Lipid lowering drugs

Question 1

Genetic defect in the metabolism of cholesterol is majority or minority of population?

Answer 1

minority

Question 2

What are the secondary causes of lipid disorders that most of the population has?

Answer 2

increased fat intake, obesity, type II DM, advanced age, hypothyroidism, obstructive liver disease, drug induced

Question 3

What does untreated hyperlipidemia lead to?

Answer 3

acute pancreatitis (hypertriglycerides) and atherosclerosis (hypercholesteremia–plasma cholesterol)

Question 4

What 2 things does atherosclerosis lead to?

Answer 4

macrovascular complications, microvascular complication

Question 5

What are examples of macrovascular complications?

Answer 5

unstable angina, MI, ischemic cerebrovascular disease, CAD

Question 6

What are examples of microvascular complications?

Answer 6

Retinopathy, nephropathy

Question 7

What are lipoproteins?

Answer 7

macromolecular lipid plus protein complexes that transport lipids to and from peripheral tissues

Question 8

How are lipoproteins classified?

Answer 8

based on density

Question 9

Are the lipid and protein portions directly related or inversely related?

Answer 9

inversely related

Question 10

What are the 5 kinds of lipoproteins in order from least protein content to most?

Answer 10

Chylomicrons, Very-Low density lipoproteints (VLDL), Intermediate density lipoproteins (IDL), Low density lipoproteins (LDL), and High density lipoproteins (HDL)

Question 11

How do you prevent HLD?

Answer 11

decrease triglycerides, cholesterol, and LDL, increase HDL

Question 12

What’s the optimal value for LDL?

Answer 12

<100mg/dl

Question 13

What’s the optimal value for cholesterol?

Answer 13

<200mg/dl

Question 14

What’s the optimal value for triglycerides?

Answer 14

<150mg/dl

Question 15

What’s the optimal value for HDL?

Answer 15

> 60mg/dl, 40mg/dl the low end

Question 16

What’s exogenous lipoproteins?

Answer 16

dietary fats, cholesterol, lipid soluble vitamins

Question 17

What’s endogenous lipoproteins?

Answer 17

hepatic cholesterol synthesis

Question 18

Who do the currently guidelines by ACC and AHA advocate for statin use for?

Answer 18

1)clinical evidence of ASCVD, 2)LDL >190, 3) age 40-70 with DM and LDL 70-189, 3)age 40-75 without DM, LDL 70-189, and an estimated 10 year risk of ASCVD.

Question 19

When preop should you implement a statin?

Answer 19

recommended start 30 days-1week prior to high risk surgery

Question 20

What are statins isolated from?

Answer 20

strain of aspergillus terreus

Question 21

What is a natural statin?

Answer 21

lovastatin

Question 22

What are the semi-synthetic statins?

Answer 22

simvastatin, pravastatin

Question 23

What are the synthetic statins?

Answer 23

atorvastatin, fluvastatin, rosuvastatin

Question 24

What is the most effective drug we have to lower LDL?

Answer 24

statins

Question 25

What else do statins do?

Answer 25

improve plaque stability, enhance endothelial function, decrease oxidative stress, decrease vascular inflammation

Question 26

What does zetia do?

Answer 26

enhances statin and decreases triglycerides

Question 27

What is another name for statin?

Answer 27

HMG-CoA reductase inhibitors

Question 28

What are the 2 MOA of statins?

Answer 28

inhibit cholesterol synthesis, competitively inhibit HMG-CoA reductase causing increased hepatic LDL-R: reduces LDL concentration from 20-60%, increase HDL 10%

Question 29

Are statins sufficient in reducing tryglycerides?

Answer 29

no, they decrease cholesterol

Question 30

Which 2 statins are prodrugs needing metabolism to become activated?

Answer 30

simvastatin and lovastatin

Question 31

How are statins metabolized?

Answer 31

most hepatic P450 enzymes

Question 32

What is the DOA for most statins?

Answer 32

24h

Question 33

What is the absolute contraindication for statins?

Answer 33

Pregancy

Question 34

What are the side effects of statins?

Answer 34

skeletal muscle issues (rhabdo rare), liver enzyme changes (plasma aminotransferase increases), drug interactions such as CYP 450 3A4 inhibitors, GI upset, fatigue, headache

Question 35

What is the MOA of Bile Acid Resins (anionic exchange)

Answer 35

increase hepatic bile synthesis from cholesterol stores, increasing LDL-R and the uptake of LDL from the blood

Question 36

What are the uses of bile acid resins?

Answer 36

primary increased LDL level with normal triglycerides

Question 37

What are some examples of bile acid resins?

Answer 37

colesevelam, cholestyramine, colestipol

Question 38

What is unique about administration of bile acid resins?

Answer 38

need to be hydrated with water, they are powders with no systemic absorption

Question 39

What's the side effects of bile acid resins?

Answer 39

constipation

Question 40

What's the MOA of niacin?

Answer 40

inhibits synthesis of VLDL in the liver, inhibits release of free fatty acid from adipose tissue, increases activity of lipoprotein lipase

Question 41

What are the uses of niacin?

Answer 41

lowers LDL and trigylderides, | MOST EFFECTIVE DRUG AT INCREASING HDL

Question 42

Does niacin undergo 1st pass metabolism?

Answer 42

yes, extensively

Question 43

What are side effects of niacin?

Answer 43

flushing, pruritis, GI upset, hepatic dysfunction, hypergycemia, gout, drug interactions, worsening hypotension. Massive histamine release.

Question 44

How should you take niacin?

Answer 44

start slow, NSAID/ASA 30 min before taking it, avoid alcohol

Question 45

What is the MOA of fibrates?

Answer 45

increased activity of lipoprotein lipase

Question 46

What's the use of fibrates?

Answer 46

MOST EFFECTIVE DRUGS AT DECREASING TRIGLYCERIDES (50%), increase LDL

Question 47

What are examples of fibrates?

Answer 47

Gemfibrozil, Fenofibrate, Bezafibrate

Question 48

What are the side effects of fibrates?

Answer 48

GI upset, headache, gallstones, statin interaction, prolonged PTT(coumadin protein binding)

Question 49

What's the MOA of Ezetimibe?

Answer 49

selective inhibitor of cholesterol absorption leading to secondary up-regulation of LDL-R

Question 50

What is the use of Zetia?

Answer 50

alone decreases LDL by 22%, potentiates the effects of statins by 17%

Question 51

What is the use of omega-3 fatty acids (fish oil)?

Answer 51

decrease triglycerides. not regulated by FDA, dose is unclear, long term safety not known, no evidence to support prevents heart disease.