在人体中静脉内和口服一种卡前列环素类似物15-环戊基-ω-五降-5（E）-卡前列环素（ONO 41483）对血小板聚集的抑制作用。

Inhibition of platelet aggregation with intravenous and oral administration of a carboprostacyclin analogue, 15-cyclopentyl-omega-pentanor-5(E)-carbacyclin (ONO 41483) in man.

作者信息

Adaikan P G, Lau L C, Tai M Y, Karim S M

出版信息

Prostaglandins Leukot Med. 1983 Jan;10(1):53-64. doi: 10.1016/s0262-1746(83)80020-1.

Abstract

Intravenous and oral administration of a chemically stable carboprostacyclin analogue, 15-cyclopentyl-omega-pentanor-5(E)-carbacyclin (ONO 41483), resulted in ex-vivo inhibition of ADP-induced platelet aggregation in man. The maximum tolerated intravenous dose was 2.5 ng/kg/min for 1 hour and this produced a mean of 27.1% inhibition in 3 volunteers. For oral administration the tolerated single dose was 200 microgram. At this dose, there was 56.3% inhibition of aggregation (mean of 3 results). High oral (400 microgram) and intravenous doses (5 and 10 ng/kg/min for 1 hour) of ONO 41483, which caused marked inhibition of aggregation (ranging 39-100%), was accompanied by flushing of face and extremities, headache and phlebitis. However, none of the doses tested produced significant changes in arterial blood pressure or heart rate.

摘要

静脉内和口服一种化学性质稳定的卡前列环素类似物，15-环戊基-ω-五降-5(E)-卡前列环素（ONO 41483），可在体外抑制人体中ADP诱导的血小板聚集。静脉内最大耐受剂量为2.5纳克/千克/分钟，持续1小时，这在3名志愿者中产生了平均27.1%的抑制作用。口服时，耐受的单次剂量为200微克。在此剂量下，聚集抑制率为56.3%（3次结果的平均值）。高剂量口服（400微克）和静脉内给药（5和10纳克/千克/分钟，持续1小时）的ONO 41483，可导致明显的聚集抑制（范围为39%-100%），同时伴有面部和四肢潮红、头痛和静脉炎。然而，所测试的任何剂量均未引起动脉血压或心率的显著变化。