Anti-Lipid Drugs Flashcards
role of HMG CoA reductase inhibitors
- block the synthesis of cholesterol - increase the uptake of LDL
pharmacokinetics issues with BABAs
- daily doses are in grams (huge) - alternate to statins during pregnancy - can be used with statins
HMG CoA reductase inhibitors role with nitric oxide
- increase endothelial nitric oxide production - vasorelaxation
common, but not serious toxicities with niacin
- flushing - pruritus
MOA of fibric acid derivatives
- increase LDL receptor expression - activates LPL - increase free fatty acid metabolism
what is the significance of some statins being taken at night?
- they have a short half life - want to reach peak effect during cholesterol synthesis peak
gemfibrozil used for
- anti-cholesterol
HMG CoA reductase inhibitors and platelets
- reduce platelet activation - reduce risk of venous thromboembolism
role of NPC1
- cholesterol transport protein
MOA of niacin
- inhibits synthesis of triglycerides in the liver
when does liver cholesterol synthesis peak?
- between midnight at 2 AM
HMG CoA reductase inhibitors and plaques
- stabilize arterial plaques - reduce risk of thrombus
cholesterol absorption inhibitors drug to know
- Ezetimibe
role of PCSK9
- induces LDL-receptor degradation - LDL-receptor bound to PCSK9 is digested in lysosome
serious, not common toxicities of niacin
- hepatotoxicity - insulin resistance
proteins in LDL
- ApoB
HMG CoA reductase inhibitors drug examples
- Atorvastatin - Rosuvastatin - Simvastatin - Pravastatin - Lovastatin
what happens if you inhibits absorption of cholesterol with ezetimibe what happens if you inhibit cholesterol synthesis with statins what do you do?
- you increase cholesterol synthesis so maybe more can be absorbed - you increase cholesterol absorption COMBINE THEM BOTH
BABA example
- colestipol
role of LPL
- breaks down triglycerides
MOA of toxicities of fibric acid derivatives with oral anticoagulants
- kick warfarin off albumin - free serum warfarin - increased bleeding risk
result of class 3 niacin
- decrease LDL - decrease triglycerides - increase HDL
results of class 2 BABAs
- decrease LDL a bit
important drugs that inhibit CYP3A4
- gemfibrozil - amlodipine - warfarin
which statins are the most potent?
- atorvastatin - Rosuvastatin
warfarin used for
- anti-coagulant
HDL composed of
- more protein - less cholesterol/triglycerides
PCSK9 drug
- Alirocumab
MOA of toxicities of fibric acid derivatives with statins
- inhibit statin absorption in liver - increased serum statin leads to myopathy