Tyrozol tablets 10mg, No. 50

• Thyrotoxicosis;

• preparation for surgical treatment of thyrotoxicosis;

• preparation for the treatment of thyrotoxicosis with radioactive iodine;

• therapy in the latent period of the action of radioactive iodine (carried out before the onset of the action of radioactive iodine - within 4-6 months);

• long-term maintenance therapy of thyrotoxicosis, when, due to a general condition or for individual reasons, it is impossible to perform radical treatment (in exceptional cases);

• prevention of thyrotoxicosis when prescribing iodine preparations (including cases of using iodine-containing X-ray contrast agents), in the presence of latent thyrotoxicosis, autonomic adenomas or thyrotoxicosis in history.

Inside, after meals, without chewing, with a sufficient amount of liquid.

The daily dose is prescribed in one dose or divided into 2-3 single doses. At the beginning of treatment, single doses are applied throughout the day at a strictly defined time.

The maintenance dose should be taken in 1 dose after breakfast.

Thyrotoxicosis: depending on the severity of the disease - 20-40 mg / day TyrozolЃ for 3-6 weeks. After normalization of thyroid function (usually after 3Ц8 weeks), they switch to a maintenance dose of 5Ц20 mg / day. From this time on, additional intake of levothyroxine sodium is recommended.

In preparation for the surgical treatment of thyrotoxicosis: appoint 20-40 mg / day until the euthyroid state is reached. From this time on, additional intake of levothyroxine sodium is recommended.

In order to reduce the time required to prepare for the operation, beta-blockers and iodine preparations are additionally prescribed.

In preparation for treatment with radioactive iodine: 20Ц40 mg / day until the euthyroid state is reached.

Therapy during the latent period of the action of radioactive iodine: depending on the severity of the disease - 5Ц20 mg before the onset of the action of radioactive iodine (4Ц6 months).

Long-term thyreostatic maintenance therapy: 1.25; 2.5; 10 mg / day with the additional intake of small doses of levothyroxine sodium. In the treatment of thyrotoxicosis, the duration of therapy is from 1.5 to 2 years.

Prevention of thyrotoxicosis when prescribing iodine preparations (including the use of iodine-containing X-ray contrast agents) in the presence of latent thyrotoxicosis, autonomic adenomas or thyrotoxicosis in history: 10-20 mg / day TyrozolЃ and 1 g of potassium perchlorate per day for 8-10 days before taking iodine funds.

Dosage in children. Not recommended for use in children from 0 to 3 years old. For children from 3 to 17 years old, TyrozolЃ is prescribed in an initial dose of 0.3Ц0.5 mg / kg, which is divided into 2Ц3 equal doses, daily; the maximum recommended dose for children weighing more than 80 kg is 40 mg / day.

Maintenance dose - 0.2Ц0.3 mg / kg of body weight per day, if necessary, additionally appoint levothyroxine sodium.

Dosage in pregnant women. Pregnant women are prescribed in the lowest possible doses: single dose - 2.5 mg, daily dose - 10 mg.

In liver failure, the minimum effective dose of the drug is prescribed under close medical supervision.

In preparation for the operation of patients with thyrotoxicosis, treatment with the drug is carried out until the euthyroid state is reached within 3-4 weeks before the planned day of the operation (in some cases, longer) and ends the day before it.

Film-coated tablets

1 tab.

active substance:

thiamazole 5 mg

excipients: colloidal silicon dioxide - 2 mg; sodium carboxymethyl starch - 2 mg; magnesium stearate - 2 mg; hypromellose 2910/15 - 3 mg; talc - 6 mg; cellulose powder - 10 mg; corn starch - 20 mg; lactose monohydrate - 200 mg film shell: iron dye yellow oxide - 0.04 mg; dimethicone 100 - 0.16 mg; macrogol 400 - 0.79 mg; titanium dioxide - 1.43 mg; hypromellose 2910/15 - 3.21 mg

Film-coated tablets

1 tab.

