Producer: Nycomed Austria GmbH (Nikomed Austria Gmbh) Austria
Code of automatic telephone exchange: H03BB02
Release form: Firm dosage forms. Tablets.
General characteristics. Structure:
Each tablet contains:
in a dosage of 5 mg:
Active component: Thiamazolum - 5 mg
Excipients: silicon dioxide colloid - 2 mg, sodium carboxymethylstarch - 2 mg, magnesium stearate - 2 mg, a gipromelloza 2910/15 - 3 mg, talc - 6 mg, cellulose powder - 10 mg, starch corn - 20 mg, lactoses monogidrat-200 mg
Film cover: ferrous oxide yellow - 0,04 mg, диметикон 100 - 0,16 mg, a macrogoal of 400 - 0,79 mg, titanium dioxide - 1,43 mg, a gipromelloza 2910/15 - 3,21 mg
in a dosage of 10 mg:
Active component: Thiamazolum of 10 mg
Excipients: silicon dioxide colloid - 2 mg, sodium carboxymethylstarch - 2 mg, magnesium stearate - 2 mg, a gipromelloza 2910/15 - 3 mg, talc - 6 mg, cellulose powder - 10 mg, starch corn - 20 mg, lactoses monogidrat-195 mg
Film cover: ferrous oxide yellow - 0,54 mg, ferrous oxide red - 0,004 mg, диметикон 100 - 0,16 mg, a macrogoal of 400-0,79 mg, titanium dioxide - 0,89 mg, a gipromelloza of 2910/15-3,21 mg
Dosage of 5 mg: light-yellow round, biconvex tablets, film coated, with risks on both sides. A look on a break: white or almost white weight.
Dosage of 10 mg: it is gray - orange round, biconvex tablets, film coated, with risks on both sides. A look on a break: white or almost white weight.
Pharmacodynamics. Anti-thyroid drug, breaks synthesis of hormones of a thyroid gland, blocking enzyme the peroxidase participating in iodination of a tironin in a thyroid gland with education трийод - and a tetrayodtironina. This property allows to carry out symptomatic therapy of a thyrotoxicosis, except for cases of development of a thyrotoxicosis owing to release of hormones after destruction of cells of a thyroid gland (after treatment by a radioiodine or at a tireoiodita). Тирозол® does not influence process of release of the synthesized tironin of follicles of a thyroid gland. Stage of latency of various duration which can precede normalization of the T3 and T4 level in a blood plasma, i.e. to improvement of a clinical picture is explained by it.
Reduces standard metabolism, accelerates removal from a thyroid gland of iodides, increases reciprocal activation of synthesis and allocation by a hypophysis of thyritropic hormone that can be followed by some hyperplasia of a thyroid gland.
Duration of action of once accepted dose makes nearly 24 hours.
Pharmacokinetics. Тирозол® at intake quickly and almost it is completely soaked up. The maximum concentration in plasma is reached within 0,4 - 1,2 hours. Practically does not contact proteins of a blood plasma. Тирозол® kumulirut in a thyroid gland where it is slowly metabolized. Small amounts of Thiamazolum are found in breast milk. The elimination half-life makes about 3 - 6 hours, at a liver failure it increases. Dependence of kinetics on a functional condition of a thyroid gland is not revealed. Metabolism of the drug Tirozol® is carried out in kidneys and a liver, removal of drug is carried out by kidneys and with bile. Kidneys within 24 hours remove 70% of the drug Tirozol®, and 7 - 12% in not changed look.
Indications to use:
• preparation for surgical treatment of a thyrotoxicosis;
• preparation for treatment of a thyrotoxicosis radioiodine;
• therapy at stage of latency of action of a radioiodine. It is carried out prior to action of a radioiodine (within 4-6 months);
• in exceptional cases - a long maintenance therapy of a thyrotoxicosis when in connection with the general state or for the individual reasons it is impossible to execute radical treatment;
• prevention of a thyrotoxicosis at purpose of drugs of iodine (including cases of use of iodinated X-ray contrast means) in the presence of a latent thyrotoxicosis, autonomous adenomas or a thyrotoxicosis in the anamnesis.
Route of administration and doses:
Pill should be taken inside after food, without chewing, with enough liquid. The daily dose is appointed in one step or divided into two-three single doses. In an initiation of treatment single doses are accepted during the day in strictly certain time.
The maintenance dose should be accepted in one step after a breakfast.
Depending on disease severity appoint 20-40 mg/days of the drug Tirozol® within 3-6 weeks. After normalization of function of a thyroid gland (usually in 3-8 weeks) pass 5-20 mg/days to reception of a maintenance dose. From now on additional reception of left thyroxine is recommended.
