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  • Clenbuterol HCL

    Clenbuterol

    (Clen)


    Clenbuterol (Clen) is a selective beta-2 agonist/antagonist and a bronchodilator. What this means, is that it stimulates your beta-2 receptors. Of great importance, is that Clenbuterol is a selective beta-2 agonist (because it works selectively on the beta-2-andrenergic-receptors), right? The thing is, Clenbuterol is selective...like hitting a tack (the tack being your beta-2 receptors) with a small hammer (the hammer being the Clen)...thus, it hits the beta-2 receptors selectively. Sorry if that seems repetitious, but itīs very important to understand that fact before we move on. Since clenbuterol has very little beta-1 stimulating ability, it has the ability to reduce certain kinds of airway obstruction without much in the way of cardiovascular effect (more about that later), and this is why it is used as an asthma medication.

    So what exactly dose a stimulant like Clen (or Ephedrine) do when it stimulates those Beta Receptors? Well, it serves to increase your body temperature a bit by increasing heat production in the Mitochondria, increase your basal metabolic rate, and decrease your appetite (1). This partly explains how Beta-2 agonists directly stimulate fat cells and increase lypolysis (fat-loss)(1)(13). And also, because it is a Beta-2 agent, clen can decrease insulin sensitivity (2), unfortunately.

    Clenbuterol Fat Loss

    Clenbuterol is a very effective repartitioning agent, and this is what itīs most often used for in athletic circles. It will increase your ratio of Fat Free Mass (FFM) to Fat Mass, by decreasing your Fat and possibly increasing your FFM (3). Lets quantify that a bit:

    In one study, horses given a semi-reasonable dose of clen (slightly over 1mcg/lb x2 a day) and exercised for 20mins, 3x a week ( I suppose they were Mentzer disciples) had significant decreases in %fat (-17.6%) and fat mass (-19.5%) at week 2, which was similar to Clen given to horses who didnīt exercise; in contrast, the exercised group had a different FFM response, which significantly increased (+4.4%) at week 6 (3). Week 6! Hereīs a chart illustrating the changes in % of Body Fat experienced in the various test groups, followed by a chart showing the increase in Fat Free Mass experienced by the same groups:
    Changes in percent body fat (%fat) over time in clenbuterol and exercise (ClenEx; A), clenbuterol only (Clen; B), exercise only (Ex; C), and control (Con; D) groups. Means with different letters (A and B) are significantly different.
    Changes in fat free mass (FFM) over time in ClenEx (A), Clen (B), Ex (C), and Con (D). Means with different letters (a-c) are significantly different.

    I think those charts should clearly illustrate the repartitioning effects of Clen, even though it is known that itīs effects on animals are typically much more dramatic than in humans& .Thereīs still no doubt about it, in my mind Clen will help you lose fat and gain muscle.

    So Letīs re-examine that first point I made: Clen vs. clen+ exercise produce roughly the same results for the first 2 weeks! This tells me that the 2 weeks on and 2 weeks off schedule for clen dosing is far from optimal, and if you want the quasi-anabolic effect from the clen, itīll take more than 2weeks on (6 weeks apparently). In addition, since clen alone is similar to clen+ exercise for those first 2 weeks...why would you ever use a 2on/2off protocol? Keep in mind that animal responses to beta-agonist/antagonists differ a bit from ours but Iīm sure that you get the idea that 2on/2off is not a great dosing protocol. If I were using clen, Iīd be using it for 6-12 weeks at a time, if I expected to get maximum results from it, but certainly, the most dramatic effects on fat loss appear to be in weeks 1-2. The reasons for the further increase in FFM around week 6 despite no changes in %fat or fat mass is not easily explained... It might be that clenbuterol can increases FFM through another nonreceptor-mediated pathway, which would be very good for us, since the anabolic effects would also be applicable in humans, despite the fact that animals often respond more dramatically to beta-agonist/antagonists, due to receptor properties.. However, clenbuterol is highly lipophylic and can also enter muscle tissue (12), so that could indicate a possible mechanism of work. Maybe that would explain the significant increase in FFM of 13 kg in at 8 wks in the study? Certainly, muscle protein synthesis (MPS) must be a part of it, since clen will increase MPS in your body (17)& But it has even been speculated that the growth-promoting effect of clenbuterol may be specific to muscle and that the drug may act in a not-yet-understood manner which circumvents (!) the physiological mechanisms responsible for the control of muscle growth (13). This may mean that clenbuterol can help blast you past "sticking points" in your training by circumventing the usual mechanisms by which anabolism is experienced! It is of note that both muscle composition and fiber size has been shown to increase with administration of clen (14).

