Thermogenesis, Thermogenic's and fat burning
I decided to do a small write up on fat loss, thermogenesis and Thermogenic?s to help anyone out there who is interested or confused about this topic.
So I will start off with some info for the people who might not know this subject well;
Types of Thermogenesis:
Exercise-associated thermogenesis (EAT)
Non-exercise activity thermogenesis (NEAT)
Diet-induced thermogenesis (DIT)
One of many ways to raise the body?s temperature is through shivering. It produces heat because the conversion of Adenosine-5'-triphosphate ?Some metabolic processes use ATP as an energy source? into kinetic energy causing a rise in temperature.[1]
Another way is though Obligatory (non-shivering) thermogenesis that is when the heat is produced on its own caused by the metabolic rate and that can vary depending on many factors like; the amount of brown fat you have, diet, levels of some hormones or even what supplements you are consuming.
I feel it?s a good thing to have a higher amount of brown fat in the body over white fat because white fat cells contain a single lipid droplet and brown fat contains numerous droplets along with a having much higher number of mitochondria which means it has a much greater need for oxygen and burns more calories (more thermogenic) than white fat. As you can see from Reference study; ?The Origins of Brown Adipose Tissue Sven Enerb?ck, M.D ?[2] It seems those that may happen to have more brown fat would have better fat burning capabilities over those with a greater number of white fat cells.
As a important part of the metabolic rate, thermogenesis can be stimulated to increase energy expenditure and fat burning.
It is not just the amount of white fat vs. brown fat that effects thermogenesis, macro nutrients also have an effect on the Thermogenic response by the body. When a meal is consumed, the metabolic rate increases above the fasting level it was before eating. This rise is referred to as ?specific dynamic action?.[3]
So as you can see thermogenesis happens in many ways with many factors. What I want to talk about in this article are Thermogenic compounds that can help boos the metabolic rate and an inhibitor of down regulation of beta receptors that fits right in with them.
What is a thermogenic compound?
Well ?thermogenic? means to produce heat and is commonly directed at drugs which increase heat through metabolic stimulation.[4]
There are a number of thermogenic compounds out there, but today I will be talking about Clenbuterol, Albuterol, T3 and Ketotifen.
I chose these because they are some of the most well-known and used compounds today in the underground use of Thermogenic?s and fat loss.
There is a lot to know about ANYTHING you put in your body or do tests with to be able to do so safely. You should also understand what it is that is happening in the body when these compounds are used.
Here is some basic information on these compounds followed by how they synergise with each other:
Clenbuterol:
Clenbuterol is a ?2 agonist (Beta-2 adrenergic agonist) with some similarities to epinephrine and Albuterol. Beta-2 stimulants are usually used in the treatment of asthma attacks. Clenbuterol has a much longer lasting active life per dose than Albuterol. It causes an increase in aerobic capacity and it increases the rate that body fat is metabolized while increasing the body's base metabolic rate. It is commonly used for smooth muscle relaxant properties. A smooth muscle is an involuntary muscle like the gastrointestinal tract or respiratory tract. Hence the use for asthma attacks as a bronchodilator.
As you can see form this study; ?Therapeutic dose (20, 40 and 80 micrograms/man) of clenbuterol hydrochloride, a beta 2-adrenergic stimulant, was orally administered to healthy volunteers, and the unmetabolized drug in plasma and urine was determined by enzyme immunoassay. The plasma levels of clenbuterol reached the maximum value of 0.1, 0.2 and 0.35 ng/ml, respectively, in a dose-dependent manner within 2.5 h, which lasted for over 6 h after the administration. The half-life of clenbuterol in plasma was estimated to be about 35 h ?[5] It has a fairly long active life of around 35 hours, so dosing of once a day would seem to be the best. Clenbuterol also seems to have some anti-catabolic or anabolic effects.
Albuterol:
Albuterol is also a Beta-2 adrenergic agonist with some structural similarities to epinephrine and Clenbuterol.
