Methimazole Treatment for Hyperthyroidism
For hyperthyroidism treatment, methimazole should be administered at an initial daily dose of 15 mg for mild disease, 30-40 mg for moderate disease, and 60 mg for severe disease, typically given as a single daily dose. 1
Dosing Guidelines
Initial Dosing
- For adults with mild hyperthyroidism: 15 mg daily 1
- For adults with moderately severe hyperthyroidism: 30-40 mg daily 1
- For adults with severe hyperthyroidism: 60 mg daily 1
- For pediatric patients: 0.4 mg/kg of body weight daily 1
Administration
- While the FDA label recommends dividing the total daily dose into three equal portions given at 8-hour intervals 1, more recent evidence supports using methimazole as a single daily dose due to its prolonged intrathyroidal effect 2, 3
- Single daily dosing has shown equal efficacy to divided doses with potentially fewer side effects 2
- Intrathyroidal concentrations of methimazole are maintained for at least 26 hours, supporting once-daily administration 3
Maintenance Dosing
- Adult maintenance dose: 5-15 mg daily 1
- Pediatric maintenance dose: Approximately half of the initial dose 1
- Dose adjustments should be made based on thyroid function tests, typically every 4-6 weeks 4
Monitoring
- TSH and Free T4 should be used for case detection and monitoring in symptomatic patients 4
- For asymptomatic patients on therapy, TSH can be checked every 4-6 weeks 4
- After initiating treatment, monitor thyroid function every 2-3 weeks to catch potential transition to hypothyroidism 4
- T3 levels can be helpful in highly symptomatic patients with minimal FT4 elevations 4
Special Considerations
Pregnancy
- Both methimazole and propylthiouracil (PTU) have similar therapeutic efficacy and placental transfer kinetics 5
- However, methimazole use in pregnancy has been associated with rare congenital anomalies (aplasia cutis and choanal/esophageal atresia) 5
- Therefore, PTU is generally preferred during pregnancy, particularly in the first trimester 5
- Women treated with methimazole can safely breastfeed 4, 5
Graves' Disease
- Consider TSH receptor antibody testing if there are clinical features suggestive of Graves' disease (e.g., ophthalmopathy, T3 toxicosis) 4
- Physical examination findings of ophthalmopathy or thyroid bruit are diagnostic of Graves' disease and should prompt early endocrine referral 4
- Graves' disease is generally persistent and may require longer-term therapy 4
Thyroid Storm
- In severe cases or thyroid storm, hospitalization is recommended 4
- Treatment includes methimazole or propylthiouracil, beta-blockers, potassium iodide solutions, and supportive care 4
- General supportive measures including oxygen, antipyretics, and appropriate monitoring are also important 4
Side Effects and Safety
- Major side effects include agranulocytosis, hepatitis, vasculitis, and thrombocytopenia 5
- Agranulocytosis typically presents with sore throat and fever - if these develop, obtain a complete blood count and discontinue the medication 4
- Single daily dosing may be associated with fewer adverse effects compared to divided dosing 2
- Research has shown that doses above 15 mg/day do not significantly increase intrathyroidal concentrations of methimazole, suggesting 15 mg/day may be the most satisfactory dose for treating hyperthyroidism in many cases 3