Description
Latin name
THYROZOL
Release form
Film-coated tablets are light yellow, round, biconvex, with risks on both sides of the cross section of the core is white or almost white.
packaging 10 pcs – blisters (5) – packs of cardboard.
Pharmacological action of
Antithyroid drug disrupts the synthesis of thyroid hormones by blocking the peroxidase enzyme involved in the thyroid gland iodination with the formation of triiodo and tetraiodothyronine. This property allows symptomatic treatment of thyrotoxicosis, with the exception of cases of thyrotoxicosis due to the release of hormones after the destruction of thyroid cells (after treatment with radioactive iodine or with thyroiditis). Tyrosol ® does not affect the release of synthesized thyronins from thyroid follicles. This explains the latent period of various durations, which may precede the normalization of the level of T3 and T4 in blood plasma, i.e. improving the clinical picture.
Reduces the main metabolism, accelerates the excretion of iodides from the thyroid gland, increases the reciprocal activation of the synthesis and secretion of the thyroid stimulating hormone, which may be accompanied by some thyroid hyperplasia.
Duration of a single dose is almost 24 hours.
Pharmacokinetics of
Tyrosol ® when administered orally is rapidly and almost completely absorbed. Cmax in plasma is reached within 0.4 1.2 hours. It practically does not bind to plasma proteins. Tyrosol ® accumulates in the thyroid gland, where it is slowly metabolized. Small amounts of thiamazole are found in breast milk. T1 / 2 – about 3-6 hours, with liver failure, it increases. No dependence of kinetics on the functional state of the thyroid gland was revealed. Metabolism of the drug Tyrosol ® is carried out in the kidneys and liver, excretion of the drug is carried out by the kidneys and with bile. 70% of Tyrosol ® is excreted by the kidneys within 24 hours, with 7-12% unchanged.
Indications
Thyrotoxicosis
preparation for the surgical treatment of thyrotoxicosis
preparation for the treatment of thyrotoxicosis with radioactive iodine
therapy in the latent period of radioactive iodine (performed before the onset of radioactive iodine – for 4 ² 6 months) when, due to the general condition or for individual reasons, it is impossible to perform radical treatment
the prevention of thyrotoxicosis with the prescription of drugs yo a (including cases of iodinated contrast media) in the presence of latent thyrotoxicosis or hyperthyroidism autonomous adenomas history.
Contraindications
Hypersensitivity to thiamazole and thiourea derivatives
agranulocytosis during previous treatment with carbimazole or thiamazole
granulocytopenia (including a history of sr up to 3 years.
Tyrosol ® contains lactose, therefore, it is not recommended for use in patients with rare hereditary diseases associated with galactose intolerance, lactase deficiency or glucose-galactose malabsorption syndrome.
With caution, the drug should be used for very large goiter with narrowing of the trachea (only short-term treatment in preparation for surgery), with liver failure.
Use during pregnancy and lactation
Lack of treatment for thyroid hyperfunction during pregnancy can lead to serious complications: premature birth, fetal malformations. However, hypothyroidism caused by treatment with inadequate doses can lead to miscarriage.
Thiamazole crosses the placental barrier and reaches the same concentration in the fetal blood as in the mother. Therefore, 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 additional use of levothyroxine sodium.
Thiamazole in doses significantly higher than recommended may cause goiter, hypothyroidism in the fetus, and a reduced birth weight in the newborn is possible.
During lactation, treatment of thyrotoxicosis with the drug Tyrosol ® can be continued if necessary. Since thiamazole is excreted in breast milk and can reach a concentration in it that corresponds to the level of thiamazole in the mother ² ¢s blood, hypothyroidism may develop in a newborn. It is necessary to regularly monitor thyroid function in newborns.
Composition
1 tab.
thiamazole 5 mg
Excipients: silicon dioxide colloidal – 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.
Composition of the film coat: iron dye oxide yellow – 0.04 mg, dimethicone 100 – 0.16 mg, macrogol 400 – 0.79 mg, titanium dioxide – 1.43 mg, hypromellose 2910/15 – 3.21 mg.
Dosage and administration of
The drug is taken orally after a meal. Tablets should be taken without chewing, drinking plenty of fluids.
