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Tapazole (Methimazole) - Summary



TAPAZOLE® (Methimazole Tablets, USP) (1-methylimidazole-2-thiol) is a white, crystalline substance that is freely soluble in water.

TAPAZOLE (METHIMAZOLE) is indicated for the following:

  • In patients with Graves' disease with hyperthyroidism or toxic multinodular goiter for whom surgery or radioactive iodine therapy is not an appropriate treatment option.
  • To ameliorate symptoms of hyperthyroidism in preparation for thyroidectomy or radioactive iodine therapy.

  • See all Tapazole indications & dosage >>


    Published Studies Related to Tapazole (Methimazole)

    The outcome of 131I treatment in Graves' patients pretreated or not with methimazole. [2011.01]
    Despite extensive use of iodine-131 ((131)I) treatment for Graves' hyperthyroidism, the optimal regimen of pretreatment with antithyroid drugs is still a matter of discussion. Our aim was to evaluate the success of (131)I treatment in patients with Graves' disease without and with pretreatment with methimazole (MMI).

    Comparison of methimazole and propylthiouracil in patients with hyperthyroidism caused by Graves' disease. [2007.06]
    CONTEXT: Although methimazole (MMI) and propylthiouracil (PTU) have long been used to treat hyperthyroidism caused by Graves' disease (GD), there is still no clear conclusion about the choice of drug or appropriate initial doses. OBJECTIVE: The aim of the study was to compare the MMI 30 mg/d treatment with the PTU 300 mg/d and MMI 15 mg/d treatment in terms of efficacy and adverse reactions... CONCLUSIONS: MMI 15 mg/d is suitable for mild and moderate GD, whereas MMI 30 mg/d is advisable for severe cases. PTU is not recommended for initial use.

    Continuous methimazole therapy and its effect on the cure rate of hyperthyroidism using radioactive iodine: an evaluation by a randomized trial. [2006.08]
    BACKGROUND: A randomized clinical trial was performed to clarify whether continuous use of methimazole (MTZ) during radioiodine ((131)I) therapy influences the final outcome of this therapy... CONCLUSION: Continuous use of MTZ hinders an excessive increase of the thyroid hormones during (131)I therapy of hyperthyroid diseases. However, such a strategy seems to reduce the final cure rate, although this adverse effect paradoxically is attenuated by the concomitant reduction of the thyroid (131)I uptake.

    Effect of long-term continuous methimazole treatment of hyperthyroidism: comparison with radioiodine. [2005.05]
    OBJECTIVE: To investigate the long-term effects of continuous methimazole (MMI) therapy... CONCLUSION: Long-term continuous treatment of hyperthyroidism with MMI is safe. The complications and the expense of the treatment do not exceed those of radioactive iodine therapy.

    Serum thyrotropin-receptor autoantibodies levels after I therapy in Graves' patients: effect of pretreatment with methimazole evaluated by a prospective, randomized study. [2004.10]
    OBJECTIVE: Radioiodine therapy (131I) in hyperthyroid Graves' disease is generally followed by a transitory increase in levels of thyrotropin receptors antibodies (TRAb). Immunosuppressive effects of antithyroid drugs are still a matter of debate. In this study we evaluated the effect of methimazole pretreatment on the TRAb boost induced by 131I. DESIGN: A randomized, prospective clinical trial... CONCLUSION: Methimazole pretreatment attenuates the 131I-induced rise in serum TRAb levels. The effects of methimazole could be attributed to a direct immunomodulatory action or may be due to its effects on the control of hyperthyroidism, which is a known cause of immune dysregulation.

    more studies >>

    Clinical Trials Related to Tapazole (Methimazole)

    Evaluation of Optimal Time of Methimazole Discontinuation Before Radio-iodine Therapy in Hyperthyroid Grave's Patients [Completed]
    Iodine therapy is the best treatment for graves disease. Most patients receive methimozale prior to radio-iodine treatment. This may decrease treatment response to iodine therapy. Some physicians advice to discontinue methimazole 3 days before radioiodine therapy and

    others prefer longer off - methimazole period which bothers most patients. This study aimed

    to evaluate optimum time for methimazole discontinuation in graves disease.

