C. Canestrini, R. Testa
Feb 1, 1978
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Influential Citations
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Quality indicators
Journal
Pharmacological research communications
Abstract
Summary A non steroidal antiinflammatory agent, Alclofenac (ALCLO), is examined for its inhibitory activity on collagen induced platelet aggregation. Employing “in vitro” techniques, the extent of the ALCLO inhibition is indipendent of incubation time (IC50 = 8.8 · 10−4 M). In contrast, the effect of two other antiinflammatory drugs, acetylsalicylic acid (ASA) and ibuprofen (IBU), is enhanced with extended incubation time. Therefore, ALCLO is equally effective with short incubation (2 min) and at least 80 times less potent than ASA and IBU after long incubation (60 min). ALCLO activity is then studied in “ex vivo” experiments after dosing in rabbit. Drug plasma levels and effects on platelet aggregation are simultaneously determined. After single i.v. injection, plasma elimination kinetics of ALCLO is well correlated with the loss of the antiaggregating activity. Infusion of the drug at three different steady state levels, shows a similar behaviour.