Cox-2 Inhibitors

  • Pharmacy Author:
    Omudhome Ogbru, PharmD

    Dr. Ogbru received his Doctorate in Pharmacy from the University of the Pacific School of Pharmacy in 1995. He completed a Pharmacy Practice Residency at the University of Arizona/University Medical Center in 1996. He was a Professor of Pharmacy Practice and a Regional Clerkship Coordinator for the University of the Pacific School of Pharmacy from 1996-99.

  • Medical and Pharmacy Editor: Jay W. Marks, MD
    Jay W. Marks, MD

    Jay W. Marks, MD

    Jay W. Marks, MD, is a board-certified internist and gastroenterologist. He graduated from Yale University School of Medicine and trained in internal medicine and gastroenterology at UCLA/Cedars-Sinai Medical Center in Los Angeles.

  • Medical and Pharmacy Editor: Charles Patrick Davis, MD, PhD
    Charles Patrick Davis, MD, PhD

    Charles Patrick Davis, MD, PhD

    Dr. Charles "Pat" Davis, MD, PhD, is a board certified Emergency Medicine doctor who currently practices as a consultant and staff member for hospitals. He has a PhD in Microbiology (UT at Austin), and the MD (Univ. Texas Medical Branch, Galveston). He is a Clinical Professor (retired) in the Division of Emergency Medicine, UT Health Science Center at San Antonio, and has been the Chief of Emergency Medicine at UT Medical Branch and at UTHSCSA with over 250 publications.

What are Cox-2 inhibitors?

Prostaglandins are made by two different enzymes, cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2). The prostaglandins made by the two different enzymes have slightly different effects on the body. COX-2 inhibitors are NSAIDs that selectively block the COX-2 enzyme and not the COX-1 enzyme. Blocking this enzyme impedes the production of prostaglandins by the COX-2 which is more often the cause the pain and swelling of inflammation and other painful conditions. Because they selectively block the COX-2 enzyme and not the COX-1 enzyme, these drugs are uniquely different from traditional NSAIDs which usually block both COX-1 and COX-2 enzymes.

For which conditions are Cox-2 inhibitors prescribed?

COX-2 inhibitors are used for treating:

Which COX-2 inhibitors are available in the United States?

Celecoxib (Celebrex) is the only COX-2 inhibitor available in the United States. It is available as a generic.

Rofecoxib (Vioxx) and valdecoxib (Bextra) were withdrawn from the market in 2004 and 2005, respectively, because they excessively increased the risk of heart attacks and strokes with long term use.

What are NSAIDs (nonsteroidal anti-inflammatory drugs)?

Nonsteroidal anti-inflammatory drugs (NSAIDs) are a class of drugs that reduce inflammation but are different from steroids, another class of drugs that also reduces inflammation. NSAIDs reduce pain, fever, and swelling and are commonly prescribed for inflammation of the joints (arthritis) and other tissues, such as in tendinitis and bursitis. Examples of NSAIDs include:

NSAIDs are used frequently by millions of individuals for treatment of pain, fever and swelling caused by inflammatory conditions as well as for pain alone. NSAIDs work by blocking the production of prostaglandins, chemical messengers that often are responsible for the pain and swelling of inflammatory conditions.

The side effects of NSAIDs are listed below and are compared and contrasted with those of COX-2 inhibitors.

NSAIDs vs. COX-2 inhibitors, which is better?

COX-2 inhibitors impede prostaglandin production. COX-1 is an enzyme which is normally present in a variety of tissues in the body, including sites of inflammation and the stomach. Some of the prostaglandins made by COX-1 protect the inner lining of the stomach. Common NSAIDs such as aspirin block both COX-1 and COX-2 (see below). When the COX-1 enzyme is blocked, inflammation is reduced, but the protection of the lining of the stomach also is lost. This can cause stomach upset as well as ulceration and bleeding from the stomach and even the intestines.

The other cyclooxygenase, COX-2, also produces prostaglandins, but the COX-2 enzyme is located specifically in areas of the body that commonly are involved in inflammation but not in the stomach. When the COX-2 enzyme is blocked, inflammation is reduced; however, since the COX-2 enzyme does not play a role in protecting the stomach or intestine, COX-2 specific NSAIDs do not have the same risk of injuring the stomach or intestines.

Older NSAIDs (for example, aspirin, ibuprofen, naproxen, etc.) all act by blocking the action of both the COX-1 and COX-2 enzymes. COX-2 inhibitors selectively block the COX-2 enzyme and therefore have a lower risk of causing ulcers of the stomach or intestine.

Medically Reviewed by a Doctor on 10/13/2016

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