[Niacin in therapy].
Niacin (nicotinic acid and nicotinamide) is a vitamin used as a source of the NAD+ and NADP+ coenzymes required for many metabolic processes. Its low dietary levels induce the development of pellagra. Niacin has been used for decades in the treatment of patients with disturbed lipid and lipoprotein metabolism, this being the main cause of atherosclerotic changes in cardiovascular diseases. It is still the most efficacious drug in terms of its ability to increase HDL cholesterol content accompanied by a decrease in all atherogenic lipoproteins (VLDL, LDL, and L(a)) as well as fatty acids and triglycerides. Niacin also increases adiponectin level, which might result in additional atheroprotection. There are studies confirming the beneficial action of niacin against migraine and hyperphosphatemia associated with renal failure, ethanol-induced neurodegeneration, and loss of beta-cell function in type 1 diabetes. Moreover, it augments plasma tryptophan concentrations in HIV-infected patients and thyroid radiosensitivity to 131I. Inhibition of the invasion of hepatoma cells has also been proven. However, it is necessary to point out that the currently applied niacin preparations might exhibit such side effects as cutaneous flushing, gastrointestinal disturbances, and hepatotoxicity, particularly during treatment with sustained-release niacin preparations. The recent discovery of the G-protein-coupled receptor GPR109A, which mediates the antilipolytic effects induced by nicotinic acid in adipocytes as well as cutaneous vasodilation, allows the development of new agents interacting with this receptor. In view of these observations, niacin therapy must be accompanied by control of the choice of niacin preparation and its dose in order to eliminate or at least limit its side effects.
Nagalski
Andrzej
A
Zakład Regulacji Metabolizmu, Instytut Biochemii, Wydział Biologii, Uniwersytet Warszawski, Warszawa, Poland.
Bryła
Jadwiga
J
D017667:Adipocytes / Q000378:metabolism; D052242:Adiponectin / Q000378:metabolism; D000818:Animals; D008076:Cholesterol, HDL / Q000187:drug effects; D003692:Delayed-Action Preparations; D005483:Flushing / Q000517:prevention & control; D006801:Humans; D006949:Hyperlipidemias / Q000097:blood / Q000188:drug therapy*; D051379:Mice; D009525:Niacin / Q000009:adverse effects / Q000494:pharmacology* / Q000627:therapeutic use*; D009536:Niacinamide / Q000378:metabolism; D009539:Nicotinic Acids / Q000378:metabolism; D010383:Pellagra / Q000178:diet therapy* / Q000188:drug therapy* / Q000378:metabolism; D011817:Rabbits; D051381:Rats; D043562:Receptors, G-Protein-Coupled / Q000378:metabolism
D052242:Adiponectin; D008076:Cholesterol, HDL; D003692:Delayed-Action Preparations; D009539:Nicotinic Acids; D043562:Receptors, G-Protein-Coupled; D009536:Niacinamide; D009525:Niacin