Integrated Scipharmacology-Lipid Lowering Agents

Front 1

Atorvasatin (Lipitor)
Lovastatin (Mevacor)
Simvastatin (Zocor)
Fluvastatin (Lescol)
Pravastatin (Pravachol)
Rosuvastrestatin (Crestor)

Note -statin ending
Class?
Indication?
MOA?
AE?

Back 1

Class: HMG CoA reductase inhibitors
Lipid lowering agents

Indication: Lower total and LDL cholesterol, triglycerides, slightly increase HDL

MOA:Competitively inhibits the formation of cholesterol in hepatocytes; upregulates LDL receptors, increases LDL uptake in to hepatocytes and remove from plasma

AE: Pregnancy Category X, pain in skeletal muscle accompanied by increased creatinine kinase activity, rhabdomyolysis, hypersensitivity, hepatotoxicity, drug interactions increase adverse effect with other lipid lowering drugs, CYP3A4 enzyme- increase level of statin with citrus fruits

Front 2

Gemfibrozil (Lopid)
Fenofibrate (Tri-cor, Lofibra)

Class/action?
Indication?
MOA?
AE?

Back 2

Class/action: Fibrates that act as lipid lowering agents

Indication: Plasma triglyceride decreased and plasma HDL is increased.

MOA: bind to PPARa (nuclear receptor in hepatocytes, skeletal muscle, macrophages & heart(, increases trascription, increasing uptake of triglycerides into muscle, decreased inhibition of tryglycerides and increase HDL

AE? rash, myopathy, cholesterol gallstone, GI discomfort, hepatotoxic

Front 3

Colestipol (Colestid)
Cholestryramine (Questran; Prevalite)
Colesevelam (WelChol)

Class/action?
Indication?
MOA?
AE?

Back 3

Class/use: bile acid sequestrants that lower cholesterol

Indication: Management of primary hypercholesterolemia

MOA:Insoluble polymers that bind bile acids in the gut, upregulates bile acid synthesis which decrease cholesterol in hepatocytes, increase LDL clearance from plasma

AE: GI specific- constipation, bloating, nausea, malabsorption of vitamin K and fat-soluble vitamins, Pregnancy category C

Front 4

Niacin/Nicotinic acid

Indication?
MOA?
AE?

Back 4

Indication: Increase HDL synthesis, used as supplement to reduce cholesterol

MOA: Inhibits synthesis of VLDL and LDL, increase rate of chylomicron triglyceride removal from plasma

AE: Cutaneous flushing, pruritis, hyperuricemia, gouty arthritis, impaired insulin sensitivity, hyperglycemia, myopathy

Front 5

Ezetimibe (Zetia)

Class/Indication?
MOA?
AE?

Back 5

Class/Indication: Cholesterol absorption inhibitors. Use in conjunction with statins to further lower cholesterol

MOA: Inhibits absorption of cholesterol at the brush border, decrease delivery of cholesterol to liver, reduce hepatic cholesterol stores (work inside enterocytes)

AE: Very few noted, considered a "safe" drug. This is a new (2003) drug