The daily dose is prescribed in 1 dose or divided into 2-3 single doses. At the beginning of treatment, single doses are taken throughout the day at a strictly defined time. A maintenance dose should be taken in one dose after breakfast.
With thyrotoxicosis, depending on the severity of the disease, the drug is prescribed in a dose of 20-40 mg / day for 3-6 weeks. After normalization of thyroid function (usually after 3-8 weeks), they switch to receiving a maintenance dose of 5-20 mg / day. From this time, an additional intake of levothyroxine sodium is recommended.
In preparation for the surgical treatment of thyrotoxicosis, 20-40 mg / day is prescribed until the euthyroid state is reached. From this time, an 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, 20-40 mg / day is prescribed until the euthyroid state is reached.
During therapy in the latent period of action of radioactive iodine, depending on the severity of the disease, 5-20 mg / day is prescribed before the onset of action of radioactive iodine (4-6 months).
With prolonged thyreostatic maintenance therapy, Tyrosol ® is prescribed in doses of 1.25-2.5-10 mg / day with additional administration of levothyroxine sodium in small doses. In the treatment of thyrotoxicosis, the duration of therapy is from 1.5 to 2 years.
In order to prevent thyrotoxicosis in the appointment of iodine preparations (including cases of the use of iodine-containing radiopaque agents) in the presence of latent thyrotoxicosis, a history of autonomous adenomas or thyrotoxicosis Tyrosol ® is prescribed at a dose of 10-20 mg / day and potassium perchlorate 1 g / day for 8-10 days before taking iodine-containing drugs.
For children aged 3 to 17 years, Tyrosol ® is prescribed in an initial dose of 0.3-0.5 mg / kg body weight in 2-3 equal divided doses daily. The maximum recommended dose for children weighing more than 80 kg is 40 mg / day. The maintenance dose is 0.2-0.3 mg / kg / day. If necessary, sodium levothyroxine is additionally prescribed.
Not recommended for use in children aged 0 to 3 years.
During pregnancy, the drug is prescribed in minimal doses: single – 2.5 mg, daily – 10 mg.
In liver failure, the drug is prescribed in the minimum effective dose under close medical supervision.
When preparing patients with thyrotoxicosis for surgery, the drug is treated until the euthyroid state is reached within 3-4 weeks before the planned day of surgery (in some cases, longer) and ends the day before it.
Side effects of the
From the hematopoietic system: infrequently – agranulocytosis (symptoms can appear even weeks and months after the start of treatment and lead to the need for drug withdrawal) very rarely – generalized lymphadenopathy, thrombocytopenia, pancytopenia.
From the endocrine system: very rarely – insulin autoimmune syndrome with hypoglycemia.
From the nervous system: rarely – a reversible change in taste, dizziness is very rare – neuritis, polyneuropathy.
From the digestive system: very rarely – an increase in the salivary glands, vomiting.
From the liver and biliary tract: very rarely – cholestatic jaundice and toxic hepatitis.
From the skin and subcutaneous tissues: very rarely – generalized skin rashes, alopecia, lupus-like syndrome.
Allergic reactions: skin manifestations (itching, redness, rash).
From the musculoskeletal system: often – slowly progressive arthralgia without clinical signs of arthritis.
General reactions: rarely – fever, weakness, weight gain.
Overdose
Symptoms: prolonged use of the drug in high doses may lead to the development of subclinical and clinical hypothyroidism, as well as an increase in thyroid size due to an increase in TSH in the blood. This can be avoided by reducing the dose of the drug to the state of euthyroidism or, if necessary, additional prescription of levothyroxine sodium preparations. As a rule, after the withdrawal of the drug Tyrozol ®, there is a spontaneous restoration of thyroid function. Thiamazole intake at very high doses (about 120 mg / day) can lead to the development of myelotoxic effects. The drug in such doses should be used only for special indications (severe forms of the disease, thyrotoxic crisis).
Treatment: cancellation of the drug, gastric lavage, symptomatic therapy, switching to another group antithyroid drug, if necessary.
Storage conditions
The drug should be stored out of the reach of children, in a dry place at a temperature not exceeding 25 ° C.
The Expiration of
is 4 years.
Active e substance
thiamazole
tablet dosage form
dosage form
tablets
Merck KGaA, Germany
