Pharmacologic class: Thiomidazole derivative
Therapeutic class: Antithyroid drug
Pregnancy risk category D
Directly interferes with thyroid synthesis by preventing iodine from combining with thyroglobulin, leading to decreased thyroid hormone levels
Tablets: 5 mg, 10 mg
➣ Mild hyperthyroidism
Adults and adolescents: Initially, 15 mg P.O. daily in three equally divided doses at approximately 8-hour intervals. For maintenance, 5 to 15 mg/day in equally divided doses at approximately 8-hour intervals.
Children: Initially, 0.4 mg/kg/day in three divided doses at 8-hour intervals. For maintenance, approximately 0.2 mg/kg/day in three divided doses at 8-hour intervals.
➣ Moderate hyperthyroidism
Adults and adolescents: Initially, 30 to 40 mg P.O. daily in three equally divided doses at approximately 8-hour intervals. For maintenance, 5 to 15 mg/day in three equally divided doses at approximately 8-hour intervals.
Children: 0.4 mg/kg/day P.O. as a single dose or in divided doses at 8-hour intervals. For maintenance, approximately 0.2 mg/kg/day as a single dose or in three divided doses at 8-hour intervals.
➣ Severe hyperthyroidism
Adults and adolescents: Initially, 60 mg/day P.O. in three equally divided doses at approximately 8-hour intervals. For maintenance, 5 to 15 mg/day in three equally divided doses at approximately 8-hour intervals.
Children: Initially, 0.4 mg/kg/day P.O. as a single dose or in three divided doses at 8-hour intervals. For maintenance, approximately 0.2 mg/kg/day as a single dose or in three divided doses at 8-hour intervals.
• Hypersensitivity to drug
• Breastfeeding
Use cautiously in:
• bone marrow depression
• patients older than age 40
• pregnant patients.
• Give with meals as needed to reduce GI upset.
CNS: headache, vertigo, paresthesia, neuritis, depression, neuropathy, CNS stimulation
GI: nausea, vomiting, constipation, epigastric distress, ileus, salivary gland enlargement, dry mouth, anorexia
GU: nephritis
Hematologic: thrombocytopenia, agranulocytosis, leukopenia, aplastic anemia
Hepatic: jaundice, hepatic dysfunction, hepatitis
Metabolic: hypothyroidism
Musculoskeletal: joint pain, myalgia
Skin: rash, urticaria, skin discoloration, pruritus, erythema nodosum, exfoliative dermatitis, abnormal hair loss
Other: fever, lymphadenopathy, lupuslike syndrome
Drug-drug. Aminophylline, oxtriphylline, theophylline: decreased clearance of both drugs
Amiodarone, iodine, potassium iodide: decreased response to methimazole
Anticoagulants: altered requirements for both drugs
Beta-adrenergic blockers: altered beta blocker clearance
Digoxin: increased digoxin blood level
Drug-diagnostic tests. Granulocytes, hemoglobin, platelets, white blood cells: decreased values
• Check for agranulocytosis in patients older than age 40 and in those receiving more than 40 mg/day.
• Assess hematologic studies. Agranulocytosis usually occurs within first 2 months of therapy and is rare after 4 months.
• Monitor thyroid function tests periodically. Once hyperthyroidism is controlled, elevated thyroid-stimulating factor indicates need for dosage decrease.
• Assess liver function tests and check for signs and symptoms of hepatic dysfunction.
• Monitor patient for fever, sore throat, and other evidence of infection as well as for unusual bleeding or bruising.
• Assess patient for signs and symptoms of hypothyroidism, such as hard edema of subcutaneous tissue, drowsiness, slow mentation, dryness or loss of hair, decreased temperature, hoarseness, and muscle weakness.
• Tell patient to take with meals if GI upset occurs.
• Advise patient to take exactly as prescribed to maintain constant blood level.
• Tell patient to report rash, fever, sore throat, unusual bleeding or bruising, headache, rash, yellowing of skin or eyes, abdominal pain, vomiting, or flulike symptoms.
• Caution female patient not to breastfeed while taking drug.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs and tests mentioned above.