Mercazolil (Mercazolil)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
Read on
Active substanceThiamazoleThiamazole
Similar drugsTo uncover
  • Mercazolil
    pills inwards 
    MARBIOFARM, OJSC     Russia
  • Mercazolil
    pills inwards 
    HEALTH PHARMACEUTICAL COMPANY, LTD.     Ukraine
  • Mercazolil
    pills inwards 
    AKRIKHIN HFK, JSC     Russia
  • Tirozol®
    pills inwards 
    Merck KGaA     Germany
    • Dosage form: & nbsppills
    Composition:

    1 tablet contains:

    active substance: thiamazole in terms of 100% substance - 5 mg;

    Excipients: Lactose monohydrate 55.7 mg microcrystalline cellulose 75.8 mg Sodium carboxymethyl starch 1.4 mg Colloidal silicon dioxide 1.4 mg Calcium stearate 0.7 mg.

    Description:
    Tablets from white to white with a yellowish or creamy shade of color, flat-cylindrical, with a facet and a risk. There is an insignificant "marble".
    Pharmacotherapeutic group:Antithyroid agent
    ATX: & nbsp

    H.03.B.B   Imidazole derivatives containing sulfur

    H.03.B.B.02   Thiamazole

    Pharmacodynamics:

    Antithyroid medication; It gives thyroid hormone synthesis by blocking the enzyme peroxidase, which participates in the iodination in the thyroid thyronine to form triyod- and tetraiodothyronine reduces internal secretion of thyroxine (T4).

    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 level of triiodothyronine (T3) and T4 in blood plasma, i.e. improvement of clinical picture. Mercazolilum does not influence a thyrotoxicosis, developed owing to release of hormones after destruction of cells of a thyroid gland (after treatment by a radioiodine or at a 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.

    The duration of the single dose is almost 24 hours.

    Pharmacokinetics:
    The drug is well absorbed when taken orally, eating does not affect the amount and speed of absorption. Bioavailability - 93%. Plasma proteins are practically not bound. Concentrates in the tissue of the thyroid gland. Small amounts are found in breast milk. The volume of distribution is 0.6 l / kg.Time to reach the maximum concentration in the plasma is 30-60 minutes after taking the drug; the maximum plasma concentration reaches 1.184 μg / ml with an oral dose of 60 mg. Metabolism is carried out in the liver with the formation of inactive metabolites. The period of lunation is 5-6 hours. It is excreted from the body by the kidneys, and less than 10% is 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 given before the onset of action of radioactive iodine (within 4-6 months);
    • in exceptional cases, prolonged maintenance therapy of 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:
    • Hypersensitivity to thiamazole or thiourea derivatives;
    • agranulocytosis during previous therapy with carbimazole or thiamazole;
    • granulocytopenia (including in the anamnesis);
    • cholestasis before treatment;
    • lactation period.
    Carefully:In pregnant women; in patients with goitre 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 through the placental barrier and in the fetal blood reaches the same concentration as the mother. Therefore, during pregnancy, the drug should be used only in case of emergency in a minimally effective dose without additional administration of thyroid hormone drugs under the strict supervision of a doctor. A high dose of thiamazole can cause goiter and hypothyroidism in the fetus. Thiamazole also penetrates into breast milk and can achieve in it a concentration corresponding to the blood level of the mother. If it is necessary to continue treatment of thyrotoxicosis during breastfeeding, breast-feeding should be stopped.
    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 the thyroid function, maintenance doses of the drug are prescribed - from 2.5 to 10 mg / day (1 / 2-2 tablets) in 1 or 2 doses.

    In pregnancy, the drug is prescribed in the lowest possible doses - 2.5-1 mg / day.

    Children 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.

    Children up to 3 years of age, the drug is dissolved in water to a fine suspension, which is prepared immediately before use.

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

    In preparation for surgical treatment of thyrotoxicosis prescribe 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 reception of levothyroxine 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: prescribe 20-40 mg / cyr 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 radioactive iodine (4-6 months).

    Long-term thyrostatic maintenance therapy:

    2.5-10 mg / day with the additional intake of small doses of levothyroxine.

    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 the anamnesis: 10-20 mg / day of thiamazole and 1 g of potassium perchlorate are prescribed per day for 8-10 days before taking iodine-containing drugs.

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

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

    Side effects:

    Allergic reactions (itching, rash, hives), inhibition of myelopoiesis (agranulocytosis, granulocytopenia, thrombocytopenia), aplastic anemia, drug fever, autoimmune syndrome, hypoglycemia, generalized lymphadenopathy, sialadenopatiya, neuritis, taste disturbances, alopecia, polyneuritis, lupus syndrome, hypoprothrombinemia ( petechiae, bleeding), periarteritis, hepatitis, cholestatic jaundice, skin itching, nausea, vomiting, epigastric pain, arthralgia, myalgia, paresthesia, severe weakness, headache, headaches whirling, skin hyperpigmentation, edema, weight gain, rarely - jade.

    Subclinical and clinical hypothyroidism can develop when taking high doses of the drug. An enlargement of the thyroid gland may also occur, which is associated with an increase in the TSH content in the blood.

    Overdose:

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

    Treatment: gastric lavage, Activated carbon, symptomatic therapy.

    Chronic overdose of thiamazole 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 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.

    Leukogen and folic acid with simultaneous use with thiamazole reduce the risk of developing leukopenia. Gentamicin strengthens the antithyroid effect of thiamazole.

    In patients receiving thiamazole about thyrotoxicosis, after reaching the euthyroid state, it may be necessary to reduce the intake of cardiac glycosides (digoxin and digitoxin), aminophylline, and increase the dose of warfarin and other anticoagulants, coumarin and indanedione (pharmacodynamic interaction).

    Special instructions:

    During treatment, it is necessary to carry out control of peripheral blood (with an interval of 1-2 weeks during the selection of the dose and once a month - during the period of 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,since with prolonged use it is possible to increase the goiter and even more compression of the trachea. It is necessary to carry out careful monitoring of the patient (control of the level of TSH, tracheal lumen).

    The patient, who is appointed Merkazolil, should be warned about the necessity of compulsory treatment to a doctor when fever, chills, cough, sore throats, inflammation of the mucous membrane of the mouth, furuncles, tk. 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.

    Form release / dosage:
    Tablets 5 mg.
    Packaging:

    10 tablets per contour cell pack.

    5 or 10 contour mesh packages together with instructions for use in a pack of cardboard.

    Storage conditions:
    List B. In a dry, the dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.
    Shelf life:
    5 years. Do not use the drug after the expiration date.
    Terms of leave from pharmacies:On prescription
    Registration number:P N001150 / 01
    Date of registration:31.03.2008 / 08.02.2017
    Expiration Date:Unlimited
    The owner of the registration certificate:AKRIKHIN HFK, JSC AKRIKHIN HFK, JSC Russia
    Manufacturer: & nbsp
    Representation: & nbspAKRIKHIN OJSC AKRIKHIN OJSC Russia
    Information update date: & nbsp01.05.2018
    Illustrated instructions
      Instructions
      Up