By preparation for surgical treatment of a thyrotoxicosis appoint 20-40 mg/days of the drug Tirozol® before achievement of an euthyroid state. From now on additional reception of left thyroxine is recommended.
For the purpose of reduction of time necessary for a preparation for surgery, in addition appoint beta adrenoblockers and drugs of iodine.
By preparation for treatment by a radioiodine: appoint 20-40 mg/days of the drug Tirozol® before achievement of an euthyroid state.
Therapy at stage of latency of action of a radioiodine: depending on disease severity appoint 5-20 mg/days of the drug Tirozol® before action of a radioiodine (4 - 6 months).
Long thyreostatic maintenance therapy:
1,25 - 2,5 - 10 mg/days of the drug Tirozol® with additional reception of small doses of left thyroxine. At treatment of a thyrotoxicosis duration of therapy makes from 1,5 to 2 years.
Prevention of a thyrotoxicosis at purpose of drugs of iodine (including cases of use of iodinated X-ray contrast means) in the presence of a latent thyrotoxicosis, autonomous adenomas or a thyrotoxicosis in the anamnesis: appoint 10-20 mg/days of the drug Tirozol® and 1 g of potassium perchlorate a day within 8 10 days before reception of iodinated means.
Dosage at children
It is not recommended for use for children from 0 to 2 years. To children from 3 to 17 years the drug Tirozol® appoint 0,3 - 0,5 mg/kg of body weight which is divided into two-three equal doses daily in an initial dose. Most recommended dose for children with body weight more than 80 kg - 40 mg/day.
Maintenance dose: 0,2 - 0,3 mg/kg of body weight a day. If necessary in addition appoint left thyroxine.
Dosage at pregnant women
To pregnant women appoint in the lowest doses: one-time - 2,5 mg, daily - 10 mg.
At a liver failure appoint minimum effective dose of drug under careful medical control.
At a preparation for surgery of patients with a thyrotoxicosis treatment by drug is carried out before achievement of an euthyroid state within 3-4 weeks about the planned day of operation (in some cases - is longer) and comes to an end a day before it.
Features of use:
To patients with significant increase in the thyroid gland narrowing a gleam of a trachea, Tirozol® appoint quickly in a combination with sodium left thyroxine as at prolonged use increase in a craw and a bigger prelum of a trachea is possible. It is necessary to make careful observation of the patient (control of the TTG level, a tracheal gleam).
During treatment by drug regular control of a picture of peripheral blood is necessary.
Thiamazolum and derivative thioureas can reduce sensitivity of tissue of thyroid gland to radiation therapy.
If during treatment by drug suddenly there are pharyngalgias, the complicated swallowing, fervescence, symptoms of stomatitis or a furunculosis (possible symptoms of an agranulocytosis) it is necessary to stop administration of drug and to see immediately a doctor.
At emergence during treatment of hypodermic hemorrhages or bleedings of not clear genesis, generalized skin rash and an itch, persistent nausea or vomiting, jaundice, severe epigastric pains and the expressed weakness drug withdrawal is required.
In case of the early termination of treatment the disease recurrence is possible.
Emergence or deterioration in a course of an endocrine ophthalmopathy is not side effect of the treatment by the drug Tirozol® which is carried out properly.
In rare instances after the end of treatment there can be a late hypothyroidism which is not side effect of drug, and is connected with the inflammatory and destructive processes in tissue of a thyroid gland proceeding within a basic disease.
Influence on ability to manage vehicles and mechanisms
Thiamazolum does not exert impact on ability to manage vehicles and mechanisms.
Frequency of side effects of drug is regarded as follows:
Very frequent: ≥1/10
Frequent: ≥1/100, <1/10
Infrequent: ≥1/1000, <1/100
Rare: ≥1/10 000, <1/1000
Very rare: <1/10 000
Circulatory and lymphatic systems Infrequently: agranulocytosis. Its symptoms (See. "Special instructions") can appear even weeks and months later after an initiation of treatment and to result in need of drug withdrawal; Very seldom: generalized lymphadenopathy, thrombocytopenia, pancytopenia.
Very seldom: an insulin autoimmune syndrome with a hypoglycemia.
Seldom: reversible change of flavoring feelings, dizziness;
Very seldom: neuritis, polyneuropathy.
Very seldom: increase in sialadens, vomiting.
Disturbances from a liver and biliary tract:
Very seldom: cholestatic jaundice and toxic hepatitis.
