Sengeløv H, Winther K
Medical Department C, Bispebjerg Hospital, Copenhagen, Denmark.
Eur J Clin Pharmacol. 1989;37(5):453-7. doi: 10.1007/BF00558123.
Fourteen healthy male volunteers (age 21-29 years, mean 23.7 years) were given placebo for 14 days followed immediately by felodipine 5 mg b.d. for a further 14 days. After each period of treatment blood for analysis was taken at rest and after exercise on a cycle ergometer. Platelet aggregation, plasma beta-thromboglobulin (B-TG), platelet factor 4 (PF-4), adrenaline and noradrenaline, and serum thromboxane B2 (TXB2), 6-keto-prostaglandin (F1 alpha (6-keto-PGF1 alpha), and euglobulin clot lysis time (ECLT), were measured on each occasion. The ECG, heart rate and blood pressure were monitored during the exercise tests. After felodipine therapy there was a significant decrease in the plasma level of PF-4 and B-TG at rest. This effect was maintained during exercise. There was no significant change in platelet aggregation, ECLT, TXB2 or 6-keto-PGF1 alpha at rest or during exercise. Irrespective of therapy, the plasma levels of adrenaline and noradrenaline were increased and the ECLT was decreased when measured immediately after exercise. Thus, felodipine in modest therapeutic dosage decreases the plasma levels of B-TG and PF-4, indicating an inhibitory effect on platelet on release. The effect also occurred during exercise. Felodipine did not change fibrinolytic activity or the production of TXB2 or 6-keto-PGF1 alpha.
14名健康男性志愿者(年龄21 - 29岁,平均23.7岁)先服用安慰剂14天,随后立即服用非洛地平,每日2次,每次5毫克,持续14天。在每个治疗阶段结束后,于静息状态及在自行车测力计上运动后采集血样进行分析。每次均检测血小板聚集、血浆β - 血小板球蛋白(B - TG)、血小板因子4(PF - 4)、肾上腺素和去甲肾上腺素、血清血栓素B2(TXB2)、6 - 酮 - 前列腺素(F1α(6 - 酮 - PGF1α)以及优球蛋白凝块溶解时间(ECLT)。运动试验期间监测心电图、心率和血压。非洛地平治疗后,静息时血浆PF - 4和B - TG水平显著降低。运动期间该效应持续存在。静息或运动时血小板聚集、ECLT、TXB2或6 - 酮 - PGF1α均无显著变化。无论治疗情况如何,运动后立即检测时,血浆肾上腺素和去甲肾上腺素水平升高,ECLT降低。因此,中等治疗剂量的非洛地平可降低血浆B - TG和PF - 4水平,表明对血小板释放有抑制作用。该效应在运动时也会出现。非洛地平未改变纤溶活性或TXB2及6 - 酮 - PGF1α的生成。