Contents of this review
- Contrave Background
- Mechanisms : Why antidepressant medications work for weight loss?
- Lipolysis weight loss mechanism
- A note on Stimulants and antidepressants
- How Contrave works?
- Pros of Contrave
- Cons of Contrave
- Diet and Exercise guidelines while using Contrave
- Administration of the drug
Hi, I am Natasha, a blogger and product reviewer of health and anti-aging products and author of this article on Contrave.
In this article, I’ll explain my take on Contrave pills and why I think these pills are not the best product for weight loss, for both men and women.
Although Contrave is marketed as an exciting new pill that shows assurance in being able to act on neurons in the hypothalamus to coalesce into an increased energy output and a loss of appetite, it has its own disadvantages too. The products is not as efficient as it is hyped to be, because it does not target all the hormonal and neurotransmitters’ mechanisms required for effective and long term weight loss.
In my opinion, Phen375 is the best and safe weight loss product available as of now in the market, for both men and women.
Phen375 and Genf20 Plus seem to better weight loss pills and using them together is a great strategy to target all the hormones and neurotransmitters required for weight loss that I mention in this article.
See the Cons of Contrave section below.
A promising new weight loss pill hit the market in 2014 after successful completion of clinical trials on about 4000 obese people. The pill is manufactured by Orexigen Therapeutics, and is called Contrave.
Contrave is a weight loss product that combines Bupropion, an antidepressant medication, with the addiction-treating drug Naltrexone. Both drugs are combined in Contrave in order to aid a reduction in food intake and increase in calorie burning by manipulating the chemicals and neurotransmitters in the human brain.
Instead of trying to block certain certain fats or starches within the body, like carb or fat blocker diet pills do (think Alli , Xenical etc.), Contrave works within the brain’s behavior-reward center to suppress appetite and food cravings.
Read more on how to modify your brain’s behavior-reward center and optimize your hormones comprehensively for weight loss.
During it’s clinical trial, those who took Contrave along with a diet and exercise program lost 9% to 15% of their body weight. Trial patients who were solely on the exercise program lost an average of 5% of their body weight.
The primary use of Contrave is to help with long-term lifestyle changes that assist and reinforce weight loss.
Mechanisms : Why antidepressant medications work for weight loss?
As explained in this comprehensive review on diet pills on ScammedFatty.com, the unconscious mind, hormones, and brain neurotransmitters play a huge role in deciding what your weight and health will be like.
Lets try to understand the mechanism of ‘Contrave’ and why it works and and if there are better options.
The human body makes use of certain hormones and neurotransmitters for carrying out its daily functions. These hormones signal the body to burn or store calories and fat, and expending energy in various activities like running, jogging or mental functions like reading, thinking, writing etc.
The body maintains the balance of these hormones and neurotransmitters, by secreting them from certain cells of the body and brain, and then reabsorbing (or re-uptaking) them on certain parts of brain.
How much of the amount is reabsorbed or re-uptaken, makes the body’s homeostasis system know what are the quantities of the hormones and neurotransmitters present in the body.
Some of these hormones and neurotransmitters are:-
Leptin, the anti-hunger hormone,
Insulin, the anti leptin hormone, Read more on leptin and insulin here
Cortisol, the stress hormone
Human growth hormone, the Master hormone that enhances Lipolysis, breakdown of fat
Functions of hormones and neurotransmitters
So basically, the functions of these hormones and neurotransmitters is to mobilize the brain and body for action and activities and create a systematic balance of fat and muscle in the body needed for survival.
Some of these hormones and neurotransmitters like dopamine, norepinephrine and acetylcholine increase arousal and alertness, promote vigilance, enhance formation and retrieval of memory, focus and attention. They also increase motivation and/or possibly restlessness.
They also increase heart rate and blood pressure, trigger the release of glucose from energy stores, increase blood flow to skeletal muscle, reduce blood flow to the gastrointestinal system, and promotes voiding of the bladder and large intestines.
