lipid lowering drugs Flashcards
What is HMG-CoA reductase?
rate-limiting step in cholesterol synthesis
found in endoplasmic reticulum cells especially in the liver
Name 3 HMG-CoA reductase inhibitors
ALL THE STATINS
1. atorvastatin
2. pravastatin
3. simvastatin
HMG-CoA reductase inhibitors MOA
- inhibit HMG-CoA reductase, inhibit biosynthesis of cholesterol
- upregulates LDL receptors on cell surface: depletion of intracellular cholesterol causes cell to increase LDLr to bind and internalise LDL-Cs
HMG-CoA reductase inhibitor clinical use
- lower plasma cholesterol LDL-C in ALL types of hyperlipidaemia
- reduce risk of coronary events and mortality
HMG CoA reductase inhibitor adverse effects
- liver dysfunction
- myopathy and rhabdomyolysis
- contraindicated in pregnant women, children or teenagers
Name 2 PCSK9 inhibitor
- evolocumab
- alirocumab
MONOCLONAL AB
PCSK9 inhibitor MOA
- inhibition of hepatic proprotein convertase subtilisin-kexin (PCSK9) which targets LDL receptors for degradation in lysosomes
- decrease LDLr degradation, increase in LDL receptors on cell surface that can bind and internalise circulation LDL-C
PCSK9 inhibitors clinical uses
- used for intolerance to statins (HMG CoA reductase inhibitors)
- indication for lowering plasma LDL-C levels
- used for familial hypercholesterolaemias
- used on top of statins and diet control for patients with significant atherosclerotic CVD
PCSK9 inhibitors adverse effects
- hypersensitivity
- inflammatory reactions at site of injection
- increased incidence of nasopharyngitis and sinusitis
Name 2 fibrates derivatives
- gemfibrozil
- fenofibrate
fibrates derivatives MOA
- fibrates derivatives are ligands for PPAR-alpha protein
- binding results in increased activity of lipoprotein lipase
- decrease in plasma triacylglycerol levels
- decreased secretion by liver
- levels of VLDL decrease
HDL levels rise moderately
fibrates derivatives clinical uses
treatment of hypertriacylglycerol with VLDL elevation
especially for dysbetalipoproteinemia
fibrates derivatives adverse effect
- GI disturbance
- skin rashes
- gall stones
- myositis (inflammation of the muscle)
What are omega-3 acid ethyl esters?
omacor
- eicosapentaenoic acid (EPA) + docosahexaenoic acid (DHA) ethyl esters
people eat it from fish oil supplements too
omega-3 acid ethyl esters clinical uses
- hypertriglyceridemia type 4
- familial combined hyperlipidemia in combination with statins
- NOT indicated for hyperchylamicronaemia