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The History of Nuclear Medicine
Published in Michael Ljungberg, Handbook of Nuclear Medicine and Molecular Imaging for Physicists, 2022
During the last two decades, the number of PET examinations has increased significantly with 18F-FDG being the most used radiopharmaceutical. In 1998, the first study using 18F-FDG was conducted in PET imaging to analyse chemotherapy response to predict the response to subsequent high-dose chemotherapy [44]. Another positron-emitting radiopharmaceutical that is widely used is 18F-NaF (sodium fluoride). This agent has become an alternative to 99Tcm-phosphate substances for skeletal scintigraphy, but the latter is still the most typically used. The 18F-NaF was developed and used occasionally already in the 1970s; however, because it was expensive and PET was rarely accessible at the time, 99Tcm-MDP was the preferred choice for many years [45]. Other positron-emitting radionuclides that have been introduced after the millennium shift include 68Ga. It is mainly produced in by the generator system, and typically used for the diagnosis of neuroendocrine as 68Ga-DOTATOC or 68Ga-DOTATOC [46, 47]. This radiopharmaceutical is often used in combination with radionuclide therapy involving 90Y- or 177Lu- DOTATOC.
Sodium Fluoride
Published in Anton C. de Groot, Monographs in Contact Allergy, 2021
Sodium fluoride is an inorganic salt of fluoride used topically or in municipal water fluoridation systems to prevent dental caries. Fluoride appears to bind to calcium ions in the hydroxyapatite of surface tooth enamel, preventing corrosion of tooth enamel by acids. This agent may also inhibit acid production by commensal oral bacteria. When topical fluoride is applied to hypersensitive exposed dentin, the formation of insoluble materials within the dentinal tubules blocks transmission of painful stimuli (1).
Community-Based Methods for Preventing Dental Caries and Periodontal Disease
Published in Lars Granath, William D. McHugh, Systematized Prevention of Oral Disease: Theory and Practice, 2019
Materials and supplies for daily mouthrinsing naturally cost more than they do for the weekly regimen. There is no notably greater effectiveness from the daily procedure, and daily rinsing makes greater demands on participants and supervisory personnel, so weekly mouthrinsing with 0.2% sodium fluoride is the preferred school-based procedure. (Daily rinsing with 0.05% sodium fluoride, where appropriate, is recommended for individual self-care because it fits in better with an individual’s daily routine).
Virgin coconut oil complements with its polyphenol components mitigate sodium fluoride toxicity in vitro and in vivo
Published in Drug and Chemical Toxicology, 2022
Soorya Parathodi Illam, Sruthi Panniyan Kandiyil, Arunaksharan Narayanankutty, Soumya Valappan Veetil, Thekkekara Devassy Babu, Rao M. Uppu, Achuthan C. Raghavamenon
The human body is exposed to several chemicals which induce oxidative stress conditions. Sodium fluoride (NaF) is one of such environmental pollutants widely found in drinking water. It promotes oxidative stress and thereby interrupts tissue homeostasis in organs, including the kidney and liver. Recent studies have demonstrated that fluoride intoxication for an extended period may cause oxidative injury, widely known as ‘fluorosis.’ Fluorine present in drinking water is totally in ionic form, and hence it is rapidly and passively absorbed through the intestinal mucosa and interferes with major metabolic pathways. Adults' average daily fluorine intake from food and water is reported to be 1 mg if they are in a community with a low amount (<0.7 ppm) of fluoride in the water and about 2.7 mg; if the water is fluoridated (Guo et al. 2017). Reports from various laboratories have established a close correlation between oxidative stress in animals and fluoride intoxication (Bhatnagar et al. 2002, Mesram et al. 2017). Studies have also shown that fluoride induces excessive oxygen free radicals, depleting antioxidants and overwhelming the antioxidant defense (Hassan and Yousef 2009). Hence, fluoride-induced oxidative stress is used as a model system in preclinical studies to analyze the antioxidant properties of compounds.
Exacerbation of diclofenac-induced gastroenterohepatic damage by concomitant exposure to sodium fluoride in rats: protective role of luteolin
Published in Drug and Chemical Toxicology, 2022
Akinleye S. Akinrinde, Kehinde O. Soetan, Monsuru O. Tijani
Taken together, exposure of rats to diclofenac resulted in significant gastroenterohepatic damage, as evidenced by the macroscopic and microscopic lesions seen as well as the results of the examination of the rats, in accordance with the biochemical parameters of oxidative stress, particularly in the gastric and duodenal tissues, and to a lesser extent, in the liver. An important finding in this study was that these alterations were significantly exacerbated in rats that were treated concomitantly with sodium fluoride. The data from this study suggests that formulations combining the concurrent use of these compounds must be administered with caution, because of potential interactions that may aggravate gastrointestinal damage. The gross and histologic manifestations of gastrointestinal injury may be partly explained by the alterations observed in the oxidative status of the tissues. However, there is a need for future studies to investigate underlying molecular mechanisms involved in the process. The flavonoid, Luteolin, was studied and its protective influence against diclofenac and sodium fluoride-induced injury was documented. This influence may be attributed to its antioxidant and/or anti-inflammatory activities. Based on the findings of the study, Luteolin may thus be considered an important agent for the amelioration of gastrointestinal and hepatic damage elicited by combined administration of gastrointestinal toxicants such as diclofenac and sodium fluoride.
An update on the importance of plasma protein binding in drug discovery and development
Published in Expert Opinion on Drug Discovery, 2021
When the mechanisms of compound instability are known, inhibitors can be added to inhibit the enzymes and stabilize the compounds for binding measurements. PMSF (phenylmethylsulfonyl fluoride, 2 mM), AEBSF (4-(2-aminoethyl) benzenesulfonyl fluoride, 8 mM), dichlorvos (20 mM), and protease inhibitor cocktail (Sigma-Aldrich) are commonly used to inhibit hydrolase activities. BNPP (bis-para-nitrophenyl phosphate, 200–500 μM) was reported to stabilize esters and amides for plasma protein binding [59,60]. Sodium fluoride (10 mg/mL, a general enzyme inhibitor) was shown to be effective to stabilize compounds in plasma [61]. GSH (glutathione, 10 mM) is often used as a protective agent against reactive species and electrophiles [62]. MAO inhibitor (100 μM tranylcypromine) was shown to improve stability of MAO substrates in brain homogenate for brain binding studies [30]. Inhibitor concentration required to stabilize the compounds can be compound dependent. It may need to be optimized for specific compounds and matrices if the standard concentrations are not effective. High inhibitor concentrations may interfere with fu measurement [59,60]. It is important to verify if inhibitors alter fu values by comparing fu of a stable species with and without inhibitors or using another approach such as the low temperature method.