[fog_hat1981]

http://www.superiormuscle.com/vbulle...ad.php?t=29264

Clenbuterol

Article by PartyBoy - MuscleTalk Moderator

What is Clenbuterol and what does it do?

Clenbuterol (often referred to simply as 'Clen') is not a steroid, but a Beta 2 Sympathomitetic and central nervous system (CNS) stimulant. It is a specific agonist, stimulating the adrenergic beta 2 receptors. It is used in certain countries in a medical sense as a bronchodilator in the treatment of asthma, though not in the UK and USA, mainly due to its long half life.

Athletes and bodybuilders use the drug due to its thermogenic and anti-catabolic effects. This is down to its ability to slightly increase the body's core temperature, thereby raising calorie (energy) expenditure. It is thought that a 1°F increase yields around a 5% increase in maintenance calories burned. Studies on livestock suggest that clenbuterol also has anabolic properties. However, this seems not to be the case in humans, thought to be due to the fact that humans lack the abundance of beta 3 receptors which increase insulin production and sensitivity.

Clenbuterol is dosed in micrograms (mcg/µg), most commonly in tablet form, though there are other forms of administration such as liquids, nasal sprays and injectables. Note: Although dosages are in microgram amounts, many manufacturers will list the active ingredient as milligrams (mg), so a tablet of 20mcg will be labelled as 0.02mg.

What are the side effects/possible implications?

Side effects are dose dependant, though most users will find that most tend to subside with persistent use. Caution is advised when employing the use of Clenbuterol in conjunction with other adrenoceptor agonists as side effects
are likely to be cumulative. It is for this reason that it is generally not recommended to use ephedrine/ephedra (or ma huang) or the ECA stack (ephedrine-caffeine-aspirin) whilst using clen.

Common side effects of clenbuterol include:

Headaches
Muscular tremors (especially hand shakes)
Muscular cramps
Nervousness
Insomnia
Sweating
Increased appetite
Nausea
Palpitations
Hypertension (high blood pressure)
Possible cardiac hypertrophy as clen also targets cardiac and smooth muscle fibres
Heart muscle necrosis has been demonstrated in animal studies

In view of the above side effects, it is obvious to assume that anyone with cardiac issues and/or hypertension should not use a stimulant such as Clenbuterol and caution must be observed by those already using similar compounds in the treatment of existing medical conditions. In addition, there is very little conclusive knowledge of the cardiac effects of supra-physiological dosages in humans.

Commonly used doses

It is well known that Clenbuterol use results in rapid down-regulation of beta 2 receptors. This is due to the powerful stimulatory effect of the drug. It is therefore pointless to use clen for long periods without a break. Some believe thata two day on, two day off dosing schedule will allow adequate potential for receptor up-regulation. However, I doubt this to be the case due to the relatively long half life of clen, resulting in continued stimulation even throughout the "off" days. A much better regime would be a two week on, two week off cycle. Maximum plasma levels are reached around 2-3 hours after oral administration, and terminal half life at 34 hours (Zimmer, 1976).

A tapering up of dosages is recommended in an attempt to limit harsh side effects. Most commonly, a user will start by taking one 20mcg tablet on day 1, followed by an increase of one tablet on subsequent days. Subject to personal tolerance levels, a dosage of 140mcg (seven tabs) will be used by day 7, and this level should be maintained for the entire second week. It would be fruitless to exceed seven or eight tablets daily due to receptor over-saturation. There is no requirement to taper down.

For the next 'cycle' of clen (i.e. weeks 5 & 6), there is no requirement to taper up from one tablet as your tolerance level should now be known. As an example, if the user finished the first cycle of clen on 7 tabs, they could
recommence at a slightly lower dose of 4 or 5, and taper up again from this level. Again though, the user should again limit their intake to 7 or 8 tabs daily.

During the two 'off' weeks, an ECA stack can be used as required. ECA will not cause such a pronounced down regulation and desensitization of the receptors, certainly not to the extent of clen. Ephedrine has a short half life in contrast to clen which results in times throughout the day where the betas will partially recover from stimulation by adrenaline and nor-adrenaline. Potency is also much weaker that that of clen, as it is not a specific agonist.
Ephedrine is also thought to increase the conversion of andogenous/exogenous T4 to T3 through the activation of deiodinase enzymes responsible for this process. This is important as clen is known to slow the rate of T4 to T3 conversion. As a side note, some bodybuilders will use T3 concurrently with the Clenbuterol/ECA cutting cycle (together with certain anabolic/androgenic steroids no doubt!) in an attempt to at least maintain plasma T3 levels.

