lipid lowering drugs Flashcards
LDL cholesterol
- transports from the liver to peripheral tissue
- adverse effects
HDL cholesterol
- transports from peripheries back to the liver
- beneficial effects
Triglycerides
- adverse vascular effects
- transported by VLDLs
lipid lowering therapy
- drugs
- lifestyle e.g. diet, exercise, weight
who should be treated with lipid-lowering therapy?
secondary prevention
- angina, MI - Cerebrovascular accident (CVA) - Peripheral vascular disease (PVD)
diabetics
primary prevention
-CVS risk >305 over 10years
targets for lipid-lowering therapy
LDL <1.8mmol/L
name 2 statins
- simvastatin
- atorvastatin
describe the mechanism of statins
- competitive inhibition of HMG-CoA reductase -> blocks cholesterol synthesis
- in response to blocked synthesis hepatocytes up-regulate LDL-R –> takes up circulating LDL
- statins also block the production of isoprenoids (involved in inflammation, cell signalling, apoptosis)
interactions of statins
- simvastatin metabolized by CYP3A4
- inhibitors of CYP3A4 = amiodarone, diltiazem, verapamil, erythromycin
side effects of statins
- myopathy
- myalgia (muscle pain)
- myositis (muscle inflammation & breakdown)
- rhabdomyolysis
- abnormal LFTs
- teratogenic
- potential predisposition to diabetes
what is an example of a fibrate and what is its effect
bezafibrate
- decrease in triglycerides (30-50%)
- slight decrease in LDL and slight increase in HDL
indications for fibrates
isolated hypertriglyceridaemia
- tx first by diet, exercise, weight loss, reduce alcohol etc
combine therapy w/ statin in resistant high cholesterol
mechanism of fibrates
- stimulate PPAR agonist –> produces proteins that:
- decrease VLDL production
- increase FA storage by SM
- activates lipoprotein lipase (breaks down TGs)
side effects of fibrates
- GI upset
- abnormal LFTs
- myositis
