The composition and form of issue:
Tablets, film-coated. 1 tablet contains:
Tiamazol 5 mg
excipients: silicon dioxide colloidal carboximetilkrahmal sodium magnesium stearate hypromellose 2910/15 talc powder cellulose corn starch lactose monohydrate 100 Dimethicone titanium dioxide iron oxide yellow macrogol 400 hypromellose 2910/15
in blister packs of 10 or 25 PCs per cartons 2, 4, 5 or 10 blisters.
Tablets, film-coated. 1 tablet contains:
Tiamazol 10 mg
excipients: silicon dioxide colloidal carboximetilkrahmal sodium magnesium stearate hypromellose 2910/15 talc powder cellulose corn starch lactose monohydrate 100 Dimethicone titanium dioxide iron oxide yellow iron oxide red macrogol 400 hypromellose 2910/15
in blister packs of 10 or 25 PCs per cartons 2, 4, 5, or 10 blisters.
Description pharmaceutical form:
Tiamazol, 5 mg: light yellow, round, biconvex tablets, film-coated, scored on one side.
Tiamazol, 10 mg: grey-orange, round, biconvex tablets, film-coated, scored on one side.
The Matochkin: white or almost white mass.
Tiamazol when administered quickly and almost completely absorbed. Cmax in plasma is reached within 0.4 to 1.2 hours. proteins of blood plasma practically does not bind. Tiamazol accumulates in the thyroid gland, where it is slowly metabolized. A small number of Tiamazol detected in breast milk. T1/2 — about 3 — 6 hours, when liver failure is increasing. No correlation of the kinetics of the functional state of the thyroid gland. The metabolism of the drug Tiamazol is carried out in the kidneys and liver, excretion of the drug is by the kidneys and bile. The news is 70% of Tiamazol in a period of 24 hours, and 7-12% in an unmodified form.
Description pharmacological action:
Impairs the synthesis of thyroid hormones by blocking the enzyme peroxidase that is involved in thyronine iodine in the thyroid gland with the formation of triad and tetrajodtironina. This property allows symptomatic therapy of hyperthyroidism, except for the development of thyrotoxicosis due to the release of hormones after destruction of thyroid cells (after treatment with radioactive iodine or when thyroiditis). Tiamazol does not affect the process of releasing tironina synthesized from the follicles of the thyroid gland. This explains the latent period of varying duration, which may be preceded by the normalization of the level of T3 and T4 in blood plasma, i.e. the improvement of the clinical picture.
Reduces basal metabolism, accelerates the excretion from the thyroid gland of iodide enhances reciprocal activation of synthesis and excretion of pituitary thyroid-stimulating hormone, which may be accompanied by some enlargement of the thyroid gland.
The duration of the action once the dose is nearly 24 h.
- preparation for surgical treatment of thyrotoxicosis
- the preparation for the treatment of hyperthyroidism with radioactive iodine
- therapy in the latent period of action of radioactive iodine (held prior to the commencement of radioactive iodine — for 4-6 months)
- in exceptional cases, long-term maintenance therapy of hyperthyroidism, when the overall condition or for individual reasons, it is impossible to perform radical treatment
- prevention of thyrotoxicosis in the appointment drugs iodine (including the use of iodinated Radiocontrast dye) in the presence of latent thyrotoxicosis, Autonomous adenomas or thyrotoxicosis in history.
- hypersensitivity to thiamazole and a derivative of thiourea
- agranulocytosis during previous therapy carbimazole or thiamazole
- granulocytopenia (including in history)
- cholestasis before treatment
- therapy temazepam in combination with levothyroxine during pregnancy.
A relative contraindication is the previously observed allergic skin reactions to a derivative of thiourea.
- patients with goiter is very large with narrowing of the trachea (only short-term treatment in preparation for surgery)
- liver failure.
Application of pregnancy and breast-feeding:
Untreated hyperthyroidism during pregnancy can lead to serious complications such as premature birth, fetal malformations. Telazol crosses the placental barrier and the fetal blood may reach the same concentration as the mother. Due to the fact that the impact of Tiamazol on the fetus cannot be completely avoided in pregnancy, the drug should be administered after a full assessment of the benefits and risks of its use in minimum effective dose without additional intake of levothyroxine.
Thiamazole doses, greatly exceeding recommended, can cause the formation of goiter and hypothyroidism in the fetus and low birth weight.
Lactation treatment of hyperthyroidism drug Tiamazol, if necessary, can be continued. As teamadol passes into breast milk and may achieve concentrations corresponding to its level in the blood of the mother, the newborn may develop hypothyroidism. So if you need to continue treatment of hyperthyroidism during breast feeding Tiamazol should be taken in low doses (10 mg/day) without supplementation of levothyroxine.
Sometimes — allergic skin reactions (itching, redness, rash), vomiting, dizziness, weakness.
Fever, change in taste are rare and are reversible.
Approximately 0.3–0.6% of cases can occur agranulocytosis. Its symptoms (see “Special instructions”) can appear even after weeks and months after the start of treatment and necessitate discontinuation of the drug.
In a few cases there were reports about arthralgia, developing, as a rule, slowly and gradually, a few months after the start of treatment. Clinical signs of arthritis were absent.
Described isolated cases of cholestatic jaundice and toxic hepatitis.
