Effects of nicotinic acid on serum cholesterol concentrations of high density lipoprotein subfractions HDL², and HDL³, in hyperlipoproteinaemia

Abstract

Nicotinic acid was given in a 4-g daily dose for 6 weeks to 41 weight-stable patients of mean age (+/- SD) 52 +/- 9 years, with type IIa, type IIb or type IV hyperlipoproteinaemia (HLP), in order to study its effects on serum cholesterol concentrations of high density lipoprotein (HDL) subfractions HDL2 and HDL3. The triglyceride and cholesterol levels of serum very low density (VLDL) and low density (LDL) lipoproteins decreased during treatment (P less than 0.001). Serum HDL and HDL2 cholesterol levels increased by 37% and 135%, respectively. These changes were positively correlated (r = 0.93; P less than 0.001). There was no significant change in mean serum HDL3 cholesterol concentration. A negative correlation existed between changes in HDL3 and HDL2 cholesterol levels (r = -0.54; P less than 0.001). Multiple stepwise linear regression analyses revealed that the initial HDL3 cholesterol predicted more than 30% of the increase in HDL2 cholesterol. Changes in the concentrations of HDL2 and HDL3 cholesterol after 6 weeks of drug treatment were not related to the type of HLP, neither were these effects of nicotinic acid correlated with changes in VLDL or LDL lipid levels. The concept has previously been proposed, on the basis of in vitro data, that HDL2 is formed from HDL3 particles in the blood. Our results suggest that, in man, this reaction is stimulated in vivo by prolonged nicotinic acid therapy.

Niacin: chemical forms, bioavailability, and health effects

“…High‐dose NA (above 50 mg) is marketed in the United States as a dietary supplement (which may not make drug claims) and also as a prescription drug (which may make approved therapeutic claims). The beneficial lipid‐lowering effects of both NA and ER‐NA are well established, with data showing reduction of total triglyceride levels by 20–50%, reduction of LDL‐C levels by 10–25%, increases of HDL‐C levels by 10–30%, and reduction of lipoprotein a levels by 10–30%, 30–35 which includes preferential reduction of the more atherogenic, small, dense LDL‐C 36 . Both NA and ER‐NA are effective in treating a range of lipid disorders, but neither has become a first‐line therapy because of the uncomfortable flushing side effect and the potential risk of liver and gastrointestinal side effects.…”

Effects of Established Hypolipidemic Drugs on HDL Concentration, Subclass Distribution, and Function

“…Several studies have confirmed this observation in patients with different types of dyslipidemia treated with 2, 3, or 4 g/day of regular or ER niacin (Johansson and Carlson 1990;Knopp et al 1998;Morgan et al 2003;Wahlberg et al 1990) and in patients with coronary artery disease (Kuvin et al 2006). A very recent study showed that also 1 g/day of ER niacin increases large HDL particles in dyslipidemic patients, with a concomitant significant increase in mean HDL size (Franceschini et al 2013).…”

Pharmacotherapy and HDL Cholesterol

“…In contrast to fibrates, nicotinic acid exerts a larger effect on HDL 2 than HDL 3 [57][58][59]. Conversely these agents are less potent than fibrates in reducing triglyceride levels with reductions generally around 20%.…”