Tyrosol minimum dosage. Tyrosol instructions for use, contraindications, side effects, reviews. Treatment before radioactive iodine therapy

Side effects after taking the medication

What reactions may occur after taking Tyrozol tablets? The side effects of this drug are described in each instruction. We will talk about them in more detail in this section of the article.

In most cases, the drug mentioned is tolerated quite well by patients. However, it should be noted that sometimes while taking the medication, people may develop allergic reactions on the skin (in the form of itching, redness and rashes) and arthralgia, in addition, in rare cases, dizziness, weakness and vomiting may occur.

What other negative consequences can be caused by the drug "Tirozol"? Side effects and reviews of this medication are presented in this section of the article. So, we are talking about such unpleasant reactions:

• generalized lymphadenopathy;
• thrombocytopenia;
• neuritis;
• temperature increase;
• cholestatic jaundice, toxic hepatitis and arthralgia (develop very slowly);
• autoimmune syndrome together with hypoglycemia;
• pronounced enlargement of the salivary glands;
• pancytopenia;
• lupus-like reaction;
• changes in taste sensations of a reversible nature;
• agranulocytosis (manifests immediately or several months after the start of therapy, which leads to the need to discontinue the drug);
• polyneuropathy.

According to reviews from those patients who are taking or have ever taken this medication, it can easily cause weight gain. As a rule, such a negative effect occurs after taking large dosages of the drug.

Side effects

Taking tyrosine as a supplement can cause a number of unpleasant side effects

People with an overactive thyroid gland should take this substance with particular caution.

1. Anxiety.

Unexplained anxiety may be a side effect of taking tyrosine. This amino acid affects cognitive abilities and also acts as a stimulant of the central nervous system. And taking a pharmaceutical analogue of tyrosine can increase the frequency of impulses in the brain several times. An increased sense of fear and panic is a possible result of regular use of the substance.

1. Digestive disorder.

Tyrosine in dietary supplement form has been shown to benefit the health of the digestive system. First of all, its not the best effect is felt by the mucous membrane of the digestive tract. Irritation from the amino acid causes stomach discomfort. If there is blood in your stool, you should immediately stop taking tyrosine and consult a doctor.

After the “chemical” tyrosine enters the digestive system, reflux can develop. Due to the effects of the amino acid, the sphincter in the digestive canal relaxes and allows stomach contents back into the esophagus, causing heartburn and other discomfort.

1. Migraine.

Migraine in severe and prolonged form is one of the side effects of long-term use of the amino acid. In this case, you should stop taking the drug containing tyrosine and replenish its reserves exclusively from natural foods.

1. Tachycardia.

Chest fluttering can be caused by tyrosine, which, by stimulating the central nervous system, speeds up and intensifies the heartbeat.

1. Nervousness.

Influencing the nervous system, it can cause the development of nervousness, which arises seemingly for no reason. In fact, there is a reason - the body does not accept a drug containing an amino acid.

Instructions for use

pharmachologic effect

Antithyroid drug; disrupts the synthesis of thyroid hormones, blocks the peroxidase enzyme involved in the iodination of thyronine in the thyroid gland with the formation of monoiodothyronine and diiodothyronine, and then triiodo- and tetraiodothyronine, reduces the internal secretion of T4.

Reduces basal metabolism, accelerates the removal of iodides from the thyroid gland, increases reciprocal activation of the synthesis and secretion of 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 T3 and T4, but usually the concentration of hormones is normalized after 7 weeks of constant administration of the drug at 30 mg or after 4 weeks when using a dose of 40 mg. 5 days after discontinuation, the concentration of hormones may increase again.

Indications

Thyrotoxicosis (diffuse struma). Preoperative period, for preliminary and intermediate treatment in addition to radioiodine therapy, postoperative relapses of thyrotoxicosis, nodular goiter.

Contraindications

Hypersensitivity, severe leukopenia or granulocytopenia (including

history), lactation period. With caution. Pregnancy, very large goiter with narrowing of the trachea (only short-term treatment in preparation for surgery), liver failure.

Side effects

Аллергические реакции (сыпь, крапивница), подавление миелопоэза (агранулоцитоз, гранулоцитопения, тромбоцитопения), апластическая анемия, лекарственная лихорадка, инсулиновый аутоиммунный синдром, генерализованная лимфоаденопатия, сиаладенопатия, неврит, нарушения вкуса, алопеция, полиневрит, волчаночноподобный синдром, гипопротромбинемия (петехии, кровотечения ), periarteritis, hepatitis, cholestatic jaundice, skin itching, nausea, vomiting, epigastric pain, arthralgia, myalgia, paresthesia, severe weakness, headache, dizziness, skin hyperpigmentation, edema, rarely - nephritis.

Application and dosage

Inside, after eating. For mild and moderate forms of thyrotoxicosis - 5 mg 3-4 times a day. After the onset of remission (after 3-6 weeks), the daily dose is reduced every 5-10 days by 5-10 mg and the minimum doses are gradually selected (5 mg once a day, every other day or once every 3 days), which are prescribed until obtaining a lasting therapeutic effect.

In severe forms of thyrotoxicosis - 40-60 mg/day in 3-4 doses, after improvement of the condition 5-20 mg/day. Course – 1-1.5 years.

Higher doses for adults: single – 10 mg, daily – 60 mg. Pregnant women - in the lowest possible doses - 2.5-10 mg; children – 0.3-0.5 mg/kg, maintenance doses for children – 0.2-0.3 mg/kg; maintenance doses – once, in the morning after breakfast.

special instructions

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

Large struma of the thyroid gland with narrowing of the trachea should be treated briefly, because with long-term treatment, goiter growth is possible.

A patient who is prescribed thiamazole should be warned about the need to consult a doctor if fever, chills, cough, sore throat, inflammation of the oral mucosa, or boils occur, because these manifestations may be symptoms of agranulocytosis.

The appearance during treatment of subcutaneous hemorrhages or bleeding of unknown origin, generalized skin rash and itching, persistent nausea or vomiting, jaundice, severe epigastric pain and severe weakness requires discontinuation of the drug.

If treatment is stopped early, relapse is possible.

Interaction

Li+ drugs, beta-blockers, reserpine, amiodarone increase the effect of thiamazole (its dose adjustment is required).

Sulfonamides and metamizole sodium increase the risk of developing leukopenia.

Myelotoxic drugs increase the manifestations of hematotoxicity of the drug.

Iodine deficiency increases, and excess (for example, arising from taking drugs containing large amounts of iodine) weakens the effect.

Instructions for use of Tyrosol

The antithyroid drug (lowering the level of thyroid hormones) Thyrozol is used to treat thyrotoxicosis (a disease in which the number of thyroid hormones increases). This drug disrupts the synthesis process in the thyroid gland by blocking the enzyme peroxidase, which is involved in the iodination of the hormone thyronine with the formation of tetraiodothyronine (T4) and triiodothyronine (T3).

Composition and release form

The drug is available in the form of oral round tablets, coated with a yellow or orange film enteric coating, convex on both sides. The medicine is packaged in blisters of 10 pieces. Each tablet of the drug contains 10 or 5 mg of the active ingredient Thiamazole and several auxiliary components. The composition of the drug is indicated in the table:

Pharmacological properties

An antithyroid drug interferes with the synthesis of thyroid hormones. The medicine is effective in the symptomatic treatment of thyrotoxicosis, except in cases where the disease appears as a result of the release of hormones after the destruction of thyroid cells due to thyroiditis (inflammatory lesion) or after treatment with radioactive iodine.

Tyrosol does not affect the process of hormone release from thyroid follicles. This explains the incubation period of varying lengths, which may precede the stabilization of T3 and T4 levels in the blood plasma. The medicine accelerates the excretion of iodides, reduces metabolism, increases the activation of secretion and synthesis of TSH (thyroid-stimulating hormone) by the pituitary gland, which is accompanied by hyperplasia (enlargement of cells) of the thyroid gland.

Pharmacokinetics. After taking the drug orally, the substance Thiamazole is quickly absorbed into the gastrointestinal tract (gastrointestinal tract). The half-life is 3 hours and is prolonged in liver disease. Thiamazole does not bind to plasma proteins; accumulation (cumulation) occurs only in the thyroid gland. Metabolized slowly in the liver and kidneys. Excretion (removal) occurs with bile and urine (during the day - 70% of the substance, with 12% unchanged). The duration of action of the medicine after a single use is almost a day.

Is Tyrosol a hormonal drug or not?

Often patients who have been prescribed to take Tyrozol tablets are interested in whether this medicine is hormonal or not. The instructions for use of the product contain information according to which this medicinal product does not include hormones or their synthetic analogues. The medication itself can affect T3, T4 and TSH of the thyroid gland, but it is not a hormonal agent.

• during preparatory therapy with radioactive iodine;
• for the prevention of thyrotoxicosis, when the patient is prescribed iodine preparations (including iodine-containing radiocontrast agents);
• when preparing a patient for surgery on the thyroid gland;
• during the latent period of radioactive iodine action (for 6 months);
• in exceptional cases of treatment of thyrotoxicosis, when, for individual reasons, radical treatment cannot be carried out.

