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Rimonabant

Rimonabant
Drug information
Systematic (IUPAC) name
IUPAC name5-(4-Chlorophenyl)-1-(2,4-dichloro-phenyl)-
4-methyl-N-(piperidin-1-yl)-
1H-pyrazole-3-carboxamide
Chemical data
Mol. mass463.79 g/mol
BioavailabilityUndetermined
Protein bindingNearly 100%
MetabolismHepatic, CYP3A4 involved
Half-lifeVariable:
6 to 9 days with normal BMI
16 days if BMI >30
ExcretionFecal (86%) and renal (3%)
Therapeutic considerations
Pregnancy cat Not assigned, use not recommended
RoutesOral

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Rimonabant (also known as SR141716; trade names Acomplia, Bethin, Monaslim, Remonabent, Riobant, Slimona, Rimoslim, Zimulti, and Riomont) is an anorectic antiobesity drug that has been withdrawn from the market. It is an inverse agonist for the cannabinoid receptor CB1. Its main effect is reduction in appetite.

Rimonabant was the first selective CB1 receptor blocker to be approved for use anywhere in the world. In Europe, it was 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 was available beginning in July 2006. As of 2008, the drug was available in 56 countries. On 23 October 2008, the European Medicines Agency (EMEA) issued a press release stating its Committee for Medical Products for Human Use (CHMP) had concluded the benefits of Acomplia no longer outweighed its risks, and subsequently recommended the product be suspended from the UK market. Sanofi-Aventis later released a press statement stating the drug had been suspended. Approval of the drug was officially withdrawn by the EMEA on 16 January 2009.

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Warrington bucks the cost of obesity trend - Warrington Guardian Tweet this news
Warrington Guardian--By contrast in Warrington the cost for ingredients sibutramine and -rimonabant- fell from £59605 in 2006/07 to £26827 in 2009/10. Orlistat ingredients cost the PCT £134000 in both 2006/07 and 2009/10. In 2006/07 NHS Warrington spen - Date : Thu, 14 Apr 2011 08:08:33 GMT+00:00
Why isn't there a safe weight-loss pill? - CNN International Tweet this news
CNN International--The weight-loss busts are plenty: Meridia (heart attacks, strokes), Fen-phen (heart risk), -Rimonabant- (suicidal thoughts), ephedra (heart attacks, strokes). "Losing weight doesn't mean anything if the drug is counteracti - Date : Fri, 15 Apr 2011 19:55:45 GMT+00:00
Dall'Università di Salerno una promettente strategia contro il cancro - Universy.it Tweet this news
Universy.it--L'impiego di un farmaco, il -Rimonabant-, in grado di “spegnere” il gene ed impedirne il funzionamento ha consentito per la prima volta di bloccare la neoangiogenesi in modelli animali di retinopatia. Oltre che in patologie tumorali, - Date : Mon, 11 Apr 2011 13:21:57 GMT+00:00
Sanofi Disappointed Case Against 2 Executives Not Dismissed - Wall Street Journal Tweet this news
Wall Street Journal---Rimonabant-, which the company had planned to market as Zimulti in the US and was branded Acomplia in Europe, was considered to have blockbuster potential as a treatment for obesity, substance abuse, smoking and diabetes before being - Date : Thu, 31 Mar 2011 15:26:25 GMT+00:00
Pills are not the answer to Scotland's obesity problem - Herald Scotland Tweet this news
Herald Scotland---Rimonabant- was banned by the EU Medicines Agency when it was shown that the benefits did not outweigh the risks and Sibutramine was withdrawn because of a suspected link with heart attacks. The landmark Kerr Report on the future of heal - Date : Wed, 30 Mar 2011 10:25:58 GMT+00:00
Hundreds of people from Dumfries and Galloway are taking obesity pills. - Dumfries and Galloway Standard Tweet this news
Dumfries and Galloway Standard--Sibutramine and -Rimonabant- are appetite suppressants. A spokesman for NHS Dumfries and Galloway said: “For a small proportion of patients, ... - Date : Thu, 03 Feb 2011 09:56:49 GMT+00:00
Factbox: A troubled history for weight-loss drugs - Reuters Tweet this news
Reuters--The drug, known generically as -rimonabant-, never won US approval after a panel of experts rejected it amid fears it may cause suicidal thoughts. ... - Date : Tue, 01 Feb 2011 18:01:48 GMT+00:00
Orexigen Rejection Kills Obesity Drug Field - Forbes Digital Download (blog) Tweet this news
Forbes Digital Download (blog)---Rimonabant-, a drug from Sanofi-Aventis, was touted as potentially the biggest medicine in history but was rejected by the FDA because it might cause suicide ... - Date : Tue, 01 Feb 2011 13:06:17 GMT+00:00
"Prescrit et ne cherche pas". "Secret commercial", rétention d'information ... - Le Post (Blog) Tweet this news
Le Post (Blog)--(1) Parmi ceux-ci : le rofécoxib (ex-Vioxx) anti-inflammatoire ; le -rimonabant- (ex-Acomplia) et le benfluorex (ex-Mediator) à visée amaigrissante ... - Date : Tue, 01 Feb 2011 18:43:18 GMT+00:00
Le Mediator et autres retraits de médicaments : les bases d'un vrai débat! - Categorynet.com (Communiqué de presse) Tweet this news
Categorynet.com (Communiqué de presse)---...- le rofécoxib (Vioxx®) du laboratoire Merck ou plus récemment le -rimonabant- (Acomplia®) du laboratoire Sanofi-Aventis. Récemment, la revue Prescrire a ... - Date : Mon, 10 Jan 2011 07:30:28 GMT+00:00

