COX-2 Inhibitors

by Pravin Shukle, MD

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    00:01 Let's move on to a different class of drugs called the cyclooxygenase 2 inhibitors or COX-2 inhibitors.

    00:07 There are several different variation of cyclooxygenase. COX-1, COX-2, COX-3. So these are COX-2 inhibitors.

    00:15 These are very effective pain medications. And the nice thing about these pills is that they have reduced GI side effects.

    00:23 They also reduce the risk of colon cancer which is kind of a bonus.

    00:27 They have a mild increased risk however of myocardial infarction and arterial thrombosis which is why these medications are a little bit more controversial in the sense that there's a lot of people saying "Are they really worth the increased cost?" Now, we have an increased reduction in prostaglandin 1 or prostaglandin I formation and also we are not sure what its effect is on thromboxane A2.

    00:53 Now, prostacyclin promotes vasodilation and inhibits platelet aggregation.

    00:58 Perhaps this is a mechanism that makes this issue relevant here. Thromboxane A2 inhibits vasodilation and promotes platelet aggregation.

    01:07 We believe that perhaps thromboxane A2 activity may be the culprit of how myocardial infarction occurs with the COX-2 inhibitors.

    01:17 Suffice to say we are not really sure.

    01:19 The prototypical example of this medication is celecoxib, also sold as Celebrex. This was the first member of this new group.

    01:31 Now, rofecoxib which was Vioxx and valdecoxib which was Bextra are also both more specific to COX-2.

    01:38 These two products were taken off the market by their manufacturers.

    01:43 Now the reason why these drugs were taken off the market, in my opinion it was silly, I think that they were just being misused by physicians who didn't know how to use the drugs.

    01:53 Suffice it to say, one physician in Australia using 8 times the regular dose of this drug and killing his patients, ended up resulting in taking away medication that were used all over the world.

    02:04 They were relatively good drugs but not available anymore.

    02:07 And I think the only relevant drug in this class left is Celebrex.

    About the Lecture

    The lecture COX-2 Inhibitors by Pravin Shukle, MD is from the course Inflammation Pharmacology.

    Included Quiz Questions

    1. Celecoxib
    2. Aspirin
    3. Tylenol
    4. Ibuprofen
    5. Ketorolac
    1. Slightly increased risk of myocardial infarction
    2. Increases risk of osteopenia and bone fracture
    3. Increases risk of lung fibrosis
    4. This drug causes early menopause.
    5. This drug can cause Reye's syndrome in children.

    Author of lecture COX-2 Inhibitors

     Pravin Shukle, MD

    Pravin Shukle, MD

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