Cycles of Clen/ECA are normally limited to 12 weeks in total, though are often shorter.

Female dosages tend to be slightly lower than those of male users, with an upper limit of 80-120mcg (4-6 tabs).

Aside from its fat burning properties, Clen is often used as an anti-catabolic to maintain muscular gains following a steroid cycle. A dosage of 40mcg daily would be suited to this situation.

There is no particular requirement to split the dosage throughout the day due to the long half life. Most will take the full daily dose in the morning, though some prefer to take their dose just before bed in an attempt to avoid most of
the side effects as they sleep.

Some user accounts suggest that splitting the dose may lessen side effects slightly. It is a trial and error process in essence, to ascertain which method suits you personally.

Muscular cramping

Cramping whilst using Clenbuterol is a fairly common side effect. This is most probably due to depletion of the amino acid taurine in the liver together with deficits in the electrolytes sodium and potassium, as well as inadequate
hydration. Taurine helps stabilize cell membranes and prevent nerves from becoming over-excited. Some studies show that giving taurine supplements relieves painful muscle cramps. Japanese researchers found that the longer
rats exercised, the more taurine they lost from their muscles (Matsuzaki et al, 2002).

Symptoms of cramping may be alleviated by:

Eating fruit particularly bananas
Ensuring adequate hydration
Taurine supplementation - 3-5g daily
Potassium supplementation - 200-400mg daily taken before bed on an empty stomach

Ketotifen

Ketotifen is an anti-histamine used medically to treat bronchial asthma and allergies. It has a sedative and depressant effect on the brain. It acts by decreasing the release of histamine which is a chemical released when an
allergic reaction occurs. Ketotifen blocks the action of histamine on special histamine receptors and reduces the nerve response when an allergic reaction occurs.


Histamine is the chemical in the body that causes the symptoms of an allergic (hypersensitivity) reaction. These can include inflammation of the skin, airways or tissues, rashes, itching and of the skin, eyes or nose, nasal congestion and narrowing of the airways. By blocking the actions of histamine, ketotifen may prevent and relieve the narrowing of the airways that occurs in asthma due to allergies.

However, bodybuilders are interested in the drug as it has been shown to inhibit the down regulation of the beta receptors, including the beta 2s that clen stimulates. As long as you are taking ketotifen, it will continue to clean
these receptors, never allowing them to downregulate, even while on a heavy clen cycle. That means you can continue to take clen indefinitely without having to cycle off to regenerate the receptors. A dose of 2-3mg daily can upregulate even severely shut down receptors within a week.

It also means that you don't need as much clen to get the same benefits. It seems you can take about 30-40% less clen and it be equally effective.

No studies have been done to find the most effective dose though most users should find 3-4mg daily ideal, which can be split or taken in one sitting. Higher doses are likely to cause (sometimes severe) drowsiness and increase
appetite.

References

1.Matsuzaki et al (2002). Decreased taurine concentration in skeletal muscles after exercise for various durations. Med & Sci Sp & Ex. 34(5):793-797.

2.Zimmer (1976). Single and multiple applications and metabolite pattern of clenbuterol in man (author's transl). Arzneimittelforschung 26(7a):1446-50.

Warning! Articles related to the use of illegal performance enhancing drugs are for information purposes only and are the sole expressions of the individual authors opinion. We do not promote the use of these substances and the information contained within this publication is not intended to persuade or encourage the use or possession of illegal substances. These substances should be used only under the advice and supervision of a qualified, licensed physician.

[mindstar]

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.1 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.

[roccodart440]

ECA, or a thermo genic + cardio is more effective, better for you and doesn't make you feel nearly as fucked up.

[lil_big_junior]

thats true

[mindstar]

I'm off the clen for life....I'd rather diet harder and do more cardio than have my heart give out on me. I posted it as a warning/counter to the original post.

[lil_big_junior]

yea. i'll never do clen again either...prolly just ephedrine by itself or the eca stack...

[roccodart440]

Have you guys seen the liquid ECA that some of the research companys have out?

[mindstar]

no...i'll look into it. is it at *ology?

[roccodart440]

Originally Posted by mindstar

no...i'll look into it. is it at *ology?

If you go to ology you can PM me or even ask on the open forum. Since research companies are legal we at ology have no problme discussing them on the board.