Review of extended-release niacin/laropiprant fixed combination in the treatment of mixed dyslipidemia and primary hypercholesterolemia

Abstract

Although statins reduce cardiovascular morbidity and mortality further risk reduction is needed. In this respect low HDL-cholesterol concentrations and/or elevated triglyceride concentrations may be potential treatment targets. Niacin (nicotinic acid) is an effective drug which increases the plasma concentration of high-density lipoprotein (HDL)-cholesterol and decreases the concentration of low-density lipoprotein (LDL)-cholesterol, triglycerides and lipoprotein(a). Clinical studies indicate that niacin can significantly reduce the risk for cardiovascular events. However, niacin is not very commonly used because of significant side effects (especially flushing). Laropiprant is a potent selective antagonist of PGD2-receptor subtype-1 and can thus reduce niacin-induced flushing. Although the addition of laropiprant will reduce the frequency of flushing, it will not completely eliminate this side effect. Laropiprant does not change the effect of niacin on lipids or other side effects of niacin (ie, gastro-intestinal problems, glucose elevation). The combination of niacin with laropiprant may therefore enable use of niacin at higher doses and therefore exploit the full potential of the drug. Endpoint studies that will be published over the next few years will show whether this treatment modality also translates into clinical effect in patients treated with statins. Until publication of these studies niacin/laropiprant should be used only in high-risk patients not achieving lipid goals on statins.

Keywords: dyslipoproteinemia; flushing; hyperlipidemia; nicotinic acid.

Figure 1

The figure describes a possible algorithm for treating patients with different forms of dyslipidemia. Notes: ^aIn patients with established cardiovascular disease lifestyle modification and drug therapy will usually be implemented simultaneously; ^bisolated hypertriglyceridemia refers to a LDL-cholesterol < 100 mg/dL and elevated triglycerides; fibrates, omega-3 fatty acids or ERN/LRPT may be used if lifestyle modification is not sufficient; in selected patients combination therapy may be necessary; ^cif LDL-cholesterol goal is not achieved the statin dose may be increased or switched to a more potent statin; ^dstatin/fibrate combination is associated with significant side effects and should therefore be only used in selected patients. Abbreviations: ω-3-FA, omega-3 fatty acids; ERN/LRPT, extended release niacin/laropiprant.