| Autor: |
Del Maschio, Aldo, Livio, Manuela, Cerletti, Chiara, De Gaetano, Gionvani |
| Zdroj: |
European Journal of Pharmacology; June 1984, Vol. 101 Issue: 3-4 p209-214, 6p |
| Abstrakt: |
Sulfinpyrazone and three of its major metabolites were compared in vitro for their inhibitory effect on human platelet cyclo-ocygenase activity. Sulfinpyrazone appeared to be about 15–20 times less potent than its sulfide metabolite (G25671) adn 6–7 times less potent than the other two compounds, the sulfone metabolite (G31442) and p-hydroxysulfide (G33378). All four compounds were apparently competitive inhibitors of platelet cyclo-oxygenase acitivity. Comparison of the potnecy fo sulfinpyrazone and its metabolites, as determined in the present study and the plasma levels previously measured in man, indicates that sulfinpurazone and G33378 were not potent enough to be effective in man. G31442 showed inhibitory potency slightly lower than its corresponding plasma levels, whereas G25671 was effective at concentrations well below those found in human plasma. This study supports the hypothesis that sulfinpyrazone metabolites (in particular the sulfide) rather than the drug itself affect platelet function when administered therapeutically. |
| Databáze: |
Supplemental Index |
| Externí odkaz: |
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