Ephedrine and caffeine: Little known facts about this dynamic duo

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    Ephedrine and caffeine: Little known facts about this dynamic duo


    Ephedrine and caffeine: Little known facts about this dynamic duo
    by Bryan Hay****

    [NOTE: whenever I talk about taking ephedrine, assume I am also talking about caffeine] Ephedrine has truly moved into the mainstream over the last few years. With the onslaught of Metabo-whatever products in every mall and grocery store, nearly every housewife in America is on it. Today even the term "thermogenic" is a household word. Nevertheless, bodybuilders were the first to put ephedrine to widespread use and it remains today as one of our most important tools in contest prep.

    Despite the widespread use of ephedrine, knowledge about how it works and how best to use it is rare. Even bodybuilders, who should know better, take it haphazardly without any rhyme or reason to their dosing schedule. Sure, most understand the synergistic 1:10 ratio of ephedrine to caffeine, but there is a lot more that can be done to further increase its effectiveness.

    Ephedrine's mechanism of action

    Let's start with ephedrine's basic mechanism of action. Ephedrine is a sympathomimetic, which means it acts to increase sympathetic activity. Why is this important? Because there is a drop in sympathetic activity when you cut calories. When you get a drop in sympathetic activity you get a decrease in metabolic rate and lower rates of lipolysis (fat mobilization). This can play a significant role in why you plateau on long-term diets. The use of ephedrine and caffeine can stave off this drop in metabolic rate and allow fat loss to continue unabated for several additional weeks.

    People often want to compare ephedrine to Clenbuterol. This is fine as long as you realize that they act in different ways. Clenbuterol is a specific beta-2 adrenergic agonist. As such, Clenbuterol interacts directly with beta-2 receptors on muscle and fat tissue. Ephedrine, on the other hand, is not a direct beta-2 agonist. In fact, ephedrine is a poor ligand for the beta-2 receptor. Instead, ephedrine stimulates the release of noradrenaline from sympathetic nerve terminals. The noradrenaline then goes on to interact with muscle and fat cells as a nonspecific adrenergic agonist. This simply means that noradrenaline activates beta-2 receptors, but also other beta-receptors as well as alpha-receptors. So to compare ephedrine and Clenbuterol you must take into account their differences.

    The differences between ephedrine and Clenbuterol are important. For example, Clenbuterol is a very potent beta-2 agonist. As a result, within 14 to 21 days, the beta-2 receptors on muscle and fat cells will be drawn into the cell membrane to reduce their availability to Clenbuterol. Then, if you continue to take it, they will be disassembled all together, leaving you insensitive to Clenbuterol. It then takes at least 2-3 weeks for receptors to replenish themselves on muscle and fat cells. Once again, ephedrine is different with respect to down regulation. Ephedrine, being a much weaker agonist, does not cause rapid desensitization and/or down-regulation of adrenergic receptors. This allows ephedrine to be used effectively for many months. Despite these differences, both drugs should be tapered over the course of several weeks before discontinuing them. If you don't, you will quickly replace the fat you just lost due to an increased appetite and a decreased ability of fat cells to mobilize stored fat.


    Choosing the right diet to use with Ephedrine/Caffeine

    Your diet will also make a difference in what effects ephedrine will produce. Insulin prevents lipolysis. Insulin has been shown to inhibit lipolysis in a phosphatidylinositol 3-kinase- (PI3K) and phosphodiesterase 3B (PDE3)-dependent manner and to stimulate fractional re-esterification of free fatty acids (FFAs), resulting in inhibition of FFA release (1,2). Even in the presence of ephedrine and/or noradrenaline, a high carbohydrate diet will reduce the fat mobilizing effects of ephedrine. This being the case, I generally recommend a low carb diet to get the most out of ephedrine and caffeine. Keep in mind, however, that over time, your body will not respond so well to ephedrine when on a low carb diet. This should not surprise you considering your metabolic rate (reflecting CNS activity) will drop like a led zeppelin on a low carb diet anyway. So, a periodic carb up is helpful in keeping ephedrine's thermogenic properties high. A carb up should last no longer than 2 days. I may be helpful to keep fat low during these two days, or if you must eat fat, make sure it is n-3 and/or n-6 fatty acids.