Albuterol?s active life is much shorter lasting than Clenbuterol as you can see from this study; ?Following oral administration of 4 mg albuterol, the elimination half-life was five to six hours ?[6]
So at only 5 or so hours I feel that at least 2X a day dosing to be optimal. Albuterol has had great success and has been used for the treatment of asthma for many years.[7] Albuterol is taken by some as an alternative to Clenbuterol for burning fat. And/or as a performance enhancer because it seems to have some sort of anabolic or anti-catabolic effect as you can see from this snippit from a study; ?Animal and human studies suggest that ?2-adrenergic agonists exert anabolic effects on muscles, inducing and preventing atrophy ? and ?albuterol did not improve global strength or function in patients with FSHD, it did increase muscle mass and improve some measures of strength. ?
This is great news because the use of T3 is known to be catabolic so combine it may lead to more fat loss and less muscle loss.
Triiodothyronine (T3):
The thyroid gland secretes two hormones; thyroxine (T4) and triiodothyronine (T3). T3 is considered the most active and seems to be the most used for fat loss of the two. T4 is converted into T3 by the enzyme deiodinase about 80% of the body's T3 comes from this conversion.[8]
Thyroid hormones play a big role in energy homeostasis and this has been known for well over 100 years, and its been over 70+ years since hormones were first used for weight loss although it seems no one likes to talk about that which I find a bit disturbing. Despite the great length of time these compounds have been known about, exactly how they exert their fat burning effects are not completely understood. Despite clinical studies having shown that the administration of thyroid hormone induces weight loss, it is not currently officially indicated as a weight loss compound.
Regardless triiodothyronine (T3) is a mainstay in the arsenal of compounds used by people for their fat loss goals. The widespread underground use of T3 for fat loss in my oppinon gives a great reason to have an understanding of its mechanism of action and also how it is most effectively and safely used while minimizing any possible side effects.
Ketotifen Fumarate:
Ketotifen is a second-generation non-competitive h1-antihistamine sort of like what cough syrup has in it. The elimination half-life is 12 hours.[9]
Ketotifen is best known for its ability to inhibit the down regulation of beta receptors (adrenergic receptors) caused by some compounds like Clenbuterol or Albuterol.
Clenbuterol and its sister drug Albuterol are usually cycled on and off every 2-3 weeks because they desensitize the receptors they act on to produce their fat mobilizing effect. Ketotifen used with either would allow you to use these fat burning drugs for much longer periods of time without needing to cycle on and off. This is great for a person who wants to do a T3 cycle for a month or maybe six weeks and use Albuterol to enhance T3's fat burning without needing to cycle on and off.
By Adding Ketotifen you could use the Albuterol or Clenbuterol throughout the entire T3 cycle without needing time off due to receptor down regulation.
I feel I have covered the basics on these compounds above and as you can see the Ketotifen could be very useful if used in conjunction with Clenbuterol or Albuterol.
What I love about these compounds is how they work synergistically together for better overall results.
T3 alone might cause more muscle loss then wanted while losing fat with its use, but stacked with Albuterol which seems to have some sort of anabolic or anti-catabolic effect would minimize this along with adding to the total fat loss. Add in Ketotifen and now you can have a long successful fat loss cycle of Clen or Albut with Keto and T3!
Keto would make you able to run the Albuterol or Clenbuterol the whole time while taking the T3 without needing a break. This as mentioned above would lead to less lost muscle, longer duration of effectiveness and MORE total fat loss! It's a win win.
OH but wait it seems Keto might ALSO have some anabolic/anti-catabolic effect! It is used by people suffering from AIDS or cancer to prevent muscle wasting caused due to a large extent by TNF-alpha. In one study involving AIDS patients, ?combining Ketotifen and oxymetholone showed that 18 out of 22 patients gained an average of 11.4 pounds after treatment of an average of 3.9 weeks.?[10]
TNF-alpha has also been implicated as a cause in insulin resistance; Ketotifen could potentially improve insulin sensitivity in muscle. (R-ALA is so popular for this same reason)
Like the hypothalamic-pituitary-gonadal axis (Think testies), the thyroid gland is under negative feedback control when thyroid levels are too high above normal. When T3 levels go up, TSH secretion goes down. This is the mechanism where exogenous thyroid hormone suppresses natural thyroid production.
There is a difference though between the way anabolic steroids would suppress your testosterone production and the way T3 suppresses the thyroid. With steroids like testosterone or deca, the longer and heavier the cycle is, the longer/harder your natural testosterone may be suppressed. This does not seem to be the case with using exogenous thyroid hormone.
