How does Rimonabant work?

The active substance rimonabant, is a cannabinoid receptor antagonist. It acts by blocking a specific type of receptor, the cannabinoid type 1 (CB1) receptors. These receptors are found in the nervous system, and they are part of the system the body uses to control food intake. The receptors are also found in adipocytes (fat tissue).

 

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What is Rimonabant?

Rimonabant is an anorectic anti-obesity drug. Its main avenue of effect is reduction in appetite.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 has been available since the end of July 2006.

It is a CB1 cannabinoid receptor antagonist. Rimonabant is the first selective CB1 receptor blocker to be approved for use anywhere in the world. Belgian researchers writing in the Lancet 2005 said people taking rimonabant lost an average of 8.6 kilograms (18.9 pounds) in a year. They also lost an average of 8.5 centimetres (over three inches) from their waists. However, in May 2007, Canadian researchers reported also in the Lancet that the long-term impact of the drugs was not clearly known with side effects including increased blood pressure and pulse rate for sibutramine and mood-related disorders for rimonabant reported.

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.


How is Rimonabant used?
Rimonabant pills are taken as one tablet once a day, before breakfast. The patients should also follow a reduced calorie diet and increase their level of physical activity. The drug should not be used in patients who have severe problems with their liver or their kidneys.

How does Rimonabant work?
The active substance rimonabant, is a cannabinoid receptor antagonist. It acts by blocking a specific type of receptor, the cannabinoid type 1 (CB1) receptors. These receptors are found in the nervous system, and they are part of the system the body uses to control food intake. The receptors are also found in adipocytes (fat tissue).

Does Rimonabant slimming pills also aid smoking cessation?

Generic Acomplia has been studied by the french company Sanofi-Aventis as an aid to smoking cessation based on studies for up to one year in over 6,500 smokers motivated to quit smoking

What is the risk associated with Rimonabant ?
During the studies, the most common side effects with Rimonabant (seen in more than 1 patient in 10) were nausea (feeling sick) and infections of the upper respiratory tract. For the full list of all side effects reported with thie medicine, see the Package Leaflet. Rimonabant should not be used on people who may be hypersensitive (allergic) to rimonabant or any of the other ingredients, or in women who are breast feeding. It must also not be used in patients with ongoing major depression or who are being treated with antidepressants, since it can increase the risk of depression, including thoughts about suicide in a small minority of patients. Patients who experience symptoms of depression should speak to their doctor and may need to stop treatment. Caution should be used when taking Rimonabant with some medicines, such as ketoconazole or itraconazole (anti-fungal medicines), ritonavir (used in HIV infection), or telithromycin or clarithromycin (antibiotics).

Rimonabant and Smoking
While millions of obese people are excited at rimonabant's potential in helping them reduce their weight, some researchers believe this revolutionary drug could have a major role to play in helping smokers quit smoking even though regulators on the first go-round refused to approve it for this use.

While the EC System is associated with regulating the body's intake of food, it also is involved in tobacco dependency. Chronic tobacco use over-stimulates the EC system creating an imbalance. rimonabant, by blocking the CB1 receptor, helps restore balance to the EC system resulting in reduced dependence on tobacco.

Rimonabant has "roughly doubled the odds of quitting smoking," said Dr. Robert Anthenelli, associate professor of psychiatry at the University of Cincinnati College of Medicine in Ohio. "We also found remarkably reduced postcessation weight gain: a 77% reduction versus placebo....

"These dual effects on smoking cessation and reduced weight gain make rimonabant a promising agent for treating tobacco dependence," Anthenelli added.

Doctors say that while the percentage of smokers who benefit from rimonabant is considerably less than the very high number of obese and overweight individuals who benefit, the result among smokers is still significant and compares favorably with other smoking cessation products.

But while the initial smoking-cessation trial seemed pomising, results from a second trial were less encouraging and Sanofi was denied approval for use of rimonabant as a smoking cessation aid by both the U.S. Food and Drug Administration and the European Medicines Agency (EMEA).

The regulators asked for an additional clinical trial of rimonabant as an aid to helping break the smoking habit, and Sanofi has not yet indicated whether it intends to proceed with such a trial.

Obesity questions

Is obesity in pregnancy linked to poor outcomes for the mother or baby?
Answer:
We found a number of trials in this area and have therefore limited our response to a relative small number of the more recent trials.

A 2006 Australian paper examined the effect of obesity in an obstetric population and this concluded:

“Overweight and obesity are common in pregnant women. Increasing BMI is associated with maternal and neonatal outcomes that may increase the costs of obstetric care. To assist in planning health service delivery, we believe that BMI should be routinely recorded on perinatal data collection sheets.”

A 2007 paper “Maternal obesity in early pregnancy and risk of spontaneous and elective preterm deliveries: a retrospective cohort study.” , concluded:

“Obese nulliparous women are at increased risk of elective preterm deliveries. This in turn leads to an increased risk of perinatal mortality and is likely to lead to increased risks of long-term disability among surviving offspring.”

Another 2007 paper examined obesity and stillbirth , concluding:

“Maternal obesity is associated with an increased risk of stillbirth, although the mechanisms to explain this association are not clear.”

The final 2007 paper we found reported:

What investigations are recommended to rule out underlying causes of weight gain?
Answer:
We could find no recommendations regarding investigations related to unexplained weight gain.

The only information we could find was via the website WrongDiagnosis has a section on it’s website that lists 176 causes of weight gain , it also has a section on workup and diagnosis [2] which seems pertinent to the question. It should be noted that Wrong Diagnosis is not a source we usually use and the information is unreferenced, so use with caution.

“High maternal weight seems to increase the risk of neonatal mortality, especially in infants born after preterm PROM. Inflammation or infection related to obesity may be part of the causal pathway.”

In 2004 Bandolier reported on BMI and pre-eclampsia giving the following ‘Clinical bottom line’:

“Risk of pre-eclampsia generally doubles with each 5-7 kg/sq metre increase in pre-pregnancy body mass index.”

However, it should be noted that a recent paper reported:

“BMI appears to be a fairly weak predictor for pre-eclampsia. Although BMI is virtually free of cost, noninvasive, and ubiquitously available, its usefulness as a stand-alone test for risk stratification must await formal cost-utility analysis. The findings of this review may serve as input for such analyses.”

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