Espa-Carb 10mg 50 tablets — Made in Germany — Free Delivery

Pharmacological properties

Pharmacodynamics. Carbimazole, depending on the dosage, inhibits the incorporation of iodine into tyrosine, and, consequently, the additional synthesis of thyroid hormones. this property makes possible symptomatic therapy of hyperfunction of the thyroid gland, regardless of its etiology. Whether carbimazole, in addition, affects the natural course of the disease in an immunologically determined form of hyperthyroidism (Graves' disease), that is, whether it slows down the immunopathogenetic process that underlies the disease, is currently impossible to determine with complete certainty. carbimazole does not affect the release of already synthesized thyroid hormones. this explains in some cases the different duration of the latent period of the preparation action until the normalization of the concentration of thyroxine and triiodothyronine in the blood plasma, that is, until the clinical improvement of the condition. the preparation also does not affect hyperthyroidism due to the release of hormones after the destruction of thyroid cells, for example, after radiotherapy or with thyroiditis.

Pharmacokinetics. Carbimazole is rapidly and completely absorbed and immediately after absorption is converted into its active form - thiamazole. After taking 15 mg of carbimazole for 24–72 minutes, the maximum plasma level is reached - 150 ng / nl.

The binding of thiamazole to blood plasma proteins can be neglected. Thiamazole accumulates in the thyroid gland, where it is slowly metabolized and, since the duration of its action is directly more related to the concentration of the substance in the thyroid gland than to its T½ from plasma, this leads to an increase in antithyroid activity. This predetermines the almost 24-hour duration of the action of a single dose and makes it possible to use the preparation once a day. The kinetics of thiamazole, according to currently available data, does not depend on the state of the thyroid gland.

T½ from the body is about 3 hours, with insufficient liver function, it lengthens. Thiamazole is excreted in both urine and bile. But biliary excretion is insignificant, which makes it possible to conclude about enterohepatic circulation. The kidneys excrete 70% of thiamazole for 24 hours, of which only a small amount is unchanged. There are currently no data on the pharmacological activity of metabolites.

Indications

Dysfunction of the thyroid gland associated with overproduction of its hormones (hyperthyroidism). preparation for thyroidectomy for hyperthyroidism. therapy before and after treatment with radioactive iodine.

Application

Espa-carb is used only for hyperthyroidism, which has been confirmed by laboratory tests.

Adults. The dose at the beginning of treatment should be 20-60 mg, which must be titrated depending on the function of the thyroid gland until the patient is euthyroid, in order to reduce the risk of over-treatment and, as a result, hypothyroidism. Further treatment is carried out in one of two ways.

Maintenance therapy: The final dose is usually 5-15 mg / day, which can be taken as a single daily dose. The therapy is continued for at least 6-18 months. Continuous monitoring of thyroid function at the same time as appropriate dose selection is recommended to maintain the euthyroid state.

Block-replacement regimen: initial doses of 20–60 mg / day are maintained, and levothyroxine sodium 50–150 mcg / day is additionally prescribed to prevent hypothyroidism. The therapy lasts for at least 6-18 months.

Elderly patients. If there are no contraindications or warnings, then such patients do not require special dosing.

Contraindications

Individual hypersensitivity to carbimazole, thiamazole or other components of the preparation. severe disorders of the blood system, severe hepatic failure, cholestasis. simultaneous use of radioactive iodine preparations. additional therapy with the use of thyroid hormones during pregnancy.

Side effects

The frequency analysis of the occurrence of side effects identified the following categories: very often (≥10%); often (≥1% –10%); infrequently (≥0.1% –1%); rarely (≥0.01% –0.1%); very rarely (0.01%); unknown (frequency not estimated due to lack of data).

On the part of the blood and lymphatic system

Uncommon: about 0.3-0.6% of cases develop agranulocytosis, which can also occur weeks or months after the start of therapy and forces you to stop taking the preparation. In most cases, agranulocytosis disappears spontaneously. For the treatment of preparation-induced agranulocytosis, the latest data confirm the use of factors for stimulating granulocyte colonies (granulocyte colony-stimulating factor filgrastim). However, the use of such factors should be done in consultation with the hematologist.

Very rare: thrombocytopenia, pancytopenia, aplastic anemia, hemolytic anemia.

From the endocrine system

Due to increased dosage, subclinical or clinical hypothyroidism may occur, as well as the growth of goiter, which is associated with an increase in the level of thyroid-stimulating hormone (TSH). In this regard, after reaching the euthyroid state, the dose of Espa-carb should be reduced and / or additionally applied with levothyroxine sodium. It is inappropriate to completely stop taking the preparation Espa-carb and continue therapy with thyroid hormones.

An increase in goiter during therapy with Espa-carb with a suppressed TSH level should be perceived as a consequence of the underlying disease and should not be treated with additional intake of thyroid hormones.

After a single thyrostatic therapy, there is a negligible incidence of post-hypothyroidism. In such cases, we are not talking about the side effect of the preparation, but about the inflammatory and destructive processes in the parenchyma of the thyroid gland within the framework of the underlying disease.

On the part of the organs of vision

It is possible that endocrine orbitopathy may develop or worsen regardless of the course of thyroid disease: such a complication, in itself, is not a reason for changing the therapeutic program (thyreostatics, surgery, radioactive iodine), and should not be perceived as a side effect of qualified therapy.

From the nervous system: headache.

From the digestive tract: nausea, minor gastrointestinal disturbances.

General disorders: fever, malaise, bruises.