The drug Tyrosol instructions for use

If a doctor prescribes this drug to a patient, he is obliged to advise the patient about the specifics of its use. As a rule, the medicine is taken only after eating. At the very beginning of therapy, experts recommend using the medication at a strictly defined time.

During the treatment of thyrotoxicosis, patients are usually prescribed 2-4 tablets of the drug per day (10 mg each). In this case, the duration of therapy should be at least 6 weeks.

After thyroid function has been fully or partially restored, doctors recommend switching to a maintenance dose. In this case, patients need to take 5-20 mg of medication per day (simultaneously with the drug Levothyroxine).

During the period of preparation for therapy of thyrotoxicosis with radioactive iodine, as well as for surgery, patients are prescribed a similar dosage as in the usual treatment of the disease (up to the euthyroid state). After this, patients are additionally prescribed the medication Levothyroxine, beta-blockers and iodine preparations.

When treatment is carried out before exposure to radioactive iodine, patients are prescribed a dosage equal to 1-4 tablets (5 mg each). This medication should be taken for a month.

During long-term therapy (maintenance), the dosage of the medication, according to the instructions, ranges from 1.25 to 10 mg per day. In this case, a small dose of the drug Levothyroxine is prescribed at the same time.

For preventive purposes, the development of thyrotoxicosis during the period of taking iodine preparations, the drug “Tyrozol” is very effective in the following dosage: from 10 to 20 mg per day.

As a rule, this drug is prescribed to children based on body weight. Typically, the initial dosage of the drug is prescribed in an amount of 0.3-0.5 mg. If maintenance therapy is necessary, the child should take 0.2-0.3 mg of the drug. In this case, Levothyroxine is prescribed only in case of urgent need.

The maximum single dose for adults is 10 ml, and the daily dose is 60 ml. The duration of taking the medication we are considering can be increased to 1.5-2 years (depending on the course of the disease). If therapy was interrupted, then until the patient recovers completely, he may develop a relapse of the disease.

In rare cases, after stopping the medication, a person may experience late hypothyroidism, which is not a side effect, but is associated only with inflammatory and destructive processes occurring in the tissues of the thyroid gland.

pharmachologic effect

Tyrosol tablets are positioned in the instructions for use as an antithyroid medication that disrupts the process of formation and release of thyroid hormones.

The pharmacological effect of the drug is due to the main substance included in its composition.

Thyrozol tablets block peroxidase, an enzyme that takes part in the iodization of the thyroid gland and promotes the formation of the hormones T3 and T4.

As a result of the use of the medication, symptomatic treatment of thyrotoxicosis is performed.

This effect will not work if the development of the disease and the release of hormones occurred due to the destruction of gland tissue due to thyroiditis or the use of radioactive iodine.

When treated with Tyrozol, the following properties are achieved:

• the level of T3 and T4 in the blood is normalized,
• the excretion of iodides from the thyroid gland is accelerated,
• reciprocal activation of TSH synthesis increases,
• does not affect the release of synthesized thyronones from thyroid follicles.

After consuming the medication, the active component is quickly absorbed, reaching its maximum in the blood within 30-90 minutes.

After 3-6 hours, the amount of the active component in the body is reduced by half.

Indications for use

The abstract describes the indications for use, which are limited to the list:

• thyrotoxicosis,
• preparation for surgical treatment for thyrotoxicosis,
• preparation for treatment with radioactive iodine,
• prevention of drug toxicosis due to excessive use of iodine preparations.

The speed of action of the medication is different for each patient.

This is due to the fact that a latent period of varying duration occurs at the beginning of using the medication, after which a noticeable result occurs and the symptoms of thyrotoxicosis disappear.

Contraindications

For the drug Tyrozol, contraindications are limited to the list:

• high sensitivity to the active substance,
• agranulocytosis, leukopenia, provoked by drugs containing thiamazole,
• granulocytopenia, including after normalization of indicators,
• cholestasis,
• treatment with Tyrosol with Levothyroxine during pregnancy,
• child's age up to 3 years.

With extreme caution and only under the supervision of a doctor, the medicine is prescribed for excessive enlargement of the thyroid gland to a very large size with narrowing of the trachea; usually such therapy is short-term. In case of liver diseases, liver failure, the effect of the drug and the effect on the organ may be negative, so you should first consult your doctor

In case of liver diseases or liver failure, the effect of the drug and the effect on the organ may be negative, so you should first consult with your doctor.

Tyrosine Supplements and Dosage Information

Tyrosine is available in powder form, capsule form, and is also found in some supplements for athletes. What are the reasons for taking a daily tyrosine supplement? Some of the most common reasons for taking tyrosine are to manage mood and symptoms of depression. And also increase energy and support weight loss.

Another reason to use a tyrosine supplement is to treat an inherited disease called phenylketonuria (PKU). In this condition, the amino acid phenylalanine cannot be properly converted into tyrosine, resulting in low levels. For people with PKU, it is best to get tyrosine from food and supplements. But there is very little phenylalanine in supplements because it cannot be artificially processed. Four to six grams of tyrosine per day is usually recommended for the treatment of PKU. Pregnant women with PKU should consume even more, up to 7.6g per day.

How much tyrosine should you take?

In most studies, adults safely took 100 to 150 mg per kg of body weight, which is equivalent to approximately 7 g per day for an adult. In some situations, higher dosages are recommended. For example, in stressful situations, to improve mental abilities, it is better to take 300 mg per 1 kg of body weight.

To increase alertness and prevent fatigue, it is recommended to divide the dose and take it in several stages. Depending on your health condition, your dosage may be individual. Therefore, it is better to start with a low dose and increase it as needed.

When should you take tyrosine?

For greater benefit, tyrosine should be taken on an empty stomach before meals. Because eating other amino acids may interfere with its absorption. Tyrosine may stimulate and potentially reduce sleepiness. Based on this, it is best to take it in the morning, and not in the evening before bed, and especially in large quantities.

How long does it take for tyrosine to take effect?

The effects of tyrosine in supplements can be felt in as little as 30-60 minutes, depending on the dosage and timing of the meal. Consuming this amino acid on an empty stomach has a faster effect.

Side effects

Every patient should be warned about them. When taking Tyrozol, side effects do not always occur, but there is a possibility of their occurrence, and this is what the patient may encounter:

• Fever.
• Cholestatic jaundice.
• Generalized lymphadenopathy.
• Agranulocytosis. Signs of this pathology may appear even weeks or months after the start of drug treatment.
• Enlarged salivary glands.
• Polyneuropathy.
• Thrombocytopenia.
• Pancytopenia.
• Generalized skin rashes.
• Vomit.
• Hirata disease accompanied by hypoglycemia.
• Changing taste preferences.
• Lupus-like syndrome.
• Weakness.
• Intensive weight gain.
• Neuritis.
• Dizziness.
• Alopecia.
• Manifestations of an allergic reaction (rash, itching, redness).
• Slowly progressive arthralgia.
• Toxic hepatitis.

Of course, every side effect of Tyrozol is fraught with its own, no less serious consequences.

That is why it is important to constantly be monitored by an endocrinologist during treatment, so that if something happens, you can quickly stop the drug and eliminate problems that have arisen but have not yet developed.

Taking the drug as part of preparation

As mentioned earlier, it can be appointed for these purposes. Typically, Tyrosol 10 mg is prescribed to prepare a patient for surgery. The instructions for use state that the daily dosage is from 20 to 40 mg - it is necessary to achieve a euthyroid state of the thyroid gland. In parallel, levothyroxine is also indicated.

In order to reduce the time it takes to prepare, the patient is also prescribed beta-blockers and iodine preparations.

You also need to drink Tyrosol in other cases. Namely, when the patient is preparing for therapy that involves the use of radioactive iodine. The dosage is the same – from 20 to 40 mg.

As part of long-term maintenance treatment, this drug is also taken, but in smaller quantities. Daily doses are 10, 2.5 or 1.25 mg. In this case, “Tyrozol” containing 5 mg of active substance per tablet is convenient - it is more convenient to divide it. At the same time, the notorious levothyroxine is also taken. In such cases, therapy lasts about one and a half to two years.

• Prevention of thyrotoxicosis.
• Treatment of autonomous adenomas.
• Latent thyrotoxicosis.
• History of this disease.

In such cases, it is necessary to drink potassium perchlorate in an amount of 1000 mg in parallel. And always within 8-10 days that precede taking medications containing iodine.

What about age guidelines? The instructions for use of the drug "Tirozol" say that patients aged 3 to 17 years are advised to take a daily dose of 0.3-0.5 mg per 1 kg of weight. This amount should be divided into 2-3 doses.

If a child weighs more than 80 kg, then a maximum of 40 mg of the drug can be taken per day.

The maintenance dosage is 0.2-0.3 mg per 1 kg of weight. Therapy may be supplemented with levothyroxine.

