NSAIDs in the Management of Rheumatoid Arthritis

Original Editor - Kristie Nguyen Top Contributors - Kristie Nguyen, Nupur Smit Shah, Kim Jackson and Lucinda hampton

Overview[edit | edit source]

Non-steroidal anti-inflammatory drugs (NSAIDs) are the first drugs used to symptomatically treat RA.[1] While they are not as potent anti-inflammatory drugs as glucocorticoids, they tend to have fewer side effects and offer pain relief.[2][3] In addition, they may later be combined with DMARDs to control the disease process.[4] The NSAIDs focused on below are ibuprofen, diclofenac, and celecoxib.

Pharmacokinetics[edit | edit source]

NSAIDS exert their effects by inhibiting the COX-1 and COX-2 forms of enzymes that synthesize prostaglandins.[5] Inhibition of COX-1 blocks the production of beneficial and protective prostaglandins, whereas inhibition of COX-2 blocks the synthesis of prostaglandins in inflamed tissues. Ibuprofen and diclofenac block both forms of the enzyme (Roberts & Morrow, 2001).[6] Celecoxib, on the other hand, selectively inhibits only COX-2.[5]

To determine which NSAID should be prescribed, the pharmacokinetics of the drugs should be considered. The half-lives of NSAIDs vary, ranging from a couple of hours (ibuprofen and diclofenac) to eleven hours (celecoxib). Absorption methods also differ. Ibuprofen is primarily absorbed by the GI tract and diclofenac undergoes first-pass metabolism via the liver, resulting in 50% bioavailability. The exact absorption mechanism for celecoxib is still unknown. All three undergo metabolism via the liver and are typically excreted in urine.[7][8][9]

Therapeutic Effects Of NSAIDS[edit | edit source]

  • NSAIDs are the first line of treatment for rheumatoid arthritis which helps in symptomatic relief.
  • It mainly reduces pain and stiffness of the affected joints. the mechanism behind this is inhibition of prostaglandin production in peripheral tissues. Prostaglandin also plays an important role in neuronal sensitization.
  • It also has an anti inflammatory effect on juvenile rheumatoid arthritis.[10]

Adverse Effects[edit | edit source]

There are various toxicities linked with NSAIDS. The effect of it varies based on the compound and dosage.

  • Gastrointestinal- ulcer, colitis, Esophagitis
  • Cardiovascular- Myocardial infarction, stroke
  • Neuro- dizziness, confusion, seizures
  • Renal- water retention, hypertension, weight gain[11][8][9]

References[edit | edit source]

  1. ↑ O'Dell JR. Therapeutic strategies for rheumatoid arthritis. N Engl J Med. 2004;350(25):2591-2602.
  2. ↑ Gotzche PC, Johansen HK. Short-term low-dose corticosteroids vs placebo and nonsteroidal antiinflammatory drugs in rheumatoid arthritis. Cochrane Databse Syst Rev. 2004;(3):CD000189. doi:10.1002/14651858.CD000189.pub2
  3. ↑ Adebajo A. Non-steroidal anti-inflammatory drugs for the treatment of pain and immobility-associated osteoarthritis: consensus guidance for primary care. BMC Fam Pract. 2012;13:23. doi:10.1186/1471-2296-13-23.
  4. ↑ Blumenauer B, Cranney A, Clinch J, Tugwell P. Quality of life in patients with rheumatoid arthritis: which drugs might make a difference. Pharmacoeconomics. 2003;21(13):927-940.
  5. ↑ 5.0 5.1 Vane JR, Botting RM. The mechanism of action of aspirin. Thromb Res. 2003;110(5-6):255-258.
  6. ↑ Roberts LJ, Morrow JD. Analgesic-antipyretic and antiinflammatory agents and drugs employed in the treatment of gout. In: Hardman JG et al, ed. The Pharmacological Basis of Therapeutics. 10th ed. New York, NY: McGraw Hill;2001.
  7. ↑ U.S. Food and Drug Administration. Motrin® Ibuprofen Tablets, USP. https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/017463s105lbl.pdf. Last Modified January 20, 2007. Accessed November 21, 2018.
  8. ↑ 8.0 8.1 U.S. Food and Drug Administration. Voltaren® (diclofenac sodium enteric-coated tablets). https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/019201s046lbl.pdf. Last Modified January 20, 2007. Accessed November 21, 2018.
  9. ↑ 9.0 9.1 U.S. Food and Drug Administration. Celebrex® celecoxib capsules. https://www.accessdata.fda.gov/drugsatfda_docs/label/2008/020998s026lbl.pdf. Last Modified January 20, 2007. Accessed November 21, 2018.
  10. ↑ Crofford LJ. Use of NSAIDs in treating patients with arthritis. Arthritis research & therapy. 2013 Jul;15:1-0.
  11. ↑ Crofford LJ. Use of NSAIDs in treating patients with arthritis. Arthritis research & therapy. 2013 Jul;15:1-0.
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