Uncommon: preparation  fever, taste disturbances (dysgeusia, ageusia) or smell disturbances that disappear after stopping treatment, and normalization may take several weeks.

Very rare: arthralgia and myalgia, which usually develop slowly and continue after many months of prolonged therapy. There are no clinical signs of joint inflammation.

Generalized lymphadenopathy, arthritis, nephritis, acute swelling of the salivary gland, vasculitis, neuritis and polyneuropathy, insulin-autoimmune syndrome (with a pronounced decrease in blood glucose levels).

When taking Espa-carb, due to a reduction in the pathologically increased energy requirement in hyperthyroidism, an increase in body weight (in general, the desired) may occur. Patients should be advised that with an improvement in the picture of the disease, the energy requirement of the body is normalized.

From the hepatobiliary system

Very rare: cholestatic jaundice or toxic hepatitis. In general, symptoms disappear after the preparation is discontinued. Clinically latent signs of cholestasis during treatment should be distinguished from the already increased activity of gamma-glutamyltransferase in blood plasma before the start of therapy as a sign of enzyme induction due to hyperthyroidism, as well as an increase in alkaline phosphatase or its bone isoenzymes.

On the part of the skin and its derivatives

Very often: allergic skin manifestations (itching, rash, urticaria) of a periodic nature. In most cases, they are mild and often disappear with continued therapy.

Very rare: severe manifestations of generalized dermatitis. Hair loss, preparation-induced lupus erythematosus.

From the musculoskeletal system: in isolated cases - myopathy. In patients who develop muscle pain after treatment with carbimazole, the CPK level should be constantly monitored.

Hypersensitivity reactions: Quincke's edema, multisystem hypersensitivity reactions (cutaneous vasculitis, reactions from the liver, lungs and kidneys).

From the side of the vessels: bleeding.

Special instructions

If the first signs and symptoms of liver dysfunction occur (pain in the upper abdomen, lack of appetite, general itching), the preparation should be discontinued and liver function should be monitored immediately.

Carbimazole should be used with caution in patients with mild to moderate hepatic impairment.

In case of severe liver dysfunction, treatment should be discontinued. T½ can increase with impaired liver function.

During the appointment of radioactive iodine for this period, treatment with carbimazole should be discontinued.

Patients who cannot follow instructions for the use of the preparation or cannot be examined regularly should not take carbimazole.

Blood tests should be done regularly in patients who may have seizures or memory impairment.

Patients with rare hereditary forms of galactose intolerance, lactase deficiency or glucose-galactose malabsorption syndrome should not take this preparation.

Precautions are needed in patients with intrathoracic goiter, which may worsen initial treatment with carbimazole. Tracheal obstruction can occur due to intrathoracic goiter.

The use of carbimazole in non-pregnant women of reproductive age is possible only when assessing the risk / benefit.

There is a risk of cross-allergy between carbimazole, thiamazole and propylthiouracil.

Use during pregnancy and lactation. Carbimazole crosses the placenta. If the mother's dose is within the standard range and her thyroid condition is monitored, there is no evidence of a neonatal thyroid disorder. Studies have noted that the incidence of congenital malformations is higher in those children whose mothers had untreated hyperthyroidism than those who received carbimazole therapy.

However, very rarely, congenital developmental defects were noted after the use of carbimazole or its active metabolite methimazole during pregnancy. The relationship between the occurrence of malformations, in particular choanal atresia and congenital aplasia of cutis, is possible, which cannot be excluded with the transplacental effect of carbimazole and methimazole. Thus, the use of carbimazole during pregnancy and in women of reproductive age is possible only when the expected benefit to the mother outweighs the potential risk to the fetus.

There have also been reports of dysfunction of the kidneys, skull, congenital malformations of the cardiovascular system, umbilical hernia, gastrointestinal malformations, navel malformations, and duodenal atresia. Therefore, carbimazole should be given during pregnancy only when propylthiouracil is not appropriate. If carbimazole is to be used during pregnancy, the dose should be adjusted depending on the patient's clinical condition. You can use the preparation in low doses and stop treatment 3-4 weeks before delivery to reduce the risk of neonatal complications. It is impossible to stop treatment during pregnancy, since a very small amount of thyroxine crosses the placenta in the last trimester of pregnancy.

Additional treatment with thyroid hormones is prohibited (the blocking-replacement scheme is not applied, since a small amount of thyroxine can pass through the placenta in the last trimester of pregnancy).

During therapy with carbimazole, it is possible to continue feeding, however, it is allowed to take it only in low doses (up to 10 mg / day) without additional intake of thyroid hormones. In this case, it is necessary to monitor the function of the child's thyroid gland.

Children. There is not enough experience with the use of carbimazole in children, therefore, the preparation is not prescribed to patients of this age group.

The ability to influence the reaction rate when driving and operating other mechanisms. The effect on the ability to drive vehicles or work with other mechanisms is unknown.

Interactions

There is insufficient data on the interaction of carbimazole with other preparations. carbimazole should be used with caution with agents that may cause agranulocytosis. since carbimazole is a vitamin K antagonist, the effect of anticoagulants may be enhanced. it is possible to increase the level of theophylline in the blood plasma and develop toxicity if patients receive therapy with antithyroid preparations without reducing the dose of theophylline. there is a risk of cross-allergy between carbimazole, thiamazole and propylthiouracil.

Overdose

Overdose cases are not described.

Storage conditions

In its original packaging at a temperature not exceeding 25 ° C.