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Archive for August, 2007

Acomplia (Rimonabant) - Investigational Agent for the Management of Obesity

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Under development by Sanofi-Aventis, Acomplia (rimonabant) is a selective CB1 endocannabinoid receptor antagonist indicated for the treatment of obesity.

“Acomplia is a selective CB1 endocannabinoid receptor antagonist.”

It works by blocking endogenous cannabinoid binding to neuronal CB1 receptors. Activation of these receptors by endoegenous cannabinoids, such as anadamide, increases appetite. It is the most advanced endocannabinoid receptor antagonist in clinical development and offers a novel therapeutic approach to appetite control and weight reduction.

Obesity is now the most common nutritional disorder in western industrialised countries and arises from the accumulation of excess fat in the body from over consumption of fatty foods. 

Data from the World Health Organisation’s MONICA project show that in some parts of Europe over 70% of men aged 55-64 years are clinically obese or overweight (BMI >25) and almost 70% of women in this age group. One in five of all Americans is obese and one in three overweight. Furthermore, increasing rates of childhood obesity are likely to exacerbate the trend towards increasing obesity in adulthood.

“The central cannabinoid (CB1) receptors are believed to play a role in controlling food consumption.”

There is a strong association between obesity and increased risk of cardiovascular disease and diabetes and possibly certain cancers, such as breast and colorectal cancer.

The dramatic rise in the incidence of type 2 diabetes is due largely to the increased prevalence of obesity. Increases in body weight lead to changes in blood lipid and cholesterol levels, predisposing to increased risk of atherosclerosis.

THERAPEUTIC APPROACHES TO TREATMENT OF OBESITY

Not surprisingly, the growing prevalence of obesity has stimulated the search for drugs to treat this condition. Various therapeutic strategies have been explored, including:

  • Serotonin and noradrenaline reuptake inhibitors (anorectic agents)
  • Lipase inhibitors
  • ß 3-adrenoreceptor agonists
  • Leptin agonists
  • Melanocortin-3 agonists

Sanofi-Aventis’ approach is completely different to the above. It developed from the knowledge that cannabis smokers often experience extreme hunger pangs, which cannabis smokers refer to as “the munchies”. Sanofi-Aventis worked on the premise that if cannabinoids stimulate appetite, blocking cannabinoid receptors in the brain might reduce appetite.

The central cannabinoid (CB1) receptors are believed to play a role in controlling food consumption and the phenomena of dependence / habituation. To develop suitable drugs against this target, the human cannabinoid receptor was first cloned and then expressed in cells.

Compounds with potential inhibitory activity against this receptor were then screened for inhibitory activity. Rimonabant emerged from this screening process as a potent CB1 receptor antagonist. Preclinical animal studies subsequently showed that it could reduce consumption of fats and sugars, which contribute to weight gain.

PHASE III DATA HIGHLIGHT EFFICACY AND SAFETY

The promising preclinical findings with Acomplia (rimonabant) have been confirmed in a series of clinical studies, including pivotal phase III trials involving over 6,000 obese subjects that were carried out in both the US and Europe.

Two-year data from the phase III multicentre Rimonabant In Obesity (RIO) trials, which compared rimonabant at doses of 5mg and 20mg with placebo with respect to weight reduction and prevention of weight gain, showed that the positive results seen after a year’s treatment were sustained over the full two-year trial period.

“There is a strong association between obesity and increased risk of cardiovascular disease, diabetes and possibly certain cancers.”

Consistent with the one-year data, the results showed that overweight and obese patients taking rimonabant 20mg/d achieved significant reductions in body weight, waist circumference (an indicator of abdominal obesity) and improved lipid and glycaemic profiles compared with placebo recipients. Rimonabant also had a significant impact on metabolic CVD risk factors, greater than that expected by weight loss alone.

Efficacy and safety in long-term use is important feature of any antiobesity drug. Some potential antiobesity medications have proved effective in the first six months of treatment only to lose effectiveness as subjects develop resistance to treatment.

Data from the RIO trials suggest rimonabant is effective for maintaining weight loss for periods of at least two years. Long-term safety is also a major concern. In the US, the FDA generally requires two years of safety data before approving antiobesity drugs.

