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Enzyme Kinetics and Drugs as Enzyme Inhibitors
Published in Peter Grunwald, Pharmaceutical Biocatalysis, 2019
Niacin (nicotinic acid, 3-pyridinecarboxylic acid, a B vitamin) has been used since several decades as lipid-lowering agent; it reduces the level of plasma triglyceride by about 35%, and LDL-cholesterol levels by 10–15%, whereas it increases the concentration of HDL-cholesterol by up to 25% by a so far not precisely known mechanism. Despite these properties, results from recent studies suggest that there are no benefits from niacin therapy concerning prevention of cardiovascular disease events (Krumholz, 2016; Schandelmaier, 2017). Niacin has been withdrawn from many markets (Pedersen, 2016). Acipimox, a derivative of nicotinic acid that also lowers serum lipid levels by reducing the production of VLDL and LDL, has been reported to increase peripheral and hepatic insulin sensitivity (Vestergaard et al., 2017).
PET Imaging of Heart and Skeletal Muscle: An Overview
Published in Robert J. Gropler, David K. Glover, Albert J. Sinusas, Heinrich Taegtmeyer, Cardiovascular Molecular Imaging, 2007
Oral administration of a nicotinic acid or its derivatives have been shown to provide easy approach to stimulate myocardial glucose utilization and improve image quality (9,15). Nicotinic acid inhibits peripheral lipolysis and, thus, reduces plasma FFA concentrations. Acipimox is a very potent nicotinic acid derivative. The FDG image quality has been reported to be comparable with insulin clamping in most of the patients. Importantly, with the exception of flushing, no side effects of acipimox were observed.
Adipose tissue lipolytic inhibition enhances the glucoregulatory properties of exercise in type 2 diabetes patients
Published in European Journal of Sport Science, 2018
Dominique Hansen, Kenneth Verboven, Jan-Willem van Dijk, Antoine Zorenc, Lennert Minten, Kevin Smeets, Lex B. Verdijk, Luc J. C. van Loon
One of the mechanisms by which exercise is believed to improve insulin sensitivity is the mobilization and oxidation of the intramuscular lipid depots (Wojtaszewski et al., 2003), which is largely determined by circulating plasma FFA concentrations (van Loon et al., 2005a; van Loon et al., 2005b). The elevated plasma FFA concentrations in obese or type 2 diabetes patients inhibit the hydrolysis of intramuscular lipid stores (van Loon et al., 2005b). Of interest, administration of the nicotinic acid analogue acipimox has previously been shown to increase intramuscular triglyceride use during exercise in type 2 diabetes patients, reduce intramuscular lipid contents and lower circulating insulin concentrations in type 2 diabetes patients (van Loon et al., 2005b). We hypothesize that adipose tissue lipolytic inhibition during endurance-type exercise will help to further improve postprandial glycemic control in type 2 diabetes patients. To test our hypothesis, we determined the impact of a single bout of moderate-intense endurance-type exercise with or without adipose tissue lipolysis inhibition (acipimox administration) on subsequent postprandial blood glucose and insulin excursions throughout the day in male type 2 diabetes patients.