Effects of taprostene, a stable prostacyclin analogue, on haemodynamics, platelet function and arachidonate metabolism in healthy volunteers.
In order to assess the effect of taprostene on haemodynamics, platelet function and arachidonate metabolism in 4 healthy volunteers an intravenous infusion of 25 ng.kg-1.min-1 was given for 6 h. During the infusion period systolic blood pressure dropped from 130 to 111 mm Hg and diastolic blood pressure from 77 to 69 mm Hg. The heart rate rose from 77 to 84 beats/min. During the taprostene infusion the slope and height of the ADP and collagen induced platelet aggregation curves were significantly inhibited and the sensitivity of platelets to PGI2 and PGE1 was increased. Plasma and serum thromboxane B2, conversion of exogenous radiolabelled arachidonic acid, WU-test, circulating endothelial cell count, concentration of platelet factor 4, beta-thromboglobulin, malondialdehyde and the PGI2-synthesis stimulating plasma factor did not show any clear drug-related alteration. It is concluded that infusion of taprostene 25 ng.kg-1.min-1 caused measurable inhibition of platelet function ex vivo.
Virgolini
I
I
Atherosclerosis Research Group, Vienna.
Fitscha
P
P
Sinzinger
H
H
Barth
H
H
D000328:Adult; D001095:Arachidonic Acids / Q000378:metabolism*; D011464:Epoprostenol / Q000494:pharmacology* / Q000031:analogs & derivatives; D006439:Hemodynamics / Q000187:drug effects*; D006801:Humans; D008297:Male; D010974:Platelet Aggregation / Q000187:drug effects*; D010975:Platelet Aggregation Inhibitors; D011465:Prostaglandins, Synthetic / Q000494:pharmacology*
D001095:Arachidonic Acids; D010975:Platelet Aggregation Inhibitors; D011465:Prostaglandins, Synthetic; C039188:taprostene; D011464:Epoprostenol