HMG CoA Reductase Inhibitors (Statins)
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Questions and Answers

What is a contraindication for bile acid binding resins?

  • Digestive issues
  • Hypercholesterolemia
  • Hypersensitivity (correct)
  • Pregnancy/Breastfeeding mother (correct)

What is the effect of bile acid binding resins on LDL receptors?

  • Increased (correct)
  • Variable
  • No effect
  • Decreased

What is a side effect of bile acid binding resins?

  • Improved digestion
  • Increased energy
  • Weight gain
  • GI discomfort (correct)

What is the mechanism of action of Cholestyramine?

<p>Binding to bile acid (A)</p> Signup and view all the answers

When should bile acid binding resins be administered in relation to other drugs?

<p>4 hours after other drugs (C), 4 hours before other drugs (D)</p> Signup and view all the answers

What is the effect of bile acid binding resins on absorption of vitamins and drugs?

<p>Decreased (D)</p> Signup and view all the answers

What type of patients may be prescribed Cholesterol absorption inhibitors as monotherapy?

<p>Statin-intolerant patients (A)</p> Signup and view all the answers

What is the effect of combining bile acid binding resins with statins?

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

What is the primary mechanism of action of Ezetimibe?

<p>Inhibiting reabsorption of cholesterol excreted in bile (B)</p> Signup and view all the answers

What is a potential side effect of Ezetimibe?

<p>Abdominal pain (D)</p> Signup and view all the answers

How do Bile acid binding resins affect Ezetimibe?

<p>Inhibit the absorption of Ezetimibe (C)</p> Signup and view all the answers

What is the mechanism of action of PCSK9 inhibitors?

<p>Inhibiting the action of PCSK9 (B)</p> Signup and view all the answers

What population should avoid PCSK9 inhibitors?

<p>Both pregnant women and breastfeeding mothers (A)</p> Signup and view all the answers

What effect do PCSK9 inhibitors have on LDL-c levels?

<p>Decrease LDL-c levels in patients with very high LDL-c (D)</p> Signup and view all the answers

What is the mechanism of action of HMG CoA reductase inhibitors?

<p>Inhibit HMG-CoA reductase, a rate-limiting enzyme (D)</p> Signup and view all the answers

What is the effect of HMG CoA reductase inhibitors on LDL receptors?

<p>Increase LDL receptors (C)</p> Signup and view all the answers

Which of the following is a side effect of HMG CoA reductase inhibitors?

<p>Myopathy, especially rhabdomyolysis (A)</p> Signup and view all the answers

Which of the following HMG CoA reductase inhibitors is metabolized by CYP3A4?

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

What is the clinical usage of HMG CoA reductase inhibitors?

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

What is the effect of HMG CoA reductase inhibitors on atherosclerosis?

<p>Decrease plaque rupture (B)</p> Signup and view all the answers

Which of the following medications may interact with HMG CoA reductase inhibitors?

<p>Itraconazole, Ketoconazole (A)</p> Signup and view all the answers

What is the alternative medication that may be considered in case of myopathy or rhabdomyolysis?

<p>Rosuvastatin or Pravastatin (D)</p> Signup and view all the answers

What is the purpose of using siRNA, including Inclisiran, in addition to statins?

<p>To reduce PCSK9 levels and increase LDL receptor recycling (C)</p> Signup and view all the answers

What is the main side effect of Gemfibrozil?

<p>Myopathy, which needs to be monitored by CK levels (B)</p> Signup and view all the answers

What percentage of fenofibrate is excreted in the urine?

<p>60-90% (D)</p> Signup and view all the answers

What is the main mechanism of action of fibric acid derivatives like fenofibrate?

<p>Stimulating PPARα and increasing FA oxidation (A)</p> Signup and view all the answers

What is the indication for using fibric acid derivatives like Gemfibrozil?

<p>Hypertriglyceridemia and chylomicronemia syndrome (D)</p> Signup and view all the answers

What is a potential complication of using fibric acid derivatives like fenofibrate?

<p>Increased risk of gallstone formation (B)</p> Signup and view all the answers

What is the effect of ω3-fatty acids on Liver TG?

<p>↓ (D)</p> Signup and view all the answers

What is a potential side effect of Eicosapentaenoic acid (EPA)?

<p>Prolonged bleeding time (A)</p> Signup and view all the answers

What is the relationship between ω3-fatty acids and PPARα activity?

<p>May modulate (A)</p> Signup and view all the answers

What is the effect of Decosahexaenoic acid (DHA) on triglycerides?

<p>45%↓ (A)</p> Signup and view all the answers

What is a potential interaction of ω3-fatty acids with other medications?

<p>Antithrombotic drugs (D)</p> Signup and view all the answers

What is a potential benefit of ω3-fatty acids in liver disease?

<p>Reduced liver hyperlipidemia (B)</p> Signup and view all the answers

Study Notes

HMG CoA Reductase Inhibitors

  • Also known as statins
  • Inhibit HMG-CoA reductase, a rate-limiting enzyme
  • Result: inhibition of de novo synthesis of cholesterol
  • Clinical usage: hypercholesterolemia, CVD prevention, and restoration of vessel function
  • Increase LDL receptors and HDL
  • Examples: Atorvastatin, Lovastatin, Simvastatin
  • Side effects: transaminase enzyme increase, myopathy, and rhabdomyolysis
  • Contraindications: liver disease, pregnancy, breastfeeding, and hypersensitivity

Bile Acid Binding Resins

  • Examples: Cholestyramine, Colestipol, Colesvelam
  • Mechanism of action: inhibit enterohepatic circulation by binding to bile acid
  • Clinical usage: hypercholesterolemia, especially when statins are contraindicated
  • Generally safe, but may cause GI discomfort and decrease absorption of vitamins and drugs

Cholesterol Absorption Inhibitors

  • Example: Ezetimibe
  • Mechanism of action: inhibit intestinal absorption of cholesterol by blocking NPC1L1
  • Clinical usage: hypercholesterolemia, especially in statin-intolerant patients
  • Side effects: abdominal pain, diarrhea, and steatorrhea
  • Bile acid binding resins inhibit absorption of ezetimibe

PCSK9 Inhibitors

  • Examples: Alirocumab, Evolocumab, Inclisiran
  • Mechanism of action: monoclonal antibody that binds to PCSK9, increasing LDL receptor recycling
  • Clinical usage: severe hypercholesterolemia, especially in addition to statins
  • Avoided in pregnancy and breastfeeding mothers

Fibric Acid Derivatives

  • Examples: Gemfibrozil, Fenofibrate, Bezafibrate
  • Mechanism of action: stimulate PPARα, increasing FA oxidation and decreasing VLDL and LDL
  • Clinical usage: hypertriglyceridemia, chylomicronemia syndrome, and dysbetalipoproteinemia
  • Side effects: myopathy, increased risk of gallstone formation, and liver hyperlipidemia
  • Contraindications: liver disease, pregnancy, and gout

ω3-Fatty Acids

  • Examples: Eicosapentaenoic acid (EPA), Decosahexaenoic acid (DHA)
  • Mechanism of action: uncertain, may modulate PPARα activity
  • Clinical usage: triglyceride reduction
  • Side effects: prolonged bleeding time, interaction with antithrombotic drugs

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Description

Learn about statins, a type of medication that inhibits HMG-CoA reductase, a rate-limiting enzyme, and its effects on cholesterol synthesis, clinical usage, and side effects.

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