Lipid lowering agents

Drug	Mechanism of action	Adverse effect	Indication
Hydroxymethyl-glut-aryl coenzyme A (HMG CoA) reductase inhibitors : Statins like atorvastatin, lovastatin, rosuvastatin, simvastatin etc.	Decreased synthesis of cholesterol by inhibiting the rate limiting enzyme of cholesterol synthesis. Indirectly activates SREBP 2* causing increased expression of LDL receptors on the cell surface, increasing cellular uptake of LDL	Myalgia, myopathy, increased creatine kinase, myositis, rhabdomyolysis, hepatotoxicity, elevated liver enzymes; Statin plus gemfibrozil or niacin increases the risk of severe myopathy	Lower LDL; Lower triglycerides; Raise HDL
Ezetimibe	Inhibits NPC1L1 or Niemann Pick C1 like 1, an intestinal protein promoting cholesterol absorption	Elevated liver enzymes, diarrhea	Lower LDL
Fibrates: gemfibrozil, fenofibrate	Activate PPAR** alpha increasing the oxidation of free fatty acids, decreases triglyceride synthesis by the liver, increases the expression of lipoprotein lipase	Myopathy, cholesterol gallstones	Lower triglycerides; Increase HDL; Lower LDL
Bile acid sequestrants/resins: cholestyramine, colestipol	Prevent enterohepatic recycling of bile acids, leading to increase in using hepatic cholesterol to form bile acids, thereby decreasing serum cholesterol levels and increasing LDL receptor synthesis	Nausea, GI upset, decreased absorption of drugs and fat soluble vitamins	Lower LDL
Niacin (vitamin B3)	Inhibits the release of fatty acids from adipose tissue, decreases hepatic uptake of fatty acids and decreases triglyceride synthesis by the liver	Skin flushing, dizziness, hypotension, tachycardia, itching, gout, diarrhea, hyperglycemia/diabetes, liver damage; Flushing occurs due to increased arachidonic acid and prostaglandin D2 and E2 with cutaneous vasodilation. Aspirin taken 30 minutes before niacin prevents flushing.	Lower triglycerides; Lower LDL; Increase HDL
Omega three fatty acids	Decrease hepatic synthesis and secretion of VLDL; increase activity of lipoprotein lipase, decrease lipogenesis, anti-inflammatory	Headache, nausea, diarrhea, heartburn, bleeding tendency if used with anticoagulants	Lower triglycerides
PCSK9 or proprotein convertase subtilisin/kexin type 9 inhibitors: Evolocumab and alirocumab are monoclonal antibody to PCSK9	Inhibit enzyme PCSK9 that degrades LDL receptors	Myalgia, delirium, dementia	Lower LDL; Lower triglycerides; Increase HDL
Inhibitors of apolipoprotein B synthesis: mipomersen	Inhibits Apo B synthesis in the liver	Injection site reactions, flu-like syndrome, headache, elevation of liver enzymes	Lower LDL; Lower VLDL; Lower Lp(a)
Inhibitors of microsomal triglyceride transfer protein or MTP: lomitapide	Binds to and inhibits MTP thus preventing the transfer of triglycerides to Apo B	Nausea, gastrointestinal upset, elevation of liver enzymes	Lower LDL especially in patients who lack LDL receptors

*SREBP 2 is sterol regulatory element binding protein

**PPAR alpha is peroxisome proliferator activated receptor alpha