    In any case, Clearly the results you want to reproduce for yourself are those to be gained by clen + exercise, for 6 weeks or more. This type of dramatic anabolic effect hasnīt been confirmed in human studies (8), but the anabolic effects of clen in animal (specifically equine and rodent) studies are clearly quite astounding.
    Now that I told you how great clen is; Iīll tell you how to take it.

    Clen has a biphastic elimination, which means that it is technically reduced in your body in 2 different stages. This isnīt particularly important, as a recent study has shown that for most intents and purposes, clen concentrations in the body decline with a ― life (approximately) equivalent to 7-9.2hours and again up to as much as 35 hours later(4)(5). If youīre really interested, though, clen technically declines biphastically at 10 and then 36 hours. But really, in our little world, where we use ― life to tell us when to take our next dose, who the hell is going to take clen, then a dose 10 hours later, then a dose 36 hours later? Weīll stick with the earlier 7-9 hour ― life for dosing purposes, and take our clen every 3.5-4.5 hours that weīre awake, stopping early enough to still be able to get to bed. Clen can, in some people, cause insomnia (and as with all stimulants, can cause anxiety in some). Recently, itīs become popular to take a whopping dose of clen in the morning, and thatīs it for the day. Thereīs nothing wrong with this, I guess, but Iīd rather not go through that kind of roller-coaster of sweating and shaking until it wore off.

    Clenbuterol Cycle
    Based on its rate of elimination from the body, and how much is usually needed to be effective for athletes, my recommendations are the same for both men and women. Youīll need to take 20mcgs upon rising, and then repeat that same dose again later in the day, and then once again in that day (if you find you can tolerate the effects). So youīll start with 20mcgs, and then repeat that dose 2 more times that same day if you can tolerate it (side effects will determine this hand shaking, sweating, etc& classic stimulant sides). Then you can start increasing the dose gradually. Personally, I wouldnīt work my way up to more than 200mcg/day. 60-120mcg/day is an average dose. And keep your Blood Pressure at (or under) 140/90, while on clen, just to be safe. If you go over that, lower the dose. Youīll also want to know your body temperature, upon rising, for the week before you start taking your clen, and then monitor it (again, as soon as you wake up) throughout your clen regimen. When it returns to the level it was at before you began taking the clen, youīll need to start taking your Benadryl or Ketotifen, as the decrease in Body Temperature back to original levels indicates the thermogenic effect is beginning to decline.

    Clenbuterol can also cause a downregulation in testicular androgen receptors and in pulmonary, cardiac and central nervous system beta-adrenergic receptors(6.) possibly making steroids less effective (if there is androgen receptor downregulation elsewhere as well, then itīs highly probable) while you are on clen; but definitely making clen less effective as time goes on and you keep taking it. To counteract this, you can take some ketotifen every 3rd or 4th week that you remain on clen. Itīs a prescription anti-histimines, so itīll make you drowsy (take before bedtime). Basically, the way this works is to reduce beta-2 receptor activity, and restore receptor function (15).
    Another option, if you are worried about receptor downgrade, is taking Benadryl, at around 50-100mgs/night before bed (every 3rd week or so, for that week). Benadryl is sold as an anti-histamine in the United States, and/or a sleep aid elsewhere in the world. However, Beta receptors are embedded in the cellīs outer phospholipid membrane. The stability of the membrane has a lot to do with the proper function of the receptors. Methylation of the phospholipids is stimulated by the binding of beta agonists to their receptors. Methylated phospholipids are foreign to the body, and when the body recognizes them as foreign, it breaks them down with phospholipase A2. This changes the structure of the outer membrane which results in desensitization of the beta receptors. On the other hand, agents that inhibit phospholipase A2 slow desensitization.