Antiobesity Agents/Anorectics (A08)

Central
Stimulants4-Methylamphetamine * Amfecloral * Amfepentorex * Amfepramone * Aminorex * Amphetamine * Amphetaminil * Atomoxetine * Benfluorex * Benzphetamine * Bupropion * Cathine * Cathinone * Chlorphentermine * Ciclazindol * Clobenzorex * Cloforex * Clominorex * Clortermine * Dexfenfluramine * Dextroamphetamine * Dextromethamphetamine * Dexmethylphenidate * Difemetorex * Dimethylcathinone * Diphemethoxidine * Ephedrine * Ephedra * Ethylamphetamine * Etolorex * Fenbutrazate * Fencamfamine * Fenethylline * Fenfluramine * Fenproporex * Fludorex * Fluminorex * Furfenorex * Indanorex * Khat * Levopropylhexedrine * Lisdexamfetamine * Manifaxine * Mazindol * Mefenorex * Methamphetamine * Methylphenidate * Pemoline * Pentorex (Phenpentermine) * Phendimetrazine * Phenethylamine * Phenmetrazine * Phentermine * Phenylpropanolamine * Pipradrol * Prolintane * Propylhexedrine * Pseudoephedrine * Pyrovalerone * Radafaxine * Reboxetine * Setazindol * Sibutramine * Synephrine * Tesofensine * Viloxazine * Xylopropamine * Zylofuramine
CannabinoidsIbipinabant * Otenabant * Rimonabant * Surinabant * Taranabant
Others5-HTP * Galactomannan (Guar Gum) * Glucomannan * L-DOPA * L-Phenylalanine * L-Tryptophan * L-Tyrosine * Lorcaserin * Lu AA-33810 * Metformin * Naltrexone * Naloxone * Oxyntomodulin * P57 * Peptide YY * Topiramate * Yohimbine (Yohimbe) * Zonisamide
Peripheral
Cetilistat * Dinitrophenol * Oleoyl-Estrone * Orlistat * Simmondsin * Sterculia

Cannabinoids

Plant cannabinoids
CBCV * CBD * CBDV * CBGM * CBGV * CBN * CBG * CBV * CBL * THC * THC-C4 * THCV |
Cannabinoid metabolites
8,11-DiOH-THC * 11-COOH-THC * 11-OH-THC |
Endogenous cannabinoids
Arachidonoyl ethanolamide (Anandamide or AEA) * 2-Arachidonoylglycerol (2-AG) * 2-Arachidonyl glyceryl ether (noladin ether) * Virodhamine * Palmitoylethanolamide (PEA) * N-Arachidonoyl dopamine (NADA) * Oleamide * RVD-Hpα |
Synthetic cannabinoid
receptor agonists
Classical cannabinoids
(Dibenzopyrans)
A-40174 * A-41988 * A-42574 * 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 * HHC * HU-210 * HU-243 * JWH-051 * JWH-133 * JWH-139 * JWH-229 * JWH-359 * L-759,633 * L-759,656 * Levonantradol (CP 50,5561) * Nabazenil * Nabidrox (Canbisol) * Nabilone * Nabitan * Naboctate * O-806 * O-823 * O-1057 * O-1125 * O-1238 * O-2545 * O-2694 * Parahexyl * Perrottetinene * Pirnabine * THC-O-acetate * THC-O-phosphate
Nonclassical cannabinoids CP 47,497 * CP 55,244 * CP 55,940 * HU-308 * Nonabine * SPA-229 * Tinabinol * 2-Isopropyl-5-methyl-1-(2,6-dihydroxy-4-nonylphenyl)cyclohex-1-ene
Benzoylindoles AM-630 * AM-694 * AM-1241 * GW-405,833 (L-768,242) * Pravadoline
Naphthoylindoles AM-1220 * JWH-007 * JWH-015 * JWH-018 * JWH-019 * JWH-073 * JWH-081 * JWH-122 * JWH-182 * JWH-200 * JWH-210 * JWH-398 * WIN 55,212-2
Phenylacetylindoles JWH-203 * JWH-250 * JWH-251 * JWH-302
Naphthoylpyrroles 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 A-836,339 * Abnormal cannabidiol * BAY 38-7271 * BAY 59-3074 * CB-13 * GW-842,166X * JWH-171 * O-1918 * O-2220 * Leelamine * Org 28611 * VSN-16
Endocannabinoid
activity enhancers
AM-404 * CAY-10401 * CAY-10402 * JZL184 * N-arachidonoyl-serotonin * O-1624 * PF-622 * PF-750 * PF-3845 * URB-597 * URB-602 * Genistein * Arvanil * Olvanil * Kaempferol * Biochanin A * URB-754 |
Cannabinoid receptor
antagonists and
inverse agonists
AM-251 * AM-281 * AM-630 * BML-190 * CAY-10508 * CB-25 * CB-52 * Drinabant * Hemopressin * Ibipinabant * JTE-907 * LY-320,135 * MK-9470 * NESS-0327 * O-1184 * O-1248 * O-2050 * O-2654 * Org 27569 * Otenabant * Rimonabant * SR-144,528 * Surinabant * Taranabant * VCHSR |



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