Mercazolil instructions for use analogues. Mercazolil-health analogues, synonyms and group drugs. Cross-drug interactions


Mercazolil is an antithyroid substance. The active component provokes blocking of peroxidase. As a result, iodination of thyroid hormones and the synthesis of thyroxine and triiodothyronine are disrupted. In case of pathological hypersecretion of these hormones when using the drug, normalization of metabolic processes in the tissues of the thyroid gland is observed. The substance can reduce basal metabolism.

Indications for use

A drug Mercazolil prescribed for:
- diffuse toxic goiter;
- preparation for radioiodine therapy;
- Graves' disease;
- Plummer's disease;
- preparation for surgical interventions regarding thyrotoxicosis;
- prevention of thyrotoxicosis during treatment with iodine-containing agents.

Mode of application

Pills Mercazolil taken orally. The dosage form is not chewed, taken after meals, washed down with water. The standard dosage for mild to moderate diseases is 5 mg three times a day. In severe forms, the dosage is doubled: 10 mg three times a day. After remission, doses are reduced. The reduction is carried out every 5 days by 5-10 mg. It is possible to use 5 mg once a day, then once every two days, then once every three days.
The drug should be taken until a lasting therapeutic effect is obtained. The course is selected individually. The maximum single dosage is 10 mg, daily dosage is 40 mg. Children's dosages: initial - 0.4 mg/kg body weight (taken once or divided into two doses), maintenance daily dosage - 0.2 mg/kg body weight.

Side effects

Taking the drug Mercazolil may be accompanied by:
- agranulocytosis; dizziness; leukopenia; alopecia; paresthesias; headaches; lupus-like syndrome; thrombocytopenia; itchy skin; swelling; goitrogenic effect; arthralgia; nephrotic syndrome; cholestatic hepatitis; rise in temperature; liver damage; skin rash; visual impairment; nausea; drug-induced hypothyroidism; aplastic anemia.
If undesirable effects occur, a decision is made to discontinue the drug or adjust its dosage.

Contraindications

:
A drug Mercazolil not prescribed for:
- lactation;
- granulocytopenia;
- pregnancy;
- severe leukopenia;
- nodular forms of goiter (except for severe cases).

Pregnancy

:
During pregnancy, thiamazole-containing drugs are not prescribed.

Interaction with other drugs

Drug, group of drugs Possible result of interaction with thiamazole
Iodine-containing products Weakening the effects of the drug Mercazolil
Amiodarone Potentiation of the effects of thiamazole
Beta-blockers Potentiation of the action of the drug Mercazolil
Lithium preparations Enhancing the effects of thiamazole
Sulfa drugs Possible development of leukopenia
Reserpine Potentiation of the effects of thiamazole

Overdose

:
If doses are exceeded Mercazolil, designated as therapeutic, dry skin, myasthenic manifestations, pathological changes in the menstrual cycle, and drowsiness occur. No specific antidote to thiamazole has been found. Therapy is prescribed by a doctor in accordance with symptomatic manifestations.

Storage conditions

Tablet storage temperature Mercazolil- up to 25 degrees Celsius. The shelf life of the drug is 5 years. Storage conditions should take into account the need to maintain constant low humidity and avoid exposure of the dosage form to direct sunlight.

Release form

A drug Mercazolil Available in tablets. The packaging is as follows:
- 50 tablets/jar/packaging;
- 100 tablets/jar/packaging;
- 40 tablets/blister packaging/packaging.

Compound

:
1 tablet Mercazolil contains thiamazole 5 mg. Auxiliary components: sucrose, calcium stearate, starch, talc.

Synonyms

:
Metizol, Thiamazol Henning, Mercazolil-Health, Thiamazol, Tyrozol.

Additionally

:
If treatment is completed prematurely, relapses of the disease often occur.
There are therapeutic data on the advisable combination of lithium carbonate with the drug Mercazolil.
Weekly monitoring of peripheral blood parameters is important during therapy with Mercazolil.
The drug may increase bleeding of thyroid tissue.

Main settings

Name: MERCAZOLIL
ATX code: H03BB02 -

INN:

thiamazole

Pharmacotherapeutic group:

antithyroid drug.

Indications for use

  • thyrotoxicosis;
  • preparation for surgical treatment of thyrotoxicosis;
  • preparation for treatment of thyrotoxicosis with radioactive iodine;
  • therapy during the latent period of radioactive iodine action. It is carried out before the onset of radioactive iodine action (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;
  • prevention of thyrotoxicosis when prescribing iodine preparations (including cases of use of iodine-containing radiocontrast agents) in the presence of latent thyrotoxicosis, autonomous adenomas or a history of thyrotoxicosis.

