The Straight Dope on Clenbuterol and Weight Loss

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Maria Lorenz
Join me on my "I Fit and Healthy" journey! Maria is an Upstate New Yorker interested in all things healthy-living related! She started the "I Fit and Healthy" Blog to document life and her pursuit of healthy living. By day she work in digital media and advertising. By night she’s a first-rate wife and mom of two crazy little girls! She is self-proclaimed addicted to her iPhone/iPad and always on the hunt for the latest health tools and fitness gadgets.

Hence the warning: Clenbuterol is illegal and potentially very dangerous for humans. We, here at iFitandHealthy, in no way, shape, or form, endorse its use.

The information presented here is strictly for educational purposes only and is not intended to replace the advice or attention of healthcare professionals.

Every generation of print media, television and motion pictures holds several examples of celebrities who were or are overly susceptible to the pressures to be thin.

Add to that the number of female athletes forced to strip away all body fat, the innumerable multitudes of common people subjected to abuse or scorn based on society’s fickle standards, and individuals suffering from eating disorders and unhealthy compulsions and it’s easy to understand why there’s such a huge demand for powerful weight-loss drugs.

Living Under a Microscope

America is an image-conscious society. Too often we judge and are judged purely by physical criteria, ignoring more important qualities such as character and intelligence in favor of blond hair, fluorescent white smiles, prominent cheekbones and tight skin that doesn’t jiggle, crease or pucker.

Consider the people you see daily around the office, at the gym or in stores. It’s likely that you spend more time commenting on their appearance than discussing their dreams, goals or accomplishments.

You might know details about every outfit your officemate has worn, but have no idea if she’s taking night classes, owns her own home or takes care of elderly parents.

Perhaps, because so many of our relationships are shallow and superficial, more time is spent discussing hairstyles, fashion and skinfolds than worrying about improving our education, environment or understanding current events.

Women who live under the microscope of scrutiny unique to visual media like magazines, television and motion pictures have learned to fear the possibility that a tabloid photographer might catch a snapshot of them with a belly roll as they’re fetching the morning paper off the porch, strutting the red carpet in a designer gown, or waving to their ubiquitous fans – all of which is recorded in high definition to be displayed in the pages of Peoplethe Star or on TV.

Further, talent agents, marketing consultants and casting directors offer fame and fortune to those who are willing to drop 15 pounds to fill a role on a moment’s notice, regardless of current weight.

Fashion designers and super-stylists may be the worst offenders of all by forcing models and clients to fit into size zero (and below) outfits in a perverted and distorted perception of what looks good.

Recently, popular news shows and magazines have been reporting on the revelation of a specific practice that’s been going on for well over a decade among Hollywood’s “A” list.

It’s no surprise that actresses and models use drugs for any purpose- long gone are the days of celebrities being role models.

While the hotel room-trashing days of the ’70s and ’80s are passed, drug use remains as pervasive as ever, with one clear distinction among today’s glamourati – the favored drugs of abuse are no longer street drugs, but prescription drugs.

Even though examples of cocaine or heroin abuse among Hollywood’s elite still make headlines, more than ever, our leading men and ladies are abusing – and in many cases becoming addicted to – prescription medications.

Relative to the anorexic pursuits of celebrity sylphs, there’s a long history of misusing prescription drugs to blunt the appetite, burn fat and boost energy, including the use of thyroid hormones, amphetamines, Redux and fen-phen.

Ever more exotic drugs are entering the off-label formulary as certain medications used to treat seizures, depression, diabetes and attention-deficit are being prescribed in numbers exceeding the known population of patients suffering from the relevant conditions.

This month’s headline grabber is a unique example of a prescription drug intended to treat an unrelated disease being used successfully, but not without consequences, to rapidly cut weight beyond what’s healthy or attractive.

A New Skinny Pill

Clenbuterol is a stimulant drug used in some countries to treat asthma, but is only available (legally) for use in horses in the United States.

Known by a variety of brand names (Ventipulmin, Spiropent, Novegam and Oxyflux) and commonly called “Clen,” clenbuterol is circulating among the image-conscious more rapidly than rumors of a television series’ cancellation.

Though the gossip columns treat clenbuterol use as an emerging practice, it has been used for decades by bodybuilders preparing for a contest, as the drug is a very potent aid in stripping body fat down to paper-thin levels.

Female bodybuilders are particularly fond of the drug as it not only is incredibly effective for fat loss, but also provides increases in strength and muscle size without the risk of masculinizing side effects (such as facial hair and a deepening voice) seen with most anabolic steroids.

