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Cholesterol/Hypercholesterolemia/Hyperlipidemia
Published in Charles Theisler, Adjuvant Medical Care, 2023
Nicotinic acid (vitamin B3) is the most powerful agent currently available for raising low levels of good cholesterol (HDL-C).7 Niacin and statins also lower triglycerides (fats) in the blood.6,7 There is some indication that patients on statins benefit further from niacin supplementation to slow the progression of heart disease.8
Micronutrients
Published in Chuong Pham-Huy, Bruno Pham Huy, Food and Lifestyle in Health and Disease, 2022
Chuong Pham-Huy, Bruno Pham Huy
Niacin (nicotinic acid), but not niacinamide, has been used for decades as a lipid-lowering drug. Niacin is considered a valuable therapeutic agent to boost levels of high-density lipoprotein cholesterol (HDL-C) or good cholesterol. It also lowers levels of low-density lipoprotein cholesterol (LDL-C) or bad cholesterol, as well as decreases hypertriglyceridemia and high lipoprotein A (33, 39, 42). These effects are only observed in high amounts of niacin (two to three g/day). However, the clinical use of niacin to treat hyperlipidemic diseases is limited by its side effects, such as flushing of the skin, liver damage, itching, burning sensation, stomach upset, headache, dizziness, blurred vision, glucose intolerance, paresthesia (tingling), rashes, nausea, mouth pain, and runny nose (33, 39, 42). Moreover, it remains unclear whether niacin, either in the setting of well-controlled LDL-Cholesterol or in combination with other lipid-lowering agents, confers any therapeutic benefit, and if so, by which mechanism (42). The results of recent trials reject the hypothesis that simply raising HDL-Cholesterol is cardioprotective (42). It is of note that nicotinamide does not have the pharmacologic action of the nicotinic acid that is used at high doses to lower blood lipids (3). Therefore, the use of niacin at high doses for the treatment of hypercholesterolemia and hyperlipidemia must be supervised by a cardiologist to calculate the benefits and risks of the treatment.
Nutritional Deficiencies
Published in Philip B. Gorelick, Fernando D. Testai, Graeme J. Hankey, Joanna M. Wardlaw, Hankey's Clinical Neurology, 2020
Deepa Bhupali, Fernando D. Testai
Nicotinic acid has vasodilatory and cholesterol-lowering properties. Thus, it is used in patients with dyslipidemia and cardiovascular disease. The most common side effects are flushing, vomiting, pruritus, hives, and transaminitis. Niacin-induced myopathy has also been described. In comparison, nicotinamide lacks the vasodilatory and cholesterol-lowering properties and does not produce skin flushing.
Hydrolysis kinetics of the prodrug myristyl nicotinate
Published in Pharmaceutical Development and Technology, 2022
Bashar Altaani, Razan Haddad, Aliaa Al-Tarakji, Nasr Alrabadi
Nicotinic acid has two main pharmacological actions. The first is the known pharmacological action of vitamin B3 that is potent in milligram doses, and the second is the broad-spectrum lipid-lowering action that is potent in gram doses (Carlson 2005; Julius and Fischer 2013). Interestingly, studies showed that this drug has chemo-preventive and anticancer effects especially for skin cancer (Nikas et al. 2020). Nicotinic acid is also emerging as a key factor in protecting the skin from sun damage and aging. It may provide benefits to photodamaged skin by mechanisms that involve both its nutrient and drug effects (Jacobson et al. 2007; Tashtoush et al. 2007). Other studies showed that nicotinic acid treatment improves neurological functional recovery in experimental autoimmune encephalomyelitis mice (Zhang et al. 2008). A recent study showed that nicotinic acid provided an anti-inflammatory effect in silk-based scaffolds (Siavashani et al. 2019).
Applications of fluorine to the construction of bioisosteric elements for the purposes of novel drug discovery
Published in Expert Opinion on Drug Discovery, 2021
Despite being shown to have a range of clinical benefits such as lowering low density lipoprotein cholesterol and reducing the rate of myocardial infarction, the use of nicotinic acid as a therapeutic is limited by related side effects (flushing, hepatotoxicity) and the need to take high doses due to the short half-life of the drug [167–172]. The biological target of nicotinic acid is the G-protein coupled receptor GPR109a which is expressed in human adipose tissue [173,174]. Activation of GPR109a is proposed to decrease intracellular cAMP levels in adipocytes leading to a downstream reduction in the activity of protein kinase A. Subsequently, there is a decrease in hormone sensitive lipase activity resulting in a reduction on both intracellular triglyceride (TG) hydrolysis and free fatty acid (FFA) secretion. Decrease in FFA production from adipocytes leads to a substrate deficiency in the liver leading to the decrease in LDL-levels, etc., observed in plasma [175–177].
UHPLC/QTOF-MS-based metabolomics reveal the effect of Melastoma dodecandrum extract in type 2 diabetic rats
Published in Pharmaceutical Biology, 2019
Jingyu Weng, Jingkai Zhou, Liqing Liang, Li Li
Nicotinuric acid is a molecule produced via the nicotinic acid metabolism pathway and is significantly altered following MDE treatment. Nicotinic acid derivatives include nicotinamide adenine dinucleotide (NAD, coenzyme I) and nicotinamide adenine dinucleotide phosphoric acid (NADP, coenzyme II), which are important coenzymes in oxidative reactions. Studies have shown that nicotinic acid regulates lipid metabolism and can reduce the synthesis of LDL-C, TC and TG (Lukasova et al. 2011).