Results from the phase III RIO trial programme suggest rimonabant is well tolerated in long-term use. Among patients who were randomly assigned to continue their first-year treatment for a second year, 6.7%, 8.3% and 6.0% discontinued from the placebo, rimonabant 5mg and 20mg groups respectively.

The ongoing phase IIIb trial programme for rimonabant includes studies in patients with diabetes (SERENADE), dyslipidaemia (ADAGIO) and cardiovascular disease (STRADIVARIUS, AUDITOR, CRESCENDO).

“There is a strong association between obesity and increased risk of cardiovascular disease, diabetes and possibly certain cancers” so Buy Acomplia for TREATMENT OF OBESITY now !

Clinical Tests of Acomplia

The use of Acomplia as a treatment to aid weight loss received a letter of approval from the FDA . It also has passed other testing as well. All this testing has been going on for some time, as described below. However, on February 17, 2006, the FDA declined to issue final approval in early 2006 as hoped until a number of issues were resolved.

Recent Testing Developments

Obesity is now the most common nutritional disorder in western industrialised countries. Defined as a body mass index of greater than 30, it arises from the accumulation of excess fat in the body from over consumption of fatty foods. Prevalence of obesity in the US and Europe has reached epidemic levels.

In March, 2006, compiled data from four trials that were part of the “Rimonabant (Acomplia/Zimulti) in Obesity and Related Metabolic Disorders” (RIO) program was released. Surprisingly, Acomplia’s beneficial effect on blood sugars and fats went 57 percent beyond the benefit that would have been expected from weight loss alone. The drug, which affects the body’s cannabinoid system, appears to reduce interrelated risks for heart and metabolic diseases.

The Rimonabant In Obesity (RIO) Study

The RIO study involved more than 6,000 patients worldwide. Results from the RIO programme demonstrated that one Acomplia 20 milligram tablet taken every day significantly decreased weight and waist circumference, HbA1c, and triglycerides and increased HDL-cholesterol levels. Importantly, the label granted by the European Commission states that an estimated 50 percent of the observed improvements in HbA1c, HDL-cholesterol and triglycerides were beyond that expected from weight loss alone.

The RIO study was conducted in several global locations. The primary focus was measuring weight loss after one year of Acomplia intake with a controlled diet. The secondary focus was on risk factors related to obesity and metabolism.

The primary objective of the trial was to assess weight loss over one year, and then to determine the ability of Acomplia to prevent regaining weight during a second year of treatment. Results were positive and researchers concluded that safety concerns were minimal.

Acomplia works by selectively targeting and blocking the CB1 receptors, helping normalize the over-activation of the EC system and making hunger or cigarette pangs more manageable.

In the RIO-Lipids trial, weight loss was accompanied by a decrease in waist size of 3.4 inches demonstrating a significant reduction in abdominal obesity, an independent marker for heart disease.

Dramatic improvements also were reported in lipid profile with a 23% increase in HDL-cholesterol (good cholesterol) and a 15% decrease in triglycerides. Improvements in glucose tolerance and insulin levels were also reported. Approximately half of the patients diagnosed at the start of the study with metabolic syndrome, who received the higher 20 mg daily dose of Acomplia, no longer had this condition at the conclusion of the trial.

Alcohol Use Reduction

In March, 2006, the National Institute on Alcohol Abuse and Alcoholism (NIAAA) began recruiting participants for a test on the possible use of rimonabant to reduce alcohol consumption.

This research shows patients who took 20 mg rimonabant (Acomplia/Zimulti) for 1 year were then re-randomized to either continue on rimonabant (Acomplia/Zimulti), or to switch to placebo. Patients who stayed on rimonabant for the second year did not lose additional weight, while those switched to placebo gained weight. At the end of 2 years, patients who took rimonabant for one year and placebo for the second year had about the same amount of overall weight loss as patients who took placebo from the beginning.

