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波吲洛尔对高血压患者静息及运动时血小板功能的影响。

Effects of bopindolol on platelet function in hypertension at rest and during exercise.

作者信息

Virgolini I, Fitscha P, Rauscha F, Sinzinger H

机构信息

Atherosclerosis Research Group (ASF) Vienna, University of Vienna, Austria.

出版信息

Prostaglandins Leukot Essent Fatty Acids. 1990 Jun;40(2):125-30. doi: 10.1016/0952-3278(90)90154-d.

DOI:10.1016/0952-3278(90)90154-d
PMID:2143586
Abstract

The effects of bopindolol, a new nonselective beta-blocking agent, on platelet function have been studied in 10 male hypertensive patients given the drug (1 mg/day) in turn for eight weeks. Bopindolol significantly (p less than 0.01) decreased the bicycle exercise- (1.5 W/kg body weight for 6 minutes) induced increase in platelet aggregation. During bopindolol-treatment both the slope and the height of the platelet aggregation response curve were moderately decreased at rest before exercise and significantly (p less than 0.05) decreased at rest after exercise. During exercise the slope amounted to 75.4 +/- 44 degrees before and to 70.8 +/- 5.3 degrees after therapy (p less than 0.01), the height to 64.0 +/- 11.9% before and to 58.1 +/- 14.7% (p less than 0.05) after therapy. Furthermore, bopindolol significantly increased the exercise-induced decrease in platelet sensitivity to PGI2 (p less than 0.05; IC-50-value: 2.10 +/- 0.47 vs 1.88 +/- 0.31 ng/ml) and PGD2 (p less than 0.05; IC-50-value: (19.88 +/- 2.10 vs 18.57 +/- 1.63 ng/ml). Bopindolol also significantly (p less than 0.05) decreased the exercise-induced elevation in serum-TXB2 (244.9 +/- 35.2 vs 237.3 +/- 27.2 ng/ml) and plasma-TXB2 (15.7 +/- 6.3 vs 13.1 +/- 3.7 pg/ml). The platelet count, the plasma levels of 6-oxo-PGF1 alpha, beta-thromboglobulin (beta-TG) and platelet factor 4 (PF4) were not affected by bopindolol. It is concluded that bopindolol favourably affects platelet function, in that it lowers exercise-induced platelet aggregation and TXB2-formation in therapeutical doses and increases platelet sensitivity to antiaggregatory prostaglandins.(ABSTRACT TRUNCATED AT 250 WORDS)

摘要

在10名男性高血压患者中依次给予新的非选择性β受体阻滞剂波吲洛尔(1毫克/天),持续八周,研究其对血小板功能的影响。波吲洛尔显著(p<0.01)降低了自行车运动(1.5瓦/千克体重,持续6分钟)诱导的血小板聚集增加。在波吲洛尔治疗期间,运动前静息时血小板聚集反应曲线的斜率和高度均适度降低,运动后静息时显著(p<0.05)降低。运动期间,斜率治疗前为75.4±44度,治疗后为70.8±5.3度(p<0.01),高度治疗前为64.0±11.9%,治疗后为58.1±14.7%(p<0.05)。此外,波吲洛尔显著增加运动诱导的血小板对前列环素I2(p<0.05;半数抑制浓度值:2.10±0.47对1.88±0.31纳克/毫升)和前列腺素D2(p<0.05;半数抑制浓度值:19.88±2.10对18.57±1.63纳克/毫升)敏感性的降低。波吲洛尔还显著(p<0.05)降低运动诱导的血清血栓素B2(244.9±35.2对237.3±27.2纳克/毫升)和血浆血栓素B2(15.7±6.3对13.1±3.7皮克/毫升)升高。血小板计数、6-氧代前列腺素F1α、β-血小板球蛋白(β-TG)和血小板因子4(PF4)的血浆水平不受波吲洛尔影响。结论是,波吲洛尔对血小板功能有有利影响,即它在治疗剂量下降低运动诱导的血小板聚集和血栓素B2形成,并增加血小板对抗聚集前列腺素的敏感性。(摘要截取自250字)

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Bopindolol. A review of its pharmacodynamic and pharmacokinetic properties and therapeutic efficacy.波吲洛尔:其药效学、药代动力学特性及治疗效果综述
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