TABLE OF CONTENTS:
- What is Tesofensine?
- How Does It Work?
- Tesofensine and Dopamine
- Study & Development
- Side Effects
- FAQ (Frequently Asked Questions)
Ever wonder how athletes are able to burn so many calories from fast food? Tesofensine may clue you in on this is possible and even how you can do it yourself. Tesofensine is located in the brain and is mainly used because of its ability to decrease appetite and elevate your basal metabolic rate or how many calories you burn while at rest.
Well, some researchers recently discovered that participants in a prior study trying to find out if tesofensine is effective in treating obesity met all its endpoint goals. This includes a general 5–10% decrease in baseline body weight and a decrease in BMI.
Body fat, visceral body fat, and waist and hip circumference were all decreased in contrast to those receiving the placebo. Read about why Tesofensine could be the answer you’ve been looking for that awesome change that can you can definitely rely on!
What is Tesofensine?
NS2330 or more commonly known as Tesofensine is a presynaptic serotonin-norepinephrine-dopamine reuptake inhibitor that is obviously difficult to understand but the gist of it is this; the body responds by feeling less hungry when these three neurotransmitters are prevented from being reabsorbed by the central nervous system. But here’s the main kicker: Tesofensine predominantly suppresses hunger while also having an impact on fat oxidation and resting energy expenditure. Tesofensine also modulates dopamine in a specific region of the brain, which is thought to impact the pleasure associated with eating.
The effects alone are enough to even consider using this medication! Tesofensine was initially made to treat Parkinson’s and Alzheimer’s diseases. The first few kinds of research on tesofensine for these dangerous diseases, however, came up empty-handed. In the first trials, weight loss was regularly mentioned as a negative outcome, especially in patients who were overweight or obese, the researchers discovered. Finally, research on tesofensine for the treatment of obesity started after the development of the drug for neurological uses was halted. This is unfortunate because it was pretty obvious that the medication was showing signs that it could help lose weight.
How Does It Work?
Tesofensine was initially created to treat Parkinson’s disease because of its capacity to raise dopamine levels. However, a significant “side effect” of weight reduction was frequently observed during clinical trials. The decision was taken to switch the focus of the trials to weight reduction because the substance was found to be less effective than currently available drugs in treating neurodegenerative illness but nearly twice as effective in inducing weight loss.
Tesofensine’s capacity to raise neurotransmitter levels in the brain does not immediately explain how well it can boost sensations of satiety and fullness. This aspect also does not explain how tesofensine might be able to change the energy balance and boost metabolism. It is still unknown why tesofensine is such a successful weight loss supplement.
Tesofensine was once believed to be a well-balanced reuptake inhibitor, raising levels of dopamine, norepinephrine, and serotonin in nearly equal amounts. It transpires that this is untrue. Tesofensine is far more effective than serotonin at raising norepinephrine levels, according to further in-depth research. It increases the levels of both of those neurotransmitters more effectively than dopamine. This distinction could be the reason the medication wasn’t very effective in treating Parkinson’s disease.
However, tesofensine activity is not solely restricted to the neurotransmitters mentioned above. According to research, it also indirectly enhances cholinergic neurotransmission. Naturally, this explains why the medication was initially studied for Parkinson’s disease and raises the possibility that its effects on dopamine may be more complex than currently thought. Tesofensine appears to work through the cholinergic route to enhance cognition, learning, and memory. In the end, this route raises BDNF levels in the brain]. Previous studies have demonstrated that BDNF promotes neuron growth and has positive effects on depressive disorders, cognitive decline, and several neurological problems.
Tesofensine and Dopamine
Let’s first examine why it matters that tesofensine affects dopamine by discussing dopamine adaption. Dopamine is a neurotransmitter that aids in generating sensations of pleasure and satisfaction.
We risk losing these crucial advantages when things are out of balance. Weight gain, obesity, and glucose intolerance can all be brought on by abnormal dopamine transmission. According to estimates, obese people have 70% fewer dopamine receptors than people of normal weight. There are two explanations for this.
It’s possible that obese people have fewer dopamine receptors than average or that their systems are trying to make up for chronically elevated dopamine levels caused by chronic overeating. The regulation of body weight is incredibly detailed and has a variety of very important processes as well as brain activity. In obese individuals, dealing with the lack of dopamine in the body or figuring out different strategies to maintain dopamine may help lessen the temptation to overeat.
Tesofensine inhibits dopamine transporter proteins, prolonging the time that dopamine receptors are activated following activation and enhancing the reward system in the brain. This nootropic also raises levels of the monoamines serotonin and noradrenaline by a similar method of action.
At various sites across the brain, each of these transmitters affects appetite and metabolism in a significant way. Dopamine modulates reward and the “pleasure” sense of food through its action in the nucleus accumbens of the forebrain. The hypothalamus is where the two additional transmitters work to boost metabolism and suppress hunger.
Tesofensine’s distinct action, along with a proper diet and a good lifestyle, can assist obese people to overcome a blunted dopamine response. This may work well with good routine exercise, which also increases dopamine, to help people lose weight.
Study and Development
How efficient is tesofensine for weight loss? According to the results of a highly thorough clinical investigation, tesofensine produces around 12.8 kg of weight loss over the course of six months when given to people with a 300 kcal dietary deficit when administered as a 1 mg dose. Comparing this to a placebo, a significant increase in weight reduction is produced. Tesofensine is two times as effective as the other weight-loss medications that have received FDA approval. In all other clinical trials of drugs that are already on the market, weight loss over 6 months averaged only 3-5 kg. In other words, tesofensine doubles the amount of weight reduction compared to other FDA-approved weight-loss medicines already available.