In some cases, have been described: generalized lymphadenopathy, acute increase of salivary glands, thrombocytopenia, pancytopenia, neuritis, neuropathy, volchanochnopodobny reaction, and an autoimmune syndrome with hypoglycemia.
The increase in body weight.
Subclinical and clinical hypothyroidism can develop when high doses of the drug. You can also start the thyroid gland, which is associated with increasing TSH in the blood.
In appointing the drug after the use of iodinated Radiocontrast dye in high dose may reduce the action of Tiamazol.
Lack of iodine increases the effects of Tiamazol.
In patients receiving Tiamazol about of hyperthyroidism after reaching the euthyroid state, i.e., normalization of content of thyroid hormones in the blood serum, it may be necessary to reduce the received dose of cardiac glycosides (digoxin and digitoxin), aminophylline, as well as increasing the received dose of warfarin and other anticoagulants — coumarin derivatives and indandiona (pharmacodynamic interaction).
The drugs lithium, beta-adrenoblokatora, reserpine, amiodarone increases the effect of thiamazole (requires correction of the dose).
While the use of sulfonamides, metamizol sodium and mielotoksicskie drugs increases the risk of leukopenia.
Stronger and folic acid while the use of Tiamazol reduce the risk of leukopenia.
Gentamicin enhances the antithyroid action of Tiamazol.
Data on the impact of other drugs on the pharmacokinetics and pharmacodynamics of a drug. However, it should be borne in mind that thyrotoxicosis accelerates the metabolism and elimination of substances. Therefore, in some cases it is necessary to adjust the dose of other drugs.
Method of application and dose:
Inside, after eating, without chewing, with enough fluid. The daily dose is administered in one time or divided into 2-3 single doses. At the beginning of treatment single doses applied throughout the day at certain times.
The maintenance dose should be taken at once after Breakfast.
Hyperthyroidism: depending on the severity of the disease 20-40 mg/day of Tiamazol in 3-6 weeks. After normalization of thyroid function (usually 3-8 weeks) move on to receive a maintenance dose of 5-20 mg/day. Since that time, it is recommended additional intake of levothyroxine.
When preparing for the surgical treatment of hyperthyroidism: appoint 20-40 mg/day to achieve euthyroid status. Since that time, it is recommended additional intake of levothyroxine.
With the aim of reducing the time required to prepare for operation, additionally prescribe beta-blockers and iodine.
In preparation for radioactive iodine treatment: 20-40 mg/day to achieve euthyroid status. It should be remembered that tiamazol and derivatives of thiourea may reduce the sensitivity of thyroid tissue to radiation therapy.
Therapy in the latent period of action of radioactive iodine: depending on the severity of the disease on 5-20 mg before the onset of action of radioactive iodine (4-6 months).
Long thyreostatics supportive therapy: 1,25–2,5–10 mg/day with additional use of low-dose levothyroxine.
Prevention of thyrotoxicosis in the appointment drugs iodine (including the use of iodinated Radiocontrast dye) if you have latent thyrotoxicosis, Autonomous adenomas or thyrotoxicosis in history: 10-20 mg/day of Tiamazol and 1 g potassium perchlorate a day for 8-10 days before taking iodine-containing drugs.
Children: initial dose of 0.3–0.5 mg/kg daily maintenance dose 0.2–0.3 mg/kg, optionally prescribe levothyroxine.
Pregnant administered in the lowest possible doses: single dose of 2.5 mg daily, 10 mg.
When liver failure prescribe the minimum effective dose.
In the treatment of hyperthyroidism duration of therapy ranges from 1.5 to 2 years.
In preparation for operation in patients with hyperthyroidism, the treatment is carried out until reaching a euthyroid state is longer) and ends the day before her. In all cases, the duration of therapy determined by the physician.
Symptoms: chronic overdosing leads to enlargement of the thyroid gland and the development of hypothyroidism.
Reception of very high doses of thiamazole (about 120 mg per day) may lead to the development of myelotoxic effects.
Treatment: stop taking the drug. Replacement therapy with levothyroxine is carried out in case if this is justified by the severity of hypothyroidism. Usually after the drug is observed spontaneous recovery of thyroid function.
When taking very high doses of the drug elimination of the drug, gastric lavage, the appointment activated carbon, symptomatic therapy.
Patients with significant thyroid enlargement and narrowing of the lumen of the trachea, Tiamazol prescribed short-term in combination with levothyroxine, as prolonged use may increase the goiter and even greater compression of the trachea. Careful monitoring of the patient (monitoring of the TSH level, the lumen of the trachea).
During treatment should regularly monitor picture peripheral blood.
If, during the treatment sudden pain in the throat, difficulty swallowing, increased body temperature, signs of sores or abrasions (possible symptoms of agranulocytosis), you should immediately stop taking the drug and consult a doctor.
The appearance during treatment, n/a hemorrhage or bleeding of unknown origin, generalized skin rash and itching, persistent nausea or vomiting, jaundice, severe epigastric pain and severe weakness should stop the drug.
In the case of early termination of treatment possible relapse.
The emergence or worsening of endocrine ophthalmopathy is not a side effect of treatment with Tiamazol conducted properly.
In rare cases after treatment can occur late hypothyroidism, which is not a side effect of the drug and is associated with inflammatory and destructive processes in the thyroid tissue occurring in the framework of the underlying disease.