Tirozol - instructions for use, dose, side effects, contraindications

carboxymethyl starch sodium - 2 mg, mAgnia stearate-2 mg, hypromellose 2910 / 15-3 mg, talc-6 mg, powder cellulose - 10 mg, starch corn-20 mg, lactose monohydrate-200 mg

Film coating: 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

in a dosage of 10 mg:

Core:

Active ingredient: thiamazole 10 mg

Excipients: silicon colloid dioxide - 2 mg,

sodium carboxymethyl starch-2 mg, Magnesium stearate-2 mg, hypromellose 2910 / 15-3 mg, talc-6 mg, powder cellulose - 10 mg, starch corn-20 mg, lactose monohydrate 195 mg

Film coating: iron dye oxide yellow - 0.54 mg, dye iron oxide red - 0.004 mg, dimethicone 100 0.16 mg, macrogol 400- 0.79 mg, titanium dioxide-0.89 mg, hypromellose 2910 / 15- 3.21 mg.

Description:

Dosage 5 mg: light yellow round, biconcave tablets, coated with a film sheath, with risks on both sides. On cross-section of the nucleus of white or almost white.

Dosage 10 mg: gray-orange round, biconcave tablets, covered with a film sheath, with risks on both sides. On the cross section, the nucleus is white or almost white in color.

Pharmacotherapeutic group:antithyroid agent

ATX: & nbsp

H.03.B.B Imidazole derivatives containing sulfur

H.03.B.B.02 Thiamazole

Pharmacodynamics:

The antithyroid drug disrupts the synthesis of thyroid hormones by blocking the enzyme peroxidase involved in iodination of thyronin in the thyroid gland with the formation of triiod - and tetraiodothyronine. This property allows to carry out symptomatic therapy of thyrotoxicosis, except for cases of thyrotoxicosis development due to release of hormones after destruction of thyroid cells (after treatment with radioactive iodine or with thyroiditis). Tirozol® does not affect the release of synthesized tyronins from follicles of the thyroid gland. This explains the latent period of different duration, which may precede the normalization of the level of T3 and T4 in blood plasma, i.e. improvement of clinical picture.

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

The duration of the single dose is almost 24 hours.

Pharmacokinetics:

Tirozol® is rapidly and almost completely absorbed when ingested. The maximum concentration in plasma is reached within 0.4 - 1.2 hours. With blood plasma proteins are practically not associated. Tyrosol® cumulates in the thyroid gland, where it is slowly metabolized. Small amounts of thiamazole are found in breast milk. The half-life is about 3-6 hours, with hepatic insufficiency it increases. The dependence of kinetics on the functional state of the thyroid gland was not revealed. Metabolism of the preparation Tyrosol® is carried out in the kidneys and liver, the drug is excreted by the kidneys and with bile. In the course of 24 hours, 70% of the preparation Tyrozole® is excreted by the kidneys, 7 - 12% unchanged.

Indications:

thyrotoxicosis;

preparation for surgical treatment of thyrotoxicosis;

preparation for treatment of thyrotoxicosis with radioactive iodine;

therapy in the latent period of action of radioactive iodine. It is carried out before the start of the action of radioactive iodine (within 4-6 months);

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

prophylaxis of thyrotoxicosis when prescribing iodine preparations (including cases of using iodine-containing radiocontrast agents) in the presence of latent thyrotoxicosis, autonomic adenomas or thyrotoxicosis in anamnesis.

Contraindications:

It is not recommended for use in children from 0 to 3 years.

hypersensitivity to thiamazole, to derivatives thiourea or any other component of the preparation;

agranulocytosis during previous therapy with carbimazole or thiamazole;

granulocytopenia (including in the anamnesis);

cholestasis before treatment;

Therapy with thiamazole in combination with levothyroxine sodium during pregnancy.

Tirozol® contains lactose, therefore its use is not recommended for patients with rare hereditary diseases associated with intolerance to galactose, a deficiency of lactase or a syndrome of glucose-galactose malabsorption.

Carefully:

Carefully should be applied in patients with goiter very large dimensions with narrowing of the trachea (only short-term treatment in the period of preparation for surgery), with hepatic insufficiency.