    Methimazole to Treat Polymyositis and Dermatomyositis [Completed]
    This study will test the safety and effectiveness of the drug methimazole in treating polymyositis and dermatomyositis-inflammatory muscle diseases causing weakness and muscle wasting. Although it is not known what causes of these diseases, abnormal immune function is thought to be involved. Recent studies indicate that methimazole, which has been used for many years to treat thyroid disease, may alter immune activity by affecting the interaction between white blood cells called lymphocytes and certain molecules on cell surfaces. This study will examine the effects of methimazole on immune activity and muscle strength in patients with inflammatory muscle diseases and evaluate the drug side effects. Patients with polymyositis and dermatomyositis who have normal thyroid function may be eligible for this study [age requirement?]. Candidates will undergo a history and physical examination; blood and urine tests; chest X-ray; muscle strength testing, daily living skills questionnaire, and speech and swallowing evaluation; magnetic resonance imaging of muscles; and muscle biopsy (removal of a small piece of muscle tissue under local anesthetic). When indicated, some candidates may also have cancer screening tests (for example, mammogram, Pap smear), a lung function test to measure breathing capacity, or an electromyogram, in which small needles are inserted into a muscle to measure the electrical activity . Participants will take 30 mg of methimazole by mouth twice a day for 6 months. They will have blood tests weekly for the first 2 weeks and then every other week for the rest of the study to measure blood counts and liver and thyroid function. Blood will also be drawn for white blood cell studies during the screening evaluation, at the beginning of therapy, 6 to 12 weeks after therapy starts, at the end of the 6-month treatment period, and 1 and 3 months after therapy ends. Muscle enzyme and urine tests will be done once a month.. During drug treatment, patients will have periodic physical examinations and blood and muscle function tests to evaluate the response to therapy.

    Block-replacement Therapy During Radioiodine Therapy [Completed]
    Background: The use of radioactive iodine (131I) therapy as the definite cure of hyperthyroidism is widespread. According to a survey on the management of Graves' disease, thirty per cent of physicians prefer to render their patients euthyroid by antithyroid drugs (ATD) prior to 131I therapy. This strategy is presumably chosen to avoid 131I induced 'thyroid storm', which, however, is rarely encountered. Several studies have consistently shown that patients who are treated with ATD prior to 131I therapy have an increased risk of treatment failure. Mostly, patients with Graves' disease have been studied, while other studies were addressed also toxic nodular goiter. Thus, it is generally accepted that ATD have 'radioprotective' properties, although this view is almost exclusively based on retrospective data and is still under debate. Indeed, this dogma was recently challenged by two randomized trials in Graves' disease, none of which showed such an adverse effect of methimazole pretreatment. It cannot be excluded that the earlier results may have been under influence of selection bias, a source of error almost unavoidable in retrospective studies. Whether ATD is radioprotective also when used in the post 131I period has also been debated. In the early period 131I therapy following a transient rise in the thyroid hormones is seen which may give rise to discomfort in some patients. The continuous use of ATD during 131I therapy, possibly in combination with levothyroxine (BRT: block-replacement therapy), leads to more stable levels of the thyroid hormones. By resuming ATD following 131I therapy, euthyroidism can usually be maintained until the destructive effect of 131I ensues. Nevertheless, many physicians prefer not to resume ATD, probably due to reports supporting that such a strategy reduces the cure rate. Parallel to the issue of ATD pretreatment, the evidence is based on retrospective studies and the ideal set-up should be reconsidered. To underscore the importance of performing randomized trials we showed recently that resumption of methimazole seven days after 131I therapy had no influence on the final outcome. Aim: To clarify by a randomized trial whether BRT during radioiodine therapy of hyperthyroid patients influences the final outcome of this therapy, in a comparison with a regime in which methimazole as mono-therapy is discontinued 8 days before radioiodine. Patients and Methods: Consecutive patients suffering from recurrent Graves' disease (n=50) or a toxic nodular goiter (n=50) are included. All patients are rendered euthyroid by methimazole (MMI) and randomized either to stop MMI eight days before 131I or to be set on BRT. This latter medication continues until three months after 131I. Calculation of the 131I activity (max. 600 MBq) includes an assessment of the 131I half-life and the thyroid volume. Patients are followed for one year with close monitoring of the thyroid function.

    Prevention Relapse of Graves' Disease by Intrathyroid Injection of Dexamethasone [Completed]
    Antithyroid drugs are widely used in treatment of Graves' disease (GD), but after therapy withdrawal, relapse rate is very high. The aim this trail is to evaluate the effects of intrathyroid injection of dexamethasone combined with antithyroid drugs on patients with newly diagnosed GD.

