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β受体阻滞剂在原发性高血压血流动力学效应方面的药理差异的潜在意义。

Possible significance of the pharmacological differentiation of beta-blocking agents in hemodynamic effects in essential hypertension.

作者信息

Tsukiyama H, Otsuka K, Horii M, Yoshii Y, Hatori Y, Nakamura Y, Nemoto E, Yamato T, Sakai T, Yamamoto Y

出版信息

Jpn Circ J. 1983 Mar;47(3):313-22. doi: 10.1253/jcj.47.313.

Abstract

Thirteen beta-blocking agents with different pharmacological properties were administered orally to 161 outpatients with essential hypertension for 5 weeks to assess their hemodynamic effects. Cardioselective ones, such as atenolol, metoprolol and acebutolol, reduced mean blood pressure (MBP) and the cardiac index. (CI) without any changes of the total peripheral resistance index. (TPRI). In the total 44 patients treated with these drugs, a positive correlation (r = 0.529, p less than 0.005) was found between the decrease in MBP and that of TPRI, but the decrease in MBP did not correlate with that of CI. Effects of non-cardioselective ones were classified arbitrarily into the following 3 patterns: 1) reduction of CI of more than 0.50 L/min/m2 and a slight increase of TPRI by more than 150 dyne . sec . cm-5 . m2 (nadolol, propranolol, o.prenolol and penbutolol), 2) reduction of TPRI by more than 150 dyne . sec . cm-5 . m2 (pindolol, bunitrolol and labetalol) and 3) the intermediate hemodynamic responses between the two patterns described above (carteolol, bupranolol and bufetolol). In all these 3 groups, the decrease in MBP correlated with that of TPRI (the first group, n = 45, r = 0.557, p less than 0.005; the second, n = 37, r = 0.525, p less than 0.005; the third, n = 35, r = 0.612, p less than 0.005), but did not correlate with the decrease of CI. These results suggest that the antihypertensive effects of beta-blocking agents mainly depend on the reduction of peripheral resistance, although their pharmacological properties are not uniform and their cardiodepressant effects are variable. Reduction of cardiac performance with these beta-blocking agents seemed to be a consequence of overall pharmacological actions including beta-receptor blockade, central effects and membrane stabilizing effects, and it may be antagonized by intrinsic sympathomimetic activity and the reduction in afterload for the heart. Vascular beta-receptor blocking action may play a part in decreasing the degree of reduction of the total peripheral resistance index, while their intrinsic sympathomimetic action on the vascular site may induce vasodilating effects.

摘要

对161例原发性高血压门诊患者口服13种具有不同药理特性的β受体阻滞剂,持续5周,以评估其血流动力学效应。阿替洛尔、美托洛尔和醋丁洛尔等心脏选择性β受体阻滞剂可降低平均血压(MBP)和心脏指数(CI),而总外周阻力指数(TPRI)无变化。在总共44例接受这些药物治疗的患者中,发现MBP的降低与TPRI的降低呈正相关(r = 0.529,p < 0.005),但MBP的降低与CI的降低无相关性。非心脏选择性β受体阻滞剂的效应可任意分为以下3种模式:1)CI降低超过0.50 L/min/m²,TPRI轻微升高超过150达因·秒·厘米⁻⁵·米²(纳多洛尔、普萘洛尔、氧烯洛尔和喷布洛尔),2)TPRI降低超过150达因·秒·厘米⁻⁵·米²(吲哚洛尔、布尼洛尔和拉贝洛尔),3)上述两种模式之间的中间血流动力学反应(卡替洛尔、丁呋洛尔和丁苄醇)。在所有这3组中,MBP的降低与TPRI的降低相关(第一组,n = 45,r = 0.557,p < 0.005;第二组,n = 37,r = 0.525,p < 0.005;第三组,n = 35,r = 0.612,p < 0.005),但与CI的降低无相关性。这些结果表明,β受体阻滞剂的降压作用主要取决于外周阻力的降低,尽管它们的药理特性并不一致,且其心脏抑制作用也各不相同。使用这些β受体阻滞剂导致心脏功能降低似乎是包括β受体阻滞、中枢效应和膜稳定效应在内的整体药理作用的结果,并且可能被内在拟交感活性和心脏后负荷的降低所拮抗。血管β受体阻滞作用可能在降低总外周阻力指数的降低程度中起作用,而它们在血管部位的内在拟交感作用可能诱导血管舒张效应。

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