Talk:ECA stack

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Ephedrine acts to increase energy by its actions as a symptomimetic amine. It increases dopamine and noradrenaline levels in the brain, and also serves as a dopamine reuptake inhibitor.

Is ephedrine really a dopamine reuptake inhibitor?

-- Yes, AFAIK, all phenethylamines are due to the related uptake action for dopamine, adrenaline, and noradrenaline. As ephedrine binds at noradrenaline receptors that also transport dopamine, the effect is less than cocaine or amphetamine, but still seems to be present. I've included two references that should help clarify this.

--- (76.98.177.253 06:27, 31 October 2007 (UTC)) Ephedrine is not a reuptake inhibitor in the manner of cocaine or methylphenidate; rather it releases catecholamines by reversing the norepinephrine (NE) uptake pump (NET). It has little affinity for the dopamine (DA) uptake pump (DAT), but like amphetamine (which only moderate DAT affinity, but high NET affinity) it can release ectopic dopamine from noradrenergic terminals. The NET actually has a higher affinity for DA than it does for NE, so free-floating extrasynaptic DA can be uptaken and accumulate over time in noradrenergic terminals. Methamphetamine releases DA directly from dopaminergic terminals by reversing DAT. Of course, both amphetamine and ephedrine release relatively more NE than DA. Amphetamine releases less NE at the same dopaminergic potency because of its moderate affinity for DAT, which ephedrine does not significantly bind to. Methamphetamine has even less noradrenergic load at the same dopaminergic potency, and causes the least amount of sympathetic side-effects, but also the least amount of thermogenesis.

But unlike amphetamines & cocaine, ephedrine also has potent direct agonist action at the beta adrenoceptors; depletion of NA does not interfere with its pressor action: [1] The tolerance to thermogenic and anorectic effects that develops after prolonged release of NE & DA is a result of stimulation of the alpha-2 adrenoceptors. These are feedback autoreceptors/heteroreceptors that decreases synthesis of catecholamines. Secondly prolonged activation of central D2 dopamine and adrenoceptors in the hypothalamus results in their desensitization. The direct agonist effects of ephedrine (on the beta-3 adrenoceptor) and the nonsteroidal anabolic clenbuterol (on the beta-2 adrenoceptor) is independent of NE & DA levels, so their thermogenic effects last much longer than the anorectic & thermogenic effects of amphetamines and other diet drugs.

Yohimbine, an alpha-2 adrenoceptor antagonist is sometimes used to prolong and enhance the thermogenic effects of NE and adrenaline (AD), which can be released by ephedrine, pseudoephedrine, an amphetamine, or naturally from the sympathetic ganglia during intense exercise. However, blocking the sole manner in which the sympathetic nervous system inhibits its own feedback can result in malignant hyperthermia if you overdose on thermogenics.

Well written points about reuptake inhibition with phenethylamines; however, my understanding of tolerance was it was mediated via beta-receptor downregulation, which is histamine mediated and essentially consists of the receptor sinking into the cell membrane further; in fact, I think that study was about clen specifically, and also covered an antihistamine being used to slow the tolerance (which I think is dumb, but hey). Can you point to any significant studies showing the role of alpha-2 receptors in the desensitization process? I just find it hard to believe clen would slow this down, rather than speeding it up. Further, aren't D2 receptors in the hypothalamus typically inhibitory? I also read one study that implicated tolerance to amphetamine's anorectic effect was due to suppression of the kappa opioid system, which isn't too far of a logical leap given the connections between DA and dynorphin, but I'm not sure how that applies to ephedrine (which has similar anorectic and tolerance to amphetamine which far less effects on DA). More confusing are studies showing infusion of kappa opioid agonists producing an anorectic effect; in rats, at least. Anyway, there are so many downstream effects of these drugs I think it's hard to say for certain at some point.

Ok, answered my own questions here. The thermogenic effect is ultimately due to the action of the noradrenaline, rather than any direct effect of the ephedrine on beta-3 receptors, as l-ephedrine, the kind sold OTC, has little beta-3 agonist activity.

I emailled Dr. Wellman, author of the study comparing various stimulants' thermogenic properties in human BAT. Unfortunately, while this study is not fully available online (just the abstract), he told me the results were that d-pseudoephedrine had three times less thermogenic activity as l-ephedrine.

I assume that ephedrine increases the body temperature by 2 degrees Fahrenheit, but shouldn't this be spelled out?