Tesofensine’s attractiveness as a weight loss supplement extends beyond just its efficiency in several aspects. The drug is also easily given orally over the course of just one day. Clinical trials have also revealed a minimal adverse effect profile, with headaches, difficulty sleeping, and dry mouth as the main side effects. Depending on the dosage, dry mouth and sleep issues are more or less common, though their frequency decreases with continuing use. Therefore, it is possible to considerably limit these adverse effects by starting with a low dose of tesofensine and then increasing it once attenuation has occurred.
Tesofensine is optimal for weight loss when paired with calorie restriction and exercise, according to a study. Studies show that outcomes are still predictable even when tesofensine is administered without suggestions for dietary or exercise adjustments. In one study, males using tesofensine lost weight despite being instructed to maintain their diets and exercise schedules. These males lost roughly 1.8 kg in two weeks as compared to placebo, along with feeling sated, full, and having less of an appetite. Additionally, there was proof that men taking tesofensine while they slept expended a little bit more energy compared to guys taking a placebo.
One noteworthy finding of the tesofensine trial in obesity is the realization that satiety appears to be centrally controlled and, possibly, is harder to change permanently than was previously supposed. Tesofensine therapy drastically affects satiety and hunger, which considerably reduces appetite. Even after losing weight, stopping the medication produces an almost immediate return of the same symptoms. Administration of tesofensine will reestablish their repression. This shows that hunger pangs are longer-lasting and more ingrained than previously assumed, and they may even play a bigger role in weight growth than previously thought. Or, to put it another way, it really isn’t a matter of willpower as some people constantly give off signs that they are not content.
Tesofensine also assists in the process by which the nerves interact with one another, which in turn supports cognitive function. This has been shown to have advantageous effects on a number of cognitive processes, including memory, thinking, and learning. Another study examining the efficacy of tesofensine produced the first clinical proof that the drug considerably enhanced cognitive performance. A rising body of research indicates that obesity is a substantial risk factor for cognitive impairment, particularly in the older population. Tesofensine’s ability to combat obesity may aid in preventing cognitive decline.
Tesofensine is generally well accepted, has few side effects, and functions very similarly to a placebo. At all of the studied doses, there was no appreciable change in blood pressure, although there was a small but statically significant rise in heart rate when testing cardiovascular effects. The following are potential results and advantages for tesofensine users:
- Loss of body weight and a drop in BMI
- alterations in hip and waist measurements
- reduction of body fat
- a reduction in visceral fat
- Reduced levels of triglycerides and very low-density lipoprotein
- reduced insulin
- improved control of glucose metabolism
- Reversibility of type 2 diabetes in its early stages
There are already almost 1,600 individuals using a therapeutic dose of tesofensine for up to a year in the combined clinical safety database from more than 20 clinical trials with the drug, providing solid safety evidence. The FDA has approved it as an orphan medicine.
Side effects from tesofensine are quite rare. There have been a few instances of tesofensine side effects where the patient experienced one of the problems listed below while using the medication. These negative effects weren’t confirmed to be connected to the medication and might not have been caused by using tesofensine at all. Despite this, it was labeled as a tesofensine side effect even though these side effects are extremely rare. Tesofensine’s adverse effects could include the following:
- mouth ache
- higher blood pressure
- higher heart rate
In a double-blind experiment with 203 participants, of whom half received a placebo, those using the active ingredient-containing drug lost 2.0% of body weight, while those taking the placebo saw much less favorable outcomes.
- Average weight loss was 6.5% for those using the lowest dose of 0.25 mg
- 11.2% for those taking the middle dose of 0.5%
- 12.6% for those taking the maximum dose of 1 mg.
In the two groups receiving the maximum dose, the medication caused a 4-point decrease in BMI over the course of 24 weeks.
What is the purpose of tesofensine?
Tesofensine is a triple reuptake inhibitor of dopamine, serotonin, and noradrenaline that was first created by NeuroSearch to treat Parkinson’s and Alzheimer’s diseases.
How long does tesofensine take to start working?
Tesofensine-treated patients also showed the following benefits: a decrease in appetite sensations within a 14-day period, with those receiving treatment expressing a higher degree of satiety and less desire to eat. Reduction in fat tissue and a substantial increase in fat oxidation.
Tesofensine: A peptide or not?
The newest game-changing peptide for weight loss is called tesofensine. Tesofensine functions at the level of the brain as a serotonin-norepinephrine-dopamine reuptake inhibitor by decreasing hunger and raising resting energy expenditure.
Is tesofensine a mood stabilizer?
Tesofensine inhibits the reuptake of serotonin, norepinephrine, and dopamine (SNDRI). A group of psychotropic antidepressants is known as SNDRIs.
Peptides: do they burn abdominal fat?
Growth Hormone Releasing Peptides is the name given to them. The peptides CJC 1295, Ipamorelin, Tesamorelin, Hexamorelin, GHR-2, and GHR-6 are just a handful that will not only boost muscle mass but also efficiently burn visceral fat, which is the fat that covers the belly.
What purposes do peptides serve?
Peptides can be purchased as part of dietary supplements like tablets or protein drinks. They assert that they will aid in muscle rehabilitation, weight loss, and muscular gain.
Tesofensine’s effects and upsides are definitely showcased in the article but the question is is it really worth it? Should you give this a try and stick with it? With tesofensine’s ability to control weight loss together with the recovery of decreased dopamine levels, indicating that at least some of tesofensine’s anti-obesity effects are linked to positive dopamine levels it’s difficult to not ignore this medication.
It is definitely something you should try at least once. Nevertheless, if you’re ever considering this product long-term, you should know that Danish producers Neurosearch are still working on tesofensine. An encouraging step forward is that they are currently meeting with the Food and Drug Administration in the US to determine the specifics of the third stage of clinical testing.
When you want a physique that can put most others to shame, Tesofensine is the answer
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