Contraindications

  • hypersensitivity to thiamazole or thiourea derivatives;
  • agranulocytosis during previous therapy with carbimazole or thiamazole;
  • granulocytopenia (including history);
  • cholestasis before starting treatment;
  • lactation period.

Carefully should be used in pregnant women; in patients with very large goiters with narrowing of the trachea (only short-term treatment in preparation for surgery); with liver failure; in patients receiving anticoagulants, cardiac glycosides, and aminophylline.

Use during pregnancy and breastfeeding

During pregnancy, the drug should be used only in case of emergency in the minimum effective dose without additional intake of thyroid hormones under the strict supervision of a physician. If it is necessary to continue treatment of thyrotoxicosis during breastfeeding, breastfeeding should be discontinued.

Directions for use and doses

The tablets should be taken orally after meals, without chewing, with a sufficient amount of liquid. The daily dose is prescribed in one dose or divided into two or three single doses. At the beginning of treatment, single doses are taken throughout the day at strictly defined times.
The maintenance dose should be taken in one dose after breakfast.
Thyrotoxicosis:
In adults, at the beginning of treatment, depending on the severity of thyrotoxicosis, Mercazolil is used 3 times a day (every 8 hours) in a total dose:
- 15 mg/day (3 tablets) in case of mild thyrotoxicosis;
- 20-30 mg/day (4-6 tablets) in case of moderate thyrotoxicosis;
- 40 mg/day (8 tablets) in severe cases of thyrotoxicosis.
After normalization of thyroid function, maintenance doses of the drug are prescribed - from 2.5 to 10 mg/day (½ - 2 tablets) in 1 or 2 doses.
During pregnancy, the drug is prescribed in the lowest possible doses - 2.5-1 mg/day. At the beginning of treatment, children are usually prescribed 300-500 mcg/kg body weight/day in 3 doses; maintenance dose - 200-300 mcg/kg body weight per day in 2 divided doses.
For children under 3 years of age, the drug is dissolved in water to form a thin suspension, which is prepared immediately before administration.
The duration of treatment with Mercazolil is determined by the individual needs of the patient. Experience in the therapeutic use of the drug shows that the duration of treatment for thyrotoxicosis in diffuse toxic goiter should be 1.5-2 years.
In preparation for surgical treatment of thyrotoxicosis prescribe 20-40 mg/day until a euthyroid state is achieved within 3-4 weeks before the planned day of surgery (in some cases, longer); From this time on, additional levothyroxine is recommended. Stop taking thiamazole the day before surgery.
In order to reduce the time required to prepare for surgery, beta-blockers and iodine preparations are additionally prescribed.
In preparation for treatment with radioactive iodine: prescribe 20-40 mg/day until a euthyroid state is achieved. Note: Thiamazole and thiourea derivatives may reduce the sensitivity of thyroid tissue to radiation therapy.
Therapy during the latent period of radioactive iodine action: depending on the severity of the disease, 5-20 mg/day is prescribed until the onset of the effect of radioactive iodine (4-6 months).
Long-term thyreostatic maintenance therapy: 2.5-10 mg/day with additional small doses of levothyroxine.
Prevention of thyrotoxicosis when prescribing iodine preparations (including cases of use of iodine-containing radiocontrast agents) in the presence of latent thyrotoxicosis, autonomous adenomas or a history of thyrotoxicosis: Prescribe 10-20 mg/day of thiamazole and 1 g of potassium perchlorate per day for 8-10 days before taking iodine-containing drugs.
For liver failure the minimum effective dose of the drug is prescribed.
In all cases, the duration of treatment with the drug is determined by the doctor.

Side effect

Allergic reactions (itching, rash, urticaria), suppression of myelopoiesis (agranulocytosis, granulocytopenia, thrombocytopenia), aplastic anemia, drug fever, autoimmune syndrome with hypoglycemia, generalized lymphadenopathy, sialadenopathy, neuritis, taste disturbances, alopecia, polyneuritis, lupus-like syndrome, hypoprothrombinemia ( petechiae, bleeding), periarteritis, hepatitis, cholestatic jaundice, skin itching, nausea, vomiting, epigastric pain, arthralgia, myalgia, paresthesia, severe weakness, headache, dizziness, skin hyperpigmentation, edema, weight gain, rarely - nephritis.
Subclinical and clinical hypothyroidism can develop when taking high doses of the drug. The thyroid gland may also begin to enlarge, which is associated with an increase in TSH levels in the blood.

Release form

Tablets 5 mg.
10 tablets per blister pack.
5 or 10 blister packs along with instructions for use in a cardboard pack.

Storage conditions

In a dry place, protected from light, at a temperature not exceeding 25 ° C.
Keep out of the reach of children.

