Atherosclerosis Pharm

Question 1

What is the dominant mechanism for controlling LDL plasma concentration?

Answer 1

regulation of hepatic LDL receptor pathway

Question 2

What are the three HMG CoA reductase inhibitors?

Answer 2

Statins;
lovastatin
simvastatin
atorvastatin

Question 3

What is the mechanism of action of statins?

Answer 3

structural similarity to HMG CoA substrate; reversible competitive inhibitor

Question 4

How do statins increase LDL receptor gene expression?

Answer 4

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

Question 5

What are the minor adveerse effects of statins?

Answer 5

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

Question 6

What are the major adverse effects of statins?

Answer 6

myopathy, rhabdomyalisis

Question 7

What are the myopathy risk factors?

Answer 7

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

Question 8

Why are statins contraindicaated in younger women.

Answer 8

Pregnancy risk

Question 9

What are the cinical use of statins?

Answer 9

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

Question 10

What is the mechanism of action of cholestyramine?

Answer 10

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

Question 11

What are the adverse effects of cholestyramine?

Answer 11

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

Question 12

What is the mechanism of action of niacin?

Answer 12

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

Question 13

What are the major adverse effects of niacin?

Answer 13

intesnse flush and pruritis, GI ffects

concurrent use of niacin and statins can cause myopathy

Question 14

What are the clincial use of niacin?

Answer 14

hypertriglyceridemias adn elevated LDL-cholesterol

only ipid lowering drug that reduces Lp(a)

Question 15

What is the mechanism of action of Ezetimibe?

Answer 15

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

Question 16

What is the clinical use of Exetimibe?

Answer 16

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

Question 17

What are the mechanism of action of PPAR activators?

Answer 17

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

Question 18

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

Answer 18

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

Question 19

What are the adverse effects of PCSK9 inhibitors?

Answer 19

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

Question 20

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

Answer 20

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

Question 21

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

Answer 21

flu like symptoms
headache
increase liver fat
hepatotoxicity