Mercazolil (Mercazolil)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceThiamazoleThiamazole
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  • 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:

    For one tablet:

    thiamazole 0.005 g,

    Excipients: Laktozy.monogidrat (milk sugar) - 0.094 g, potato starch - 0.098 g talc - 0.002 g Calcium stearate Monohydrate - 0.001 g

    Description:Round tablets of flat-cylindrical shape with a bevel; from white to white with a yellowish or kremovatym shade of color.
    Pharmacotherapeutic group:Antithyroid agent
    ATX: & nbsp

    H.03.B.B   Imidazole derivatives containing sulfur

    H.03.B.B.02   Thiamazole

    Pharmacodynamics:

    Antithyroid, drug; gives thyroid hormone synthesis, inhibits yodidperoksidazu participating in tironina- iodination in the thyroid gland and to form monoyodtironina diiodothyronine, then triyod- tetrayodgironina and reduces the 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 concentration of triiodothyronine (T3) and T4 in blood plasma, that is, an improvement in the 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).

    Reduces the basal metabolism, accelerates the excretion of the thyroid gland of iodides, increases the reciprocal activation of the synthesis and secretion of the thyroid-stimulating hormone (TSH) by the pituitary gland, which is accompanied by some hyperplasia of the thyroid gland.

    The rate of onset of the effect depends on the initial concentration of triiodothyronine (T3) and thyroxine, but usually the hormone concentration is normalized after 3 weeks of continuous use of the drug at 30 mg or 4 weeks after taking a dose of 40 mg. After 5 days after the cancellation, the concentration of hormones may rise again.

    Pharmacokinetics:Mercazolil is well absorbed when administered orally, eating does not affect the amount and speed of absorption. Bioavailability - 93%. Time to reach the maximum concentration in the plasma is 30-60 minutes after taking the drug, the maximum concentration (Cmax) reaches 1.184 μg / ml with oral administration.Virtually does not bind to plasma proteins. 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 is carried out in the liver with the formation of inactive metabolites. The half-life (T 1/2) 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 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, autonomic adenomas or thyrotoxicosis in anamnesis.
    Contraindications:
    Hypersensitivity to thiamazole or thiourea derivatives; agranulocytosis during previous therapycarbimazole or thiamazole; severe leukopenia or granulocytopenia (including in history); cholestasis before treatment; lactation period.
    Carefully:
    Pregnancy, goiter of very large size with narrowing of the trachea (only short-term treatment during the preparation for surgery), liver failure; in patients receiving anticoagulants, cardiac glycosides, and aminophylline.
    Pregnancy and lactation:

    Contraindicated in pregnancy and during breastfeeding. Thiamazole penetrates the placental barrier. Application: after the first trimester of pregnancy is associated with the threat of development of hypothyroidism in the fetus.

    Excreted in breast milk.

    Dosing and Administration:

    Inside, after eating. 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 the onset of remission (after 3-6 weeks), the daily dose is reduced every 5-10 days by 5-10 mg and gradually selected the minimum dose (5 mg once a day, every other day or every 3 days),which are prescribed until a persistent therapeutic effect is obtained.

    After the normalization of the thyroid function, maintenance doses of the drug are prescribed - 2.5 to 10 mg / day (1 / 2-2 tablets) in 1 or 2 doses.

    Maximum doses for adults: single dose - 10 mg, daily - 40 mg. Pregnant women - at the lowest possible doses - 2.5-10 mg / day.

    Children - 0.3-0.5 mg / kg body weight / day in 3 doses, supporting doses for children - 0.2-0.3 mg / kg body weight / 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 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 reception of levothyroxine is recommended. Stop taking thiamazole the day before the surgery.

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

    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:

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

    On the part of the organs of the gastrointestinal tract: hepatitis, cholestatic jaundice, nausea, vomiting, epigastric pain.

    On the part of the cardiovascular system and hematopoiesis system: depression of myelopoiesis (agranulocytosis, granulocytopenia, thrombocytopenia), aplastic anemia, hypoprothrombinemia (petechiae, bleeding).

    From the nervous system and sense organs: neuritis (including polyneuritis), taste disorders, paresthesia, severe weakness, headache, dizziness.

    Other: drug fever, insulin autoimmune syndrome, generalized lymphadenopathy, sialadenopathy, alopecia, lupus-like syndrome, periarteritis, arthralgia, myalgia, hyperpigmentation of the skin, peripheral edema, weight gain; rarely - jade.

    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.

    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 stimulation of the central nervous system.

    Treatment: gastric lavage, Activated carbon, symptomatic therapy.

    Long-term use of excessive doses (chronic overdose) in addition to hyperplasia of the thyroid glandleads to the development of hypothyroidism; In this case, treatment with the drug is stopped.

    Interaction:

    Preparations of lithium, beta-blockers, reserpine, amiodarone increase the effect of Mercazolil (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 a large amount of iodine) weakens the effect.

    Leukogen and folic acid with simultaneous use with thiamazole reduce the risk of developing leukopenia.

    Gentamicin increases the antithyroid effect of thiamazole.

    In patients receiving thiamazole about thyrotoxicosis, after reaching the euthyroid state, there may be a need to reduce the intake of cardiac glycosides, aminophylline, as well as an increase in the intake of doses of warfarin and other anticoagulants.

    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 sodium, as long-term use may increase the goiter and even more compression of the trachea. It is necessary to conduct careful monitoring of the patient (monitoring the concentration 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 of 5 mg.
    Packaging:

    For 10 or 20 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil.

    For 50 or 100 tablets in a jar of polymer materials.

    Each bank or 5 contour packs of 10 tablets, or 2 contour packs of 20 tablets together with instructions for use, are placed in a pack of cardboard for consumer containers.

    Storage conditions:

    In a dry, protected from light place at a temperature of no higher than 25 ° C.

    Keep out of the reach of children.

    Shelf life:2 years. Do not use after the expiration date.
    Terms of leave from pharmacies:On prescription
    Registration number:LP-001264
    Date of registration:24.11.2011
    Expiration Date:24.11.2016
    The owner of the registration certificate:MARBIOFARM, OJSC MARBIOFARM, OJSC Russia
    Manufacturer: & nbsp
    Representation: & nbspMARBIOFARM, OJSCMARBIOFARM, OJSC
    Information update date: & nbsp29.04.2018
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