hyperlipidemia drugs

Question 1

Statins

Answer 1

HMG-coA reductase inhibitors - stops our body from making cholesterol from acetyl coA, also increases LDL receptors on hepatocytes = lower plasma LDL, may also decrease plasma triglycerides and raise HDL

DOC for familial hypercholesterolemia or defective apoB100, also best for combined hyperlipidemia (sometimes combine with fibrates or niacin)

four groups of individuals that should be on statin: with clinical athersclerotic events (angina, MI), LDL-C > 190, 40-75 yo with diabetes and LDL 70-189, 40-75 yo witout atherosclerotic disease with LDL 70-189 with 10 year ASCVD of 7.5% or higher

first line therapy for increased LDL levels - dont use in preg women

best given at night (when chol synthesis occurs)

AE: can get transient elevations in serum aminotransaminase - but hepatic tox is usually not a problem, can cuase increased creatinine kinase activity = rhabdomyolysis

simvistatin cuased rhabdomyolysis is made worse in patienst taking amiodarone

pro drugs - lovastatin, simvastatin

Question 2

Niacin

Answer 2

can use for treatment of defective apoB100

water soluble vitamine converted to amide -> incorperated into niacinamide adenine dinucleotide (NAD) and excreted in urine

imporves virtually every lipid parameter (LDL, triglycerides, elevate HDL)

DOC: patienst with elevated LDL and lowered HDL

tox: cutanous flushing (increase prosta levels)

Question 3

fenofibrate

Answer 3

fibrates

activate hepatic PPAR-a = decreases plasma triglycerides, VLDL, LDL, increase HDL

DOC for treatment of familial hypertriglyceridemia and dysbetalipoprotinemia

may increase risk of myopathy in patienst on statins

Question 4

gemfibrozil

Answer 4

fibrate

may enhance rhabdomyolysis in statins

Question 5

omega 3 FA

Answer 5

activate PPARa (like fibrates)

dont use omega 6 found in veg oil - this can increase triglycerides

Question 6

cholestyramine

Answer 6

bile acid binding resin - they bind to the bile acids (cant reabsorb them)

less reabsorption of bile acid chol

lowers LDL and increases HDL

tox: bloating and constipation , they may decrease abosrption of fat soluble vits (ADEK)

use for primary hypercholestreolemia, may reduce VLDL, may be used for digoxin tox

Question 7

colesavelam

Answer 7

bile acid binding resin

Question 8

colestipol

Answer 8

bile acid binidng resin

Question 9

ezetimibe

Answer 9

sterol uptake inhibitor

less cholesterol intake from food

used for treatment of hypercholesteormia

Question 10

Simcor

Answer 10

drug combo - extended relase niacin plus simvastatin

combs are good when: VLDL levels increase during resin therapy for hypercholesteronmia, VLDL and LDL are elevated, VLDL or LDL are not normalized by a single drug, elevated lipoprotien A or HDL deficiency occurs with other hyperlipidemias

Question 11

vytorin

Answer 11

drug combo - ezetimibe plus simvastatin