Lipid Lowering Agents Flashcards Preview

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Flashcards in Lipid Lowering Agents Deck (20):
1

What lipoprotein is major carrier of triglycerides?

VLDL

2

What lipoprotein is major carrier of cholesterol and the major form of cholesterol transport in humans?

LDL

3

True or False: the greater the number of CV RFs a pt has, the lower target value we set for cholesterol.

True

4

What is target for total cholesterol?

<5.2 mmol/L

5

What are different types of hyperlipoproteinemias?

Type IIa
- inc LDL
- normal triglycerides
- inc cholesterol

Type IIB:
- inc LDL & VLDL
- inc TGs
- inc TGs

6

What is the cumulative estimate of % drop in LDL that can be attained with therapeutic lifestyle changes?

20-30% drop in LDL

7

What are statins used to treat? What is their mechanism of action ?

Rx: high LDL cholesterol

HMG-CoA reductase inhibitors (inhibits early step in cholesterol synthesis)
Dec hepatocyte store of cholesterol.
Because liver is not depleted of cholesterol, it makes LDL-Rs which accelerates LDL clearance from blood through receptor-mediated endocytosis.

Can dec plasma LDL 30-50%. Help prevent MI and stroke.

8

What is the most potent and effective drug class for reducing LDL levels?

Statins

9

What are pleiotropic cardioprotective effects of statins?

dec coagulation/platelet activation
inc endothelial fcn and NO activity
dec inflammation

10

What are s/e of statins?

inc serum aminotransferase activity - concern for pts with liver disease
inc sCr
severe myopathy (rhabdo)
drug-drug interactions b/c met by CYP 3A4
coadmin drugs may inc/dec plasma levels

11

What is the MoA of niacin?

inhibits lipolysis in adipose tissue (blocks breakdown of Tgs into FFAs)
dec sFAs and uptake by liver
dec hepatic TG synthesis
dec hepatic VLDL synthesis & secretion
dec serum LDL (the catabolism of VLDL in the circulation leads to inc LDL so if you dec VLDL you also dec LDL)
inc VLDL via lipoprotein lipase mediated mechanism
inc HDL moderately

NOT dependent on LDL-R function

12

What are the side effects of niacin?

subQ vasodilation and sensation of warmth; flushing
nausea, GIT irritation
inc serum aminotransferase activity - concern: pts with liver disease

13

What is the MoA of bile-acid binding (cation exchange) resins?

facilitate conversion of cholesterol to bile salts and facilitate excretion of bile in feces
dec cholesterol
inc LDL-Rs
inc LDL clearance
dec plasma LDL

14

What are s/e of bile-acid exchange resins?

constipation/bloating/diarrhea
dec absorption of dietary vitamins (eg vitamin K) - attn: INR in pts on anticoagulants
may impair absorption of other drugs

15

What is the MoA of sterol absorption inhibitors?

inhibit cholesterol and sterol absorption from small intestine
dec hepatic cholesterol
inc LDL-R expression
dec serum LDL
minor beneficial effects on HDL and TGs

16

What are s/e of sterol absorption inhibitors?

reversible impaired liver function (rare)
myositis (rare)

17

What is the only lipid reducing agent that does not depend on LDL-R function?

niacin

18

What is the MoA of fibrates? What are they used to treat?

Rx: inc VLDLs, inc TGs and/or dec HDL
1 - inc lipoprotein lipase to inc clearance of TGs and VLDL
2 - inc hepatic fatty acid oxidation
3 - inc serum HDL by inc VLDL catabolism

19

What are s/e of fibrates?

rash
GIT irritation
gallstones
inc risk of myopathy when given with statins

20

Homozygotes for familial hypercholesterolemia lack what? WHat is Rx?

LDL-R function
Rx: LDL aperesis, Lomitapide (MTTP), Mipomersen (apoB)

Lomitapide & Mipomersen affect VLDL secretion