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What is the effect of decreased intracellular cholesterol concentrations on hepatic uptake of cholesterol-containing LDL-C particles?

  • It increases the hepatic uptake of cholesterol-containing LDL-C particles (correct)
  • It decreases the hepatic uptake of cholesterol-containing LDL-C particles
  • It stabilizes the hepatic uptake of cholesterol-containing LDL-C particles
  • It has no effect on the hepatic uptake of cholesterol-containing LDL-C particles

    • What is a common side effect of cholestyramine?

  • Constipation (correct)
  • Diarrhea
  • Hypertension
  • Hypoglycemia

    • What is the mechanism of action of ezetimibe?

  • Inhibition of PCSK9 enzyme
  • Increase in the production of LDL receptors
  • Stimulation of cholesterol synthesis
  • Prevention of absorption of dietary cholesterol and cholesterol that is excreted in bile (correct)

    • What is the indication for using colesevelam in addition to its use in hyperlipidemias?

    <p>Type 2 diabetes</p> Signup and view all the answers

    What is the effect of PCSK9 enzyme on LDL receptors?

    <p>It increases the degradation of LDL receptors</p> Signup and view all the answers

    What is the indication for using proprotein convertase subtilisin kexin type 9 inhibitors?

    <p>All of the above</p> Signup and view all the answers

    What is the advantage of colesevelam over other bile acid sequestrants?

    <p>It has fewer GI side effects</p> Signup and view all the answers

    What is the effect of ezetimibe on LDL-C when used as monotherapy?

    <p>It decreases LDL-C by about 18%</p> Signup and view all the answers

    What is the indication for using cholestyramine?

    <p>Type IIA and type IIB hyperlipidemias</p> Signup and view all the answers

    What is the percentage of LDL-C lowering when PCSK9 inhibitors are combined with statin therapy?

    <p>50% to 70%</p> Signup and view all the answers

    What is the primary site of PCSK9 enzyme production?

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

    What is a common adverse drug reaction associated with PCSK9 inhibitors?

    <p>Injection site reactions</p> Signup and view all the answers

    In which patients may PCSK9 inhibitors be considered as an additional therapy?

    <p>Patients with high ASCVD risk and statin intolerance</p> Signup and view all the answers

    What is the name of the target enzyme inhibited by PCSK9 inhibitors?

    <p>Proprotein convertase subtilisin kexin type 9</p> Signup and view all the answers

    What is the class of antihyperlipidemic drugs that PCSK9 inhibitors belong to?

    <p>Proprotein convertase subtilisin kexin type 9 inhibitors</p> Signup and view all the answers

    What is the primary mechanism by which fibrates increase HDL levels?

    <p>Increased expression of PPARα</p> Signup and view all the answers

    Which of the following side effects of fibrates can be increased when used in combination with statins?

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

    What is the effect of fibrates on LDL levels?

    <p>0-20% decrease</p> Signup and view all the answers

    What is the effect of fibrates on triglyceride levels?

    <p>20-50% decrease</p> Signup and view all the answers

    Which of the following is a common adverse effect of fibrates?

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

    What is the effect of fibrates on warfarin?

    <p>Increased risk of bleeding</p> Signup and view all the answers

    Which of the following antihyperlipidemic drugs works by inhibiting the absorption of dietary cholesterol?

    <p>Cholesterol absorption inhibitors</p> Signup and view all the answers

    Which of the following antihyperlipidemic drugs is most likely to increase high-density lipoprotein (HDL) cholesterol levels?

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

    Which of the following antihyperlipidemic drugs can cause skin rash as a side effect?

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

    Which of the following antihyperlipidemic drugs works by inhibiting the production of very-low-density lipoprotein (VLDL) in the liver?

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

    Which of the following antihyperlipidemic drugs can cause muscle pain as a side effect?

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

    Which of the following antihyperlipidemic drugs is most likely to reduce triglyceride levels?

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

    Which of the following antihyperlipidemic drugs can cause gastrointestinal side effects such as diarrhea?

    <p>Bile acid sequestrants</p> Signup and view all the answers

    Which of the following antihyperlipidemic drugs is most likely to increase the risk of liver damage?

