| 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
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