Two studies have been published on the strength-enhancing effect of clenbuterol and salbutamol, a similar beta-2 agonist, in healthy patients in an orthopedic clinic.

Clenbuterol’s history and the vast majority of research have been in the animal sciences. It’s well known that adding clenbuterol to the feed of animals will increase meat production; it also appears to increase egg-laying in chickens.

However, clenbuterol is banned from use in animals that are destined for food production, as the high doses given to the animals to promote growth are retained in the meat and many examples of localized epidemics of clenbuterol poisoning from tainted meat have been reported.

Despite the ban, many farmers continue to use the product illegally. The drug is even allegedly used by members of 4-H and the Future Farmers of America, who frequently dope their show cows, sheep, etc. in the pursuit of a blue ribbon.

Thermogenic Effects

Though it’s often wrongly referred to as a steroid or steroid alternative due to its muscle-building properties, clenbuterol is a stimulant drug known as a beta-2 adrenergic agonist (β2), which means that it creates some of the same reactions experienced with adrenalin (the hormone that causes your heart to race when you get scared or excited).

However, as opposed to adrenalin, which creates all sorts of physiologic responses, clenbuterol is much more selective, primarily affecting only one type of adrenalin-sensitive receptor – the β2 receptor.

There are two main classes of adrenergic receptors and several subtypes (categories) within these two groups. The beta (β) receptors are responsible for most of the recognized effects of adrenalin, including increasing the heart rate and burning fat, as well as promoting muscle growth.

The racing heartbeat is a result of β1 stimulation, so by being relatively specific to the β2 receptors, clenbuterol is able to promote fat loss and muscle growth without substantially affecting the heart rate.

Working at these two sites (the fat cell and the muscles) give clenbuterol the ability to combine both thermogenic (burning calories through heat production) and lipolytic (releasing stored body fat) properties in a single pill.

However, the therapeutic window for clenbuterol is narrow, meaning that people who are very sensitive to the drug or use it in excess will experience a rapid, possibly irregular heartbeat and other side effects that may require hospitalization.

Clenbuterol is distributed in two forms: as a pill or a syrup. Most users prefer the pill, as it can be carried and used discretely. Clenbuterol is commonly dosed at 20 micrograms per tablet, which is a very small amount.

In comparison, a caffeine tablet usually contains 200 milligrams, which is 10,000 times greater by weight. This should offer a clear idea of the potency of this drug.

Users who haven’t tried clenbuterol or those who’ve been off the drug for several weeks or months typically start with one tablet as they’re so sensitive to the drug that a higher dosage may cause tremors, insomnia, nausea and a fast heart rate.

Generally, the dose is gradually increased, based on how well the drug is tolerated, to a typical daily dose range or two to four (40-80 micrograms) tablets for women and two to eight (40-160 micrograms) tablets for men.

Dramatic Shifts in Weight

Though users would love to stay on clenbuterol indefinitely, it’s rarely used for more than a month at a time, even among professional weightlifters. It’s believed that the loss of effect is due to the body reducing the number of β2 receptors, making the drug less effective.

Bodybuilders monitor for this transition by taking their temperature. If the clenbuterol is working, body temperature will be higher than normal while off the drug due to the thermogenic effect of the drug.

After a few weeks, normal body temperature or even lower body temperature will be noted and clenbuterol is discontinued at this time. If the dose is increased, little additional benefit is realized and side effects become prominent.

Due to this down-regulating phenomenon, users cycle on and off clenbuterol, perhaps explaining some of the dramatic changes in weight documented by paparazzi.

Many elaborate dosing schemes have been devised to delay this shutdown in effectiveness, such as using the drug in a two days on/two days off cycle, but to little avail.

The body appears to be defending against overstimulation, and a drug holiday of several weeks is usually necessary to recalibrate the system. Bodybuilders have circumvented the downregulation to some degree by combining a number of other drugs with clenbuterol to maximize and prolong its effectiveness.

Considered pioneers by some, human guinea pigs by others, many of the techniques used in muscle building or weight loss originated among weightlifters.

They are known to use thyroid hormone (Cytomel or T3) and growth hormone to accelerate fat loss, as these agents promote fat loss via separate pathways and protect against β2 receptor down-regulation.

A little known drug called ketotifen, an anti-histamine used to treat allergy symptoms, is also combined with clenbuterol as it’s been shown to upregulate β2 receptors.

