Hernández Hernández R, Angeli-Greaves M, Carvajal A R, Guerrero Pajuelo J, Armas Padilla M C, Armas-Hernández M J
Clinical Pharmacology Unit, School of Medicine, Universidad Centro Occidental Lisandro Alvarado, Barquisimeto, Venezuela.
Am J Hypertens. 1996 May;9(5):437-44. doi: 10.1016/0895-7061(95)00436-x.
Antihypertensive effect, platelet aggregation, and plasma lipid profile were studied in a group of 14 hypertensive patients with diastolic blood pressure between 96 and 116 mm Hg during placebo and terazosin phases. Terazosin, an alpha 1-adrenergic blocking agent, was given initially at the dosage of 1 mg daily. Then it was continued at a dosage of 2 mg daily and 5 mg daily respectively, each dosage for 4 weeks. Blood pressure was taken every 2 weeks. Ex vivo platelet aggregation induced by epinephrine, collagen, and adenosine diphosphate (ADP) were carried out twice during the first placebo phase, once at the end of each terazosin dosage, and once in the second placebo phase. Total cholesterol, HDL cholesterol, and triglycerides were measured at the end of first placebo and terazosin phases. Blood from eight patients was taken during the second placebo phase to carry out in vitro response of platelet aggregation induced by ADP, collagen, and epinephrine before and after incubation with terazosin (1, 2 and 5 micrograms/L or doxazosin (100, 200, and 500 micrograms/L for 5 min. Terazosin induced a statistically significant decrease in 14.2/8.0 mm Hg, 26.1/13.4 mm Hg, and 33.9/16.5 mm Hg in the supine position for 1, 2, and 5 mg/daily, respectively. No changes in heart rate were observed. Terazosin inhibited significant ex vivo platelet aggregation induced by epinephrine, collagen, and ADP in a range from 20% to 45% for different concentrations of inducers. Reductions in platelet aggregation seemed not to be dose dependent, as reductions were statistically equivalent for dosages of 1, 2, and 5 mg daily. Terazosin significantly reduced the level of total cholesterol (8.71%) and triglycerides (14.31%), and increased (although not significantly) levels of HDL cholesterol (3.91%). In vitro platelet aggregation was inhibited by doxazosin to a significant extent but not by terazosin.
在14名舒张压在96至116毫米汞柱之间的高血压患者中,研究了安慰剂期和特拉唑嗪期的降压效果、血小板聚集及血脂情况。特拉唑嗪是一种α1肾上腺素能阻滞剂,初始剂量为每日1毫克。然后分别以每日2毫克和每日5毫克的剂量持续给药,每个剂量给药4周。每2周测量一次血压。在第一个安慰剂期进行两次由肾上腺素、胶原蛋白和二磷酸腺苷(ADP)诱导的体外血小板聚集检测,在每个特拉唑嗪剂量结束时进行一次,在第二个安慰剂期进行一次。在第一个安慰剂期和特拉唑嗪期结束时测量总胆固醇、高密度脂蛋白胆固醇和甘油三酯。在第二个安慰剂期采集8名患者的血液,在与特拉唑嗪(1、2和5微克/升)或多沙唑嗪(100、200和500微克/升)孵育5分钟前后,进行由ADP、胶原蛋白和肾上腺素诱导的血小板聚集的体外反应检测。特拉唑嗪使仰卧位血压分别在每日1毫克、2毫克和5毫克剂量时显著下降14.2/8.0毫米汞柱、26.1/13.4毫米汞柱和33.9/16.5毫米汞柱。未观察到心率变化。特拉唑嗪在20%至45%的范围内抑制了由不同浓度诱导剂引起的显著体外血小板聚集。血小板聚集的降低似乎与剂量无关,因为每日1毫克、2毫克和5毫克剂量的降低在统计学上是等效的。特拉唑嗪显著降低了总胆固醇水平(8.71%)和甘油三酯水平(14.31%),并使高密度脂蛋白胆固醇水平有所升高(尽管不显著)(3.91%)。多沙唑嗪在很大程度上抑制了体外血小板聚集,但特拉唑嗪没有。