Which medications in the drug class Nonsteroidal Anti-inflammatory Drugs (NSAIDs) are used in the treatment of Osteoarthritis?

Updated: Jun 10, 2020
  • Author: Carlos J Lozada, MD; Chief Editor: Herbert S Diamond, MD  more...
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Answer

Nonsteroidal Anti-inflammatory Drugs (NSAIDs)

NSAIDs have analgesic, anti-inflammatory, and antipyretic activities. They are used to relieve osteoarthritis pain when the clinical response to acetaminophen is unsatisfactory. The mechanism of action is nonselective inhibition of cyclooxygenase (COX)-1 and COX-2, resulting in reduced synthesis of prostaglandins and thromboxanes. Other mechanisms may also exist, such as inhibition of leukotriene synthesis, lysosomal enzyme release, lipoxygenase activity, neutrophil aggregation, and various cell-membrane functions.

In more inflammatory presentations of osteoarthritis, such as knee involvement with effusion, these agents may be used as first-line pharmacologic therapy. Use the lowest effective dose or intermittent therapy if symptoms are intermittent. All of these medications increase the risk for GI ulcers and have been associated with increased risk of cardiovascular disease. Patients at high risk for GI toxicity may consider adding misoprostol or a proton-pump inhibitor to the regimen or substituting a COX-2–specific inhibitor for the NSAID.

The FDA approved a submicron low-dose product (Zorvolex) for osteoarthritis that allows treatment at a lower dose than the diclofenac sodium and potassium salts. Submicron diclofenac 35 mg PO TID significantly improved Western Ontario and McMasters Universities Osteoarthritis Index (WOMAC) pain subscale scores from baseline at 12 weeks (-44.1; p = 0.0024) compared with placebo (-32.5). [158]

Ketoprofen

Ketoprofen is indicated for relief of mild-to-moderate pain and inflammation. Small dosages are initially indicated in small and elderly patients and in those with renal or liver disease. Doses higher than 75 mg do not increase therapeutic effects. Administer high doses with caution, and closely observe the patient for response.

Piroxicam (Feldene)

Piroxicam decreases the activity of cyclooxygenase, which in turn inhibits prostaglandin synthesis. These effects decrease formation of inflammatory mediators.

Ibuprofen (Advil, Motrin IB, Caldolor, Neoprofen)

Ibuprofen relieves pain and inflammation. It is widely available and is relatively inexpensive as a generic drug. After the very early stages of osteoarthritis, inflammation begins to play a role in the disease. Thus, medications with a combination of analgesic and anti-inflammatory properties become more desirable, at least in theory.

Meloxicam (Mobic)

To some extent, meloxicam is more selective for COX-2 receptors than traditional NSAIDs are. It decreases the activity of cyclooxygenase, thereby, in turn, inhibiting prostaglandin synthesis. These effects decrease the formation of inflammatory mediators.

Diclofenac (Voltaren XR, Cataflam, Cambia, Zipsor)

Diclofenac is one of a series of phenylacetic acids that have demonstrated anti-inflammatory and analgesic properties in pharmacologic studies. It is believed to inhibit cyclooxygenase, which is essential in the biosynthesis of prostaglandins. Diclofenac can cause hepatotoxicity; hence, liver enzymes should be monitored in the first 8 weeks of treatment.

Diclofenac is rapidly absorbed; metabolism occurs in the liver by demethylation, deacetylation, and glucuronide conjugation. The delayed-release, enteric-coated form is diclofenac sodium, and the immediate-release form is diclofenac potassium. It poses a relatively low risk for bleeding GI ulcers.

Celecoxib (Celebrex)

Celecoxib is a COX-2–specific inhibitor. At therapeutic concentrations, COX-2 (inducible by cytokines at sites of inflammation, such as the joints) is inhibited, and COX-1 isoenzyme (present in platelets and the GI tract) is spared; therefore, in nonaspirin users, the incidence of GI toxicity (eg, endoscopic peptic ulcers, bleeding ulcers, perforations, and obstructions) is decreased in comparison with that seen in patients taking nonselective NSAIDs.

Naproxen (Aleve, Anaprox, Anaprox DS, Naprelan, Naprosyn)

Naproxen is used for relief of mild to moderate pain. It inhibits inflammatory reactions and pain by decreasing the activity of cyclooxygenase, which is responsible for prostaglandin synthesis. NSAIDs decrease intraglomerular pressure and decrease proteinuria.


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