Conditions for dispensing from pharmacies

On prescription.

*Full information on the drug is contained in the Instructions for medical use of the drug

Manufacturer/Organization receiving consumer complaints

Open Joint Stock Company "Chemical and Pharmaceutical Plant "AKRIKHIN" (JSC "AKRIKHIN"), Russia 142450, Moscow region, Noginsky district, Staraya Kupavna, st. Kirova, 29.

In case of dysfunction of the thyroid gland, thyrotoxicosis, diffuse toxic goiter, it is important to take medications that reduce the risk of severe intoxication due to hormonal imbalance. During the period of preparation for radioiodine therapy, it is necessary to stabilize the levels of thyroxine, triiodothyronine and thyroid-stimulating hormone.

The drug Mercazolil supports the body and normalizes the functions of the affected gland. The medicine has many advantages: it is effective in the treatment of acute conditions and for maintenance therapy; if prescribed by a doctor, it is allowed to take tablets for 1.5 years or more; low price. It is important to strictly follow the instructions for use, monitor blood counts and hormone levels.

Composition and action

Thiamazole 5 mg is the active ingredient of the drug Mercazolil. Active absorption from the digestive tract is noted, the process of biotransformation occurs, the half-life is 6 hours. Residues in the form of unchanged substance and metabolites are excreted from the body in the urine.

Mercazolil is an antithyroid drug. After taking the tablets, the active substance blocks the production of the enzyme pyroxidase, without which the process of iodination and triiodothyronine is disrupted. As a result of the reaction, the synthesis of the hormones T3 and T4 decreases.

Release form

Flat-cylindrical tablets with a bevel, color - white or white with a slight yellowish tint. Mercazolil Health (Ukraine) is supplied to pharmacies in plastic containers: 50 and 100 units, Mercazolil Akrikhin (Russia) - in blisters: 50 or 100 units. The cardboard box contains instructions for using the antithyroid drug.

Indications for use

Tablets based on thiamazole are prescribed for damage to the thyroid gland:

  • mixed form of toxic. Mercazolil is combined with drugs containing doses of thyroid hormones;
  • to eliminate the symptoms and consequences of thyrotoxic crisis;
  • diffuse form of toxic goiter;
  • during preparation for radioiodine therapy;
  • for prevention during treatment with the use of iodine-containing compounds;
  • as a maintenance drug during the latent period after taking a capsule with radioactive iodine;
  • in preparation for surgery for severe thyrotoxicosis.

Contraindications

The drug Mercazolil is not prescribed:

  • with excessive sensitivity to thiamazole;
  • against the background of a pronounced violation of blood counts: granulocytopenia and leukopenia;
  • during pregnancy, especially in the second and third trimester: thiamazole actively overcomes the placental barrier. In the later stages of pregnancy, an analysis of deviations showed: there is a high probability of developing hypofunction of the thyroid gland in the fetus;
  • during breastfeeding.

Instructions for use

The dosage is determined by the endocrinologist on an individual basis, taking into account the stage of the thyroid disease. The daily maintenance rate and the amount of active substance to stop the acute process are significantly different. It is prohibited for the patient to independently adjust the number of tablets, which needs to be taken throughout the day, especially when there is compression of the trachea due to the growth of a goiter.

Take the tablets strictly after meals, with plenty of water, without chewing. In the acute stage, to relieve signs of thyrotoxicosis, it is important to receive thiamazole at regular intervals. When switching to a maintenance dosage, take the tablets after breakfast in one dose.

Up to three years of age, children receive a thin suspension based on the drug (dissolve the tablet in boiled water shortly before use). During treatment, supervision by a pediatrician and pediatric endocrinologist is required.

With diffuse toxic goiter, the course duration reaches one and a half to two years. Correction of the daily norm is carried out by the doctor observing the patient.

The average norm is from 15 mg (mild stage of thyrotoxicosis) to 40 mg of thiamazole in severe forms of the pathology, necessarily in three doses. When normalizing the functioning of a weakened gland, a lower maintenance dosage is needed - from 2.5 to 10 mg per day.

On a note! During the period of preparation for taking the capsule for radioiodine therapy, the endocrinologist selects the dosage to achieve a euthyroid state. Values ​​vary from 20 mg thiamazole to 40 mg of active substance. Before the onset of a pronounced therapeutic effect during treatment with radioactive iodine, the patient receives from 5 to 20 mg of the antithyroid component for four to six months.

Side effects

Negative reactions from the digestive, nervous system, allergic manifestations occur rarely. Even with long-term use of Mercazolil tablets, patients note good tolerability of thiamazole. Based on test results, doctors detect hyperplasia of an important organ in some patients.

