Thyrozol 10mg 50 tablets — Made in Germany — Free Delivery

(Thyrozol )
Thyrozol 10mg 50 tablets — Made in Germany — Free Delivery
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MERCK Brand: MERCK

Pharmacological properties

Pharmacodynamics. Thiamazole, depending on the dose, inhibits the incorporation of iodine into tyrosine, respectively, inhibits the de novo synthesis of thyroid hormones. this property allows symptomatic treatment of thyrotoxicosis regardless of its etiology. to date, the effect of thiamazole has not been established, in addition, on the natural course of the disease in the immunologically determined form of hyperthyroidism (graves' disease), that is, whether it suppresses the immunopathogenetic process underlying the disease.

Thiamazole does not affect the secretion of previously synthesized thyroid hormones, this explains the duration of the latency period until the concentration of thyroxine and triiodothyronine in the blood plasma normalizes and the clinical picture improves as a result. Thyroxine does not affect thyrotoxicosis, which develops as a result of the release of hormones after the destruction of thyroid cells (after treatment with radioactive iodine or with thyroiditis).

Pharmacokinetics. Thiamazole is rapidly and completely absorbed from the gastrointestinal tract. After oral administration, Cmax in blood plasma is reached within 0.4-1.2 hours. It binds to blood plasma proteins to a very insignificant extent. Thiamazole accumulates in the thyroid gland and is slowly metabolized in it. Despite fluctuations in blood plasma levels, the accumulation of thiamazole in the thyroid gland maintains a concentration plateau, as a result of which the duration of action lasts for about 24 hours after taking a single dose of the preparation. According to the latest data, the kinetics of thiamazole metabolism does not depend on the function of the thyroid gland. T½ is about 3-6 hours. In patients with hepatic insufficiency, it is longer. Thiamazole is excreted in urine and bile, to a lesser extent in feces, which indicates enterohepatic circulation. 70% is excreted in the urine within 24 hours. Only a small amount of thiamazole is excreted unchanged. Information on the pharmacological activity of metabolites is currently not available. Limited data are available on the pharmacokinetics of thiamazole in patients with impaired renal and hepatic function (see APPLICATION). There are no data regarding repeated use of the dose (see APPLICATION).

Indications

Treatment of thyrotoxicosis:

  • conservative treatment of thyrotoxicosis, especially with an absent or small goiter;
  • preparation for surgical treatment for all forms of thyrotoxicosis;
  • preparation for the treatment of thyrotoxicosis with radioactive iodine, especially in patients with severe hyperthyroidism;
  • therapy in the latent period of the action of radioactive iodine;
  • prophylactic treatment of patients with a subclinical form of hyperthyroidism, autonomic adenomas or thyrotoxicosis in history, which require exposure to iodine (for example, diagnostics using iodine-containing contrast agents).

Application

The daily dose is used once or in several doses during the day. at the beginning of treatment, single doses are taken throughout the day, at regular intervals. the maintenance dose should be taken at one time, during or after breakfast. take the tablets without chewing, drinking plenty of fluids.

General dosage recommendations

Adults. Depending on the severity of the disease and the intake of iodine in the body, the recommended dose is 10–40 mg / day. In many cases, suppression of the production of thyroid hormone is provided by taking 20-30 mg of Thyrozol per day. In the case of a mild illness, the preparation should be prescribed in a minimum dose, in case of a severe illness - in an initial dose of 40 mg / day.

Dose adjustment is carried out individually, taking into account the activity of metabolic processes due to the level of thyroid hormone production. For maintenance therapy, the following dosage is recommended: maintenance dose of Thyrozol- 5–20 mg / day in combination with levothyroxine to prevent hypothyroidism; in the form of monotherapy - 2.5-10 mg of Thyrozol per day.

In the case of thyrotoxicosis caused by an increased iodine content, it is possible to use the preparation in higher doses.

Children. Thyrozol is prescribed to children at an initial dose of 0.5 mg / kg of body weight per day. After normalization of thyroid function, the dose is gradually reduced to a maintenance dose, determined taking into account the individual characteristics of metabolism. If necessary, levothyroxine is additionally prescribed.

Conservative treatment of thyrotoxicosis. The duration of Thyrozol therapy is from 6 months to 2 years (on average, 1 year). The possibility of prolonging 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 impossible, Thyrozol can be used for long-term therapy at the lowest effective doses.

In patients with tracheostenosis and very large goiter, Thyrozol should be used for a short period. Long-term therapy can lead to an increase in goiter.

Preparation for surgical treatment for all forms of thyrotoxicosis. Short-term preparatory therapy (within 3-4 weeks, in some cases the preparation 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. The therapy can be completed the day before the operation. During the last 10 days before the operation, the surgeon may additionally prescribe high-dose iodine preparations to strengthen the thyroid tissue.

