Term
Cholestryamine, Colestipol (mechanism of action and clinical application) |
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Definition
Bile Acid Sequestrant; Bile Acid binding Resin
Used to treat Elevated LDL levels |
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Term
Cholestryamine, Colestipol (effect) |
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Definition
↑ the fecal excretion of bile salts and cholesterol; ↓ in cholesterol is also d/t up regulation of LDL receptors in the liver |
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Term
Cholestryamine, Colestipol (side effect other jazz) |
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Definition
SE: Constipation, Deficiency of Fat Soluble vitamins, Increased Triglycerides (ppt. pancreatitis)
NB: These binding resins are neither digested nor absorbed
NB: There is a compensatory ↑ in the activity of HMG CoA reductase resulting in ↑ cholesterol synthesis & ↑ VLDL secretion (Transient effect) |
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Term
Lovastatin, Simvastatin (mechanism of action and clinical use) |
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Definition
HMG CoA reductase Inhibitor
Used to treat elevated LDL levels; Cardio protective actions |
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Term
Lovastatin, Simvastatin (effect) |
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Definition
• ↑ in LDL receptor expression on the liver; Hepatic synthesis of VLDL is ↓; ↑ in HDL • Also has cardio protective actions: ↑ endothelial NO synthesis, plaque stability, anti-inflammatory action, ↑ activity of paraoxonase (anti-oxidative enzyme); anti-coagulation |
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Term
Lovastatin, Simvastatin (side effects other jazz) |
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Definition
SE: Headaches, Sleep disturbances, Hepatotoxicity, Myopathy (Rhabdomyolysis) Contraindication: Pregnancy (b/c inhibits progesterone)
NB: Both drugs are lipid soluble, so they can cross the BBB and cause side effects: headaches ; Metabolized by CYP450 |
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Term
Atorvastatin , Rosuvastatin (mechanism of action and clinical use) |
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Definition
HMG CoA reductase Inhibitor
Used to treat elevated LDL levels; Cardio protective actions (↓VLDL = ↓ TG) |
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Term
Atorvastatin , Rosuvastatin (effect) |
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Definition
• ↓Liver Cholesterol • ↑ in LDL receptor expression on the liver; Hepatic synthesis of VLDL is ↓; ↑ in HDL • Also has cardio protective actions: ↑ endothelial NO synthesis, plaque stability, anti-inflammatory action, ↑ activity of paraoxonase; anti-coagulation |
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Term
Atorvastatin , Rosuvastatin (side effects and other jazz) |
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Definition
SE: Sleep disturbances, Hepatotoxicity, Myopathy (Rhabdomyolysis)
Contraindication: Pregnancy (b/c inhibits progesterone)
NB: These drugs do not cross the BBB; Atovastatin has an anti-oxidant effects; Rosuvastatin is the MOST potent; Metabolized by CYP450 |
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Term
Fenofibrate ; Gemfibrozil (mechanism of action and clinical use) |
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Definition
Fibric Acid Derivatives; PPAR α agonist
Works best to treat High Triglycerides |
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Term
Fenofibrate ; Gemfibrozil (effect) |
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Definition
• Act by activating lipoprotein lipase (LPL) which is a key enzyme in the degradation of VLDL--- resulting in lowering of TG, also ↓ VLDL secretion, ↓ LDL levels, ↑ HDL synthesis |
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Term
Fenofibrate ; Gemfibrozil (side effects and other jazz) |
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Definition
SE: Gallstones, Myopathy
NB: PPAR α agonist involved in the regulation of carbohydrate & lipid metabolism (causes transcript. of a # of genes of DNA that facilitate lipid metabolism) |
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Term
Nicotinc Acid (mechanism of action and clinical use) |
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Definition
Broad spectrum antihyperlipidemic drug
Works Best to treat low HDL levels d/t ↑ LDL &/or TG |
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Term
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Definition
• ↓ VLDL & TG production results in a ↓ exchange of Cholesterol esters & TG & a subsequent ↑ in HDL • Acts on a G-protein to ↓ cAMP, ↓ activity of HSL which ↓FA in circulation |
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Term
Nicotinc Acid (side effects) |
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Definition
SE: Cutaneous Dilator (flushing, itching), Liver dysfunction, Gout, Hyperglycemia (do not want to give to DM patient) |
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Term
Ezetimibe (mechanism of action and clinical use) |
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Definition
Antihyperlipidemic
Used to Lower Cholesterol |
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Term
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Definition
• Inhibits cholesterol absorption by enterocytes of the small intestine by localizing at the brush border • Ultimately this leads to a ↓ cholesterol absorption which leads to an ↑ in LDL-Cholesterol uptake into cells, thus ↓LDL & TG levels in the plasma |
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Term
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Definition
NB: Can be used in combination with a statin which has been shown to lower cholesterol by 25% more than a statin alone (Ezetimibe + Simvastatin = Vytorin) |
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