首页> 外国专利> ARTIFICIAL REPRODUCTION OF PHARMACEUTICAL CONDITIONS OF DEPENDENCY TO TOBACCO AND OTHER ADDICTIVE DRUGS (OPIACEA, PSYCHOSTIMULANTS, ALCOHOL) BY COMBINATION OF NICOTINE AND A LIGAND (AGONIST OR 5 ANTAGONIST) OF 5-HT1A RECEPTORS

ARTIFICIAL REPRODUCTION OF PHARMACEUTICAL CONDITIONS OF DEPENDENCY TO TOBACCO AND OTHER ADDICTIVE DRUGS (OPIACEA, PSYCHOSTIMULANTS, ALCOHOL) BY COMBINATION OF NICOTINE AND A LIGAND (AGONIST OR 5 ANTAGONIST) OF 5-HT1A RECEPTORS

机译：通过烟碱和5-HT1A受体配体（配体或5种拮抗剂）的组合人工复制与烟草和其他成瘾药物（鸦片，精神分裂症，酒精）有关的药物条件

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The invention enables smokers to stop consuming tobacco without indefinitely and without suffering from significant undesired effects, and also enables consumers of generally addictive drugs (opiacea, psychostimulants, alcohol) to stop consuming said drugs. CONTEXT OF THE INVENTION. The products available on the market for controlling smoking include three types: a. nicotine additives (patch, chewing gum, etc.): nicotine has no toxic effect, but additives solely containing nicotine have a significant effect on tobacco consumption only during the first weeks of the treatment. Relapses are very frequent (higher than 75 %). b. Zyban (Bupropion): Zyban, whether consumed with or without nicotine, does not act as an addictive substitute. From a clinical point of view, relapse up to 80% is observed after a month treatment. It further has undesired cardiovascular effects. c. Champix (Varenicline): Champix has been released recently on the market. Its function is to partially inhibit the effect of nicotine. It does not operate as an addictive substitute. From a clinical point of view, the quitting figures published until today are approximately 44% after one month, with very high levels of relapse in the following months. Significant side effects, such as sleep disorders, have been reported since it has been made available on the market. The main current research has not been able to compensate for the deficiencies of these products: a. Rimonabant, a cannabinoid receptor antagonist product, was not released on the market because clinical tests revealed a strong depression-promoting effect. b. Other research focuses on the action of compounds associated with nicotine for explaining the strong addictive potential of tobacco; however, the selected compounds did not appear as effective solutions. Indeed, several works suggest that the monoamine oxidase inhibitors (IMAOs) contained in tobacco and in the smoke thereof are the compounds that, in association with nicotine, impart an addictive effect to tobacco (4, 10, 11). The research focuses on the addition of monoamine oxidase inhibitors (IMAOs) to nicotine. This solution is not effective enough in that the blocking of monoamine oxidases may have dangerous physiological consequences (serotoninergic syndrome). Consequently, we do not currently know of any tobacco substitution product, either on the market or in development, which is sufficiently effective in smoking control. There is no substitution product for psychostimulants (cocaine, amphetamine), and two products are available on the market as a substitute for opiacea, i.e. subutex (buprenorphine) and methadone. Although they are effective as substitution products, the latter are not advantageous in that they maintain the consumer in a strong physical addiction state (10 days and more), which makes weaning difficult or even impossible. Furthermore, there is no substitution product for alcohol, and the products used today are intended for repelling a drinker and are not sufficient for weaning.

机译：本发明使吸烟者可以无限期地停止食用烟草，而不会遭受明显的不良影响，并且还使通常上瘾的药物（鸦片类，精神兴奋剂，酒精）的消费者停止消费所述药物。发明内容。市场上用于控制吸烟的产品包括三种类型：尼古丁添加剂（贴剂，口香糖等）：尼古丁没有毒性作用，但仅包含尼古丁的添加剂仅在治疗的最初几周对烟草消费有显着影响。复发非常频繁（高于75％）。 b。 Zyban（安非他酮）：Zyban，无论是否与尼古丁一起食用，都不能作为成瘾的替代品。从临床角度来看，治疗一个月后，复发率高达80％。它进一步具有不希望的心血管作用。 C。 Champix（Varenicline）：Champix最近已在市场上发布。它的功能是部分抑制尼古丁的作用。它不能作为令人上瘾的替代品。从临床角度来看，直到今天公布的戒烟数据在一个月后大约占44％，在接下来的几个月中复发率很高。自从它在市场上销售以来，已经报道了诸如睡眠障碍之类的重要副作用。当前的主要研究未能弥补这些产品的不足：大麻素受体拮抗剂产品Rimonabant并未投放市场，因为临床测试显示出强烈的促抑郁作用。 b。其他研究集中在与尼古丁有关的化合物在解释烟草强大的成瘾潜力方面的作用。但是，所选化合物并未显示为有效溶液。确实，有几项研究表明，烟草及其烟中所含的单胺氧化酶抑制剂（IMAOs）是与尼古丁结合而赋予烟草成瘾作用的化合物（4，10，11）。该研究集中在向烟碱添加单胺氧化酶抑制剂（IMAOs）。该解决方案不够有效，因为单胺氧化酶的封闭可能会带来危险的生理后果（5-羟色胺能综合症）。因此，我们目前不知道在市场上或在开发中的任何烟草替代产品都能有效地控制吸烟。没有精神兴奋药（可卡因，苯丙胺）的替代产品，市场上有两种产品可以替代鸦片类药物，即subutex（丁丙诺啡）和美沙酮。尽管它们作为替代产品有效，但后者的不利之处在于它们使消费者保持强烈的身体成瘾状态（10天以上），这使断奶变得困难，甚至是不可能的。此外，没有替代酒精的产品，并且今天使用的产品旨在排斥饮酒者，并且不足以断奶。

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公开/公告号WO2009090556A8

专利类型
公开/公告日2009-10-01

原文格式PDF
申请/专利权人 TASSIN THOMAS;
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申请/专利号WO2009IB00468
发明设计人 TASSIN JEAN-POL;
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申请日2009-03-09
分类号A61K31/135;A61K31/15;A61K31/343;A61K31/404;A61K31/4525;A61K31/465;A61K45/06;A61P25/30;
国家 WO
入库时间 2022-08-21 19:17:47

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