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