Furlong R, Brogden R N
ADIS Drug Information Services, Auckland, New Zealand.
Drugs. 1988 Oct;36(4):455-74. doi: 10.2165/00003495-198836040-00004.
Xamoterol is a partial agonist at the beta 1-adrenoceptor. Haemodynamic studies indicate that xamoterol moderately increases myocardial contractility, improves diastolic relaxation and lowers left ventricular filling pressure at rest and during moderate exercise. At higher levels of sympathetic activity (e.g. strenuous exercise) it produces negative chronotropic responses whilst the reduced filling pressure is maintained. Studies in patients with mild to moderate chronic heart failure demonstrate an advantage for xamoterol 200mg twice daily over placebo and digoxin with respect to improvement in exercise capacity and symptoms. In limited trials to date the initial response seems to be maintained during periods of up to 12 months. Preliminary small studies suggest that xamoterol is useful in the treatment of some patients with angina pectoris, sinoatrial disease or postural hypotension, although further studies are needed to confirm its clinical role in such patients. Xamoterol appears to be generally well tolerated, but deleterious effects in a small number of patients with asthma, or severe heart failure due to dilated cardiomyopathy indicate the need for cautious use of xamoterol in patients with these diseases. Thus, xamoterol is a promising addition to the drugs available to the physician for treating patients with mild to moderate heart failure although further controlled studies are required to clearly establish its precise role.
扎莫特罗是β1肾上腺素受体的部分激动剂。血流动力学研究表明,扎莫特罗可适度增强心肌收缩力,改善舒张期松弛,并在静息和中度运动时降低左心室充盈压。在交感神经活动较高水平(如剧烈运动)时,它会产生负性变时反应,同时维持降低的充盈压。对轻至中度慢性心力衰竭患者的研究表明,与安慰剂和地高辛相比,每日两次服用200mg扎莫特罗在改善运动能力和症状方面具有优势。在迄今为止的有限试验中,最初的反应似乎在长达12个月的期间内得以维持。初步的小型研究表明,扎莫特罗对某些心绞痛、窦房结疾病或体位性低血压患者的治疗有用,尽管需要进一步研究来证实其在此类患者中的临床作用。扎莫特罗似乎总体耐受性良好,但少数哮喘患者或扩张型心肌病所致严重心力衰竭患者出现的有害作用表明,对于患有这些疾病的患者,使用扎莫特罗需要谨慎。因此,扎莫特罗是医生用于治疗轻至中度心力衰竭患者的现有药物中一个有前景的补充药物,尽管需要进一步的对照研究来明确确立其确切作用。