Chapter 21: Hyperlipidemias

Question 1

What is the MOA, indications, pharmokinetics, and adverse effects of HMG CoA reductase inhibitor? (Drug that lowers serum [lipoprotein])

Answer 1

MOA: inhibits HMG CoA reductase; Lovastatin, simvastatin, pravastatin, atorvastatin, fluvastatin, pitavastatin, rosuvastatin are all analogs of HMG (precursor of cholesterol)
-increase LDL receptors to increase catabolism of LDL

indications: effective in lowering plasma cholesterol levels in all types of hyperlipidemias
pharmokinetics: oral; excretion through bile/feces

adverse effects: liver function, myopathy and rhabdomyolysis, drug interacts with warfarin; contraindicated in pregnancy and in nursing mothers

Question 2

What is the MOA, indications, pharmokinetics, and adverse effects of Niacin?

Answer 2

MOA: decreases lipolysis in adipose tissue to lower free floating fatty acids; increases HDL cholesterol levels

indications: familial hyperlipidemias
pharmokinetics: excreted in urine

adverse effects: intense cutaneous flushing and pruritus ; inhibits tubular secretion of uric acid

Question 3

What is the MOA, indications, pharmokinetics, and adverse effects of the fibrates: Fenofibrate and Gemfibrozol?

Answer 3

MOA: fibrate mediated gene expression leads to decreased triacylglycerol concentrations by increasing expression of lipoprotein lipase

indications: used to treat hypertriacylglycerolemias
pharmokinetics: completely absorbed after oral dose

adverse effects: GI disturbances, lithiasis, myositis,

Question 4

What is the MOA, indications, pharmokinetics, and adverse effects of Bile acid-binding resins?

Answer 4

MOA: Cholestyramine, cholestipol, colesevelam bind extra bile acids and excrete them in the feces, preventing bile acids from returning to the liver ;
-lowering bile acid forces liver to make more by converting cholesterol to bile acids

Question 5

What is the MOA, indications, pharmokinetics, and adverse effects of Bile acid-binding resins?

Answer 5

MOA: Cholestyramine, cholestipol, colesevelam bind extra bile acids and excrete them in the feces, preventing bile acids from returning to the liver ;
-lowering bile acid forces liver to make more by converting cholesterol to bile acids

indications: drug of choice in treating Type IIA and Type IIB hyperlipidemias
pharmokinetics: taken orally and excreted in feces

adverse effects: GI disturbances, impair absorption of fat soluable vitamins, drug interactions

Question 6

What is the MOA, indications, pharmokinetics, and adverse effects of Ezetimibe? (Cholesterol absorption inhibitor)

Answer 6

MOA: inhibits absorption of dietary and biliary cholesterol; lowers LDL and triacylglycerols, increases HDL