Clenbuterol is a drug that has gained attention for its potential to promote weight loss and muscle gain. While it is sometimes prescribed for asthma and breathing difficulties in some countries, its use in humans is banned in the United States. This article explores how clenbuterol works, its uses, risks, and other important information.
What is Clenbuterol?
Clenbuterol is a beta-2-adrenergic agonist, functioning as a decongestant and bronchodilator by widening airways. It is a long-acting and potent β2-adrenergic agonist with sympathomimetic actions. In some countries, doctors prescribe clenbuterol as a treatment for asthma or chronic pulmonary obstructive disorder (COPD). However, it is illegal for human consumption in the United States due to its hazardous health effects. It is also banned worldwide in sports and competitions.
The drug's effects are similar to those of amphetamines, leading to:
- Excitability
- Nervousness
- Increased energy
- Increased metabolism
- More rapid fat burning
Misuse of Clenbuterol
Since becoming available, people have misused clenbuterol in various ways, including:
- Building muscle
- Enhancing athletic performance
- Losing weight
- Increasing the growth of livestock
- Lacing other drugs, such as heroin and cocaine
Athletes and bodybuilders taking clenbuterol will have differing doses depending on individual factors, such as drug tolerance. They will often take the drug in a cycle that includes “on” and “off” periods. Individuals using clenbuterol off-label to promote leanness often resort to 2-3 week on-off cycles to offset tolerance development. Although the concept of tolerance development upon chronic exposure to β2-agonists is a well-described phenomenon, less is known about its implication for myocellular signalling events important for muscle hypertrophy.
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Clenbuterol for Weight Loss and Muscle Gain
Clenbuterol is misused as a way of gaining muscle, increasing athletic performance, or losing weight. However, there is little research showing the drug causes these effects in humans. The same beta2-adrenergic receptors that activate when taking clenbuterol for asthma also help increase lean muscle mass while decreasing body fat. Because of such effects, clenbuterol is sometimes seen as an alternative to anabolic steroids - the drugs that typically come to mind when you think of performance-enhancing substances. Clenbuterol is not a steroid, but it acts a bit like one. It can build lean muscle mass and decrease fat. So, bodybuilders misuse clenbuterol to reshape their bodies. They may take clenbuterol along with anabolic steroids or growth hormone. Some may have body dysmorphia, thinking that their body is flawed and not muscular or strong enough.
Clenbuterol increases the resting metabolic rate by 10%-50%. That means your metabolism is primed to burn more calories. Energy is stored in the body’s cells, including fat cells. When your body uses stored energy, it will burn the sugars and fats you’ve stored. This can reduce your body fat and overall weight.
Studies in livestock have indicated that the increase in muscle growth occurs at the expense of fat tissue. This is part of a process referred to as repartitioning. A study in horses found that long-term administration of high doses of clenbuterol increased the expression of genes related to various muscle components and fat metabolism.
Scientific Studies on Clenbuterol
Despite the prevalent abuse of clenbuterol and claims of it being ‘probably the best fat burner,’ hailed for its ability to induce leanness and enhance performance, randomized controlled trials in healthy humans are sparse. However, whether this translates into lean mass gain and fat mass reduction with prolonged treatment is unclear. Based on studies in animals, there is a good reason to assume this is the case.
Horses treated with clenbuterol gained around 8% lean mass and lost in the excess of 15% fat mass after just 2 weeks of treatment. We also know from other substances within the drug class that β2-agonists effectively induce muscle hypertrophy in humans. The commonly prescribed β2-agonists salbutamol and formoterol, both of which have shorter half-lives and durations of action than clenbuterol, have been shown to act muscle anabolic in humans. Furthermore, terbutaline, a short-acting β2-agonist commonly prescribed in Northern Europe, increased lean mass by around 1.5 kg at the same time as lowering fat mass over the course of only 2-4 weeks.
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In young healthy men, clenbuterol ingestion significantly influences various metabolic parameters. It increases the resting metabolic rate by 21% and enhances fat oxidation by 39%. At the molecular level, clenbuterol elevates the phosphorylation of mTOR at Ser2448 by 121% and protein kinase A (PKA) substrates by 35%, indicating enhanced anabolic and adrenergic signaling.