Ephedrine was NEVER banned in the United States, Ephedra was. I think it is important to make this distinction in the article. The stack was most commonly "built" with Ma Hung or similar standardized for 25mg ephedrine alkaloids. The ban was for supplements on dietary supplements containing ephedrine alkaloids. Volksgeist 14:47, 26 March 2006 (UTC)

I've made a couple small changes to the page. Ephedrine was never banned and can legally be purchased with (or without) an expectorant. For example D&E Pharm sells pure Ephedrine HCL, although you must show ID to purchase. Ephedrine has always been able to be legally purchased OTC in products such as Bronchaid. Many companies that sell "bodybuilding" products started selling Ephedrine HCL (with an expectorant) -- such as VasoPro and BioTek. Although the ephedra ban was lifted I've seen very few products still being sold that contain ephedra alkaloids (most likely because of the fear of lawsuits). Volksgeist 14:54, 26 March 2006 (UTC)
You guys sure? AFAIK the regulatory change was just to prohibit marketing ephedrine (or ephedra) as a weight loss / performance supplement (as its uses for asthma kept it on the market), but it's been a while since I read the FDA ruling. Some states have more intrusive bans, such as mine which requires ephedrine to be sold with guaifenesin.

[edit] fahrenheit/celsius?

I assume that ephedrine increases the body temperature by 2 degrees Fahrenheit, but shouldn't this be spelled out?

You can still purchase ephedra at http://www.thatswholesale.com if you have any doubts.

[edit] Tags

This article seems to downplay some of the risks of ephedrine/caffeine, and doesn't mention that it's been shown to be ineffective for long-term weight loss in a few studies. Also, it really needs to cite sources. Hence the tags. MastCell 19:03, 8 February 2007 (UTC)

Yes, this article suggests a lot of really questionable things, like using pseudoephedrine or asthma medication to get around the FDA's ephedra ban, and claims "great effectiveness" (which is false) and minimizes the side effects. Needs a major rewrite and is even potentially dangerous. MastCell 19:38, 15 February 2007 (UTC)
I agree with the "questionable" things. However, are you referring to the "great effectiveness" of using pseudoephedrine or the ECA stack in general? —The preceding unsigned comment was added by Aturaten (talk • contribs) 00:30, 26 February 2007 (UTC).
The article states there's a "great deal of evidence" that ECA is effective (without providing a reference, of course). I'm not aware of a great deal of evidence - there are a number of small, older studies looking at short-term weight loss. The largest meta-analysis of ephedra (not ECA) didn't find evidence that it was effective for long-term weight loss or performance enhancement. I'd just like to see a citation for this statement, because I'm not sure it's correct. MastCell 17:59, 26 February 2007 (UTC)
Hey, I originally wrote the article. Yes, I should've done a better job providing references, but everything I said was qualified in my references, though I failed to link them in any sort of organized fashion. And yes, ephedrine by itself is ineffective for weight loss-- I don't think anyone ever disputed that. The issue at hand is that EC or ECA have been in shown in large, long-term, well-designed studies to be effective. The initial weight loss is very significant, via loss of water weight and appetite suppression, but after that it still has a thermogenic effect noted in multiple studies and will still prevent muscle catabolism to some degree. To be sure, this article could use a rewrite, but the fact is EC/ECA has been shown to be clinically significant both short and long term, and one of the most effective tools for improving body composition, especially in combination with a diet and exercise program. The pseudoephedrine reference was covered here on this discussion page though I suppose I should've listed it more formally; I could not get the full text of one study so I emailed the study's author and he replied with the information I cited above, which is that PSE has 1/3rd the thermogenic effect relative to E. It is a greatly lesser effect, but I still felt it was worth noting and was interesting. And yes, EC/ECA can have side effects and does have risks, most of which it also shares with the FDA-approved Meridia. Ephedrine has minimal effects on dopamine but they have been specifically quantified in at least one rat study I read. The part about it being a reuptake inhibitor applies likely to only massive doses, and probably should be deleted if it hasn't. There are also other theories that current peripheral cAMP-based model for ephedrine's effectiveness are simply wrong and from rat data, and the only reason it's effective is central actions at the hypothalamus. Regardless, after seeing some of that data, I'm not even really sure I can say with confidence how the ECA stack works; the mechanisms have only truly been shown in animal models to which humans respond differently (lack of BAT); selective beta-3 agonists haven't been tremendously successful. However, I can say that ephedrine+caffeine in combination has been shown in studies both short and long term to be a very effective means of weight loss in humans with few noted adverse effects. And the article should at least note that. No, there haven't been any 6000-person studies published in the journal "Nature" over a 20-year time span, but I think EC/ECA has been studied in far more depth than most drugs do to gain FDA approval. As to why EC/ECA is not a specific FDA approved process, the lack of an ability to patent it means that no pharmaceutical company could protect their investment in the research, thus there is little incentive to pursue something with a negative return on investment. Anyway, this brick of text aside, I'm not sure I really want to rewrite the whole thing right now. But if anyone else wants to, feel free. —Preceding unsigned comment added by 69.146.16.67 (talk) 19:56, 10 December 2007 (UTC)
Could you point me toward "large, long-term, well-designed studies" showing that EC or ECA is effective? MastCell Talk 21:38, 12 December 2007 (UTC)
I don't understand why there is so much speculation regarding the efficacy of the ECA stack. Nothing is a miracle pill, but it can indeed be a *significant* aid in leaning out if you're going to eat right and exercise. As for your reseach studies, there have been a TON of them so I simply cannot believe you put any effort whatsoever into trying to find any of them if you are disputing the fact that numerous such studies have been done showing how well EC/ECA works under controlled circumstances. And who cares if there was 1 study showing that EC/ECA didn't help with long term weight loss because long term weight loss is a choice of lifestyle... of course some fat slob who is part of a study and is forced to eat right and exercise while using EC/ECA will lose weight and of course he/she is going to finish the study and have a high probability of pigging out on junk food soon after the study is over... DUH! Barring a serious medical condition, that's why fat people are fat to begin with. Anyways, here is a TINY PERCENTAGE of the research that has been done regarding EC/ECA showing it is effective... search through medical journals and you'll notice that there are LITERALLY A HUNDRED OR MORE of these studies, both experimental and theoretical:

