Yoshikawa M, Hirai S, Aizawa T, Kuroiwa Y, Goto F, Sofue I, Toyokura Y, Yamamura H, Iwasaki Y
J Am Geriatr Soc. 1983 Jan;31(1):1-7. doi: 10.1111/j.1532-5415.1983.tb06280.x.
Basic pharmacologic evidences have suggested the effects of dihydroergotoxine mesylate (DEM) on neurotransmitters. In its clinical use, however, various therapeutic effects and side effects are observed when the dose is changed, because of the complexity of this compound and the delicate mechanism of neurotransmitters in the brain, especially when modified by aging and vascular lesions. In order to investigate the optimal dose, a double-blind study in 550 patients with cerebrovascular disorders was carried out at 68 centers under observation by experienced specialists. Dihydroergotoxine mesylate in sublingual tablets, 3 mg daily, and in oral tablets, 6 mg daily, respectively, was given for 12 weeks, and therapeutic effects at those doses were compared by a double-blind method. In utility ratings for subjective and psychiatric symptoms, the effects in the oral tablet group at a daily dose of 6 mg were significantly superior to those in sublingual tablet group at a daily dose of 3 mg. There was no significant difference between those two groups in the comparison of side effects. These results show that the daily oral administration of 6 mg of DEM is more suitable for the improvement of subjective and psychiatric symptoms due to cerebrovascular disorders than is the daily sublingual administration of 3 mg. These results suggest that, despite much complexity in the neurohumoral transmitter mechanism in the brain, relatively simple dose-dependent efficacy of the drug in the range of the therapeutic doses was confirmed for many subjective and psychiatric symptoms of patients with cerebrovascular disorders.
基础药理学证据表明甲磺酸双氢麦角毒碱（DEM）对神经递质有作用。然而，在其临床应用中，由于该化合物的复杂性以及大脑中神经递质的精细机制，尤其是受到衰老和血管病变影响时，改变剂量会观察到各种治疗效果和副作用。为了研究最佳剂量，在68个中心由经验丰富的专家对550例脑血管疾病患者进行了一项双盲研究。分别给予舌下片甲磺酸双氢麦角毒碱每日3毫克和口服片每日6毫克，持续12周，并通过双盲法比较这些剂量的治疗效果。在主观和精神症状的效用评级方面，每日剂量6毫克的口服片组效果显著优于每日剂量3毫克的舌下片组。两组在副作用比较方面无显著差异。这些结果表明，每日口服6毫克DEM比每日舌下含服3毫克更适合改善脑血管疾病引起的主观和精神症状。这些结果表明，尽管大脑中神经体液传递机制非常复杂，但在治疗剂量范围内，该药物对脑血管疾病患者的许多主观和精神症状具有相对简单的剂量依赖性疗效。