Special instructions are contained in the instructions for use of Tyrozol tablets for pregnant women. They need to take minimal doses of the drug. The recommended single dose is 2.5 mg. And the maximum daily dosage is 10 mg.

But patients with insufficient liver function should take the drug even more carefully.

What is it and what is it eaten with?

L-tyrosine is a precursor to the neurotransmitter dopamine. This is what determines its effect on mood and nervous state. With a lack of dopamine, we quickly get tired and experience decreased motivation. In addition, it is also a precursor of the adrenal hormones - adrenaline and norepinephrine.

We usually get L-tyrosine from protein foods. Most of it is found in chicken, turkey, seafood, avocados, almonds, milk, fish, soybeans, sesame seeds, beans, bananas, and pumpkin seeds. In addition, tyrosine can be synthesized in the body independently from another (essential) amino acid - phenylalanine.

special instructions

If the thyroid gland is significantly enlarged, narrowing the lumen of the trachea, Tyrozol is prescribed for a short time in combination with Levothyroxine sodium, since long-term treatment can lead to an increase in goiter and even greater compression of the trachea. The condition of patients requires careful monitoring, including monitoring of the tracheal lumen and the level of thyroid-stimulating hormone.

During use of the drug, it is necessary to regularly monitor the peripheral blood picture.

Therapy with thiamazole and thiourea derivatives can lead to a decrease in the sensitivity of thyroid tissue to radiation therapy.

If symptoms of agranulocytosis suddenly appear (sore throat, difficulty swallowing, increased body temperature, signs of stomatitis, furunculosis), you should immediately discontinue Tirozol and consult a doctor for advice.

In cases of subcutaneous hemorrhages or bleeding of unknown etiology, vomiting or persistent nausea, generalized skin rash, itching, jaundice, severe epigastric pain, severe weakness, Tirozol is discontinued.

If therapy is stopped early, a relapse of the disease may occur.

Worsening of the course/appearance of endocrine ophthalmopathy is not a side effect of adequate treatment.

In rare cases, after stopping use of Tyrozol, late hypothyroidism may develop. It is not a side effect, but is associated with destructive and inflammatory processes in the tissues of the thyroid gland, which occur as part of the underlying disease.

Use in childhood

For liver dysfunction

In case of liver failure, the drug is prescribed in the minimum effective dose under close medical supervision.

During pregnancy and lactation

Untreated hyperthyroidism during pregnancy can cause serious complications, including fetal malformations and premature birth. In turn, hypothyroidism, formed as a result of the administration of inadequate doses of Tyrozol, can lead to miscarriage.

A characteristic feature of thiamazole is its penetration through the placental barrier, after which a drug concentration similar to that of the mother is observed in the fetal blood. For this reason, the prescription of Tyrosol during pregnancy can be justified only in extreme cases, after a full assessment of the benefits/risks of its use for the mother/fetus, in minimal effective daily dosages (up to 10 mg) and without parallel use of levothyroxine sodium.

Taking high doses of thiamazole by a pregnant woman can lead to the formation of hypothyroidism and goiter in the fetus, as well as to a decrease in the child’s body weight at birth.

During breastfeeding, therapy for thyrotoxicosis in the mother can be continued in minimal dosages, since the concentration of thiamazole in breast milk corresponds to its content in the mother’s blood and can cause the development of hypothyroidism in the newborn. Taking Tyrosol by nursing women requires monitoring the functionality of the thyroid gland in newborns.

1 tablet may contain 5 mg or 10 mg thiamazole .

Additionally (together with the shell): sodium carboxymethyl starch, colloidal silicon dioxide, lactose monohydrate, hypromellose 2910/15, magnesium stearate, cellulose powder, talc, corn starch, dimethicone 100, titanium dioxide, macrogol 400, yellow iron oxide (red iron oxide for tablets 10 mg).

Release form

Tyrosol is produced in the form of tablets, 10 pieces in a blister, 2 or 5 blisters (20 or 50 tablets) in a cardboard box.

pharmachologic effect

Antithyroid (disturbs the production of thyroid hormones).

Pharmacodynamics and pharmacokinetics

Tyrosol is an antithyroid medication containing as an active ingredient thiamazole , which disrupts processes hormonal synthesis in the thyroid gland by blocking peroxidases participating in iodization of thyronine with the formation And tetraiodothyronine . This property of the drug makes it possible to carry out symptomatic treatment thyrotoxicosis , in addition to cases of the formation of this pathology due to the release of hormones due to the destruction of the cellular structure of the thyroid gland (with or after use radioactive iodine ). Wherein thiamazole does not affect the processes of release from the follicles of the thyroid gland synthesized thyronines , which explains the different duration of the latent period preceding the normalization of plasma levels of T3 and T4, which is an indicator of improvement in the clinical picture of the pathological process.

Effects thiamazole in the thyroid gland are characterized by a decrease in basal metabolism, acceleration of excretion iodides , as well as an increase in reciprocal activation of synthesis and secretion processes thyroid-stimulating hormone pituitary gland, which may be accompanied by the development hyperplasia of the thyroid gland .

Single dose thiamazole continues to operate for almost 24 hours.

Oral administration thiamazole leads to rapid and almost complete absorption from the gastrointestinal tract. The time period for the drug to reach plasma Cmax varies within 0.4-1.2 hours. Binding to plasma proteins is negligible. Cumulation thiamazole occurs in the thyroid gland, where it undergoes primary metabolic transformations. A certain amount of the drug is found in the milk of nursing mothers.

T1/2 thiamazole takes from 3 to 6 hours and extends with . Kinetics dependencies thiamazole from the functionality of the thyroid gland was not detected. Further metabolism occurs in the liver and kidneys. Excretion occurs via bile and urine, with approximately 70% being excreted by the kidneys throughout the day. thiamazole , of which 7-12% falls to the unchanged drug.

Indications for use

The drug Tyrosol is indicated for the following purposes:

• for therapy ;
• during the preparation of the patient for surgical intervention on the thyroid gland regarding thyrotoxicosis ;
• while preparing the patient for treatment thyrotoxicosis using radioactive iodine (radiiodine);
• in the latent period of therapy radioactive iodine (assigned before the start of the action radioiodine for 4-6 months);
• for prevention thyrotoxicosis in cases where medications are prescribed to a patient (including radiopaque iodine-containing agents ), with autonomous , latent thyrotoxicosis or thyrotoxicosis in the anamnesis;
• for the purpose of long-term maintenance treatment thyrotoxicosis when the general health of the patient or other individual reasons do not allow radical therapy (in exceptional cases).

Contraindications

The use of Tyrosol is absolutely contraindicated for:

• agranulocytosis during the period of previous treatment with the use of thiamazole or carbimazole ;
• personal hypersensitivity To thiamazole , auxiliary ingredients of tablets, as well as derivatives thiourea ;
• granulocytopenia (including indications of it in the anamnesis);
• parallel reception levothyroxine sodium during pregnancy;
• cholestasis observed before starting therapy;
• pathologies associated with sugar intolerance ;
• under the age of 3 years.

Relative contraindications to taking Tyrozol are:

• liver failure ;
• formed significant size;
• narrowing of the trachea (only short-term therapy is possible in the preoperative period).

Side effects of Tyrosol

During treatment, the following side effects of Tyrosol were sometimes noted:

• temperature increase;
• (symptoms of this pathology may appear even several weeks or even months after the start of therapy and cause the need to discontinue treatment);
• cholestatic jaundice ;
• generalized lymphadenopathy ;
• enlarged salivary glands;
• thrombocytopenia;
• polyneuropathy ;
• generalized skin rashes;
• pancytopenia ;
• vomiting;
• Hirata disease with hypoglycemia ;
• lupus-like syndrome ;
• change in taste;
• weakness;
• weight gain;
• neuritis ;
• allergic skin manifestations ( redness , , rashes );
• development ;
• toxic ;
• arthralgia (slowly progressive and without clinical manifestations ).

Tyrosol, instructions for use (Method and dosage)

Instructions for use of Tyrosol involve oral (oral) administration of the drug tablets after meals (without chewing) with a sufficient volume of water.

The recommended daily dosage of Tyrosol can be taken once or 2-3 times. At the beginning of the therapeutic course, single doses of the drug during the day should be taken strictly at the same time. The maintenance dosage is indicated to be taken once a day, immediately after breakfast.

For treatment thyrotoxicosis , depending on the severity of the observed symptoms of the disease, 20-40 mg of Tyrosol is prescribed per day for 3-6 weeks. When the functional functioning of the thyroid gland normalizes, usually observed after 3-8 weeks of treatment, the patient is transferred to a maintenance daily dose varying between 5-20 mg. From this point on, it is additionally recommended to take levothyroxine .

Preparation for surgery for thyrotoxicosis requires a course of taking Tyrosol tablets in a daily dose of 20-40 mg, until the thyroid gland reaches euthyroid state . From this point on, it is additionally recommended to take levothyroxine . To shorten the time period of the preoperative preparatory process, the patient is given a parallel appointment iodine preparations And beta blockers .

