What is COX-2 (COX2)?

What are COX2 (COX-2) Inhibitors and How to They Work?

To understand COX-2 (COX2) Inhibitors, you first have to understand COX-1 (COX1) and what its role in the body is. Regular NSAIDS (generally COX-1 and COX-2 Inhibitors) work by inhibiting the production of prostaglandins (PGs). Prostaglandins are fatty-acid derivatives located throughout your body that are well known for their inflammation and immune response effects. However, they also have many different roles in the body. A scientific list would read as such: PG’s are involved in as diverse normal processes as ovulation, blood clotting, renal function, wound healing, vasomotor tone, platelet aggregation, differentiation of immune cells, nerve growth, bone metabolism and initiation of labor. Pretty essential to your body, wouldn’t you say?

If you are familiar with the fact that when you are using drugs such as aspirin, your blood thins and you bruise easily. That is a “side effect” of the COX-1 inhibitor. In the above list, that would fall under the blood clotting category. Remember, COX-1 inhibitors work by inhibiting PG’s. Due to the acidity of the stomach, the cells of your stomach are replaced very quickly, within a few days. One of the major roles of PG’s is to keep the lining of the stomach intact, and when your PG system is disrupted, by taking COX-1 drugs, stomach irritation, digestive tract problems, intestinal or stomach bleeding and even death could occur.

COX-2 inhibitors were discovered later, as a healthier, more targeted way of treating the inflammation, without the side effects. This makes sense as COX-2 is found more commonly in inflammatory and immune cells than COX-1 drugs. Unfortunately, this would prove to be far, far from the truth. While COX-2 is more specific to inflammation, the side effects can be worse than COX-1 drugs.

NSAID Side Effects

The side effects of COX-1 drugs are pretty terrible. It is estimated that 25% experience some kind of side effect and 5% develop SERIOUS health consequences such as GI (stomach) bleeding, acute renal failure, or worse. Anti-inflammatory drugs (i.e., Advil®, Motrin®, Aleve®, Ordus®, Aspirin) alone cause over 16,500 deaths and over 103,000 hospitalizations per year in the US, according to a review article published in the New England Journal of Medicine1.

You can see why researchers would believe there was a cut and dry line between COX-1 and COX-2. Unfortunately, like many things, it was not nearly as cut and dry as this. Over the counter drugs such as Ibuprofen and Naproxen work to inhibit COX-1 and COX-2. Aspirin works more on COX-1. Some others such as diclofenac work primarily on COX-2 but also affect COX-1. However, even “selective” COX-2 inhibitors aren’t that selective. At therapeutic dosages, they inhibit enough COX-1 to potentially cause the same stomach toxicity and other associated problems as COX-1. Not to the exact same extent but more than enough to do damage. In development are other “newer aspirins” that may prove to ACTUALLY be more selective for COX-2 than COX-1, but in the mean time – despite claims of being “selective” – the current COX-2’s such as Celebrex® are simply not selective enough, not to mention some of their potentially horrible side effects and the associated lawsuits that have been filed due to side effects such as heart attacks, stroke and blood clots. Our advice is to explore other alternatives that are cheaper and far more effective in treating your pain. Glucosamine is a natural substance that has been shown to not just rebuild cartilage, but also repair the damage that has already occurred. Not even a pure “second generation” COX-2 drug will be able to do that.

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Be sure to visit the Glucosamine Product Guide for a review of commercially available glucosamine products broken down by 9 different categories such as price per month, quality and type. Learn what the best products out there are and what criteria was used to ranked each.

1. Wolfe MM, et. al. NEJM 1999;340(24):1888-99