Cholesterol Pharmacology Flashcards Preview

Pharmacology > Cholesterol Pharmacology > Flashcards

Flashcards in Cholesterol Pharmacology Deck (27):
1

Why is cholesterol management important

Cholesterol and LDL levels are major risk factors for CVD

2

What are indications for cholesterol pharmacological therapy

Primary prevention
Secondary prevention
Of cardiovascular disease

3

Who require statin therapy for primary prevention

10yr CV risk >10% on QRISK2 assessment
CKD with eGFR <60
T1DM with: >40yo, >10yrs diabetic, established nephropathy, other CVD risk factors

4

What treatment is given for primary prevention

Artorvastatin 20mg

5

How do you screen for hyperlipidaemia

Full lipid profile:
Total cholesterol
HDL
Non-HDL cholesterol
TAG

6

Who require treatment for secondary prevention

Anyone with established CVD:
IHD
Stroke
Peripheral arterial dienes

7

What treatment is given for secondary prevention

80mg artorvastatin

8

What is mechanism of action of statins

Inhibit HMG-CoA reductase
Inhibit cholesterol synthesis at hepatocytes
Reduce LDL synthesis
Increase LDL uptake (low cholesterol in hepatocytes causes increased LDLR expression)

Thus lower serum cholesterol

9

What are secondary benefits of statins

Anti inflammatory
Reduce plaque formation
Improve endothelial function

10

What are side effects of statins

GI disturbance
Myopathy: Muscle aches, myositis, rhabdomyolysis, raised CK
Liver impairment: raised transaminases

11

What are PK properties of statins

30-80% absorption
5-30% systemic availability
CYP450 metabolism (some types)
Taken at night: time of cholesterol synthesis

12

What monitoring is required for statins

LFTs
Baseline, 3 monthly, 12 monthly

13

What is mechanism of action of fibrates

PPAR alpha agonist
Stimulate lipoprotein lipase
Significant Decrease in TAG levels
Mild decrease in LDL
Mild increase in HDL

14

Give examples of fibrates

Bezafibrate

15

What are indications of fibrates

Mixed hyperlipidaemia:
Hyperlipidaemia with low HDL
Hypertriglyceridaemia

Combination with statins

16

What caution is required when given in combination with statins

Increased risk of myopathy, rhabdomyolysis

17

What are side effects of Fibrates

GI disturbance
Myopathy
Liver impairment - raised transaminases
Cholelithiasis

18

What are contra indications of fibrates

Liver impairment
Renal impairment
Pre existing gall bladder disease

19

What is mechanism of action of Ezetimibe

Inhibit cholesterol receptors in enterocytes
Selective inhibition of cholesterol absorption
Reduced intestinal delivery to hepatocytes
Increased LDL R expression by hepatocytes

20

What are indications of Ezetimibe

Monotherapy:
statin therapy contraindicated or not tolerated

Combination:
Failed to achieve adequate reduction on statins

21

What are side effects of Ezetimibe

GI disturbance headache

22

Give examples of nicotinic acid

Niacin

23

What is mechanism of action of niacin

Inhibit VLDL release from hepatocytes
Reduced LDL
Increased HDL

24

What are indications of niacin

Best agent to raise HDL

25

What are side effects of niacin

Flushing, itching
Hepatotoxicity
Activation of peptic ulcer

26

Give examples of PCSK9 Inhibitors

Alirocumab

27

What is mechanism of action of PCSK9 Inhibitors

Inhibit PCSK9 activity
PCSK9 normally binds to LDL-LDLR complex and promotes destruction than recycling
Thus increase LDLR recycling
Increased LDL uptake by hepatocytes