When preparing the patient for therapy thyrotoxicosis using radioactive iodine It is recommended to take 20-40 mg of Tyrosol daily until the thyroid gland reaches euthyroid state .

Taking Tyrosol in latent period carrying out treatment radioactive iodine , depending on the severity of the disease, is carried out in a daily dose of 5-20 mg, before the onset of action radioiodine , as a rule, for 4-6 months.

Long-term maintenance thyrostatic treatment can take place in daily doses of 1.25 mg; 2.5 mg or 10 mg, with parallel administration levothyroxine in small doses. Therapy thyrotoxicosis usually takes 1.5-2 years.

For the purpose of prevention thyrotoxicosis when received by the patient iodine preparations (including ) in the presence of autonomous adenoma , latent thyrotoxicosis or instructions for thyrotoxicosis history, prescribe 10-20 mg of Tyrosol, together with 1000 mg potassium perchlorate , at 24 hours for 8-10 days preceding the dose iodine-containing drugs .

The minimum permissible age for prescribing Tyrozol is 3 years. Patients aged 3-17 years are advised to take Tyrosol daily at an initial dose of 0.3-0.5 mg per kilogram of weight, divided into 2-3 equal doses. Adolescents weighing more than 80 kg can take a maximum of 40 mg of the drug per day. The maintenance dosage varies around 0.2-0.3 mg per kilogram of weight. If necessary, therapy is supplemented levothyroxine .

When prescribing Tyrozol to pregnant women, they try to use minimal doses of the drug. The recommended single dose for pregnant women is 2.5 mg; The daily dosage is 10 mg.

At liver failure They practice prescribing minimally effective doses of Tyrosol under constant medical supervision.

To prepare the patient for surgery for thyrotoxicosis , therapy using Tyrozol continues until the thyroid gland reaches euthyroid state , as a rule, for 3-4 weeks (sometimes longer) until the planned day of surgery and ends the day before the operation.

Overdose

In case of prolonged use thiamazole in high dosages it is possible to form clinical And subclinical , and goitre due to increased TSH levels. These negative effects can be avoided by additionally prescribing the patient levothyroxine sodium or by reducing the dose thiamazole before reaching the thyroid gland euthyroid states . As a rule, when therapy is discontinued thiamazole There is an independent restoration of normal functioning of the thyroid gland.

When taking ultra-high doses thiamazole , at a level of 120 mg per 24 hours, development may be observed myelotoxic phenomena . Therefore, taking the drug in such doses is allowed only if there are special indications ( thyrotoxic crisis , very severe course of the disease).

As a treatment for overdose conditions thiamazole cancellation of the ongoing treatment with its use is indicated, cleaning the gastrointestinal tract and further relief of negative symptoms with adequate medications. If necessary, transfer the patient to take an antithyroid drug from another group.

Interaction

In case of use thiamazole after using high quantities iodine-containing radiocontrast agents its effectiveness may be reduced.

Iodine deficiency in the thyroid gland increases the effect thiamazole .

In case of sudden appearance during treatment with Tyrozol elevated body temperature , difficulty swallowing , sore throat , signs furunculosis or (possible symptoms ) it is necessary to interrupt therapy and consult a doctor immediately.

If detected while taking Tyrosol or subcutaneous hemorrhages unknown origin, permanent nausea or vomiting , generalized rash and/or itching skin, expressed epigastric pain , severe weakness, jaundice treatment should be discontinued.

Premature cessation of Tyrozol therapy may cause relapse diseases.

In case of correct treatment, the occurrence or worsening of endocrine ophthalmopathy is not associated with the side effects of Tyrosol.

In isolated cases, after completion of therapy with Tyrozol, the occurrence of late hypothyroidism , which is not a side effect of therapy, but is associated with destructive and inflammatory processes in the tissues of the thyroid gland, characteristic of the underlying disease.

Analogs

Analogs of Tyrosol can be divided into two groups; these are hormonal drugs that include thyroid hormones or their synthetic analogues (mostly levothyroxine sodium ): , Bagotirox , , L-Tirok , Tiro-4 , and drugs that affect the synthesis and/or metabolism of thyroid hormones: , , Microiodide , Thiamazole , Metizol , Propycyl .

Propicil or Tyrosol?

When considering these two analogue drugs, it is worth noting that although they contain different active ingredients ( thiamazole for Tyrosol and propylthiouracil for ), but have a fairly similar mechanism of action in relation to the functionality of the thyroid gland. You can also trace similar contraindications and side effects of both drugs. Often, for example, with personal hypersensitivity patient to one of the active ingredients of the drugs ( thiamazole or propylthiouracil ) replace one remedy with another.

Judging by patient reviews, if used Propycyla the positive dynamics of the treatment develops faster in comparison with Tyrozol, therapy with which, in turn, more often leads to long-term remission diseases. In connection with all of the above, it is worth leaving the choice between these drugs at the discretion of the doctor, taking into account the individual characteristics of the patient’s body.

For children

In pediatrics, it is possible to prescribe Tyrosol only when the child reaches 3 years of age.

With alcohol

Despite the absence of contraindications for use in the official instructions against the background of treatment with Tyrozol, such a combination a priori cannot lead to any positive aspects and even vice versa, most likely due to synergy will cause an increase in the severity of side effects of therapy, and possibly more severe reactions. In this regard, Tyrosol and alcohol in the treatment of thyroid diseases are incompatible.

During pregnancy and lactation

No therapy hyperthyroidism during pregnancy can cause serious complications, including fetal malformations And . In its turn, hypothyroidism , formed as a result of the administration of inadequate doses of Tyrosol, may lead to miscarriage .

Characteristic for thiamazole is its penetration through placental barrier , after which the concentration of the drug in the fetal blood is similar to that of the mother. For this reason, the prescription of Tyrosol for may be justified only in extreme cases, after a full assessment of the benefits/risks of its use for the mother/fetus, in minimal effective daily dosages (up to 10 mg) and without parallel use levothyroxine sodium .

Reception pregnant high dose woman thiamazole may lead to the formation hypothyroidism And goiter in the fetus, as well as to a decrease in the child’s body weight at birth.

During therapy thyrotoxicosis in the mother can be continued in minimal dosages, since the concentration thiamazole in breast milk corresponds to its content in the mother’s blood and can cause the development hypothyroidism in a newborn. Taking Tyrosol by nursing women requires monitoring the functionality of the thyroid gland in newborns.

Compound

Each tablet contains:

at a dosage of 5 mg;

Active ingredient: thiamazole - 5 mg

Excipients: colloidal silicon dioxide anhydrous - 2 mg, sodium starch glycolate (type C) - 2 mg, magnesium stearate - 2 mg, hypromellose 2910/15 - 3 mg, talc - 6 mg, microcrystalline cellulose - 10 mg, corn starch - 20 mg, lactose monohydrate - 200 mg

Film coating: iron oxide yellow (E 172) - 0.04 mg, dimethicone 100 - 0.16 mg, macrogol 400 - 0.79 mg, titanium dioxide (E 171) - 1.43 mg, hypromellose 2910/15 - 3 .21 mg

at a dosage of 10 mg:

Active ingredient: thiamazole - 10 mg

Excipients: colloidal silicon dioxide anhydrous - 2 mg, sodium starch glycolate (type C) - 2 mg, magnesium stearate - 2 mg, hypromellose 2910/15 - 3 mg, talc - 6 mg, microcrystalline cellulose - 10 mg, corn starch - 20 mg, lactose monohydrate -195 mg

Film coating: iron oxide yellow (E 172) - 0.54 mg, iron oxide red (E 172) - 0.004 mg, dimethicone 100 - 0.16 mg, macrogol 400 - 0.79 mg, titanium dioxide (E 171) - 0.89 mg, hypromellose 2910/15 - 3.21 mg

Description

Dosage 5 mg: light yellow, round, biconvex, film-coated tablets, scored on both sides.

Dosage 10 mg: gray-orange round, biconvex film-coated tablets, scored on both sides.

Pharmacotherapeutic group

Drugs for the treatment of thyroid diseases. Antithyroid drugs. CodeATX: Н03ВВ02.

Pharmacological properties

Pharmacodynamics

Thiamazole inhibits the binding of iodine to tyrosine in a dose-dependent manner and, accordingly, affects the neosynthesis of thyroid hormones. This property allows for symptomatic treatment of thyrotoxicosis, regardless of the cause of its occurrence. At present, it is impossible to say with certainty whether thiamazole affects the natural course of the immunologically induced type of hyperthyroidism (Graves' disease), that is, whether it suppresses the underlying immunopathogenetic processes. Thiamazole does not affect the release of synthesized thyroid hormones from thyroid tissue. This explains individual differences in the duration of the latent period preceding normalization of the levels of thyroxine and triiodothyronine in the blood plasma, i.e. improvement of the clinical picture. Hyperthyroidism, which occurs as a result of the release of hormones after the destruction of thyroid cells, for example, after treatment with radioactive iodine or thyroiditis, is also not affected.

