12 Questions
What is the main effect of MOA (various) on stored triglycerides in adipose tissue?
Decrease lipolysis
What is the major side effect of Niacin?
Flushing and GI distress
What is the impact of R1 in Fibric Acids derivatives on oral absorption?
It increases oral absorption
What is the chemical name of the active anionic form that gives Fibric Acids their name?
Fibrate
What is the enzyme targeted by statins to decrease cholesterol?
Hydroxymethyl glutaryl CoA reductase (HMGR)
What is the primary mechanism of action of fibrates like propyl group?
Enhancing lipoprotein lipase
What is the consequence of R2 being highly protein bound and displacing anticoagulants and sulfonylureas?
Risk of myopathy
What is the coenzyme required by HMGR for the conversion of HMG-CoA to Mevalonic acid?
NADPH
Which enzyme metabolizes fluvastatin?
CYP2C9
What inhibits CYP3A4, a key enzyme for metabolizing several statins?
Naringin in grapefruit juice
Which statin is resistant to CYP3A4 and is oxidized in the gut/liver?
Pravastatin
Why are lipophilic groups important for the transport of drug molecules into the liver?
They can be passively transported across barriers
This quiz covers the metabolism of statin pro-drugs, including the hydrolysis process by esterases and the role of CYP3A4 and 2C9 enzymes in metabolizing different statins. It also delves into the impact of grapefruit juice on CYP450 isoforms and the unique metabolism of pravastatin.
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