Chu D, Cocco G, Schweda E, Haeusler G, Strozzi C
Eur J Clin Pharmacol. 1980 Aug;18(2):141-6. doi: 10.1007/BF00561581.
The influence of two beta-adrenoceptor antagonists, propranolol and pindolol, on the haemodynamic effects of papaverine, isoprenaline and noradrenaline was investigated in 9 male patients with first degree essential hypertension. Propranolol and pindolol were given according to a doubleblind, crossover scheme. Heart rate and blood pressure were measured before and after each treatment. Propranolol 670 microgram/kg i.v. reduced the supine and standing systolic blood pressures by 2.3% and 1.6%, respectively. Similarly, the intravenous administration of pindolol 35 microgram/kg reduced supine and standing systolic blood pressure by 5.5% and 8.3% respectively (clinically insignificant). Neither drug affected diastolic blood pressure. Following propranolol, there were moderate reduction in supine and standing heart rates, respectively by 24% and 20% (p < 0.001). Similarly, but to a lesser extent, pindolol reduced supine and standing heart rate by 12% and 17% (p < 0.001). The effects of papaverine, which, at 1.5 mg/kg i.v. reduced systolic blood pressure by 5-10% and increased heart rate by 8-15%, were not significantly influenced by the beta-blockers. The blood pressure and heart rate responses to isoprenaline, on the other hand, were attenuated or inhibited by both beta-blockers. While the beta-blockers inhibited the beta-adrenoceptor component of noradrenaline, the pressor component of noradrenaline, which is mediated through the alpha-adrenoceptors, was not influenced by propranolol, but was inhibited after pindolol. It is concluded that pindolol differs qualitatively from propranolol in that it inhibited both the alpha and beta-adrenoceptor effects of noradrenaline.
在9例原发性轻度高血压男性患者中,研究了两种β-肾上腺素能受体拮抗剂普萘洛尔和吲哚洛尔对罂粟碱、异丙肾上腺素和去甲肾上腺素血流动力学效应的影响。普萘洛尔和吲哚洛尔按照双盲、交叉方案给药。每次治疗前后均测量心率和血压。静脉注射670微克/千克普萘洛尔后,仰卧位和站立位收缩压分别降低2.3%和1.6%。同样,静脉注射35微克/千克吲哚洛尔后,仰卧位和站立位收缩压分别降低5.5%和8.3%(临床意义不显著)。两种药物均未影响舒张压。服用普萘洛尔后,仰卧位和站立位心率分别适度降低24%和20%(p<0.001)。同样,吲哚洛尔也使仰卧位和站立位心率降低,但程度较小,分别为12%和17%(p<0.001)。静脉注射1.5毫克/千克罂粟碱可使收缩压降低5%-10%,心率增加8%-15%,其效应不受β受体阻滞剂的显著影响。另一方面,两种β受体阻滞剂均减弱或抑制了对异丙肾上腺素的血压和心率反应。虽然β受体阻滞剂抑制了去甲肾上腺素的β-肾上腺素能受体成分,但由α-肾上腺素能受体介导的去甲肾上腺素升压成分不受普萘洛尔影响,但在吲哚洛尔作用后受到抑制。结论是,吲哚洛尔在性质上与普萘洛尔不同,因为它抑制了去甲肾上腺素的α和β肾上腺素能受体效应。