    Cationic ampiphylic drugs are known for their ability to inhibit phospholipase A2. Benadryl (diphenhydramine) is a cationic ampiphylic drug.
    Ergo, Benadryl slows desensitization of Beta receptors (i.e. Upgrades them) by inhibiting phospholipase A2, which is the enzyme that breaks down methylated phospholipids, and this action in turn keeps the phospholipid membrane stable, and thus keeps the receptors functioning properly. (7). This will allow you to use clen for much longer and itīll still have the same effects. Also, since Benadryl is an anti-histamine, and histamines have a direct effect on beta-adrenoreceptors (not just Beta-2īs but all of them), using an anti-histamine will have a direct effect on reducing beta-receptor stimulation (16), and thus upregulating your beta-receptors.

    Ephedrine

    Since weīre speaking about beta-receptors and upregulation, here, let me address the claim that you can use ephedrine (or the ECA stack), alternating with clen, in order to avoid receptor downgrade. Iīm not sure where this rumor came from, but it is totally incorrect.

    To dispel this myth, lets examine ephedrine for a second. Remember when I said that using clenbuterol to stimulate the beta-2 receptors is like hitting a tack with a hammer? Well, Ephedrine is like a sledge-hammer, it hits the beta-2īs and everything around them. Thatīs because itīs not selective, but rather it stimulates other receptors to a great degree as well.

    Anyway, one of those receptors that ephedrine hits is the Beta-2 (yeah...the same one as Clen). As you can see from the graph below (ephedrine is represented by the the solid circles), it reduced Beta-2-AndrenergicReceptor (what we call, in laymens terms, the "Beta-2 receptor") levels to 32% of the control level after 24 hours. Read this again:

    Ephedrine, in this study, reduces Beta-2 receptor levels to 32% of control after 24 hours.
    (see the solid circles in this graph represent ephedrine)
    Granted, itīs not perfect, itīs not in vivo, etc...But thereīs no denying that ephedrine will down-regulate beta-2 receptors....ergo you will not be able to use it on the weeks in between your clen to upgrade your receptors.

    Clenbuterol Side Effects

    Also, bear in mind that clenbuterol has some side effects. It isnīt great for your heart, and can cause some issues there (enlargement of ventricles, etc, ) but most studies showing clen to cause heart problems are with animals, and even though the dosing is almost similar to what humans take (in some studies itīs within the range of what would be double of a large human dose...) itīs important to remember that animals have more beta-2 receptors and they cause certain event chains that humansī beta-2 receptors may not. Clen causes cardiac hypertrophy and cardiac necrosis (cell death) to some degree, in some cases. Again though, many studies showing the more significant, possibly irreversible, heart problems are with mg dosing. We humans take clen in mcg doses.

    If we want to duplicate those "theraputic" levels of clen seen in the more conservative studies, weīd still be taking just over 1mcg/lb of bodyweight, twice a day. Iīd suggest a bit less than half of that dose, however.

    Performance issues with clen also vary. Some studies show reduced exercise (cardiovascular) performance with clen (9), while some show that clen can alleviate exercise induced asthma (10)!Clearly, this compound will have different effects on different people, and I suspect that a lot of it is sports specific. Many bodybuilders claim that clen makes it difficult for them to do cardio, yet I can play a full game of rugby on it. You need to figure out how it affects you, and tailor your dose personally.

    Finally, this brings me to the issue of cramps while on clen. I donīt get them. My friends donīt get them. Most of us are athletes who use clen during the season as well as the off season, and one of my friends even claims that it gives him more "wind" (cardiovascular stamina). Take on enough water every day and you should be fine. If youīre really concerned, you can take some extra minerals and taurine, since clen depletes taurine (11) as do most if not all beta-agonists. I donīt take anything more than my usual vitamins and minerals.

