Statins Flashcards
What are the 3 key features of statins?
Lactone ring - ionisable
Bicyclic framework - lipophilic
Ethylene bridge
How do synthetic statins differ from natural statins?
Open chain hydroxy acid instead of lactone ring
Linker can be alkene
Why is the length of the statins linker important?
Linker stereochemistry has an effect on biological activity
What has a large effect on the clearance and uptake of statins?
Lipophilicity
What increases the hepatic uptake of LDL?
Statins
Why are statins taken at night?
Cholesterol synthesis increases at night and statins have a short half life
What are the different statins?
Lipophilic and hydrophilic but no clinical rational to decide, except side effects
What do LDL do?
Make deposits on blood vessel walls which results in a build up of cholesterol plaque and blocks blood vessels
What do HDL do?
Collect cholesterol particles as they travel through blood vessels and deposit them in the liver where they are transferred to bile acids and disposed of
Why does LDL receptor activity diminish?
Due to diets that are high in cholesterol
What is HMG-CoA Reductase?
The enzyme that catalyses the conversion of HMG-CoA to mevanolate - rate determining step
