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阿扑吗啡:关于勃起功能障碍和打哈欠的临床研究。

Apomorphine: clinical studies on erectile impotence and yawning.

作者信息

Lal S, Tesfaye Y, Thavundayil J X, Thompson T R, Kiely M E, Nair N P, Grassino A, Dubrovsky B

机构信息

Douglas Hospital Research Centre, Montreal General Hospital, Quebec, Canada.

出版信息

Prog Neuropsychopharmacol Biol Psychiatry. 1989;13(3-4):329-39. doi: 10.1016/0278-5846(89)90122-x.

Abstract
  1. The erectile response to the short-acting dopamine (DA) receptor agonist, apomorphine (Apo) HCl (0.25, 0.5, 0.75 and 1.0 mg sc), and placebo was evaluated in 28 impotent patients and penile circumference monitored using a mercury strain gauge and strip chart recording. 2. A full erection (increment in penile circumference greater than 2 cm and lasting at least one minute) occurred in 17 patients with Apo; no erection developed after placebo. An erection occurred in 6/8 patients with impaired glucose tolerance, 2/6 patients with diabetes mellitus and in both patients on lithium. 3. Nine patients who responded to Apo were treated in an open trial with bromocriptine; 6 reported improvement in potency. 4. Impairment in DA function may play a role in idiopathic impotence and in impotence associated with impaired glucose tolerance and diabetes mellitus. 5. An erectile response to Apo may predict therapeutic response to bromocriptine or other long acting dopaminergic agents. 6. Lithium, which inhibits DA-sensitive adenylate cyclase, does not prevent Apo-induced erections. This provides further support indicating that Apo induces erections by an effect on D2 receptors. 7. The yawning response to placebo and four doses of Apo HC1 (3.5, 5.0, 7.0, and 10.5 ug/kg sc) was evaluated in five normal men using a polygraphic technique. The yawning response was also assessed in normal young (less than 30 yrs; N = 16) and elderly (greater than 60 yrs; N = 12) volunteers. 8. Under experimental conditions of study, placebo induced spontaneous yawning. This was antagonized by 3.5 and 5.0 ug/kg Apo HC1 but increased by 7.0 ug/kg Apo HC1. These observations are compatible with the view that Apo HC1 in doses of 3.5-5.0 ug/kg stimulates presynaptic DA receptors whereas 7.0 ug/kg stimulates postsynaptic DA receptors. 9. Spontaneous and Apo-induced yawning were significantly decreased in the elderly which suggests that D2 receptor function declines with normal aging.
摘要
  1. 在28例阳痿患者中评估了对短效多巴胺(DA)受体激动剂阿扑吗啡盐酸盐(0.25、0.5、0.75和1.0mg皮下注射)和安慰剂的勃起反应,并使用水银应变仪和带状图表记录监测阴茎周长。

  2. 17例使用阿扑吗啡的患者出现完全勃起(阴茎周长增加大于2cm且持续至少1分钟);安慰剂后未出现勃起。6/8例糖耐量受损患者、2/6例糖尿病患者以及2例服用锂盐的患者出现勃起。

  3. 9例对阿扑吗啡有反应的患者在开放试验中接受了溴隐亭治疗;6例报告性功能有改善。

  4. DA功能受损可能在特发性阳痿以及与糖耐量受损和糖尿病相关的阳痿中起作用。

  5. 对阿扑吗啡的勃起反应可能预测对溴隐亭或其他长效多巴胺能药物的治疗反应。

  6. 抑制DA敏感腺苷酸环化酶的锂并不阻止阿扑吗啡诱导的勃起。这进一步支持了阿扑吗啡通过对D2受体的作用诱导勃起的观点。

  7. 使用多导记录技术在5名正常男性中评估了对安慰剂和四剂阿扑吗啡盐酸盐(3.5、5.0、7.0和10.5μg/kg皮下注射)的打哈欠反应。在正常年轻(小于30岁;N = 16)和老年(大于60岁;N = 12)志愿者中也评估了打哈欠反应。

  8. 在研究的实验条件下,安慰剂诱导自发打哈欠。这被3.5和5.0μg/kg阿扑吗啡盐酸盐拮抗,但被7.0μg/kg阿扑吗啡盐酸盐增强。这些观察结果与以下观点一致,即3.5 - 5.0μg/kg剂量的阿扑吗啡盐酸盐刺激突触前DA受体,而7.0μg/kg刺激突触后DA受体。

  9. 老年人的自发和阿扑吗啡诱导的打哈欠明显减少,这表明D2受体功能随着正常衰老而下降。

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