Medications for Hyperthyroidism
Primary Treatment Options
Hyperthyroid patients typically take antithyroid drugs—either methimazole or propylthiouracil—to block excessive thyroid hormone synthesis, with methimazole being the preferred first-line agent in most cases. 1, 2, 3
Methimazole (Preferred Agent)
- Initial dosing: 15 mg daily for mild hyperthyroidism, 30-40 mg daily for moderate disease, and 60 mg daily for severe hyperthyroidism, divided into 3 doses at 8-hour intervals 1
- Maintenance dosing: 5-15 mg daily once control is achieved 1
- Methimazole is the drug of choice due to its longer half-life, once-daily dosing capability, and lower incidence of severe side effects compared to propylthiouracil 4
- Single daily dosing is effective in most patients, with euthyroid state typically achieved in approximately 16-17 weeks 5
Propylthiouracil (Alternative Agent)
- Initial dosing: 300 mg daily in divided doses; may increase to 400 mg daily for severe hyperthyroidism or very large goiters, with occasional patients requiring 600-900 mg daily 2
- Maintenance dosing: 100-150 mg daily 2
- Generally not recommended as first-line except in specific situations: first trimester of pregnancy, thyroid storm, or patients with severe reactions to methimazole 2, 3
- Propylthiouracil carries higher risk of severe hepatotoxicity, particularly at doses of 300 mg/day or higher 2
Treatment Duration and Strategy
- Antithyroid drugs are typically prescribed for 12-18 months with the goal of inducing long-term remission in Graves' disease 6, 7
- Recurrence after standard 12-18 month treatment occurs in approximately 50% of patients 7
- Long-term treatment (5-10 years) is associated with fewer recurrences (15%) compared to short-term treatment 7
- Antithyroid drugs are also used short-term to render patients euthyroid before definitive therapy with radioiodine or thyroidectomy 6
Adjunctive Medications
Beta-Blockers
- Used as second-line agents to control hyperthyroid symptoms (tachycardia, tremor, anxiety) while awaiting antithyroid drug effect 4
Corticosteroids
- Reserved for severe cases of destructive thyrotoxicosis (subacute thyroiditis) 7
- May be used as prophylaxis when radioiodine is administered to patients with Graves' ophthalmopathy 6
Other Second-Line Agents
- Potassium perchlorate, iodine, and lithium carbonate are rarely used alternatives 4
Disease-Specific Considerations
Graves' Disease (70% of hyperthyroidism cases)
- Antithyroid drugs are the preferred initial treatment 7
- Risk factors for recurrence include: age <40 years, FT4 ≥40 pmol/L, TSH-binding inhibitory immunoglobulins >6 U/L, and goiter size ≥WHO grade 2 7
Toxic Nodular Goiter (16% of cases)
- Antithyroid drugs will not cure this condition—they only provide temporary control 6
- Radioiodine is the treatment of choice for definitive management 6
Critical Safety Considerations
- Pediatric use: Propylthiouracil is generally not recommended in children except when alternative therapies are inappropriate; methimazole is preferred 2
- Pregnancy: Propylthiouracil is preferred in the first trimester due to lower risk of congenital anomalies 2
- Hepatotoxicity monitoring: Both drugs require monitoring, but propylthiouracil carries significantly higher risk of severe liver injury 2
- Most patients with hyperthyroidism will eventually require definitive treatment with radioiodine ablation (most common in the United States) or thyroidectomy, as antithyroid drugs alone rarely provide permanent cure 3, 6