Possible reactions to thiamazole:

  • skin rashes, febrile syndrome;
  • change in taste, nausea, vomiting;
  • development of leukocytosis and leukopenia, very rarely - generalized lymphadenopathy;
  • headaches, polyneuropathy.

Overdose

Violation of the daily norm of thiamazole can provoke negative phenomena: skin itching, the development of aplastic anemia, tissue swelling, nausea, pain in the epigastrium, fever, vomiting. Less commonly, nephrotic syndrome, neuropathy, excessive nervous excitement or a depressed state, and inhibition of reactions occur.

Against the background of signs of overdose, you need to stop Mercazolil tablets, rinse your stomach, and take an effective sorbent: Multisorb, Enterosgel, White Coal, Polysorb MP. With prolonged overdose, development is observed, the thyroid gland enlarges, which requires mandatory withdrawal of the drug. In case of pronounced hypofunction of the endocrine organ, replacement therapy is carried out using levothyroxine.

Additional Information

The antithyroid drug Mercazolil based on thiamazole can affect blood counts and the size of the thyroid gland. During the period of selecting the optimal dose, control studies are carried out every 2 weeks, during maintenance therapy - once every 30 days. To exclude severe side effects, you need to take tests to determine the level of red blood cells, leukocytes, eosinophils, basophils, platelets, and other blood components.

There are other nuances of therapy that the patient should know about:

  • against the background of large struma with narrowing of the trachea, a short-term course of the drug Mercazolil is allowed: taking tablets with thiamazole over a long period can provoke an increase in the size of the affected areas. To reduce the risk of adverse events, a combination of thiamazole with levothyroxine is indicated;
  • when preparing for surgical treatment against the background of thyroid hyperplasia, taking Mercazolil tablets is discontinued 7-14 days before surgery. Next, the patient takes iodine-containing formulations;
  • It is important to know: the therapeutic effect of taking thiamazole is reduced by excessive doses of iodine;
  • the patient should immediately contact an endocrinologist if signs of agranulocytosis develop: sore throat, furunculosis, inflammation of tissues in the oral cavity;
  • discontinuation of the drug Mercazolil is mandatory in the event of severe weakness, bleeding of unknown origin, itching and rashes over a large area, frequently recurring nausea and vomiting, and the development of jaundice;
  • You should not stop taking thiamazole-based tablets before the time specified by the endocrinologist: the risk of relapse increases;
  • ophthalmopathy with damage to the thyroid gland is not included in the list of adverse reactions to thiamazole;
  • In some patients, tests show the development of late hypothyroidism after discontinuation of Mercazolil tablets. The decrease in the function of the endocrine organ is not associated with the course of therapy: the cause of the disorders lies in tissue destruction and inflammation of the thyroid gland.

Drug interactions

The drug Mercazolil is taken strictly according to the dosage prescribed by the endocrinologist. Before starting therapy, the attending physician must know about all the names of medications that the patient receives: thiamazole interacts with the components of individual drugs.

Important points:

  • the risk of leukopenia is increased when taking Mercazolil simultaneously with sulfonamides and acetylsalicylic acid;
  • the antithyroid effect of the active substance increases when taking the antibacterial agent Gentamicin;
  • To reduce the risk of leukopenia during treatment with thiamazole, the patient should receive folic acid or Leukogen.

Go here to learn about the signs of high blood sugar in women and how to lower your levels.

Price

The drug based on thiamazole is an inexpensive name. The cost of the medicine depends on the packaging, the average price of Mercazolil is 35 rubles (50 tablets). An acceptable price category reduces the cost of a long course of maintenance therapy after stabilization of the functions and size of the thyroid gland.

Mercazolil tablets should be stored in a ventilated area, at temperatures up to + 25 C, in a closed cardboard package. The shelf life of the antithyroid drug is 5 years.

Mercazolil: analogues

The endocrinologist may prescribe another thiamazole-based drug if Mercazolil tablets are not suitable for the patient for any reason. Effective substitutes for antithyroid drugs: Metizol.

Tablets with the same active ingredient are suitable for long courses of therapy. It is important to take into account contraindications: Mercazolil analogues have differences in the list of restrictions.

Instructions

for medical use

medicine

MERCAZOLIL-HEALTH

Tradename

Mercazolil-Health

International nonproprietary name

Thiamazole

Dosage form

Tablets, 5 mg

Compound

One tablet contains:

active substance - thiamazole 5 mg,

Excipients: potato starch, calcium stearate, refined sugar, talc.

Description

Tablets are white or white with a yellowish tint, with a flat surface and a bevel

Pharmacotherapeutic group

Drugs for the treatment of thyroid diseases. Antithyroid drugs. Sulfur-containing imidazole derivatives. Thiamazole.

