic properties of the drug in this group of patients. Elderly patients are recommended individual dose adjustment and constant monitoring, there are no data on the accumulation of the drug in the body. The drug is recommended to be used in the lowest effective doses. Use during pregnancy or breastfeeding Usually, during pregnancy, thyroid function returns to normal. However, continued treatment of thyrotoxicosis is often required, especially in the first months of pregnancy. Due to the increased activity of the thyroid gland during pregnancy, serious complications are possible, such as premature birth or intrauterine malformations. The use of thiamazole in high doses for the treatment of thyrotoxicosis also increases the risk of miscarriage. Thiamazole crosses the placental barrier. In the case of taking the drug in incorrectly selected doses, there is a threat of growth of the thyroid gland and the development of hypothyroidism in the fetus, as well as a decrease in the body weight of the fetus. There are repeated reports of cases of partial skin aplasia in newborns from women who received thiamazole. The defect healed spontaneously after a few weeks. Also, the occurrence of various malformations, such as choanal atresia, esophageal atresia, nipple hypoplasia, as well as mental and motor retardation, which are associated with the use of high doses of thiamazole during the first weeks of pregnancy. However, studies of several cases of prenatal exposure to thiamazole did not reveal violations of morphological development and did not confirm the effect of the drug on the development of hypothyroidism or on the physical and mental development of children. Due to the impossibility of completely eliminating the toxic effect on the fetus, the drug should be prescribed during pregnancy after a thorough benefit / risk assessment. The drug should be used in the lowest effective dose, do not prescribe additional hormones. Thiamazole passes into breast milk, where its concentration reaches the level of concentration in the mother’s blood serum, which causes the risk of developing hypothyroidism in a child. During breastfeeding, the drug should be prescribed in the lowest effective doses, not exceeding 10 mg per day, without additional prescription of hormones. It is necessary to regularly monitor the function of the thyroid gland in newborns. Side effects The side effects listed below are presented in accordance with the following gradation of frequency: very often (? 1/10); often (?1/100, <1/10), infrequently (?1/1000, <1/100), rarely (?1/10000, <1/1000), very rarely (<1/10000), frequency unknown (it is not possible to determine the frequency from the available data). On the part of the blood and lymphatic system: infrequently: agranulocytosis (may occur in 0.3-0.6% of cases, symptoms may appear weeks or months after the start of treatment, in most cases disappears on their own after stopping the drug); very rarely: thrombocytopenia, pancytopenia, generalized lymphadenopathy. On the part of the endocrine system: very rarely - insulin autoimmune syndrome with a sharp decrease in the concentration of glucose in the blood. On the part of the nervous system: rarely: taste disturbances (dysgeusia, ageusia), which disappear on their own after discontinuation of the drug (sometimes taste sensations are restored a few weeks after the end of the course of treatment); very rarely: neuritis, polyneuropathy; medicinal fever. From the digestive system: very rarely: acute inflammation of the salivary glands. From the hepatobiliary system: very rarely - cholestatic jaundice or toxic hepatitis. Symptoms usually disappear after stopping the drug. Clinical subtle symptoms of bile stasis during the treatment period should be distinguished from dysfunctions caused by hyperthyroidism, such as increased levels of ?-glutamyltransferase and alkaline phosphatase. On the part of the skin: very often: allergic skin reactions (itching, rashes, urticaria), usually of moderate severity, which disappear with further therapy; very rarely: severe forms of allergic skin reactions, including generalized dermatitis, alopecia, drug-induced lupus erythematosus. From the musculoskeletal system: often: arthralgia, which develops gradually and may occur even after several months of therapy. Children and adolescents The frequency, type and severity of side effects in children and adults are similar. Very rarely, severe skin hypersensitivity reactions such as generalized dermatitis, including Stevens-Johnson syndrome, have been reported in adults and in children and adolescents. Report suspected adverse reactions. It is important to report suspected adverse reactions after registration of a medicinal product in order to ensure continuous monitoring of the benefit-risk balance of the medicinal product. Medical professionals are advised to report any suspected adverse drug reactions through the national system for reporting adverse reactions (UE Center for Expertise and Testing in Healthcare M3 RB, rceth.by), as well as to the manufacturer LLC Pharmaceutical Company Zdorovye. accidental intake of high doses of thiamazole are unknown.Overdose can lead to the development of hypothyroidism and, due to the effect of a lack of hormones, to activation of the adenohypophysis with