Dominic J, McAllister R G, Kuo C S, Reddy C P, Surawicz B
Clin Pharmacol Ther. 1979 Dec;26(6):710-4. doi: 10.1002/cpt1979266710.
The acute effect of verapamil on the ventricular rate in atrial fibrillation and flutter was studied in 15 patients, 13 of whom had heart rate inadequately controlled with digitalis. Plasma concentrations were measured 5 and 10 min after intravenous doses of 0.075 mg/kg and 0.15 mg/kg verapamil. In 9 patients who were clinically compensated, the 0.075-mg dose alone decreased the ventricular rate to under 100/min (responders); in the remaining 6, who had acute congestive heart failure manifested by orthopnea, rales, and pulmonary congestion, ventricular rates were above 100/min after the 0.075-mg dose (nonresponders). The 6 nonresponders received the 0.15-mg dose 30 min later. In all, the response was greater when plasma drug concentration rose after the high dose, although the rate decrease was smaller than in the 9 compensated patients who received the low dose. These results can be explained by assuming an antagonism of the verapamil effect by sympathetic stimulation in nonresponders.
对15例患者研究了维拉帕米对房颤和房扑时心室率的急性效应,其中13例患者使用洋地黄后心率控制不佳。静脉注射0.075mg/kg和0.15mg/kg维拉帕米后5分钟和10分钟测量血浆浓度。在9例临床症状得到缓解的患者中,仅0.075mg剂量就使心室率降至100次/分钟以下(有反应者);其余6例患者表现为端坐呼吸、啰音和肺充血等急性充血性心力衰竭症状,0.075mg剂量后心室率高于100次/分钟(无反应者)。30分钟后,6例无反应者接受了0.15mg剂量。总体而言,高剂量后血浆药物浓度升高时反应更大,尽管心率下降幅度小于接受低剂量的9例症状缓解患者。这些结果可以通过假设无反应者中交感神经刺激对维拉帕米效应的拮抗作用来解释。