TIROZOL

978 7 minutes read

Active material: Tiamazol
When ATH: H03BB02
CCF: Antithyroid drug
ICD-10 codes (testimony): E05
When CSF: 15.04.04
Manufacturer: MERCK KGaA (Germany)

Pharmaceutical form, composition and packaging

Pills, Film-coated light yellow, round, lenticular, with Valium on one side; on the fracture looks like a white or almost white mass.

	1 tab.
tiamazol	5 mg

Excipients: colloidal silicon dioxide, sodium carboxymethyl starch, magnesium stearate, gipromelloza 2910/15, talc, cellulose (powder), corn starch, lactose monohydrate, iron oxide yellow, Dimethicone 100, macrogol 400, Titanium dioxide.

10 PC. – blisters (2) – packs cardboard.
10 PC. – blisters (4) – packs cardboard.
10 PC. – blisters (5) – packs cardboard.
10 PC. – blisters (10) – packs cardboard.
25 PC. – blisters (2) – packs cardboard.
25 PC. – blisters (4) – packs cardboard.
25 PC. – blisters (5) – packs cardboard.
25 PC. – blisters (10) – packs cardboard.

Pills, Film-coated grayish orange, round, lenticular, with Valium on one side; on the fracture looks like a white or almost white mass.

	1 tab.
tiamazol	10 mg

Pharmacological action

Antithyroid drug. Violates the synthesis of thyroid hormones, blocking the enzyme peroxidase, participating in the iodization thyronine in the thyroid gland to form a tri- and tetraiodothyronine.

The drug is effective in the symptomatic treatment of hyperthyroidism (except in cases of disease due to the release of hormones after the destruction of thyroid cells during treatment with radioiodine, or thyroiditis).

Tirozol^® It does not affect the release of the synthesized thyronines of thyroid follicles. This explains the latent period of varying duration, which may precede the normalization of T₃ and T₄ in plasma and improve the clinical picture.

The drug reduces the basal metabolic rate, It accelerates the removal of the thyroid iodides, increases reciprocal activation of synthesis and secretion of pituitary thyroid stimulating hormone, which may be accompanied by a thyroid hyperplasia.

The duration of action of the drug after a single dose is approximately 24 no.

Pharmacokinetics

Absorption

After taking the drug inside tiamazol rapidly and almost completely absorbed from the gastrointestinal tract. FROM_max It reached within 0.4-1.2 no.

Distribution

Almost does not bind to plasma proteins. It accumulates in the thyroid gland.

Metabolism

Slowly metabolized by the thyroid gland, and kidney and liver.

Deduction

Small amounts Tiamazol found in breast milk. T_1/2 is about 3-6 no. Tiamazol urine output c (during 24 no 70% product, and 7-12% in unchanged form) and bile.

Pharmacokinetics in special clinical situations

In patients with liver failure T_1/2 increases.

Pharmacokinetic parameters of the drug are not dependent on the functional state of the thyroid gland.

Testimony

- Thyrotoxicosis;

- Preparation for the surgical treatment of hyperthyroidism;

- Preparation for the treatment of hyperthyroidism with radioactive iodine;

- Therapy in the latent period of radioactive iodine (It carried out before the start of the radioactive iodine / for 4-6 months /);

- In exceptional cases, long-term treatment of hyperthyroidism, when in connection with the general condition or for personal reasons can not perform radical treatment;

- Prevention of hyperthyroidism in the appointment of iodine preparations (including cases of use of iodinated contrast media) in the presence of latent hyperthyroidism, autonomous adenomas or a history of hyperthyroidism.

Dosage regimen

The tablets should be taken after meals, without chewing, drinking plenty of fluids. The daily dose is administered in 1 reception or share on 2-3 single doses. At the beginning of the treatment unit doses taken during the day at a fixed time. The maintenance dose should be taken at once after breakfast.

At thyrotoxicosis depending on the severity of the disease designate 20-40 mg / day for 3-6 Sun. After normalization of thyroid function (usually via 3-8 weeks) move on to receive a maintenance dose 5-20 mg / day. Since that time, we recommend supplementation of levothyroxine.

At preparation for the surgical treatment of hyperthyroidism appointed 20-40 mg / day until a euthyroid state. Since that time, we recommend supplementation of levothyroxine. In order to reduce the time, required for preparation for surgery, additionally prescribe beta-blockers and iodine.

At preparations for the treatment of radioactive iodine appointed 20-40 mg / day until a euthyroid state. It will be appreciated, that tiamazol and thiourea derivatives can reduce the sensitivity of the thyroid to radiation therapy.

At therapy in the latent period of radioactive iodine depending on the severity of the disease designate 5-20 mg / day until the action radioiodine (4-6 Months).

At thyreostatic long-term maintenance therapy Tirozol^® administered in doses 1.25-2.5-10 mg / day with an additional intake of levothyroxine in small doses.

With the aim of prevention of hyperthyroidism in the appointment of iodine preparations (including cases of radiopaque agents yodosoderzhashih) in the presence of latent hyperthyroidism, autonomous adenomas or a history of hyperthyroidism Tirozol^® administered at a dose of 10-20 mg / day, and potassium perchlorate 1 g / day for 8-10 days before taking iodine-containing agents.

Babies Tirozol^® administered in an initial dose of 0.3-0.5 mg / kg body weight daily. Maintenance dose – 0.2-0.3 mg / kg / day. If necessary, further prescribe levothyroxine.

At pregnancy drug administered in minimal doses: single – 2.5 mg, daily – 10 mg.

At hepatic insufficiency prescribe the minimum effective dose.

