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?

<p>Fibrate (B)</p> Signup and view all the answers

What is the enzyme targeted by statins to decrease cholesterol?

<p>Hydroxymethyl glutaryl CoA reductase (HMGR) (B)</p> Signup and view all the answers

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

<p>Enhancing lipoprotein lipase (D)</p> Signup and view all the answers

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

<p>Risk of myopathy (A)</p> Signup and view all the answers

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

<p>NADPH (C)</p> Signup and view all the answers

Which enzyme metabolizes fluvastatin?

<p>CYP2C9 (C)</p> Signup and view all the answers

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

<p>Naringin in grapefruit juice (B)</p> Signup and view all the answers

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

<p>Pravastatin (B)</p> Signup and view all the answers

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

<p>They can be passively transported across barriers (C)</p> Signup and view all the answers

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