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钙通道阻滞剂加洛帕米对乙酰甲胆碱诱导的支气管收缩的作用持续时间。

Duration of effect of gallopamil, a calcium channel blocker, on methacholine-induced bronchoconstriction.

作者信息

Massey K L, Harman E, Hendeles L

机构信息

Department of Clinical Pharmacy, University of Tennessee, Memphis 38163.

出版信息

Pharmacotherapy. 1988;8(3):189-92. doi: 10.1002/j.1875-9114.1988.tb04073.x.

Abstract

We previously demonstrated a modest but significant protective effect of inhaled gallopamil (D600), the methoxy derivative of verapamil, against methacholine-induced bronchoconstriction; however, the duration of the protective effect of this and other calcium channel blockers is unknown. We therefore evaluated the duration of this protective effect in 15 asthmatic subjects in a prospective, placebo-controlled trial. Methacholine challenges (Cockcroft method) were performed 2 hours before and 30 minutes after the administration of placebo, and 1 mg and 10 mg of inhaled gallopamil. Gallopamil did not alter resting airway caliber, but significantly increased the concentration of methacholine required to decrease the FEV1 20% 30 minutes after the dose. Results with both the 10-mg and 1-mg doses were significantly different from placebo, but not from each other. The duration of this protective effect was transient in the group as a whole; the mean drug activity ratios were not significantly different with this sample 2.5 hours after the dose. Thus the short duration of effect limits the potential clinical usefulness of gallopamil in suppressing the signs and symptoms of chronic asthma.

摘要

我们之前证明了吸入维拉帕米的甲氧基衍生物加洛帕米(D600)对乙酰甲胆碱诱发的支气管收缩具有适度但显著的保护作用;然而,这种及其他钙通道阻滞剂的保护作用持续时间尚不清楚。因此,我们在一项前瞻性、安慰剂对照试验中评估了15名哮喘患者中这种保护作用的持续时间。在给予安慰剂以及1毫克和10毫克吸入性加洛帕米之前2小时和之后30分钟进行乙酰甲胆碱激发试验(科克罗夫特方法)。加洛帕米并未改变静息气道口径,但显著增加了给药后30分钟使第一秒用力呼气容积(FEV1)降低20%所需的乙酰甲胆碱浓度。10毫克和1毫克剂量的结果均与安慰剂有显著差异,但两者之间无显著差异。总体而言,该组中这种保护作用的持续时间是短暂的;给药后2.5小时,该样本的平均药物活性比率无显著差异。因此,作用持续时间短限制了加洛帕米在抑制慢性哮喘体征和症状方面的潜在临床应用价值。

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