 

Acomplia Information

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Widely proclaimed as the ultimate weight loss pill by manufacturer Sanofi-Aventis, Acomplia was released for sale in the UK on a prescription only basis on 21st June 2006. Acomplia is different from most other weight loss pills available in the market today in the sense that it does not act on any of the known weight gain factors but uses a totally different approach for weight loss. Acomplia acts on the Endocannabinoid system in the brain. You can buy Acomplia online in 20 mg tablets on the prescription of a certified doctor from www.rimonabant-acomplia.co.uk.

  How does Acomplia work?Acomplia attacks and reduces a person’s urge or craving to eat more. Acomplia has the active ingredient Rimonabant which works directly on the Endocannabinoid system. This system affects energy balance, glucose and lipid metabolism in addition to weight in the human body. Rimonabant blocks certain receptors in this system known as cannabinoid receptors and thereby creates a feeling of false fullness in the person on Acomplia. As a result the person will eat less. When used in conjunction with a calorie reduced diet and regular exercise, Acomplia will lead to significant weight loss in obese patients.

How much weight can I lose by taking Acomplia?

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Exhaustive clinical trials conducted with Acomplia on more than 6800 patients yielded substantial results. Patients given Acomplia for a period of one year achieved an average weight loss of six and half kg as compared to just over one and half kg achieved by those on placebo. Most of the weight loss was achieved in the first 9 months of the trial with Acomplia.

Acomplia was also found to reduce the risk of regaining weight. When a group of patients from one of the clinical trials was re-randomized and split into Acomplia and placebo groups, those patients who continued on Acomplia achieved a total weight loss of 7.5 kg over the two year trial period. On the other hand patients who were transferred to placebo achieved a much lower weight loss of only 3.1 kg over the same period.

The best part about Acomplia is that it brings about sizeable reduction in the waist circumference – nearly 6 to 7 cm on an average. This measure is an indication of intra-abdominal fat and is believed to be more important that BMI. If you have a large waist circumference, you should buy Acomplia for reducing it.

Buy Rimonabant (Acomplia)Online

Rimonabant (Acomplia), discovered and developed by French pharmaceutical company Sanofi-Synthelabo, is a new drug thas has shown great promise in trials for the treatment of obesity and related metabolic risk factors. Rimonabant is already on the market in Europe, being sold under the trade name Acomplia and under the name as Zimulti in USA.

How Acomplia/Rimonabant/Zimulti Works?

Acomplia works by selectively targeting and blocking the CB1 receptors, helping normalize the over-activation of the EC system and making hunger or cigarette pangs more manageable.

In the RIO-Lipids trial, weight loss was accompanied by a decrease in waist size of 3.4 inches demonstrating a significant reduction in abdominal obesity, an independent marker for heart disease.

Dramatic improvements also were reported in lipid profile with a 23% increase in HDL-cholesterol (good cholesterol) and a 15% decrease in triglycerides. Improvements in glucose tolerance and insulin levels were also reported. Approximately half of the patients diagnosed at the start of the study with metabolic syndrome, who received the higher 20 mg daily dose of Acomplia, no longer had this condition at the conclusion of the trial.

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Acomplia Rimonabant has been approved as a new weight loss drug in a lot of European countries. It is available in many European countries and can be bought online by the consumers from US.

Buying Rimonabant Acomplia helps you to treat obesity but this new class weight loss drug Rimonabant Acomplia is not yet approved for smoking cessation. It is still waiting for the approval from European union for smoking cessation.

 

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What is Rimonabant?

Rimonabant is the antismoking, slimming super-drug for the new generation. Rimonabant (Acomplia) helps in losing weight. Approximately two thirds of the U.S. adults have been found to be overweight or obese, which greatly increases the risk of developing diabetes mellitus and cardiovascular disease and death from related causes.

The number of people who are obese is rising at a very fast rate. About 1.2 billion people in the world are overweight and at least 300 million of them are obese, even though obesity is said to be one of the 10 most preventable health risks, according to the findings of World Health Organization.

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What is Rimonabant?

Rimonabant is the antismoking, slimming super-drug for the new generation. Rimonabant (Acomplia) helps in losing weight. Approximately two thirds of the U.S. adults have been found to be overweight or obese, which greatly increases the risk of developing diabetes mellitus and cardiovascular disease and death from related causes.

