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心力衰竭(心衰)病人应用β受体阻断剂时,最大问题是β受体阻断剂的负性变力及变时作用。在引起心衰恶化和明显缓脉情况下,就不能应用β受体阻断剂。β受体阻断剂关键的药理学特性是反激动作用,这种作用就是把与内源性激活无关的受体由活化型转为非活化型。这种现象与β受体阻断剂的“鸟嘌呤核苷酸调节障碍(guanine nucleotide modu-latable binding)”现象及β肾上腺素受体的有无上调密切相关。这种作用在美托洛尔显著,而卡维地洛不明显。因此对重症心衰病人,期待应用反激动作用小的β受体阻断剂。
Heart failure (heart failure) patients with β-blockers, the biggest problem is β-blockers negative force and time-varying role. Beta-blockers can not be used in cases of worsening heart failure and apparently slow pulse conditions. The key pharmacological properties of beta blockers are anti-agonism, which is the conversion of the receptor independent of endogenous activation from activated to inactive. This phenomenon is closely related to the phenomenon of “guanine nucleotide modu-latable binding” of β-blockers and the up-regulation of β-adrenoceptors. This effect is significant in metoprolol, while carvedilol is insignificant. Therefore, patients with severe heart failure, the expected application of anti-small beta blockers.