Eutirox tablets 50mkg, No. 100

• Hypothyroidism;

• euthyroid goiter;

• replacement therapy and prevention of goiter recurrence after surgery on the thyroid gland;

• thyroid cancer (after surgery);

• diffuse toxic goiter, after reaching the euthyroid state against the background of antithyroid therapy (in the form of combination or monotherapy);

• as a diagnostic tool for performing a thyroid suppression test.

The daily dose is determined individually, depending on the indications, the patient's clinical condition and laboratory examination data.

Tablets are white, round, flat on both sides, with a bevel; on both sides of the tablet there is a dividing line, on one side of the tablet there is an engraving 'EM + dosage'.

1 tab.

levothyroxine sodium 25 mcg

-'- 50 mcg

-'- 75 mcg

-'- 88 mcg

-'- 100 mcg

-'- 112 mcg

-'- 125 mcg

-'- 137 mcg

-'- 150 mcg

Excipients: corn starch - 25 mg, gelatin - 5 mg, croscarmellose sodium - 3.5 mg, magnesium stearate - 0.5 mg, lactose monohydrate - 65.975 mg / 65.95 mg / 65.925 mg / 65.912 mg / 65.9 mg / 65.888 mg / 65.875 mg / 65.863 mg / 65.85 mg.

• Increased individual sensitivity to the drug;

• untreated thyrotoxicosis;

• untreated pituitary insufficiency;

• untreated adrenal insufficiency;

• use during pregnancy in combination with antithyroid drugs.

Do not start drug treatment in the presence of acute myocardial infarction, acute myocarditis and acute pancarditis. The drug contains lactose, so its use is not recommended for patients with rare hereditary diseases associated with galactose intolerance, lactase deficiency or glucose-galactose malabsorption syndrome.

With care: coronary heart disease (atherosclerosis, angina pectoris, myocardial infarction in history), arterial hypertension, arrhythmia, diabetes mellitus, severe long-term hypothyroidism, malabsorption syndrome (dose adjustment may be required), patients with a predisposition to psychotic reactions.

pharmachologic effect

Levothyroxine sodium is a synthetic levorotatory isomer of thyroxine, in its action identical to thyroxine, which is synthesized by the human thyroid gland. After partial transformation into triiodothyronine (in the liver and kidneys) and transition into the cells of the body, it affects the development and growth of tissues, and metabolism. In small doses, it has an anabolic effect on protein and fat metabolism. In medium doses, it stimulates growth and development, increases tissue oxygen demand, stimulates the metabolism of proteins, fats and carbohydrates, increases the functional activity of the cardiovascular system and the central nervous system. In large doses, it inhibits the production of thyrotropin-releasing hormone of the hypothalamus and thyroid-stimulating hormone (TSH) of the pituitary gland.

The therapeutic effect is observed after 7-12 days, during the same time the effect persists after the drug is discontinued. The clinical effect in hypothyroidism appears after 3-5 days. Diffuse goiter decreases or disappears within 3-6 months.

Pharmacokinetics

Suction

When taken orally, levothyroxine sodium is absorbed mainly in the upper part of the small intestine. Up to 80% of the taken dose of the drug is absorbed. Food intake reduces the absorption of levothyroxine sodium.

Cmax in serum is reached approximately 5-6 hours after oral administration.

Distribution

After absorption with 99% of the drug, it binds to serum proteins (thyroxine-binding globulin, thyroxine-binding prealbumin and albumin). In various tissues, monodeiodination of approximately 80% of levothyroxine occurs with the formation of triiodothyronine (T3) and inactive products.

Metabolism

Thyroid hormones are metabolized primarily in the liver, kidneys, brain and muscles. A small amount of the drug undergoes deamination and decarboxylation, as well as conjugation with sulfuric and glucuronic acids (in the liver). Estimated Vd is 10-12 liters. Metabolic clearance is about 1.2 liters of blood plasma per day.

Withdrawal

T1 / 2 drug is 6-7 days. With thyrotoxicosis, T1 / 2 is shortened to 3-4 days, and with hypothyroidism it is extended to 9-10 days. Metabolites are excreted by the kidneys and through the intestines.

Side effect

With the correct use of EutiroxЃ under the supervision of a physician, side effects are not observed.

Cases of allergic reactions in the form of angioedema have been reported.

Application during pregnancy and lactation

During pregnancy and especially during breastfeeding, thyroid hormone treatment should be carried out sequentially. During pregnancy, an increase in the dose of the drug may be required. Because an increase in the concentration of TSH in blood plasma can be observed already from the 4th week of pregnancy, pregnant women receiving therapy with levothyroxine sodium should determine the concentration of TSH in blood plasma during each trimester to ensure that it is within the recommended range for this trimester of pregnancy. An increase in the concentration of TSH in blood plasma should be corrected by increasing the dose of levothyroxine sodium. Since the concentration of TSH in the postpartum period is similar to its values ??before pregnancy, immediately after childbirth, the woman should be switched to a dose of levothyroxine sodium,which she received before pregnancy. Plasma TSH concentration should be determined 6-8 weeks after delivery.