Disturbances from skin and hypodermic fabrics:
Very often: allergic skin reactions (itch, reddening, rashes);
Very seldom: generalized enanthesis, allopecia, volchanochnopodobny syndrome.
Disturbances from musculoskeletal and connecting fabric:
Often: a medlennoprogressiruyushchy arthralgia without clinical signs of arthritis.
Complications of the general character and reaction in an injection site:
Seldom: temperature increase, weakness, increase in body weight.
Interaction with other medicines:
At purpose of drug after use of iodinated X-ray contrast means in a high dose weakening of effect of the drug Tirozol® is possible.
The lack of iodine strengthens effect of the drug Tirozol®.
The patients accepting Tirozol® for treatment of a thyrotoxicosis after achievement of an euthyroid state, i.e. normalization of content of hormones of a thyroid gland in blood serum, can have a need of reduction of the accepted doses of cardiac glycosides (digoxin and digitoxin), Aminophyllinum, and also increase in the accepted doses of warfarin and other anticoagulants - derivative coumarin and an indandion (pharmakodinamichesky interaction).
Lithium drugs, beta adrenoblockers, Reserpinum, Amiodaronum increase effect of Thiamazolum (dose adjustment is required).
At simultaneous use with streptocides, metamizole sodium and myelotoxic medicines the risk of development of a leukopenia increases. Leucogenum and folic acid at simultaneous use with Thiamazolum reduce risk of development of a leukopenia. Gentamycin strengthens anti-thyroid action of Thiamazolum. There are no data on influence of other medicines on pharmacokinetics and a pharmacodynamics of drug. However it must be kept in mind that at a thyrotoxicosis metabolism and elimination of substances accelerates. Therefore in some cases it is necessary to adjust a dose of other drugs.
• hypersensitivity to Thiamazolum, to derivatives of thiourea or any other component of drug;
• an agranulocytosis during earlier carried out therapy by carbimazole or Thiamazolum;
• a granulocytopenia (including in the anamnesis);
• a cholestasia before an initiation of treatment;
• therapy by Thiamazolum in a combination with sodium left thyroxine during pregnancy.
Тирозол® contains lactose therefore its use is not recommended to patients with the rare hereditary diseases connected with intolerance of a galactose, deficit of lactase or a syndrome glucose - galaktozny malabsorption.
With care it is necessary to apply at patients with a craw of very big sizes with a tracheostenosis (only short-term treatment in the period of a preparation for surgery), at a liver failure.
Use during pregnancy and during breastfeeding
Lack of treatment of hyperfunction of a thyroid gland during pregnancy can lead to serious complications, such as premature births, fruit malformations. Nevertheless, the hypothyroidism caused by treatment by inadequate doses can lead to pregnancy not incubation.
Thiamazolum gets through a placental barrier and in blood of a fruit can reach the same concentration, as at mother. In this regard, at pregnancy drug has to be appointed after an omnibus estimate of advantage and risk of its use in minimum effective dose (to 10 mg/days) without additional reception of left thyroxine.
Thiamazolum doses considerably exceeding recommended can cause formation of a craw and a hypothyroidism in a fruit, and also the lowered weight at the birth.
In the period of a lactation treatment of a thyrotoxicosis the drug Tirozol® if necessary can be continued. As Thiamazolum gets into breast milk and can reach in it the concentration corresponding to level it in blood at mother at the newborn development of a hypothyroidism is possible.
It is regularly necessary to control function of a thyroid gland at newborns.
At long reception of high doses of drug development of a subclinical and clinical hypothyroidism, and also increase in the sizes of a thyroid gland owing to increase in the TTG level is possible
It can be avoided by a drug dose decline before achievement of a condition of an euthyroidism or if it is necessary, additional purpose of drugs of left thyroxine. As a rule, after drug withdrawal of Tirozol® spontaneous recovery of function of a thyroid gland is observed. Reception of very high doses of Thiamazolum (about 120 mg a day) can lead to development of myelotoxic effects. Such doses of drug have to be applied only according to special indications (severe forms of a disease, thyrocardiac crisis). Treatment: drug withdrawal, gastric lavage, symptomatic therapy, if necessary, switching to anti-thyroid drug of other group.
In the dry place at a temperature not above 25 °C. To store in the place, unavailable to children. Period of validity 4 years. Drug cannot be used after a period of validity.
According to the recipe
Tablets are film coated, on 5 mg and 10 mg. On 10 or 25 tablets in the blister from PVH/AL; on 2, 4, 5 or 10 blisters together with the application instruction place in a cardboard pack.