THE INFLUENCE OF PROMINAL ON THYROID FUNCTION IN THE RAT

1955 ◽  
Vol 18 (4) ◽  
pp. 460-461
Author(s):  
F. Schwarz
Keyword(s):  
Thyroid Function ◽  
Barbituric Acid ◽  
Animal Experiments ◽  
Normal Subjects ◽  
Graves Disease ◽  
Unexpected Result ◽  
Experimental Animals ◽  
Thyroid Uptake ◽  
Barbituric Acid Derivatives ◽  
Methyl Phenyl

SUMMARY Prominal (methyl-phenyl-ethyl barbituric acid) and other barbituric acid derivatives can depress the basal metabolic rate in hypermetabolism, in normal subjects and in experimental animals. It has been assumed that, particularly in the case of Graves disease, this is caused by an effect on the diencephalic centres controlling thyroid function (Falta & Fenz, 1937). We were interested in this problem because of the variable results obtained in the clinical treatment of thyrotoxicosis and other hypermetabolic conditions with Prominal. Some animal experiments were therefore done in which, much to our surprise Prominal appeared to raise the I131 uptake of the thyroid gland of rats instead of depressing it. This unexpected result led us to further investigation. Prominal administered for 7 days in a dosage of 15 mg. raised the thyroid uptake of I131 significantly. This was confirmed in three strains of rats. Barbital and phenobarbital appeared to have the same effect as

scholarly journals Preserved activation of thyrotropin receptor antibody to stimulate thyroid function despite long-term treatment in euthyroid patients with Graves' disease

1998 ◽  
pp. 281-285 ◽  
Author(s):  
M Akuzawa ◽  
M Murakami ◽  
M Yamada ◽  
T Satoh ◽  
H Shimizu ◽  
...  
Keyword(s):  
Thyroid Function ◽  
Normal Subjects ◽  
Term Treatment ◽  
Graves Disease ◽  
Thyrotropin Receptor ◽  
Receptor Antibody ◽  
Thyrotropin Receptor Antibody ◽  
Long Term Treatment ◽  
Tsh Levels

Clinical evaluation was conducted to ascertain whether thyrotropin receptor antibody (TRAb) in the normal range may still be involved in the regulation of thyroid function after prolonged treatment for Graves' disease. All patients (n = 33) were treated with antithyroid drugs for an average of 10.6 years and were under euthyroid conditions in which normal blood levels of tri-iodothyronine (T3) were significantly correlated with blood thyrotropin (TSH) levels, but not with titers of TRAb. A significant correlation was observed between TRAb titer and thyroid-stimulating antibody (TSAb) activity. In contrast, this correlation was not found in normal subjects. After administration of T3 (75 microg daily for 8 days), the patients showed increased levels of T3 with concomitant suppression of TSH levels. Under these conditions, linear regression analysis showed significant correlations of TRAb titer and TSAb activity with 24-h thyroid radioiodine uptake (r = 0.641 and 0.621 respectively, P < 0.01), in contrast to declining blood thyroxine levels. Moreover, the immunoglobulin G (IgG) of the patients precipitated to a greater extent than IgG from normal subjects a peptide consisting of the amino acid sequence near the terminus of the human TSH receptor. These findings indicated that TRAb at normal levels possessed significant unremitting activities on thyroid function despite long-term treatment in euthyroid patients with Graves' disease.

scholarly journals Serum concentrations of proinflammatory cytokines in Graves' disease: effect of treatment, thyroid function, ophthalmopathy and cigarette smoking

2000 ◽  
pp. 197-202 ◽  
Author(s):  
M Salvi ◽  
M Pedrazzoni ◽  
G Girasole ◽  
N Giuliani ◽  
R Minelli ◽  
...  
Keyword(s):  
Cigarette Smoking ◽  
Thyroid Function ◽  
Interleukin 1 ◽  
Antithyroid Drug ◽  
Normal Subjects ◽  
Tnf Alpha ◽  
Graves Disease ◽  
Serum Concentrations ◽  
Necrosis Factor Alpha ◽  
Disease Effect