There is a well known study that looked at thyroid function and recovery under the influence of exogenous thyroid hormone. This was undertaken by Greer- ?In 1951, Greer reported the pattern of recovery of thyroid function after stopping suppressive treatment with thyroid hormone in normal subjects based on sequential measurements of their thyroidal uptake of radioiodine, He further observed that thyroid function returned as rapidly in those subjects whose glands had been depressed by several years of thyroid medication as it did in those whose gland had been depressed for only a few days ?
So you see these compounds can be used safely and effectively for aiding fat loss without much risk of the compounds are understood.
I hope that I have shed some light on these compounds for those of you out there that are not well versed in this area.
There is a lot of debate of course on what is ?the best way? to use/cycle these. But the basics are the same regardless and along the same lines when used properly.
An example of a possible cycle for fat loss would be as follows:
wk1-6 T3 (wk1-2 25mcg ed/wk3-6 50mcg ed)
wk1-6 Albuterol 7-10mg 2X a day (or 20mg 1X a day but 2X seems best)
wk2-6 Keto 1mg ed (I recommend just before bed time, as it may make you sleepy)
With something like that (and proper diet of course) VERY good fat loss results can be had.
I look forward to implementing another article with thermogens + aas and or peptide cycles for optimal results in gains and fatloss, so look out for that along with other topics I plane to work on over the coming months.
I have seen a lot of questions about fat burners and cutting recently (spring time I guess HA) and a lot of people just simply don't seem to understand how this stuff works and just seem to want dosing information.
Well I feel to do things safely you should know what the compound are doing, not just what some guy tells you is the dosage it to take. So with this small article I hope I have helped someone out there understand these compounds, there effects and how to make the most of it all safely.
Thank you for reading!
References:
1) Enzyme-Catalyzed Phosphoryl Transfer Reactions Annual Review of Biochemistry
Vol. 49: 877-919 (Volume publication date July 1980) J R Knowles Enzyme-Catalyzed Phosphoryl Transfer Reactions - Annual Review of Biochemistry, 49(1):877
2) The Origins of Brown Adipose Tissue Sven Enerb?ck, M.D., Ph.D. N Engl J Med 2009; 360:2021-2023May 7, 2009 MMS: Error
3) IJSNEM Volume 13, Issue 3, September, The Effect of Resistance Exercise on the Thermic Effect of Food, The Effect of Resistance Exercise on the Thermic Effect of Food
4) Clapham, J. C. and Arch, J. R. S. (2007), Thermogenic and metabolic antiobesity drugs: rationale and opportunities. Diabetes, Obesity and Metabolism, 9: 259?275. Thermogenic and metabolic antiobesity drugs: rationale and opportunities - Clapham - 2006 - Diabetes, Obesity and Metabolism - Wiley Online Library
5) J Pharmacobiodyn. 1985 May;8(5):385-91. ?Pharmacokinetics of plasma and urine clenbuterol in man, rat, and rabbit.? Yamamoto I, Iwata K, Nakashima M. Pharmacokinetics of plasma and urine clenbu... [J Pharmacobiodyn. 1985] - PubMed - NCBI
6) Albuterol Sulfate Albuterol Sulfate (Albuterol Sulfate Inhalation Solution) Drug Information: Clinical Pharmacology - Prescribing Information at RxList
7) J Bryan, Pharmaceutical Journal, 13 Oct 2007, vol. 279, no. 7473, p. 404-405
8) Deiodinases: implications of the local control of thyroid hormone action Antonio C. Bianco and Brian W. Kim Deiodinases: implications of the local control of thyroid hormone action
9) Grahn?n, A., L?nnebo, A., Beck, O., Eckern?s, S.-?., Dahlstr?m, B. and Lindstr?m, B. (1992), Pharmacokinetics of ketotiffn after oral administration to healthy male subjects. Biopharm. Drug Dispos., 13: 255?262 Pharmacokinetics of ketotiffn after oral administration to healthy male subjects - Grahn[]n - 2006 - Biopharmaceutics & Drug Disposition - Wiley Online Library
10) GMHC Treat Issues. 1995 May;9(5):7-8, 12. Other therapies for wasting. Other therapies for wasting. [GMHC Treat Issues. 1995] - PubMed - NCBI
I decided to do a small write up on fat loss, thermogenesis and Thermogenic?s to help anyone out there who is interested or confused about this topic.