Doses and Administration
When clenbuterol is prescribed to treat asthma in other countries, the dose is usually 0.04-0.06 milligrams per day. Athletes and bodybuilders who use clenbuterol - also called clen - typically take two to three times that amount (0.06 to 0.12 milligrams) per day. Even at low doses, clenbuterol can be toxic.
Clenbuterol used for weight loss or performance enhancement can be acquired as a tablet, liquid, or injection. People using clenbuterol for this purpose typically use between 0.06 and 0.12 milligrams per day, which is higher than the recommended dosage for asthma treatment.
Side Effects and Risks
Clenbuterol has serious risks for those who take it regularly, which is why many governing bodies have banned it in many countries. The risks include:
- Unpleasant side effects, such as anxiety, shaking, sweating, and headaches
- Fast heart rate
- High blood sugar
- Low potassium
- Low magnesium
- Low phosphate levels
- High lactate levels
All beta-agonists have the potential to harm the heart by making it work harder. A 2018 study notes there is evidence clenbuterol can lead to:
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- A fast heart rate
- Atrial fibrillation, which is an irregular and often fast heartbeat
- Myocardial ischemia, which is when the heart does not receive enough oxygen and blood
Clenbuterol can cause serious poisoning and, in some cases, death. A 2020 case study notes that there is an increasing number of such cases in United States hospitals. The symptoms of clenbuterol toxicity include:
- Nausea
- Chest pain
- Shortness of breath
- Agitation
- Confusion
- Shaking
- Seizures
- Rhabdomyolysis
- Myocardial ischemia
- Cardiogenic shock
- Heart attack
Clenbuterol can be fatal, even in what seems like small doses. Most people who experience poisoning need hospital treatment.
Long-Term Effects
Prolonged use of clenbuterol can also impose adverse effects on cardiac function and exercise capacity. Individuals using clenbuterol off-label to promote leanness often resort to 2-3 week on-off cycles to offset tolerance development. Repeated exposure to clenbuterol may lead to attenuated activation of β2-adrenergic signalling pathways, including canonical cAMP-PKA signalling and downstream effectors regulating protein synthesis.
Clenbuterol and the Liver
Oral clenbuterol affects the liver and may cause liver toxicity or damage over prolonged use or in high enough doses.
Detection in Drug Tests
Clenbuterol can show up in drug tests that look for traces of performance-enhancing drugs. However, standard drug panels that look for common recreational drugs, such as cocaine or cannabis, may not include tests for clenbuterol. It will depend on the type of test a person is taking.
Effects on the Heart
Clenbuterol is not beneficial for the heart. It can increase heart rate and force this organ to work harder. Over time, this can lead to heart enlargement. Clenbuterol can also cause an irregular heartbeat and atrial fibrillation. At some doses, the drug may lead to a heart attack.
Clenbuterol for Women
Clenbuterol may be more popular than anabolic steroids with female bodybuilders because of fewer side effects. Anabolic steroids typically cause side effects such as increased facial hair, thickening of the skin, and deepening of your voice.
Ethical Concerns
The widespread misuse of clenbuterol raises ethical concerns in competitive environments. Testing is conducted in World Anti-Doping Agency (WADA)-accredited laboratories, and even unintentional ingestion must be proven by the athlete. If confirmed, the athlete may face provisional suspension, sanctions, or disqualification.
Motivations for Unsupervised Use
The unsupervised utilization of clenbuterol among athletes and bodybuilders is a growing concern, driven by a desire to enhance physical appearance and performance without medical oversight.
- Desire for an "extraordinary self": Bodybuilders often perceive clenbuterol as a means of rapidly achieving a competitive physique, aligning with their identity as high-performing athletes.
- Balancing athletic aspirations and everyday life: Athletes may rationalize the use of clenbuterol as a necessary step to maintain both their athletic goals and personal lives.
- Peer influence and social norms: The normalization of clenbuterol use within bodybuilding communities significantly influences unsupervised utilization.
- Societal expectations and media influence: Social media platforms and online fitness communities often portray clenbuterol as a harmless and effective shortcut to the ideal physique.
- Ambiguity in risk perception: Users often perceive themselves as sufficiently knowledgeable to manage the risks associated with clenbuterol.
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