ARTICLE: The Rise and Fall of Clenbuterol
- 12-21-2007, 03:53 AM
ARTICLE: The Rise and Fall of Clenbuterol
The Rise and Fall of Clenbuterol
by Jerry Brainium
Clenbuterol is a beta-2 adrenal agonist drug, which means it has a structure similar to the natural catecholamine hormones in the body, such as epinephrine. The primary medical uses for clenbuterol are for treatment of asthma and other respiratory diseases. Clenbuterol assists in respiration because, like epinephrine, it promotes dilation of the bronchial tubes in the lungs. Asthma is characterized by constriction and inflammation of the bronchial tubes.
Clenbuterol, however, has never been approved for sale in the United States for use by people. Drug companies are most interested in profit, and clenbuterol offers no particular medical advantages over existing beta-2 asthma drugs. Clenbuterol does have notable disadvantages, however. It has a long half-life, remaining active in the body for up to 36 hours. While that sounds good, it also increases the likelihood of serious side effects, thus making it less attractive to litigation-wary pharmaceutical companies. In contrast, the body degrades and eliminates the current leading beta-2 agonist drug sold in the U.S. after only about six hours.
Clenbuterol is sold in other countries, chiefly by Mexican pharmacies, under various trade names, such as Clenasma, Spiropent and the veterinary injectable Ventipulmin. It first attracted the attention of bodybuilders years ago after animal research showed that it offered potent repartitioning effects—it appeared to decrease bodyfat while simultaneously fostering increased muscle size, particularly in the type 2 fast-twitch fibers, the fibers most amenable to hypertrophy from weight training.
Those animal studies, however, typically used dosages in the one-to-five-milligram-per-kilogram-of-bodyweight range. That amounts to a daily dose of 450 milligrams of clenbuterol in a 200-pound athlete. For human use clenbuterol comes in microgram amounts. One thousand micrograms equal one milligram.
Despite those discrepancies, clenbuterol quickly earned a reputation as an anabolic and “cutting” drug, favored in precontest cycles, and athletes who tried it soon discovered two things: 1) Its effects didn’t last more than three to four weeks, since beta-adrenergic receptors are extremely sensitive and turn off, or downregulate, rapidly; and 2) it provided no discernible anabolic effect. It did, however, provide a potent thermogenic effect conducive to fat oxidation. You could tell the thermogenic properties were working by the perception of increased body heat.
The most common suggested clenbuterol dosage was one to two tablets a day, gradually increasing to eight to 10 per day. To extend its therapeutic potency and blunt down-regulation of beta-adrenergic receptors, users were advised to take the drug on a two-days-on/one-day-off cycle; however, it was never proven scientifically that the off-and-on cycle offered any real advantages.
The same holds true for another drug, ketotifen, said to help maintain the potency of beta receptors. Whatever benefits ketotifen confer on open beta receptors come at a price. Ketotifen is an antihistamine, which can cause acute drowsiness—not exactly conducive to intense training. What of side effects? Taking too much clenbuterol has the same effect as a flood of epinephrine in your body. Symptoms include increased blood pressure, possible heart-rhythm disturbances, muscle tremor and insomnia. In Europe clenbuterol was used in meat processing, and some who ate the drug-laden beef experienced the same side effects.
More recent animal studies—again using far higher doses than would ever be ingested by humans—showed that clenbuterol decreases endurance by degrading the heart structure. Indeed, some of the research animals died from heart failure. A recent study that examined the heart and skeletal muscles of rats given clenbuterol identified direct toxic effects from the drug. What’s particularly interesting about that study is that the bad effects resulted from just a single dose of injectable clenbuterol—a form favored by some bodybuilders and other athletes.
The results showed that clenbuterol didn’t just harm heart-muscle cells but actually killed them. Heart-muscle-cell loss led to increased collagen deposition. In effect, active heart cells were replaced by scar tissue, setting the stage for sudden heart failure.
Several theories explain clenbuterol’s adverse effects. The first involves the fact that clenbuterol depletes the amino acid taurine in the heart; taurine has protective properties, such as modulating the calcium levels that keep heart rhythm stable. Clenbuterol may also increase norepinephrine-induced stimulation of the heart, which can damage the heart if excessive.
You may reason that the research animals got megadoses of clenbuterol and that the lesser doses athletes use wouldn’t have the same effects—but that’s just wishful thinking. According to something called Kleiber’s law, the animal dose of clenbuterol is equal to a human dose of five to six tablets. So the same side effects could be expected. In addition, because of the extended time that clenbuterol takes to degrade in the body, it could build up and have cumulative effects.
The findings of heart damage from clenbuterol could partly explain the mysterious deaths of a few bodybuilders who combined clen with anabolic steroids. That is, of course, pure speculation. Athletes who use clenbuterol should ensure that they also supplement taurine, which may offer some heart protection.
Other studies send further grim news about clenbuterol.2,3 When it was given to pigs, the portion of the testes that synthesizes testosterone (Leydig cells) increased in size, suggesting increased testosterone production. But the testes cells where sperm is manufactured (Sertoli cells) were permanently damaged. That implies that clenbuterol may adversely affect fertility.
