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

Active substanceThiamazoleThiamazole

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Mercazolil

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MARBIOFARM, OJSC Russia

Mercazolil

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HEALTH PHARMACEUTICAL COMPANY, LTD. Ukraine

Mercazolil

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AKRIKHIN HFK, JSC Russia

Tirozol®

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Merck KGaA Germany

Dosage form: & nbsppills

Composition:

In 1 tablet:

active substance: thiamazole 5 mg;

Excipients: potato starch, calcium stearate, sucrose (refined sugar), talc.

Description:Tablets are white or white with a yellowish hue of color, flat-cylindrical shape, with a bevel.

Pharmacotherapeutic group:Antithyroid agent

ATX: & nbsp

H.03.B.B Imidazole derivatives containing sulfur

H.03.B.B.02 Thiamazole

Pharmacodynamics:

Antithyroid medication; breaks the synthesis of thyroid hormones, inhibiting iodide peroxidase, involved in iodination of thyronin in the thyroid gland with the formation of triiodo- and tetraiodothyronine (thyroxine), reduces the internal secretion of thyroxin. This property allows to carry out symptomatic therapy of thyrotoxicosis regardless of etiology. Mercazolil does not affect the release of synthesized thyronins from thyroid follicles. This explains the latent period of different duration, which may precede the normalization of the concentration of triiodothyronine (T3) and thyroxine (T4) in blood plasma, i.e.improvement of clinical picture. Mercazolil does not affect thyrotoxicosis, which is due to the release of hormones after the destruction of thyroid cells (after treatment with radioactive iodine or thyroiditis).

Mercazolil reduces basal metabolism, accelerates the excretion of iodides from the thyroid gland, increases the reciprocal activation of the synthesis and excretion of the thyroid-stimulating hormone by the pituitary, which is accompanied by some hyperplasia of the thyroid gland.

Pharmacokinetics:

Suction. Thiamazole well absorbed after ingestion, eating does not affect the amount and speed of absorption. The maximum concentration in the blood is reached within 30-60 minutes and is 1.184 μg / ml with an oral dose of 60 mg. Bioavailability is 93%.

Distribution. With blood proteins is virtually not associated. It accumulates in the tissues of the thyroid gland. Small amounts are found in breast milk. The volume of distribution is 0.6 l / kg. Metabolism. Metabolism is carried out in the liver with the formation of inactive metabolites. Excretion. The half-life is 5-6 hours. It is excreted from the body by the kidneys, and less than 10% - in unchanged form.In patients with hepatic insufficiency, the half-life increases.

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 performed 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, atonic adenomas or thyrotoxicosis in the anamnesis.

Contraindications:

Hypersensitivity to thiamazole or thiourea derivatives;
agranulocytosis during previous therapy with carbimazole or thiamazole;
granulocytopenia (including in the anamnesis);
severe leukopenia;
cholestasis before treatment;
lactation period;
deficiency of sucrose / isomaltase, intolerance to fructose, glucose-galactose malabsorption;
children's age till 9 years.

If you have any of these diseases, consult a doctor before taking the drug.

Carefully:In pregnant women; in patients with goiter of very large size with narrowing of the trachea (only short-term treatment in the period of preparation for surgery); with hepatic insufficiency; in patients receiving anticoagulants, cardiac glycosides, and aminophylline.

Pregnancy and lactation:Thiamazole penetrates the placental barrier. The use after the first trimester of pregnancy is associated with the threat of development of hypothyroidism in the fetus. During pregnancy, the drug is prescribed only for vital signs in the event that the expected effect of therapy for the mother exceeds the potential risk for the fetus, in a minimally effective dose without additional intake of thyroid hormone drugs under the strict supervision of a doctor. If you need to use during lactation, breastfeeding should be discontinued, as the drug is excreted in breast milk.

Dosing and Administration:

Tablets should be taken orally after a meal, without chewing, with a sufficient amount of liquid.The daily dose is prescribed in one session or divided into two to three single doses. At the beginning of the treatment, single doses are taken during the day at a strictly defined time. The maintenance dose should be taken in one session after breakfast.

Thyrotoxicosis:

In adults at the beginning of treatment, depending on the degree of severity of thyrotoxicosis, Mercazolil is applied 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 moderately expressed thyrotoxicosis;

- 40 mg / day (8 tablets) in severe cases of thyrotoxicosis.

After normalization of thyroid function, maintenance doses of the drug are prescribed - from 5 to 10 mg / day (1-2 tablets) in 1 or 2 doses.

In pregnancy, the drug is prescribed in the lowest possible doses - 5-10 mg / day.

Children older than 9 years at the beginning of treatment usually appoint 300-500 μg / kg of body weight / day in 3 divided doses; maintenance dose - 200-300 mkg / kg body weight per day in 2 divided doses.

The duration of treatment with Mercazolil is determined by the individual need of the patient. The duration of treatment of thyrotoxicosis in diffuse toxic goiter should be 1.5-2 years.

When preparing for surgical treatment, thyrotoxicosis is prescribed 20-40 mg / day until the euthyroid state is reached within 3-4 weeks before the planned operation day (in some cases, longer); from this time, an additional intake of levothyroxine sodium is recommended.

Stop taking thiamazole the day before the surgery.

In order to reduce the time needed to prepare for the operation, additionally prescribe beta-blockers and iodine preparations.

When preparing for treatment with radioactive iodine: 20-40 mg / day is prescribed until the euthyroid state is reached. Note: thiamazole and thiourea derivatives can 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, prescribe 5-20 mg / day before the onset of the action of radioactive iodine (4-6 months). Long-term thyrostatic maintenance therapy:

5-10 mg / day with the additional intake of small doses of levothyroxine sodium.

