Abstract |
Five metabolites of diclofenac sodium ( Voltarol) have been identified in human plasma. All five metabolites were more than 50 times less potent than diclofenac in inhibiting PGE2 production in zymosan-stimulated mouse macrophages and LTC4 synthesis was not inhibited in these cells. Anti-inflammatory activity ( adjuvant arthritis and carragheenan-induced paw oedema in rats) and analgesic activity ( phenyl-p-benzoquinone writhing, mouse) of the metabolites were at least 10 times lower when compared to diclofenac. There was a good correlation between in vitro PGE2 inhibition and in vivo activities for diclofenac and its metabolites indicating that inhibition of prostaglandin synthesis is a major mechanism responsible for their pharmacological actions.
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Authors | I Wiesenberg-Boettcher, J Pfeilschifter, A Schweizer, A Sallmann, P Wenk |
Journal | Agents and actions
(Agents Actions)
Vol. 34
Issue 1-2
Pg. 135-7
(Sep 1991)
ISSN: 0065-4299 [Print] Switzerland |
PMID | 1793018
(Publication Type: Comparative Study, Journal Article)
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Chemical References |
- SRS-A
- Diclofenac
- Dinoprostone
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Topics |
- Animals
- Arthritis, Experimental
(drug therapy)
- Diclofenac
(analogs & derivatives, blood, pharmacology)
- Dinoprostone
(biosynthesis)
- Edema
(drug therapy)
- Humans
- In Vitro Techniques
- Macrophages
(drug effects, metabolism)
- Mice
- Pain
(prevention & control)
- Rats
- Rats, Inbred Strains
- SRS-A
(biosynthesis)
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