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Antithyroid Drugs: Their Mechanism of Action and Clinical Use

  • Chapter
Pharmacotherapeutics of the Thyroid Gland

Part of the book series: Handbook of Experimental Pharmacology ((HEP,volume 128))

Abstract

The treatment of hyperthyroidism is directed towards reducing thyroid hormone production and release from thyroid follicular cells. The mainstay of treatment is the use of antithyroid drugs (Cooper 1984), though cure of the disease often relies on either surgical treatment by partial thyroidectomy or the use of radioactive iodine (Franklyn 1994). Studies in the early 1940s demonstrated that the treatment of rats with thiourea or sulphaguanidine led to goitre formation, with subsequent studies demonstrating that these goitres resulted from the inhibition of thyroid hormone production, and the consequent stimulation of thyroid gland growth by the rise in thyroid-stimulating hormone (TSH) secretion. Based on these initial observations, Astwood conducted clinical trials with these agents which demonstrated that they were effective in controlling hyperthyroidism in man (Astwood 1943). The two main groups of antithyroid drugs (known collectively as thionamides) (Fig. 1) can be divided into the thiouracils, which have a six-membered ring, with propylthiouracil (6-propyl-2-thiouracil, PTU) being the only compound of this group in current clinical use, and the imidazoles, which have five-membered rings; the drugs in current clinical use from this group are methimazole (1-methyl-2-mercaptoimidazole, MMI) and carbimazole (1-methyl-2-thio-3-carbethoxy-imidazole, CBZ). CBZ is rapidly metabolised to MMI following ingestion.

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Authors
  1. M. El Sheikh
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  2. A. M. McGregor
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Editor information

Editors and Affiliations

  1. Department of Medicine Clinical Sciences Centre Northern General Hospital, The University of Sheffield, Sheffield, S5 7AU, UK

    A. P. Weetman (Professor of Medicine) (Professor of Medicine)

  2. Department of Endocrinology, St. Bartholomew’s Hospital, West Smithfield, London, EC1A 7BE, UK

    A. Grossman

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© 1997 Springer-Verlag Berlin Heidelberg

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El Sheikh, M., McGregor, A.M. (1997). Antithyroid Drugs: Their Mechanism of Action and Clinical Use. In: Weetman, A.P., Grossman, A. (eds) Pharmacotherapeutics of the Thyroid Gland. Handbook of Experimental Pharmacology, vol 128. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-642-60709-7_8

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  • DOI: https://doi.org/10.1007/978-3-642-60709-7_8

  • Publisher Name: Springer, Berlin, Heidelberg

  • Print ISBN: 978-3-642-64519-8

  • Online ISBN: 978-3-642-60709-7

  • eBook Packages: Springer Book Archive

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