    How to use ephedrine to keep that hard earned muscle

    You may have heard the Clenbuterol prevents muscle loss during a diet. This is true. Beta-adrenergic stimulation can preserve muscle protein. If you ask your average bodybuilder they will usually tell you that indeed Clenbuterol saves muscle, but ephedrine won't. They are wrong, of course. In studies measuring body composition as well as weight loss, ephedrine has shown the ability to prevent lean tissue loss (3). In a small double blind study lasting eight weeks, two groups of obese women were given either 20 mg ephedrine with 200 mg caffeine (E+C) or placebo (P) three times daily. After eight weeks weight loss was not significantly different between the groups, but the E + C group lost 4.5 kg more body fat and 2.8 kg less fat free mass (FFM). That is a difference of more than six pounds in eight weeks. The expected decrease in 24-hour energy expenditure (EE) seen in the P group was 10% at day 1 and 13% at day 56, but was only 7% and 8% in the treated group. The higher EE in the E +C group was entirely covered by fat oxidation.

    It's no secret that Clenbuterol has potent anabolic effects in animals when used in dosages around 4 mg per kg body weight. What does seem to be a secret is that this effect is dependent on Clenbuterol?s long and steady activation of the beta receptors (4). The half-life of Clenbuterol is between 34-35 hours. All of the other beta agonists that have been labeled ineffective at preserving or even building muscle have half-lives much shorter, around only 6 hours. It has been demonstrated however, that when you infuse beta agonists with short half-lives, you can elicit the same anabolic activity (4). The reason is because infusion circumvents the half-life issue all together, providing a steady stream of agonist for the beta-receptors.

    So what does all this have to do with ephedrine? Well, ephedrine also has a very short half-life, only about 3-4 hours. Keep in mind that this does not mean that ephedrine levels are high for the full 3-4 hours. In reality, they will peak early and then begin to decline quite rapidly. So if you are taking ephedrine every 4 hours, levels are pretty low for most of that time. What's the solution? Simple. Take ephedrine at least every 2 hours. You will find in doing so that you don't get the hills and valleys in your mood either. NOTE: if you are taking 20 mg ephedrine with 200 mg caffeine every 4 hours, you should half the dose to take it every 2 hours. That way you are still taking the same total amount over the course of the day. You will be surprised at how such a small change can dramatically improve the experience and results of using ephedrine and caffeine.

    Points to take home

    Keep carbs low while using ephedrine. Insulin counter-acts the effects of ephedrine and will ultimately hinder fat loss if carbs remain too high. This does not mean you must go on a ketogenic diet. If total calories are low enough, carbs become less of an issue. But if you are trying to keep muscle by lowering calories only slightly, the carbs will sabotage ephedrine's action.

    Ephedrine and Clenbuterol have two different, yet similar mechanisms of action. Nevertheless, don't use Clenbuterol and ephedrine at the same time, or even in an alternating fashion. Both drugs work through the beta-adrenergic receptor, however, Clenbuterol will shut down beta-receptors within a few weeks. Taking ephedrine at that time will do little for you. Better to use ephedrine from the start of your diet, only switching to Clenbuterol no further than 3 weeks out from the contest.
    In order to get the most benefit from ephedrine on muscle loss, adjust your dosing schedule to every 2 hours. This will enhance the duration and consistency of beta-adrenergic activity. Be sure to adjust the amount you take each time in order to maintain the total amount taken over the course of a day. For example, instead of taking 20 mg ephedrine and 200 mg caffeine 3 times daily, take 10 mg ephedrine and 100 mg caffeine 6 times daily.

    References:
    1. Van Harmelen V, Reynisdottir S, Cianflone K, Degerman E, Hoffstedt J, Nilsell K, Sniderman A, Arner P. Mechanisms involved in the regulation of free fatty acid release from isolated human fat cells by acylation-stimulating protein and insulin.J Biol Chem 1999 Jun 25;274(26):18243-51
    2. Paquot N, Schneiter P, Jequier E, Tappy L. Effects of glucocorticoids and sympathomimetic agents on basal and insulin-stimulated glucose metabolism.Clin Physiol 1995 May;15(3):231-40
    3. Astrup A, Buemann B, Christensen NJ, Toubro S, Thorbek G, Victor OJ, Quaade F. The effect of ephedrine/caffeine mixture on energy expenditure and body composition in obese women. Metabolism Jul;41(7):686-688. 1992
    4. Choo J, Horan M, Litlle R, and Rothwell N. Anabolic effects of Clenbuterol on skeletal muscle are mediated by beta2-adrenoreceptor activation. Am J Physiol 1992; 263:E50-E56
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    Great post and lots of info!
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    Quote Originally Posted by MAxximal View Post
    Ephedrine and caffeine: Little known facts about this dynamic duo
    by Bryan Hay****

    [NOTE: whenever I talk about taking ephedrine, assume I am also talking about caffeine] Ephedrine has truly moved into the mainstream over the last few years. With the onslaught of Metabo-whatever products in every mall and grocery store, nearly every housewife in America is on it. Today even the term "thermogenic" is a household word. Nevertheless, bodybuilders were the first to put ephedrine to widespread use and it remains today as one of our most important tools in contest prep.

