| 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
|