ATX code Н03ВВ02

Pharmacological properties

Pharmacokinetics

After oral administration, it is quickly and almost completely absorbed from the gastrointestinal tract. Bioavailability is 93%. The maximum concentration in the blood is reached after 40-80 minutes. It practically does not bind to blood proteins. Cumulates in the thyroid gland. It is slowly metabolized in the thyroid gland, liver and kidneys, and therefore a plateau is formed under the pharmacokinetic curve, which persists for 24 hours after taking a single dose. No dependence of pharmacokinetic parameters on the functional state of the thyroid gland was revealed. Penetrates into breast milk and can reach a concentration in it corresponding to the concentration in the blood. The half-life is 3-6 hours, prolonged in patients with liver failure. It is excreted in the form of metabolites and unchanged by the kidneys (70% within 24 hours) and with bile.

Pharmacodynamics

An antithyroid agent that inhibits the formation of thyroid hormones - thyroxine (T 4) and triiodothyronine (T 3), which allows for symptomatic treatment of thyrotoxicosis, with the exception of cases of thyrotoxicosis development due to the release of hormones after the destruction of thyroid cells (after treatment with radioactive iodine or with thyroiditis) .

The mechanism of thyreostatic action is due to inhibition of the activity of the peroxidase enzyme involved in the iodination of thyroid hormones of the thyroid gland, which leads to inhibition of their synthesis. It does not affect the secretion of previously synthesized thyroid hormones, therefore a latent period precedes the decrease in the concentration of thyroxine and triiodothyronine in the blood under the influence of the drug.

The drug normalizes metabolic processes in the thyroid gland, reduces the basic metabolic metabolism in the body (increased with hyperfunction of the thyroid gland), accelerates the removal of iodides from the thyroid gland, increases the reciprocal activation of the synthesis and release of thyroid-stimulating hormone by the pituitary gland.

Indications for use

Thyrotoxicosis

Preparation for surgical treatment of thyrotoxicosis

Preparation for treatment of thyrotoxicosis with radioactive iodine

Therapy during the latent period of radioactive iodine action (before the onset of radioactive iodine action for 4-6 months)

Long-term maintenance therapy for thyrotoxicosis in exceptional cases when the patient’s general condition or other individual reasons do not allow radical treatment

Prevention of thyrotoxicosis when prescribing iodine preparations (including iodine-containing X-ray contrast agents) in the presence of latent thyrotoxicosis, autonomous adenomas or a history of thyrotoxicosis

Directions for use and doses

Prescribed orally, after meals, without chewing, with a sufficient amount of liquid. The initial and maintenance doses are set individually. The daily dose is prescribed in one dose or divided into 2-3 single doses. At the beginning of treatment, single doses are taken throughout the day at regular intervals. The maintenance dose is taken in 1 dose after breakfast.

Adults

Thyrotoxicosis

Depending on the severity of the disease, the drug is prescribed in a daily dose of 10-40 mg (2-8 tablets). After normalization of thyroid function (usually after 3-8 weeks), they switch to taking a maintenance dose of 5-20 mg (1-4 tablets) per day. The duration of therapy ranges from 6 months to 2 years (average 1 year). The possibility of extending the period of remission depends on the duration of therapy.

Preparation for surgical treatment of thyrotoxicosis

Prescribed in a daily dose of 20-40 mg (4-8 tablets) until a euthyroid state is achieved within 3-4 weeks before the planned operation (in individual cases, the drug is started earlier) and is stopped 1 day before the operation. During the last 10 days before surgery, the surgeon may additionally prescribe iodine preparations to strengthen the thyroid tissue.

Preparation for treatment of thyrotoxicosis with radioactive iodine

Prescribed in a daily dose of 20-40 mg (4-8 tablets) until a euthyroid state is achieved. It should be taken into account that thiourea derivatives may reduce the sensitivity of thyroid tissue to radiation therapy.

Therapy during the latent period of radioactive iodine action

Depending on the severity of the disease, the drug is prescribed in a daily dose of 5-20 mg (1-4 tablets) before the onset of radioactive iodine action.

Long-term maintenance therapy for thyrotoxicosis

The minimum effective dose is prescribed - 2.5-10 mg per day; if necessary, additional administration of levothyroxine is possible. If it is necessary to prescribe a dose of 2.5 mg, the drug should be used with the appropriate dosage.

Prevention of thyrotoxicosis when prescribing iodine preparations (including cases of use of iodine-containing radiocontrast agents) in the presence of latent thyrotoxicosis, autonomous adenomas or a history of thyrotoxicosis

Patients with liver failure

The minimum effective dose of the drug is prescribed under close medical supervision.

