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Published in Caroline Ashley, Aileen Dunleavy, John Cunningham, The Renal Drug Handbook, 2018
Caroline Ashley, Aileen Dunleavy, John Cunningham
Liothyronine is metabolised by deiodination to inactive di-iodothyronine and mono-iodothyronine. Iodine released by deiodination is largely reused within the thyroid cells. Further metabolites result from conjugation and decarboxylation; tiratricol (triac) is one such metabolite.
Iodine
Published in Judy A. Driskell, Ira Wolinsky, Sports Nutrition, 2005
There might also be a danger from consumption of thyroid preparations. Scally et al.68 reported case studies of two physically fit adults who supplemented with tiratricol, an over-the-counter thyroid preparation marketed as a metabolic accelerator and fat loss aid. They presented with lethargy, loss of appetite and muscle weakness, symptoms that were accompanied by low serum TSH and profoundly elevated T3 concentrations. These cases illustrate the danger of consumption of substances marketed as “nutritional” supplements, but which may have pharmacological effects capable of inducing thyroid abnormalities when consumed inappropriately.
Nutritional Ergogenic Aids: Introduction, Definitions and Regulatory Issues
Published in Ira Wolinsky, Judy A. Driskell, Nutritional Ergogenic Aids, 2004
Ira Wolinsky, Judy A. Driskell
Safety is always of paramount importance, but there will never be enough data on any food, drug or supplement to conclusively prove safety or lack of safety. The real question is: are products being sold for the sake of profit over legitimate concerns for consumer safety? Examples of such practices were gamma hydroxybutyrate (GHB) and its related compounds (gamma butyrolactone and butanediol) and tiratricol (a thyroid hormone). Both were sold as dietary supplements by a small number of companies to the weight-loss and weightlifter market niches, in spite of well-known published adverse effects, and use as prescription drugs prior to 1994 (which DSHEA specifically forbade). Both types of products were shown to cause or to be associated with expected adverse effects, and use spread to nonathletic groups. The FDA and Department of Justice quickly took action and removed these products from the marketplace. Judicial agencies investigated and brought criminal charges against manufacturers or distributors of these
Discovery of antimicrobial compounds targeting bacterial type FAD synthetases
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2018
María Sebastián, Ernesto Anoz-Carbonell, Begoña Gracia, Pilar Cossio, José Antonio Aínsa, Isaías Lans, Milagros Medina
We then move to identify which one of the activities (RFK or FMNAT), and in which extension, was affected by each one of these 37 HTS hits. With this aim, we assayed the effect of the HTS hits both on the CaFADS RFK and FMNAT activities. Figure 2 and Table 1 summarise the results. Comparison of Figure 2(A,B) shows that, in general and under the assay conditions, the 37 HTS hits produced a stronger deleterious effect on the FMNAT activity (all decreased the activity of the controls in more than 50%) than on the RFK one. The FMNAT module of CaFADS does not have sequence or structural homology with the mammalian protein but the RFK module belongs to the eukaryotic RFKs family. Therefore, we decided to continue the study with the HTS hits that inhibit the FMNAT activity, since they are more likely to be specific to the bacterial proteins. Thus, we choose the HTS hits that decreased the FMNAT activity below 5% of that of the controls, but maintained over 75% the RFK activity (Figure 2, Table 1). Thus, among (2)\(11), tiratricol (15), benzbromarone (17), oxantel pamoate (19), Chicago sky blue 6B (24), gossypol (27), flunixin meglumine (31) and oxaprozin (43) (Chart 1) were selected as FMNAT hits. It is worth noticing that although some of these compounds are apparently structurally related with other of the HTS hits, slight differences in functional groups and geometries induce different enzymatic responses in the FMNAT or RFK activities. This is a fact of particular interest when developing specific inhibitors.
Toxicity from illegitimate slimming agents – a 10-year case series at a tertiary toxicology laboratory in Hong Kong
Published in Clinical Toxicology, 2021
Nike Kwai Cheung Lau, Magdalene Huen Yin Tang, Sau Wah Ng, Yeow Kuan Chong, Sammy Pak Lam Chen, Hencher Han Chih Lee, Chor Kwan Ching, Tony Wing Lai Mak
A total of 203 urine specimens and 743 drug specimens were received and analyzed. Seventy-nine patients submitted urine specimen only with no drug specimen, while 49 patients submitted more than four drug specimens, and in 10 patients more than 10 drug samples were received. The major classes of drugs identified in these samples were stimulants (e.g., sibutramine, caffeine, and phentermine), laxatives (e.g., anthraquinones, phenolphthalein, and bisacodyl), diuretics (e.g., hydrochlorothiazide, furosemide) and thyroid hormones (animal thyroid tissue, triiodothyroacetic acid, and thyroxine) (Table 2). Notably a new psychoactive substance, 2-(diphenylmethyl)-pyrrolidine (desoxy-D2PM), was detected in three patients, including two patients in a previous report [11]. In 39 patients, undeclared Western medications were detected in the slimming agents they submitted, which were alleged to be herbal or “all natural”. The means of obtaining the slimming agent(s) or the geographical source of the drugs were reported only in a limited number of patients. These patients reported obtaining the slimming agent(s) from Internet sources (69 patients), over-the-counter in community pharmacy (28 patients), unspecified local sources (eight patients), or friends (three patients). In particular, eight patients were found to be taking drugs which were prescribed by registered medical practitioners but not approved for slimming purposes. These drugs included sibutramine, phentermine, norpseudoephedrine, tiratricol, tri-iodothyronine, and diuretics or laxatives. Otherwise the source of these drug items was unknown. In 45 patients, they reported using slimming products brought in from outside Hong Kong, including Thailand (28 patients), mainland China (12 patients), and Indonesia (5 patients). In particular, the number of patients using slimming agents obtained from Thailand increased from 0.3 per year (2008 to 2012), to 2.5 per year (2013 to 2017) (Supplementary Table 3). Polypharmacy was a common practice in these patients as we observed the median number of drug specimens submitted to us per patient was seven, and the maximum was 11. Common analytical findings on these drug combinations included appetite suppressants (e.g., sibutramine, lorcaserin), diuretics (e.g., hydrochlorothiazide, furosemide), laxatives (e.g., bisacodyl, anthraquinones), and animal thyroid tissue amongst other drugs.