CVD WK9 Lowering lipid agent
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40 Terms
What is the target of statins?
HMG-CoA reductase
What is the rate-limiting enzyme in cholesterol synthesis?
HMG-CoA reductase
What is the mechanism of statins?
Competitive and reversible inhibition of HMG-CoA reductase → ↓ cholesterol synthesis → ↑ LDL receptors → ↓ LDL
What is the effect of statins on LDL receptors?
Increase them
What is the effect of statins on LDL?
Decreases LDL
What is the effect of statins on triglycerides?
Small decrease
What is the effect of statins on HDL?
Small increase
What are examples of statins?
Atorvastatin, Rosuvastatin, Simvastatin, Fluvastatin, Pravastatin
Which statins are long-lasting?
Atorvastatin and Rosuvastatin
Which statins are fast-acting?
Simvastatin and Pravastatin
Which statin is a prodrug?
Simvastatin (metabolised in liver to active form)
How are statins metabolised?
CYP450 and glucuronidation
What is the effect of statins on CV events?
Reduce CV events and mortality
What are fibrates?
Derivatives of fibric acid, structurally related to thiazolidinediones
What are examples of fibrates?
Bezafibrate, Ciprofibrate, Gemfibrozil, Fenofibrate
What is the target of fibrates?
PPARα
What is the main effect of fibrates?
↓ Triglycerides
What is the effect of fibrates on HDL?
Increases HDL
What is the clinical use of fibrates?
Hypertriglyceridaemia (TG >10 mmol/L) or when statins are contraindicated
What is ezetimibe?
A drug that inhibits cholesterol absorption
What is the target of ezetimibe?
NPC1L1 in the brush border of enterocytes
How much does ezetimibe lower LDL?
17%
What is ezetimibe metabolised to?
Ezetimibe glucuronide (also active)
What is the mechanism of ezetimibe?
Blocks NPC1L1 → ↓ cholesterol absorption → ↓ LDL
What is nicotinic acid/niacin?
An old lipid-lowering drug that lowers LDL, TG, and increases HDL
Why is niacin no longer recommended?
Vasodilatory side effects (flushing)
What is the function of PCSK9?
Binds to hepatic LDL receptors and promotes their lysosomal degradation
What is the effect of PCSK9 on LDL?
Increases LDL (by destroying LDL receptors)
What is the mechanism of PCSK9 inhibitors?
Block PCSK9 → ↑ LDL receptors → ↓ LDL
What type of drugs are PCSK9 inhibitors?
Monoclonal antibodies
How are PCSK9 inhibitors given?
Subcutaneous injection
What is inclisiran?
A small interfering RNA (siRNA) that inhibits PCSK9 translation
What is the mechanism of inclisiran?
Gene silencing - inhibits translation of PCSK9 mRNA → ↓ PCSK9 → ↑ LDL receptors → ↓ LDL
How often is inclisiran given?
Twice-yearly (subcutaneous injection)
What is bile acid binding resins?
Old lipid-lowering drugs that bind bile acids
Why are bile acid resins no longer recommended?
Can aggravate hypertriglyceridaemia
What are plant stanols and sterols?
Supplements and functional foods that lower LDL modestly
What is the difference between statins and fibrates?
Statins = ↓ LDL (main). Fibrates = ↓ TG (main)
What is the role of NPC1L1?
Mediates cholesterol absorption in the intestine
What is the effect of PCSK9 inhibitors on LDL receptors?
Increase LDL receptors