Module 10 Lipid Management

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HGM CoA Reductase Inhibitors
Statins

Back 1

Prevents formation of cholesterol in hepatocytes, and upregulates LDL receptors which increases hepatic uptake of LDL from plasma
Rosuvastatin (2.5), Atorvastatin (5), Simvastatin (10), Pravastatin (20), Lovastatin (20), Fluvastatin (40)
AE myopathy, myositis, rhabdomyolysis, elevated transaminases,
Atorv/Simva/Lova metabolized by 3A4
used in combo bile sequestrants, absorption inhib, naicin and fibrates (N & F increase risk rhabdo)

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Bile Acid Sequestrants

Back 2

Choleystiramine, Colesevalem, Colestipol
Cationic polymer resins bind (noncovalent) to negatively charged bile acids in small intestines and complex connot be absorbed, decreased bile acid reabsorption by ileum partially interrupts enterohepatic bile acid circulation l/t hepatocytes upregulation 7a-hydroxylase the rate limiting step in bile acid synthesis which decreases hepatocyte cholesterol concentration which increases expression of LDL Rc and LDL clearance from circulation increases
Dose 1h after meals,
AE Gi effects (bloating, dyspepsia) interacts with other drugs, decrease absorption of fat soluble vit

Front 3

Cholesterol Absorption Inhibitors

Back 3

Plant sterols, Ezetimibe
reduction of cholesterol absorption by the small intestine, compensatory increase in hepatic cholesterol synthesis possible, ised in combo w/ statins
systematically absorbed but well tolerated
metabolized by glucoronidation

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Fibrates

Back 4

Gemfibrozil, fenofibrate, clofibrate
PPAR-alpha activation leads to increase HDL and decreased triglycerides
AE GI discomfort, increased transaminases, rare myopathy arrhythmias
Drug interactions displace warfarin from albumni, increase cyclosporin clearance

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Niacin

Back 5

Increase plasma HDL and decrease triglyceride synthesis
AE cutaneous flushing (relaese of prsotaglandins w/i skin) pretx with ASA Nsaid, pruritis, myopathy, impaired insulin sensitivity

Front 6

Omega-3 Fatty Acids

Back 6

Eicosapantaenoic acid 9EPA) and docosahexaenoic acid (DHA) RX Lovaza
Reduce triglyceride biosynthesis and increase fatty acid oxidation in liver