active substance:

thiamazole 10 mg

excipients: colloidal silicon dioxide - 2 mg; sodium carboxymethyl starch - 2 mg; magnesium stearate - 2 mg; hypromellose 2910/15 - 3 mg; talc - 6 mg; cellulose powder - 10 mg; corn starch - 20 mg; lactose monohydrate - 195 mg film shell: iron dye yellow oxide - 0.54 mg; iron dye red oxide - 0.004 mg; dimethicone 100 - 0.16 mg; macrogol 400 - 0.79 mg; titanium dioxide - 0.89 mg; hypromellose 2910/15 - 3.21 mg

• Hypersensitivity to thiamazole and thiourea derivatives or any other component of the drug;

• agranulocytosis during previous therapy with carbimazole or thiamazole;

• granulocytopenia (including history);

• cholestasis before starting treatment;

• therapy with thiamazole in combination with levothyroxine sodium during pregnancy;

• patients with rare hereditary diseases associated with galactose intolerance, lactase deficiency or glucose-galactose malabsorption syndrome (contains lactose);

• children age from 0 to 3 years.

With caution: should be used in patients with a very large goiter, narrowing of the trachea (only short-term treatment in preparation for surgery), with liver failure.

pharmachologic effect

Antithyroid drug. Disrupts the synthesis of thyroid hormones by blocking the enzyme peroxidase, which is involved in the iodination of thyronine in the thyroid gland to form triiodine and tetraiodothyronine. This property allows for symptomatic therapy of thyrotoxicosis, with the exception of cases of thyrotoxicosis development due to the release of hormones after the destruction of thyroid cells (after treatment with radioactive iodine or thyroiditis).

TyrozolЃ does not affect the release of synthesized thyronines from the thyroid follicles. This explains the latency period of varying duration, which may precede the normalization of the level of T3 and T4 in blood plasma, i.e. improving the clinical picture.

Reduces basal metabolism, accelerates the excretion of iodides from the thyroid gland, increases reciprocal activation of synthesis and secretion of TSH by the pituitary gland, which may be accompanied by some hyperplasia of the thyroid gland.

The duration of action of the drug after a single dose is almost 24 hours.

Pharmacokinetics

TyrozolЃ is rapidly and almost completely absorbed when taken orally. Cmax in plasma is reached within 0.4-1.2 hours. It practically does not bind to blood plasma proteins. TyrosolЃ accumulates in the thyroid gland, where it is slowly metabolized. Small amounts of thiamazole are found in breast milk. T1 / 2 is about 3-6 hours, with liver failure it increases. No dependence of kinetics on the functional state of the thyroid gland was revealed.

The metabolism of the TyrozolЃ drug is carried out in the kidneys and liver, the drug is excreted by the kidneys and with bile. 70% of the TyrozolЃ preparation is excreted by the kidneys within 24 hours, with 7-12% unchanged.

Side effect

Blood and lymphatic system: infrequently - agranulocytosis (symptoms may appear even weeks or months after the start of treatment and lead to the need to discontinue the drug); very rarely - generalized lymphadenopathy, thrombocytopenia, pancytopenia.

Endocrine system: very rarely - autoimmune insulin syndrome with hypoglycemia.

Nervous system: rarely - a reversible change in taste, dizziness; very rarely - neuritis, polyneuropathy.

Gastrointestinal disorders: very rarely - an increase in the salivary glands, vomiting.

From the liver and biliary tract: very rarely - cholestatic jaundice and toxic hepatitis.

Violations of the skin and subcutaneous tissues: very often - allergic skin reactions (itching, redness, rashes); very rarely - generalized skin rashes, alopecia, lupus-like syndrome.

From the musculoskeletal system and connective tissue: often - slowly progressive arthralgia without clinical signs of arthritis.

Complications of a general nature and reactions at the injection site: rarely - fever, weakness, weight gain.

Application during pregnancy and lactation

Lack of treatment for hyperthyroidism during pregnancy can lead to serious complications such as premature birth and fetal malformations. Hypothyroidism caused by treatment with inadequate doses of thiamazole can lead to miscarriage.

Thiamazole crosses the placental barrier and in the fetal blood it can reach the same concentration as in the mother. In this regard, during pregnancy, the drug should be prescribed only after a full assessment of the benefits and risks of its use, in the minimum effective dose (up to 10 mg / day) and without the additional use of levothyroxine sodium.

