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Pharmacology · Hormone preparations, their synthetic substitutes, and antagonists

Drugs for thyroid disease

Pharmacological correction of thyroid disorders is based on the use of two functionally opposite groups of drugs. The choice of a specific agent depends on whether there is a need to compensate for a deficiency of endogenous hormones or, conversely, to suppress their excessive production.

Replacement therapySynthetic analogues of natural hormones (T3 and T4) are used.
Target of antithyroid drugsThe enzyme thyroid peroxidase, which is involved in hormone synthesis.
Goitrogenic effectEnlargement of the gland (goiter) during the administration of antithyroid agents.
Role of TSHHypersecretion of TSH by the pituitary gland stimulates the growth of thyroid tissue.
2 min readFor medical studentsUpdated 09/24/2026
Material prepared by WhiteCoat Pro editorial team based on platform study guidesReviewed by medical editor: Aulov A. A., general practitioner · 09/24/2026

Classification of agents affecting thyroid function

All medicinal substances affecting the functional activity of the thyroid gland can be divided into two main groups that exert directly opposite effects on the patient's body:

  1. Thyroid hormone preparations — used as replacement therapy for hypofunction.
  2. Antithyroid agents (thionamides) — used to suppress excessive hormone synthesis.

Replacement therapy: hormone preparations

This group of drugs is intended to compensate for the deficiency of endogenous thyroid hormones. Synthetic analogues of natural compounds are used in clinical practice:

  • Levothyroxine — a synthetic analogue of the T4 hormone.
  • Liothyronine — a synthetic analogue of the T3 hormone.
  • Combination preparations — contain several active components simultaneously to more closely mimic the natural secretion of the gland.
Test your knowledge on the topicTasks from the «Pharmacology» course bank — instant answers and explanations.

Antithyroid agents (Thionamides)

Antithyroid drugs are prescribed for conditions accompanied by thyroid hyperfunction. The main representative of this group is Thiamazole (also known by the brand name Mercazolil).

Mechanism of action: The action of thiamazole is based on inhibiting the activity of a specific enzyme, thyroid peroxidase. Blockade of this enzyme leads to disruption of the iodination of tyrosine residues within the thyroglobulin protein molecule. As a result of this cascade of reactions, the synthesis of the main thyroid hormones — T3 and T4 — is critically impaired and halted.

Side effects: goitrogenic effect

The most characteristic and clinically significant side effect of antithyroid drugs (particularly thiamazole) is the goitrogenic effect — a pathological enlargement of the thyroid gland leading to the formation of goiter.

Mechanism of the goitrogenic effect: The development of goiter is explained by the physiological principle of negative feedback. During the administration of antithyroid drugs, there is a sharp drop in the levels of circulating thyroid hormones (T3 and T4). The body responds to this deficiency with hypersecretion of TSH (thyroid-stimulating hormone) by the pituitary gland. Excess TSH exerts a powerful stimulating effect on thyroid tissue, provoking its compensatory growth and hyperplasia.

Briefly: answers to topical questions

What are the indications for prescribing levothyroxine, apart from replacement therapy for hypothyroidism?

  • Suppressive hormone therapy (levothyroxine sodium suppressive hormone therapy) — indicated in intermediate-risk groups, biochemical recurrence, and indeterminate tumor status in differentiated thyroid cancer to improve survival rates.
How to memorize

To memorize the mechanism of antithyroid drugs: Thiamazole Inhibits Thyroid peroxidase — T3 and T4 are Terminated — TSH Triggers Tissue growth (goiter).

Class and exam questions

What drugs are used for the replacement therapy of thyroid diseases?

Replacement therapy utilizes levothyroxine (synthetic T4), liothyronine (synthetic T3), and their combinations.

What is the mechanism of action of thiamazole?

Thiamazole inhibits the enzyme thyroid peroxidase, which blocks the iodination of thyroglobulin tyrosine residues and disrupts T3 and T4 synthesis.

Why can goiter develop when taking antithyroid drugs?

A decrease in T3 and T4 levels causes pituitary TSH hypersecretion via a feedback mechanism. High TSH levels stimulate the proliferation of thyroid tissue (goitrogenic effect).

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What else to study on this topic

  • The role of thyroglobulin in hormone storage
  • The relationship between ACTH and endocrine regulation
  • Pharmacokinetics of levothyroxine and liothyronine
  • Features of the use of combined T3 and T4 preparations

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