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11-SEPTEMBER-2008 12:20:15 - Rimonabant Rimonabant Systematic IUPAC name 5-4-Chlorophenyl-1-2,4-dichloro-phenyl- 4-methyl-N-piperidin-1-yl- 1H-pyrazole-3-carboxamide Identifiers CAS number 158681-13-1 ATC code A08AX01 PubChem 104850 Chemical data Formula C22H21Cl3N4O Mol. mass 463.79 g/mol Pharmacokinetic data Bioavailability Undetermined Protein binding Nearly 100% Metabolism Hepatic, CYP3A4 involved Half life Variable: 6 to 9 days with normal BMI 16 days if BMI 30 Excretion Fecal 86% and renal 3% Therapeutic considerations Licence data EU Pregnancy cat. Not assigned. Use not recommended Legal status POMUK Routes Oral Rimonabant also known as SR141716, Acomplia, Bethin, Monaslim, Remonabent, Riobant, Slimona, Rimoslim, and Zimulti1 is an anorectic anti-obesity drug. It is an inverse agonist for the cannabinoid receptor CB1. Its main avenue of effect is reduction in appetite. Rimonabant is the first selective CB1 receptor blocker to be approved for use anywhere in the world. In Europe, it is indicated for use in conjunction with diet and exercise for patients with a body mass index greater than 30 kg/m², or patients with a BMI greater than 27 kg/m² with associated risk factors, such as type 2 diabetes or dyslipidaemia. In the UK, it has been available since the end of July 2006. As of 2008, the drug was available in 56 countries. Contents 1 Approval 2 Side effects 3 Other uses 3.1 Smoking cessation 3.2 Addiction 3.3 Memory 3.4 Blockade of Cannabis effects 4 References Approval Despite the FDA issuing an approvable letter in February 2006 for the obesity indication and a non-approvable letter for smoking cessation, the drug did not enter the market in the United States in 2006.citations needed The French pharma firm Sanofi-Aventis disclosed that a complete response to the FDA's approvable letter was submitted on October 26, 2006, triggering a Class I two-month or Class II six-month review process. On June 13, 2007, FDA's Endocrine and Metabolic Drugs Advisory Committee EMDAC concluded that the French manufacturer Sanofi-Aventis failed to demonstrate the safety of rimonabant and voted against recommending the anti-obesity treatment for approval.2 Subsequently, Sanofi-Aventis announced that it was withdrawing the new drug application NDA for rimonabant and that it would resubmit an application at some point in the future. On 21 June 2006, the European Commission approved the sale of rimonabant in the then 25-member European Union. Sanofi announced that the first country in which Acomplia will be sold is the United Kingdom. Sales began in July 2006. Sanofi also announced that it projects that the drug will be sold shortly thereafter in Denmark, Ireland, Germany, Finland and Norway. It is expected in Belgium3 and Sweden in 2007. Ordinary obesity will, according to official medical recommendations, not be enough to acquire the prescription in Sweden; there are additional requirements concerning abnormal blood lipid levels.4 The EU's approval was not a blanket approval, nor did it approve Acomplia for non-obesity related problems such as smoking cessation, although off-label use of the drug is still possible. The approval is in combination with diet and exercise for the treatment of obese patients BMI greater than or equal to 30, or overweight patients BMI greater than 27 with associated risk factors, such as type 2 diabetes or dyslipidaemia. Side effects Shortly after market introduction, press reports and independent studies suggest that side effects occur stronger and more commonly than shown by the manufacturer in their clinical studies. Reports of severe depression are frequent. This is deemed to result from the drug being active in the