Hyperlipidemia drugs

Question 1

cholesterol drug classes that affect exogenous pathway?

Answer 1

bile acid resins

transport inhibitors

Question 2

cholesterol drug classes that affect endogenous pathway?

Answer 2

statins
fibric acid
acid- niacin

Question 3

Bile acid resin drugs?

Answer 3

cholestyramine

colestipol

Question 4

cholestyramine/colestipol MOA

Answer 4

bind negatively-charged bile acids in small intestine-forming insoluble complex excreted in feces
loss of bile acids leads to increase in LDL uptake receptors–>reduced plasma cholesterol

Question 5

cholestyramine/colestipol TOX

Answer 5

increase TG levels in first few weeks
bad taste-like drinking sand
bloating
constipation/steatorrhea, anal leakage/fissures
impairment of other drug and fat soluble vitamin absorption
decrease LDL, slight increase of HDL, TG

Question 6

Ezetimibe MOA

Answer 6

class: transport inhibitor
prevent cholesterol reabsorbtion at small intestine brush border
additive decrease in LDL when used with statins
little effect on HDL/TG

Question 7

Ezetimibe TOX

Answer 7

Rare hepatic toxicity
drug interaction with cyclosporine
elevated transaminases

Question 8

HMG CoA reductase (statins) MOA

Answer 8

inhibit HMG CoA reductase which catalyzes the conversion of acetyl CoA to melvonic acid
liver increases LDL receptors in response to low hepatic cholesterol causing increased reuptake
anti-inflammatory by reducing c reactive protein

Question 9

HMG CoA reductase (statins) Uses

Answer 9

preferred lipid lowering drug

decrease LDL. TG, increase HDL

Question 10

HMG CoA reductase (statins) TOX

Answer 10

hepatotoxicity-check liver enzymes
rhabdomyolysis- myopathy rare but life threatening
contraindicated with CYP450 inhibitors

Question 11

deciding between older and newer statins?

Answer 11

older- cheaper, safer, more reliable

newer- more potent and efficacious, decrease LDL with smaller dose to minimize SEs

Question 12

Niacin MOA

Answer 12

inhibition of VLDL secretion into circulation

inhibits lipolysis in adipose tissue

Question 13

Niacin USE

Answer 13

most effective drug for increasing HDL

reduction in LDL and TG

Question 14

Niacin TOX

Answer 14

only acid form is active- need to check vitamin OTC
intense flushing and pruritis
nausea, abd pain
hyperuricemia
hyperglycemia
hepatotoxicity

Question 15

Fibrates?

Answer 15

GEMFIBROZIL
CLOFIBRATE
bezafibrate
fenofibrate

Question 16

fibrate MOA

Answer 16

enhance lipoprotein lipase, increasing TG clearance
decrease fatty acid synthesis
stimulates synthesis of apoA1 which increases HDL

Question 17

fibrate use

Answer 17

DECREASE TG

minor decrease LDL and increase HDL

Question 18

fibrate TOX

Answer 18

myositis-worse with statins
hepatotoxicity
cholesterol gallstones

Question 19

Rules for lipid treatment

Answer 19

rule out secondary dyslipidemia from:
diabetes, hypothyroid, obstructive liver disease, chronic renal failure
know target levels for individualized patients with other conditions
use COMBO therapies for resistant lipid profiles