Lipid drug pharmacology

Question 1

Statin MOA

Answer 1

HMG CoA reductase inhibitor

Reduce cholesterol synthesis
Increase hepatic cholesterol uptake
Reduce LDL, modest TAG, increase HDL

SE: myositis, deranged LFTs

Question 2

Ezetimibe MOA

Answer 2

Decreased cholesterol absorption in small intestine
-blocks the critical mediator of cholesterol absorption, the Niemann-Pick C1-like 1 (NPC1L1) protein on the gastrointestinal tract epithelial cells as well as in hepatocytes

This means LDL receptors upregulated so taken up from blood so less atherogenic.

SE: headache

Question 3

Nicotinic acid MOA

Answer 3

Probably reduce fatty acid releast from peripheral adipose tissue.

Reduce LDL and TAG
Increase HDL
Lower potentially atherogenic lipoprotein

Decrease hepatic VLDL secretion
Decrease TAG synthesis overall by reducing fatty acid synthesis

Also reduce HDL catabolism so more garbage collectors working

AKA vitamin B3

SE: flushing, myositis

Question 4

Fibrates

Answer 4

Agonist of PPAR-alpha–>increase lipoprotein lipase expression (increase VLDL to IDL)

SE: myositis, pruritis, cholestasis

Reduce TAG
Modest increase HDL
Variable LDL

Question 5

Cholestyramine

Answer 5

Decreases bile acid reabsorption in the small intestine, upregulating the amount of cholesterol that is converted to bile acid

SE: GI

Question 6

Au targets for lipids?

Answer 6

LDL under 1.8
HDL over 1
Triglycerides under 2
NonHDL under 2.5

Question 7

When should you start assessing someone with Framingham risk assessment for CV risk?

Answer 7

Caucasian over age 45 or A/TSI over 35 and none of the high risk features which automatically shuttle the person to a high risk group 
-Diabetic over 60
-Microalbumin
-180/110 higher than
-CKD with GFR under 45
Chol over 7.5
-Familial hypercholesterolaemia
-Or A/TSI over age 74
-->this means already have over 15% risk CVD within next 5 years

If then calculated to be moderate risk (10-15% CVD over 5 years)- review in 6-12 months
Low risk calculate every 2 years

Question 8

What are you allowed to combine with a statin?

Answer 8

Ezetimibe -safe- this reduces LDLs
Fenofibrate better than gemfibrozil with statin as reduces risk of myopathy
Bile acid binding resin
Nicotinic acid