Jansen W, Seibel K, Bühling M
Arzneimittelforschung. 1985;35(7):1083-5.
The influence of equimolar oral doses of etilefrine pivalate (K 30 052, Ep) and etilefrine on blood pressure of patients suffering from orthostatic dysregulation was compared. Both drugs augmented the systolic blood pressure in both, the upright and horizontal body posture. Diastolic blood pressure was not influenced. The resulting increase in blood pressure amplitude points to an augmentation of cardiac stroke volume. Ep in equimolar doses was nearly twice as active as etilefrine. This result is in line with the hypothesis that acylation of etilefrine with pivalinic acid inhibits the first-pass inactivation nearly completely.
比较了等摩尔口服剂量的匹伐依替福林(K 30 052,Ep)和依替福林对体位调节异常患者血压的影响。两种药物均使直立和卧位时的收缩压升高。舒张压未受影响。血压幅度的升高表明心搏量增加。等摩尔剂量的Ep活性几乎是依替福林的两倍。这一结果符合以下假设:依替福林与新戊酸的酰化作用几乎完全抑制了首过灭活。