12 December 2008

Clenbuterol was approved 8 years ago for use in treating respiratory disease in horses. It's very similar to the bronchodilator albuterol, and is the only beta-2 agonist that has been licensed for use in treating respiratory disease in horses. Clenbuterol lasts for a much longer period of time, and the second is that it appears to have some activity at the beta-3 receptor. Of interest, beta-3 receptors are located on fat cells, so clenbuterol may act to stimulate the metabolism of fat cells.

It is abused generally by bodybuilders and athletes for its ability to increase lean muscle mass and reduce body fat. However, clenbuterol is also associated with significant adverse cardiovascular and neurological effects.

FDA doesn’t approve clenbuterol for human use; the only approved use is for horses. In 1998, the FDA approved the clenbuterol-based Ventipulmin Syrup, manufactured by Boehringer Ingelheim Vetmedica, Inc., as a prescription-only drug for the treatment of airway obstruction in horses (0.8-3.2 m g/kg twice daily). This product is not intended for human use or for use in food-producing animals.

Outside the U.S., clenbuterol is available by prescription for the treatment of bronchial asthma in humans. It is available in tablets (0.01 or 0.02 mg per tablet) and liquid preparations. The recommended dosage is 0.02-0.03 mg twice daily.

Chemistry and Pharmacology
Clenbuterol is a beta2-adrenergic agonist. Stimulation of the beta2-adrenergic receptors on bronchial smooth muscle produces bronchodilation. However, clenbuterol also stimulates beta2-adrenergic receptors in other tissues, as well as beta1-adrenergic receptors, producing adverse cardiovascular and neurological effects, such as heart palpitations, muscle tremors, and nervousness. Activation of beta-adrenergic receptors also accounts for clenbuterol’s ability to increase lean muscle mass and reduce body fat, although the downstream mechanisms by which it does so have yet to be clearly defined.

After ingestion, clenbuterol is readily absorbed (70-80%) and remains in the body for awhile (25-39 hours). As a result of its long half life, the adverse effects of clenbuterol are often prolonged.

Is Clen the best thermogenic drug?
By raising body temperature (thermogenesis), fat calories are wasted allowing you to either get leaner while on a diet or to prevent excessive fat accumulation while on a bulking up phase. Beta agonists are able to accelerate body metabolism which generates excessive heat on top of mobilizing fat from adipocytes. Building muscles and burning fat are two very different processes.

Can Clen increase performance?
Depending on the dosage, Clen can improve (with low dosages) or reduce performance (with high dosages). Therefore, if you are using high doses of Clen (past 10 to 15 tablets), I recommend that you split up the dosage into two uneven parts. Before training, use a small to moderate amount of Clen to optimize both your strength and your muscle pump. It is up to you to find this individual dose but it is fairly easy. After training, use the rest of the Clen in order to reach your predetermined dose for the day. But avoid using Clen late in the day, as it can make it hard for you to fall asleep.

Abuse with Clenbuterol
Clenbuterol was found to have a repartitioning effect. With the calories you take in, this drug will make it so that those go toward muscle rather than fat. It'll boost the metabolic rate, so you'll burn fat and lay down more muscle.

It is typically abused by athletes and bodybuilders at a dose of 60-120 m g per day. It is often used in combination with other performance enhancing drugs, such as anabolic steroids and growth hormone.

Clenbuterol is typically abused by athletes. It is thought to be more popular among female athletes as the repartitioning effects are not associated with the typical androgenic side effects (facial hair, deepening of the voice, and thickening of the skin) of anabolic steroids. Professional athletes in several different sports have recently tested positive for clenbuterol. Clenbuterol is also marketed and abused for weight-loss purposes.

If you are a bodybuilder Clen is probably going to decrease glycogen storage not only from lower GLUT 4 levels but also from enhanced glycogenolytic activity. It is wrong to assume that ephedrine would be any different. Anything that is going to enhance adenylate cyclase activity such as clenbuterol, ephedrine, or even forskolin, is going to prevent these adaptive processes in response to exercise training. Fortunately, metabolic adaptations are not the key to muscle growth. Nevertheless, increases in oxidative capacity and increased GLUT 4 content are valuable adaptations when trying to train and recover at ever increasing levels.

Clenbuterol Dose
Some believe that a two day on, two day off dosing schedule will allow adequate potential for receptor up-regulation. Doubt it, 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.

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 endogenous/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.

To be continue in Clenbuterol for Weight Loss II
See more about Clenbuterol-Weight Loss Drug

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