Introduction
Illustrated mechanism of action
Examples of Medication Brand Names (with Images)
Indication
Side Effects
Precautions & Contraindications
Monographs
Reference
Antithyroid medications are a class of drugs primarily used to treat hyperthyroidism, a condition in which the thyroid gland overproduces the hormones triiodothyronine (T3) and thyroxine (T4). These hormones regulate metabolism, heart rate, and body temperature, so excess levels can cause significant health issues.
The main goal of antithyroid therapy is to restore normal thyroid function (euthyroidism) by reducing hormone synthesis. This is especially important in autoimmune disorders like Graves’ disease, where antibodies stimulate the thyroid to produce more hormones. Antithyroid drugs are often the first-line treatment, particularly in younger patients and those with mild to moderate disease.
There are two main medications in this class:
•Methimazole (MMI) – the most commonly used due to better efficacy and safety profile
•Propylthiouracil (PTU) – reserved for specific situations, like early pregnancy or thyroid storm
These medications are usually prescribed as long-term therapy (12–18 months) to achieve remission or as a bridge to definitive treatments such as radioactive iodine therapy or surgery.
MOA
• Both Methimazole (MMI) and Propylthiouracil (PTU) inhibit thyroid peroxidase, blocking:
• Iodide oxidation
• Iodination of tyrosine residues
• Coupling of iodotyrosines
• PTU also inhibits peripheral conversion of T4 to T3, making it useful in thyroid storm.
Examples of Medication Brand Names
•Methimazole: Tapazole
•Propylthiouracil (PTU): PTU
Indication
• Treatment of hyperthyroidism
• Graves’ disease
• Pre-operative preparation before thyroid surgery
• Temporary use during pregnancy (depending on trimester)
Side Effects
•Skin rash, itching
•Elevated liver enzymes
•Agranulocytosis (a serious condition)
•Hepatitis (more common with PTU)
Precautions & Contraindications
Precautions:
•Regular monitoring: CBC, LFTs, TFTs
•Educate patients on warning signs (fever, sore throat)
Contraindications:
•Previous severe reaction (e.g., agranulocytosis)
•Severe liver disease (PTU especially)
•Known hypersensitivity to the drug
Monographs
Reference
•Katzung’s Basic & Clinical Pharmacology
•Goodman & Gilman’s: The Pharmacological Basis of Therapeutics
•Drugs.com
•Medscape