Efficacy of single daily dosage of methimazole <i>vs.</i> propylthiouracil in the induction of euthyroidism

Homsanit, Mayuree; Sriussadaporn, Sutin; Vannasaeng, Sathit; Peerapatdit, Thavatchai; Nitiyanant, Wannee; Vichayanrat, A

doi:10.1046/j.1365-2265.2001.01239.x

Cited by 38 publications

(21 citation statements)

References 20 publications

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“…Maximal clinical responses are seen after 4 --6 weeks, when the dose can be reduced by 30 --50% or more in order to achieve a euthyroid state [4,35]. The relative potency of both drugs has been also evaluated in several comparative trials in adults [36,37]. While the potency of MMI has been estimated about 10 times that of PTU, more recent data propose an even greater ratio, possibly up to 50:1.…”

Section: Antithyroid Drugsmentioning

confidence: 96%

Toxicological considerations for antithyroid drugs in children

Karras¹,

Tzotzas²,

Krassas

2011

Expert Opinion on Drug Metabolism & Toxicology

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The FDA recently reported that use of PTU is associated with a higher risk for clinically serious or fatal liver injury compared to MMI in both adult and pediatric patients. They also found that congenital malformations were reported approximately three times more often with prenatal exposure to MMI compared with PTU and especially with the use of MMI during the first trimester of pregnancy. The authors believe that PTU should not be used in pediatric patients unless the patient is allergic to or intolerant of MMI, and there are no other treatment options available. That being said, PTU may be the treatment of choice during, and just before, the first trimester of pregnancy.

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Section: Antithyroid Drugsmentioning

confidence: 96%

Toxicological considerations for antithyroid drugs in children

Karras¹,

Tzotzas²,

Krassas

2011

Expert Opinion on Drug Metabolism & Toxicology

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“…Arbeiten von Okamura et al [16] sowie von Homsanit [9] zeigen außerdem, dass sich bei hyperthyreoter Stoffwechsellage sowohl T 3 als auch T 4 unter einer Therapie mit Thiamazol im Vergleich zu PTU rascher normalisieren und die Euthyreose in einem signifikant kürzeren Zeitraum zu erreichen ist.…”

Section: Thyreostatische Therapieunclassified

Prävention und multimodale Therapie der Hyperthyreose

Palitzsch

2008

Internist

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Subclinical and overt hyperthyroidism have been associated with various negative clinical outcomes as for example an increased risk of atrial fibrillation or increased cardiovascular mortality, especially in old age. In order to avoid hyperthyroidism it is strongly recommended not to start any iodine containing drug therapy or to avoid application of contrast agents unless the patient presents with an unremarkable clinical course. TSH suppressive therapy for the treatment of endemic goiter or differentiated low risk thyroid carcinoma is unnecessary, since it favours the development of subclinical hyperthyroidism. Overt hyperthyroidism is treated with antithyroid drugs and/or radioiodine therapy or surgery according to the underlying disease (toxic nodular goiter, Graves' disease).

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“…The drug binding mechanism of PTU/MMZ to TPO have only been done in-vivo [36][37][38][39], however the molecular insights are yet to be understood. Due to the close homology, LPO has been used as surrogates to study interaction of TPO with anti-Thyroid drug MMZ.…”

Section: Introductionmentioning

confidence: 99%

“…Both ATDs obstructs the iodination of tyrosyl residues in Thyroglobulin catalyzed by Thyroid Peroxidase, thereby arresting the production of thyroid hormones [27][28][29]. MMZ is preferred to PTU, due to its better adherence and bioavailability [23,[30][31][32]; however, PTU is also recommended for pregnant women [33,34]. Irradiation studies too have been done to treat hyperthyroidism [35].…”

Section: Introductionmentioning

confidence: 99%

Comparative Study on the Binding Affinity of Methimazole and Propylthiouracil to Thyroid Peroxidase as an Anti-Thyroid Drug: An Insilico Approach

Pradhan¹,

Sarma²,

Bharadwaz³

et al. 2017

J Mol Imaging Dynam

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Graves' disease (GD), an autoimmune disorder, scars majority of women worldwide, causing hyperthyroidism, Graves's ophthalmopathy and goitre. Thyroid Peroxidase (TPO) is an active target of anti-thyroid drugs, Methimazole and Propylthiouracil, which inhibit the enzyme function of catalysing the thyroid hormones synthesis. Most of the protein-drug interaction studies so far have been focussed mainly at in vivo level, or by using Myeloperoxidase and Lactose peroxidases as TPO surrogates for the same. This makes the molecular interaction of TPO with the drugs crucial to understand. In this study, we used the molecular dynamics (MD) to study the molecular interaction differences between TPO 201-500 and both drugs. The binding free energy calculation done using Molecular Mechanics Poisson-Boltzmann (MM-PBSA) and generalized Born and surface area continuum solvation (GBSA) results indicated that both drugs bind strongly to TPO 201-500 , with Propylthiouracil having slightly higher binding energy than Methimazole. We found that both drugs interacted with the residues-Asp238, His239, Phe243, Thr487 and His494 through hydrophobic interactions and formed stable hydrogen bonds with residue Arg491 of TPO 201-500 . Since both drugs engage residues-Asp238, His239 and His494 which falls within the proximal heme binding site and catalytic site of TPO 201-500 , we can conclude that these drugs may be conducive in inhibiting the enzymatic activity of TPO 201-500 .

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Efficacy of single daily dosage of methimazole vs. propylthiouracil in the induction of euthyroidism

Cited by 38 publications

References 20 publications

Toxicological considerations for antithyroid drugs in children

Toxicological considerations for antithyroid drugs in children

Prävention und multimodale Therapie der Hyperthyreose

Comparative Study on the Binding Affinity of Methimazole and Propylthiouracil to Thyroid Peroxidase as an Anti-Thyroid Drug: An Insilico Approach

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