    1st Graph Reference:
    ASPET Journals, Vol. 58, Issue 2, 421-430, August 2000
    Kinetic Analysis of Agonist-Induced Down-Regulation of the 2-Adrenergic Receptor in BEAS-2B Cells Reveals High- and Low-Affinity Components
    Bruce R. Williams, Roger Barber, and Richard B. Clark
    2nd set of Graph references:
    J Appl Physiol 91: 2064-2070, 2001; 8750-7587/01
    Chronic administration of therapeutic levels of clenbuterol acts as a repartitioning agent
    Charles F. Kearns1, Kenneth H. McKeever1, Karyn Malinowski1, Maggie B. Struck1, and Takashi Abe2
    References:


    1. Int J Obes Relat Metab Disord. 1994 Jun;18(6):429-33.
    2. Am J Physiol Endocrinol Metab. 2002 Jul;283(1):E146-53
    3. J Appl Physiol. 2001 Nov;91(5):2064-70
    4. J Anal Toxicol. 2001 May-Jun;25(4):280-7.
    5. J Pharmacobiodyn. 1985 May;8(5):385-91.
    6. J Anim Physiol Anim Nutr (Berl). 2004 Apr;88(3-4):94-100
    7. Prog Clin Biol Res. 1981;63:383-8
    8. Ann Pharmacother. 1995 Jan;29(1):75-7
    9. Med Sci Sports Exerc. 2002 Dec;34(12):1976-85.
    10. Respiration. 1987;51(3):205-13.
    11. Adv Exp Med Biol. 1996;403:233-45
    12. Food Addit Contam 13: 259-274, 1996
    13. Biochem J. 1989 Jul 1;261(1):1-10.
    14. Biosci Rep. 1987 Feb;7(2):143-9.
    15. Z Erkr Atmungsorgane. 1990;175(3):141-6
    16. Comp Biochem Physiol C. 1989;92(1):143-8.
    17. Biosci Rep. 1984 Jan;4(1):83-91.


    Anthony Roberts

    Information is for educational purposes ONLY. Consult a medical doctor before using any medication. heavyiron does not advocate readers engage in any illegal activity. Research chemicals are not meant for human consumption.
    Last edited by heavyiron; August 6th, 2014, 01:31 PM.
    All posts are for entertainment and may contain fiction. Consult a doctor before using any medication.


  • #2
    Anthony Roberts

    Back in 2004 I wrote the first heavily researched article of my career. It was about Clenbuterol, and you can still find it in article forums and profile sections on most major sites. One of the most controversial points I made was that Clenbuterol is anabolic. At the time there was a pretty reasonable amount of animal data (rodents, horses, etc…) and I was fairly confidant saying that Clen has anabolic – or at least strongly anti-cabtabolic – effects in humans. Back when I wrote that article, and my subsequent book(s), there was no published medical data on the accrual of fat free mass in humans using Clenbuterol. And frankly, most bodybuilders who used the stuff were also using a lot of other stuff too.

    Naturally, because there was no human data to support this notion, online steroid”experts” rallied behind the notion that because there was no human data proving otherwise, Clen must not have that effect outside of animals. Anyway, a couple of studies have recently popped up in the US National Library of Medicine, that are new or were previously unavailable or unpublished. One is from all the way back in 1993, and was conducted in the UK, and seems to indicate that Clen helped patients regain muscle strength more quickly after orthopedic surgery:

    Clin Sci (Lond). 1993 Jun;84(6):651-4.

    Clenbuterol, a beta-adrenoceptor agonist, increases relative muscle strength in orthopaedic patients.

    Maltin CA, Delday MI, Watson JS, Heys SD, Nevison IM, Ritchie IK, Gibson PH.

    Rowett Research Institute, Bucksburn, Aberdeen, U.K.

