Cholesterol drugs

Question 1

Effects of cholesterol

Answer 1

Causes atherosclerosis: LDL deposits=plaque
attract macrophages
activate inflammatory cytokines
Damage epithelium
NO/Prostacyclin inhibited

Question 2

What does High cholesterol eventually lead to

Answer 2

Angina
Stroke
MI

Question 3

Which is the enzyme that produces Cholesterol

Answer 3

HMG CoA reductase

Question 4

Which are the drugs that treat Dyslipidaemia

Answer 4

Statins
Fibrates
Cholestyramine
Ezetimibe
PCSK-9 inhibitors

Question 5

What is Cholestyramine

Answer 5

Is a intestinal binding resin

Question 6

MOA of Cholestyramine

Answer 6

large -ively charged molecule that binds to bile acid in the gut=formation of insoluble complex–> complex eliminated

Question 7

Effects of Cholestyramine

Answer 7

As bile+resin is eliminated, liver synthesizes new LDL Receptors to make new cholesterol

Question 8

TUs of Cholestyramine

Answer 8

Only used as add-on to Statins
For puritis from bile acid

Question 9

Can cholestyramine be used as monotherapy

Answer 9

nope, its not potent enough

Question 10

AEs of Cholestyramine

Answer 10

Insoluble–> poorly tolerated

Question 11

What are Statins

Answer 11

They are HMG Co-A reductase inhibitors

Question 12

Which are the Statins

Answer 12

Simvastatin
Pravastatin
Fluvastatin
Atorvastatin
Rosuvastatin

Question 13

MOA of Statins

Answer 13

Inhibit HMG Co-A reductase in liver
=increase synthesis of LDL-C receptors and serum cholesterol levels drop

Question 14

Effects of Simvastatin

Answer 14

Primarily lowers total cholesterol and LDL
Trigylcerols are also reduced but v.little
HDL remains unchanged

Question 15

Effects of Atorvastatin and Rosuvastatin

Answer 15

Reduce hepatic production of cholesterol, incr. LDL Receptor production.
Inhibition of LDL=incr. LDL Rs=reduced atherogenic LDL

Question 16

TUs of Statins

Answer 16

Most effective drugs in decr. LDL
Drop in LDL–> drop in CVD events such as STROKES, CAD, MI and MORTALITY

Question 17

AEs of Statins

Answer 17

Rhabdomyolisis: breakdown of skeletal m.
Myalgia
Liver problems: transient

Question 18

What is Ezetemibe

Answer 18

Is a GIT Cholesterol Blocker
–> blocks cholesterol uptake in gut

Question 19

MOA of Ezetemibe

Answer 19

blocks cholesterol uptake in gut–> new LDL Rs synthesized= LDL cholesterol levels drop

Question 20

Effect of Ezetemibe

Answer 20

Primarily lowers total cholesterol and LDL
No effect on HDL and trigycerols

Question 21

TUs of Ezetemibe

Answer 21

Used as add-on to statins to reduce LDL in Familial Hypercholesterolinaemia

Question 22

Which are the Fibrates

Answer 22

Bezafibrate
Gemfibrozil

Question 23

When are fibrates used

Answer 23

In mixed dyslipidaemia

Question 24

MOA of Fibrates

Answer 24

reduce VLDL synthesis and incr. HDL synthesis
Stimulates LPL act.–>incr. adipose tissue deposition of lipids= serum drop of Triglycerols

Question 25

Effects of Fibrates

Answer 25

Primarily reduce Triglycerols
HDL incr. by 10-15%
More effective than statins in incr. HDL
Little effect on LDL
Stimulate PPRA-gamma which is proliferative peroxisome agonist receptor gamma which should improve glucose utilisation

Question 26

TUs of Bezafibrate

Answer 26

Only used as add-on therapy or if there is very high trigs/very low HDL

Question 27

TUs of Gemfibrozil

Answer 27

Have no activity on LDL

Question 28

AEs of Fibrates

Answer 28

Rhabdomyolisis
Myalgia
Liver problems: transient
CNS problems

Question 29

DIs with Fibrates

Answer 29

Statins