The DOI matches its Crossref record; 39 of the 39 references it cites were found in a registry or an index.
Comparative Inhibitory Activity of Rofecoxib, Meloxicam, Diclofenac, Ibuprofen, and Naproxen on COX‐2 versus COX‐1 in Healthy Volunteers
Abstract
Steady‐state inhibitory activity of rofecoxib (Vioxx™) on COX‐2 versus COX‐1 was compared with that of commonly used nonsteroidal anti‐inflammatory drugs (NSAIDs) in 76 healthy volunteers randomized to placebo, rofecoxib 12.5 mg qd, rofecoxib 25 mg qd, diclofenac 50 mg tid, ibuprofen 800 mg tid, sodium naproxen 550 mg bid, or meloxicam 15 mg qd. All of these doses include the high end of the approved clinical dose range. Ex vivo whole‐blood assays were used to determine the effect on COX‐2 and COX‐1 activity, respectively. Urinary prostanoids were also measured. Mean inhibition of COX‐2 (measured as the weighted average inhibition [WAI] of lipopolysaccharide [LPS]‐induced PGE2 generation over 8 hours on day 6 vs. baseline) was −2.4%, 66.7%, 69.2%, 77.5%, 93.9%, 71.4%, and 71.5% for placebo, rofecoxib 12.5 mg, rofecoxib 25 mg, meloxicam, diclofenac, ibuprofen, and naproxen, respectively. Corresponding values for mean inhibition of COX‐1 (measured as TXB2 generation in clotting whole blood) were −5.15%, 7.98%, 6.65%, 53.3%, 49.5%, 88.7%, and 94.9%. Rofecoxib had no significant effect on urinary excretion of 11‐dehydro TXB2, a COX‐ 1‐derived product. These data support the contention that rofecoxib is the only drug of the regimens tested that uniquely inhibits COX‐2 without affecting COX‐1.
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Cites
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New insights into the mode of action of anti-inflammatory drugs
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Adverse Upper Gastrointestinal Effects of Rofecoxib Compared With NSAIDs
Langman, M. J. (1999) · JAMA · doi:10.1001/jama.282.20.1929 · Cited by 686
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Cited by
Risk of Cardiovascular Events Associated with Selective COX-2 Inhibitors
Mukherjee, D. (2001) · JAMA · doi:10.1001/jama.286.8.954 · Cited by 1,741
Cyclooxygenase Inhibitors and the Antiplatelet Effects of Aspirin
Catella-Lawson, F., Reilly, M. P., Kapoor, S. C., Cucchiara, A. J., DeMarco, S., Tournier, B., Vyas, S. N., & FitzGerald, G. A. (2001) · New England Journal of Medicine · doi:10.1056/nejmoa003199 · Cited by 1,394
Risk of cardiovascular events and rofecoxib: cumulative meta-analysis
Jüni, P., Nartey, L., Reichenbach, S., Sterchi, R., Dieppe, P. A., & Egger, M. (2004) · The Lancet · doi:10.1016/s0140-6736(04)17514-4 · Cited by 846
Diclofenac: an update on its mechanism of action and safety profile
Gan, T. J. (2010) · Current Medical Research and Opinion · doi:10.1185/03007995.2010.486301 · Cited by 600
Cannon, C. P., Curtis, S. P., FitzGerald, G. A., Krum, H., Kaur, A., Bolognese, J. A., Reicin, A. S., Bombardier, C., Weinblatt, M. E., van der Heijde, D., et al. (2006) · The Lancet · doi:10.1016/s0140-6736(06)69666-9 · Cited by 522
Metadata
- Authors
- van Hecken, A., Schwartz, J. I., Depré, M., de Lepeleire, I., Dallob, A., Tanaka, W., Wynants, K., Buntinx, A., Arnout, J., Wong, P. H., Ebel, D. L., Gertz, B. J., & de Schepper, P. J.
- Venue
- The Journal of Clinical Pharmacology
- Publisher
- Wiley
- Published
- 2000-10
- Volume
- 40
- Issue
- 10
- Pages
- 1109-1120
- ISSN
- 0021-9754 (ISSN-L)
- 0091-2700
- 1552-4604
- OpenAlex
- W1565253767
- Cited by
- 354
- References
- 39
- FWCI
- 17.13
- Type
- journal article
- Language
- en
- Open access
- closed
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- The paper
- van Hecken, A., Schwartz, J. I., Depré, M., de Lepeleire, I., Dallob, A., Tanaka, W., Wynants, K., Buntinx, A., Arnout, J., Wong, P. H., Ebel, D. L., Gertz, B. J., & de Schepper, P. J. (2000). Comparative Inhibitory Activity of Rofecoxib, Meloxicam, Diclofenac, Ibuprofen, and Naproxen on COX‐2 versus COX‐1 in Healthy Volunteers. The Journal of Clinical Pharmacology. https://doi.org/10.1177/009127000004001005
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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
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