Topic
Propylthiouracil
About: Propylthiouracil is a research topic. Over the lifetime, 2181 publications have been published within this topic receiving 46996 citations. The topic is also known as: Thyreostat® & 2,3-dihydro-6-propyl-2-thioxo-4(1H)-pyrimidinone.
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TL;DR: This study shows that MMI, but not PTU, is able to scavenge H2O2 in the micromolar range and that both PTU and MMI can impair thyroid H 2O2 generation in addition to their potent thyroperoxidase inhibitory effects.
Abstract: H2O2 generation is a limiting step in thyroid hormone biosynthesis. Biochemical studies have confirmed that H2O2 is generated by a thyroid Ca2+/NADPH-dependent oxidase. Decreased H2O2 availability may be another mechanism of inhibition of thyroperoxidase activity produced by thioureylene compounds, as propylthiouracil (PTU) and methimazole (MMI) are antioxidant agents. Therefore, we analyzed whether PTU or MMI could scavenge H2O2 or inhibit thyroid NADPH oxidase activity in vitro. Our results show that PTU and thiourea did not significantly scavenge H2O2. However, MMI significantly scavenged H2O2 at high concentrations. Only MMI was able to decrease the amount of H2O2 generated by the glucose–glucose oxidase system. On the other hand, both PTU and MMI were able to partially inhibit thyroid NADPH oxidase activity in vitro. As PTU did not scavenge H2O2 under the conditions used here, we presume that this drug may directly inhibit thyroid NADPH oxidase. Also, at the concentration necessary to inhibit NADPH oxidase activity, MMI did not scavenge H2O2, also suggesting a direct effect of MMI on thyroid NADPH oxidase. In conclusion, this study shows that MMI, but not PTU, is able to scavenge H2O2 in the micromolar range and that both PTU and MMI can impair thyroid H2O2 generation in addition to their potent thyroperoxidase inhibitory effects.
27 citations
TL;DR: Treatment with thyroxin neonatally, after prenatal PTU administration, prevented the late pituitary-thyroidal changes but not the gonadal effects, and the possibility that pregnant women receiving PTU during pregnancy may have children with mild late gonadal and thyroidal alterations must be considered.
27 citations
TL;DR: The data suggest that mild changes in thyroid status associated with PTU affects regulation of T3, T4 and TSH more than GH or IGF-I in steers.
27 citations
TL;DR: In general goitrogenesis and activation of the iodide concentrating mechanism induced by antithyroid agents go hand in hand, but rats bearing hypothalamic lesions and subjected to PTU treatment may display a rise of the iodine gradient without a concomitant goitrous response of the thyroid.
Abstract: There is no doubt that the primary action of propjdthiouracil (PTU) and other drugs of the thiocarbamide series on the thyroid is an interference with the iodination of tyrosine. It is also well established that the ensuing hypothyroid condition evokes compensatory hypersecretion of thyrotrophin (TSH) resulting in two characteristic effects of enhanced thyrotrophic stimulation of the thyroid: a) hypertrophy and hyperplasia of the thyroid epithelium (Astwood, 1944–45), and b) activation of the thyroidal iodide concentrating mechanism, as shown by an increase in the thyroid: serum iodide gradient (VanderLaan and VanderLaan, 1947; Taurog et al., 1947) and an expanded capacity of the gland for iodide (Halmi, 1954a). In general goitrogenesis and activation of the iodide concentrating mechanism induced by antithyroid agents go hand in hand, but rats bearing hypothalamic lesions and subjected to PTU treatment may display a rise of the iodide gradient without a concomitant goitrous response of the thyroid
27 citations
Journal Article•
TL;DR: Control of thyrotoxicosis early in pregnancy using minimal doses of propylthiouracil or carbimazole, followed by subtotal thyroidectomy in the middle trimester, is safe for both mother and fetus.
Abstract: Between April 1985 and June 1995, 20 patients being treated for thyrotoxicosis became pregnant. These patients are reviewed. Control of thyrotoxicosis early in pregnancy using minimal doses of propylthiouracil or carbimazole, followed by subtotal thyroidectomy in the middle trimester, is safe for both mother and fetus.
27 citations