This study compared the efficacy and safety of a once-a-night, time-release
niacin formulation, Niaspan (Kos
Pharmaceuticals, Miami Lakes, FL), with plain
niacin and placebo for the treatment of primary
hypercholesterolemia. The study was conducted in nine academic
lipid research clinics in a randomized, double-blind design. Niaspan 1.5 g at bedtime was compared with plain
niacin 1.5 g/d after 8 weeks and 3.0 g/d after 16 weeks in divided doses and with placebo. A total of 223 hypercholesterolemic adult men and women participated. Compared with placebo at 8 weeks, Niaspan versus plain
niacin at 1.5 g/d showed comparable efficacy, comparably lowering total
cholesterol (C) (8%/8%),
triglycerides (16%/18%),
low-density lipoprotein (
LDL)-C (12%/12%),
apolipoprotein (
apo B) (12%/12%),
apo E (9%/7%), and
lipoprotein(a) [Lp(a)] (15%/11%), and raising
high-density lipoprotein (HDL)-C (20%/17%), HDL2-C (37%/33%), HDL3-C (17%/16%), and
apo A-I (8%/6%) (P < or = .05 in all instances). After 16 weeks, the Niaspan effect on
LDL-C and
triglyceride was unchanged while the plain
niacin effect approximately doubled. At equal doses of 1.5 g/d of Niapan versus plain
niacin, respectively, AST increased 5.0% versus 4.8% (difference not significant [NS]), fasting plasma
glucose increased 4.8% versus 4.5% (NS), and
uric acid concentrations increased less, 6% versus 16% (P=.0001).
Flushing events were more frequent with plain
niacin versus Niaspan (1,905 v 576, P < .001).
Flushing severity was slightly greater with Niaspan, but still well tolerated. In conclusion, Niaspan 1.5 g hour of sleep (hs) has comparable efficacy, a lower incidence of
flushing, a lesser
uric acid rise, and an equivalent hepatic
enzyme effect than 500 mg thrice-daily plain
niacin in hyperlipidemic subjects. Niaspan may be an equivalent or better alternative to plain
niacin at moderate doses in the management of
hyperlipidemia.