Cyclooxygenase selectivity and the risk of gastro-intestinal complications of various non-steroidal anti-inflammatory drugs: a clinical consideration.

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Kawai S

Cyclooxygenase selectivity and the risk of gastro-intestinal complications of various non-steroidal anti-inflammatory drugs: a clinical consideration.

Inflamm Res. 1998 Oct;47 Suppl 2:S102-6.

PubMed ID

9831331 [View in PubMed

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Abstract

Severe gastro-intestinal complications are a major cause of NSAID-induced deaths in cases of rheumatoid arthritis. We measured COX selectivity by using an intact cell assay system, and found that NS-398 is a highly COX-2-selective inhibitor. Meloxicam, etodolac and diclofenac also showed high COX-2 selectivity. Zaltoprofen, loxoprofen-SRS (active metabolite of loxoprofen), 6-MNA (active metabolite of nabumetone) and ibuprofen showed intermediate COX-2 selectivity. The lowest COX-2 selectivities, which means the highest COX-1 selectivities, were observed in indomethacin, aspirin, and oxaprozin. There appears to be a good relationship between our data and some clinical data of severe gastro-intestinal toxicity. The more a given NSAID is selective for COX-2, the safer it is for clinical use. In conclusion, to anticipate the safety of NSAIDs, we find that an intact cell assay system, using human cells for measurement of COX selectivity, may be more useful than using direct enzyme assay systems.

DrugBank Data that Cites this Article

Drug Targets

Drug	Target	Kind	Organism	Ph值armacological Action	Actions
Oxaprozin	Prostaglandin G/H synthase 1	Protein	Humans	Yes	Inhibitor	Details
Oxaprozin	Prostaglandin G/H synthase 2	Protein	Humans	Yes	Inhibitor	Details