Pharmacokinetics

Thiamazole, when taken orally, is rapidly and almost completely absorbed. After administration, maximum plasma concentration is achieved within 0.4-1.2 hours. It practically does not bind to blood plasma proteins. Thiamazole accumulates in the thyroid gland, where it is slowly metabolized. Despite fluctuations in serum levels, accumulation of thiamazole in the thyroid gland leads to the creation of a concentration plateau. As a result, the duration of action of a single dose is approximately 24 hours. In accordance with the data obtained, the kinetics of thiamazole does not depend on the functional state of the thyroid gland. The half-life is about 3-6 hours, and increases in liver failure. Metabolism of thiamazole occurs in the kidneys and liver; excretion in feces is insignificant due to the enterohepatic circulation. 70% of the substance is excreted by the kidneys within 24 hours. Only a small amount is excreted unchanged. Currently, there are no data regarding the activity of metabolites. Pharmacokinetic data in patients with impaired renal and hepatic function are limited (see section "Dosage and Administration"). There are no data on the use of multiple doses (see section "Method of administration and dosage").

Indications for use

Treatment of hyperthyroidism, including:

Conservative treatment of hyperthyroidism, especially with little or no goiter; preparation for surgery for all forms of hyperthyroidism; preparation for treatment with radioactive iodine, in particular, in patients with severe forms of thyrotoxicosis; for intermediate treatment after intermittent radioiodine therapy; prophylactic treatment of patients with a history of subclinical hyperthyroidism, autonomic adenoma or thyrotoxicosis who require iodine (for example, examination with iodinated contrast media).

Contraindications

Tyrosol should not be prescribed to patients with:

Hypersensitivity to thiamazole, other thiourea derivatives or any of the excipients; with moderate to severe changes in blood count (granulocytopenia); previous cholestasis not associated with hyperthyroidism; history of bone marrow damage after treatment with thiamazole or carbimazole. Combination therapy with thiamazole and thyroid hormones is contraindicated during pregnancy (see section “Use during pregnancy and breastfeeding”).

Directions for use and doses

Thiamazole is an active metabolite of carbimazole, however, 1 mg of thiamazole is not equivalent to 1 mg of carbimazole. This must be kept in mind when starting therapy with thiamazole or when switching from carbimazole to thiamazole. The following dosage recommendations should be followed.

Dosage in adults

Depending on the severity of the disease and the supply of iodine with antithyroid therapy, treatment is usually started with a daily dose of thiamazole from 10 to 40 mg. In many cases, suppression of thyroid hormone production is usually achieved with an initial dose of 20 to 30 mg of thiamazole daily. In less severe cases, a complete blocking dose is not required, so lower initial doses are used. In severe cases of thyrotoxicosis, the initial dose can reach 40 mg of thiamazole.

The dosage is selected individually, depending on the metabolic state of the patient, in accordance with the level of thyroid hormones.

a) Daily dose of 5 to 20 mg thiamazole in combination with levothyroxine to avoid hypothyroidism.

b) Monotherapy: daily dose from 2.5 to 10 mg of thiamazole.

Higher doses may be required for iodine-induced thyrotoxicosis.

Dosagein children

Use in children and adolescents (3-17 years):

The initial dose for the treatment of children and adolescents (3-17 years) should be calculated according to the patient's body weight. As a rule, treatment begins with a dose of 0.5 mg/kg, divided into two or three equal doses per day. The maintenance dose may be reduced depending on the patient's response to therapy and administered once daily. To avoid hypothyroidism, additional levothyroxine may be required. The total daily dose should not exceed 40 mg of thiamazole.

Use in children first 2 years of life:

The safety and effectiveness of thiamazole in children 2 years of age and younger have not been studied. Therefore, the use of thiamazole in children aged 2 years and younger is not recommended.

Conservative treatmenthyperthyroidism

The goal of therapy is to achieve a euthyroid state and long-term remission after a limited period of treatment. Depending on patient choice, remission can be achieved in a maximum of 50% of patients after one year. It was found that the time to achieve remission varies greatly depending on baseline factors. Possible influencing factors are the type of hyperthyroidism (immunogenic or non-immunogenic), duration of treatment, dose of thiamazole, and source of iodine: dietary or iatrogenic.

In the conservative treatment of hyperthyroidism, therapy usually lasts from 6 months to 2 years (1 year on average). Statistically, the likelihood of remission increases with increasing duration of therapy. In cases where remission of the disease is not achieved and certain therapeutic measures are not applied or rejected, thiamazole can be used as long-term antithyroid therapy at the lowest dose without the addition of or in combination with a low dose of levothyroxine.

Patients with a large goiter and narrowing of the trachea should undergo short-term treatment with thiamazole, as long-term use may lead to growth of the goiter. Particularly careful monitoring of therapy is required (TSH level, tracheal lumen). Treatment is preferably carried out in combination with additional levothyroxine.

Preoperative therapy

Temporary treatment may be used in the preoperative period (approximately 3 to 4 weeks or longer if necessary, determined individually) to achieve a euthyroid metabolic state, thereby reducing the risks associated with surgery.

Surgery should be performed as soon as the patient reaches a euthyroid state, otherwise additional thyroid hormones will need to be administered. Treatment may be stopped the day before surgery.

Thiamazole increases bone fragility and the tendency to bleeding from thyroid tissue, which can be compensated by additional preoperative use of high doses of iodine for ten days preceding surgery (Plummer iodine therapy).

Treatment before radioactive iodine therapy

Achieving a euthyroid state before starting radioiodine therapy appears to be especially important in severe hyperthyroidism, since in some cases post-therapeutic thyrotoxic crisis has developed after such therapy without prior treatment.

Note: Thiourea derivatives may reduce the radiosensitivity of thyroid tissue. When planning radioiodine therapy for an autonomous adenoma, activation of paranodal tissue should be prevented by prescribing pretreatment.

Intermediateantithyroidtherapy after exposure to radioactive iodine

The duration and dose of treatment should be determined individually depending on the severity of the clinical picture and the expected period before the start of effective radioiodine therapy (approximately 4 to 6 months).

Preventive treatment of patients at risk of developing hyperthyroidism as a result of administration of iodine-containing substances stvdlI'm safeth diagnostics

Typically, daily doses of 10 to 20 mg thiamazole and/or 1 g perchlorate are prescribed for 10 days (eg, for a contrast agent that is excreted by the kidneys). The duration of treatment depends on the period of time during which the iodine-containing substance remains in the body.

Special patient groups

In patients with liver failure, plasma clearance of thiamazole is reduced. Therefore, the dose should be kept as low as possible and patients should be closely monitored.

Due to the lack of pharmacokinetic data for thiamazole in patients with renal impairment, careful individual dosage selection and monitoring is recommended for such patients, with the dose being kept as low as possible.

Despite the lack of accumulation of the drug, for elderly patients it is recommended to select an individual dose with caution with careful monitoring.

Mode of application

The tablets should be swallowed whole with sufficient liquid.

When starting high-dose therapy for hyperthyroidism, the daily dose can be divided into several doses to be taken at regular intervals throughout the day. The maintenance dose can be taken at a time in the morning immediately after breakfast.

If one dose of tablets is missed, you should not increase the dose the next time you take the tablets.

Use during pregnancy and breastfeeding

In general, pregnancy has a positive effect on hyperthyroidism. However, especially in the first months of pregnancy, treatment for hyperthyroidism is often required. Untreated hyperthyroidism during pregnancy can lead to serious complications such as premature birth and birth defects. However, hypothyroidism caused by treatment with inadequate doses of thiamazole is also associated with a tendency to spontaneous abortion. Thiamazole passes through the placental barrier and reaches concentrations in the fetal blood equal to those contained in the maternal blood serum. With inadequate dosage, this can lead to the formation of goiter and hypothyroidism in the fetus, as well as a decrease in birth weight. There have been repeated reports of partial aplasia of the skin on the head of newborns born to women receiving thiamazole. This defect resolves spontaneously within a few weeks.

In addition, a connection has been identified between a certain group of various malformations and the use of high doses of thiamazole during the first weeks of pregnancy, for example, choanal atresia, esophageal atresia, nipple hypoplasia, delayed mental and motor development. In contrast, several studies of prenatal exposure to thiamazole have not shown any morphological developmental abnormalities, effects on thyroid development, or the physical and mental development of children.

Since embryotoxic effects cannot be completely excluded, Tyrozol should be prescribed during pregnancy only after a careful assessment of the balance of benefits and risks and only in the lowest effective doses without additional administration of thyroid hormones.

Thiamazole passes into breast milk, where it can reach concentrations corresponding to levels in the mother's blood serum, so there is a risk of hypothyroidism in the infant.

Breastfeeding is possible during treatment with thiamazole, however, only when taking low doses of up to 10 mg per day without additional administration of thyroid hormones. The child's thyroid function should be monitored regularly.