Notably, Bill Llewellyn, author of the book Anabolics 2006, reports on a published study demonstrating an increase in β2 receptors in humans when ketotifen is used in combination with clenbuterol, as compared to using clenbuterol by itself.

These findings agree with other published studies.

Unfortunately, despite its effectiveness and popularity, clenbuterol isn’t without risk. Use without proper supervision and training can lead to serious short-term side effects and unknown long-term side effects.

Doomsayers are quick to point out (speculatively) that clenbuterol might cause “heart stiffening” due to animal studies that use exaggeratedly high doses. Curiously, it may actually have protective effects for the heart, according to another animal study.

This conflicting data highlights the need for well-designed studies and monitoring of human clenbuterol exposure.

Buyer Beware

Though it’s of some relief to realize clenbuterol is used safely and effectively as a prescription asthma drug in many countries, one of the greatest concerns in the United States is the modes of acquiring clenbuterol.

The black market – including the many Internet sites – offer a formulary of drugs without the benefits of quality assurance and safety that are taken for granted by U.S. consumers.

Illegitimate products sold as clenbuterol may not contain the drug or the dose may not be consistent with the label or from tablet to tablet, greatly increasing the risk of an adverse event.

Given the increase in demand that’s certain to arise from the widely circulated news stories regarding celebrity use of this drug, it’s certain that the number of phony products or incorrectly dosed tablets will increase.

Adulterated street drugs containing clenbuterol have been reported for years, including a recent outbreak of clenbuterol-adulterated heroin that sent at least 26 identified people into the hospital.

The number of heroin users affected by the drug is certainly much higher, as clenbuterol isn’t detected by most drug screens. In addition, heroin addicts may not have sought medical care or been honest about the cause of their symptoms.

Much of the toxicological history of clenbuterol revolves around tainted meat reaching consumers. However, several reports more relevant to the use of the drug for dieting are found in the literature.

Though the risks and dangers of this drug are overstated when it’s used wisely and under proper supervision, it’s clear that abuse of this drug is dangerous- even deadly.

Consider these demonstrative cases of the risks associated with clenbuterol:

-28-year-old female – dangerous heart rhythm and electrolyte imbalance

-17-year-old male bodybuilder – heart attack

-Two male bodybuilders- tremors, weakness, fast heart rate and palpitations due to tainted, black market drugs

-26-year-old male bodybuilder – heart attack

-73-year-old male – tardive dyskinesia (uncontrolled movements) after five years of 20 micrograms twice a day (two pills daily)

-22-year-old female – suicide attempt, massive overdose, severe muscle breakdown

-34-year-old male bodybuilder – muscle breakdown

Clenbuterol is very effective for fat loss. As a prescription drug in Europe, it’s considered safe and effective for long-term use in treating asthma.

Bodybuilders, baseball players, cyclists and other athletes have been using the drug illicitly for decades and its introduction to Hollywood probably occurred in the late ’80s or early ’90s.

Yet, because the tabloid media is pointing an accusatory finger at anorexic-looking actresses – particularly those who have experienced rapid weight fluctuations – and claiming those emaciated figures are the result of clenbuterol use, demand is already escalating as message boards are filling up with queries and posts about how to obtain and use clenbuterol.

Camp Survivors

Sadly, many people will fall prey to unscrupulous black market dealers selling bogus pills.

Even worse, some are destined to suffer from clenbuterol overdose, either purposefully, in their haste to lose weight, or accidentally, due to poor quality control at a black market lab.

Perhaps worst of all is the revelation of how distorted the image of beauty has become in certain circles.

Few people outside the glamour industries would ever wish to become so thin that bones protrude, muscles become wasted, breasts disappear (unless augmented) and the health and function of most organs become compromised.

These women are forcing themselves, or being forced by others, to experience nutritional deprivation similar to the inhumane practices of prisoner-of-war camp survivors.

Clenbuterol is extremely potent; many cases of clenbuterol poisoning or overdose have already been reported, which likely represent a small percentage of the actual number.

It’s a shame that this potent and effective drug is making news as a black market drug, because legislation will likely make it difficult, if not impossible, to investigate the legitimate use of this or similar drugs for fat loss.

For those who’ve already chosen to use the drug, consider carefully your drug source and monitor your health closely.

Perhaps some good may come of these exploitive news stories if it causes certain powers in Hollywood, New York and Paris to change the demands they place on vulnerable actresses and models.


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