Prophylaxis of thyrotoxicosis when prescribing iodine preparations (including cases of using iodine-containing X-ray contrast media) in the presence of latent thyrotoxicosis,atonic adenomas or thyrotoxicosis in history: 10-20 mg / day of thiamazole and 1 g of potassium perchlorate per day are prescribed for 8-10 days before taking iodine-containing drugs.

With hepatic insufficiency appoint a minimally effective dose of the drug.

In all cases, the duration of treatment with the drug is determined by the doctor.

Side effects:

From the side of metabolism: drug fever, autoimmune syndrome with hypoglycemia, generalized lymphadenopathy, sialadenopathy, weight gain, swelling.

On the part of the blood system: suppression of myelopoiesis (agranulocytosis, granulocytopenia, thrombocytopenia), aplastic anemia, hypoprothrombinemia (petechiae, bleeding).

Allergic reactions: itching of the skin, skin rash, hives.

From the central and peripheral nervous systems: headache, dizziness, neuritis, polyneuropathy, polyneuritis, paresthesia.

From the gastrointestinal tract: nausea, vomiting, taste disorders, epigastric pain, cholestatic jaundice, hepatitis.

Other: severe weakness, lupus-like syndrome, arthralgia, myalgia, periarteritis, alopecia, hyperpigmentation of the skin, nephritis.

When taking high doses of the drug, subclinical and clinical hypothyroidism may develop. An enlargement of the thyroid gland may also begin, which is associated with an increase in the thyroid-stimulating hormone (TSH) content in the blood.

Most side effects are dose-dependent and occur during the first 4-8 weeks of treatment. With the development of side effects, reduce the dose or stop taking the drug. If any of the side effects listed in the manual are aggravated, or if you notice any other side effects not indicated in the instructions, tell your doctor.

Overdose:

Symptoms: nausea, vomiting, epigastric pain, fever, arthralgia, skin itching, swelling. Aplastic anemia (pancytopenia) or agranulocytosis can manifest in the first hours. More rarely - hepatitis, nephrotic syndrome, exfoliative dermatitis, neuropathy, oppression or excitation of the central nervous system. With prolonged intake of excessive doses, hyperthyroidism of the thyroid gland.

Treatment: gastric lavage, Activated carbon, symptomatic therapy.

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

Interaction:

Preparations of lithium, beta-blockers, reserpine, amiodarone increase the effect of thiamazole (requires correction of its dose). Sulfanilamides, metamizol sodium increase the risk of developing leukopenia. Myelotoxic drugs increase the manifestation of hematotoxicity of the drug. Deficiency of iodine increases, and excess (for example, arising on the background of medications containing large amounts of iodine) weakens the effect.

Gentamicin increases the antithyroid effect of thiamazole.

In patients receiving thiamazole about hyperthyroidism, after reaching the euthyroid state may need to reduce the dose received cardiac glycosides (digoxin and digitoxin), aminophylline and increasing doses received warfarin and other anticoagulant - coumarin and indandione derivatives (pharmacological interaction).

If you are taking other medications, be sure to consult a doctor.

Special instructions:

During treatment, it is necessary to monitor peripheral blood (at intervals of 1-2 weeks at the time of dose selection and once a month - during maintenance therapy).

Patients with a significant increase in the thyroid gland narrowing the lumen of the trachea, Merkazolil is prescribed for a short time in combination with levothyroxine sodium, as with prolonged use, it is possible to increase the goiter and even more squeezing of the trachea.

It is necessary to carry out careful monitoring of the patient (monitoring the concentration of TSH, lumen of the trachea).

The patient should be warned about the necessity of compulsory treatment to a doctor when fever, chills, coughing, sore throats, inflammation of the oral mucosa, furuncles, these manifestations may be symptoms of agranulocytosis.

Occurrence of subcutaneous hemorrhages or bleeding of unclear genesis, generalized skin rash and itching, persistent nausea or vomiting, jaundice, severe epigastric pain and severe weakness require treatment cancellation.

In the event of early cessation of treatment, relapse is possible.

The appearance or deterioration of the course of endocrine ophthalmopathy is not a side effect of treatment with Mercazolil, carried out properly.

In rare cases, after the end of treatment, late hypothyroidism may occur, which is not a side effect of the drug, but is associated with inflammatory and destructive processes in the thyroid tissue that occur within the underlying disease.

Effect on the ability to drive transp. cf. and fur:

The drug may cause dizziness and other side effects that affect the ability to drive vehicles and engage in potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Form release / dosage:

Tablets, 5 mg.

Packaging:

For 30, 50 or 100 tablets in a plastic container for medicines, equipped with a lid with a control of the first opening.

Free space in the container is filled with cotton absorbent cotton.

The label is self-adhesive on the container. Container along with instructions for use in a pack of cardboard. For 10 or 50 tablets in a contour mesh package.

For 1, 2, 5 or 10 contour cell packs of 10 tablets together with instructions for use in a pack of cardboard.

For 1 or 2 outline cell packs of 50 tablets together with instructions for use in a pack of cardboard.

Storage conditions:In dry, protected from light and out of reach of children, at a temperature of 8 to 25 ° C.

Shelf life:5 years. Do not use the product after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:П N015131 / 01

Date of registration:01.07.2008 / 02.02.2016

Expiration Date:Unlimited

The owner of the registration certificate:HEALTH PHARMACEUTICAL COMPANY, LTD. HEALTH PHARMACEUTICAL COMPANY, LTD. Ukraine

Manufacturer: & nbsp

HEALTH PHARMACEUTICAL COMPANY, LTD. Ukraine

Information update date: & nbsp01.05.2018

Illustrated instructions

Instructions

Mercazolil (Mercazolil)