central nervous system, an area of human physiology so complex that the effects of a drug are extremely difficult to predict or anticipate.5 Because the drug has the opposite effects of cannabinoid receptor agonists such as tetrahydrocannabinol THC, one of the substances found in marijuana, which is neuroprotective against excitotoxicity,6 it can be theorized that Rimonabant promotes the development of neurodegenerative diseases of the central nervous system such as Multiple sclerosis, Alzheimer's disease, Amyotrophic lateral sclerosis ALS, Parkinson's disease, and Huntington's disease in persons who are susceptible.7 The reported development of previously clinically silent multiple sclerosis in one patient taking Rimonabant suggests that any patients with an underlying neurological condition should not take Rimonabant, given the neuroprotective role of the endocannabinoid system in many experimental paradigms of neurological disease. On 15 June 2007 the BBC News reported 8 that a committee advising the US FDA has voted not to recommend the drug's approval because of concerns over suicidality, depression and other related side effects associated with use of the drug. The risk benefit ratio on the usage of Rimonabant is not yet established, so better alternates can be chosen until FDA gives clearance for the same to avoid possible side effects. Other uses Smoking cessation Rimonabant may also be found to be effective in assisting some smokers to quit smoking. Sanofi-Aventis is currently conducting studies to determine the possible value of rimonabant in smoking-cessation therapy. The Studies with Rimonabant and Tobacco Use STRATUS Program involves more than 6,000 subjects. STRATUS is designed to explore two smoking-related therapies: first, to use rimonabant directly to aid in smoking cessation; second, to help prevent weight gain in former smokers. Initial results apparently suggest that rimonabant is effective for both uses. However, the FDA has explicitly stated to Sanofi-Aventis that without additional studies rimonabant cannot be approved in the United States for smoking cessation therapy. According to Cochrane review in 2007 Rimonabant may increase the odds of quitting approximately 11/2-fold9. Addiction Rimonabant reduced resumption of cocaine-seeking responses triggered by two of the three most common triggers of relapse in humans, priming and cues. It may also reduce ethanol and opiate seeking behavior10. Memory TetrahydrocannabinolTHC is known to impair short-term memory. It was therefore hypothesised that Rimonabant may improve short-term memory. Indeed in animal studies it significantly improved the performance of rats to encode information in the short-term memory11. Blockade of Cannabis effects Rimonabant blocks the psychoactive and some of the cardiovascular effects of Δ9-TetrahydrocannabinolTHC in humans without affecting the pharmacokinetics12. References ^ Rimonabant is currently being sold in the United Kingdom by Sanofi-Aventis and in Denmark by Sanofi-Synthelabo under the trade name Acomplia which is the name used in 18 countries, as of 2007. Bethin, Monaslim, Remonabent, Riobant, Slimona and Rimoslim are generic forms available in India. If approved in the United States, it is intended to be marketed under the name Zimulti. ^ Zimulti Acomplia Report - Diet Drug Acomplia / Zimulti Gets Thumbs Down From FDA Panel ^ Article from the Belgian newspaper De Standaard ^ Article from the Swedish TV station TV 4 website ^ Kassen müssen nicht für Acomplia zahlen. tagesschau.de 2006-10-17. Retrieved on 2007-06-13. ^ 1 Neuroprotection by 9-Tetrahydrocannabinol, the Main Active Compound in Marijuana, against Ouabain-Induced In Vivo Excitotoxicity, M. van der