Dyslipidemia Drugs: Cholestyramine and ezetimibe

Question 1

What is the site of cholesterol and bile acid absorption

Answer 1

Lumen of small intestine

Question 2

Bile acids are derived from

Answer 2

cholesterol

Question 3

Bile acids are released into the

Answer 3

intestinal lumen

Question 4

The liver metabolized cholesterol into

Answer 4

bile acids (conjugated to become water soluble)

Question 5

Bile acids (derived from cholesterol) are

Answer 5

secreted from the liver into the biliary tract

Question 6

Normally ____% of bile acids in the ileum are recycled back to the liver through

Answer 6

95%

Question 7

Normally 95% of bile acids in the ileum are recycled back to the liver through

Answer 7

enterohepatic circulation

Question 8

Normally 95% of bile acids in the ileum are

Answer 8

recycled back to the liver through enterohepatic circulation

Question 9

Bile acid resins prevent

Answer 9

recycling of bile acids to the liver

Question 10

Bile acid binding resins include

Answer 10

1. Cholestyramine
2. Colestipol
3. Colesevelam

Question 11

Resins

Answer 11

interrupt bile acid recycling and promote synthesis of new bile acids, depleting liver cholesterol stores

Question 12

Resins interrupt bile acid recycling, causing

Answer 12

1. HMG CoA reductase to synthesize more cholesterol

2. Upregulation of LDL receptors and uptake of circulating LDL

Question 13

Triglycerides are carried on

Answer 13

VLDLs

Question 14

VLDLs exit the

Answer 14

liver

Question 15

Bile acid resins side effects

Answer 15

1. Hypertriglyceridemia (increased VLDLs)
2. Cholesterol gallstones
3. Constipation
4. Bloating
5. Impaired absorption of fat-soluble vitamins A, D, E and K
6. Decreased statin absorption

Question 16

Statins and Bile acid Resins must be given

Answer 16

4 hours apart

Question 17

Ezetimibe

Answer 17

1. Blocks intestinal absorption of cholesterol

2. Restricts liver’s access to exogenous cholesterol

Question 18

Ezetimibe blocks intestinal cholesterol absorption, causing

Answer 18

1. HMG CoA reductase to synthesize more cholesterol

2. Upregulation of LDL receptors and uptake of circulating LDL

Question 19

Ezetimibe side effects

Answer 19

1. Diarrhea
2. Steatorrhea
3. Increased liver function tests (LFTs)

Question 20

Evolocamab is a

Answer 20

PCSK9 inhibitor

Question 21

PCSK9 normally causes

Answer 21

degradation of LDL receptors

Question 22

many PCSK9 inhibitors (evolocumab) are

Answer 22

antibodies

Question 23

Evolucamab binds PCKS9 and

Answer 23

evolucamab binds PCKS9 and prevents degradation of LDL receptors, increasing uptake of circulating LDL