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Generic Tapazole ( Methimazole )
Tapazole (methimazole) is an antithyroid agent indicated for the treatment of hyperthyroidism, including Graves' disease, and for the preparation of hyperthyroid patients for thyroidectomy or radioactive iodine therapy. Methimazole works by inhibiting the enzyme thyroid peroxidase, thereby blocking the iodination of tyrosine residues in thyroglobulin and the coupling of iodotyrosines, which reduces the synthesis of thyroid hormones T3 and T4. It does not affect the release of preformed thyroid hormone, so clinical improvement may be delayed until existing hormone stores are depleted. Tapazole is available only by prescription in Canada.
Usual adult dose: For the initial treatment of hyperthyroidism, the usual dose is 15 mg to 60 mg per day in divided doses, depending on severity. Mild hyperthyroidism may be treated with 15 mg daily, moderate with 30 mg to 40 mg daily, and severe with 60 mg daily. The 5 mg and 10 mg tablets allow flexible dosing: for example, 10 mg three times daily, or 5 mg three times daily for milder disease. Doses are typically taken every 8 hours; once thyroid function is controlled (usually after 6 to 8 weeks), the dose may be reduced to a maintenance level of 5 mg to 15 mg per day, given as a single daily dose or in divided doses. Tapazole may be taken with or without food. If a dose is missed, it should be taken as soon as remembered, but two doses should not be taken at the same time. In patients with severe hepatic impairment or renal impairment, dose reduction may be required; the drug should be used with caution. Treatment duration is usually 12 to 18 months for Graves' disease, after which remission may be assessed.
Dosage form: Oral tablets: 5 mg (white, round, scored) and 10 mg (white, round, scored). The 5 mg tablet is used for fine dose adjustment and maintenance; the 10 mg tablet is used for higher initial and divided dosing. Available in bottles of 100 or 500 tablets.
Onset of action: Methimazole begins to inhibit thyroid hormone synthesis within hours of the first dose, but clinical improvement in symptoms such as tachycardia, tremor, and sweating may take 1 to 2 weeks because preformed hormone stores must be depleted. Thyroid function tests typically normalize after 6 to 8 weeks of continuous therapy.
Duration of action: The elimination half-life of methimazole is approximately 6 to 8 hours, but the antithyroid effect persists longer because of accumulation in the thyroid gland. Once-daily dosing is possible for maintenance, but initial therapy is usually divided every 8 hours. The therapeutic effect lasts as long as the drug is taken regularly; after discontinuation, thyroid hormone synthesis resumes within days to weeks.
Alcohol recommendation: No direct interaction between methimazole and alcohol has been clearly established. However, alcohol may worsen liver function, and methimazole can rarely cause hepatotoxicity. Patients with pre-existing liver disease or those who consume alcohol heavily should exercise caution and have liver function monitored. Moderation is advisable.
Most common side effects: Rash, pruritus, urticaria, nausea, vomiting, headache, and arthralgia. Mild leukopenia is common. The most serious adverse effect is agranulocytosis (severe neutropenia), which is rare (0.2% to 0.5%) but life-threatening; patients must be instructed to stop the drug immediately and seek medical attention if they develop fever, sore throat, or mouth ulcers. Other serious effects include hepatotoxicity (cholestatic jaundice, hepatitis), vasculitis, and aplastic anemia. Hypothyroidism may result from overtreatment and is managed by dose reduction or addition of levothyroxine. Methimazole is contraindicated in patients with known hypersensitivity to the drug, and it should not be used in the first trimester of pregnancy due to the risk of fetal anomalies; propylthiouracil is preferred during the first trimester. Patients should have baseline and periodic complete blood counts and liver function tests. Tapazole is available only by prescription in Canada and must be prescribed and monitored by a healthcare professional experienced in thyroid disorders.
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