Sofuoglu Mehmet, Kosten Thomas R
School of Medicine, Department of Psychiatry and VA Connecticut Healthcare System, Yale University, 950 Campbell Ave., Bldg 36/116A4, West Haven, CT 06516, USA.
CNS Drugs. 2005;19(1):13-25. doi: 10.2165/00023210-200519010-00002.
Cocaine addiction continues to be an important public health problem with over 1.7 million users in the US alone. Although there are no approved pharmacotherapies for cocaine addiction, a number of medications have been tested with some promising results. In this review, we summarise some of the emerging targets for cocaine pharmacotherapy including dopaminergic and GABA medications, adrenoceptor antagonists, vasodilators and immunotherapies. The brain dopamine system plays a significant role in mediating the rewarding effects of cocaine. Among dopaminergic agents tested for cocaine pharmacotherapy, disulfiram has decreased cocaine use in a number of studies. Amantadine, another medication with dopaminergic effects, may also be effective in cocaine users with high withdrawal severity. GABA is the main inhibitory neurotransmitter in the brain, and accumulating evidence suggests that the GABA system modulates the dopaminergic system and cocaine effects. Two anticonvulsant medications with GABAergic effects, tiagabine and topiramate, have yielded positive findings in clinical trials. Baclofen, a GABA(B) receptor agonist, is also promising, especially in those with more severe cocaine use. Some of the physiological and behavioural effects of cocaine are mediated by activation of the adrenergic system. In cocaine users, propranolol, a beta-adrenoceptor antagonist, had promising effects in individuals with more severe cocaine withdrawal symptoms. Cerebral vasodilators are another potential target for cocaine pharmacotherapy. Cocaine users have reduced cerebral blood flow and cortical perfusion deficits. Treatment with the vasodilators amiloride or isradipine has reduced perfusion abnormalities found in cocaine users. The functional significance of these improvements needs to be further investigated. All these proposed pharmacotherapies for cocaine addiction act on neural pathways. In contrast, immunotherapies for cocaine addiction are based on the blockade of cocaine effects peripherally, and as a result, prevent or at least slow the entry of cocaine into the brain. A cocaine vaccine is another promising treatment for cocaine addiction. The efficacy of this vaccine for relapse prevention is under investigation. Many initial promising findings need to be replicated in larger, controlled clinical trials.
可卡因成瘾仍然是一个重要的公共卫生问题,仅在美国就有超过170万使用者。尽管目前尚无获批用于治疗可卡因成瘾的药物疗法,但已有多种药物经过测试并取得了一些有前景的结果。在本综述中,我们总结了可卡因药物治疗中一些新出现的靶点,包括多巴胺能和GABA类药物、肾上腺素能受体拮抗剂、血管扩张剂和免疫疗法。脑多巴胺系统在介导可卡因的奖赏效应中起重要作用。在用于可卡因药物治疗测试的多巴胺能药物中,双硫仑在多项研究中减少了可卡因的使用。金刚烷胺是另一种具有多巴胺能效应的药物,对戒断症状严重的可卡因使用者可能也有效。GABA是大脑中的主要抑制性神经递质,越来越多的证据表明,GABA系统调节多巴胺能系统和可卡因效应。两种具有GABA能效应的抗惊厥药物,噻加宾和托吡酯,在临床试验中取得了阳性结果。巴氯芬是一种GABA(B)受体激动剂,也很有前景,尤其对那些可卡因使用更严重的患者。可卡因的一些生理和行为效应是由肾上腺素能系统的激活介导的。在可卡因使用者中,β肾上腺素能受体拮抗剂普萘洛尔对戒断症状更严重的个体有显著效果。脑血管扩张剂是可卡因药物治疗的另一个潜在靶点。可卡因使用者的脑血流量减少,存在皮质灌注缺陷。使用血管扩张剂氨氯吡咪或伊拉地平治疗可减少可卡因使用者中发现的灌注异常。这些改善的功能意义有待进一步研究。所有这些针对可卡因成瘾提出的药物疗法都作用于神经通路。相比之下,可卡因成瘾的免疫疗法是基于在外周阻断可卡因的作用,从而预防或至少减缓可卡因进入大脑。可卡因疫苗是另一种有前景的可卡因成瘾治疗方法。这种疫苗预防复发的疗效正在研究中。许多初步的有前景的发现需要在更大规模的对照临床试验中重复验证。