The increase in the cells that secrete testosterone isn’t that surprising. Natural catecholamines like epinephrine, for which clenbuterol serves as a synthetic substitute to some degree, are known to promote testosterone synthesis. Short-term stress, characterized by increased catecholamine release into the blood, leads to upgraded testosterone. But if the stress persists, other stress hormones, such as cortisol, are released and reverse that effect—that is, decrease testosterone synthesis and release.
- 12-21-2007, 09:33 AM
- 12-21-2007, 09:38 AM
12-21-2007, 06:11 PM
Also there is a prescription injectable form of Clen sometimes used in countries where Clen is approved.
12-21-2007, 06:15 PM
There have been several studies lately showing that clen increases heart strength.
M.Ed. Ex Phys
12-21-2007, 09:35 PM
12-21-2007, 09:37 PM
12-21-2007, 09:38 PM
12-21-2007, 11:57 PM
Me hates clen.
Now - clen transdermally is fine.
I do like albuterol though.
02-14-2008, 08:36 AM
welp, good thing i don't take clen. sucks for ppl who do.
02-14-2008, 11:16 AM
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 it´s within the range of what would be double of a large human dose...) it´s important to remember that animals have more beta-2 receptors and they cause certain event chains that humans´ 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, we´d still be taking just over 1mcg/lb of bodyweight, twice a day.......and this is a very high dose of clen. most users take less than 1/4 to 1/2 this amount.
02-14-2008, 03:52 PM
Serious Nutrition Solutions Representative
02-14-2008, 08:59 PM
So when we rationalize and say "hey the studies were animal studies and the dosages were high...I'm a human and my dosage will be low" what we really are doing is accepting Clen into our lives for one really effective cycle and then cycles that are less effective then a tried and true EC run.
So is it worth it? Well pre-ORD there were a lot of forums on the internet devoted to bodybuilding & chemical enhancement...and some of those forums had been around for many years. On all these boards people would discuss many things including any issues they might have with a drug such as Clen. The vast majority were possitive.
BUT it seems that if you made your way around 30+ forums you would bump into posts from guys who complained of heart palpitations and irregular heart beats that were not present before Clen use but appeared after a Clen cycle. Some guys used very small doses, some even for as few as 10 days...and a lot of these guys had these heart problems still 6+ months after a single clen cycle.
So you bump into a couple of such posts here and there... but now you are curious so you actively look for such posts and search the archives of those 30+ boards and after a while you have a dozen... then more then two dozen such reports. Not a lot in the scheme of things for sure...but enough to make ME believe that the potential risk just ain't worth it.
By-the-way William Llewellyn has an article in this month's MD magazine on Clenbuterol poisoning. He discusses a case where a man made a dosing error and ingested 108.75 mcgs of Clen and the result was a heartbeat of 254 beats per minute which took the use of 3 drugs and 3 nights in the hospital to return him to normal. (J. Med. Toxicol, 2007 Jun;3(2):56-60)
108.75mcgs of Clen sounds like a dose a bodybuilder would take or as you say a dose "most users take"...and yet there were bad effects on his heart.
02-14-2008, 10:43 PM
good points datBtrue.
i believe that it all comes back to moderation.
any and all supplements can be harmful if taken irresponsibly or to excess. even water is harmful in large quantities.
i've also spent a lot of time reading a lot of feedback from several boards.
like you i see mostly positive feedback on all supps and drugs but there is always a few negative reports. and i'm not talking just about clen, this goes for everything.
i notice a few re-occuring themes in these negative reports -
the user took the substance to excess or likly had a pre-existing health condition that they were unaware of or knew about but ignored.
too many times i see reports of people taking supplements and chemical substances when they know their health isn't 100% (overweight, high blood pressure, poor diet, poor cardio vascular health). but they take these supplements anyway thinking it will fix their problem when in reality is exagerates it.
IMO if you are in top physical and mental health and use pefrormance enhancing supplements in strict moderation the risks are controlable and slight.
02-15-2008, 02:58 AM
How often do we see a guy at 20% bodyfat...no thats to easy...say 25-30% bodyfat who wants to run a cycle of steroids to bulk up. He wants to run it so bad because he thinks he'll be transformed into a guy that looks like the guys in the magazines. There is no way he'll ever see his abs or even get down to 15%.
Then afer he bulks up is so fat he thinks Clenbuterol will be the magic bullet to get his abs to show...thank God DNP is hard to get or we'd see a lot of these guys misusing that.
So yes I see your point of view and agree.
So many guys want to stack steroids or stack weight loss chemicals or even supplements OR start w/ high doses without first seeing how their body responds to a single compound & low dose.
So yes I agree w/ you on this as well. Hank you are a young guy with a patient "old school" approach to this hobby and I think that is great.
02-15-2008, 03:23 AM
I am using Helios right now, it is made with Albuterol not Clen. So far I like it. My tolerance to AAS and fat burners is pretty remarkable I must say, I rarely get any sides.
Great post, I was going to use clen but the sides look damn intimidating.
02-20-2008, 06:42 PM
Yeah, one should use clen with some caution.
02-20-2008, 11:50 PM
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