Acta Pharm. 66 (2016) 449-469
Review
Pleiotropic effects of niacin: Current possibilities
for its clinical use
MIROSLAV ZEMAN, MAREK VECKA,
FRANTIŠEK PERLÍK, BARBORA STAŇKOVÁ, ROBERT HROMÁDKA, EVA TVRZICKÁ, JAKUB ŠIRC,
JAKUB HRIB and ALEŠ ŽÁK
1 4th Department of Medicine, 1st
Faculty of Medicine, Charles University in Prague Prague,
Czech Republic
2 Institute of Pharmacology,
1st Faculty of Medicine, Charles University in Prague Prague, Czech Republic
3 Research and Development Center, C2P s.r.o., Chlumec/n Cidlinou, Czech Republic
4 Institute of Macromolecular Chemistry, Academy of
Sciences of the Czech Republic Prague, Czech Republic
Accepted July 1, 2016
Published online September 8, 2016
Niacin was the first hypolipidemic drug to significantly reduce both major cardiovascular events and mortality in patients with cardiovascular disease. Niacin favorably influences all lipoprotein classes, including lipoprotein[a],and belongs to the most potent hypolipidemic drugs for increasing HDL-C. Moreover, niacin causes favorable changes to the qualitative composition of lipoprotein HDL. In addition to its pronounced hypolipidemic action, niacin exerts many other, non-hypolipidemic effects (e.g., antioxidative, anti-inflammatory, antithrombotic), which favorably influence the development and progression of atherosclerosis. These effects are dependent on activation of the specific receptor HCA2. Recent results published by the two large clinical studies, AIM-HIGH and HPS2-THRIVE, have led to the impugnation of niacin’s role in future clinical practice. However, due to several methodological flaws in the AIM-HIGH and HPS2-THRIVE studies, the pleiotropic effects of niacin now deserve thorough evaluation. This review summarizes the present and possible future use of niacin in clinical practice in light of its newly recognized pleiotropic effects.
Keywords: niacin, pleiotropic effects, HCA2 receptor, dyslipidemia, cardiovascular mortality/morbidity