Fat Absorption and MTP Inhibitors – Lipid Control

by Pravin Shukle, MD

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    00:01 Let's talk quickly about fat absorption inhibitors.

    00:04 Orlistat which is sold as Xenical is sold as an obesity treatment but it does have reduction in cholesterol too.

    00:13 Now 50% of patients who take orlistat have a 5% reduction in body mass.

    00:18 The reduction in diabetes mellitus incidence is also recorded, probably related to weight loss.

    00:23 There is a modest reduction in blood pressure and a mild reduction in LDL as well.

    00:28 Now this reduction in LDL is actually independent of the weight loss.

    00:33 So, whatever LDL reduction you get from weight loss, there seems to be a little bit more.

    00:40 The primary serious side effect of Orlistat is an increased risk of renal failure.

    00:45 This complication is relatively rare but it is worth mentioning.

    00:49 The renal failure is related to an increase in oxalate stone formation.

    00:53 The other side effects are generally based around the therapeutic action of the medication.

    00:57 For instance patients complain of loose stools and incontinent, both of which are due to increase fat now being excreted in their stool.

    01:04 Luckily, most of these side effects can be significantly reduced by dietary modification.

    01:09 Let's move on to the MTP inhibitors. This is a new class of drugs.

    01:15 They're fiendishly expensive but they are now coming on to the market.

    01:19 The prototypical drug I would say is lomitapide or Juxtapid. It's an oral tablet.

    01:27 Now, it acts on the microsomal triglyceride transfer protein or MTP, and it is inhibitor of that protein.

    01:38 VLDL and triglyceride assembly and secretion in the liver is what is being affected here.

    01:44 It is used for the treatment of familial hypercholesterolemia.

    01:49 And what it does is it reduces VLDL and all of the non-HDL fraction of the cholesterol profile.

    01:56 It also will reduce apolipoprotein B, because remember that apolipoprotein B are these proteins that are going to be attached to either VLDL or LDL.

    02:08 It can be used in combination with statins and some reports indicate up to 60% reduction in LDL cholesterol with these medications.

    02:19 The adverse events, it may increase hepatic triglyceride levels and it may cause a transaminitis.

    About the Lecture

    The lecture Fat Absorption and MTP Inhibitors – Lipid Control by Pravin Shukle, MD is from the course Cardiovascular Pharmacology. It contains the following chapters:

    • Fat Absorption Inhibitors
    • MTP Inhibitors

    Included Quiz Questions

    1. Increased triglyceride levels
    2. Weight loss
    3. Reduced LDL
    4. Reduced blood pressure
    5. Improved glycemic control
    1. Increased hepatic transaminase levels
    2. Colon cancer
    3. Glucose intolerance
    4. Kidney injury
    5. Myopathy

    Author of lecture Fat Absorption and MTP Inhibitors – Lipid Control

     Pravin Shukle, MD

    Pravin Shukle, MD

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