Preparation for treatment of thyrotoxicosis with radioactive iodine. The preparation is used to achieve the euthyroid state before starting therapy with radioactive iodine. Especially preliminary therapy with Thyrozol is necessary for patients with severe thyrotoxicosis, since there have been isolated cases of thyrotoxic crisis after treatment with iodine without previous therapy with Thyrozol.

It should be borne in mind that thiourea derivatives can reduce the sensitivity of thyroid tissue to radiation therapy. When carrying out the planned therapy with the use of radioactive iodine in connection with autonomic adenomas, it is necessary to carry out preliminary therapy with Thyrozol to prevent the activation of paranodular tissue.

Therapy during the latent period of the action of radioactive iodine. The duration of treatment and the dose of Thyrozol are selected individually and depend on the severity of the disease, and this also takes into account the period before the onset of radioactive iodine action (approximately 4–6 months).

Prevention of thyrotoxicosis when prescribing iodine preparations, in the presence of latent thyrotoxicosis, autonomic adenomas or thyrotoxicosis in history. The usual recommended dose is 10–20 mg of Tyrosol per day and / or 1 g of perchlorate daily for 10 days (for example, if it is necessary to administer a radiopaque contrast agent that is secreted by the kidneys). The duration of preventive treatment is determined taking into account the duration of the period during which iodine preparations are in the body.

Special patient groups. In patients with impaired liver function, the rate of elimination of thiamazole decreases. In this regard, the preparation is recommended to be used in the lowest effective doses; during the period of preparation therapy, it is necessary to monitor the patient's condition.

Individual dose adjustment and continuous monitoring are recommended for patients with renal insufficiency, since there is insufficient data on the pharmacokinetic properties of the preparation in this group of patients.

Elderly patients are recommended to individually adjust the dose and constant monitoring, there is no data on the accumulation of the preparation in the body. The preparation is recommended to be used in the lowest possible effective doses.

Contraindications

Hypersensitivity to thiamazole, other thionamide derivatives and preparation components; moderate and severe violations of the quantitative composition of the blood (granulocytopenia); cholestasis before starting treatment, not caused by thyrotoxicosis; bone marrow damage during previous therapy with thiamazole or carbimazole.

Combined therapy with Thyrozol and thyroid hormones during pregnancy is contraindicated (see Use during pregnancy or lactation).

Side effects

In terms of frequency of occurrence, undesirable effects are classified into the following categories: very often (1/10), often (1/100, 1/10), infrequently (1/1000, 1/100), rarely (1/10 000, 1/1000 ), very rarely (1/10 000).

From the side of the blood and lymphatic system: infrequently - agranulocytosis (occurs in 0.3-0.6%). It can also appear weeks or months after starting treatment, which requires discontinuation of the preparation. In most cases, agranulocytosis disappears on its own; very rarely - thrombocytopenia, pancytopenia, generalized lymphadenopathy.

From the endocrine system: very rarely - insulin autoimmune syndrome (there is a pronounced decrease in blood glucose levels).

From the side of the nervous system: rarely - a violation of taste sensations (dysgeusia, ageusia), which disappear on their own after stopping the preparation. However, the sense of taste may recover after a few weeks; very rarely - neuritis, polyneuropathy.

From the side of the digestive tract: very rarely - acute inflammation of the salivary glands.

On the part of the hepatobiliary system: very rarely - individual cases of cholestatic jaundice or toxic hepatitis have been described. Symptoms usually disappear when the preparation  is stopped. Clinically subtle symptoms of bile stagnation during treatment should be distinguished from dysfunctions caused by hyperthyroidism, such as an increase in the level of γ-glutamyltransferase and ALP or an increase in the level of the specific bone isoenzyme ALP.

Skin and subcutaneous tissue disorders: very often - allergic skin reactions of varying severity (itching, rash, urticaria). Allergic skin reactions of moderate severity usually occur, often disappearing with further therapy; very rarely - severe forms of allergic skin reactions, including generalized dermatitis, alopecia, preparation-induced lupus erythematosus.

On the part of the musculoskeletal system and connective tissue: often - arthralgia, which develops gradually, may occur even after several months of therapy.

General disorders: rarely, preparation fever.

special instructions

Tiamazole is not recommended for use in patients with a history of moderate hypersensitivity reactions (eg, allergic rash, itching).

Patients with a very large goiter and narrowing of the tracheal lumen should, for the shortest possible period and under the supervision of a physician, use Thyrozol  due to the risk of progression of goiter growth.

Agranulocytosis is observed in 0.3-0.6% of cases. Before starting treatment, special attention should be paid to the symptoms of agranulocytosis (stomatitis, pharyngitis, high body temperature). Symptoms usually appear during the first weeks of treatment, but they may appear after a few months or with a second course of treatment. It is recommended to carefully monitor blood counts before and after starting therapy, especially in patients with 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 preparation therapy should be discontinued.