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

    Which of the following statements about the mechanism of action of bile acid sequestrants is TRUE?

    <p>They increase the excretion of cholesterol into the bile.</p> Signup and view all the answers

    Which of the following side effects is LESS likely to occur with colesevelam compared to other bile acid sequestrants?

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

    What is the effect of ezetimibe on the absorption of fat-soluble vitamins?

    <p>It impairs their absorption.</p> Signup and view all the answers

    Which of the following statements about PCSK9 inhibitors is FALSE?

    <p>They are used in patients with type IIA hyperlipidemia.</p> Signup and view all the answers

    What is the effect of PCSK9 inhibitors on LDL receptors?

    <p>They increase the availability of LDL receptors.</p> Signup and view all the answers

    Which of the following statements about the effect of ezetimibe on LDL-C is TRUE?

    <p>It decreases LDL-C by about 18%.</p> Signup and view all the answers

    Which of the following medications is indicated for the treatment of familial hyperlipidemia?

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

    What is the primary mechanism of action of fibrates?

    <p>Activating PPARα receptors</p> Signup and view all the answers

    Which of the following side effects is associated with niacin treatment?

    <p>Prostaglandin-mediated flushing and pruritus</p> Signup and view all the answers

    What is the effect of fibrates on HDL levels?

    <p>Increase of 10-20%</p> Signup and view all the answers

    Which of the following medications is contraindicated with statin therapy?

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

    What is the effect of fibrates on LDL levels?

    <p>Decrease of 0-20%</p> Signup and view all the answers

    What is the primary mechanism by which bile acid sequestrants decrease plasma LDL-C?

    <p>Decreased intracellular cholesterol concentrations</p> Signup and view all the answers

    Which of the following antihyperlipidemic drugs is NOT indicated for type 2 diabetes?

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

    What is a common side effect of bile acid sequestrants that is minimized with colesevelam?

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

    What is the effect of proprotein convertase subtilisin kexin type 9 inhibitors on LDL receptors?

    <p>Increased availability of LDL receptors for LDL-C clearance</p> Signup and view all the answers

    Which of the following antihyperlipidemic drugs is used in addition to maximally tolerated statin therapy in patients with heterozygous or homozygous familial hypercholesterolemia?

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

    What is the mechanism by which ezetimibe reduces LDL-C?

    <p>Inhibition of cholesterol absorption in the intestine</p> Signup and view all the answers

    What is a potential interaction between bile acid sequestrants and other medications?

    <p>Impaired absorption of certain medications</p> Signup and view all the answers

    What is the approximate percentage reduction in LDL-C when ezetimibe is used as monotherapy?

    <p>18%</p> Signup and view all the answers

    Study Notes

    Hyperlipidemia

    • Elevated levels of circulating lipids, specifically cholesterol and triglycerides (TG)
    • Correlated with an increased incidence of atherosclerosis and coronary artery disease (CAD)

    Factors Influencing Hyperlipidemia

    • Age
    • Sex
    • Family history
    • Smoking
    • Alcoholic
    • Hypertension
    • Diabetes
    • Obesity
    • Low HDL levels

    Treatment of Hyperlipidemia

    • Non-Pharmacological Therapy (First Line)
      • Diet modification:
        • Decrease intake of total fat and especially saturated fat
        • Increase fiber intake
        • Increase Omega-3-fatty acids (found in fish)
        • Increase fruits and vegetables (antioxidants)
        • Decrease simple sugars (sucrose)
      • Exercise (↑ HDL levels)

    Antihyperlipidemic Drugs

    • Statins
    • Niacin
    • Fibrates
    • Bile acid sequestrants
    • Cholesterol absorption inhibitors
    • Proprotein convertase subtilisin kexin type 9 (PCSK9) inhibitors

    Statins

    • Competitive inhibitor of HMG CoA reductase, the rate-limiting step in cholesterol synthesis
    • Reduce hepatic cholesterol, resulting in:
      • Increased LDL receptor expression
      • Increased removal of LDL-C from the blood
      • Decreased cholesterol synthesis
      • Decreased VLDL synthesis and secretion
    • Side effects:
      • Elevated liver enzymes
      • Myopathy and rhabdomyolysis
      • Enzyme CYP-3A4 interaction
      • GIT disturbance
      • Contra-indicated in pregnancy
    • Indications:
      • Used in hypercholesterolemia
      • Used in Coronary Artery Disease (CAD)
      • Used in patients with triglycerides levels higher than 250 mg/dL and with reduced HDL-C levels

