Brunnée T, Engelstätter R, Steinijans V W, Kunkel G
Dept of Clinical Immunology, Free University, Berlin, Germany.
Eur Respir J. 1992 Sep;5(8):982-5.
Zardaverine is a newly developed selective phosphodiesterase III and IV inhibitor. This study investigates the bronchodilatory properties of zardaverine, administered by inhalation. Twelve patients with reversible bronchial obstruction (increase in forced expiratory volume in one second (change FEV1 % predicted) at least 15% after 200 micrograms salbutamol, median age 31 yrs, range 21-54 years) entered the double-blind, crossover study. Four puffs of either zardaverine (total dose 6 mg) or placebo were inhaled at 15 min intervals. Pulmonary function (specific airway conductance (sGaw) and FEV1 was measured by body plethysmography at regular intervals (5 and 12 min after each puff and, in addition, 30, 60, 120, 180 and 240 min after the last puff). Compared to placebo, sGaw and FEV1 increased significantly during the first hour of repeated inhalations, but not during the entire observation period of almost 5 h. The maximum mean difference between zardaverine and placebo for FEV1 was 0.3 l or 12% and occurred approximately 1 h after inhalation of the first puff. In seven patients FEV1 increased by > 15%. The duration of action varied considerably between patients. Three patients complained of side-effects (headache, drowsiness, vertigo, nausea), and one of these dropped out of the study due to vomiting. We conclude that inhalational administration of zardaverine has a modest and short-lasting bronchodilating activity.
扎达维林是一种新开发的选择性磷酸二酯酶III和IV抑制剂。本研究调查了吸入给药的扎达维林的支气管扩张特性。12例可逆性支气管阻塞患者（吸入200微克沙丁胺醇后一秒用力呼气量增加（预测FEV1变化百分比）至少15%，中位年龄31岁，范围21 - 54岁）进入双盲交叉研究。每隔15分钟吸入4喷扎达维林（总剂量6毫克）或安慰剂。定期（每次喷药后5分钟和12分钟，此外，最后一次喷药后30、60、120、180和240分钟）通过体容积描记法测量肺功能（比气道传导率（sGaw）和FEV1）。与安慰剂相比，重复吸入的第一小时内sGaw和FEV1显著增加，但在近5小时的整个观察期内未增加。扎达维林和安慰剂之间FEV1的最大平均差异为0.3升或12%，在吸入第一喷后约1小时出现。7例患者的FEV1增加> 15%。患者之间的作用持续时间差异很大。3例患者抱怨有副作用（头痛、嗜睡、眩晕、恶心），其中1例因呕吐退出研究。我们得出结论，吸入扎达维林具有适度且持续时间短的支气管扩张活性。
