Lipid drugs

Question 1

describe the growth of plaque in arteries

Answer 1

cholesterol infiltrates artery wall > plaque forms > plaque grows > plaque grows to block artery or ruptures and blood clots form

Question 2

what is bad cholesterol

Answer 2

LDL= stored in blood stream

Question 3

what contributes to plaque build up

Answer 3

LDL and triglycerides

Question 4

what is good cholesterol

Answer 4

HDL

Question 5

what does HDL do

Answer 5

regulates LDL storage and promotes secretion

Question 6

what are the 3 mechanical means of clearing plaque buildup

Answer 6

balloon angioplasty, stents, high pressure jetting

Question 7

what are the 5 drugs to treat Dyslipidemia

Answer 7

fibrates
nicotinic acid
bile acid sequestrates
inhibitors of HMG CoA reductase
cholesterol absorption inhibitors

Question 8

What do fibric acid derivatives do (fibrates)

Answer 8

Fibrates= INC peripheral lipolysis and DEC hepatic triglyceride
DEC Trigylceride levels!!

Question 9

What are fibrates agonists of and what does this lead to

Answer 9

Fibrates = agonists of PPAR alpha - interaction leads to lipid metabolism and atherosclerosis

Question 10

What is the concern of long term fibrate use?

Answer 10

concern about an INC in non cardiac mortality in patients on long term fibrate use

Question 11

name the side effects of antilipemics (fibrates)

Answer 11

abdominal discomfort, diarrhea, nausea, blurred vision, INC risk of gallstones, prolonged prothrombin time, INC liver function

Question 12

What are suitable as vitamin B3

Answer 12

niacin and niacinamide

Question 13

what is the only vitamin B3 suitable for treating dyslipidemia

Answer 13

NIACIN!

Question 14

Does the Vitamin B3 activity of niacin affect its activity in lipid control

Answer 14

NO!! must use high high doses

Question 15

What are the 2 actions of nicotinic acid

Answer 15

1. agonist of GPR 109A and 109B receptors

2. inhibitor of diacylglycerol acetyltranferase

Question 16

describe the pathway of Nicotinic acid MoA

Answer 16

acts on GI inhibiting cAMP > inhibit PKA > inhibit HSL > INC good cholesterol

Question 17

Side effects of Niacin (nicotinic acid)

Answer 17

flushing (due to histamine release), itching, GI distress

Question 18

What are cholestyramine and colesevelam

Answer 18

bile acid sequestrants

Question 19

how do bile acid sequestrates work

Answer 19

keep bile acids from getting absorbed as they pass through intestine thus DEC secretion of bile salts to hepatocytes

Question 20

what stimulates hepotcytes to secrete more bile salts

Answer 20

95% of the bile salts reabsorbed into intestinal capillaries via enterohepatic circulation

Question 21

What happens in the liver to cholesterol

Answer 21

cholesterol is converted to bile acid which is excreted to the intestine through the action of C7H

Question 22

by preventing bile acid resorption what doe bile acid sequestrates do

Answer 22

INC cholesterol metabolism to bile acid

Question 23

What do bile acid sequestrates do to LDL? to HDL? Triglycerides (TG)?

Answer 23

Bile Acid Sequestrates
reduced LDL by 5-30%
INC HDL by 3-5%
INC trigylcerides

Question 24

side effects of bile acid sequestrates

Answer 24

GI distress and constipation

DEC absorption of other drugs

Question 25

Contraindications of bile acid sequestrates

Answer 25

PTS with dysbetalipoproteinemia | PTS with HIGH triglyceride levels (HIGHer than 400 mg/dl)

Question 26

what do inhibitors of HMG CoA reductase (statins) do

Answer 26

block HMG CoA thus preventing cholesterol synthesis and lowering levels of LDL

Question 27

What 2 drugs to lower cholesterol have the most side effects

Answer 27

FIbrates and Statins

Question 28

what 2 drugs to lower cholesterol have the least side effects

Answer 28

Cholesterol absorption inhibitors and bile acid sequestrates

Question 29

What is the current opinion on statins and longevity of life

Answer 29

Statins are helpful for people at risk of having a heart attack

Question 30

What do cholesterol absorption inhibitors do?

Answer 30

inhibit LDL formation by inhibiting absorption of dietary cholesterol and reabsorption of billiard cholesterol

Question 31

what is NPC1L1? what blocks NPC1L1?

Answer 31

NPC1L1: a transport protein moving cholesterol from lumen into enterocyte and back into blood NPC1L1 is blocked by Ezetimibe

Question 32

Describe the MoA of Ezetimibe

Answer 32

Ezetimibe selectively inhibits intestinal cholesterol absorption by DEC intestinal delivery of cholesterol to liver and INC expression of hepatic LDL receptors

Question 33

What do Ezetimibe and its active gluconoride do?

Answer 33

both metabolite circulate enterohepatically delivering agent back to site of acton and limiting systemic exposure

Question 34

what does ezetimibe do to LDL

Answer 34

lowers LDL by 18-20% and can be used as "add- on" to statins | DOES NOT change TG and HDL

Question 35

What are adverse effects of Ezetimibe (cholesterol absorption inhibitors)?

Answer 35

Main: abdominal pain and diarrhea Minor: headache, dizziness, fatigue, URI, back pain, muscle aches, and pain