The number of people who are obese is rising at a very fast rate. About 1.2 billion people in the world are overweight and at least 300 million of them are obese, even though obesity is said to be one of the 10 most preventable health risks, according to the findings of World Health Organization.

If you are one of them - it’s high time you Order Rimonabant online.

How does it work?

In a human body there are nerve receptors that exist in the brain and fat cells. These receptors urge the body to overeat (and/or intake nicotine). Rimonabant blocks signals of these receptors and stops them from telling us to overeat. Overeaters and addicted smokers have very active receptors of this kind. By blocking the signals, the overeater or nicotine addict does not have the same urge to eat or smoke. There is no other drug like it - one that helps you stop smoking and overeating.

Benefits of Rimonabant

Rimonabant’s benefits are by helping to reduce appetite, and thus help those who use the drug lose weight. There is also hope that Acomplia will help the health of patients in other ways. There is also evidence that it helps with lipid levels (such as cholesterol) in the blood and might help with other metabolism-related health problems, as well as help smokers quite smoking.

Weight LossSome test results have indicated that Acomplia can positively affect a variety of risk factors for human cardiovascular problems. These include levels of cholesterol and trigylcerides in the blood, insulin, haemoglobin and adinopectin levels. Rimonabant has been shown in some studies to increase “good” cholesterol. Triglyceride levels have also dropped. “Good” cholesterol levels went up more than 40%, relative to what would be expected from weight loss alone. Other risk factors, such as adinopectin, a protein that interacts with the body’s action dependent on insulin, also changed favourably

Side Effects of Rimonabant

Side effects are minor and temporary, the most frequent being diarrhoea, nausea, vomiting and dizziness. Some anticipated side effects, especially depression, did not materialize. Nausea occurred in 13% of patients, vs. in 4% of those who got placebo. Anxiety and diarrhoea slightly occurred at a higher rate in patients taking Rimonabant. Depression and anxiety scores as measured by the Hospital Anxiety and Depression (HAD) scale. Rimonabant was found to increase blood pressure even as it facilitated weight loss.

 

Rimonabant (Acomplia) for Obesity

Buy Rimonabant Acomplia - an anti obesity drug for quick weight loss online. Some tests of Rimonabant conducted on humans since last two years have shown significant results on losing weight through rimonabant acomplia pill.

In the most recent trial of rimonabant acomplia, 1507 overweight and obese 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, and also improvement in lipid profiles, compared to patients on placebo. (Those taking 5 mg of Rimonabant doses also had more weight loss than placebo patients, but the magnitude of weight loss was much less.) In addition, waist measurements significantly improved in rimonabant acomplia patients. There are so many advantages of rimonabant to know.

In the first study of Rimonabant Acomplia, designed to measure the drug’s ability to induce weight loss, 44% of patients who took rimonabant acomplia for 1 year lost more than 10% of their body weight.

Furthermore, Patients treated with rimonabant acomplia tended to have increased HDL cholesterol levels (i.e., the “good” cholesterol) and reduced triglyceride levels.

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POSSIBLE SIDE EFFECTS

Like all medicines, Acomplia can cause side effects, although not everybody gets them.

Very common side effects, that affect more than 1 per 10, have occurred in patients on Acomplia include:

* nausea and upper respiratory tract infection

Common side effects, that affect more than 1 per 100 but less than 1 per 10, that have occurred in patients on Acomplia include:

* upset stomach, vomiting, trouble with sleeping, depression, irritability, dizziness, diarrhea, anxiety, itching, excessive sweating, muscle cramps or spasm, fatigue, bruising, tendon pain and inflammation (tendonitis), memory loss, back pain (sciatica), altered sensitivity of the hands and feet, hot flush, fall, influenza, and joint sprain.

Uncommon side effects, that affects less than 1 per 100 but more than 1 per 1000, that have occurred in patients on Acomplia include:

* sleepiness (lethargy), night sweats, panic symptoms, hiccups, anger, restlessness (dysphoria), emotional disorder.

Rare side effects, that affect less than 1 per 1000, that have occurred in patients on Acomplia include:

* hallucinations

If any of the side effects gets serious, or if you notice any side effects not listed in this leaflet, please tell your doctor or pharmacist.

