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年龄对两种维拉帕米制剂药效学和药代动力学的影响。

The effects of age on the pharmacodynamics and pharmacokinetics of two formulations of verapamil.

作者信息

Hosie J, Hosie G, Meredith P A

机构信息

The Surgery, Stobhill Hospital, Glasgow, Scotland.

出版信息

J Cardiovasc Pharmacol. 1989;13 Suppl 4:S60-2. doi: 10.1097/00005344-198900134-00017.

DOI:10.1097/00005344-198900134-00017
PMID:2475690
Abstract

The present study, undertaken in general practice, was designed to evaluate the effects of age on the pharmacodynamics and pharmacokinetics of a conventional and a slow-release formulation (Securon SR) of verapamil. Two groups of 12 patients with essential hypertension were treated in an open, randomized, crossover study. One group was younger than 65 years, mean 58 (range 50-64 years) and the other was 65 years and older, mean 72 (range 66-77 years). The patients were titrated through three steps with the two different formulations to efficacy or to maximal dosage. During a 4-week drug-free run-in period the mean blood pressures were 167 +/- 14/103 +/- 4, 168 +/- 18/105 +/- 6, and 168 +/- 18/105 +/- 5 mm Hg at 0, 2, and 4 weeks, respectively, for the whole group. The final blood pressure at control showed a fall with sustained-release verapamil for systolic blood pressure (SBP) and diastolic blood pressure (DBP) of 15 +/- 16 and 17 +/- 5 mm Hg for the younger group and 14 +/- 16 and 14 +/- 6 mm Hg for the older group. For the conventional formulation the falls of SBP and DBP were 14 +/- 18 and 18 +/- 8 mm Hg for the younger group and 19 +/- 16 and 13 +/- 9 mm Hg for the older group. There were no significant differences between the responses to the two formulations nor between the two age groups. The pharmacokinetics of both formulations were investigated at steady state and no significant effects of age were observed. However, there were significant differences between the time-concentration profiles for the formulations. These findings suggest that there are no significant effects of age on the pharmacodynamics and pharmacokinetics of verapamil.

摘要

本研究在全科医疗中开展,旨在评估年龄对维拉帕米常规制剂和缓释制剂(Securon SR)药效学和药代动力学的影响。在一项开放、随机、交叉研究中,对两组各12例原发性高血压患者进行了治疗。一组年龄小于65岁,平均58岁(范围50 - 64岁),另一组年龄在65岁及以上,平均72岁(范围66 - 77岁)。患者使用两种不同制剂分三步滴定至有效剂量或最大剂量。在为期4周的无药导入期,全组在0、2和4周时的平均血压分别为167±14/103±4、168±18/105±6和168±18/105±5 mmHg。对照时的最终血压显示,年轻组使用缓释维拉帕米后收缩压(SBP)和舒张压(DBP)分别下降15±16和17±5 mmHg,老年组分别下降14±16和14±6 mmHg。对于常规制剂,年轻组SBP和DBP的下降幅度分别为14±18和18±8 mmHg,老年组分别为19±16和13±9 mmHg。两种制剂的反应之间以及两个年龄组之间均无显著差异。在稳态下研究了两种制剂的药代动力学,未观察到年龄的显著影响。然而,两种制剂的时间 - 浓度曲线存在显著差异。这些发现表明,年龄对维拉帕米的药效学和药代动力学没有显著影响。

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引用本文的文献

1
Verapamil. An updated review of its pharmacodynamic and pharmacokinetic properties, and therapeutic use in hypertension.维拉帕米。对其药效学和药代动力学特性以及在高血压治疗中的应用的最新综述。
Drugs. 1989 Jul;38(1):19-76. doi: 10.2165/00003495-198938010-00003.