Pregnancy and lactation:

Absence of hyperfunction treatment of the thyroid gland during pregnancy can lead to Serious complications, such as premature birth development of the fetus. Hypothyroidism, caused by treatment inadequate doses of thiamazole may result in miscarriage.

Thiamazole penetrates through placental barrier in fetal blood can achieve the same concentration, as in the mother. Due with this, during pregnancy the drug should be appointed after full assessment of the benefits and risks of its use in a minimally effective dose (up to 10 mg / day) without additional admission levothyroxine sodium.

Doses of thiamazole, significantly exceeding recommended, can cause the formation of goiter and hypothyroidism in the fetus, and decreased birth weight.

During lactation treatment thyrotoxicosis with Tirozol® If necessary, it can be continued. As thiamazole penetrates into breast milk and can to achieve concentration in it, corresponding to its level in the blood the mother, the newborn is development of hypothyroidism.

Needed regularly control thyroid function glands in newborns.

Dosing and Administration:

Tablets should be taken orally after eating, without chewing, with with a sufficient amount of liquid.

The daily dose is prescribed in one reception or divided into two or three single doses. At the beginning of treatment single doses are taken within day at a specific time.

The maintenance dose should be take in one go after breakfast.

Thyrotoxicosis:

Depending on the severity of the disease prescribe 20-40 mg / day of the drug Tirozole® for 3-6 weeks. After normalization of thyroid function glands (usually in 3-8 weeks) go on receiving supportive doses of 5-20 mg / day. Since that time an additional welcome is recommended levothyroxine sodium.

When preparing for surgery treatment of thyrotoxicosis appoint 20 - 40 mg / day of Tirozol® preparation up to achievement of the euthyroid state.

From this time it is recommended additional reception of levothyroxine sodium.

In order to reduce the time, necessary to prepare for operations, additionally appointed beta-blockers and drugs iodine.

When preparing for treatment radioactive iodine: 20-40 mg / day of Tirozol® preparation before achievement of the euthyroid state.

Therapy in the latent period of action radioactive iodine: depending on the severity of the disease is prescribed 5- 20 mg / day of Tirozol® preparation the onset of radioactive iodine (4-6 months).

Prolonged thyreostatic maintenance therapy: 1,25 - 2,5 - 10 mg / day of the drug Tirozol® with an additional method small doses of levothyroxine sodium.

In the treatment of thyrotoxicosis The duration of therapy is from 1,5 to 2 years.

Prophylaxis of thyrotoxicosis when administration of iodine preparations (including cases of iodine-containing radiocontrast agents) with the presence of latent thyrotoxicosis, autonomous adenomas or thyrotoxicosis in history: appoint 10-20 mg / day of Tirozol® and 1 g perchlorate potassium per day for 8-10 days before admission iodine containing agents.

Dosage in children

Not recommended for use in children from 0 to 3 years. Children from 3 to 17 years, the preparation Tyrozol® is prescribed in initial dose of 0.3-0.5 mg / kg body weight body, which is divided into two or three equal dose daily. Maximum recommended dose for children with body weight of more than 80 kg-40 mg / day.

Maintenance dose: 0.2-0.3 mg / kg body weight per day. If necessary additionally appointed levothyroxine sodium.

Dosage in pregnant women

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

With hepatic insufficiency designate a minimally effective dose of the drug under careful medical supervision.

When preparing for surgery patients with thyrotoxicosis treatment preparation is carried out up to achievement of euthyroid status within 3-4 weeks to planned operation day (in in some cases, longer) and ends the day before it.

Side effects:Frequency of adverse effects of the drug is assessed 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. Him symptoms (See"Special instructions") may appear even after weeks and months after the start of treatment and lead to the need for withdrawal of the drug;

Rarely: generalized lymphadenopathy, thrombocytopenia, pancytopenia.

Endocrine system:

Rarely: insulin autoimmune syndrome with hypoglycemia.

Nervous system:

Rarely: reversible change taste sensations, dizziness;

Rarely: neuritis, polyneuropathy.

Gastrointestinal disorders:

Rarely: increased salivary glands, vomiting.

Disorders from the liver and bile ducts:

Rarely: Cholestatic jaundice and toxic hepatitis.

