Rimonabant
Rimonabant (also known as SR141716; trade names Acomplia and Zimulti) is an anorectic anti-obesity drug originally approved in Europe in 2006. Developed by Sanofi-Aventis, Rimonabant was designed as a treatment to reduce appetite and aid in weight loss. However, it was withdrawn worldwide in 2008 due to serious psychiatric side effects and was never approved for use in the United States.[1][2]
Mechanism of Action[edit | edit source]
Rimonabant is a selective inverse agonist of the CB1 receptor, which is part of the endocannabinoid system that regulates appetite, mood, and energy balance. By blocking CB1 receptors, Rimonabant reduces appetite and food intake. Research indicated that Rimonabant also affected the μ-opioid receptor, which may have contributed to both its effectiveness and side effects.[3]
Development and Approval[edit | edit source]
Sanofi-Aventis discovered and developed Rimonabant, achieving approval from the European Commission on June 21, 2006. It was marketed as a prescription drug for patients with a BMI of over 30 kg/m² or over 27 kg/m² if associated with risk factors like type 2 diabetes or dyslipidaemia. However, approval requests in the United States were denied by the FDA, citing unresolved safety concerns.[4]
Clinical Trials and Studies[edit | edit source]
Rimonabant's effectiveness and risks were assessed in several trials, including the RIO (Rimonabant In Obesity) trials. These studies showed significant weight loss and improvements in metabolic syndrome parameters. However, the trials also revealed notable psychiatric side effects, such as depression, anxiety, and suicidal ideation.[5]
Adverse Effects and Safety Concerns[edit | edit source]
Rimonabant's side effects included psychiatric disorders in up to 10% of subjects, with suicidal ideation affecting around 1%. Additional common side effects were nausea, gastroenteritis, insomnia, muscle cramps, and fatigue. The European Medicines Agency recommended suspension due to these psychiatric risks, and sales were subsequently halted worldwide in 2008.[6]
Withdrawal and Regulatory Actions[edit | edit source]
In October 2008, the European Medicines Agency (EMA) recommended suspension of Rimonabant, citing the risks of serious psychiatric side effects, including suicidal ideation. In 2009, the FDA reaffirmed its stance against approval. India also banned its manufacture and sale. Consequently, Rimonabant was withdrawn from all markets.[7]
Pharmacodynamics and Chemistry[edit | edit source]
Rimonabant's action as an inverse agonist at the CB1 receptor highlights its novel mechanism for obesity treatment. The compound also antagonizes the μ-opioid receptor, potentially enhancing side effects. The molecular structure of Rimonabant comprises several key functional groups, contributing to its biological activity.[8]
Current Status[edit | edit source]
Rimonabant was first approved in Europe in 2006. However, it was withdrawn worldwide in 2008 due to serious psychiatric side effects. Rimonabant was never approved in the United States. Since its withdrawal, Rimonabant is not available for prescription. However, its mechanism of action continues to be studied for potential therapeutic uses, particularly in the treatment of addictions and metabolic disorders.
Future Perspectives and Research[edit | edit source]
Although withdrawn, Rimonabant's effects on the endocannabinoid system have informed ongoing research in obesity and metabolic disorders. Investigations into safer CB1 antagonists or modulators continue. The knowledge gained from Rimonabant has also guided the development of alternative weight management strategies without associated psychiatric risks.[9]
External links[edit | edit source]
See Also[edit | edit source]
References[edit | edit source]
- ↑ "Rimonabant". AdisInsight. Retrieved 21 February 2017.
- ↑
- ↑
- ↑
- ↑ "Acomplia EPAR" (PDF). EMA. January 30, 2009. Retrieved February 21, 2017.
- ↑
- ↑ "Anti-obesity drug use suspended". BBC News. 23 October 2008.
- ↑
- ↑
 | This pharmacology-related article is a stub. You can help WikiMD by expanding it. |
Search WikiMD
Ad.Tired of being Overweight? Try W8MD's physician weight loss program.
Semaglutide (Ozempic / Wegovy and Tirzepatide (Mounjaro / Zepbound) available.
Advertise on WikiMD
|
WikiMD's Wellness Encyclopedia |
| Let Food Be Thy Medicine Medicine Thy Food - Hippocrates |
Translate this page: - East Asian
中文,
日本,
한국어,
South Asian
हिन्दी,
தமிழ்,
తెలుగు,
Urdu,
ಕನ್ನಡ,
Southeast Asian
Indonesian,
Vietnamese,
Thai,
မြန်မာဘာသာ,
বাংলা
European
español,
Deutsch,
français,
Greek,
português do Brasil,
polski,
română,
русский,
Nederlands,
norsk,
svenska,
suomi,
Italian
Middle Eastern & African
عربى,
Turkish,
Persian,
Hebrew,
Afrikaans,
isiZulu,
Kiswahili,
Other
Bulgarian,
Hungarian,
Czech,
Swedish,
മലയാളം,
मराठी,
ਪੰਜਾਬੀ,
ગુજરાતી,
Portuguese,
Ukrainian
Medical Disclaimer: WikiMD is not a substitute for professional medical advice. The information on WikiMD is provided as an information resource only, may be incorrect, outdated or misleading, and is not to be used or relied on for any diagnostic or treatment purposes. Please consult your health care provider before making any healthcare decisions or for guidance about a specific medical condition. WikiMD expressly disclaims responsibility, and shall have no liability, for any damages, loss, injury, or liability whatsoever suffered as a result of your reliance on the information contained in this site. By visiting this site you agree to the foregoing terms and conditions, which may from time to time be changed or supplemented by WikiMD. If you do not agree to the foregoing terms and conditions, you should not enter or use this site. See full disclaimer.
Credits:Most images are courtesy of Wikimedia commons, and templates Wikipedia, licensed under CC BY SA or similar.
Contributors: Prab R. Tumpati, MD
