Espa-carb (carbimazole) tablets 10 mg. №50

Description

Espa-carb Storage
active substance: carbimazole;

1 tablet contains carbimazole 5 mg or 10 mg;

Espa-carb excipients:

tablets of 5 mg of mannitol (E 421), microcrystalline cellulose, corn starch, anhydrous citric acid, sodium starch glycolate (type A), magnesium stearate;

tablets of 10 mg of mannitol (E 421), microcrystalline cellulose, corn starch, anhydrous citric acid, sodium starch glycolate (type A), magnesium stearate, iron oxide yellow (E 172);

Espa-carb Dosage form
Tablets.

Basic physical and chemical properties:

5 mg round, convex white tablets with a score line on one side;

tablets of 10 mg round, convex tablets of yellowish color with a dividing line on one side.

Pharmacotherapeutic group
Antithyroid drugs. Sulfur-containing imidazole derivatives.

ATX code H03B B01.

Pharmacological properties

Pharmacodynamics.

Carbimazole, depending on its dosage, inhibits the incorporation of iodine into tyrosine, and hence the additional synthesis of thyroid hormones. This property allows symptomatic therapy of hyperthyroidism, regardless of its etiology. Whether carbimazole, in addition, affects the natural course of the disease in immunologically determined form of hyperthyroidism (base disease), ie whether it inhibits the immunopathogenetic process underlying the disease, at this time it is impossible to determine with certainty. It does not affect the secretion of already synthesized thyroid hormones. This explains in some cases the different duration of the latent period of the drug to normalize the concentration of thyroxine and triiodothyronine in the serum, ie to clinical improvement. The drug also does not affect hyperthyroidism due to the release of hormones after the destruction of thyroid cells, for example, after radiotherapy or 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 serum level is reached -150 ng / nl.

Protein binding of thiamazole can be neglected. Thiamazole accumulates in the thyroid gland, where it is only slowly metabolized, and because its duration of action is more directly related to the concentration of the substance in the thyroid gland than to its plasma half-life, this leads to a prolongation of antithyroid activity. This causes an almost 24-hour duration of action of a single dose and allows you to use the drug once a day. The kinetics of thiamazole, according to currently available information, does not depend on the state of thyroid function.

The half-life from the body is about 3 hours, with insufficient liver function, it is greater. Thiamazole is excreted in both urine and bile. But fecal excretion is insignificant, which allows us to conclude about enterohepatic circulation. The kidneys excrete 70% of thiamazole within 24 hours, of which only a small amount is unchanged. There is currently no information on the pharmacological activity of metabolites.

Indication
Thyroid dysfunction associated with hyperproduction of its hormones (hyperthyroidism).

Preparation for thyroidectomy for hyperthyroidism.

Therapy before and after treatment with radioactive iodine.

Contraindication
Hypersensitivity to individual carbimazole, thiamazole or to other components of the drug.

Severe disorders of the blood system, severe liver failure, cholestasis.

Simultaneous use of radioactive iodine preparations.

Additional therapy with the use of thyroid hormones during pregnancy.

Acute pancreatitis in the history after taking carbimazole or thiamazole.