Lecture 10.5 Anti-Hyperlipidemics

Question 1

what drug class causes the largest drop in TG's? 
what about LDL?
What drug class increases HDL the most?

Answer 1

fibrates;
statins;
niacin

Question 2

statins (competitively or non-competitively) inhibit ______. they also upregulate _____

Answer 2

competitively inhibit HMG CoA reductase;

LDL receptors = reduces plasma chol

Question 3

with low cholesterol, the SCAP/SREPB complex is (bound or unbound)? what does it do?

Answer 3

unbound; moves to golgi, binds DNA, increases LDL receptor expression

Question 4

statins are indicated in patients with high _____ or those that have had an _____

Answer 4

LDL, acute MI

reduce LDL by 20-60%

Question 5

short half-life statins should be taken in the _____.

Answer 5

evening (to inhibit nocturnal synthesis)

Question 6

simvastatin and lovastatin should be taken when?

what about rosuvastatin, atorvastatin, and pravastatin?

Answer 6

with a meal;

whenever

Question 7

which statin does not undergo hepatic metabolism ? (ie it undergoes sulfation)

Answer 7

pravastatin

Question 8

what is the most common side effect of statins? how do you follow this?

what is another important side effect?

Answer 8

rhadomyolysis/myopathy, follow with CPK;

hepatotoxicity (Follow LFTs)

Question 9

mechanism of action of bile acid resins:

Answer 9

prevent intestinal reabsorption of bile acids by forming insoluble complexes with them;
upregulate LDL receptors

Question 10

name 3 bile acid resins

Answer 10

cholestyamine, colestipol, colesevelam

Question 11

bile acid resins primary effect on lipoproteins:

Answer 11

decrease LDL (by 20%); slightly increase HDL

Question 12

side effects of bile acid resins (2)

Answer 12

GI upset, decreased absorption fat soluble vitamins/drugs ie statins

Question 13

what drug inhibits small intestinal absorption of cholesterol? what transporter is specifically inhibited?

Answer 13

ezetimibe;

NPC1L1

Question 14

ezetimibe primarily reduces ____;

Answer 14

LDL;

rarely causes liver/muscle damage

Question 15

juxtapid and mipomersen both inhibit _____ synthesis. what disease are they indicated for?

Answer 15

Apo B;

homozygous familial hypercholesterolemia

Question 16

alirocumab and evolocumab both inhibit ____.

Answer 16

PCSK9 protein

Question 17

what does PCSK9 usually do?

Answer 17

promotes degradation of LDL receptors

Question 18

fibrates activate ____ to upregulate ____ and induce ____ synthesis

Answer 18

PPAR alpha; Lipoprotein lipase, HDL

Question 19

hit me with 2 fibrates:

Answer 19

fenofibrate, gemfibrozil

others exist as well

Question 20

fibrates are especially indicated in patients with ____ in which VLDLs predominate

Answer 20

hyper-TG-emia

Question 21

2 side effects of fibrates

Answer 21

myopathy (watch with statins);
gall stones

also potentiate effects of warfarin

Question 22

what dietary supplement can reduce TG synthesis?

Answer 22

omega 3 FA (Fish oil/lovaza)

Question 23

niacin is thought to increase ____ activity and decrease _____ production. niacin ____ hormone synthesis lipase in adipose tissue

Answer 23

lipase (increases VLDL clearance);
VLDL (in liver);
inhibits

Question 24

in MQs, niacin increases expression of CD36 and ____, causing increased Reverse cholesterol transport

Answer 24

ABCA1

Question 25

most common side effect of niacin:

how to help treat this?

Answer 25

cutaneous vasodilation, warmth;
use NSAIDs (inhibits PG release)

Question 26

3 other side effects of niacin:

Answer 26

hyperglycemia, hyperuricemia, hepatotoxicity