You might be wondering why bring up Tesofensine when GLP-1 works great, right? Well GLP-1’s are not for everyone especially when you are trying to maintain muscle mass and still want to loose extra “fat,” I would be doing a disservice if I don’t mention this drug as it’s one “hot item” among the bodybuilding community. Read on!
Tesofensine a triple reuptake inhibitor serotonin-noradrenaline-dopamine reuptake inhibitors (SNDRI) which was initially designed to treat neurological disorders such as Parkinson’s disease and Alzheimer’s disease, however it showed limited efficacy on neurogenic disorders and the drug was then orphaned. While on trials overweight participants achieved significant weight loss.
*In September 2007* <www.sciencedirect.com/topics/medicine-and-dentistry/tesofensine#:~:text=In%20September%202007%20NeuroSearch%20reported,loss%20of%206.5%E2%80%9312%25.> “ reported the outcome of a Phase IIb study with Tesofensine for the treatment of obesity. Data from the study in 203 patients showed that 24-weeks’ treatment with tesofensine resulted in a dose-dependent weight loss of 6.5%-12%. Tesofensine was reported to have a good safety profile and was well tolerated”
*How it works?*
By inhibiting the reuptake of these neurotransmitters, there’s more concentration of these neurotransmitters causing several physiological and psychological effects:
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*Serotonin:* An increase in serotonin levels can contribute to an improved mood and a sense of well-being. This may help individuals using Tesofensine experience enhanced emotional stability and potentially reduce emotional eating –
*Noradrenaline:* Increased noradrenaline levels can stimulate the “fight” or “flight” response in the body, which can lead to increased alertness and energy expenditure. This effect may help boost metabolic rate and calorie burning –
*Dopamine:* Dopamine is a key neurotransmitter involved in the rewards and pleasure pathways of the brain. By increasing dopamine levels, Tesofensine may lead to a reduced sense of craving and reward-driven eating behavior.
*Potential Benefits*
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Increased basal metabolic rate due to its reuptake inhibitor on noradrenaline. Noradrenaline can stimulate thermogenesis which is the production of heat by the body. This process involves the activation of brown adipose tissue, commonly referred to as “brown fat”, which is specialized in burning calories to produce heat. Noradrenaline has also been studied on its ability to promote lipolysis, which is the breakdown of stored fat cells that can be used for energy. –
Decreased hunger due to the reuptake of serotonin causing a heightened sense of fullness and satisfaction after meals, ultimately reducing the drive to consume additional calories. –
Decreased mental cravings due to its influence on dopamine, a neurotransmitter critical for the brain’s reward and pleasure pathways. Dopamine plays a pivotal role in the brain’s response to pleasurable experiences, including the consumption of palatable, high calorie foods. By enhancing dopamine activity, Tesofensine reduces the cravings for these rewarding foods. This reduction is scientifically grounded in the notion that elevated dopamine levels can dampen the desire for indulgent food items. –
Tesofensine lowers levels of risk associated with biomarkers such as ‘bad’ cholesterol, its effects on body weight and metabolism can indirectly impact these important cardiovascular risk factors thus improving cardiovascular health (such as atherosclerosis, heart disease and stroke). The findings of the study suggested that individuals who underwent weight loss with Tesofensine experienced a reduction in LDL-C levels. This reduction is particularly significant because it represents an improvement in a key cardiovascular risk factor.
*Potential Side effects*
Dry mouth, headache, nausea, insomnia, increased heart rate, increased blood pressure.
In summary, Tesofensine’s mechanism of action centers on its ability to modulate these neurotransmitter systems in the brain. By inhibiting the reuptake of serotonin, noradrenaline and dopamine, it can influence mood, appetite regulation and energy balance. This ultimately results in a feeling of fullness, reduced cravings and enhanced satiety, making it a proposed option for weight management.
