Hyperlipidaemia Flashcards
Statin MoA
Inhibits HMG CoA reductase
Pro drug
extensive first pass metabolism
Statin additional effects
Upregulates LDL receptors stabilies atherosclerotic plaque antioxidant increase NO anti-inflammatory
Statin ADR
GI disruption
Rhabdomyolysis
Myalgia
Statin warning
Pregnancy
Breast feeding
Hepatic impairment
Statin drug reactions- CYP
CYP34A- grapefruit juice, macrolides, amlodipine, diltiazem
Inhibitors increase [statin]
Statin drug example
Atorvastatin- 20mg primary prevention, 80 mg secondary prevention
Simvastatin
Why is simvastatin taken at night?
Due to circadian rhythm of LDL receptor
Fibric acid derivatives MoA
Activate PPAR alpha (nuclear transcription factor)- increases production of lipoprotein lipase
Fibric acid derivatives additional effects
increase HDL
increase LDL affinity for receptor
Fibric acid derivatives ADR
Gallstones (choleithiasis) - prevent metabolism of cholesterol into metabolites for bile = cholesterol stones
GI upset
Fibric acid derivatives drug & use
Fenofibrate
Co-prescribed with statins
Cholesterol absorption inhibitor MoA
e.g. Ezetimibe
Inhibits NPC1L1 on brushborder of small intestine
decrease GIT cholesterol absroption by 50%
Cholesterol absorption inhibitor additional effects
e.g. Ezetimibe
Increase hepatic LDL receptor expression
Cholesterol absorption inhibitor e.g. Ezetimibe important DDI
Increase risk of rhabdomyolysis if prescribed with statin
Ezetimibe use
2nd line
Secondary prevention CVD in patients that cant tolerate statins
