PCSK9 Inhibitors – Lipid Control

by Pravin Shukle, MD

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    Okay, let's go on to the PCSK9's. So this is a whole new world for you guys because you are entering medicine at a time that's really very exciting. These class of drugs which are monoclonal antibodies are changing the entire landscape of medicine. You are getting drugs that no longer follow the normal rules of pharmacology. So all of that stuff we've been learning about, binding curves and everything has changed. I very much encourage you to watch the immunology lecture through Lecturio because it's going to explain how these drugs are working in different systems. Let me explain to you why these drugs are so exciting using cholesterol control as an example. But remember this stuff, this monoclonal antibody stuff, it's in every system, whether it's dermatology, or rheumatology, or bone mineral physiology. The immune globulins and the monoclonal antibodies are so exciting as to make me want to see what happens in the next 15 years no matter what. This is really exciting stuff. The only downside of these agents is they are really hard to pronounce. So if you'll forgive me, I'm going to use the trade names instead of the generic names because I can barely get my mouth around them. Praluent, Repatha and bococizumab which does not have a trade name yet as of the time of making this lecture are monoclonal antibodies that are humanized. So if you look at the suffix of these drugs it will tell you what percentage are humanized and not. And if it ends in 'umab' then you know that it's fully humanized. These are not drugs in a typical sense. These are immuneglobulins that are binding to your target. And they are not cleared by the liver or the kidney. They are cleared by the reticuloendothelial system....

    About the Lecture

    The lecture PCSK9 Inhibitors – Lipid Control by Pravin Shukle, MD is from the course Cardiovascular Pharmacology.

    Included Quiz Questions

    1. Clearance by the reticuloendothelial system is by a linear, non-specific pathway.
    2. Clearance via the target mediated drug disposition pathway is non-saturable and non-linear.
    3. They require glucuronidation in the liver before they are biologically active.
    4. They are usually excreted by the kidney.
    5. They are affected by drugs that affect the CYP450 system.
    1. Injection site reactions
    2. Elevation of hepatic transaminases
    3. Increased hepatic triglyceride levels
    4. Increased risk of colon cancer
    5. Increased risk of renal failure
    1. Less intracellular cholesterol production
    2. Increased degradation of LDL receptor complexes.
    3. Elevated levels of PCSK9
    4. Very low levels of intracellular cholesterol
    5. Decreased LDL receptor recycling.

    Author of lecture PCSK9 Inhibitors – Lipid Control

     Pravin Shukle, MD

    Pravin Shukle, MD

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