In the case of using the preparation in the recommended doses, adverse reactions due to toxic effects on the bone marrow occurred in rare cases. It has often been reported about the development of such reactions when taking Thyrozol in very high doses (about 120 mg). Such doses are prescribed in individual cases (severe forms of the disease, thyrotoxic crisis). If symptoms of toxic effects on the bone marrow appear during treatment with Thyrozol, further use of the preparation must be discontinued and, if necessary, switch to the use of an antithyroid preparation of another group.

An excess of the preparation in the body after taking very high doses can lead to the development of subclinical / clinical hypothyroidism or an increase in goiter due to an increase in the level of thyroid-stimulating hormone secretion. In this regard, the dose of Thyrozol must be reduced immediately after the restoration of the normal functioning of the thyroid gland; if necessary, levothyroxine is additionally prescribed. It is not recommended to completely stop treatment with Thyrozol and use only levothyroxine.

An increase in goiter during therapy with the use of the preparation Thyrozol, despite the inhibition of the secretion of thyroid-stimulating hormone, occurs as a result of the disease itself and cannot be prevented with the help of additional intake of levothyroxine.

Maintaining a normal level of thyroid-stimulating hormone secretion is important to minimize the risk of manifestation or worsening of endocrine ophthalmopathy. However, this pathology is often independent of the course of the thyroid disease. Such complications are not a reason for changing an adequate treatment regimen, as well as an adverse reaction if the course of treatment is carried out correctly.

In rare cases, after a course of antithyroid therapy without additional surgery, there have been cases of late hypothyroidism. This is probably not an adverse reaction to the preparation, 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 Thyrozol. Patients should be informed that an improvement in the clinical picture indicates the normalization of energy exchange.

Tyrosol contains lactose, so patients with rare hereditary diseases such as galactose intolerance, lactase deficiency, Lapp lactase deficiency or impaired glucose-galactose malabsorption should not use this preparation.

Application during pregnancy or lactation. Thyroid function usually returns to normal when pregnancy occurs. However, continuation of thyrotoxicosis treatment 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 improperly selected doses of thiamazole for the treatment of thyrotoxicosis also increases the risk of miscarriage.

Thiamazole crosses the placental barrier, and its concentration in the fetal blood is equal to the concentration in the mother's blood plasma. In the case of taking the preparation 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 fetal body weight. Cases of partial skin aplasia in newborns whose mothers took thiamazole have been repeatedly reported. The elimination of the defect occurred spontaneously after a few weeks.

The occurrence of various malformations has also been reported, such as choanal atresia, esophageal atresia, nipple hypoplasia, mental retardation and motor development, which is associated with the use of high doses of thiamazole during the first weeks of pregnancy. However, in the study of several cases of prenatal exposure to thiamazole, no disturbances in morphological development were detected and the effect of the preparation on the thyroid gland or the physical and mental development of children was not confirmed.

Due to the impossibility of completely eliminating the toxic effect on the fetus, Thyrozol should be prescribed during pregnancy after a careful assessment of the benefit / risk ratio. The preparation should be used in the lowest effective dose, no additional hormones should be prescribed.

Thiamazole passes into breast milk, where its concentration reaches that in the mother's blood plasma, which causes the risk of hypothyroidism in the child. During breastfeeding, Thyrozol  should be prescribed in the lowest possible effective doses, not exceeding 10 mg / day, without the additional administration of hormones. It is necessary to regularly monitor the function of the thyroid gland in newborns.

Children. The preparation should not be administered to children under the age of 3 years in this dosage form. Thyrozol is prescribed at an initial dose of 0.5 mg / kg of body weight per day. After normalization of thyroid function, the dose is gradually reduced to a maintenance dose, which is determined taking into account the individual characteristics of metabolism. If necessary, levothyroxine is additionally prescribed.

The ability to influence the reaction rate when driving or operating other mechanisms. The preparation does not affect the ability to drive vehicles or operate other mechanisms.

Interactions

Lack of iodine increases the susceptibility of the thyroid gland to tyrosol, and excess iodine reduces it. other direct interactions with other preparations are unknown. it should be borne in mind that the metabolism and excretion of other preparations in hyperthyroidism may increase. these indicators are normalized when thyroid function is restored. if necessary, the dosage of the preparation should be adjusted.

Overdose

Overdose leads to the development of hypothyroidism with the corresponding symptoms of a slowdown in metabolism and, according to the feedback mechanism, to the activation of the adenohypophysis with a further increase in goiter. this can be avoided by reducing the dose of the preparation until the euthyroid state is reached and, if necessary, additionally prescribing thyroid hormones.

Storage conditions

At a temperature not exceeding 25 ° С in a place protected from moisture.

Tags: Thyrozol

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