Lipid lowering drugs (3.2) Flashcards
How are lipids transported in the blood?
Lipoproein particles or bound to albumin
What is the role of Chylomicrons?
Carry dietary TAG from the intestines to the tissues
What is the role of VLDLs?
Carry TAG synthesised in the liver to adipose tissue
What is the role of LDLs?
Carry synthesised Cholesterol from the liver to the tissues
What is the role of HDLs?
Carry excess Cholesterol from the tissues to the Liver where it can be disposed of as bile salts
What maintains stability of lipoprotein molecules?
Lecithin Cholesterol Acyltransferase (LCAT)
- Converts surface lipid to core lipid
- If deficient will have deposition of lipids in many tissues*
Name the six main classes of lipid lowering drugs
Statins (Simvastatin) Ezetimibe Fibrates Cholesterol lipase inhibitors Nicotinic acid (Niacin) Plant steols
What is the mode of action of Statins?
Acts in the liver - Inhibits HMG CoA reductase which results in inhibition of Cholesterol synthesis
Increase LDL clearance
What are the main ADRs of Statins?
Myalgia - measure creatinine kinase levels to determine level of muscle breakdown
Headaches
What is the mode of action of Ezetimibe?
Selectively inhibits Cholesterol absorption in the brush border of the intestine.
Increases hepatic LDL receptor expression
What are the main ADRs of Ezetimibe?
Diarrhoea
Headache
Hypersensitivity reactions
Raised ALT/ASTs
What is the mode of action of Fibrates?
Increase production of lipoprotein lipase
Decrease TAG production
Increase FA uptake and oxidation
What are the main ADRs of Fibrates?
Diarrhoea
Gallstones (As increase Cholesterol content of bile)
Rhabdomyolosis (When combined with a Statin)
What is the mode of action of Nicotinic acid?
Increases HDL
Decreases VLDL
Decreases Lipoprotein synthesis
What are the main ADRs of Nicotinic acid?
Flushes Itching Headaches Hepatotoxicity Peptic ulcers Hyperglycaemia
