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: It is concluded that thyroid hormones regulate the number of α1-adrenoceptors in membranes of the rat cerebral cortex, leaving their affinities unchanged.
Abstract: The influence of thyroid hormones on the concentration and properties of alpha 1-adrenoceptors in a crude membrane fraction obtained from the rat cerebral cortex was investigated using the [3H]-WB 4101 binding assay. Animals were made hypothyroid by feeding 6-propyl-2-thiouracil for 8 weeks. Hyperthyroidism was induced by triiodothyronine injections (50 microgram/100 g body weight) for 9 days. 1. The binding of [3H]-WB 4101 was saturable and of high affinity in controls as well as in hyper- and hypothyroid animals. The maximal number of binding sites (Bmax), which amounted to 95 fmol/mg protein in control animals, was increased by 27% in cortical membranes from hyperthyroid rats and reduced by 23% in the hypothyroid group. 2. The reduction in [3H]-WB 4101 binding due to 6-propyl-2-thiouracil feeding was reversible by triiodothyronine treatment. 3. Dissociation constants (KD) calculated from saturation experiments (0.25 nM) or kinetic data (0.21 nM) remained unchanged in altered thyroid states. 4. Inhibition of [3H]-WB 4101 binding by adrenergic agonists and antagonists revealed no differences between euthyroid and hypothyroid animals. The higher affinity of prazosin to the binding sites compared with yohimbine indicated that [3H]-WB 4101 predominantly labeled alpha 1-adrenoceptors. It is concluded that thyroid hormones regulate the number of alpha 1-adrenoceptors in membranes of the rat cerebral cortex, leaving their affinities unchanged.
27 citations
TL;DR: Frequent monitoring for PTU-induced hepatic dysfunction is strongly advised because timely discontinuation of this drug and implementation of noninvasive therapeutic interventions may prevent progression to liver failure or even death.
Abstract: Propylthiouracil- (PTU-) induced hepatotoxicity is rare but potentially lethal with a spectrum of liver injury ranging from asymptomatic elevation of transaminases to fulminant hepatic failure and death. We describe two cases of acute hepatic failure due to PTU that required liver transplantation. Differences in the clinical presentation, histological characteristics, and posttransplant management are described as well as alternative therapeutic options. Frequent monitoring for PTU-induced hepatic dysfunction is strongly advised because timely discontinuation of this drug and implementation of noninvasive therapeutic interventions may prevent progression to liver failure or even death.
27 citations
Journal Article•
TL;DR: Quantitative information has been presented which indicates the intimate relationship between brain function and level of activity of the thyroid gland, and the possibility that propyithiouracil has a direct depressant effect on the central nervous system must be considered.
Abstract: In order to elucidate the effects of thyroid function on central nervous activity, the thresholds for electrically- and chemically-induced seizures, the pattern of maximal electroshock convulsions and the duration of postictal depression were determined in normal, thyroxin-treated, thyroidectomized and propylthiouraciltreated rats. The results obtained were as follows: 1 . Thyroxin decreased electroshock threshold for minimal seizures (increased brain excitability), whereas thyroidectomy and propylthiouracil increased this threshold (decreased brain excitability). 2. Thyroxin decreased total duration of maximal (tonic-clonic) electroshock seizures by shortening the clonic phase. Thyroidectomy increased total duration by markedly prolonging the hindleg extensor component of the tonic phase whereas propyithiouracil increased total duration by prolonging the flexor component. 3. Thyroxin slightly accelerated and thyroidectomy markedly accelerated recovery from maximal electroshock seizures. In contrast, propylthiouracil moderately prolonged postictal recovery. 4. Thyroxin increased susceptibility to Metrazol-induced seizures, whereas thyroidectomy and propyithiouracil both decreased susceptibility to such seizures. Since certain effects of propylthiouracil unexpectedly differed from those of thyroidectomy, the possibility that propyLthiouracil has a direct depressant effect on the central nervous system must be considered. All the changes in seizure properties exhibited by the propyithiouracil-treated rats are characteristic of those caused by anticonvulsant drugs. A comparison of propyithiouracil with phenobarbital and diphenylhydantion is presented (table 4). Quantitative information has been presented which indicates the intimate relationship between brain function and level of activity of the thyroid gland.
27 citations
TL;DR: awareness of this rare, but potentially serious, adverse drug reaction is important because prompt discontinuation of medication is essential and cross-reactivity between propylthiouracil and methimazole must be considered when selecting alternative therapies.
27 citations
27 citations