The analgesic drug tramadol has been shown to relieve pain in inflammatory conditions, to inhibit the development of experimental inflammation, and to reduce prostaglandin (PG)E 2 concentrations in the inflammatory exudate. In this study, we evaluated the putative activity of tramadol to suppress prostaglandin endoperoxide synthase-1 (PGHS-1), and prostaglandin endoperoxide synthase-2 (PGHS-2) activities in human whole blood in vitro. Platelet thromboxane (Tx)B 2 production and monocyte PGE 2 production in LPS-stimulated blood were measured in samples incubated with different concentrations (300 ng/ml, 3 μg/ml, 30 μg/ml) of tramadol or its enantiomers. Neither tramadol nor the enantiomers inhibited the formation of arachidonic acid metabolites. Our results indicate that the anti-inflammatory effect of tramadol demonstrated in some models is not related to a direct inhibitory effect on the formation of prostanoids.

Tramadol anti-inflammatory activity is not related to a direct inhibitory action on prostaglandin endoperoxide synthases / C. Buccellati, A. Sala, R. Ballerio, M. Bianchi. - In: EUROPEAN JOURNAL OF PAIN. - ISSN 1090-3801. - 4:4(2000), pp. 413-415.

Tramadol anti-inflammatory activity is not related to a direct inhibitory action on prostaglandin endoperoxide synthases

C. Buccellati;A. Sala;
2000

Abstract

The analgesic drug tramadol has been shown to relieve pain in inflammatory conditions, to inhibit the development of experimental inflammation, and to reduce prostaglandin (PG)E 2 concentrations in the inflammatory exudate. In this study, we evaluated the putative activity of tramadol to suppress prostaglandin endoperoxide synthase-1 (PGHS-1), and prostaglandin endoperoxide synthase-2 (PGHS-2) activities in human whole blood in vitro. Platelet thromboxane (Tx)B 2 production and monocyte PGE 2 production in LPS-stimulated blood were measured in samples incubated with different concentrations (300 ng/ml, 3 μg/ml, 30 μg/ml) of tramadol or its enantiomers. Neither tramadol nor the enantiomers inhibited the formation of arachidonic acid metabolites. Our results indicate that the anti-inflammatory effect of tramadol demonstrated in some models is not related to a direct inhibitory effect on the formation of prostanoids.
Settore BIO/14 - Farmacologia
2000
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/2434/185239
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