Pharm Hyperlipidemia (Block 1)

Front 1

Cholestyramine, Colestipol

Back 1

Quart Ammonium Anion Exchange Resin; NOT Absorbed

Binds Bile Acids in Intestine, Preventing Bile Reabsorption and Enterohepatic Circulation

Uses:
1) Type IIa Primary Hypercholesterolemia
2) Type IIb Multifactorial
3) Pruritus associated with Biliary Obstruction

Side Effects:
1) Increased Hepatic VLDL Assembly and Secretion
2) Nausea
3) Constipation
4) Diarrhea

Drug Interactions:
Interferes with absorption of ACIDIC Drugs:
1) Digitalis
2) Warfarin
3) Phenobarbital
4) Tetracycline
Interferes with Absorption of Fat-Soluble Vitamins (DEAK)

Front 2

Cholesevelam (Welchol)

Back 2

Newest member of Anion Exchange Resin Family

Binds Bile Acids

Fewer drug-drug interactions than Cholestyramine and Colestipol

Front 3

Lovastatin (Mevacor)

Back 3

Competitive Inhibitor of HMG-CoA Reductase

Uses:
1) Hypercholesterolemia
2) Mixed Hyperlipidemia (in combo)
3) Promote regression of established atherosclerotic plaques


Benefits not attributable to altered cholesterol metabolism:
1) Decreased Smooth Muscle Proliferation and Migration
2) Increased Bone Formation in Women
3) Anti-Inflammatory
4) Decreases some Cancers

Side Effects:
1) Hepatotoxicity
2) Myopathy (Rhabdomyolysis with Myalgia, with or without acute renal failure secondary to myoglobiniurtia.
3) Increased risk of Myopathy in two drug regimens with Niacin or Gemfibrozil
4) DONT Use if Pregnant
5) DONT Use if Nursing

Front 4

Rosuvastatin (Crestor)

Back 4

"Super-Statin"

Reductions in LDL as high as 55%!

Front 5

Ezetimibe (Zetia)

Back 5

Interferes with Cholesterol Absorption from Gut at Enterocyte (Interacts with Neimann-Pick C1-Like Protein NPC1L1)

Uses:
1) Hypercholesterolemia
2) Phytosterolemia

Adverse Reactions:
1) Hypersensitivity or Anaphylactoid Reactions
2) Depression
3) Nausea/Vomiting
4) Cholecystitis
5) Cholelithiasis
6) Pancreatitis
7) Thrombocytopenia

Unlike some statins, has NOT been shown to prevent Heart Disease or Heart Attacks!

Front 6

Niacin, Nicotinic Acid

Back 6

Inhibits Lipolysis in Adipose Tissue by Decreasing cAMP

Uses:
1) MOST Potent to Increase HDL!
2) Combo with Resins for Hypercholesterolemia and Mixed Hyperlipidemia
3) Hypertrigylceridemia

3-5 Weeks Required for Maximal Effect

Adverse Reactions:
1) Cutaneous Flushing and Pruritus
2) GI Disturbances (Peptic Ulcer)
3) Liver Dysfunction (Jaundice)
4) Impaired Glucose Tolerance
5) Increase Plasma Uric Acid

Contraindications:
1) Peptic Ulcer
2) Hepatic Disease
3) Diabetes
4) Gout or Gouty Arthritis
5) Cardiac Arrhythmias
6) Slow Release Formulation --> Hepatic Toxicity and a Hepatitis-Like Syndome: Nausea, Lethargy, Loss of Appetite

Front 7

Fenofibrate (Tricor), Clofibrate

Back 7

Binds to PPAR, Increases LPL Activity

Uses:
1) Type III Familial Dysbetalipoproteinemia who do NOT respond to Gemfibrozil

Adverse Effects:
1) Cholelithiasis
2) Cholecystitis
3) Flu-Like Syndrome

Cardiac Arrhythmias in CAD:
1) Displaces Warfarin from Albumen Binding Site
2) Has a DIRECT effect to INHIBIT Platelet Aggregation

Front 8

Gemfibrozil (Lopid)

Back 8

Activates PPAR, Increase LPL Activity

Uses:
1) Hypertriglyceridemia
2) Mixed Hyperlipidemia (in combo)

Adverse Effects:
1) GI Disturbances
2) Rash
3) Increased activity of LPL
4) Increased Cell membrane LDL Receptors
5) Increased LCAT

Front 9

Atorvastatin (Lipitor)

Back 9

Competitive Inhibitor of HMG CoA Reductase AND Inhibits Hepatic Synthesis of VLDL

May not increase HDL as much as other statins.