OBJECTIVE: In the present study we have measured the concentrations of interleukin-6 (IL-6), soluble IL-6 receptor (sIL-6R), tumor necrosis factor-alpha (TNF-alpha), interleukin-1 beta (IL-1 beta) and IL-1 receptor antagonist (IL-1Ra) in the serum of patients with Graves' disease (GD). By multivariate analysis, we have evaluated the effect of antithyroid treatment, thyroid function, the presence or absence of active thyroid-associated ophthalmopathy (TAO), the patient's smoking habits and the relation to circulating anti-thyrotropin (TSH) receptor (TRAb) and anti-thyroperoxidase antibodies (TPOAb). SUBJECTS: We studied 84 GD patients, 51 untreated and 33 receiving methimazole (MMI) therapy. Twenty-three (45%) untreated patients and 18 (54%) patients on MMI had active TAO. We also studied 67 normal subjects as controls. Thirty-one GD patients (43%) and 16 controls (36%) were smokers. RESULTS: Serum IL-6 concentrations were significantly higher in both untreated patients (P<0.001) and treated patients (P<0.006), when compared with controls. Serum sIL-6R concentrations were significantly affected by treatment (P=0.001). Serum IL-1Ra concentrations were not different in GD patients, whether treated or untreated, compared with controls. Serum IL-6 concentrations were not influenced by thyroid function and there was a significant interaction between treatment and the presence of active TAO (P=0.003). In hyperthyroid patients with active TAO serum, sIL-6R concentrations were significantly higher than in those with inactive TAO (P=0.003). In untreated GD patients there was no significant effect of thyroid function and TAO activity on the serum concentrations of TNF-alpha and IL-1 beta. Serum IL-1Ra concentrations were not affected by the presence of TAO. Smoking had no effect on serum IL-6, sIL-6R, TNF-alpha, IL-1 beta and IL-1Ra concentrations, even in the presence of an active TAO. Serum concentrations of IL-6, sIL-6R, TNF-alpha and IL-1 beta and IL-1Ra were not different in patients with and without TRAb or TPOAb, in relation to either thyroid function, TAO activity or smoking. CONCLUSIONS: Our work shows that: (i) the proinflammatory cytokine pattern in GD is greatly influenced by antithyroid drug treatment; (ii) the increased circulating IL-6/sIL-6R concentrations observed in patients with active TAO may derive from the activation of humoral reactions in sites other than the thyroid; and, (iii) cigarette smoking has no effect on serum IL-1/IL-1Ra concentrations in TAO.

Abstract #1202: A Case of Graves’ Disease With Fluctuating Thyroid Function

2016 ◽  
Vol 22 ◽  
pp. 305-306
Author(s):  
Sheela Metgud ◽  
Anup Kumar ◽  
Erin Drever ◽  
Tahira Yasmeen
Keyword(s):  
Thyroid Function ◽  
Graves Disease

Radioiodine treatment of feline hyperthyroidism in Germany

2002 ◽  
Vol 41 (06) ◽  
pp. 245-251 ◽  
Author(s):  
M. Knietsch ◽  
T. Spillmann ◽  
E.-G. Grünbaum ◽  
R. Bauer ◽  
M. Puille
Keyword(s):  
Radiation Exposure ◽  
Radiation Protection ◽  
Thyroid Function ◽  
Radioiodine Therapy ◽  
Whole Body ◽  
Radioiodine Treatment ◽  
Normal Thyroid ◽  
Normal Thyroid Function ◽  
Body Activity ◽  
Thyroid Uptake

SummaryAim: Establishment of radioiodine treatment of feline hyperthyroidism in veterinary routine in accordance with German radiation protection regulations. Patients and methods: 35 cats with proven hyperthyroidism were treated with 131I in a special ward. Thyroid uptake and effective halflife were determined using gammacamera dosimetry. Patients were released when measured whole body activity was below the limit defined in the German “Strahlenschutzverordnung”. Results: 17/20 cats treated with 150 MBq radioiodine and 15/15 cats treated with 250 MBq had normal thyroid function after therapy, normal values for FT3 and FT4 were reached after two and normal TSH levels after three weeks. In 14 cats normal thyroid function was confirmed by controls 3-6 months later. Thyroidal iodine uptake was 24 ± 10%, effective halflife 2.5 ± 0.7 days. Whole body activity <1 MBq was reached 13 ± 4 days after application of 131I. Radiation exposure of cat owners was estimated as 1.97 Sv/MBq for adults. Conclusion: Radioiodine therapy of feline hyper-thyroidism is highly effective and safe. It can easily be performed in accordance with German radiation protection regulations, although this requires hospitalisation for approximately two weeks. Practical considerations on radiation exposure of cat owners do not justify this long interval. Regulations for the veterinary use of radioactive substances similar to existing regulations for medical use in humans are higly desirable.

