Drugs That Lower LDL Cholesterol Levels
Repatha
- PCSK9 inhibitor - PCSK9 = attached to LDL receptors to tell the liver to get rid of the receptor --> without enough receptors = LDL numbers too high - injected monoclonal antibodies
Cholestyramine (Questran)
- bile acid sequestrant - increases LDL receptors on hepatocytes - prevents re-absorption of bile acids - biologically inert - low-fat diet - adverse effects = constipation, decreased absorption of fat-soluble vitamins
Colesevelam (Welchol)
- bile acid sequestrant - new, better tolerated
Gemfibrozil (Lopid)
- fibric acid derivatives (fibrates) - effects on plasma lipoproteins = decreases plasma TG content, lowers VLDL levels, raises HDL choleseterol - MOA = unknown - reduces high levels of plasma triglycerides (VLDLs) - adverse effects = rashes, GI, gallstones myopathy, liver injury (hepatotoxic)
Praluent
- monoclonal antibody for LDL lowering - the newest one
Nicotinic Acid (Niacin, Niacor)
- reduces LDL and TG levels - increases HDL levels better than any other drug - decreases production of VLDLs - therapeutic use = lowering TG levels, elevating HDL choleseterol - niacin-lovastatin combo - slow-release formulation, Niaspan and Slo-Niacin - multiple MOA = inhibition of lipolysis in adipose tissue, vitamin - adverse effects = skin (flushing), GI, hepatotoxicity, hyperglycemia
Lovastatin (Mevacor)
- statins - dec choleseterol production - inc LDL receptors - lowers LDL - dose dependent - adverse effects = well-tolerated, headahce and rash, hepatotoxicity, muscle weakness, rhabdomyolysis, two-fold higher blood level of Crestor in Asians
Lipitor and Mevacor
- statins - most effective drugs for lowering LDL - reduction of LDL cholesterol - evelavation of HDL cholesterol - nonlipid beneficial cardiovascular actions = reduce risk of CV events, increased bone formation
Ezetimibe (Zetia)
- widely used and unique drug - blocks cholesterol absorption - generally well-tolerated - combined with diet modification or monotherapy - can be combined with a statin - some drug interactions