Patent WO-2009090556-A2 (WO)
Title: 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
Inventor: TASSIN JEAN-POL
IPC: A61K31/135
Filed: 2009-03-09
Abstract: 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.