The Effect of Barbituric Acid Derivatives on Platelet Function in Vitro and in Vivo

1973 ◽  
Vol 30 (02) ◽  
pp. 315-326
Author(s):  
J. Heinz Joist ◽  
Jean-Pierre Cazenave ◽  
J. Fraser Mustard
Keyword(s):  
Platelet Aggregation ◽  
Platelet Function ◽  
Barbituric Acid ◽  
Platelet Rich Plasma ◽  
Inhibitory Effect ◽  
Primary Response ◽  
Sodium Pentobarbital ◽  
Barbituric Acid Derivatives

SummarySodium pentobarbital (SPB) and three other barbituric acid derivatives were found to inhibit platelet function in vitro. SPB had no effect on the primary response to ADP of platelets in platelet-rich plasma (PRP) or washed platelets but inhibited secondary aggregation induced by ADP in human PRP. The drug inhibited both phases of aggregation induced by epinephrine. SPB suppressed aggregation and the release reaction induced by collagen or low concentrations of thrombin, and platelet adherence to collagen-coated glass tubes. The inhibition by SPB of platelet aggregation was readily reversible and isotopically labeled SPB did not become firmly bound to platelets. No inhibitory effect on platelet aggregation induced by ADP, collagen, or thrombin could be detected in PRP obtained from rabbits after induction of SPB-anesthesia.

SUBACUTE THYROIDITIS

1960 ◽  
Vol XXXIII (III) ◽  
pp. 457-472 ◽  
Author(s):  
B.-A. Lamberg ◽  
G. Hintze ◽  
R. Jussila ◽  
M. Berlin
Keyword(s):  
Thyroid Function ◽  
Early Phase ◽  
Radioactive Iodine ◽  
Serum Proteins ◽  
Conversion Ratio ◽  
Subacute Thyroiditis ◽  
Synthetic Analogues ◽  
The Third ◽  
Thyroid Uptake ◽  
Iodine Metabolism

ABSTRACT A series of cases of clinically diagnosed subacute thyroiditis comprising 11 patients is reported. Studies on the iodine metabolism, electrophoretic distribution of the serum proteins and the responsiveness to TSH were carried out. The patients were observed for periods up to 16 months from the onset of the disease. In the early phase there was an elevation of the serum PBI in a few cases and hyperthyroid signs in some, accompanied by depressed thyroid uptake of radioactive iodine and a fairly good response to TSH. Later, the thyroid grew hard and the iodine metabolism changed. In several cases there was a marked increase in the conversion ratio and the serum PB131I level. The responses to TSH was variable for different parameters of thyroid function, suggesting a state of »low thyroid reserve« as defined by Jefferies et al. (1956). Hypothyroidism developed in 3 cases; in two of them there was a response to exogenous TSH, in the third no response was seen at this stage of the disease. Cortisone and synthetic analogues seem to be of great benefit in the treatment of the acute symptoms of the disease.

Graves' disease and radioiodine therapy

2008 ◽  
Vol 47 (04) ◽  
pp. 153-166 ◽  
Author(s):  
I. Weber ◽  
W. Eschner ◽  
F. Sudbrock ◽  
M. Schmidt ◽  
M. Dietlein ◽  
...  
Keyword(s):  
Success Rate ◽  
Thyroid Function ◽  
Therapeutic Dose ◽  
Radioiodine Therapy ◽  
Antithyroid Drugs ◽  
Graves Disease ◽  
Inclusion Criteria ◽  
End Point ◽  
Point Measure ◽  
The Impact