Stelt, W. B. Veldhuis, P. R. Bär, G. A. Veldink1, J. F. G. Vliegenthart, and K. Nicolay, The Journal of Neuroscience, September 1, 2001 ^ Kim AH, Kerchner GA, and Choi DW. Blocking Excitotoxicity. Chapter 1 in CNS Neuroproteciton. Marcoux FW and Choi DW, ors. Springer, New York. 2002. Pages 3-36 ^ BBC NEWS | Health | Suicide risk fears over diet pill ^ Cahill K, Ussher M 2007. Cannabinoid type 1 receptor antagonists rimonabant for smoking cessation. Cochrane database of systematic reviews Online 4: CD005353. doi:10.1002/14651858.CD005353.pub3. PMID 17943852. ^ Maldonado R, Valverde O, Berrendero F 2006. Involvement of the endocannabinoid system in drug addiction. Trends Neurosci. 29 4: 225-32. doi:10.1016/j.tins.2006.01.008. PMID 16483675. ^ Deadwyler SA, Goonawardena AV, Hampson RE 2007. Short-term memory is modulated by the spontaneous release of endocannabinoids: evidence from hippocampal population codes. Behavioural pharmacology 18 5-6: 571-80. doi:10.1097/FBP.0b013e3282ee2adb. PMID 17762525. ^ Huestis MA, Gorelick DA, Heishman SJ, et al 2001. Blockade of effects of smoked marijuana by the CB1-selective cannabinoid receptor antagonist SR141716. Arch. Gen. Psychiatry 58 4: 322-8. doi:10.1001/archpsyc.58.4.322. PMID 11296091. v d e Antiobesity preparations A08 -- see also anorectic Centrally acting Phentermine - Fenfluramine - Amfepramone - Dexfenfluramine - Mazindol - Cathine - Clobenzorex - Sibutramine - cannabinoids Rimonabant, Taranabant Peripherally acting Orlistat v d e Cannabinoids Plant cannabinoids CBD CBDV CBN CBG CBV CBL THC THC-C4 THCV Cannabinoid metabolites 11-Hydroxy-THC 11-nor-9-Carboxy-THC Endogenous cannabinoids Arachidonoyl ethanolamide Anandamide or AEA 2-Arachidonoylglycerol 2-AG 2-Arachidonyl glyceryl ether noladin ether Virodhamine N-arachidonoyl-dopamine NADA; Oleamide Synthetic cannabinoid agonists Classical cannabinoids Dibenzopyrans A-41988 Ajulemic acid AM-087 AM-411 AM-855 AM-905 AM-906 AM-919 AM-938 AM-4030 AMG-1 AMG-3 AMG-36 AMG-41 Dexanabinol HU-211 DMHP Dronabinol HU-210 JWH-051 JWH-133 JWH-139 L-759,633 L-759,656 Levonantradol Nabilone Nabitan O-806 O-823 O-1057 O-1125 O-1238 O-2545 O-2694 Parahexyl THC-O-acetate THC-O-phosphate Nonclassical cannabinoids CP 47,497 CP 55,244 CP 55,940 HU-308 2-Isopropyl-5-methyl-1-2,6-dihydroxy-4-nonylphenylcyclohex-1-ene Aminoalkylindoles AM-630 AM-1241 JWH-015 JWH-018 JWH-073 JWH-081 JWH-200 L-768,242 Pravadoline WIN 55,212-2 Aminoalkylpyrroles JWH-030 JWH-147 JWH-307 Eicosanoids AM-883 Arachidonyl-2'-chloroethylamide Arachidonylcyclopropylamide Methanandamide O-585 O-689 O-1812 O-1860 O-1861 Others BAY 38-7271 BAY 59-3074 GW 842,166X JWH-171 O-2220 Endocannabinoid activity enhancers AM-404 CAY-10401 CAY-10402 N-arachidonoyl-serotonin O-1624 PF-622 PF-750 URB-597 URB-602 URB-754 Cannabinoid antagonists and inverse agonists AM-251 AM-281 AM-630 AVE-1625 BML-190 CAY-10508 CB-25 CB-52 JTE-907 LY-320,135 MK-9470 NESS-0327 O-1184 O-2050 O-2654 Rimonabant SLV-319 SR-144,528 Surinabant Taranabant VCHSR Retrieved from http://en..org/wiki/Rimonabant Categories: Anorectics | CB1 receptor antagonists | Piperidines | PyrazolesHidden categories: All articles with statements | Articles with statements since June 2007 Views Article Discussion this page History Personal tools Log in / create account Navigation Main page Contents Featured content Current events Random article Search Go Search Interaction Community portal Recent changes Contact Donate to Help Toolbox What links here Related changes Upload file Special pages Printable version Permanent link Cite this page Languages العربية Deutsch Français עברית Nederlands 日本語 Polski Português Suomi This page was last modified on 15 July 2008, at 19:54
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