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Flashcards in Atherosclerosis Pharm Deck (21)
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1

What is the dominant mechanism for controlling LDL plasma concentration?

regulation of hepatic LDL receptor pathway

2

What are the three HMG CoA reductase inhibitors?

Statins;
lovastatin
simvastatin
atorvastatin

3

What is the mechanism of action of statins?

structural similarity to HMG CoA substrate; reversible competitive inhibitor

4

How do statins increase LDL receptor gene expression?

in response to reduced free cholesterol content within hepatocytes; SREBPs are cleaved and the transcription factor then bind to sterol responsive element of LDL receptor gene

5

What are the minor adveerse effects of statins?

GI symptoms, diarrhea, constipation, excess flatus, abdominal pain/cramps and nausea

6

What are the major adverse effects of statins?

myopathy, rhabdomyalisis

7

What are the myopathy risk factors?

increased statin levels, increased age, hepatic, renal disease, hypothyroidism, or combination with drugs

8

Why are statins contraindicaated in younger women.

Pregnancy risk

9

What are the cinical use of statins?

first line therapy in pts who are at high risk for MI due to hypercholesterolemia; statins are effective in almost all pts with high LDL_C levels except for homozygous familial hypercholesterolemia

10

What is the mechanism of action of cholestyramine?

anion-exchange resins that increase bile acid excretion; highly charged + and binds bile acid; in most individuals synthesis is insufficient to make up for increased excretion

11

What are the adverse effects of cholestyramine?

poor pt compliance bc of consistancy
most elevation in TG
interfere with abosrbance of other drugs
GI issues

12

What is the mechanism of action of niacin?

not explained by a single mechansim; due to decreased cAMP levels, reducing VLDL production

13

What are the major adverse effects of niacin?

intesnse flush and pruritis, GI ffects
concurrent use of niacin and statins can cause myopathy

14

What are the clincial use of niacin?

hypertriglyceridemias adn elevated LDL-cholesterol
only ipid lowering drug that reduces Lp(a)

15

What is the mechanism of action of Ezetimibe?

inhibits cholesterol transfer from intestinal lumen into intestinal cell by binding to transporter called Niemann Pick Cl-like 1 protein within brush border membrane

16

What is the clinical use of Exetimibe?

monotherapy for treatment of primary hypercholesterolemia in pts that are resistant to statin therapy

17

What are the mechanism of action of PPAR activators?

Gemfibrozil and Fenofibrate; mediate action by interaction with proliferator activated receptros, bind to them and alter transcritption of genes

18

Proprotein convertase subtilisin/kexin 9 (PCSK9) inhibitors mechanism of action is what?

a mediator of hepatic LDL receptor degradation, is inhibited by this drug

19

What are the adverse effects of PCSK9 inhibitors?

generally well tolerated, hwoever still experimental; used to tx hypercholesterolemia

20

What is the mechanism of action of apolipoprotein B-100 inhbiition?

used to tx familial hypercholesteromeia homozygous by preventing formation of LDL or VLDL

21

What are the adverse effects of apolipoprotein B-100 inhibitors?

flu like symptoms
headache
increase liver fat
hepatotoxicity