    Despite the widespread use of ephedrine, knowledge about how it works and how best to use it is rare. Even bodybuilders, who should know better, take it haphazardly without any rhyme or reason to their dosing schedule. Sure, most understand the synergistic 1:10 ratio of ephedrine to caffeine, but there is a lot more that can be done to further increase its effectiveness.

    Ephedrine's mechanism of action

    Let's start with ephedrine's basic mechanism of action. Ephedrine is a sympathomimetic, which means it acts to increase sympathetic activity. Why is this important? Because there is a drop in sympathetic activity when you cut calories. When you get a drop in sympathetic activity you get a decrease in metabolic rate and lower rates of lipolysis (fat mobilization). This can play a significant role in why you plateau on long-term diets. The use of ephedrine and caffeine can stave off this drop in metabolic rate and allow fat loss to continue unabated for several additional weeks.

    People often want to compare ephedrine to Clenbuterol. This is fine as long as you realize that they act in different ways. Clenbuterol is a specific beta-2 adrenergic agonist. As such, Clenbuterol interacts directly with beta-2 receptors on muscle and fat tissue. Ephedrine, on the other hand, is not a direct beta-2 agonist. In fact, ephedrine is a poor ligand for the beta-2 receptor. Instead, ephedrine stimulates the release of noradrenaline from sympathetic nerve terminals. The noradrenaline then goes on to interact with muscle and fat cells as a nonspecific adrenergic agonist. This simply means that noradrenaline activates beta-2 receptors, but also other beta-receptors as well as alpha-receptors. So to compare ephedrine and Clenbuterol you must take into account their differences.

    The differences between ephedrine and Clenbuterol are important. For example, Clenbuterol is a very potent beta-2 agonist. As a result, within 14 to 21 days, the beta-2 receptors on muscle and fat cells will be drawn into the cell membrane to reduce their availability to Clenbuterol. Then, if you continue to take it, they will be disassembled all together, leaving you insensitive to Clenbuterol. It then takes at least 2-3 weeks for receptors to replenish themselves on muscle and fat cells. Once again, ephedrine is different with respect to down regulation. Ephedrine, being a much weaker agonist, does not cause rapid desensitization and/or down-regulation of adrenergic receptors. This allows ephedrine to be used effectively for many months. Despite these differences, both drugs should be tapered over the course of several weeks before discontinuing them. If you don't, you will quickly replace the fat you just lost due to an increased appetite and a decreased ability of fat cells to mobilize stored fat.


    Choosing the right diet to use with Ephedrine/Caffeine

    Your diet will also make a difference in what effects ephedrine will produce. Insulin prevents lipolysis. Insulin has been shown to inhibit lipolysis in a phosphatidylinositol 3-kinase- (PI3K) and phosphodiesterase 3B (PDE3)-dependent manner and to stimulate fractional re-esterification of free fatty acids (FFAs), resulting in inhibition of FFA release (1,2). Even in the presence of ephedrine and/or noradrenaline, a high carbohydrate diet will reduce the fat mobilizing effects of ephedrine. This being the case, I generally recommend a low carb diet to get the most out of ephedrine and caffeine. Keep in mind, however, that over time, your body will not respond so well to ephedrine when on a low carb diet. This should not surprise you considering your metabolic rate (reflecting CNS activity) will drop like a led zeppelin on a low carb diet anyway. So, a periodic carb up is helpful in keeping ephedrine's thermogenic properties high. A carb up should last no longer than 2 days. I may be helpful to keep fat low during these two days, or if you must eat fat, make sure it is n-3 and/or n-6 fatty acids.

