D. Pallapies et al., EFFECTS OF SINGLE ORAL DOSES OF LYSINE CLONIXINATE AND ACETYLSALICYLIC-ACID ON PLATELET FUNCTIONS IN MAN, European Journal of Clinical Pharmacology, 49(5), 1996, pp. 351-354
Lysine clonixinate is an analgesic drug with a so far unknown mechanis
m of action. We have determined its effect on platelet cyclooxygenase
in man. Biosynthesis of thromboxane (TX)B-2 and prostaglandin (PG)F-2
alpha in clotting whole blood ex vivo as well as collagen-induced plat
elet aggregation measured before and at various time points after oral
administration of 125 mg lysine clonixinate were compared to results
obtained with 500 mg acetylsalicylic acid (ASA). While biosynthesis of
both TXB(2) and PGF(2 alpha) measured radioimmunologically was inhibi
ted significantly 2.5 h, but not 6 h, after administration of lysine c
lonixinate, inhibition by ASA was much greater and still highly signif
icant after 48 h. Similarly, collagen-induced aggregation of platelet-
rich plasma was inhibited for a longer period and to a greater extent
after administration of ASA than after lysine clonixinate. Our results
indicate that lysine clonixinate is a cyclooxygenase inhibitor of mod
erate potency. It remains to be investigated whether mechanisms other
than inhibition of cyclooxygenase contribute to the analgesic activity
of lysine clonixinate.