Gold M S, Pottash A L, Sweeney D R, Kleber H D
Drug Alcohol Depend. 1980 Oct;6(4):201-8. doi: 10.1016/0376-8716(80)90323-3.
In a placebo-controlled, double-blind crossover trial, clonidine caused a marked and significant reduction of objective signs and subjective symptoms of opiate withdrawal in thirty hospitalized opiate addicts. In an open trial of clonidine in opiate withdrawal, clonidine was found to suppress opiate withdrawal signs and symptoms, allowing all of the patients to detoxify successfully from chronic opiate addiction. Clonidine was demonstrated to reverse and suppress the signs, symptoms, and effects associated with opiate withdrawal. These data support a release from chronic opiate-induced noradrenergic inhibition producing noradrenergic hyperactivity as the pathophysiological substrate for opiate withdrawal. Clonidine replaces opiate-mediated inhibition with alpha-2 mediated inhibition of noradrenergic nuclei.
在一项安慰剂对照、双盲交叉试验中，可乐定使30位住院阿片类成瘾者的阿片戒断客观体征及主观症状显著减轻。在一项可乐定用于阿片戒断的开放试验中，发现可乐定可抑制阿片戒断体征及症状，使所有患者成功戒除慢性阿片成瘾。已证明可乐定可逆转并抑制与阿片戒断相关的体征、症状及效应。这些数据支持慢性阿片诱导的去甲肾上腺素能抑制解除导致去甲肾上腺素能亢进这一观点，即阿片戒断的病理生理基础。可乐定以α-2介导的对去甲肾上腺素能核的抑制取代了阿片介导的抑制。