    Niacin (Nicotinic acid)

    • Inhibits lipolysis in adipose tissue, resulting in:
      • Decreased hepatic VLDL synthesis
      • Decreased production of LDL in the plasma
      • Decreased LDL and TG levels by 25 and 50%, respectively
      • Increased HDL by 35%
    • Side effects:
      • Prostaglandin-mediated flushing and pruritus
      • Nausea and abdominal discomfort
      • Hyperuricemia and hepatotoxicity
    • Indications:
      • Familial hyperlipidemia
      • Mixed elevation of LDL-C and TG (in combination with statins)
      • Elevation of TG (VLDL) and low levels of HDL

    Fibrates (gemfibrozil and fenofibrate)

    • Primarily used for reducing TG and increasing HDL serum levels
    • Mechanism of action:
      • Activators of the nuclear transcription factor peroxisome proliferator-activated receptor α (PPARα)
      • Increased LPL expression
      • Increased TG clearance from circulating VLDL
      • Increased expression of HDL levels
    • Side effects:
      • Mild GI disturbances
      • Gallstones (increased biliary cholesterol excretion)
      • Myalgia and rhabdomyolysis have been reported in patients taking gemfibrozil and statins together
      • Both fibrates may increase the effects of warfarin

    Bile Acid Sequestrants (Cholestyramine, colestipol, and colesevelam)

    • LDL-C lowering effects
    • Mechanism of action:
      • Bind negatively charged bile acids and bile salts in the small intestine
      • Resin/bile acid complex is excreted in the feces
      • Lowering bile acid concentration leads to:
        • Increased conversion of cholesterol to bile acids
        • Increased hepatic uptake of cholesterol-containing LDL-C particles
        • Decrease in plasma LDL-C
    • Indications:
      • Type IIA and type IIB hyperlipidemias
      • Cholestyramine can also relieve pruritus caused by biliary stasis
      • Colesevelam is also indicated for type 2 diabetes due to its glucose-lowering effects
    • Side effects:
      • GI disturbances (constipation, nausea, and flatulence)
      • Impairment of absorption of fat-soluble vitamins (A, D, E, and K)
      • Interference with the absorption of many drugs (digoxin, warfarin, and thyroid hormone)

    Inhibitors of Cholesterol Absorption (Ezetimibe)

    • Mechanism of action:
      • Prevention of absorption of dietary cholesterol and cholesterol that is excreted in bile
      • Increased LDL receptors in liver and increased removal of LDL-C from the blood
    • Indications:
      • Used in hypercholesterolemia
      • As monotherapy, ezetimibe reduces LDL-C by about 18%
      • When combined with a statin, it is even more effective
    • Side effects:
      • Well tolerated

    Proprotein Convertase Subtilisin Kexin Type 9 Inhibitors (Alirocumab and Evolocumab)

    • Mechanism of action:
      • Inhibit the PCSK9 enzyme, leading to:
        • Increased LDL receptors on the surface of hepatocytes
        • Increased clearance of LDL-C from the serum
    • Indications:
      • Used in addition to maximally tolerated statin therapy in patients with heterozygous or homozygous familial hypercholesterolemia
      • Clinical ASCVD who require additional LDL-C lowering

    Fibrates

    • Increase HDL by 35%
    • Indications: Familial hyperlipidemia, Mixed elevation of LDL-C and TG, Elevation of TG and low levels of HDL
    • Side effects: Prostaglandin-mediated flushing and pruritus, Nausea and abdominal discomfort, Hyperuricemia and hepatotoxicity
    • Mechanism of action: Activators of PPARα, increase LPL expression, increase TG clearance from circulating VLDL, increase expression of HDL levels
    • Adverse effects: Mild GI disturbances, Gallstones, Myalgia and rhabdomyolysis (with statins), Increased effects of warfarin

