Name: | rimonabant |
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PubChem Compound ID: | 104849 |
Molecular formula: | C22H22Cl4N4O |
Molecular weight: | 500.247 g/mol |
Synonyms: |
N-(Piperidin-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide hydrochloride; 158681-13-1; 5-(4-Chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-1-piperidinyl-1H-pyrazole-3-carboxamide monohydrochloride; SR 141716A; Rimonabant hydrochloride; SR141716A; 1H-Pyrazole-3-carboxamide, 5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-1-piperidinyl-, monohydrochloride
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Name: | rimonabant |
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Name (isomeric): | DB06155 |
Drug Type: | small molecule |
Synonyms: |
SR 141716; SR 141716A; SR141716; SR141716A
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Brand: | Rimoslim, Zimulti, Slimona, Riobant, Acomplia |
Category: | Anti-Obesity Agents |
CAS number: | 158681-13-1 |
Indication: | For use in conjunction with diet and exercise for patients with a body mass index greater than 30 kg/m<sup>2</sup>, or patients wih a BMI greater than 27 kg/m<sup>2</sup> with associated risk factors, such as type 2 diabetes or dyslipidaemia. |
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Pharmacology: | In the RIO-North America trial, 3040 patients were randomized to receive either placebo or one of two doses of rimonabant (5 mg or 20 mg per day). Patients taking 20 mg rimonabant had significant weigh loss, decrease in waist circumference, improved insulin sensitivity, and increases in HDL cholesterol, compared to patients on placebo. |
Mechanism of Action: |
Rimonabant is a specific CB1 cannabinoid receptor antagonist. There is considerable evidence that the endocannabinoid (endogenous cannabinoid) system plays a significant role in appetitive drive and associated behaviours. It is therefore reasonable to hypothesize that the attenuation of the activity of this system would have therapeutic benefit in ...
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Absorption: | Undetermined |
Protein binding: | Almost 100% |
Biotransformation: | Hepatic, CYP3A4 involved. |
Half Life: | 6 to 9 days with normal BMI and 16 days if BMI is greater than 30 |
Toxicity: | Almost twice as many people discontinued rimonabant compared with placebo because of adverse events (13.8% vs. 7.2%). These consistently involved psychiatric disorders (8.5% vs. 3.2%), including depression and anxiety. Other common side effects included insomnia, nausea, vomiting, diarrhoea and fatigue. |
Affected organisms: | Humans and other mammals |