Among these, Norepinephrine which bupropion in Contrave targets is released lowest during sleep, rises during wakefulness, and reaches much higher levels during situations of stress or danger, in what has been called the fight-or-flight response.
Lipolysis weight loss mechanism
Dopamine and norepinephrine also play a role in Lipolysis. In adipose tissue (i. e., fat cells), an increase in lipolysis, that is, conversion of fat to substances that can be used directly as energy sources by muscles and other tissues.
Stimulants and antidepressants
These are drugs whose primary effects are thought to be mediated by different neurotransmitter systems (dopamine for stimulants, serotonin for antidepressants), but many also increase levels of norepinephrine in the brain.
“Serotonin” is the satisfaction hormone. If you have more serotonin, you are generally more happy and have less urges to indulge in food intake, because you feel full.
The role of leptin and insulin can be understood by understanding the “leptin” and “insulin” resistance, as a major factor behind obesity in America.
Cortisol is related to high stress levels and weight gain. Controlling Cortisol levels, for some patients becomes absolutely necessary for weight loss.
How Contrave works?
Contrave works by inhibiting the re-uptake of neurotransmitter dopamine and minimizing the metabolic degradation of norepinephrine.
Unlike belviq and some other anti-depressant drugs for weight loss, Contrave doesn’t target “serotonin”. It maximizes norepinephrine and dopamine, and has almost no histamine or cholinergic effect at all.
The increased levels of dopamine and norepinephrine provide more energy, motivation, less desire to eat food, and automatically burning more calories with a workout program and in day to day activities, in general.
The overall effect is that the person loses weight. So, all in all Contrave can be named as a breakthrough drug, if not a miracle because it allows the patient to easily refrain from eating, while feeling happy about doing so.
However, the mechanism by which it works is not new and has been well-known and well established previously as well. And there seem to be better options available.
Pros of Contrave
During its late-stage clinical trials, Contrave faired even better than the FDA’s standards. The drug is much less invasive. Throughout its trials, those who took Contrave showed an improved quality of life, without inciting uncomfortable physical side effects.
Patients also felt an improved mental health as well, likely due to Contrave’s ingredient Bupoprion (also called Wellbutrin), which is an antidepressant. According to some experts, it is very likely Contrave will become a benchmark for future prescription diet pills.
Cons of Contrave
1. Contrave does not target the “serotonin” mechanism of losing weight. Increasing “serotonin” levels in the brain has very strong appetite suppressant benefits.
Phen375 is a much better appetite suppressant that also targets the serotonin.
Besides, there is an “appetite suppressant and growth hormone releaser” all in one called Genf20 Plus that contains several diverse ingredients, for example GABA that enhance the serotonin production and the warming-cooling effect.
2. There are equally effective herbal appetite suppressants available in the market that come without side effects like Phen375, which contains ingredients like Trimethylxanthine and L-Carnitine, that work on the dopaminergic and cholinergic systems.
The plus point it Phen375 is also an effective thermogenic fat burner and burns more calories, much like ephedra, only without the side effects of ephedra.
Unlike Contrave, Phen375 is available over the counter without prescription.
3. Contrave does not target the “acetylcholine” neurotransmitter. Acetlylcholine is a very important chemical in the body used in cell signaling and providing more energy. Although dopaminergic actions of Contrave provide good deal of motivation and energy effect, so the person feels lesser requirements of food intake.
Bupropion (wellbutrin) may infact work as anti-cholinergic. Here is the scientific study on this.
However, Acetlylcholine has two very crucial benefits in weight loss that the Contrave diet pill misses on:-
i. It has the potential to make cells perform even when they feel fatigued. It is an excellent appetite suppressant for this purpose, because the cells don’t feel they require energy from the outside. In fact, many bodybuilders are using supplements to increase acetylcholine to enhance their muscle building workouts.
ii. Acetlylcholine decreases somatostatin, an enzyme that decreases the production of human growth hormone, which again causes weight loss. Read more about this here.
