Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: KEGG:D05731 (Rimonabant)
 326 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Tobacco smoking is the largest cause of avoidable death and disease in developed countries. It is now viewed as a complex bio-psycho-social problem for which effective pharmacological treatments are needed. Nicotine is considered to be the primary compound of tobacco smoke that establishes and maintains tobacco dependence. The addictive effect of nicotine is mediated by activation of the mesolimbic system and the release of dopamine in the nucleus accumbens. Recently, the existence of a specific functional interaction between nicotine and the endocannabinoid system has been reported. Co-administration of sub-threshold doses of a cannabinoid agonist and nicotine produces rewarding effects and chronic nicotine treatment increases endocannabinoid levels in limbic regions. The CB1 receptor plays a key role in this interaction. CB1 knockout mice are less sensitive to the motivational effects of nicotine although this depends on the experimental model. The selective CB1 antagonist, rimonabant (SR141716), reduces nicotine self-administration and nicotine-seeking behavior induced by conditioned cues in rats. Rimonabant appears to reduce nicotine addiction by attenuating the hyperactivation of the endocannabinoid system and the mesolimbic dopaminergic neuronal pathway. Rimonabant may be considered as a potential alternative to the current substitutive treatments of nicotine addiction and may offer a new hope for the treatment of smokers who wish to quit.
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PMID:CB1 receptor antagonists for the treatment of nicotine addiction. 1593 55

Although the proportion of the adult population in the United States that smokes has decreased steadily, the rate of successful quit attempts is still low. Smokers develop nicotine dependence that resembles other addictions, and may require multiple attempts and long-term treatment to sustain abstinence. Currently available first-line agents for smoking cessation therapy include nicotine replacement therapy, which is available in several formulations, including transdermal patch, gum, nasal spray, inhaler, and lozenge; bupropion, an atypical antidepressant; and varenicline, a partial agonist of the alpha(4)beta(2) nicotinic acetylcholine receptor that was recently developed and approved specifically for smoking cessation therapy. Second-line agents are nortriptyline, a tricyclic antidepressant agent, and clonidine, an antihypertensive drug. With the exception of varenicline, which has been shown to offer significant improvement in abstinence rates over bupropion, all of the available treatments appear similarly effective. However, the adverse event profiles of nortriptyline and clonidine make them more appropriate for second-line therapy, when first-line treatments have failed or are not tolerated. Rimonabant, a cannabinoid-1 receptor antagonist that was being developed for smoking cessation, received a nonapprovable letter from the FDA in 2006 and there is no further information as to whether development for this indication is continuing for this agent. Nicotine vaccines are under investigation and offer promise, especially for relapse prevention. Ultimately, selection of pharmacologic agent should be based on the patient's comorbidities and preferences, as well as on the agent's adverse event profile.
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PMID:Update on pharmacologic options for smoking cessation treatment. 1834 63

Gateways to Clinical Trials are a guide to the most recent clinical trials in current literature and congresses. The data in the following tables has been retrieved from the Clinical Trials Knowledge Area of Prous Science Integrity, the drug discovery and development portal, http://integrity.prous.com. This issue focuses on the following selection of drugs: 131-I-Chlorotoxin, 423557; Abatacept, Ad.Egr.TNF.11D, Adalimumab, AE-941, Ambrisentan, AMR-001, Anacetrapib, Anakinra, Aripiprazole, Atazanavir sulfate; BAY-639044, Bazedoxifene acetate, Belimumab, Bevacizumab, Bortezomib, Botulinum toxin type B, Brivaracetam, Bucindolol hydrochloride; Carfilzomib, Carisbamate, CCX-282, CD20Bi, Ceftobiprole, Certolizumab pegol, CF-101, Cinacalcet hydrochloride, Cypher; Darifenacin hydrobromide, Degarelix acetate, Denosumab, Desvenlafaxine succinate, Dexlansoprazole, Dexverapamil, Drotrecogin alfa (activated), Duloxetine hydrochloride, Dutasteride; Efalizumab, EPs-7630, Escitalopram oxalate, Etoricoxib; Fluticasone furoate, Fondaparinux sodium, Fospropofol disodium; Hexadecyloxypropyl-cidofovir, HIV gp120/NefTat/AS02A, HPV-6/11/16/18; INCB-18424, Incyclinide, Inhalable human insulin, Insulin detemir; KNS-760704, KW-0761; Lacosamide, Lenalidomide, Levetiracetam, Licofelone, Lidocaine/prilocaine; mAb 216, MEDI-528, Men ACWY, Meningococcal C-CRM197 vaccine, Methylnaltrexone bromide; Nemifitide ditriflutate, Nicotine conjugate vaccine, Nilotinib hydrochloride monohydrate; Octaparin; Parathyroid hormone (human recombinant), Pegaptanib octasodium, Pitrakinra, Prasterone, Pregabalin; Ranelic acid distrontium salt, Rasagiline mesilate, Retigabine, Rimonabant, RTS,S/AS02D; Sarcosine, Sitaxentan sodium, Solifenacin succinate, Sunitinib malate; Taranabant, Taxus, Teduglutide, Teriparatide, Ticagrelor, Travoprost, TRU-015; USlipristal acetate, Urocortin 2; Vardenafil hydrochloride hydrate; YM-155, Yttrium 90 (90Y) ibritumomab tiuxetan; Zanolimumab, Zoledronic acid monohydrate, Zotarolimus, Zotarolimus-eluting stent.
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PMID:Gateways to clinical trials. 1856 Jun 31

