Aellig W H
Cardiology. 1976;61 suppl 1:302-8. doi: 10.1159/000169823.
The venoconstrictor effect of dihydroergotamine in man was demonstrated by Rieckert and Pauschinger in 1967. In a study on the influence of local infusions of dihydroergotamine into superficial hand veins in man we found a direct venoconstrictor effect of the drug. In further studies the effects of dihydroergotamine were compared with those of other dihydrogenated and non-dihydrogenated ergot alkaloids and a dose-dependent venoconstrictor effect was observed after local infusion of dihydroergotamine, dihydroergostine, dihydroergovaline, ergotamine and methysergide into superficial hand veins in man. Dihydroergotamine was weight for weight somewhat less active than ergotamine. But as Mellander and Nordenfelt have shown that dihydroergotamine elicits only a weak effect on resistance vessels, this drug seems for the treatment of orthostatic hypotension to be preferable to ergotamine for which Owen and Stürmer have demonstrated a marked constriction of resistance vessels in the skin. Experiment with dihydroergotamine showed that the venoconstriction in these human veins is mainly due to alpha-adrenoceptor stimulation. As in the treatment of orthostatic hypotension drugs are usually given in oral form, the activity of dihydroergotamine was also investigated after oral administration and the venoconstrictor activity confirmed.
1967年,里克特和保辛格证实了双氢麦角胺对人体的静脉收缩作用。在一项关于向人体手部浅表静脉局部输注双氢麦角胺的影响的研究中,我们发现了该药物的直接静脉收缩作用。在进一步的研究中,将双氢麦角胺的作用与其他氢化和非氢化麦角生物碱的作用进行了比较,在向人体手部浅表静脉局部输注双氢麦角胺、双氢麦角异胺、双氢麦角缬碱、麦角胺和甲基麦角新碱后,观察到了剂量依赖性的静脉收缩作用。按重量计算,双氢麦角胺的活性略低于麦角胺。但正如梅兰德和诺登费尔特所表明的,双氢麦角胺对阻力血管仅产生微弱作用,因此对于直立性低血压的治疗,这种药物似乎比麦角胺更可取,欧文和施图默已证明麦角胺会使皮肤中的阻力血管明显收缩。对双氢麦角胺的实验表明,这些人体静脉中的静脉收缩主要是由于α-肾上腺素能受体刺激。由于在直立性低血压的治疗中,药物通常以口服形式给药,因此还研究了口服双氢麦角胺后的活性,并证实了其静脉收缩活性。