Generic Acomplia, Rimonabant
Acomplia (Rimonabant), marketed by Sanofi- Aventis is a selective CB1 endocannabinoid receptor antagonist indicated for the treatment of obesity.
Its mechanism of action is to block the endogenous cannabinoid binding to neuronal CB1 receptors.
What is endocannabinoid system?
The endocannabinoid system is in the part of the brain that regulates metabolism, energy levels and appetite.
With reference to the above drug, endocannabinoid receptors on activation will increase the appetite. Hence, drugs like Acomplia (Rimonabant) will block this endocannabinoid receptor, eventually leading to a decrease in the appetite. It is the most advanced endocannabinoid receptor antagonist in clinical development and offers a novel therapeutic approach to appetite control and weight reduction
So what is obesity?
Obesity medically is defined on the basis of Body Mass Index which is the individual's body weight divided by the square of their height in kg/m2. So, a BMI of 18.5 to 25 may indicate optimal weight; a BMI lower than 18.5 suggests the person is underweight while a number above 25 may indicate the person is overweight; a BMI below 17.5 may indicate the person has anorexia or a related disorder; a number above 30 suggests the person is obese (over 40, morbidly obese).
So technically speaking, those with their body mass index of 30 and above tend to fall in the high risk zone. It arises from the accumulation of excess fat in the body from over consumption of fatty foods and is now one of the most common nutritional disorders in the world.
Latest studies have corroborated the fact that obesity is a silent killer. It is associated with cardiovascular disease, especially angina and myocardial infarction, atherosclerosis and arteriosclerosis leading to cerebrovascular accidents/ strokes.
They also cause joint pains and are also associated with certain cancers like that of the breast or of the colon. The proportion of obese individuals in the developed countries has reached epidemic proportions. To put this picture in a better perspective, statistics show that one in five of all Americans are obese and one in three overweight.
In the presence of diabetes mellitus it forms a deadly combination and is termed as diabetisity. It shows more predilections to Type 2 diabetes mellitus
Various therapeutic strategies have been explored, including:
• Serotonin and nor adrenaline reuptake inhibitors (anorectic agents)
• Lipase inhibitors
• ß 3-adrenoreceptor agonists
• Leptin agonists
• Melanocortin-3 agonists
All these strategies have shown some amount of success.
Usually, after having cannabis these drug addicts suffer from extreme hunger pangs which these smokers refer to as ‘munchies’. This lead to the belief that cannabinoid is associated with hunger pangs and if this receptor is suppressed it will lead to decreased appetite which is what precisely the manufacturers of Acomplia [Rimonabant] Sanofi-Aventis did.
[Rimonabant] prevents the endogenous cannabinoid binding to CB1 receptors in nerve cells. These CB1 receptors, when activated, stimulate appetite. Hence this drug blocks the activation of these CB1 receptors and thus reduces appetite.
SIDE EFFECTS:
1. Nausea and vomiting
Nausea, vomiting and other gastrointestinal disorders were relatively common side effects of taking Acomplia.
2. Disorders of the nervous system
This category includes headaches, faintness and feeling dizzy.
3. Psychiatric disorders
Including mood swings, anxiety, depression, irritability, sleep disorders and other similar disorders. The current advice is that you should not take this drug if you suffer from mental health problems. The drug is not suitable for those with continuing major depressive illness and/or antidepressive treatment.
CONTRAINDICATIONS:
1. Any hypersensitivity to the drug or any of its ingredients.
2. Presence of liver damage.
3. Impaired renal function
4. Age more than 75 years and less than 16 years
5. Pregnant and lactating women.
6. In patients with lactose intolerance since it Acomplia contains lactose
7. It should only be used with caution in combination with CYP3A4 inhibitors, such as ketoconazole, ritonavir, Clarithromycin and related drugs.
8. It is not to be prescribed in patients with untreated psychiatric disease.
Acomplia [Rimonabant] taken for up to two years in conjunction with diet and exercise produces greater weight loss than the placebo, although most of the weight loss occurs in the first year.
More information on Acomplia, Rimonabant can by found at Acomplia, Rimonabant page
References:
- http://en.wikipedia.org/wiki/Body_mass_index
- http://www.acomplia.me.uk/contraindications.html
- http://www.drugdevelopment-technology.com/projects/rimonabant/
- http://www.acompliareport.com/