So, by blocking somatostatin, Acetlylcholine increases growth hormone levels in the body. And HGH is great for weight loss because it directly influencing lipolysis, and also plays a role in balancing insulin sensitivity.
4. Contrave does not target the issues of leptin and insulin resistance effectively. So, people highly addicted to sugary carbs and fructose may find it difficult to lose weight on this pill.
5. The idea behind Contrave is nothing new and there seems to be some marketing hype. However, using anti-depressants and addiction treating is a more complicated subject than you might expect, as the mechanisms aren’t always clear, and mood disorders themselves can cause weight gain or loss.
These drugs have been reviewed on the Journal of Clinical Psychiatry too, however the free journal is more a platform for advertisements for the drugs companies. Contrave also seems to be a case of good marketing.
Not all products advertised on Journal of Clinical Psychiatry are effective, mostly because they put out “supplements” bound exactly like the main journal which aren’t necessarily peer-reviewed and can be high-end academic commercials for drug companies. Although the main paid journal has some peer reviewed good stuff.
6. One of the downsides to taking Contrave is that it may require an ongoing usage to maintain its effect. Since the pill works by inhibiting the desire to eat, stopping usage of the pill may cause symptoms of overeating and craving to reappear.
7. Moreover, the overall weight loss achieved from taking Contrave is not that significant. It is not a magical weight loss pill.
Healthy eating habits and an active lifestyle are what work best, and what truly achieves weight loss. Compared to Contrave, Phen375 and Genf20 Plus are more safe options and can be considered as long term lifestyle pills.
8. Chronic norepinephrine release using bupropion, the mechanism by which Contrave works may be more potentially toxic than dopaminergic activity. Dopamine based pills and supplements like Phen375 and Genf20 Plus and drugs like Rasagiline and Deprenyl happen to be more safe.
The main active ingredients in Contrave are Bupropion and Naltrexone. Bupoprion has been used as an antidepressant to aid the cessation of smoking. Naltrexone is an opioid antagonist, which acts to bind to and block opioid receptors, aiding with addiction and dependence from alcohol to opioids, as well as smoking.
Diet and Exercise guidelines while using Contrave
Because the medicine does not act on the stomach, it is not necessary to avoid any specific foods while taking Contrave. No particular style or diet need be achieved while on Contrave, simply less eating as a whole. However, it is recommended to combine Contrave with a low-carbohydrate, low-fat diet as did the patients to took the drug during clinical trials. The drug itself will not induce weight loss, it must be combined with exercise and diet to accomplish results.
Administration of the drug
For the first week of taking Contrave, it is recommended only to take one pill in the morning, daily. The tablets are to be swallowed whole and not crushed or chewed.
During the second week of taking Contrave, one tablet is taken in the morning and in the evening.
In the third week, two pills should be taken in the morning, and one in the evening.
Finally, in the fourth week and from then onward, only two pills in the morning and two in the evening are to be taken.
Do not take more than 4 pills in one day. If a dosage is missed, do not take more than one dosage at a time, wait until your next regular time to take the medicine. It is not recommended to consume large amounts of alcohol while taking this drug.
Although Contrave is marketed as an exciting new pill that shows assurance in being able to act on neurons in the hypothalamus to coalesce into an increased energy output and a loss of appetite, it has its own disadvantages too. See the Cons of Contrave section above.
Phen375 and Genf20 Plus seem to better weight loss pills and using them together is a great strategy to target all the hormones and neurotransmitters required for weight loss that we mentioned in this article.
Contrave pill does have very few side effects, much less than competing weight loss drugs. Choosing the route of psychopharmaceuticals over physically acting medicines like Alli etc. will likely become a trend in future weight loss medicines.
Yet, weight loss on Contrave is primarily determinant upon the patient’s diet and exercise programs. The pill may also require ongoing usage in order to maintain results so the attempt by Orexigen Therapeutics, the company behind this drug seems to be to develop a lifestyle pill that will support fitness, diet and weight loss programs.
Contrave is marketed by Takeda and developed by Orexigen Therapeutics and has also been approved for use in Europe.