So I will start off with some info for the people who might not know this subject well;
Types of Thermogenesis:
Exercise-associated thermogenesis (EAT)
Non-exercise activity thermogenesis (NEAT)
Diet-induced thermogenesis (DIT)
One of many ways to raise the body?s temperature is through shivering. It produces heat because the conversion of Adenosine-5'-triphosphate ?Some metabolic processes use ATP as an energy source? into kinetic energy causing a rise in temperature.[1]
Another way is though Obligatory (non-shivering) thermogenesis that is when the heat is produced on its own caused by the metabolic rate and that can vary depending on many factors like; the amount of brown fat you have, diet, levels of some hormones or even what supplements you are consuming.
I feel it?s a good thing to have a higher amount of brown fat in the body over white fat because white fat cells contain a single lipid droplet and brown fat contains numerous droplets along with a having much higher number of mitochondria which means it has a much greater need for oxygen and burns more calories (more thermogenic) than white fat. As you can see from Reference study; ?The Origins of Brown Adipose Tissue Sven Enerb?ck, M.D ?[2] It seems those that may happen to have more brown fat would have better fat burning capabilities over those with a greater number of white fat cells.
As a important part of the metabolic rate, thermogenesis can be stimulated to increase energy expenditure and fat burning.
It is not just the amount of white fat vs. brown fat that effects thermogenesis, macro nutrients also have an effect on the Thermogenic response by the body. When a meal is consumed, the metabolic rate increases above the fasting level it was before eating. This rise is referred to as ?specific dynamic action?.[3]
So as you can see thermogenesis happens in many ways with many factors. What I want to talk about in this article are Thermogenic compounds that can help boos the metabolic rate and an inhibitor of down regulation of beta receptors that fits right in with them.
What is a thermogenic compound?
Well ?thermogenic? means to produce heat and is commonly directed at drugs which increase heat through metabolic stimulation.[4]
There are a number of thermogenic compounds out there, but today I will be talking about Clenbuterol, Albuterol, T3 and Ketotifen.
I chose these because they are some of the most well-known and used compounds today in the underground use of Thermogenic?s and fat loss.
There is a lot to know about ANYTHING you put in your body or do tests with to be able to do so safely. You should also understand what it is that is happening in the body when these compounds are used.
Here is some basic information on these compounds followed by how they synergise with each other:
Clenbuterol:
Clenbuterol is a ?2 agonist (Beta-2 adrenergic agonist) with some similarities to epinephrine and Albuterol. Beta-2 stimulants are usually used in the treatment of asthma attacks. Clenbuterol has a much longer lasting active life per dose than Albuterol. It causes an increase in aerobic capacity and it increases the rate that body fat is metabolized while increasing the body's base metabolic rate. It is commonly used for smooth muscle relaxant properties. A smooth muscle is an involuntary muscle like the gastrointestinal tract or respiratory tract. Hence the use for asthma attacks as a bronchodilator.
As you can see form this study; ?Therapeutic dose (20, 40 and 80 micrograms/man) of clenbuterol hydrochloride, a beta 2-adrenergic stimulant, was orally administered to healthy volunteers, and the unmetabolized drug in plasma and urine was determined by enzyme immunoassay. The plasma levels of clenbuterol reached the maximum value of 0.1, 0.2 and 0.35 ng/ml, respectively, in a dose-dependent manner within 2.5 h, which lasted for over 6 h after the administration. The half-life of clenbuterol in plasma was estimated to be about 35 h ?[5] It has a fairly long active life of around 35 hours, so dosing of once a day would seem to be the best. Clenbuterol also seems to have some anti-catabolic or anabolic effects.
Albuterol:
Albuterol is also a Beta-2 adrenergic agonist with some structural similarities to epinephrine and Clenbuterol.
