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Treatment of cocaine craving with as-needed nalmefene, a partial. opioid receptor agonist: first clinical experience

机译:可卡因渴望用纳美芬治疗,一部分治疗。阿片受体激动剂:首次临床经验

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摘要

The treatment of cocaine dependence is difficult as no approved pharmacotherapy is available as yet. However, in preclinical and clinical trials, a variety of compounds were tested for suitability as inhibitors of craving for and relapse into the use of cocaine, among these antidepressants, antiepileptics, dopamine agonists, disulfiram, and naltrexone. Nalmefene, a structural derivative of naltrexone, shares with its parent compound approval (granted by the European Medical Agency in 2013) as a medication for the treatment of alcohol addiction in the European Union. It differs from naltrexone by a higher affinity for the opioid-receptors and a partial agonistic affinity to the opioid-receptors. It should be noted that patients addicted to cocaine show a considerable increase in receptors in the nucleus accumbens. This report describes the case of an abstinent cocaine-addicted patient regularly afflicted with cravings for cocaine. The patient took as-needed nalmefene for 5 months whenever she developed a craving for cocaine. For most of these interventions, the patient reported an abatement of craving and could avoid relapsing into cocaine consumption. This effect may be accounted for by nalmefene acting, other than naltrexone, as a partial agonist of the opioid-receptors. Therefore, nalmefene might be a promising new option in the pharmacological repertoire for the treatment of cocaine addiction.
机译:可卡因依赖的治疗很困难,因为目前尚无批准的药物疗法。但是,在临床前和临床试验中,测试了多种化合物的适用性,作为这些抗抑郁药,抗癫痫药,多巴胺激动剂,双硫仑和纳曲酮中对可卡因的渴望和复发的抑制剂。纳曲酮的结构性衍生物纳美芬已获得其母体化合物的批准(2013年获得欧洲医学署的批准),作为欧盟治疗酒精成瘾的药物。它与纳曲酮的不同之处在于对阿片受体的亲和力更高,对阿片受体的激动剂亲和力更高。应当指出,对可卡因上瘾的患者在伏隔核中的受体显示出明显增加。该报告描述了一名经常上瘾的可卡因成瘾患者,经常渴望获得可卡因。每当患者对可卡因产生渴望时,就按需服用纳美芬5个月。对于大多数这些干预措施,患者报告称其渴望有所减轻,并且可以避免再次食用可卡因。除了纳曲酮以外,纳美芬作为阿片样物质受体的部分激动剂可能是造成这种效应的原因。因此,纳美芬可能是治疗可卡因成瘾的药理学方法中有希望的新选择。

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