Mustafa Seham, Abdulraheem Abdulkareem, Alsughayer Abdulhakeem
Department of Pharmaceutical Sciences, College of Health Sciences, The Public Authority for Applied Education & Training, Safat, Kuwait.
J Pharmacol Sci. 2008 Apr;106(4):609-14. doi: 10.1254/jphs.fp0072335.
Verapamil, a Ca(2+) entry blocker, can induce bronchorelaxation and bronchoconstriction. The mechanism of verapamil-induced bronchoconstriction is poorly understood. The present study determines the direct effect of verapamil on smooth muscle of isolated ovine airways and analyzes the mechanisms involved. Isolated tracheal strips were suspended in organ baths containing Krebs solution for isometric tension recording. Tissue responses to verapamil as assessed by basal tone were examined in the presence or absence of epithelium. The effects of verapamil on carbachol and cooling-induced contraction were also recorded. Measurement of unidirectional fluxes was carried out using (45)Ca(2+) in the absence or presence of verapamil. Verapamil induced contractions of basal tracheal smooth muscle that were proportional to its concentrations. Removal of epithelium did not affect the verapamil contractile effect. Verapamil-induced contractions were abolished in Ca(2+)-free Krebs solution containing 2 mM EGTA. Verapamil increased the (45)Ca(2+) influx into the tracheal smooth muscle. It caused relaxation of the muscle tone induced by carbachol or KCl, but it potentiated the effect of cooling-induced contraction. Verapamil induced Ca(2+) influx that may lead to bronchoconstriction. These results proved that verapamil may worsen bronchoconstriction; therefore verapamil should be used with caution in asthmatic individuals.
维拉帕米,一种钙通道阻滞剂,可诱发支气管舒张和支气管收缩。维拉帕米诱发支气管收缩的机制尚不清楚。本研究确定了维拉帕米对离体绵羊气道平滑肌的直接作用,并分析了其中涉及的机制。将离体气管条悬挂于含有 Krebs 溶液的器官浴槽中以记录等长张力。在有或无上皮的情况下,检测以基础张力评估的组织对维拉帕米的反应。还记录了维拉帕米对卡巴胆碱和冷却诱导收缩的影响。在有或无维拉帕米的情况下,使用(45)Ca(2+)进行单向通量测量。维拉帕米诱导基础气管平滑肌收缩,且收缩程度与其浓度成正比。去除上皮并不影响维拉帕米的收缩作用。在含有 2 mM EGTA 的无钙 Krebs 溶液中,维拉帕米诱导的收缩被消除。维拉帕米增加了(45)Ca(2+)流入气管平滑肌。它导致由卡巴胆碱或氯化钾诱导的肌张力松弛,但增强了冷却诱导收缩的作用。维拉帕米诱导的 Ca(2+)内流可能导致支气管收缩。这些结果证明维拉帕米可能会加重支气管收缩;因此,维拉帕米在哮喘患者中应谨慎使用。