Schwartz J B, Keefe D L, Kirsten E, Kates R E, Harrison D C
Am Heart J. 1982 Aug;104(2 Pt 1):198-203. doi: 10.1016/0002-8703(82)90192-2.
The elimination of verapamil and its n-demethylated metabolite, norverapamil, was studied in nine patients with chronic atrial fibrillation after the first oral verapamil dose and during chronic oral verapamil administration. Significant increases (p less than 0.01) were seen in the elimination half-lives (t 1/2's) of both verapamil (6.4 +/- 3.5 to 12 +/- 5 hours, mean +/- SD) and norverapamil (10.3 +/- 6 to 16.5 +/- 7 hours) during chronic oral verapamil administration. These pharmacokinetic observations have important clinical implications for the rational long-term administration of this agent. Once steady-state serum concentrations have been achieved during chronic verapamil administration, verapamil doses should be given at less frequent intervals or in smaller doses in order to produce the desired serum concentration and therapeutic response and to minimize unwanted or toxic drug effects.
在9例慢性房颤患者中,研究了首次口服维拉帕米剂量后及慢性口服维拉帕米期间维拉帕米及其N - 去甲基代谢产物去甲维拉帕米的消除情况。慢性口服维拉帕米期间,维拉帕米(6.4±3.5至12±5小时,均值±标准差)和去甲维拉帕米(10.3±6至16.5±7小时)的消除半衰期(t1/2)均显著增加(p<0.01)。这些药代动力学观察结果对于合理长期使用该药物具有重要临床意义。在慢性维拉帕米给药期间一旦达到稳态血清浓度,应减少维拉帕米给药的频率或降低剂量,以产生所需的血清浓度和治疗反应,并尽量减少不良或毒性药物效应。