subsequent growth of goiter.In this case, the drug should be discontinued and, if necessary, additional administration of thyroid hormones should be prescribed.Interaction with other drugs and other interactionsIodine deficiency increases thyroid drug sensitivity, and excess iodine reduces it Other direct interactions with other medicinal products are not known. tvenny means at a hyperthyroidism can increase. These indicators are normalized when the function of the thyroid gland is restored. If necessary, the dosage of the drug should be adjusted. There is also evidence that the correction of hyperthyroidism can normalize the increased activity of anticoagulants in patients with hyperthyroidism. Studies to identify drug interactions in children and adolescents have not been conducted. Precautions The drug is not recommended for use in patients with a history of hypersensitivity reactions (allergic rashes, itching). Patients with a very large goiter and narrowing of the trachea should use the drug with caution and for the shortest possible period. Before starting treatment, special attention should be paid to the symptoms of agranulocytosis (stomatitis, pharyngitis, high body temperature). Usually, symptoms occur at the beginning of treatment, but they may appear after a few months or during a second course of treatment. It is recommended to monitor blood counts before and after the start of therapy, especially in patients suffering from moderate granulocytopenia. If any of the above symptoms develop, especially during the first week of treatment, you should immediately consult a doctor for a blood test. If agranulocytosis is confirmed, further drug therapy should be discontinued. In the case of the use of the drug in recommended doses, adverse reactions due to toxic effects on the bone marrow occurred in rare cases. Similar reactions were observed while taking thiamazole at very high doses (about 120 mg per day). Such doses of the drug are prescribed in individual cases (severe forms of the disease, thyrotoxic crisis). If symptoms of a toxic effect on the bone marrow appear during drug treatment, further use of the drug should be discontinued. An excess of the drug in the body after taking very high doses can lead to the development of subclinical / clinical hypothyroidism or the growth of goiter due to increased secretion of thyroid-stimulating hormone. In this regard, the dose of the drug must be reduced immediately after the restoration of the normal functioning of the thyroid gland, if necessary, prescribe levothyroxine. It is not recommended to completely stop treatment with the drug and use only levothyroxine. An increase in goiter during therapy with the use of the drug, despite the inhibition of thyroid-stimulating hormone secretion, occurs due to the disease itself and cannot be prevented by additional administration of levothyroxine. In the post-marketing period, acute pancreatitis has been reported in patients treated with thiamazole or its prodrug carbimazole. In the event of acute pancreatitis, thiamazole should be discontinued immediately. Thiamazole should not be administered to patients with a history of acute pancreatitis after taking thiamazole or its prodrug carbimazole. Resumption of exposure may lead to acute recurrence of pancreatitis with a reduction in time to symptom onset. Ensuring normal levels of thyroid-stimulating hormone secretion is important to minimize the risk of manifestation or worsening of endocrine ophthalmopathy. However, this pathology often does not depend on the course of thyroid disease. Such complications are not a reason to change the treatment regimen and are not an adverse reaction if the course of treatment is carried out correctly. In the rarest cases, after a course of antithyroid therapy without surgical intervention, cases of late hypothyroidism have been observed. This is not an adverse reaction to the drug, but the result of inflammatory and destructive processes in the thyroid parenchyma caused by the underlying disease. By reducing the pathologically increased energy expenditure in hyperthyroidism, body weight may increase during treatment with the drug. The improvement of the clinical picture indicates the normalization of energy exchange. Women of childbearing age and women of childbearing potential should use a reliable method of contraception during treatment. The use of thiamazole in pregnant women should be based on an individual assessment of risk and benefit. The drug contains refined sugar, which should be taken into account in patients with diabetes mellitus. The ability to influence the reaction rate when driving vehicles or working with other mechanisms The drug does not affect the ability to drive vehicles or work with other mechanisms. Shelf life 5 years. Storage conditions Store in the original packaging at a temperature not exceeding 25 °C. Keep out of the reach of children. Packaging Tablets of 5 mg. 100 tablets in a plastic container; 1 container, together with instructions for medical use, is placed in a cardboard box. 10 tablets in a blister of PVC film and aluminum foil; 10 blisters, together with instructions for medical use, are placed in a cardboard box. Vacation categoryBy prescription. 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