• Atorvastatin, simvastatin, rosuvastatin, pitavastatin • Fluvastatin, pravastatin, lovastatin: Similar but somewhat less efficacious • Fenofibrate,gemfibrozil Peroxisome proliferator-activated receptor-alpha (PPAR-α) agonists Decrease secretion of very-low-density lipoproteins (VLDL)•increaselipoproteinlipaseactivity•increasehigh-density lipoproteins (HDL) Hypertriglyceridemia, low HDL Oral•duration3–24h•Toxicity: Myopathy, hepatic dysfunction FIBRATES
Subclass, Drug Mechanism of Action Effects Clinical Applications Pharmacokinetics, Toxicities, Interactions • Cholestyramine, colesevelam: Similar to colestipol • EzetimibeBlocks sterol transporter NPC1L1 in intestine brush border Inhibits reabsorption of cholesterol excreted in bile •decreasesLDLandphytosterolsElevated LDL, phytosterolemia Oral•duration24h•Toxicity: Low incidence of hepatic dysfunction, myositis
Decreases catabolism of apoAI•reducesVLDLsecretion from liver IncreasesHDL•decreaseslipoprotein(a) [Lp(a)], LDL LowHDL•elevatedVLDL,Lp(a); elevated LDL in statin-unresponsive or intolerant patients Oral•largedoses•Toxicity: Gastric irritation, flushing, low incidence of hepatic toxicity •mayreduceglucosetolerance• Extended-release niacin: Similar to regular niacin • Sustained-release niacin (not the same as extended-release product): Should be avoided PCSK9 HUMANIZED MONOCLONAL ANTIBODIES Evolocumab Complexes PCSK9 Inhibits catabolism of LDL receptor Familial hypercholesterolemia not Parenteral•Cost~$14,000/year•Toxicity: injection site reactions, nasopharyngitis, responsive to oral therapy • Alirocumab Similar to evolucumab flu-like symptoms, rarely myalgia, neurocognitive and ophthalmologic events
Atorvastatin Generic, Lipitor
Cholestyramine Generic, Questran, Prevalite
Colestipol Generic, Colestid
Ezetimibe Generic, Zetia
Fenofibrate Generic, Tricor, Antara, Lofibra
Fluvastatin Generic, Lescol, Lescol XL
Gemfibrozil Generic, Lopid
Lovastatin Generic, Mevacor, Altoprev
Niacin, nicotinic acid, vitamin B3 Generic only
Pravastatin Generic, Pravachol
Rosuvastatin Generic, Crestor
Simvastatin Generic, Zocor
Afshar M, Thanassoulis G: Lipoprotein(a): new insights from modern genomics. Curr Opin Lipidol 2017;28:170.
Ballantyne CM et al: Efficacy and safety of a novel dual modulator of adenosine triphosphate-citrate lyase and adenosine monophosphate-activated protein kinase in patients with hypercholesterolemia: Results of a multicenter, randomized, double-blind, placebo-controlled, parallel-group trial. J Am Coll Cardiol 2013;62:1154.
Boekholdt SM et al: Levels and changes of HDL cholesterol and apolipoprotein A-I in relation to risk of cardiovascular events among statin-treated patients: A meta-analysis. Circulation 2013;128:1504.