Patients with narrowing of the trachea and a significant increase in the size of the thyroid gland

Use for a short period, since long-term action of the drug can lead to an increase in the size of the thyroid gland.

Children

For children from 3 to 17 years of age, the drug is prescribed at an initial dose of 0.3-0.5 mg/kg body weight per day. The maintenance dose is 0.2-0.3 mg/kg body weight per day. If necessary, additional levothyroxine is prescribed.

Doses and duration of treatment are determined individually by the attending physician.

Side effects

Most side effects are dose-dependent and occur in the first 4-8 weeks of treatment. If side effects develop, reduce the dose of the drug or stop taking it.

From the blood and lymphatic system

Infrequently

Leukopenia, agranulocytosis

Rarely

Aplastic anemia, hypoprothrombinemia, thrombocytopenia, pancytopenia

Very rarely

Generalized lymphadenopathy

From the nervous system

Rarely

Headache, dizziness

Very rarely

Neuritis, polyneuropathy

From the digestive tract

Often

Nausea, vomiting

Rarely

Reversible change in taste sensations (dysgeusia, ageusia)

Very rarely

Acute inflammation of the salivary glands

From the skin and subcutaneous tissue

ABOUTvery often

Itching, hyperemia, skin rash, urticaria, which disappear with further therapy

Very rarely

Severe dermatitis

From the musculoskeletal system and connective tissue

Very rarely

Arthralgia developing gradually, sometimes even several weeks after therapy, without clinical symptoms of nonspecific arthritis

Endocrine disorders

Often

Hypothyroidism, thyroid hyperplasia, fever;

Rarely

Insulin autoimmune syndrome with a sharp decrease in blood glucose concentration

Metabolism disorders

Often

Increase in body weight (by reducing pathologically increased energy consumption in hyperthyroidism, which may indicate normalization of energy metabolism)

From the hepatobiliary system

Very rarely

Liver dysfunction, cholestatic jaundice, toxic hepatitis Other

Often

Weakness

Rarely

Increased postoperative thyroid bleeding

Increased body temperature

Very rarely

Systemic lupus erythematosus

Alopecia

Quincke's edema.

Contraindications

Increased individual sensitivity to the drug, thiourea derivatives and/or to other components of the drug

Agranulocytosis

Bone marrow damage from previous carbimazole therapy

or thiamazole

Granulocytopenia (including history)

Cholestasis before treatment

Combined therapy with thiamazole and thyroid hormones during pregnancy

Breastfeeding period

Children under 3 years of age

Drug interactions

With the simultaneous use of Mercazolil-Zdorovye with amidopyrine and its analogues, sulfonamides, the risk of developing leukopenia increases. The effectiveness of the drug is increased by a lack of iodine in the body, lithium preparations, b-blockers (especially during preparation for subtotal thyroidectomy), reserpine, amiodarone, gentamicin; reduce - excess iodine (potassium iodide, iodine).

The drug reduces the sensitivity of thyroid tissue to radiation therapy, the effectiveness of anticoagulants (coumarin, indandione derivatives), and increases the clearance of b-blockers.

The risk of developing leukopenia is reduced with simultaneous use with leukogen and folic acid.

It should be taken into account that with thyrotoxicosis, the metabolism and elimination of various drugs is accelerated, and restoration of thyroid function may require adjustment of the dosage regimen. After achieving a euthyroid state in patients taking Mercazolil-Zdorovye for the treatment of thyrotoxicosis, it may be necessary to change the doses of concomitantly used drugs: reducing the doses of cardiac glycosides, aminophylline; increasing doses of warfarin and other anticoagulants (coumarin and indanedione derivatives).

When co-administered with amiodarone, it may be necessary to reduce the dose of Mercazolil-Zdorovye.

special instructions

In patients with a significant increase in the size of the thyroid gland and narrowing of the trachea, the drug should be used with caution and for the shortest possible period.

Before starting treatment, it is necessary to pay special attention to the symptoms of agranulocytosis (stomatitis, pharyngitis, high body temperature). If any of the above symptoms develop, especially in the 1st week of treatment, you should stop taking the drug and immediately consult a doctor for a blood test.

Excess of the drug in the body after taking very high doses can lead to the development of subclinical/clinical hypothyroidism or an increase in the size of the thyroid gland due to increased levels of thyroid-stimulating hormone. Therefore, the dose of the drug should be reduced after reaching the metabolic conditions of a normally functioning thyroid gland and additionally prescribe levothyroxine.

Manifestations or worsening of endocrine pathology of the eyeball do not depend on the course of treatment prescribed for thyroid disease. Such complications are not a reason to change the treatment regimen (antithyroid drugs, surgery, radiotherapy) and are not an adverse reaction if the course of treatment is carried out correctly.

