Lipid lowering agents

Question 1

What is a example of Proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitors?

Answer 1

Alirocumab, evolocumab

Question 2

Name the drugs that mainly target LDL & total cholesterol

Answer 2

statins
cholesterol absorption inhibitors
bile acid-binding (anion exchange) resins
PCSK9 inhibitors
bempedoic acid

Question 3

Name the drugs that mainly target triglycerides

Answer 3

fibrates

Ω-3 fatty acids / fish oils

Question 4

What drugs are used to reduce LDL?

Answer 4

statins

Question 5

What drugs are used to reduce triglycerides?

Answer 5

fibrates

Question 6

What are the drugs of choice in raising HDL?

Answer 6

niacin

Question 7

Name six examples of statins

Answer 7

lovastatin, pravastatin, simvastatin, fluvastatin, atorvastatin, rosuvastatin

Question 8

What are Anti-PCSK9 monoclonal antibodies

responsible for?

Answer 8

Inhibit action of liver-produced enzyme PCSK9, responsible for promoting metabolism and subsequent degradation of LDL-R on liver cells

Question 9

PCSK9 inhibitors _______ hepatic LDL-R expression and LDL clearance
______ HDL (modest)
______ LDL, VLDL & triglycerides

Answer 9

Increase

Raise HDL

Lower LDL

Question 10

What are statins main effect?

Answer 10

To block the rate-limiting step represented by the formation of mevalonate from HMG CoA in the liver.

Question 11

What are statins secondary effects?

Answer 11

Reduce hepatic cholesterol synthesis
Increase hepatic LDL-R expression, LDL clearance & reduce VLDL production
Raise HDL
Lower LDL, VLDL & triglycerides

Question 12

How do statins manage cardiovascular risk?

Answer 12

via LDL lowering but also possibly through pleiotropic effects such as anti-thrombotic and anti-inflammatory actions

Question 13

What are Bile acid-binding (anion exchange) resins secondary effects?

Answer 13

Increase bile acid synthesis-activation by activation of hepatic 7-α-hydroxylase, more cholesterol needed to replace lost bile acids, reduces hepatic store of cholesterol.

Increase hepatic LDL-R expression & LDL clearance

May raise HDL

Lower LDL

Question 14

Name three examples of Bile acid-binding (anion exchange) resins?

Answer 14

colestipol, cholestyramine, colesevelam

Question 15

What are Bile acid-binding (anion exchange) resins main effects?

Answer 15

Reduce bile acid reabsorption,
interrupts enterohepatic bile acid circulation,
reduces (bile acid) cholesterol reabsorption

Question 16

What are Bile acid-binding (anion exchange) resins secondary effects?

Answer 16

Increase bile acid synthesis-activation of hepatic 7-α-hydroxylase, more cholesterol needed for de novo bile acid synthesis reduces hepatic store of cholesterol.

Increase hepatic LDL-R expression & LDL clearance

May raise HDL

Lower LDL

Question 17

How is PCSK9 Administered?

Answer 17

Administered by subcutaneous injection

Question 18

Give three examples of Fibrates

Answer 18

Gemfibrozil, fenofibrate, bezafibrate, ciprofibrate, clofibrate

Question 19

Fibrates _____ lipoprotein lipase (LPL) activity & increase triglyceride clearance

Answer 19

Induce

Question 20

Fibrates ______hepatic FFA uptake Increase mitochondrial FFA oxidation (ß-oxidation)

Answer 20

Increase

Question 21

Fibrates ________ hepatic VLDL & triglyceride production

Raise HDL

_______ VLDL, LDL & triglycerides.

Answer 21

Reduce

Lower

Question 22

Which drugs do Bile acid-binding (anion exchange) resins reduce the absorption of?

Answer 22

digoxin, warfarin, thyroxine, cholorothiazide

Question 23

What are Bile acid-binding (anion exchange) resins side effects?

Answer 23

reduced absorption of fat soluble vitamins (A, D, E, K),

susceptibility to bleeding (reduced vitamin K),

bloating, dyspepsia, flatulence

Question 24

Which drug is an example of cholesterol absorption inhibitors?

Answer 24

ezetimibe

Question 25

What are cholesterol absorption inhibitors main effects?

Answer 25

prevents the absorption of both dietary and bile (free) cholesterol; but does not affect the absorption of e.g. dietary TG, fat soluble vitamins or bile acids.

Question 26

What are cholesterol absorption inhibitors secondary effects?

Answer 26

Inhibit cholesterol uptake receptor
Reduce hepatic VLDL production
Increase hepatic LDL-R expression & LDL clearance
Reduce LDL

Question 27

What are ezetimibe side effects?

Answer 27

myopathy, rhabdomyolysis, dyspepsia, diarrhoea, abdominal pain, arthralgia, myalgia, headache, elevated liver function tests, angioedaema

Question 28

Fibrates can displace ____

Answer 28

Wafarin

Question 29

Give an example of Ω-3 fatty acids (fish oils)

Answer 29

eicosapentaenoic acid (EPA), docosahexaenoic acid (DHA)

Question 30

Ω-3 fatty acids are responsible for?

Answer 30

Regulate nuclear transcription factors

eg. PPARα & SREBP-1c

Question 31

Ω-3 fatty acids ______ triglyceride biosynthesis & _______ fatty acid oxidation in liver

Answer 31

Reduce triglyceride

increase fatty acid

Question 32

Ω-3 fatty acids _____ VLDL & triglycerides

_____ HDL

Answer 32

Reduce VLDL

Raise HDL

Question 33

Niacin (nicotinic acid/vitamin B3) are responsible for?

Answer 33

Inhibits hormone-sensitive lipase

reduces FFA release from adipose (lipolysis)

Question 34

Naicin ____ hepatic VLDL production & triglyceride synthesis

______ hepatic HDL uptake

Answer 34

Lowers Hepatic VLDL

Reduces hepatic HDL