1. Title: Effects of caffeine, ephedrine and their combination on time to exhaustion during high-intensity exercise. Author: Bell DG; Jacobs I; Zamecnik J Source: Eur J Appl Physiol, 77(5):427-33 1998 Apr

2. Title: Safety and efficacy of long-term treatment with ephedrine, caffeine and an ephedrine/caffeine mixture. Author: Toubro S; Astrup AV; Breum L; Quaade F Source: Int J Obes Relat Metab Disord, 17 Suppl 1():S69-72 1993 Feb

3. Title: Comparison of an ephedrine/caffeine combination and dexfenfluramine in the treatment of obesity. A double-blind multi-centre trial in general practice. Author: Breum L; Pedersen JK; Ahlstrøm F; Frimodt-Møller J Source: Int J Obes Relat Metab Disord, 18(2):99-103 1994 Feb

4. Title: The acute and chronic effects of ephedrine/caffeine mixtures on energy expenditure and glucose metabolism in humans. Author: Toubro S; Astrup A; Breum L; Quaade F Source: Int J Obes Relat Metab Disord, 17 Suppl 3():S73-7; discussion S82 1993 Dec

5. Title: Thermogenic, metabolic, and cardiovascular responses to ephedrine and caffeine in man. Author: Astrup A; Toubro S Source: Int J Obes Relat Metab Disord, 17 Suppl 1():S41-3 1993 Feb

6. Title: The effect and safety of an ephedrine/caffeine compound compared to ephedrine, caffeine and placebo in obese subjects on an energy restricted diet. A double blind trial. Author: Astrup A; Breum L; Toubro S; Hein P; Quaade F Source: Int J Obes Relat Metab Disord, 16(4):269-77 1992 Apr

7. Title: Ephedrine, caffeine and aspirin: safety and efficacy for treatment of human obesity. Author: Daly PA; Krieger DR; Dulloo AG; Young JB; Landsberg L Source: Int J Obes Relat Metab Disord, 17 Suppl 1():S73-8 1993 Feb —Preceding unsigned comment added by 70.135.218.189 (talk) 03:19, 1 June 2008 (UTC)

[edit] pseudoephedrine

The article states: "ephedra (an herb which contains both ephedrine and pseudoephedrine)..."


I do not believe the herb ephedra contains pseudoephedrine. As its "pseudo" name would imply, I believe that, by definition, pseudoephedrine is a synthetic version of the naturally occuring substance ephedrine, and does not occur naturally in any substance, herbal or otherwise. —The preceding unsigned comment was added by 68.199.66.14 (talk) 16:03, 31 March 2007 (UTC).

^^^whoever wrote that comment, you are an idiot. please do not challenge the accuracy of the article based on something you "think" but don't know for sure, especially when you don't know the facts and are merely speculating like a retard. now please kill yourself —Preceding unsigned comment added by 98.165.144.244 (talk) 07:43, 20 May 2008 (UTC)


No, ephedra contains ephedrine, pseudoephedrine and N-methylephedrine as it's main alkaloids. The pseudo- prefix has nothing to do with whether something is synthetic or not. In chemisty, pseudo is used to denote a stereoisomer of a substance that has no trivial name. Pseudoephedrine is a stereoisomer of ephedrine (the threo isomer, ephedrine is the erytho isomer). There is no such thing as a "synthetic version" as both a natural substance and the same substance made synthetically are chemically identical. 1.1.1 01:50, 3 April 2007 (UTC)

[edit] See this that I added to the Thermogenics article.

Themogenics is also the practice of deliberately exposing the body to very cold temperatures to raise Basal Metabolic Rate (BMR). This is usually done by soaking the body in icy cold water until a person can not tolerate it any longer almost to the point of inducing hypothermia. This then causes a release of thyroxine from the thyroid gland by means of the sympathetic nervous system thus raising BMR resulting in an overall increase in body temperature. The ancient Vikings used to practice this method of thermogenics. This method of thermogenics combinded with the ECA Stack mentioned above will produce a very powerful thermogenic responce. Dr CareBear 07:13, 12 July 2007 (UTC)

Reliable sources? MastCell Talk 16:51, 12 July 2007 (UTC)