The duration of tirozol^® at treatment of hyperthyroidism It is between 1.5 to 2 years.

At preparation for surgery patients with thyrotoxicosis drug treatment is carried out until a euthyroid state during 3-4 weeks before the scheduled date of the operation (in some cases – more durable) and ends the day before it. In all cases, the duration of treatment determined by the doctor.

Side effect

Sometimes – allergic skin reactions (itch, redness, rashes), vomiting, arthralgia, dizziness, weakness.

Rarely – temperature rise, change in taste (reversible).

Around 0.3-0.6% cases – agranulocytosis (symptoms can appear even after weeks and months after the start of treatment and cause a withdrawal of the drug).

In rare cases, – cholestatic jaundice, toxic hepatitis, artralgii (develop, usually, slowly and gradually, a few months after the start of treatment; no clinical signs of arthritis).

In some cases, – generalized lymphadenopathy, a sharp increase in the salivary glands, thrombocytopenia, pancytopenia, neuritis, polyneuropathy, lupus-like reaction, autoimmune syndrome with hypoglycemia.

Weight gain.

Subclinical and clinical hypothyroidism may occur while taking the drug at high doses. It may also begin thyroid enlargement, which it is associated with an increase in TSH.

Contraindications

- Agranulocytosis during their prior therapy, carbimazole or Thiamazolum;

- Granulozitopenia (incl. history);

- Cholestasis before treatment;

- Thiamazolum therapy in combination with levothyroxine in pregnancy;

- Hypersensitivity to tiamazol or thiourea derivatives.

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

FROM caution use in patients with goiter is very large with a constriction of the trachea (Only short-term treatment in preparation for surgery), hepatic failure.

Pregnancy and lactation

Untreated hyperthyroidism during pregnancy can lead to serious complications: miscarriage, fetal malformations.

Tiamazol crosses the placental barrier and fetal blood reaches the same concentration, like his mother. Since tiamazol impact on the fetus can not be excluded, during pregnancy the drug should be used only in the event, when the intended benefits to the mother outweighs the potential risk to the fetus in the minimum effective dose and without the use of levothyroxine.

Tiamazol in high doses can cause goitre, hypothyroidism and low birth weight of the fetus.

During lactation the drug treatment of hyperthyroidism tirozol^® if necessary, it may be extended. Since tiamazol excreted in breast milk and can reach concentrations of it, tiamazol appropriate level in the mother's blood, the newborn may develop hypothyroidism. Therefore, the need to continue the treatment of hyperthyroidism during breastfeeding tirozol^® It should be used in low doses (to 10 mg / day) without receiving levothyroxine.

Cautions

Patients with a significant increase in thyroid, narrowing the lumen of the trachea, Tirozol^® administered in combination with a short-term levothyroxine, tk. long-term use may increase the crop and even greater compression of the trachea. It is necessary to carry out careful monitoring of patients (control the level of TSH and tracheal lumen).

In the period of treatment requires regular monitoring of peripheral blood.

If during treatment with sudden pain in the throat, difficulty swallowing, fever, sores or abrasions signs (Possible symptoms of agranulocytosis) should stop taking the drug and seek immediate medical attention.

When during treatment bruising or bleeding of unknown origin, generalized skin rash and itching, persistent nausea or vomiting, želtuhi, severe epigastric pain and severe weakness requires removal of the drug.

In case of early termination of the treatment possible relapse.

The emergence or worsening of endocrine ophthalmopathy is not a side effect of adequate treatment tirozol.^®

In rare cases after treatment of hypothyroidism may occur later, which is not a side effect of the drug, and associated with inflammatory and destructive processes in the thyroid gland, taking place in the framework of the underlying disease.

Overdose

Symptoms: Chronic overdose tirozol^® It leads to an increase of thyroid and hypothyroidism. Admission tirozol in very high doses (about 120 mg / day) could lead to development of myelotoxic effects.

Treatment: in chronic overdose tirozol^® requires removal of the drug. Levothyroxine replacement therapy is carried out in the case, if it is justified by the severity of hypothyroidism. Usually, after canceling tirozol observed spontaneous recovery of thyroid function. With an overdose of the drug should be discontinued, wash out the stomach, take activated charcoal, symptomatic therapy.

Drug Interactions

In appointing the drug after administration of iodine-containing contrast media at a high dose may weaken the effect tirozol^®.

Iodine deficiency increases the effects of tirozol^®.

Patients, taking tirozol^® about hyperthyroidism, after achieving euthyroid state (normalization of thyroid hormones in the blood serum) It may be necessary to reduce the dose received cardiac glycosides (digoxin and digitoxin), aminofillina, as well as increasing the doses received warfarin, and other anticoagulants – coumarin derivatives and indandiona (pharmacodynamic interaction).

Preparations lithium, beta-blockers, reserpine, Amiodarone increases the effect tiamazol (requires correction of the dose).

While the use of sulfonamides and Metamizole increased risk of leukopenia.

Leucogen and folic acid, while the use Thiamazolum reduce the risk of leukopenia.

Gentamicin amplifies the action of antithyroid tiamazol.

Data on the effect of other drugs on the pharmacokinetics and pharmacodynamics of the drug available. However, it should be borne in mind, that in thyrotoxicosis accelerates metabolism, and elimination of a substance. Therefore, in some cases it is necessary to adjust the dose of other medications.

Conditions of supply of pharmacies

The drug is released under the prescription.

Conditions and terms

The drug should be stored in a dry, inaccessible to children at temperature not exceeding 25 ° C. Shelf life – 4 year.

Vladimir Andreevich Didenko

978 7 minutes read