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COX selectivity and half-life of selected NSAIDs

COX selectivity and half-life of selected NSAIDs
Drug COX-1/COX-2 IC50 ratio*[1] Half-life¶[2]
Ibuprofen 0.5 2 hours
Naproxen 0.7 12 to 17 hours
6-MNA (active metabolite of nabumetone) 1.5 24 hours
Acetaminophen 1.6 2 to 3 hours
Indomethacin 1.9 4.5 hours
Meloxicam 18 15 to 22 hours
Diclofenac 29 2 hours
Celecoxib 30 11 hours
RofecoxibΔ 267 17 hours[3]
To be used with UpToDate content on nonsteroidal antiinflammatory drugs.

6-MNA: 6-methoxy-2-napthyl-acetic acid; COX: cyclooxygenase; IC50: half maximal inhibitory concentration; NSAIDs: nonsteroidal antiinflammatory drugs.

* The COX-1/COX-2 IC50 ratio (ie, IC50 of COX-1 divided by the IC50 of COX-2) may be used to characterize relative COX selectivity among NSAIDs. When the COX-1/COX-2 IC50 ratio is close to 1, the NSAID is considered nonselective. NSAIDs with COX-1/COX-2 IC50 ratios >1 are more potent inhibitors of COX-2 than COX-1, with COX-2 selectivity increasing with higher values. This table includes the COX-1/COX-2 IC50 ratio of selected NSAIDs as measured in vitro with human whole blood assays of COX-isoenzyme activity.[1] In vivo, COX-2 selectivity decreases with higher NSAID doses, particularly at doses above the usual dosing range.

¶ Half-life is based on data for oral formulations in adult patients with normal kidney function. Kidney impairment may result in prolonged elimination.

Δ Rofecoxib was withdrawn from the market due to an increased risk of myocardial infarctions and stroke associated with long-term use.
References:
  1. Patrono C, Patrignani P, García Rodríguez LA. Cyclooxygenase-selective inhibition of prostanoid formation: Transducing biochemical selectivity into clinical read-outs. J Clin Invest 2001; 108:7.
  2. US Food & Drug Administration (FDA) approved product information. US National Library of Medicine. https://www.dailymed.nlm.nih.gov/dailymed/index.cfm (Accessed on May 7, 2024).
  3. Rofecoxib. US Food & Drug Administration (FDA) approved product information. Revised May 2016. US Food & Drug Administration. https://www.accessdata.fda.gov/scripts/cder/daf/ (Accessed on May 7, 2024).

With additional data from:

  • Hunter TS, Robison C, Gerbino PP. Emerging evidence in NSAID pharmacology: Important considerations for product selection. Am J Manag Care 2015; 21:S139.
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