Nicotine-associated paraphernalia such as cigarettes and ashtrays are potent smoking relapse triggers. In addition to these discrete cues, environmental contexts previously associated with smoking elicit strong cigarette craving, indicating that contextual stimuli also contribute to high smoking relapse rates. Nonetheless, little is known about the precise role of these stimuli in smoking relapse and the neuropharmacological mechanisms implicated herein. To address this issue, we determined whether re-exposure to the nicotine self-administration context after long-term extinction reinstates nicotine seeking behavior in rats. Further, we examined the effects of SR141716A (Rimonabant), a selective cannabinoid CB1 receptor antagonist which has been shown to attenuate cue-induced relapse to nicotine seeking, on context-induced reinstatement of nicotine seeking. Rats were trained to self-administer nicotine intravenously (30microg/kg/infusion). Nicotine infusions were paired with an audiovisual compound stimulus. Subsequently, nose poking behavior was extinguished in the presence of this discrete cue in a context different from the self-administration context. Hereafter, rats were injected with 0, 1, or 3mg/kg Rimonabant (i.p.) prior to re-exposure to either the self-administration or the extinction context. Re-exposure to the self-administration context, but not to the extinction context robustly reinstated responding for the discrete nicotine cues, an effect that was dose-dependently attenuated by Rimonabant. This is the first demonstration of contextual renewal of nicotine seeking in rodents after prolonged withdrawal. Further, our results indicate that the endocannabinoid system is involved in context-induced relapse to nicotine seeking, and as such these data provide further evidence for the use of CB1 antagonists in smoking cessation.
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PMID:Contextual renewal of nicotine seeking in rats and its suppression by the cannabinoid-1 receptor antagonist Rimonabant (SR141716A). 1858 3

Tobacco smoking is the leading cause of preventable morbidity and mortality in the world. There are nearly 1, 3 billion users of nicotine and tobacco products worldwide while approximately 4, 9 millions of them die from smoking-related disease every year. Cigarette smoking is a highly addictive behavior. Pharmacotherapy can be useful to achieve long-term abstinence. Nicotine replacement products are widely employed and recommended by the World Health Organization. There is strong evidence for the efficacy of the atypical antidepressant Bupropion as therapy for smoking cessation. The partial nicotinic receptor agonist varenicline has recently been approved as treatment for nicotine addiction in Germany. Preliminary data from clinical trials have suggested that varenicline may be an effective therapy for tobacco dependence with minimal side effects. Clonidine and nortriptyline have demonstrated some efficacy but possible side effects may limit their use. Additionally both are not approved for smoking cessation in Germany. Other promising new therapeutic drugs include Rimonabant and nicotine vaccines. They will provide smokers additional options to assist in achieving smoking cessation. Treatment of psychological dependence in addition to physiological dependence, however, is a must for long-term abstinence. For this reason a successful smoking cessation intervention requires besides pharmacological treatments motivational counseling and behavioral interventions.
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PMID:[Current and future medical drugs for smoking cessation]. 1950 11