Albuterol?s active life is much shorter lasting than Clenbuterol as you can see from this study; ?Following oral administration of 4 mg albuterol, the elimination half-life was five to six hours ?[6]
So at only 5 or so hours I feel that at least 2X a day dosing to be optimal. Albuterol has had great success and has been used for the treatment of asthma for many years.[7] Albuterol is taken by some as an alternative to Clenbuterol for burning fat. And/or as a performance enhancer because it seems to have some sort of anabolic or anti-catabolic effect as you can see from this snippit from a study; ?Animal and human studies suggest that ?2-adrenergic agonists exert anabolic effects on muscles, inducing and preventing atrophy ? and ?albuterol did not improve global strength or function in patients with FSHD, it did increase muscle mass and improve some measures of strength. ?
This is great news because the use of T3 is known to be catabolic so combine it may lead to more fat loss and less muscle loss.
Triiodothyronine (T3):
The thyroid gland secretes two hormones; thyroxine (T4) and triiodothyronine (T3). T3 is considered the most active and seems to be the most used for fat loss of the two. T4 is converted into T3 by the enzyme deiodinase about 80% of the body's T3 comes from this conversion.[8]
Thyroid hormones play a big role in energy homeostasis and this has been known for well over 100 years, and its been over 70+ years since hormones were first used for weight loss although it seems no one likes to talk about that which I find a bit disturbing. Despite the great length of time these compounds have been known about, exactly how they exert their fat burning effects are not completely understood. Despite clinical studies having shown that the administration of thyroid hormone induces weight loss, it is not currently officially indicated as a weight loss compound.
Regardless triiodothyronine (T3) is a mainstay in the arsenal of compounds used by people for their fat loss goals. The widespread underground use of T3 for fat loss in my oppinon gives a great reason to have an understanding of its mechanism of action and also how it is most effectively and safely used while minimizing any possible side effects.
Ketotifen Fumarate:
Ketotifen is a second-generation non-competitive h1-antihistamine sort of like what cough syrup has in it. The elimination half-life is 12 hours.[9]
Ketotifen is best known for its ability to inhibit the down regulation of beta receptors (adrenergic receptors) caused by some compounds like Clenbuterol or Albuterol.
Clenbuterol and its sister drug Albuterol are usually cycled on and off every 2-3 weeks because they desensitize the receptors they act on to produce their fat mobilizing effect. Ketotifen used with either would allow you to use these fat burning drugs for much longer periods of time without needing to cycle on and off. This is great for a person who wants to do a T3 cycle for a month or maybe six weeks and use Albuterol to enhance T3's fat burning without needing to cycle on and off.
By Adding Ketotifen you could use the Albuterol or Clenbuterol throughout the entire T3 cycle without needing time off due to receptor down regulation.
I feel I have covered the basics on these compounds above and as you can see the Ketotifen could be very useful if used in conjunction with Clenbuterol or Albuterol.
What I love about these compounds is how they work synergistically together for better overall results.
T3 alone might cause more muscle loss then wanted while losing fat with its use, but stacked with Albuterol which seems to have some sort of anabolic or anti-catabolic effect would minimize this along with adding to the total fat loss. Add in Ketotifen and now you can have a long successful fat loss cycle of Clen or Albut with Keto and T3!
Keto would make you able to run the Albuterol or Clenbuterol the whole time while taking the T3 without needing a break. This as mentioned above would lead to less lost muscle, longer duration of effectiveness and MORE total fat loss! It's a win win.
OH but wait it seems Keto might ALSO have some anabolic/anti-catabolic effect! It is used by people suffering from AIDS or cancer to prevent muscle wasting caused due to a large extent by TNF-alpha. In one study involving AIDS patients, ?combining Ketotifen and oxymetholone showed that 18 out of 22 patients gained an average of 11.4 pounds after treatment of an average of 3.9 weeks.?[10]
TNF-alpha has also been implicated as a cause in insulin resistance; Ketotifen could potentially improve insulin sensitivity in muscle. (R-ALA is so popular for this same reason)
Like the hypothalamic-pituitary-gonadal axis (Think testies), the thyroid gland is under negative feedback control when thyroid levels are too high above normal. When T3 levels go up, TSH secretion goes down. This is the mechanism where exogenous thyroid hormone suppresses natural thyroid production.
There is a difference though between the way anabolic steroids would suppress your testosterone production and the way T3 suppresses the thyroid. With steroids like testosterone or deca, the longer and heavier the cycle is, the longer/harder your natural testosterone may be suppressed. This does not seem to be the case with using exogenous thyroid hormone.