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Rimonabant Acomplia News

Obesity management is the technique of burning extra fat which is accumulated beneath your skin.
Your body itself can burn accumulated fat, unfortunately, it does not do so. It is not your entire body but a part of your nervous system which is responsible for it. This part is known as endo-cannabinoid receptor type-1. This receptor is present in every nerve cell and it works as a messenger. It receives signals of appetite from various cells of the body and takes these signals to the brain. With the gradual growth of weight there is always an increasing demand for food in the body. More demand means more acute signaling of hunger to the brain. Acute and subsequent signals of hunger pressurize the brain to eat excess food.

Inhibit the working of endo-cannabinoid type-1 (CB-1) receptor and you can break the supply line of extra calorie in your body. The benefit of this process is great; in the absence of extra calories your body can burn the accumulation of the already present fat in the body. There is one more advantage of blocking the functioning of CB-1 receptor; with appetite suppression it can curb the urge for smoking. Acomplia is the only medication, which inhibits the working of CB-1 receptor. Sanofi-Aventis, the manufacturer of Acomplia, has already launched it in seven European countries.
Obese in the UK, Germany, Austria, Denmark, Finland, Norway and Ireland are presently getting the benefits of Acomplia.

Acomplia is also known as Rimonabant, because this compound is the prime active ingredient of the medication. Acomplia (Rimonabant) should be taken only on a doctor’s prescription. Acomplia pills are available in the volume of 10mg and 20mg. The doctor generally prescribes the later mentioned volume of Acomplia for usage. The general dosage of Acomplia is one pill of the prescribed volume of medication daily with a glassful of plain water. Acomplia is effective only when it is taken only on an empty stomach, it should be taken an hour before breakfast. Strictly avoid overdosing of Acomplia as it can be harmful for your body.
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What is Acomplia ?

Accomplia is such a wonder drug that preliminary trials have shown that 33% of people who were put on Acomplia lost 10% of weight and could maintain that for two years. Acomplia also helped to quit smoking and in promoting healthy lipid levels thus protecting the cardiovascular system

A weight loss of 5 to 10% can help in reducing risks of obesity-related diseases and delay/prevent type 2 diabetes in persons with high risk. Obesity is nowadays a very common nutritional disorder owing to today’s stress filled lives in western countries. A person with Body mass index is said to be obese.

As well as keeping you lean, the drug also acts as antismoking drug. This will be of great interest for many smokers as they say they will put on loads of weight if they do (usually young female smokers worry about this the most).

A single pill has been found to stop both food and cigarette cravings enough to help people quit smoking and lose weight, and could also help curb other unhealthy urges. Named Acomplia the drug in one study helped people who were overweight drop an average of 20 pounds and in another doubled the chances that smokers would quit. Acomplia is made by French firm Sanofi-Synthelabo and the company says it could be available as early as 2006. Acomplia contains the active ingredient Rimonabant.

How Acomplia works?

Human’s have nerve receptors in the brain and fat cells which prompt us to overeat or indulge in smoking. Acomplia blocks the signals these receptors give out to the brain thus decreasing the wish to eat more or do more smoking. Overeater’s and addicted smokers have very active receptors of these type which are blocked from informing the brain to carry out a particular operation.

Rimonabant (which will be brought to market as Acomplia) works by blocking the CB1 receptor, one of two receptors found in a newly described physiological system called the Endocannabinoid System (EC System), believed to play a critical role in the regulation of food intake and energy expenditure.

Researchers wondered whether a drug that halted this action might curb appetite, and in 2001, the first animal study was conducted at the National Institute of Alcohol Abuse and Alcoholism in Bethesda, Md.

In the study, genetically altered mice that lacked cannabinoid receptors ate less than their litter mates, even after 18 hours of fasting. When the normal mice were given rimonabant, which blocked their CB1 receptors, the mice reduced their food intake.In 2002, Sanofi-Synthelabo began human testing.

Acomplia works by selectively targeting and blocking the CB1 receptors, helping normalize the over-activation of the EC system and making hunger or cigarette cravings more manageable.