In isolated cases, after a course of antithyroid therapy without any additional measures, late hypothyroidism may appear. This is not an adverse reaction to the drug, but the result of inflammatory and destructive processes in the thyroid parenchyma caused by the underlying disease.

The drug contains refined sugar, which should be taken into account by patients with diabetes.

Premature cessation of treatment may lead to relapse of the disease.

Pregnancy and lactation

During pregnancy, the use of the drug is possible only in cases of extreme necessity, when the expected therapeutic effect outweighs the potential risk to the fetus. In this case, the drug is prescribed in minimally effective doses that allow maintaining the level of thyroid hormones at the upper limit of normal, without additional use of thyroid hormones. A high dose can cause goiter formation and hypothyroidism in the fetus.

During lactation, treatment of thyrotoxicosis, if necessary, can be continued in minimal doses (no more than 10 mg/day) under the control of thyroid function in newborns, since thiamazole passes into breast milk, which can cause the risk of developing hypothyroidism in infants.

Features of the effect of the drug on the ability to drive vehicles and potentially dangerous mechanisms

There are no data on the effect of the drug on the ability to drive vehicles and perform potentially hazardous activities. The possibility of developing side effects (headache, dizziness, weakness, etc.) of the drug should be taken into account.

Overdose

Symptoms: nausea, vomiting, epigastric pain, fever, arthralgia, skin itching, swelling. Aplastic anemia (pancytopenia) or agranulocytosis may manifest itself in the first hours. Less commonly - hepatitis, nephrotic syndrome, exfoliative dermatitis, neuropathy, depression or stimulation of the central nervous system.

Treatment: gastric lavage, activated carbon, symptomatic therapy.

Chronic overdose of thiamazole leads to an enlargement of the thyroid gland and the development of hypothyroidism. In this case, treatment with the drug is stopped. Replacement therapy with levothyroxine is carried out if this is justified by the severity of hypothyroidism. As a rule, after discontinuation of thiamazole, spontaneous restoration of thyroid function is observed.

Release form and packaging

Attention! The information is provided for informational purposes only. This instruction should not be used as a guide to self-medication. The need for prescription, methods and doses of the drug are determined exclusively by the attending physician.

general characteristics

international and chemical names: thiamazole; 1-methyl-2-mercaptoimidazole.

basic physical and chemical properties: tablets of white or white with a yellowish tint, with a flat surface, with a bevel;

compound: Mercazolil - 0.005 g;

Excipients: sugar, potato starch, calcium stearate, talc.

Release form. Pills.

Pharmacological group

ATS N03V B02. Drugs hormones (Hormones- biologically active substances produced in the body by specialized cells or organs (endocrine glands) and having a targeted effect on the activity of other organs and tissues) for systemic use. Antithyroid drugs.

Pharmacological properties

The mechanism of action of Mercazolil is due to inhibition of thyroxine synthesis in the thyroid gland. gland (Glands- organs that produce and secrete specific substances that participate in various physiological functions and biochemical processes of the body. The endocrine glands secrete their waste products - hormones - directly into the blood or lymph. Exocrine glands - on the surface of the body, mucous membranes or in the external environment (sweat, salivary, mammary glands)), which leads to the normalization of metabolic processes in it during hyperfunction. The drug reduces basal metabolism. The effect of Mercazolil manifests itself in the acceleration of elimination from thyroid gland (Thyroid- endocrine gland. Located on the neck, in the area of ​​the laryngeal cartilages. Consists of two lobes and an isthmus. Produces the hormones thyroxine, triiodothyronine, thyrocalcitonin, which regulate the growth and development of the body (tissue differentiation, metabolic rate, etc.). Damage to the thyroid gland leads to the occurrence of certain diseases (with increased function - thyrotoxicosis, with decreased function - myxedema\; in some areas, due to a lack of iodine in water and soil, the so-called endemic goiter is common, i.e. associated with a certain area) ) iodides and inhibition of the activity of enzyme systems that oxidize iodides to iodine. As a result, inhibition of iodination of thyroglobulin and the conversion of diiodotyrosine to thyroxine is observed.

Indications for use

Mercazolil is prescribed for diffuse toxic (Toxic- poisonous, harmful to the body) goiter (Goiter- persistent enlargement of the thyroid gland. The most important clinical forms: endemic goiter (a disease of humans and animals in certain biogeochemical provinces associated with insufficient intake of iodine into the body) and diffuse toxic goiter) mild, moderate and severe forms, preparing patients for surgery for thyrotoxicosis.