    Adjuvant Treatment of Graves┬┤ Ophthalmopathy With NSAID (aGO Study) [Active, not recruiting]

    AGO study - adjuvant treatment, with NSAID, of endocrine ophthalmopathy in Graves┤


    Background - Already at diagnosis of Graves disease approximately 98% of the patients have

    morphological changes of the retrobulbar tissue concordant with ophthalmopathy. Factors known to induce clinical symptoms of ophthalmopathy are mainly unknown. An interesting observation is that a patient with stable and inactive Graves┤ disease developed ophthalmopathy when treated with a glitazone due to diabetes type 2. Glitazones have been shown to increase differentiation of orbital preadipocytes to mature adipocytes. Glitazones are PPAR-gamma agonists and recently diclofenac have been shown to interact with PPAR-gamma in physiological concentrations. Other non-steroidal antiinflammatory drugs, NSAID, like indomethacin lack this effect. In addition, diclofenac inhibit synthesis of prostaglandins which also may be of importance because the natural ligand to PPAR-gamma is prostaglandin J. Inflammation and adipogenesis are hallmarks of the pathological process in Graves ophthalmopathy and NSAID like diclofenac may affect both. There is only one earlier study demonstrating effects of NSAID (indomethacin) in 7 patients with effects on soft tissue symptoms, eye muscle symptoms and eye protrusion.

    Aim - to investigate if diclofenac can prevent ophthalmopathy and/or progress of

    ophthalmopathy. Specific aims: 1. To study the frequency of clinical ophthalmopathy in Graves┬┤ disease after 12 months treatment with or without diclofenac. 2. To study the frequency of progress of clinical signs and symptoms in ophthalmopathy after 12 months treatment with or without diclofenac. 3. To study the frequency of optic neuropathy in clinical ophthalmopathy after 12 months treatment with or without diclofenac.

    Study plan and randomisation -

    150 patients with newly diagnosed Graves┬┤disease without ophthalmopathy will be treated with anti-thyroid drugs and L-thyroxin (block and replace) according to clinical routine for 18 months. These patients will be randomized to diclofenac 50 mg twice daily or not for 12 months.

    more trials >>

    Reports of Suspected Tapazole (Methimazole) Side Effects

    Headache (7)Malaise (4)Product Tampering (4)Pyrexia (3)Dyspepsia (3)White Blood Cell Count Decreased (3)Nausea (3)Feeling Abnormal (3)Weight Decreased (2)Immunoglobulins Abnormal (2)more >>


    Based on a total of 2 ratings/reviews, Tapazole has an overall score of 8.50. The effectiveness score is 9 and the side effect score is 10. The scores are on ten point scale: 10 - best, 1 - worst.

    Tapazole review by 49 year old female patient

    Overall rating:  
    Effectiveness:   Highly Effective
    Side effects:   No Side Effects
    Treatment Info
    Condition / reason:   hyperthyroidism
    Dosage & duration:   20 mg taken once a day for the period of 3 months
    Other conditions:   none
    Other drugs taken:   none
    Reported Results
    Benefits:   My hyperthyroidism is in remission 9 months after stopping the drug. I had no side effects and even my thyroid nodules are gone. Pretty amazing!!
    Side effects:   None - I felt no different at all
    Comments:   I took the tapazole daily along with atenolol for the shaking and heart racing I was experiencing. I am completely drug free for 9 months and the thyroid is fine. I am so glad I didn't let the doctors irradiate the gland to ablate it. I would have had to be on synthoid forever.


    Tapazole review by 33 year old female patient

    Overall rating:  
    Effectiveness:   Considerably Effective
    Side effects:   No Side Effects
    Treatment Info
    Condition / reason:   hyperthyroidism
    Dosage & duration:   10mg taken 1bid for the period of 18 months
    Other conditions:   hyperthyroid associated high blood pressure
    Other drugs taken:   none
    Reported Results
    Benefits:   the drug was effective in reducing high thyroid hormone levels
    Side effects:   none
    Comments:   tapazole was used to lower high thyroid hormone levels which provided immediate relief of high blood pressure, heart palpitations, hot flashes and gastrointestinal issues associated with high thyroid hormone levels. Combined with natural/homeopathic treatment, I am now in remission from autoimmune related hyperthryoidism (Grave's Disease)

    See all Tapazole reviews / ratings >>

    Page last updated: 2011-12-09

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