Department of Cardiovascular Medicine, Hiroshima University Graduate School of Biomedical and Health Sciences, Hiroshima, Japan.
Department of Cardiology, Hiroshima City Hospital, Hiroshima, Japan.
Cardiovasc Ther. 2018 Jun;36(3):e12325. doi: 10.1111/1755-5922.12325. Epub 2018 Mar 5.
The bisoprolol transdermal patch is a newly developed β-blocker designed to deliver its pharmaceutical ingredient through the skin surface. We aimed to compare the bisoprolol transdermal patch and bisoprolol fumarate tablet using the heart rate variability (HRV).
Eligible hypertensive patients received a 2-week administration with a 2.5 mg bisoprolol fumarate tablet, followed by 24-hour Holter monitoring. The tablet was then switched to a 4 mg bisoprolol transdermal patch, and after 2 weeks of its administration, the Holter monitoring was repeated. Both drugs were given once daily. Endpoint was any alteration in the HRV caused by a change in the administration route for bisoprolol.
There was no difference in the 24-hour time-domain and frequency-domain HRV measurements before and after the drug switching among patients recruited (N = 30). However, the switching significantly altered the time-course curves of the hourly HRV measurements, including the mean normal-to-normal (NN) interval (P = .004), standard deviation of the NN index (P < .001), high frequency component (P = .01), and low frequency component (P = .003). Those alternations were attributed to the slower heart rate and more decreased short-term autonomic fluctuation resulting from the administration of the bisoprolol transdermal patch, which were observed later than 12 hours after the drug initiation. No adverse events were noted throughout the study period.
The pattern of the autonomic modulation may vary depending on either a transdermal or oral administration even though an equivalent dose of bisoprolol is given.
比索洛尔透皮贴剂是一种新开发的β受体阻滞剂，旨在通过皮肤表面输送其药物成分。我们旨在使用心率变异性（HRV）比较比索洛尔透皮贴剂和富马酸比索洛尔片。
符合条件的高血压患者接受 2.5mg 富马酸比索洛尔片治疗 2 周，随后进行 24 小时动态心电图监测。然后将片剂更换为 4mg 比索洛尔透皮贴剂，在给药 2 周后重复进行动态心电图监测。两种药物均每日给药一次。终点是比索洛尔给药途径改变引起的 HRV 任何变化。
在接受研究（N=30）的患者中，药物转换前后 24 小时时域和频域 HRV 测量无差异。然而，转换显著改变了每小时 HRV 测量的时间过程曲线，包括平均正常到正常（NN）间隔（P=0.004）、NN 指数的标准差（P<0.001）、高频成分（P=0.01）和低频成分（P=0.003）。这些变化归因于比索洛尔透皮贴剂给药导致的心率更慢和短期自主神经波动更明显减少，这些变化在药物开始后 12 小时后才出现。在整个研究期间未观察到不良事件。
即使给予等效剂量的比索洛尔，自主调节模式也可能因透皮或口服给药而有所不同。