SummaryAim: This study was performed to analyse the impact of the choice of antithyroid drugs (ATD) on the outcome of ablative radioiodine therapy (RIT) in patients with Graves' disease. Patients, material, methods: A total of 571 consecutive patients were observed for 12 months after RIT between July 2001 and June 2004. Inclusion criteria were the confirmed diagnosis of Graves' disease, compensation of hyperthyroidism and withdrawal of ATD two days before preliminary radioiodine-testing and RIT. The intended dose of 250 Gy was calculated from the results of the radioiodine test and the therapeutically achieved dose was measured by serial uptake measurements. The end-point measure was thyroid function 12 months after RIT; success was defined as elimination of hyperthyroidism. The pretreatment ATD was retrospectively correlated with the results achieved. Results: Relief from hyperthyroidism was achieved in 96 % of patients. 472 patients were treated with carbimazole or methimazole (CMI) and 61 with propylthiouracil (PTU). 38 patients had no thyrostatic drugs (ND) prior to RIT. The success rate was equal in all groups (CMI 451/472; PTU 61/61; ND 37/38; p=0.22). Conclusion: Thyrostatic treatment with PTU achieves excellent results in ablative RIT, using an accurate dosimetric approach with an achieved post-therapeutic dose of more than 200 Gy.

Synthesis, Molecular Modeling and Biological Evaluation of 5-arylidene-N,N-diethylthiobarbiturates as Potential α-glucosidase Inhibitors

2019 ◽  
Vol 15 (2) ◽  
pp. 175-185 ◽  
Author(s):  
Momin Khan ◽  
Sehrish Khan ◽  
Amir Ul Mulk ◽  
Anis Ur Rahman ◽  
Abdul Wadood ◽  
...  
Keyword(s):  
Molecular Modeling ◽  
Barbituric Acid ◽  
Aromatic Aldehydes ◽  
Biological Evaluation ◽  
Distilled Water ◽  
Sound Effects ◽  
Glucosidase Inhibitors ◽  
Ic50 Values ◽  
Antiviral Activities ◽  
Barbituric Acid Derivatives

Background:Barbituric acid derivatives are a versatile group of compounds which are identified as potential pharmacophores for the treatment of anxiety, epilepsy and other psychiatric disorders. They are also used as anesthetics and have sound effects on the motor and sensory functions. Barbiturates are malonylurea derivatives with a variety of substituents at C-5 position showing resemblance with nitrogen and sulfur containing compounds like thiouracil which exhibited potent anticancer and antiviral activities. Recently, barbituric acid derivatives have also received great interest for applications in nanoscience.Objective:Synthesis of 5-arylidene-N,N-diethylthiobarbiturates, biological evaluation as potential α-glucosidase inhibitors and molecular modeling.Methods:In the present study, N,N-Diethylthiobarbituric acid derivatives were synthesized by refluxing of N,N-diethylthiobarbituric acid and different aromatic aldehydes in distilled water. In a typical reaction; a mixture of N,N-diethylthiobarbituric acid 0.20 g (1 mmol) and 5-bromo-2- hydroxybenzaldehyde 0.199 g (1 mmol) mixed in 10 mL distilled water and reflux for 30 minutes. After completion of the reaction, the corresponding product 1 was filtered and dried and yield calculated. It was crystallized from ethanol. The structures of synthesized compounds 1-25 were carried out by using 1H, 13C NMR, EI spectroscopy and CHN analysis used for the determination of their structures. The α-glucosidase inhibition assay was performed as given by Chapdelaine et al., with slight modifications and optimization.Results:Our newly synthesized compounds showed a varying degree of α-glucosidase inhibition and at least four of them were found as potent inhibitors. Compounds 6, 5, 17, 11 exhibited IC50 values (Mean±SEM) of 0.0006 ± 0.0002, 18.91 ± 0.005, 19.18 ± 0.002, 36.91 ± 0.003 µM, respectively, as compared to standard acarbose (IC50, 38.25 ± 0.12 µM).Conclusion:Our present study has shown that compounds 6, 5, 17, 11 exhibited IC50 values of 0.0006 ± 0.0002, 18.91 ± 0.005, 19.18 ± 0.002, 36.91 ± 0.003 µM, respectively. The studies were supported by in silico data analysis.

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