的影响低于常规剂量的口服nadolol相对β1 /β2-adrenoceptor封锁。
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Wheeldon纳米化DG, Lipworth BJ
的影响低于常规剂量的口服nadolol相对β1 /β2-adrenoceptor封锁。
Br中国新药杂志。1994年8月,38 (2):103 - 8。
- PubMed ID
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7981009 (在PubMed]
- 文摘
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1。本研究的目的是评估的相对选择性β1 /β2拮抗剂beta-adrenoceptor阻滞剂nadolol,在临床剂量低于传统。2。八个正常志愿者收到单一口服剂量的安慰剂(PL), nadolol 5毫克(它们),20毫克(N20)或80毫克(歌曲到手)单盲,随机交叉设计。β1-adrenoceptor对抗被衰减运动心跳过速,评估和β2-adrenoceptor封锁的影响salbutamol-induced变时性的,hypokalaemic和手指地震响应。β2和β的相对比例衰减1-mediated响应计算和表达为β2:选择性β1比率。3所示。Nadolol产生剂量减少锻炼心动过速符合增加β1-adrenoceptor封锁;意味着减少% (95% CI)与安慰剂比较:它们被10.7 (6.6 - 14.8),N20 21.4(17.3 - 25.4),歌曲到手38.9 (34.8 - 42.9)。然而,即使最低剂量的nadolol(5毫克)产生几乎完全削弱β2-mediated效果和显著增加锻炼高钾血症; peak exercise hyperkalaemia (mmol l-1) (means and 95% CI): PL 4.88 (4.68 to 5.07), N5 5.36 (5.17 to 5.55), N20 5.48 (5.28 to 5.67), N80 5.42 (5.22 to 5.61). beta 2:beta 1 selectivity ratios significantly increased as the dose of nadolol was reduced. 4. These data suggest that whereas in the clinical dose range nadolol behaves as a non-selective beta-adrenoceptor antagonist, as the dose is reduced this drug demonstrates an increasing degree of selectivity for the beta 2-adrenoceptor.(ABSTRACT TRUNCATED AT 250 WORDS)