    How to use ephedrine to keep that hard earned muscle

    You may have heard the Clenbuterol prevents muscle loss during a diet. This is true. Beta-adrenergic stimulation can preserve muscle protein. If you ask your average bodybuilder they will usually tell you that indeed Clenbuterol saves muscle, but ephedrine won't. They are wrong, of course. In studies measuring body composition as well as weight loss, ephedrine has shown the ability to prevent lean tissue loss (3). In a small double blind study lasting eight weeks, two groups of obese women were given either 20 mg ephedrine with 200 mg caffeine (E+C) or placebo (P) three times daily. After eight weeks weight loss was not significantly different between the groups, but the E + C group lost 4.5 kg more body fat and 2.8 kg less fat free mass (FFM). That is a difference of more than six pounds in eight weeks. The expected decrease in 24-hour energy expenditure (EE) seen in the P group was 10% at day 1 and 13% at day 56, but was only 7% and 8% in the treated group. The higher EE in the E +C group was entirely covered by fat oxidation.

    It's no secret that Clenbuterol has potent anabolic effects in animals when used in dosages around 4 mg per kg body weight. What does seem to be a secret is that this effect is dependent on Clenbuterol?s long and steady activation of the beta receptors (4). The half-life of Clenbuterol is between 34-35 hours. All of the other beta agonists that have been labeled ineffective at preserving or even building muscle have half-lives much shorter, around only 6 hours. It has been demonstrated however, that when you infuse beta agonists with short half-lives, you can elicit the same anabolic activity (4). The reason is because infusion circumvents the half-life issue all together, providing a steady stream of agonist for the beta-receptors.

    So what does all this have to do with ephedrine? Well, ephedrine also has a very short half-life, only about 3-4 hours. Keep in mind that this does not mean that ephedrine levels are high for the full 3-4 hours. In reality, they will peak early and then begin to decline quite rapidly. So if you are taking ephedrine every 4 hours, levels are pretty low for most of that time. What's the solution? Simple. Take ephedrine at least every 2 hours. You will find in doing so that you don't get the hills and valleys in your mood either. NOTE: if you are taking 20 mg ephedrine with 200 mg caffeine every 4 hours, you should half the dose to take it every 2 hours. That way you are still taking the same total amount over the course of the day. You will be surprised at how such a small change can dramatically improve the experience and results of using ephedrine and caffeine.

    Points to take home

    Keep carbs low while using ephedrine. Insulin counter-acts the effects of ephedrine and will ultimately hinder fat loss if carbs remain too high. This does not mean you must go on a ketogenic diet. If total calories are low enough, carbs become less of an issue. But if you are trying to keep muscle by lowering calories only slightly, the carbs will sabotage ephedrine's action.

    Ephedrine and Clenbuterol have two different, yet similar mechanisms of action. Nevertheless, don't use Clenbuterol and ephedrine at the same time, or even in an alternating fashion. Both drugs work through the beta-adrenergic receptor, however, Clenbuterol will shut down beta-receptors within a few weeks. Taking ephedrine at that time will do little for you. Better to use ephedrine from the start of your diet, only switching to Clenbuterol no further than 3 weeks out from the contest.
    In order to get the most benefit from ephedrine on muscle loss, adjust your dosing schedule to every 2 hours. This will enhance the duration and consistency of beta-adrenergic activity. Be sure to adjust the amount you take each time in order to maintain the total amount taken over the course of a day. For example, instead of taking 20 mg ephedrine and 200 mg caffeine 3 times daily, take 10 mg ephedrine and 100 mg caffeine 6 times daily.

    References:
    1. Van Harmelen V, Reynisdottir S, Cianflone K, Degerman E, Hoffstedt J, Nilsell K, Sniderman A, Arner P. Mechanisms involved in the regulation of free fatty acid release from isolated human fat cells by acylation-stimulating protein and insulin.J Biol Chem 1999 Jun 25;274(26):18243-51
    2. Paquot N, Schneiter P, Jequier E, Tappy L. Effects of glucocorticoids and sympathomimetic agents on basal and insulin-stimulated glucose metabolism.Clin Physiol 1995 May;15(3):231-40
    3. Astrup A, Buemann B, Christensen NJ, Toubro S, Thorbek G, Victor OJ, Quaade F. The effect of ephedrine/caffeine mixture on energy expenditure and body composition in obese women. Metabolism Jul;41(7):686-688. 1992
    4. Choo J, Horan M, Litlle R, and Rothwell N. Anabolic effects of Clenbuterol on skeletal muscle are mediated by beta2-adrenoreceptor activation. Am J Physiol 1992; 263:E50-E56

    great read, repped...
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