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cyclooxygenase-2 (COX-2) specific inhibitor

Contraindications: - avoid in patients with cardiovascular risk factors - hypertension, hyperlipidemia, renal failure ... [11] * safe in patients with aspirin-exacerbated respiratory disease [12] Adverse effects: 1) hypertension (especially systolic hypertension) 2) diminished renal function 3) peripheral edema 4) heart failure 5) upper GI bleed (probably less-likely than non-selective NSAIDs) Drug interactions: - as likely as non-selective NSAIDs to potential upper GI bleeding when used in combination with warfarin [8] Mechanism of action: 1) selectively inhibit cyclo-oxygenase-2 (COX-2) - selectivity > 100-fold for COX-2 vs COX-1 [12] 2) inhibition of prostacyclin production 3) do NOT inhibit platelet aggregation Notes: December 23, 2004: The U.S. Food and Drug Administration (FDA) issued a public health advisory concerning use of non-steroidal anti-inflammatory drug products (NSAIDs) including those known as COX-2 selective agents. [5]

Interactions

drug interactions drug adverse effects (more general classes) monitor with non steroidal anti-inflammatory agents (NSIADs)

Related

cyclooxygenase-2 (COX2, PGH synthase-2, prostaglandin endoperoxide synthase-2)

Specific

carprofen (Rimadyl, Imadyl, Imafen) celecoxib (Celebrex) deracoxib (Deramaxx) etoricoxib (Arcoxia) firocoxib (Equioxx, Previcox) lumiracoxib (Prexige) parecoxib (Dynastat) robenacoxib (Onsior) rofecoxib (Vioxx) valdecoxib (Bextra)

General

non-steroidal anti-inflammatory agent (NSAID)

Properties

INHIBITS: cyclooxygenase-2

References

  1. Prescriber's Letter 7(10):55 2000
  2. Prescriber's Letter 8(6):31-32 2001
  3. Journal Watch 23(13):103, 2003 Spiegel BMR et al, Ann Intern Med 138:795, 2003
  4. Prescriber's Letter 11(11): 2004 Safety of COX-2 Inhibitors and Their Place in Therapy Detail-Document#: 201102 (subscription needed) http://www.prescribersletter.com
  5. http://www.fda.gov/cder/drug/advisory/nsaids.htm
  6. Prescriber's Letter 12(2): 2005 Update on the Safety and Use of COX-2 Inhibitors and Traditional NSAIDs Detail-Document#: 210202 (subscription needed) http://www.prescribersletter.com
  7. Prescriber's Letter 12(3): 2005 COX-2 Inhibitor Safety: An Update Detail-Document#: 210301 (subscription needed) http://www.prescribersletter.com
  8. Journal Watch 25(6):46, 2005 Battistella M, Mamdami MM, Juurlink DN, Rabeneck L, Laupacis A. Risk of upper gastrointestinal hemorrhage in warfarin users treated with nonselective NSAIDs or COX-2 inhibitors. Arch Intern Med. 2005 Jan 24;165(2):189-92. PMID: 15668365
  9. Prescriber's Letter 12(5): 2005 FDA Announces Important Changes and Additional Warnings for COX-2s and NSAIDs Detail-Document#: 210505 (subscription needed) http://www.prescribersletter.com
  10. FDA MedWatch COX-2 Selective (includes Bextra, Celebrex, and Vioxx) and Non-Selective Non-Steroidal Anti-Inflammatory Drugs (NSAIDs) http://www.fda.gov/medwatch/SAFETY/2005/safety05.htm#NSAID
  11. Medical Knowledge Self Assessment Program (MKSAP) 16 American College of Physicians, Philadelphia 2012
  12. Morales DR et al. Safety risks for patients with aspirin-exacerbated respiratory disease after acute exposure to selective nonsteroidal anti-inflammatory drugs and COX-2 inhibitors: Meta-analysis of controlled clinical trials. J Allergy Clin Immunol 2014 Jul; 134:40 PMID: 24388008