Nalmefene causes greater hypothalamic-pituitary-adrenal axis activation than naloxone in normal volunteers: implications for the treatment of alcoholism.
作者： James H. Schluger , Ann Ho , Lisa Borg , Margaret Porter , Swapnil Maniar
DOI: 10.1111/J.1530-0277.1998.TB03931.X
关键词: Opioid antagonist 、 Nalmefene 、 Internal medicine 、 Naltrexone 、 Endogenous opioid 、 (+)-Naloxone 、 Hypothalamic–pituitary–adrenal axis 、 Opioid 、 Narcotic antagonist 、 Pharmacology 、 Endocrinology 、 Medicine
摘要: Among other actions, opioid antagonists modulate the control endogenous opioids exert on hypothalamic-pituitary-adrenal (HPA) axis. Naloxone, nalmefene, and naltrexone are approved for use in man primarily mu-opioid selective. Naltrexone nalmefene have been demonstrated to be useful treatment of alcoholism. Compared with naloxone, has a longer half-life, is more potent at mu-receptor, higher affinity kappa- delta-opioid receptors. We conducted an inpatient study comparing effects 10 30 mg doses intravenous naloxone normal, nonsubstance nor alcohol-abusing, volunteers. Significant increases ACTH cortisol were observed after both antagonists, without apparent dose-response relationship; however, resulted greater HPA axis activation than either dose (ACTH: p <0.005). These results indicate that delta-opioids may play important roles regulation axis; as probe explore physiology pharmacotherapeutic agent.
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