    Bile Acid Sequestrants

    • Mechanism of action: Bind negatively charged bile acids and bile salts in the small intestine, reduce bile acid concentration, increase conversion of cholesterol to bile acids
    • Indications: High LDL-C, Statin intolerance
    • Side effects: GI disturbances, Impaired absorption of fat-soluble vitamins (A, D, E, K), Interference with absorption of certain drugs

    PCSK9 Inhibitors

    • Mechanism of action: Inhibit PCSK9 enzyme, increase LDL receptors, increase clearance of LDL-C from serum
    • Indications: Familial hypercholesterolemia, Clinical ASCVD, High ASCVD risk and statin intolerance
    • Side effects: Injection site reactions, Immunologic or allergic reactions, Nasopharyngitis, Upper respiratory tract infections

    Inhibitors of Cholesterol Absorption

    • Mechanism of action: Prevent absorption of dietary cholesterol and cholesterol in bile, increase LDL receptors in liver, increase removal of LDL-C from blood
    • Indications: Hypercholesterolemia
    • Side effects: Well tolerated

    Hyperlipidemia

    • Hyperlipidemia is a condition characterized by elevated levels of circulating lipids, specifically cholesterol and triglycerides (TG).
    • It is correlated with an increased incidence of atherosclerosis and coronary artery disease (CAD).

    Risk Factors

    • Age
    • Sex
    • Family history
    • Smoking
    • Alcoholic
    • Hypertension
    • Diabetes
    • Obesity
    • Low HDL levels

    Treatment of Hyperlipidemia

    Non-Pharmacological Therapy

    • Diet modification:
      • Decrease intake of total fat and especially saturated fat
      • Increase fiber intake
      • Increase Omega-3-fatty acids (found in fish)
      • Increase fruits and vegetables (antioxidants)
      • Decrease simple sugars (sucrose)
    • Exercise (increases HDL levels)

    Pharmacological Therapy

    Antihyperlipidemic Drugs

      1. Statins
      1. Niacin:
      • Increases HDL by 35%
      • Indications:
        • Familial hyperlipidemia
        • Mixed elevation of LDL-C and TG (in combination with statins)
        • Elevation of TG (VLDL) and low levels of HDL
      • Side effects:
        • Prostaglandin-mediated flushing and pruritus
        • Nausea and abdominal discomfort
        • Hyperuricemia and hepatotoxicity
      1. Fibrates (gemfibrozil and fenofibrate):
      • Primarily used for reducing TG and increasing HDL serum levels
      • Mechanism of action: Activators of the nuclear transcription factor peroxisome proliferator-activated receptor α (PPARα)
      • Adverse Effects:
        • Mild GI disturbances
        • Gallstones (increase biliary cholesterol excretion)
        • Myalgia and rhabdomyolysis have been reported in patients taking gemfibrozil and statins together
      1. Bile acid sequestrants (Cholestyramine, colestipol, and colesevelam):
      • Mechanism of action: Bind negatively charged bile acids and bile salts in the small intestine
      • Indications:
        • Type IIA and type IIB hyperlipidemias
        • Cholestyramine can also relieve pruritus caused by biliary stasis
        • Colesevelam is also indicated for type 2 diabetes due to its glucose-lowering effects
      • Side effects:
        • GI disturbances, such as constipation, nausea, and flatulence
        • Impair the absorption of the fat-soluble vitamins (A, D, E, and K)
      1. Inhibitors of cholesterol absorption (Ezetimibe):
      • Mechanism of action: Prevention of absorption of dietary cholesterol and cholesterol that is excreted in bile
      • Indications:
        • Hypercholesterolemia
        • As monotherapy, ezetimibe reduces LDL-C by about 18%
        • When combined with a statin, it is even more effective
      • Side effects: Generally well-tolerated
      1. Proprotein convertase subtilisin kexin type 9 inhibitors (Alirocumab and evolocumab):
      • Mechanism of action: Inhibit the PCSK9 enzyme, leading to an increase in LDL receptors on hepatocytes
      • Indications:
        • Used in addition to maximally tolerated statin therapy in patients with heterozygous or homozygous familial hypercholesterolemia
        • Clinical ASCVD who require additional LDL-C lowering

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