Directions for use and doses

Mercazolil is prescribed orally after meals. For mild to medium thyrotoxicosis (Thyrotoxicosis- a syndrome caused by the effect of excess thyroxine and triiodothyronine on target tissue. There are many causes of thyrotoxicosis\; the most common cause is diffuse toxic goiter (Graves disease). The clinical picture includes the effect of hormones on different organs. Symptoms of activation of the sympathoadrenal system are characteristic: tachycardia, tremor, sweating, anxiety. These symptoms are eliminated by beta blockers) adults take the drug 0.005 g 3-4 times a day, in severe cases - 0.01 g 3-4 times a day. After the onset of remission (usually after 3-6 weeks), the daily dose is reduced every 5-10 days by 0.005-0.01 g, gradually selecting the minimum maintenance dose: 0.005 g 1 time per day; 0.005 g every other day; 0.005 g 1 time every 3 days. Take until a lasting effect is obtained. If thyrotoxicosis relapses, the dose of the drug is increased again, adhering to the specified regimen therapy (Therapy- 1. The field of medicine that studies internal diseases is one of the oldest and main medical specialties. 2. Part of a word or phrase used to indicate the type of treatment (oxygen therapy\; hemotherapy - treatment with blood products)). The duration of administration is determined by the form and severity of the disease and the effect achieved. Higher doses for adults orally: single - 0.01 g, daily - 0.04 g. For thyrotoxicosis in children, the initial dose is 0.4 mg/kg body weight per day once, or divided into two doses; maintenance dose – 0.2 mg/kg of the child’s body weight per day once, or divided into two doses.

Side effect

Agranulocytosis (Agranulocytosis– a pathological syndrome in which the number of granulocytes in the peripheral blood sharply decreases or they are completely absent), leukopenia (Leukopenia- the content of leukocytes in the peripheral blood is less than 4000 in 1 μl, due to the influence of various damaging factors on the body), thrombocytopenia (Thrombocytopenia- decrease in platelet count), gastrointestinal disorders, liver damage, dizziness, swelling (Edema– tissue swelling as a result of a pathological increase in the volume of interstitial fluid), skin rash, paresthesia (Paresthesia(from the Greek par - near, past, outside and isthesis - feeling, sensation) - an unusual sensation of numbness of the skin, “crawling goosebumps”, which occurs without external influence or under the influence of some mechanical factors (compression of a nerve, vessel). Paresthesia can be a manifestation of diseases of the peripheral nerves, less often - of the sensory centers of the spinal cord or brain), pain in joints (Joints- movable joints of bones that allow them to move relative to each other. Auxiliary structures – ligaments, menisci and other structures), baldness, visual impairment, medication hypothyroidism (Hypothyroidism– (thyroid atrophy) replacement of thyroid tissue with connective tissue), goitrogenic effect. If a side effect occurs, the dose of the drug is reduced or the drug is discontinued.

Contraindications

Pregnancy, breastfeeding, severe leukopenia and granulocytopenia, nodular forms of goiter (exception - severe, progressive course, temporarily postponing surgery).

Overdose

Clinical symptoms. Changes menstrual cycle (Menstrual cycle– regularly recurring uterine bleeding, during which a woman loses an average of 50–100 ml of blood. The coagulability of menstrual blood is reduced, so bleeding continues for 3–5 days. The duration of the menstrual cycle is 28 days, it can be less (up to 21 days) or more (up to 30–35 days)), dry skin, drowsiness, headache, muscle weakness. Specific antidote (Antidotes- medicines used to treat poisoning in order to neutralize the poison and eliminate the pathological disorders caused by it) unknown

Interaction with other drugs

Mercazolil should not be combined with drugs that cause leukopenia: amidopyrine and its analogues, sulfonamides.

Features of application

If treatment with Mercazolil is stopped early, a relapse of the disease is possible.
There is information about the advisability of combining Mercazolil with lithium carbonate.
Mercazolil should be used under the supervision of a physician and the condition of the peripheral blood should be examined once a week. When preparing for surgery, as a result of using the drug, it is possible that increased bleeding of the thyroid gland may occur. To avoid this (when remission is achieved or a significant improvement in the condition), Mercazolil is discontinued and iodine preparations are prescribed. The operation is performed after 2-3 weeks.

General Product Information

Conditions and shelf life. Store in a dry place, protected from light.
Shelf life – 5 years.

Vacation conditions. On prescription.

Package. 50 or 100 tablets in glass jars, placed in cardboard packs;
50 or 100 tablets in plastic containers for medicines;
50 or 100 tablets in plastic containers for medicines, placed in cardboard packs.

Manufacturer.LLC "Pharmaceutical company "Zdorovye".

Location. 61013, Ukraine, Kharkov, st. Shevchenko, 22.

Website. www.zt.com.ua

This material is presented in free form on the basis of the official instructions for medical use of the drug.