Rimonabant

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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	?
PubChem	104850
Chemical data
Formula	C₂₂H₂₁N₄Cl₃O
Mol. weight	463.79 g/mol
Pharmacokinetic data
Bioavailability	?
Metabolism	?
Half life	?
Excretion	?
Therapeutic considerations
Licence data	EU
Pregnancy cat.	?
Legal status
Routes	Oral

Rimonabant (SR141716) is an anorectic anti-obesity drug. It is a CB1 cannabinoid receptor antagonist. Its main avenue of effect is reduction in appetite. Rimonabant is currently being sold in the United Kingdom by Sanofi-Aventis and in Denmark by Sanofi-Synthelabo under the trade name Acomplia. It is anticipated that if the drug is approved in the United States, it will be sold under the trade name Zimulti.

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 wih a BMI greater than 27 kg/m² with associated risk factors, such as type 2 diabetes or dyslipidaemia. In the UK it is expected to be available from the end of June 2006.^[1]

1 Approval
2 Metabolic Disorders
3 Side Effects
4 Smoking Cessation
5 References
6 External links

[edit] Approval

The drug may enter the market in the United States in 2006 but only when FDA approval is received. However, as of February 2006 FDA approval in 2006 appears still unlikely. This is because in February 2006 the FDA told Sanofi-Aventis it would need further information on rimonabant before it would be approved for the U.S. market. Neither the FDA nor Sanofi-Aventis has revealed what this information is.

On 21 June 2006, the European Commission approved the sale of rimonabant in the 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 Belgium^[2] 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.^[3]

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.

[edit] Metabolic Disorders

In addition to reducing appetite, and thus being effective in weight control, rimonabant appears to be effective against certain metabolic disorders and associated cardiovascular risk factors.^[4]^[5] Other patients may have less benefit, such as for cosmetic purposes.^[2]

[edit] 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 his 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 drug effects are highly difficult to determine reliably.^[6]

[edit] 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.

[edit] References

^ Rinaldi-Carmona M, Barth F, Heaulme M, et al. SR141716A, a potent and selective antagonist of the brain cannabinoid receptor. FEBS Lett 1994; 350: 240-244
^ ^a ^b Article from the Belgian newspaper De Standaard
^ Article from the Swedish TV station TV 4 website
^ Despres JP, Golay A, Sjostrom L. Effects of rimonabant on metabolic risk factors in overweight patients with dyslipidemia. N Engl J Med 2005; 353: 2121-34. PMID 16291982
^ Van Gaal LF, Rissanen AM, Scheen AJ, Ziegler O, Rossner S. Effects of the cannabinoid-1 receptor blocker rimonabant on weight reduction and cardiovascular risk factors in overweight patients: 1-year experience from the RIO-Europe study. Lancet 2005; 365: 1389-97. PMID 15836887
^ "Accomplia" - Schlankmacher mit Nebenwirkungen (German: Die Tagesschau)