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Tesofensine is a triple reuptake inhibitor that increases the levels of three neurotransmitters in the brain: Serotonin, norepinephrine, and dopamine.
Tesofensine causes a significant increase in weight loss and fat loss by reducing appetite, increasing resting energy expenditure (ie increasing metabolism and calories burned), increasing fat oxidation, and reducing fat tissue.
Tesofensine is an effective weight-loss medication. Studies have shown more weight loss with higher tesofensine doses up to 1 mg. A clinical study found that participants receiving tesofensine at doses of 0.25 mg, 0.5 mg, and 1.0 mg in conjunction with a prescribed diet for 6 months had a mean weight loss of 4.5%, 9.2%, and 10.6%. Comparatively, patients in this study treated with a placebo only lost an average of 2% of their body weight. There was a 4-point drop in BMI in a period of 24 weeks in those treated with 0.5 mg and 1 mg.
Tesofensine has been shown to have a good safety profile and was well tolerated although an increased number of adverse events (e.g., increased heart rate and blood pressure) were observed in the higher dose groups of 0.5 mg and 1.0 mg. Blood pressure and heart rate were increased by 1–3 mmHg and up to 8 bpm, respectively. Other side effects of Tesofensine may include dry mouth, headache, nausea, insomnia, diarrhea, and constipation. Side effects are dose-dependent and are more significant when using higher doses.
The tesofensine dosage range used in studies was 0.25 mg to 1 mg. The weight loss of 9.2% in the 0.5 mg tesofensine dose vs 10.6% in those using the 1 mg tesofensine dose may not justify the dose-dependent increases in side effects. Based on this, the best tesofensine dose for most patients would be 0.5 mg or lower.
Further Reading:
Tesofensine, a novel antiobesity drug, silences GABAergic hypothalamic neurons
Brain Health
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