    Abstract

    1. The sympathomimetic agent clenbuterol has a muscle-specific anabolic effect in normal and wasted muscles from animals. This trial was designed to examine the effect of the drug on the recovery of muscle strength and area after open medial meniscectomy. 2. A double-blind, completely randomized, placebo-controlled study was carried out on 20 healthy male patients. Muscle strength and cross-sectional area were determined before and after surgery. Patients were treated with drug or placebo for 4 weeks postoperatively and there was a 2 week washout period. 3. The results suggest that, in the operated leg, clenbuterol treatment is associated with a more rapid rehabilitation of strength in knee extensor muscles; in the unoperated leg, knee extensor strength increased above the initial values after 6 weeks (P = 0.01). However, in terms of absolute strength the differences were not significant between the two groups. 4. It is concluded that the data lend support to the proposition that clenbuterol has therapeutic potential in the treatment of muscle-wasting conditions.

    In this next study, patients with chronic heart failure were given Clenbuterol, and made some decent gains in muscle size & strength, as well as their lean mass to fat mass ratio:

    J Heart Lung Transplant. 2008 Apr;27(4):457-61.

    Clenbuterol increases lean muscle mass but not endurance in patients with chronic heart failure.

    Kamalakkannan G, Petrilli CM, George I, LaManca J, McLaughlin BT, Shane E, Mancini DM, Maybaum S.

    Division of Cardiology, Department of Medicine, Montefiore Medical Center, Albert Einstein College of Medicine, Bronx, New York, USA.

    Abstract

    Clenbuterol, a beta(2)-agonist with potent anabolic properties, has been shown to improve skeletal muscle function in healthy subjects, and in high doses, promotes cardiac recovery in patients with left ventricular assist devices. In a small, randomized controlled study, we investigated the effect of clenbuterol on skeletal muscle function, cardiac function, and exercise capacity in patients with chronic heart failure. Clenbuterol was well tolerated and led to a significant increase in both lean mass and the lean/fat ratio. Maximal strength increased significantly with both clenbuterol (27%) and placebo (14%); however, endurance and exercise duration decreased after clenbuterol. Prior data support combining exercise training with clenbuterol to maximize performance, and on-going studies will evaluate this approach.

    Anyway, the point here is that human data is beginning to filter in, albeit in a rehab/post-operative scenario, showing that Clenbuterol does in fact have an anabolic effect in humans.
    All posts are for entertainment and may contain fiction. Consult a doctor before using any medication.

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    • #3
      Amino Acids. 1998;15(1-2):13-25.

      The effects of the beta 2-agonist drug clenbuterol on taurine levels in heart and other tissues in the rat.

      Doheny MH, Waterfield CJ, Timbrell JA.
      Source

      Department of Toxicology, School of Pharmacy, University of London, United Kingdom.

      Abstract

      The administration of a single subcutaneous dose of clenbuterol to rats altered the level of taurine in certain tissues. Taurine levels in cardiac tissue were significantly decreased 3 h after the administration of 250 micrograms/kg of clenbuterol and remained significantly depressed at 12 h post-dose only returning to control values by 24 h. The level of taurine in the liver increased 3 h after clenbuterol administration but was lower than the control value at 24 h post dose. Lung taurine levels were significantly lower than the control value at 12 hr post dose and remained depressed until 24 h post dose. Clenbuterol caused a significant increase in taurine levels in serum and muscle at 3 and 6 hr postdosing respectively but not at other time points. Serum creatine kinase (CK), activity was slightly but significantly raised at the 12 and 24 h time point. The effects of clenbuterol on tissue taurine content were not dose-dependent over the range studied (63-500 micrograms/kg). However taurine levels in the lung were significantly reduced at all doses and in the heart were significantly lower in the treated groups at all except the lowest dose, 12 h post dosing. Liver taurine levels were significantly increased at the highest dose of 500 micrograms/kg. The reduction of taurine concentrations in the heart, caused by clenbuterol, is of concern as taurine has been shown to have protective properties in many tissues especially the heart.

      PMID: 9871484 [PubMed - indexed for MEDLINE]
      All posts are for entertainment and may contain fiction. Consult a doctor before using any medication.

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