Side effect

The frequency of adverse reactions is assessed as follows:

Very common: ≥ 1/10

Often: ≥ 1/100,

Uncommon: ≥ 1/1000,

Rare: ≥ 1/10,000,

Very rarely:

Blood and lymphatic system disorders

Infrequently

Agranulocytosis occurs in 0.3-0.6% of cases. Its symptoms may appear even weeks and months after the start of treatment and lead to the need to discontinue the drug. In most cases, this violation resolves on its own.

Very rarely Thrombocytopenia, pancytopenia, generalized lymphadenopathy.

Endocrine system disorders

Very rarely

Insulin autoimmune syndrome (with a pronounced decrease in blood glucose levels).

Nervous system disorders

Rarely

Disturbances in the sense of taste (dysgeusia, ageusia) occur rarely and may disappear after discontinuation of the drug. However, it may take several weeks to return to normal.

Very rarely

Neuritis, polyneuropathy.

Gastrointestinal disorders

Very rarely

Acute enlargement of the salivary glands.

Disorders of the liver and biliary tract

Very rarely

Isolated cases of the development of cholestatic jaundice and toxic hepatitis have been described. In general, symptoms disappear after stopping the drug. Clinically subtle symptoms of cholestasis that appear during treatment must be differentiated from disorders caused by hyperthyroidism, such as increased levels of gamma-GTP (gamma-glutamyltransferase) and alkaline phosphatase or its bone isoenzyme.

Skin and subcutaneous tissue disorders

Often

Allergic skin reactions of varying degrees (itching, rash, urticaria). In most cases, they are moderate in nature and often disappear with continued treatment. Very rarely

Severe forms of skin allergic reactions, including generalized dermatitis; alopecia; drug-induced lupus erythematous.

Musculoskeletal and connective tissue disorders

Often

Arthralgia, which can develop gradually and appear even after several months of therapy.

Generaldisorders and disorders at the injection site

Rarely

Drug fever.

Pediatric patients

The frequency, type and severity of adverse reactions occurring in children are comparable to those in adult patients.

Severe skin hypersensitivity reactions, including very rare cases of Stevens-Johnson syndrome (severe forms, including generalized dermatitis, have been reported only in isolated cases), have been reported in both adults and children.

Report of suspects adverse reactions

It is important to report suspected adverse reactions after drug registration. This will ensure continuous monitoring of the benefit-risk ratio of the drug.

If an undesirable reaction occurs, either listed or not mentioned in these instructions for medical use, patients are advised to consult their doctor.

Medical professionals are recommended to report any suspected adverse reactions of the drug to the Republican Unitary Enterprise “Center for Expertise and Testing in Healthcare” (see section “Information about the manufacturer”).

Overdose

An overdose leads to the development of hypothyroidism with corresponding symptoms of metabolic depression that occur as a feedback, to activation of the adenohypophysis with a subsequent increase in the size of the thyroid gland. This can be avoided by reducing the dose until a state of euthyroidism is achieved or, if necessary, by additionally prescribing levothyroxine (see section "Method of administration and dosage").

The adverse effects of accidental ingestion of high doses of thiamazole are unknown.

Interaction with other drugs

Iodine deficiency increases the sensitivity of the thyroid gland to thiamazole, while an excess of iodine reduces sensitivity. There is no known direct interaction with other drugs. However, it should be taken into account that the metabolism and elimination of other drugs may be accelerated in hyperthyroidism. They are normalized in accordance with the normalization of thyroid function. If necessary, the dose should be adjusted.

In addition, it has been shown that correction of hyperthyroidism can normalize the enhanced effect of anticoagulants in patients with hyperthyroidism.

No drug interaction studies have been conducted in pediatric patients.

Precautionary measures

Tyrosol should not be used in patients:

With a history of mild hypersensitivity reactions (eg, allergic rash, itching).

Thiamazole should be used only for short periods of time and under close supervision in patients:

With a significant enlargement of the thyroid gland, narrowing the lumen of the trachea, due to the possible risk of an increase in goiter.

Agranulocytosis has been reported to develop in 0.3-0.6% of cases, so before starting treatment the patient should be informed of the need to pay attention to its symptoms (stomatitis, pharyngitis, fever). As a rule, this condition develops in the first weeks of treatment, but may appear several months after the start of treatment, as well as with repeated therapy. Careful monitoring of blood counts before and after initiation of treatment is recommended, especially in cases of a history of moderate granulocytopenia. If any of these symptoms appear, especially in the first weeks of treatment, patients should immediately consult a doctor for a blood test. If agranulocytosis is confirmed, the drug should be discontinued.

Other myelotoxic adverse reactions are rare when thiamazole is taken at recommended doses. They most often developed as a result of taking high doses of thiamazole (about 120 mg per day). Such doses should be used only for treatment for special indications (severe forms of the disease, thyrotoxic crisis). The manifestation of signs of bone marrow toxicity during treatment with thiamazole requires discontinuation of the drug and, if necessary, switching to antithyroid drugs of another group.

Exceeding the dose can lead to subclinical or clinical hypothyroidism and goiter growth due to an increase in TSH. Therefore, the dose of thiamazole should be reduced once a euthyroid metabolic state is achieved and, if necessary, additional levothyroxine is recommended. It is not recommended to completely discontinue thiamazole and continue taking only levothyroxine.

Goiter growth during thiamazole therapy, despite TSH suppression, is the result of the underlying disease and cannot be prevented by the addition of levothyroxine.

Achieving normal TSH levels appears to be very important to minimize the risk of developing or worsening endocrine ophthalmopathy. However, this condition often develops in a manner independent of the course of treatment for thyroid disease. Such a complication in itself is not a reason to change the adequate treatment regimen and should not be considered an undesirable reaction to properly administered therapy.

A small number of patients may develop late-onset hypothyroidism after receiving antithyroid therapy without any additional ablative measures. This condition is probably not an undesirable reaction to the drug and should be considered as the presence of inflammatory and destructive processes in the thyroid parenchyma associated with the underlying disease.

Reducing energy intake, which is pathologically increased in hyperthyroidism, may lead to weight gain (generally desirable) during treatment with thiamazole. Patients should be informed that this clinical improvement indicates a normalization of their energy intake.

The drug Tyrosol contains lactose, therefore patients with rare hereditary galactose intolerance, lactase deficiency or glucose-galactose malabsorption should not take this drug.

Impact on the ability to drive vehicles and machinery

Thiamazole does not affect the ability to drive vehicles and machinery.

Package

Film-coated tablets, 5 mg and 10 mg. 10 tablets in a PVC/AL blister; 5 blisters along with instructions for medical use are placed in a cardboard box. 25 tablets in a PVC/AL blister; 2 blisters along with instructions for medical use are placed in a cardboard box.

Drug: TYROZOL
Active substance of the drug: thiamazole
ATX encoding: H03BB02
CFG: Antithyroid drug
Registration number: P No. 014893/01
Registration date: 07/31/08
Owner reg. cert.: MERCK KGaA (Germany)

Tyrozol release form, drug packaging and composition.

Light yellow film-coated tablets; round, biconvex, with a notch on one side; at the fracture it looks like a white or almost white mass.

1 tab.
thiamazole
5 mg

Film shell composition: dimethicone 100, titanium dioxide, yellow iron oxide, macrogol 400, hypromellose 2910/15.

Gray-orange film-coated tablets; round, biconvex, with a notch on one side; at the fracture it looks like a white or almost white mass.

1 tab.
thiamazole
10 mg

Excipients: colloidal silicon dioxide, sodium carboxymethyl starch, magnesium stearate, hypromellose 2910/15, talc, cellulose (powder), corn starch, lactose monohydrate.

Film shell composition: dimethicone 100, titanium dioxide, yellow iron oxide, red iron oxide, macrogol 400, hypromellose 2910/15.

10 pieces. - blisters (2) - cardboard packs.
10 pieces. - blisters (4) - cardboard packs.
10 pieces. - blisters (5) - cardboard packs.
10 pieces. - blisters (10) - cardboard packs.
25 pcs. - blisters (2) - cardboard packs.
25 pcs. - blisters (4) - cardboard packs.
25 pcs. - blisters (5) - cardboard packs.
25 pcs. - blisters (10) - cardboard packs.

The description of the drug is based on the officially approved instructions for use.

Pharmacological action Tyrozol

Antithyroid drug. It disrupts the synthesis of thyroid hormones by blocking the enzyme peroxidase, which is involved in the iodination of thyronine in the thyroid gland with the formation of triiodo- and tetraiodothyronine.

The drug is effective in the symptomatic treatment of thyrotoxicosis (except for cases of disease development due to the release of hormones after the destruction of thyroid cells during treatment with radioactive iodine or thyroiditis).

Tyrosol does not affect the process of release of synthesized thyronines from the thyroid follicles. This explains the latent period of varying duration, which may precede normalization of T3 and T4 levels in the blood plasma and improvement of the clinical picture.

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

The duration of action of the drug after a single dose is about 24 hours.

Pharmacokinetics of the drug.

Suction

After taking the drug orally, thiamazole is quickly and almost completely absorbed from the gastrointestinal tract. Cmax is achieved within 0.4-1.2 hours.

