Comparison of the oral effectiveness of etilefrine pivalate and etilefrine in a long-term trial in man.
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.
Jansen
W
W
Seibel
K
K
Bühling
M
M
D000368:Aged; D000959:Antihypertensive Agents / Q000009:adverse effects / Q000627:therapeutic use*; D001794:Blood Pressure / Q000187:drug effects; D002986:Clinical Trials as Topic; D004311:Double-Blind Method; D005039:Etilefrine / Q000009:adverse effects / Q000031:analogs & derivatives / Q000627:therapeutic use*; D005260:Female; D006801:Humans; D006973:Hypertension / Q000188:drug therapy*; D008297:Male; D008875:Middle Aged; D010656:Phenylephrine / Q000031:analogs & derivatives*; D011897:Random Allocation; D013997:Time Factors
D000959:Antihypertensive Agents; D010656:Phenylephrine; C046842:etilefrine pivalate; D005039:Etilefrine