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Celecoxib: Mechanism of Action & Structure

Instructor: Artem Cheprasov

Artem has a doctor of veterinary medicine degree.

This lesson is going to teach you about the mechanism of action behind a drug called celecoxib. You'll learn what it does and exactly how that happens.

Celecoxib

Sometimes you have to wonder how brand name drugs are named. It seems that for at least one drug manufacturer, they want to make it seem that if you take this one pill, you'll CELEBRate all night long because of how great it is since it's called CELEBRex. Celebrex is the better known brand name of celecoxib, whose structure you can see in this lesson.

The 2D structure of celecoxib.
The 2D structure of celecoxib.

We're going to learn how this drug works its magic in this lesson by learning about inflammation, celecoxib's pharmacologic categories, and its mechanism of action.

Pharmacologic Category

Celecoxib is categorized as a non-opioid analgesic. In other words, it provides pain relief (analgesia), but it's not an opioid, like morphine. In fact, celecoxib is actually an NSAID, a non-steroidal anti-inflammatory drug. Inflammation is a bodily process that produces:

  • Dolor, pain
  • Rubor, redness
  • Tumor, swelling
  • Calor, heat
  • Loss of function. In other words, the affected area may not work as well. Think of a really inflamed knee and how well that works (not)!

Celecoxib can help minimize these signs and symptoms of inflammation and maybe make you celebrate with joy. Maybe?

Mechanism of Action

Anyways, how does celecoxib do what it's supposed to do? Well, it's a specific kind of NSAID. It's a COX-2 selective NSAID at therapeutic concentrations. COX-2 stands for cyclooxygenase-2. This is an enzyme, something that speeds up biochemical reactions. Celecoxib decreases the activity of this enzyme.

The activity of this enzyme is, in the end, responsible for the formation of prostaglandins. In other words, celecoxib inhibits prostaglandin synthesis. But what is prostaglandin and why is its inhibition important? Prostaglandin is a hormone-like fatty acid that helps to promote inflammation.

During inflammation, it is COX-2 that appears to be the major source, so to speak, of prostaglandin formation. So we'd want to stop COX-2 from helping to form all those prostaglandin molecules. That's because prostaglandins are involved in the dilation of blood vessels. This increases blood flow to an area of inflammation and, in turn, leads to the redness and swelling we associate with inflammation.

Prostaglandins also act within the central nervous system and on peripheral sensory neurons in a way that leads to the sensation of pain. Peripheral neurons are nerve cells that are located outside of the central nervous system, the brain and spinal cord.

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