The essential guide to anti inflammatory drugs

by Nathan Wei, MD, FACP, FACR

Nathan Wei is a board-certified rheumatologist and author of the Second Opinion Arthritis Treatment Kit. It's available exclusively at this website... not available in stores.

Click here: Second Opinion Arthritis Treatment Kit

Non Steroidal Anti Inflammatory Drugs (NSAIDS) are among the most commonly prescribed drugs for arthritis.

The prototype of all NSAIDS is aspirin. Other NSAIDS include ibuprofen (Motrin, Advil), naproxen (Naprosyn, Aleve), sulindac (Clinoril), oxaprozin (Daypro), fenoprofen (Nalfon), etodolac (Lodine), piroxicam (Feldene), nabumetone (Relafen), indomethicin (Indocin), ketoprofen (Orudis), meclofenamate (Meclomen), tolmetin (Tolectin), diflunisal (Dolobid), diclofenac (Voltaren). NSAIDS help reduce signs and symptoms of inflammation. They do not eliminate it because they have no significant effect on the underlying disease process.

NSAIDS are organic acids that are highly protein bound in the blood. These properties allow them to penetrate into inflamed tissue which have a lower pH and which allow entrance of plasma proteins.

NSAIDS work by blocking cyclooxygenase, the enzyme that allows production of prostaglandins, and thromboxane- key factors in the initiation of inflammation.

Prostaglandins also are responsible for a multitude of normal functions in the body including maintenance of kidney blood flow, secretion of the protective mucus lining in the stomach, and enhancing the attraction of platelets (a blood constituent responsible for clotting) to each other.

Besides inhibiting inflammation, NSAIDS also decrease pain, suppress fever, and decrease the stickiness of platelets.

More recently, specific COX 2 inhibitory NSAIDS have been developed. These block the branch of the cyclooxygenase system that causes inhibition of inflammation without inhibiting the prostaglandins that protect the stomach. Theoretically, these are safer anti inflammatory drugs.

Examples include celecoxib (Celebrex), and valdecoxib (Bextra). Another one of the anti-inflammatory drugs that is relatively new but not a COX 2 drug is meloxicam (Mobic).

A new COX 2 drug in the pipeline and close to release is lumiracoxib. This promises to have potentially fewer side effects than currently available anti inflammatory drugs. Whether this is the case or not will probably be evident after this drug is more widely used after FDA approval.

Because of their mechanism of action, NSAIDS have many potential side effects.

In the gastrointestinal (GI) system, NSAIDS cause stomach irritation and ulcer. Stomach acid is increased and the protective mucus lining and bicarbonate buffer is decreased. Gastrointestinal bleeding risk is increased.

NSAIDS also cause an anticoagulant effect. Platelet adhesiveness is decreased. Aspirin will cause long-term irreversible platelet effects that last the lifetime of the platelet (about 10 days), while other NSAIDS have a reversible effect that lasts as long as the drug is in the system.

Another anticoagulant effect occurs in patients who are taking the blood-thinner, warfarin. NSAIDS, because they are so highly protein bound, displace warfarin from plasma proteins and as a result there is more warfarin available to cause more anticoagulant effect.

NSAIDS can cause liver toxicity. Up to 15 per cent of patients will have elevations in liver enzymes. While severe toxicity is unusual, life-threatening hepatitis has been reported. Regular monitoring of liver function is advised for patients who take anti inflammatory drugs regularly.

NSAIDS can have a negative effect on kidney function. They reduce blood flow to the kidney. In elderly patients and in patients who already have reduced kidney blood flow (dehydrated, congestive heart failure), these effects can be substantial leading to the possibility of kidney failure.

Patients with arthritis conditions like systemic lupus erythematosus and progressive systemic sclerosis also are increased risk for this problem. NSAIDS may cause inflammation of kidney tissue and severe protein leakage in the urine.

Other potential side effects include rashes, allergic reactions (asthma), anaphylactic shock, blood cell disorders, ringing in the ears headaches, and meningitis (particularly in patients with SLE).

More recently, COX 2 inhibitors, particularly rofecoxib (Vioxx), have been associated with an increased risk of cardiovascular side-effects (hypertension, edema, heart attack and stroke). [Vioxx is no longer available since it was removed from the market by Merck, its manufacturer.] Celecoxib (Celebrex) and valdecoxib (Bextra) have been associated with severe rashes. At the time of this writing they have not yet been associated with the same cardiovascular problems as Vioxx. However, further studies are being conducted.

Virtually all NSAIDS are converted to inactive metabolites in the liver and excreted by the kidney. Dose reduction and careful monitoring are required in the elderly and in other patients where kidney blood flow may be compromised.

The treatment of a painful disorder is dependent on the nature of the disorder. For instance a headache may require a single or perhaps two doses of NSAID for its analgesic effect. Arthritis, on the other hand, will generally require an anti inflammatory effect which calls for constant and regular dosing.

Patients who do not respond to one NSAID are often switched to another. While going to an NSAID of a different chemical class may make sense, this is not always practical.

Combining NSAIDS is not advised since toxicity is enhanced. Many patients take aspirin for cardiovascular prophylaxis. Adding an aspirin to COX 2 therapy essentially converts COX 2 therapy to NSAID therapy.

While anti inflammatory drugs are helpful for many patients, they are not a panacea and are capable of causing many potential side effects. They should only be used with the advice of a knowledgeable physician.

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