Perpiñá M, Cortijo J, Sanz C, Esplugues J, Morcillo E J
Department of Pharmacology, Faculty of Medicine, University of Valencia, Spain.
Bull Eur Physiopathol Respir. 1987 May-Jun;23(3):255-60.
When considering the therapeutic potential of calcium antagonists in asthma, attention should be paid to the existence of marked differences among these compounds. In the present study, we have compared the effect of verapamil, diltiazem, nifedipine and trifluoperazine on contractions generated by different mechanisms (CaCl2 acting on K+ depolarized preparation, depolarization by KCl, receptor activation by acetylcholine) in lung parenchyma strips isolated from control and actively sensitized guinea-pigs. It was found that verapamil and diltiazem need higher concentrations in the sensitized specimens to elicit the same degree of inhibition obtained in controls. The reverse was found for trifluoperazine while nifedipine had an intermediate position. In conclusion, acute sensitization reveals differences between the various groups of calcium antagonists in their ability to influence agonist-induced lung parenchyma strip contraction, a finding that suggests that these drugs may also behave diversely in the clinical setting.
在考虑钙拮抗剂对哮喘的治疗潜力时，应注意这些化合物之间存在显著差异。在本研究中，我们比较了维拉帕米、地尔硫䓬、硝苯地平和三氟拉嗪对从对照和主动致敏豚鼠分离的肺实质条带中不同机制（氯化钙作用于钾离子去极化制剂、氯化钾去极化、乙酰胆碱受体激活）产生的收缩的影响。结果发现，在致敏标本中，维拉帕米和地尔硫䓬需要更高的浓度才能产生与对照中相同程度的抑制作用。三氟拉嗪则相反，而硝苯地平处于中间位置。总之，急性致敏揭示了不同组钙拮抗剂在影响激动剂诱导的肺实质条带收缩能力方面的差异，这一发现表明这些药物在临床环境中可能也表现各异。