Disturbances from the skin and

subcutaneous tissues:

Often: allergic skin reactions (itching, redness, rashes);

Rarely: generalized rashes on the skin, alopecia, lupus-like syndrome. Musculoskeletal and connective tissue disorders:

Often: slow-progressing arthralgia without clinical signs of arthritis.

Complications of a general nature and reaction at the site of administration:

Rarely: temperature increase,

Overdose:

With prolonged use of high doses a possible development

subclinical and clinical hypothyroidism, as well as an increase in

thyroid size due to an increase in the level of TSH.

This can be avoided by reduce the dose to achieve a state of euthyroidism or, if necessary, additional prescribing drugs after the abolition of Tirozol® spontaneous restoration of thyroid function glands.

Taking very high doses of thiamazole (about 120 mg per day) can lead to to the development of myelotoxic effects. Such doses of the drug should only be applied to special indications (heavy forms of the disease, thyrotoxic crisis). Treatment: withdrawal of the drug, gastric lavage, symptomatic therapy, with necessary, switching to antithyroid drug another group.

Interaction:

In the appointment of thiamazole after use of iodine-containing radiopaque agents in a high dose, the effect of thiamazole may be decreased.

The lack of iodine enhances the action of thiamazole.

In patients receiving thiamazole for the treatment of thyrotoxicosis, after reaching the euthyroid state, i.e.normalization of the thyroid hormone levels in the blood serum, it may be necessary to reduce the intake of cardiac glycosides (digoxin and digitoxin), aminophylline, and increase in the dose of warfarin and other anticoagulants, coumarin and indanedione derivatives (pharmaco dynamic interaction).

Lithium preparations, beta-blockers, reserpine, amiodarone increase the effect of thiamazole (dose adjustment is required). When used simultaneously with sulfonamides, metamizol sodium and myelotoxic drugs, the risk of developing of leukopenia. Leukogen and folic acid acid at the same time use with thiamazole reduce risk of developing leukopenia.

Gentamicin strengthens antithyroid effect of thiamazole.

Data on the influence of others medicines for pharmacokinetics and pharmacodynamics There is no preparation. However, mind that with thyrotoxicosis accelerates metabolism and elimination substances. Therefore, in a number of cases it is necessary to adjust the dose other drugs.

Special instructions:

Patients with significant an increase in the thyroid gland, narrowing the lumen of the trachea, Tirozol® is administered for a short time in combination with levothyroxine sodium, because with prolonged application may increase goiter and even more compression of the trachea.

A thorough patient monitoring (control level of TTG, tracheal lumen).

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

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

If during treatment with the drug suddenly there are sore throats, difficulty swallowing, enhancing body temperature, signs of stomatitis or furunculosis (possible symptoms agranulocytosis) should be discontinued taking the drug and immediately consult a doctor.

When appearing during treatment subcutaneous hemorrhage or

bleeding of unknown origin, generalized skin rash and itching, persistent nausea or vomiting, jaundice, severe epigastric pain and severe weakness is required cancellation of the drug.

In case of early termination can relapse disease.

Appearance or deterioration of the flow endocrine ophthalmopathy is not is a side effect of treatment with Tirozol® properly.

In rare cases after graduation treatment may occur late hypothyroidism, which is not side effect of the drug, and associated with inflammatory and destructive processes in the tissue thyroid gland flowing into the the main disease.

Effect on the ability to drive transp. cf. and fur:Tand amazole does not affect the ability to drive vehicles and mechanisms.

Form release / dosage:

Tablets covered with a film membrane, 5 mg and 10 mg. For 10 or 25 tablets in a PVC / AL blister; 2, 4, 5 or 10 blisters together with the instructions for use are placed in a cardboard box.

Packaging:

Tablets covered with a film membrane, 5 mg and 10 mg. For 10 or 25 tablets in a PVC / AL blister; 2, 4, 5 or 10 blisters together with the instructions for use are placed in a cardboard box.

Storage conditions:

In a dry place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

4 years.

The drug can not be used after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:П N014893 / 01

Date of registration:31.07.2008

The owner of the registration certificate:Merck KGaAMerck KGaA Germany

Manufacturer: & nbsp

MERCK, KGaA Germany

Representation: & nbspMERK, LLCMERK, LLCRussia

Information update date: & nbsp26.08.2015

Illustrated instructions

Instructions

Tirozol® (Thyrozol® )