This blocking of signals that control cravings appears to result in weight loss, improvement of cardiovascular/ metabolic risk factors in overweight/obese patients and appears to reduce tobacco dependence without post cessation weight gain in people who smoke.

Advantages and side effects :

Advantages of Acomplia  include weight loss, easiness in quitting smoking or reduction in smoking and lowering of cardiovascular risk.
Acomplia was said to be well tolerated in early tests. The only relatively common side effects were mild GI side effects and dizziness, and these were said to be transient.

Acomplia has certain minor side effects. Nausea, headache, irritability and dizziness are certain side effects you should expect when you order Acomplia online. However, these side effects are transient in nature and will go away once your body adjusts to the medication.
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Acomplia is such a wonder drug that preliminary trials have shown that 33% of people who were put on Acomplia lost 10% of weight and could maintain that for two years. Acomplia also helped in promoting healthy lipid levels thus protecting the cardiovascular system

A weight loss of 5 to 10% can help in reducing risks of obesity-related diseases and delay/prevent type 2 diabetes in persons with high risk. Obesity is nowadays a very common nutritional disorder owing to today’s stress filled lives in western countries. A person with Body mass index of 30 or more is said to be obese.

Obesity is posing a great threat to several patients suffering these weight related disease. There can be serious consequences as well. Obesity can cause problems not only for adults but also young people, such as hypertension (high blood pressure), high cholesterol levels, liver disease, and type 2 diabetes (a disease in which the body has trouble converting food to energy resulting in high blood sugar levels). People who are obese are more likely to develop heart disease, congestive heart failure, bladder problems, and, in women, problems with the reproductive system. Obesity can further lead to stroke, greater risk for certain cancers such as breast or colon cancer, and even death.
Can I buy Acomplia online?

You can buy Acomplia online only if you have proper prescription in hand. Your doctor will prescribe you Acomplia only if you have BMI ≥ 30 kg/m2, or are overweight with BMI > 27 kg/m2 with associated risk factors such as type II diabetes or dyslipidemia. Thus, you cannot buy Acomplia online if your doctor does not agree that you are overweight after calculating your BMI or it is risky for you to order Acomplia.

What are the side effects I should expect after I order Acomplia online?

Acomplia has certain minor side effects. Nausea, headache, irritability and dizziness are certain side effects you should expect when you order Acomplia online. However, these side effects are transient in nature and will go away once your body adjusts to the medication.
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Acomplia compared to other weight-loss drugs?

The side-effects of weight-loss-drugs already on the market are quite significant.
Xenial for example can in many cases give severe diarrhea making it impossible for some patients to continue using the drug.
Meridia (Reductil in Europe) was originally a drug meant to treat depressions and can have severe side-effects as well, like high blood pressure, sleeping problems (Insomnia), constipation and dry-mouth syndrome.
Phentermine stimulates the central nervous system, making the body run on “full throttle” all the time.
This causes a lot of strain on many of the body systems and phentermine should therefore not be used for longer periods and only in obesity cases and not for treating common overweight.

How does  Acomplia it work?

Rimonabant (Acomplia), A New Diet Pill To Combat Obesity & Smoking

Human’s have nerve receptors in the brain and fat cells which prompt us to overeat or indulge in smoking. Acomplia blocks the signals these receptors give out to the brain thus decreasing the wish to eat more or do more smoking. Overeater’s and addicted smokers have very active receptors of these type which are blocked from informing the brain to carry out a particular operation.
ACOMPLIA - Advantages and side effects :
Advantages of Acomplis include weight loss, easiness in quitting smoking or reduction in smoking and lowering of cardiovascular risk.

Side Effects include anxiety & Depression, diarrhea, Vomiting, dizziness, Nausea and mood swings

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Acomplia (Rimonabant / Zimulti) is The new weight loss medication breakthrough from Sanofi-Aventis , exceeding Phentermine in it’s ability to help you lose the weight! It is a CB1 cannabinoid receptor antagonist ,and Its main avenue of effect is reduction in appetite. Acomplia acts by obstructing the receptors, which control the food intake and energy expenditure - Thus resulting in reduced appetite. Acomplia also has an added characteristic effect as a smoking cessation aid.