Pregnancy

During pregnancy, it is necessary to refrain from conducting diagnostic tests for suppressing the function of the thyroid gland, because the use of radioactive substances in pregnant women is contraindicated.

There is no data on the presence of teratogenic and fetotoxic effects in humans when taking levothyroxine sodium in the recommended therapeutic doses. Taking the drug during pregnancy in excessively high doses can negatively affect the fetus and postnatal development.

The use of the drug during pregnancy in combination with antithyroid drugs is contraindicated, because taking levothyroxine sodium may require an increase in the dose of antithyroid drugs. Since antithyroid drugs, unlike levothyroxine sodium, can cross the placenta, hypothyroidism may develop in the fetus.

Breastfeeding period

Levothyroxine sodium passes into breast milk during breastfeeding. However, when using levothyroxine sodium in recommended therapeutic doses, the concentration of thyroid hormones in breast milk does not reach a level that can cause hyperthyroidism and suppress TSH secretion in a child.

Application in children

In the treatment of congenital hypothyroidism in children, the dose of the drug depends on age.

Use in elderly patients

When carrying out replacement therapy for hypothyroidism in patients under the age of 55 in the absence of cardiovascular diseases, Eutirox is prescribed in a daily dose of 1.6-1.8 ?g / kg of body weight; in patients over the age of 55 or with concomitant cardiovascular diseases - 0.9 ?g / kg of body weight.

In case of replacement therapy for hypothyroidism, the initial dose for patients under the age of 55 (in the absence of cardiovascular diseases) is 75-100 mcg / day for women, and 100-150 mcg / day for men. For patients over 55 years of age or with concomitant cardiovascular diseases, the initial dose is 25 mcg / day; the dose should be increased by 25 ?g with an interval of 2 months until the TSH level in the blood is normalized; if symptoms of the cardiovascular system appear or worsen, correct the appropriate therapy.

special instructions

Thyroid hormones should not be prescribed for weight loss. In patients with euthyroidism, treatment with levothyroxine does not lead to weight loss. High doses of levothyroxine sodium can cause serious and life-threatening adverse reactions, particularly when combined with certain weight loss drugs, especially sympathomimetic amines.

Before starting thyroid hormone replacement therapy or before performing a thyroid suppression test, it is necessary to exclude or treat the following diseases or pathological conditions: acute coronary insufficiency, angina pectoris, atherosclerosis, arterial hypertension, pituitary insufficiency or adrenal insufficiency. Also, prior to initiation of thyroid hormone therapy, functional thyroid autonomy should be excluded or treated.

In patients at risk of developing psychotic disorders, it is recommended to start therapy with a low dose of levothyroxine sodium, followed by a slow increase at the beginning of therapy. Patient monitoring is recommended. If signs of psychotic disorders are found, the dose of levothyroxine sodium taken should be adjusted.

It is necessary to exclude the possibility of even minor drug-related hyperthyroidism in patients with coronary insufficiency, heart failure, or tachyarrhythmias. Therefore, in these cases, it is necessary to regularly monitor the concentration of thyroid hormones.

Before carrying out replacement therapy with thyroid hormones, it is necessary to find out the etiology of secondary hypothyroidism. If necessary, substitution therapy should be started to compensate for adrenal insufficiency.

If the development of functional autonomy of the thyroid gland is suspected, a TRH test or suppressive scintigraphy is recommended before starting therapy.

In postmenopausal women with hypothyroidism and an increased risk of osteoporosis, it is necessary to exclude the presence of concentrations of levothyroxine sodium in serum exceeding physiological ones. In this case, careful monitoring of thyroid function is recommended.

The use of levothyroxine sodium is not recommended in the presence of metabolic disorders accompanied by hyperthyroidism. An exception is the concomitant use of antithyroid drugs during drug therapy of hyperthyroidism.

Since the start of therapy with levothyroxine sodium, in the case of switching from one drug to another, it is recommended to adjust the dose depending on the patient's clinical response to therapy and the results of laboratory tests.

With the simultaneous use of orlistat and levothyroxine sodium, hypothyroidism may develop and / or a decrease in the control of hypothyroidism may occur. Patients taking levothyroxine sodium should consult a physician prior to using orlistat, because you may need to take orlistat and levothyroxine sodium at different times of the day and adjust the dose of levothyroxine sodium. Further monitoring of thyroid function is recommended.

Influence on the ability to drive vehicles and mechanisms

Studies of the effect of the drug on the ability to drive vehicles and mechanisms have not been conducted. However, since levothyroxine sodium is identical to the natural thyroid hormone, no effect on the ability to drive vehicles and mechanisms is expected.

Overdose

With an overdose of the drug, a significant increase in the metabolic rate is observed. Clinical signs of hyperthyroidism may occur in case of an overdose, if the individual tolerance threshold for levothyroxine sodium is exceeded, or if the dose of the drug rises too quickly since the start of therapy.

