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</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</p> Signup and view all the answers

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

    <p>Decreased</p> Signup and view all the answers

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

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

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

    <p>Synergistic</p> Signup and view all the answers

    What is the primary mechanism of action of Ezetimibe?

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

    What is a potential side effect of Ezetimibe?

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

    How do Bile acid binding resins affect Ezetimibe?

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

    What is the mechanism of action of PCSK9 inhibitors?

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

    What population should avoid PCSK9 inhibitors?

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

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

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

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

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

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

    <p>ALS</p> Signup and view all the answers

    What is the clinical usage of HMG CoA reductase inhibitors?

    <p>Hypercholesterolemia</p> Signup and view all the answers

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

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

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

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

    What percentage of fenofibrate is excreted in the urine?

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

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

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

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

    <p>↓</p> Signup and view all the answers

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

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

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

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

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

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

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

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

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

    <p>Reduced liver hyperlipidemia</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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