HMG-CoA Reductase Inhibitors – Lipid Control

by Pravin Shukle, MD

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    Let's move to the HMG-CoA reductase. Now, HMG-CoA reductase block a step in the conversion of HMG-CoA to cholesterol. So competitive inhibition of the HMG-CoA reductase enzyme is how we get the name statins, because it stops this enzyme. Now most of the effects are due to LDL receptor expression. What do I mean by that? Well, let's think of it this way. Everytime you want to catch a LDL particle from the blood to be used internally by the hepatocyte, you have to have a little baseball glove on the surface of the cell. That baseball glove catches the baseball which is the LDL particle. Now the baseball glove which is the LDL receptor and the baseball which is the LDL, get internalized into the cell and get broken down in the cell. Normally the LDL receptor is protected from being broken down and it goes back up to the surface, but every now and then one of them are clipped together with the baseball and they all get broken down. So, that means that the cell has this intrinsic way of making sure that the LDL receptors aren't to old. Now when you have HMG-CoA reductase inhibitors, you're blocking intracellular cholesterol production. So the cell, now has to rely on external cholesterol in the LDL particles. So it starts making more and more LDL receptors or more and more baseball gloves to catch more and more baseballs because it's not making it's own cholesterol. And that's how you get a reduction of LDL cholesterol with an HMG-CoA reductase inhibitor. Now there is a couple of secondary beneficial effects of the statins. We call this pleotrophic effects. Pleo means multi-coloured. So, there is some wonderful things that happened because of the statins. First of all, it actually may prevent...

    About the Lecture

    The lecture HMG-CoA Reductase Inhibitors – Lipid Control by Pravin Shukle, MD is from the course Cardiovascular Pharmacology. It contains the following chapters:

    • HMG-CoA Reductase Inhibitors
    • HMG-CoA Reductase Inhibitors: Toxicity
    • HMG-CoA Reductase Inhibitors: Important Points
    • Cholesterol Transport Inhibitors: Ezetimibe

    Included Quiz Questions

    1. Protective against contrast nephropathy
    2. Increases LDL receptor expression
    3. Induction of CYP450 3A4 system
    4. Inhibition of cholesterol transporter
    5. Inhibits intracellular production of cholesterol
    1. Rhabdomyolysis risk is increased when combined with Ezitimibe.
    2. They may produce mild elevation of CK levels.
    3. They may produce mild elevations of transaminases.
    4. Drug interactions may occur with inducers of CYP450 3A4 with simvastatin.
    5. Cerivastatin was withdrawn from the market due to risk for rhabdomyolysis.
    1. Pravastatin
    2. Cerivastatin
    3. Rosuvastatin
    4. Atorvastatin
    5. Fluvastatin
    1. Properly functioning LDL receptors are required for statins to produce their effect.
    2. VLDL synthesis is impaired, so these patients have lower LDL levels already.
    3. HMG-CoA reductase binding site is distorted in these patients making statins less effective.
    4. The high risk of drug-induced pancreatitis precludes these patients from being prescribed statins.
    5. These patients are deficient in lipoprotein lipase and rarely have elevated LDL levels.
    1. There is no increase in the risk for hepatoxicity when combined with statins.
    2. It is a prodrug that requires glucuronidation to exert its biological effect.
    3. It is one of the best tolerated drugs in the management of hyperlipidemia.
    4. It acts by inhibiting the cholesterol transporter.
    5. It results in a reactive increase in LDL receptors.

    Author of lecture HMG-CoA Reductase Inhibitors – Lipid Control

     Pravin Shukle, MD

    Pravin Shukle, MD

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