There is a well known study that looked at thyroid function and recovery under the influence of exogenous thyroid hormone. This was undertaken by Greer- ?In 1951, Greer reported the pattern of recovery of thyroid function after stopping suppressive treatment with thyroid hormone in normal subjects based on sequential measurements of their thyroidal uptake of radioiodine, He further observed that thyroid function returned as rapidly in those subjects whose glands had been depressed by several years of thyroid medication as it did in those whose gland had been depressed for only a few days ?
So you see these compounds can be used safely and effectively for aiding fat loss without much risk of the compounds are understood.
I hope that I have shed some light on these compounds for those of you out there that are not well versed in this area.
There is a lot of debate of course on what is ?the best way? to use/cycle these. But the basics are the same regardless and along the same lines when used properly.
An example of a possible cycle for fat loss would be as follows:
wk1-6 T3 (wk1-2 25mcg ed/wk3-6 50mcg ed)
wk1-6 Albuterol 7-10mg 2X a day (or 20mg 1X a day but 2X seems best)
wk2-6 Keto 1mg ed (I recommend just before bed time, as it may make you sleepy)
With something like that (and proper diet of course) VERY good fat loss results can be had.
I look forward to implementing another article with thermogens + aas and or peptide cycles for optimal results in gains and fatloss, so look out for that along with other topics I plane to work on over the coming months.
I have seen a lot of questions about fat burners and cutting recently (spring time I guess HA) and a lot of people just simply don't seem to understand how this stuff works and just seem to want dosing information.
Well I feel to do things safely you should know what the compound are doing, not just what some guy tells you is the dosage it to take. So with this small article I hope I have helped someone out there understand these compounds, there effects and how to make the most of it all safely.
Thank you for reading!
References:
1) Enzyme-Catalyzed Phosphoryl Transfer Reactions Annual Review of Biochemistry
Vol. 49: 877-919 (Volume publication date July 1980) J R Knowles Enzyme-Catalyzed Phosphoryl Transfer Reactions - Annual Review of Biochemistry, 49(1):877
2) The Origins of Brown Adipose Tissue Sven Enerb?ck, M.D., Ph.D. N Engl J Med 2009; 360:2021-2023May 7, 2009 MMS: Error
3) IJSNEM Volume 13, Issue 3, September, The Effect of Resistance Exercise on the Thermic Effect of Food, The Effect of Resistance Exercise on the Thermic Effect of Food
4) Clapham, J. C. and Arch, J. R. S. (2007), Thermogenic and metabolic antiobesity drugs: rationale and opportunities. Diabetes, Obesity and Metabolism, 9: 259?275. Thermogenic and metabolic antiobesity drugs: rationale and opportunities - Clapham - 2006 - Diabetes, Obesity and Metabolism - Wiley Online Library
5) J Pharmacobiodyn. 1985 May;8(5):385-91. ?Pharmacokinetics of plasma and urine clenbuterol in man, rat, and rabbit.? Yamamoto I, Iwata K, Nakashima M. Pharmacokinetics of plasma and urine clenbu... [J Pharmacobiodyn. 1985] - PubMed - NCBI
6) Albuterol Sulfate Albuterol Sulfate (Albuterol Sulfate Inhalation Solution) Drug Information: Clinical Pharmacology - Prescribing Information at RxList
7) J Bryan, Pharmaceutical Journal, 13 Oct 2007, vol. 279, no. 7473, p. 404-405
8) Deiodinases: implications of the local control of thyroid hormone action Antonio C. Bianco and Brian W. Kim Deiodinases: implications of the local control of thyroid hormone action
9) Grahn?n, A., L?nnebo, A., Beck, O., Eckern?s, S.-?., Dahlstr?m, B. and Lindstr?m, B. (1992), Pharmacokinetics of ketotiffn after oral administration to healthy male subjects. Biopharm. Drug Dispos., 13: 255?262 Pharmacokinetics of ketotiffn after oral administration to healthy male subjects - Grahn[]n - 2006 - Biopharmaceutics & Drug Disposition - Wiley Online Library
10) GMHC Treat Issues. 1995 May;9(5):7-8, 12. Other therapies for wasting. Other therapies for wasting. [GMHC Treat Issues. 1995] - PubMed - NCBI
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