Symptoms characteristic of hyperthyroidism: cardiac arrhythmias, tachycardia, palpitations, angina pectoris, headache, muscle weakness and muscle twitching, hyperemia (especially of the face), fever, vomiting, menstrual irregularities, benign intracranial hypertension, tremor, anxiety, anxiety, weight loss, diarrhea.

Depending on the severity of symptoms, the doctor may recommend a decrease in the daily dose of the drug, a break in treatment for several days, the appointment of beta-blockers. When taking extremely high doses, plasmapheresis may be prescribed. After the disappearance of side effects, treatment should be started with caution with a lower dose.

An overdose of levothyroxine sodium can lead to symptoms of acute psychosis, especially in patients with a predisposition to psychotic disorders.

Cases of sudden cardiac arrest have been reported in patients who have been taking excessively high doses of levothyroxine sodium for many years. In predisposed patients, there were isolated cases of seizures when the individual threshold of tolerance was exceeded.

Drug interactions

The use of tricyclic antidepressants with levothyroxine sodium can lead to an increase in the effect of antidepressants.

Levothyroxine sodium reduces the action of cardiac glycosides.

With the simultaneous use of colestyramine and colestipol (ion exchange resins), as well as aluminum hydroxide, they reduce the plasma concentration of sodium levothyroxine by inhibiting its absorption in the intestine. In this regard, levothyroxine sodium should be used 4-5 hours before taking these drugs.

With simultaneous use with anabolic steroids, asparaginase, tamoxifen, pharmacokinetic interaction is possible at the level of binding to plasma proteins.

Protease inhibitors (eg, ritonavir, indinavir, lopinavir) may interfere with the effectiveness of levothyroxine sodium. Careful monitoring of thyroid hormone concentrations is recommended. The dose of levothyroxine sodium should be adjusted if necessary.

Phenytoin can affect the effectiveness of levothyroxine sodium due to the displacement of levothyroxine sodium from the bond with plasma proteins, which can lead to an increase in the concentration of free T4 and T3. On the other hand, phenytoin increases the metabolic rate of levothyroxine sodium in the liver. Careful monitoring of thyroid hormone concentrations is recommended.

Levothyroxine sodium can reduce the effectiveness of hypoglycemic drugs. Therefore, frequent monitoring of blood glucose concentration is necessary from the moment of initiation of thyroid hormone replacement therapy. If necessary, the dose of the hypoglycemic drug should be adjusted.

Levothyroxine sodium can enhance the effect of anticoagulants (coumarin derivatives) by displacing them from the connection with plasma proteins, which can increase the risk of bleeding, for example, hemorrhage in the central nervous system or gastrointestinal bleeding, especially in elderly patients. Therefore, regular monitoring of coagulation parameters is necessary both at the beginning and during combination therapy with these drugs. If necessary, the dose of the anticoagulant should be adjusted.

Salicylates, dicumarol, furosemide in high doses (250 mg), clofibrate and other drugs can displace levothyroxine sodium from its connection with plasma proteins, which leads to an increase in the concentration of the free T4 fraction.

Orlistat: while taking orlistat and levothyroxine sodium, hypothyroidism may develop and / or a decrease in hypothyroidism control may occur. The reason for this may be a decrease in the absorption of iodine salts and / or levothyroxine sodium.

Sevelamer may decrease the absorption of levothyroxine sodium. Tyrosine kinase inhibitors (eg, imatinib, sunitinib) can reduce the effectiveness of levothyroxine sodium. Therefore, at the beginning or at the end of the course of concomitant therapy with these drugs, it is recommended to monitor changes in thyroid function in patients. If necessary, the dose of levothyroxine sodium is adjusted.

Medicines containing aluminum, iron and calcium salts: aluminum-containing medicinal products (antacids, sucralfate) are described in the literature as potentially reducing the effectiveness of sodium levothyroxine. Therefore, it is recommended to take levothyroxine sodium at least 2 hours before using aluminum-containing drugs. This recommendation applies to the use of medicinal products containing iron and calcium salts

Somatropin, when used simultaneously with sodium levothyroxine, can accelerate the closure of the epiphyseal growth zones.

Propylthiouracil, GCS, beta-sympatholytics, iodine-containing contrast agents, amiodarone inhibit the peripheral conversion of T4 to T3. Due to the high iodine content, the use of amiodarone may be accompanied by the development of both hyperthyroidism and hypothyroidism. Particular attention should be paid to the nodular goiter with the possible development of unrecognized functional autonomy.

Sertraline, chloroquine / proguanil reduce the effectiveness of levothyroxine sodium and increase serum TSH levels.

Medicines that promote the induction of hepatic enzymes (eg, barbiturates, carbamazepine) can promote hepatic clearance of levothyroxine sodium.

In women using estrogen-containing contraceptives, or in postmenopausal women receiving hormone replacement therapy, the need for levothyroxine sodium may increase.

The use of soy-containing products can help reduce the absorption of levothyroxine sodium in the intestine. Therefore, dose adjustment may be required, especially at the beginning or after stopping the use of foods containing soy.