Distribution

Practically does not bind to plasma proteins. Cumulates in the thyroid gland.

Metabolism

Slowly metabolized in the thyroid gland, as well as in the kidneys and liver.

Removal

Small amounts of thiamazole are found in breast milk. T1/2 is about 3-6 hours. Thiamazole is excreted in the urine (within 24 hours, 70% of the drug, with 7-12% unchanged) and bile.

Pharmacokinetics of the drug.

in special clinical cases

In patients with liver failure, T1/2 increases.

The pharmacokinetic parameters of the drug do not depend on the functional state of the thyroid 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 (carried out before the onset of radioactive iodine action /for 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.

Dosage and method of administration of the drug.

The tablets should be taken after meals, without chewing, with a sufficient amount of liquid. The daily dose is prescribed in 1 dose or divided into 2-3 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.

For thyrotoxicosis, depending on the severity of the disease, 20-40 mg/day is prescribed for 3-6 weeks. After normalization of thyroid function (usually after 3-8 weeks), they switch to a maintenance dose of 5-20 mg/day. From this time on, additional levothyroxine is recommended.

In preparation for surgical treatment of thyrotoxicosis, 20-40 mg/day is prescribed until a euthyroid state is achieved. From this time on, additional levothyroxine is recommended. 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, 20-40 mg/day is prescribed until a euthyroid state is achieved. It should be borne in mind that thiamazole and thiourea derivatives may reduce the sensitivity of thyroid tissue to radiation therapy.

When treating during the latent period of the action of radioiodine, depending on the severity of the disease, 5-20 mg/day is prescribed until the onset of the effect of radioiodine (4-6 months).

For long-term thyreostatic maintenance therapy, Tyrozol is prescribed in doses of 1.25-2.5-10 mg/day with additional levothyroxine in small doses.

In order to prevent 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, Tyrozol is prescribed at a dose of 10-20 mg/day and potassium perchlorate 1 g/day for 8-10 days before taking iodine-containing products.

For children, Tyrozol is prescribed at an initial dose of 0.3-0.5 mg/kg body weight daily. Maintenance dose - 0.2-0.3 mg/kg/day. If necessary, additional levothyroxine is prescribed.

During pregnancy, the drug is prescribed in minimal doses: single - 2.5 mg, daily - 10 mg.

For liver failure, the minimum effective dose of the drug is prescribed.

The duration of use of Tyrosol in the treatment of thyrotoxicosis is from 1.5 to 2 years.

When preparing patients with thyrotoxicosis for surgery, treatment with the drug is carried out until a euthyroid state is achieved within 3-4 weeks before the planned day of surgery (in some cases - longer) and ends the day before it. In all cases, the duration of treatment with the drug is determined by the doctor.

Side effects of Tyrosol:

Sometimes - allergic skin reactions (itching, redness, rashes), vomiting, arthralgia, dizziness, weakness.

Rarely - an increase in temperature, a change in taste sensations (they are reversible).

In approximately 0.3-0.6% of cases, agranulocytosis occurs (symptoms may appear even weeks and months after the start of treatment and lead to the need to discontinue the drug).

In isolated cases - cholestatic jaundice, toxic hepatitis, arthralgia (usually develop slowly and gradually, several months after the start of treatment; there were no clinical signs of arthritis).

In some cases - generalized lymphadenopathy, acute enlargement of the salivary glands, thrombocytopenia, pancytopenia, neuritis, polyneuropathy, lupus-like reaction, autoimmune syndrome with hypoglycemia.

Increase in body weight.

Subclinical and clinical hypothyroidism can develop when taking the drug in high doses. The thyroid gland may also begin to enlarge, which is associated with an increase in TSH levels in the blood.

Contraindications to the drug:

Agranulocytosis during previous therapy with carbimazole or thiamazole;

Granulocytopenia (including history);

Cholestasis before starting treatment;

Thiamazole therapy in combination with levothyroxine during pregnancy;

Hypersensitivity to thiamazole or thiourea derivatives.

Relative contraindication: history of allergic skin reactions to thiourea derivatives.

The drug should be used with caution in case of very large goiter with narrowing of the trachea (only short-term treatment during preparation for surgery), and in case of liver failure.

Use during pregnancy and lactation.

Untreated hyperfunction of the thyroid gland during pregnancy can lead to serious complications: premature birth, fetal malformations.

Thiamazole penetrates the placental barrier and reaches the same concentration in the fetal blood as in the mother. Since the effect of thiamazole on the fetus cannot be completely excluded, during pregnancy the drug should be used only if the expected benefit to the mother outweighs the potential risk to the fetus at the minimum effective dose and without additional use of levothyroxine.

Thiamazole in high doses can cause goiter, hypothyroidism and low birth weight in the fetus.

During lactation, treatment of thyrotoxicosis with Tyrozol can be continued if necessary. Since thiamazole is excreted in breast milk and can reach a concentration in it corresponding to the level of thiamazole in the mother's blood, the newborn may develop hypothyroidism. Therefore, if it is necessary to continue treatment of thyrotoxicosis during breastfeeding, Tyrozol should be used in low doses (up to 10 mg/day) without additional levothyroxine.

Special instructions for the use of Tyrosol.

For patients with a significant enlargement of the thyroid gland, narrowing the lumen of the trachea, Tyrozol is prescribed for a short time in combination with levothyroxine, because with prolonged use, an increase in goiter and even greater compression of the trachea is possible. It is necessary to carefully monitor the patient (monitoring TSH levels, tracheal lumen).

During treatment with the drug, regular monitoring of peripheral blood patterns is necessary.

If during treatment with the drug a sore throat, difficulty swallowing, increased body temperature, signs of stomatitis or furunculosis (possible symptoms of agranulocytosis) suddenly appear, you should stop taking the drug and consult a doctor immediately.

If subcutaneous hemorrhages or bleeding of unknown origin, generalized skin rash and itching, persistent nausea or vomiting, jaundice, severe epigastric pain and severe weakness appear during treatment, discontinuation of the drug is required.

If treatment is stopped early, a relapse of the disease is possible.

The appearance or worsening of endocrine ophthalmopathy is not a side effect of adequate treatment with Tyrozol.

In rare cases, after completion 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 as part of the underlying disease.

Drug overdose:

Symptoms: chronic overdose of Tyrozol leads to an enlargement of the thyroid gland and the development of hypothyroidism. Taking Tyrosol in very high doses (about 120 mg/day) can lead to the development of myelotoxic effects.

Treatment: in case of chronic overdose of Tyrosol, discontinuation of the drug is necessary. Replacement therapy with levothyroxine is carried out if this is justified by the severity of hypothyroidism. As a rule, after discontinuation of Tyrozol, spontaneous restoration of thyroid function is observed. In case of overdose, you should discontinue the drug, rinse the stomach, take activated charcoal, and carry out symptomatic therapy.

Interaction of Tyrosol with other drugs.

When prescribing the drug after using iodine-containing radiocontrast agents in a high dose, the effect of Tyrosol may be weakened.

Lack of iodine enhances the effect of Tyrosol.

In patients taking Tyrozol for thyrotoxicosis, after achieving a euthyroid state (normalization of thyroid hormone levels in the blood serum), it may be necessary to reduce the doses of cardiac glycosides (digoxin and digitoxin), aminophylline, as well as increase the doses of warfarin and other anticoagulants - derivatives coumarin and indanedione (pharmacodynamic interaction).

Lithium preparations, beta-blockers, reserpine, amiodarone increase the effect of thiamazole (dosage adjustment is required).

When used simultaneously with sulfonamides and metamizole sodium, the risk of developing leukopenia increases.

Leukogen and folic acid, when used simultaneously with thiamazole, reduce the risk of developing leukopenia.

Gentamicin enhances the antithyroid effect of thiamazole.

There are no data on the effect of other drugs on the pharmacokinetics and pharmacodynamics of the drug. However, it should be borne in mind that with thyrotoxicosis, the metabolism and elimination of substances is accelerated. Therefore, in some cases it is necessary to adjust the dose of other drugs.

Terms of sale in pharmacies.

The drug is available with a prescription.

Terms of storage conditions for the drug Tyrozol.

The drug should be stored in a dry place, out of reach of children, at a temperature not exceeding 25°C. Shelf life: 4 years.

Tyrosol is a drug that is used in the treatment of thyrotoxicosis due to its property of inhibiting the production of thyroid hormones.

The effects of thiamazole in the thyroid gland are characterized by a decrease in basal metabolism, acceleration of the excretion of iodides, as well as an increase in the reciprocal activation of the synthesis and secretion of thyroid-stimulating hormone by the pituitary gland, which may be accompanied by the development of thyroid hyperplasia.

A single dose of thiamazole continues to act for almost 24 hours.

Clinical and pharmacological group

Antithyroid drug.

Terms of sale from pharmacies

Can buy according to a doctor's prescription.

Price

How much does Tyrosol cost in pharmacies? The average price is 200 rubles.

