Nicholls D P, Taggart A J, McCann J P, Bastain W, Shanks R G
Royal Victoria Hospital, Belfast, Northern Ireland.
Br J Clin Pharmacol. 1989 Dec;28(6):718-21. doi: 10.1111/j.1365-2125.1989.tb03566.x.
The pharmacokinetics of xamoterol, a beta 1-adrenoceptor partial agonist, have been studied in patients with liver disease and a group of age- and sex-matched normal controls. No significant differences were observed after the oral administration of xamoterol 200 mg. The low bioavailability of xamoterol was confirmed (6.1% in patients, 6.9% in controls). After i.v. xamoterol 0.2 mg kg-1, no significant differences between the groups were observed. A small increase in the terminal plasma elimination half-life (t1/2) was observed in patients when compared with controls (15.3 +/- 6.4 vs 8.4 +/- 2.8 h, mean +/- s.d., P = 0.08). Renal clearance accounted for about 50% of total clearance in patients and about 30% in controls. It is suggested that in patients with heart failure, hepatic dysfunction would probably not influence xamoterol disposition.
已对β1肾上腺素能受体部分激动剂扎莫特罗的药代动力学在肝病患者及一组年龄和性别匹配的正常对照者中进行了研究。口服200 mg扎莫特罗后未观察到显著差异。扎莫特罗的低生物利用度得到了证实(患者为6.1%,对照者为6.9%)。静脉注射0.2 mg/kg扎莫特罗后,两组之间未观察到显著差异。与对照者相比,患者的终末血浆消除半衰期(t1/2)有小幅增加(分别为15.3±6.4小时和8.4±2.8小时,平均值±标准差,P = 0.08)。患者的肾清除率约占总清除率的50%,对照者约为30%。提示在心力衰竭患者中,肝功能障碍可能不会影响扎莫特罗的处置。