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Statin Metabolism: Pro-drugs and Enzyme Metabolization

12 Questions

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Statin Metabolism: Pro-drugs and Enzyme Metabolization

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Questions and Answers

What is the main effect of MOA (various) on stored triglycerides in adipose tissue?

Convert lipids into glucose

No effect on lipolysis

Increase lipolysis

Decrease lipolysis (correct)

What is the major side effect of Niacin?

Flushing and GI distress (correct)

Nausea

Headache

Dizziness

What is the impact of R1 in Fibric Acids derivatives on oral absorption?

It helps in metabolism of drugs

It has no effect on oral absorption

It increases oral absorption (correct)

It decreases oral absorption

What is the chemical name of the active anionic form that gives Fibric Acids their name?

Fibrate Signup and view all the answers

What is the enzyme targeted by statins to decrease cholesterol?

Hydroxymethyl glutaryl CoA reductase (HMGR) Signup and view all the answers

What is the primary mechanism of action of fibrates like propyl group?

Enhancing lipoprotein lipase Signup and view all the answers

What is the consequence of R2 being highly protein bound and displacing anticoagulants and sulfonylureas?

Risk of myopathy Signup and view all the answers

What is the coenzyme required by HMGR for the conversion of HMG-CoA to Mevalonic acid?

NADPH Signup and view all the answers

Which enzyme metabolizes fluvastatin?

CYP2C9 Signup and view all the answers

What inhibits CYP3A4, a key enzyme for metabolizing several statins?

Naringin in grapefruit juice Signup and view all the answers

Which statin is resistant to CYP3A4 and is oxidized in the gut/liver?

Pravastatin Signup and view all the answers

Why are lipophilic groups important for the transport of drug molecules into the liver?

They can be passively transported across barriers Signup and view all the answers