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    Experimental weight loss drug tesofensine causes weight loss of 9.2% with 0.5 mg, 10.6% with 0.5 mg


    Posted by .(JavaScript must be enabled to view this email address)
    Tuesday, May 27, 2008 6:25 am Email this article
    The experimental weight loss drug tesofensine, which inhibits reuptake of noradrenaline, dopamine and serotonin, caused a weight loss of 4.5 percent of body weight more than the placebo at a dose of 0.25 mg, 9.2 percent at a dose of 0.5 mg, and 10.6 percent at a dose of 1 mg as presented on May 16th, 2008 at the 16th European Congress on Obesity as reported by DocGuide.com.

    ““There’s no reason to pursue [a potential dose of 1.0 mg],” Dr. Arne Astrup noted, “because it doesn’t produce much more weight loss, but [it] increases problems,” as he was quoted in the article on DocGuide.com.

    Subjects

    Subjects : 203 obese people, 18-65 yrs-old

    The study involved 203 obese people with a body mass index (BMI) of 30-40 who were 18- to 65-years-old.

     

    Blood Pressure

    Blood pressure increased 2/3 mmHg at a dose of 0.5 mg

    At a dose of 0.5 mg, the drug caused in increase in blood pressure of 2/3 mmHg, and an increase in heart rate of 8 beats per minute.

     

    Adverse Effects

    Adverse effects : 20% dropped out due to side effects in 1 mg group, 8% in 0.5 mg group

    One-fifth of patients (20 percent) given 1 mg dropped out due to side effects compared with 8 percent in the 0.5 mg group and 8 percent in the placebo group.

    Altogether, 29 percent of patients in the 1 mg group did not finish the study compared to 12 percent in the 0.5 mg and 25 percent in the placebo group.

     

    Researchers

    Research lead by Arne Astrup

    The research was lead by world-class obesity researcher, Arne Astrup, MD, who is the Head of the Department of Human Nutrition, The Royal Veterinary and Agricultural University, Faculty of Life Sciences, University of Copenhagen, Frederiksberg, Denmark.

     

    Comment

    Comment : I do not like noradrenaline-reuptake inhibitors

    I do not like noradrenaline-reuptake inhibitors such as Merida (sibutramine), Dulox (duloxetine), Effexor (venfalaxine) or the drug mentioned in this article, tesofensine.

    I believe they cause the adrenaline glands to atrophy with long-term use, which makes getting off these drugs very difficult.

     

    Comment

    Comment : Noradrenaline-reuptake inhibitors may cause the adrenal glands to shrink

    I know someone—I will call him “John”—who took Elavil (amitriptyline) for years for depression.

    When “John” stopped the drug, he became extremely tired, depressed, and even suicidal.

    He could not handle even the smallest amount of stress without feeling completely exhausted.

    John’s doctor first had him try Prozac (fluoxetine) which did not work.

    Then he had him try Zoloft (sertraline) which did not work either.

    Finally, after about 5-6 months, his doctor switched him to Effexor (venlafaxine) which finally helped him to feel better.

    Effexor (venlafaxine) inhibits noradrealine reuptake as well as serotonin reuptake.

     

    Comment

    Comment : Elavil, which inhibits noradrenaline reuptake, causes the adrenal glands to shrink

    When this was happening, I did some research and found that when rats are given Elavil (amitriptyline) on a long-term basis, their adrenal glands to shrink.

    Part of the mechanism of action of Elavil (amitriptyline) is to inhibit noradrenaline reuptake.

    I assume it causes the adrenal glands to shrink because blocking noradrenaline reuptake tells the brain, “Hey brain, I have enough noradrenaline. You can tell the adrenal glands they don’t have to make any more right now.”

    So the adrenal glands get lazy and atrophy—they shrink—just like your muscles will atrophy if you lay around all day, every day and force them to work.

     

    Comment

    Comment : Noradrenaline reuptake is an important source of noradrenaline for the body

    Also of importance, Goodman and Gilman’s Pharmacelogical Basis of Therapeutics, a classic book on pharmacology, notes that noradrenaline reuptake is an important source of noradrenaline for the body.

    Therefore, I assume that blocking noradrenaline reuptake depletes the stores of noradrenaline in the body.

     

    Comment

    Comment : I have not researched the effects of blocking dopamine reuptake or serotonin reuptake

    I have not researched the effects of blocking dopamine reuptake, but I would guess it is similar.

    Nor have I researched the importance of serotonin reuptake either, but I also have concerns about this.

     

    Comment

    Comment : It may be difficult to stop reuptake inhibitors

    I can imagine these drugs might also cause problems for people who have taken them long-term and try to stop.

    Therefore, a drug like tesofensine, the one mentioned in the article above, scares me regarding long-term use.

     

    Comment

    Comment : I much prefer drugs that stimulate noradrenaline and serotonin release combined with the amino acids L-tyrosine and L-tryptophan

    I much prefer drugs such as phentermine and ephedrine which force noradrenaline release, which is the way the body has been working for 5 million years, combined with the amino acid L-tyrosine which is the precursor to dopamine, noradrenaline and adrenaline, and combined with the amino acids L-tryptophan or 5-HTP are the precursors to serotonin, to drugs that inhibit reuptake of noradrenaline, dopamine and serotonin.

    REFERENCE

    Astrup A. The efficacy and safety of tesofensine for weight loss in obese subjects. A 24-week randomised, double-blind, placebo-controlled, danish multi-centre trial. Presented on May 16, 2008 at the 16th European Congress on Obesity.

    Articles on the same subject can be found here:


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