Doses of thiamazole that are significantly higher than recommended can cause goiter and hypothyroidism in the fetus, as well as cause low birth weight.

During lactation, treatment of thyrotoxicosis with TyrozolЃ, if necessary, can be continued. Because thiamazole penetrates into breast milk and can reach a concentration in it corresponding to the level in the mother's blood; hypothyroidism may develop in a newborn. It is necessary to regularly monitor the function of the thyroid gland in newborns.

Application for violations of liver function

In liver failure, the drug is prescribed in the minimum effective dose under close medical supervision.

Application in children

Not recommended for use in children aged 0 to 3 years.

special instructions

For patients with a significant enlargement of the thyroid gland, narrowing the lumen of the trachea, TyrozolЃ is prescribed for a short time in combination with sodium levothyroxine, because with prolonged use, it is possible to increase the goiter and even more compression of the trachea. It is necessary to carry out careful monitoring of the patient (monitoring the level of TSH and tracheal lumen).

During the period of drug treatment, regular monitoring of the peripheral blood picture is necessary.

Thiamazole and thiourea derivatives can reduce the sensitivity of thyroid tissue to radiation therapy.

If during treatment with the drug suddenly appear sore throat, difficulty swallowing, fever, signs of stomatitis or furunculosis (possible symptoms of agranulocytosis), stop taking the drug and immediately consult a doctor.

If during treatment subcutaneous hemorrhage or bleeding of unknown origin, generalized skin rash and itching, persistent nausea or vomiting, jaundice, severe pain in the epigastric region and severe weakness, the drug should be discontinued.

In case of early termination of treatment, a relapse of the disease is possible.

The appearance or worsening of the course of endocrine ophthalmopathy is not a side effect of properly administered TyrozolЃ treatment.

In rare cases, after the end of treatment, late hypothyroidism may occur, which is not a side effect of the drug, but is associated with inflammatory and destructive processes in the tissue of the thyroid gland, occurring within the framework of the underlying disease.

Influence on the ability to drive vehicles and mechanisms

Thiamazole does not affect the ability to drive vehicles and mechanisms.

Overdose

With prolonged use of high doses of the drug, subclinical and clinical hypothyroidism may develop, as well as an increase in the size of the thyroid gland due to an increase in TSH levels. This can be avoided by reducing the dose of the drug until the state of euthyroidism is reached or, if necessary, by additionally prescribing levothyroxine sodium drugs. As a rule, after discontinuation of the TyrozolЃ drug, spontaneous restoration of thyroid function is observed. Taking very high doses of thiamazole (about 120 mg / day) can lead to the development of myelotoxic effects. Such doses of the drug should be used only for special indications (severe forms of the disease, thyrotoxic crisis).

Treatment: drug withdrawal, gastric lavage, symptomatic therapy, if necessary, switching to another group of antithyroid drugs.

Drug interactions

When prescribing the drug after the use of iodine-containing X-ray contrast agents in a high dose, the effect of thiamazole may be weakened.

Lack of iodine enhances the effect of thiamazole.

In patients taking thiamazole for the treatment of thyrotoxicosis, after reaching the euthyroid state, i.e. normalization of the content of thyroid hormones in the blood serum, it may be necessary to reduce the doses of cardiac glycosides (digoxin and digitoxin), aminophylline, as well as increase the doses of warfarin and other anticoagulants - coumarin and indandione derivatives (pharmacodynamic interaction).

Lithium preparations, beta-blockers, reserpine, amiodarone increase the effect of thiamazole (dose adjustment is required).

With simultaneous use with sulfonamides, metamizole sodium and myelotoxic drugs, the risk of developing leukopenia increases.

Leucogen and folic acid, when used simultaneously with thiamazole, reduce the risk of developing leukopenia.

Gentamicin enhances the antithyroid effect of thiamazole.

There are no data on the effect of other drugs on the pharmacokinetics and pharmacodynamics of the drug. However, it should be borne in mind that with thyrotoxicosis, metabolism and elimination of substances are accelerated. Therefore, in some cases, it is necessary to adjust the dose of other drugs.