Composition and release form

Tyrosol is available in the form of film-coated tablets.

• The main active ingredient of Tyrosol is thiamazole. Depending on the amount of thiamazole included in one tablet, Tyrozol is produced in 5 and 10 mg doses.

Excipients of Tyrosol are: sodium carboxymethyl starch, colloidal silicon dioxide, magnesium stearate, cellulose powder, hypromellose, talc, corn starch, lactose monohydrate.

pharmachologic effect

The effect of the active component Tyrosol on the thyroid gland inhibits the production of hormones by blocking enzymes, in particular peroxidase, which is involved in the iodination of tyrosine. Taking the drug accelerates the removal of iodides from the thyroid gland and reduces basal metabolism.

In parallel, the use of Tyrosol increases the activation of the synthesis and secretion of thyroid-stimulating hormone by the pituitary gland. This can sometimes be accompanied by a slight increase in the volume of the thyroid gland. The drug is very effective in the symptomatic treatment of thyrotoxicosis. A single dose of Tyrosol guarantees its effect for at least 24 hours.

Indications for use

According to the instructions, Tyrozol is used:

• with thyrotoxicosis;
• in preparation for radioactive iodine therapy;
• in preparation for surgery for thyrotoxicosis;
• for the purpose of preventing thyrotoxicosis when taking iodine-containing drugs for latent thyrotoxicosis, a history of thyrotoxicosis, autonomous adenomas;
• as a treatment during the latent period of radioactive iodine;
• as long-term maintenance therapy for thyrotoxicosis, when, due to the general condition of the patient or for other reasons, radical treatment cannot be performed.

Contraindications

Absolute:

• glucose-galactose malabsorption, galactose intolerance, lactase deficiency;
• hypersensitivity to thiourea derivatives and any ingredients of the drug;
• granulocytopenia (including history);
• development of agranulocytosis during previous therapy with thiamazole or carbimazole;
• therapy with thiamazole and levothyroxine during pregnancy;
• age up to 3 years.

Tyrosol is used with caution in the following cases:

• severe increase in goiter, leading to narrowing of the trachea (the drug is used only for short-term treatment in the preoperative period);
• liver failure.

Prescription during pregnancy and lactation

Untreated hyperthyroidism during pregnancy can cause serious complications, including fetal malformations and premature birth. In turn, hypothyroidism, formed as a result of the administration of inadequate doses of Tyrozol, can lead to miscarriage.

A characteristic feature of thiamazole is its penetration through the placental barrier, after which a drug concentration similar to that of the mother is observed in the fetal blood. For this reason, the prescription of Tyrosol during pregnancy can be justified only in extreme cases, after a full assessment of the benefits/risks of its use for the mother/fetus, in minimal effective daily dosages (up to 10 mg) and without parallel use of levothyroxine sodium.

Taking high doses of thiamazole by a pregnant woman can lead to the formation of hypothyroidism and goiter in the fetus, as well as to a decrease in the child’s body weight at birth.

During breastfeeding, therapy for thyrotoxicosis in the mother can be continued in minimal dosages, since the concentration of thiamazole in breast milk corresponds to its content in the mother’s blood and can cause the development of hypothyroidism in the newborn. Taking Tyrosol by nursing women requires monitoring the functionality of the thyroid gland in newborns.

Dosage and method of administration

As indicated in the instructions for use, Tyrozol is taken orally after meals. The tablets should be taken without chewing, with a sufficient amount of liquid.

The daily dose is prescribed in 1 dose or divided into 2-3 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.

1. For thyrotoxicosis, depending on the severity of the disease, the drug is prescribed at a dose of 20-40 mg/day for 3-6 weeks. After normalization of thyroid function (usually after 3-8 weeks), they switch to a maintenance dose of 5-20 mg/day. From this time on, additional intake of levothyroxine sodium is recommended.
2. In preparation for surgical treatment of thyrotoxicosis, 20-40 mg/day is prescribed until a euthyroid state is achieved. From this time on, additional intake of levothyroxine sodium is recommended. In order to reduce the time required to prepare for surgery, beta-blockers and iodine preparations are additionally prescribed.
3. In preparation for treatment with radioactive iodine, 20-40 mg/day is prescribed until a euthyroid state is achieved.
4. When treating during the latent period of the action of radioiodine, depending on the severity of the disease, 5-20 mg/day is prescribed until the onset of the effect of radioiodine (4-6 months).
5. For long-term thyreostatic maintenance therapy, Tyrozol is prescribed in doses of 1.25-2.5-10 mg/day with additional levothyroxine sodium in small doses. When treating thyrotoxicosis, the duration of therapy is from 1.5 to 2 years.
6. In order to prevent 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, Tyrozol is prescribed at a dose of 10-20 mg/day and potassium perchlorate 1 g/day for 8-10 days before taking iodine-containing products.

For children aged 3 to 17 years, Tyrozol is prescribed at an initial dose of 0.3-0.5 mg/kg body weight in 2-3 equal divided doses daily. The maximum recommended dose for children weighing more than 80 kg is 40 mg/day. Maintenance dose – 0.2-0.3 mg/kg/day. If necessary, sodium levothyroxine is additionally prescribed.

During pregnancy, the drug is prescribed in minimal doses: single - 2.5 mg, daily - 10 mg.

In case of liver failure, the drug is prescribed in the minimum effective dose under close medical supervision.

When preparing patients with thyrotoxicosis for surgery, treatment with the drug is carried out until a euthyroid state is achieved within 3-4 weeks before the planned day of surgery (in some cases longer) and ends the day before it.

Side effects

When taking Tyrozol tablets orally, patients experienced some side effects:

• Connective tissue and musculoskeletal system: often - arthralgia (slowly progressive) without clinical symptoms of arthritis;
• Skin and subcutaneous tissues: very often – itching, rashes, redness of the skin; very rarely - baldness, generalized skin rash, lupus-like syndrome;
• Gastrointestinal tract, liver and biliary tract: very rarely - vomiting, toxic hepatitis, enlarged salivary glands, cholestatic jaundice;
• Blood and lymphatic systems: uncommon – agranulocytosis; very rarely - thrombocytopenia, generalized lymphadenopathy, pancytopenia;
• Nervous system: rarely - dizziness, reversible change in taste sensations; very rarely – polyneuropathy, neuritis;
• Endocrine system: very rarely - Hirata disease (autoimmune insulin syndrome) with hypoglycemic conditions;
• Other reactions: rarely - weakness, fever, weight gain.

Overdose

With long-term use of Tyrozol tablets in large doses, the patient gradually develops signs of overdose, which are expressed by an increase in the adverse reactions described above, an increase in the size of the gland, and the formation of a goiter.

Treatment of signs of overdose is symptomatic - the patient’s stomach is washed, enterosorbents are prescribed, and after them an antithyroid drug of another group is selected.

special instructions

Before you start using the drug, read the special instructions:

1. If the course of treatment is stopped early, a relapse of the disease is possible.
2. Rarely, after the end of treatment, late hypothyroidism may occur, which is not associated with taking the drug, but with inflammatory and destructive processes in the thyroid tissue.
3. In case of severe goiter, Tyrozol is prescribed in combination with sodium levothyroxine to avoid further narrowing of the tracheal lumen.
4. During the treatment period, monitoring of the peripheral blood picture is necessary.
5. The drug may reduce the sensitivity of thyroid tissue to radiation therapy.
6. If you experience a sore throat, difficulty swallowing, increased body temperature, signs of stomatitis or furunculosis during treatment, the drug should be discontinued and consult a doctor immediately.
7. The drug is discontinued if hemorrhages or bleeding of unknown origin, generalized skin rash and itching, persistent nausea or vomiting, or jaundice occur. severe abdominal pain, severe weakness.

Interaction with other drugs

When using the drug, it is necessary to take into account interactions with other medications:

1. Gentamicin enhances the antithyroid effect of thiamazole.
2. Lack of iodine enhances the effect of thiamazole.
3. Lithium preparations, beta-blockers, reserpine, amiodarone increase the effect of thiamazole (dosage adjustment is required).
4. Leukogen and folic acid, when used simultaneously with thiamazole, reduce the risk of developing leukopenia.
5. When prescribing the drug after using iodine-containing radiocontrast agents in a high dose, the effect of thiamazole may be weakened.
6. When used simultaneously with sulfonamides, metamizole sodium and myelotoxic drugs, the risk of developing leukopenia increases.
7. There are no data on the effect of other drugs on the pharmacokinetics and pharmacodynamics of the drug. However, it should be borne in mind that with thyrotoxicosis, the metabolism and elimination of substances is accelerated. Therefore, in some cases it is necessary to adjust the dose of other drugs.
8. In patients taking Tyrozol for thyrotoxicosis, after achieving a euthyroid state (normalization of thyroid hormone levels in the blood serum), it may be necessary to reduce the doses of cardiac glycosides (digoxin and digitoxin), aminophylline, as well as increase the doses of warfarin and other anticoagulants - derivatives coumarin and indanedione (pharmacodynamic interaction).