Clenbuterol (Clenbuterol , “Maple”) – a drug that is used in medicine for the treatment of bronchial asthma. In recent years, clenbuterol is widely used in bodybuilding and fitness in relation to its ability to burn fat, so it is often used by athletes for weight loss and drying. Cycles clenbuterol often include thyroxine and ketotifen to accelerate the weight loss process. Clenbuterol is not related to anabolic steroids and belongs to the group of agonists that exert their physiological effect due to excitation of the beta 2-adrenergic receptors, resulting in the sympathetic nervous system is activated and starts lipolysis . To purchase the drug requires a prescription.
Several scientific papers have reported frequent unauthorized inclusion of clenbuterol in the sports supplements for fat burning.
The mechanism of action
It is a beta-2 agonist, clenbuterol acts as a fat burner, binding to beta-receptor type 2 in adipose and muscle tissues of the human body. Once the receptor binds clenbuterol, starts a cascade of biochemical reactions that lead to increased synthesis of cAMP (cyclic adenosine monophosphate). cAMP in turn activates enzymes that mobilize fatty acids from adipocytes (fat tissue cells).
The action of clenbuterol on the beta-2-adrenergic receptors of the presynaptic membrane is enhanced release of noradrenaline and adrenaline, which possess potent fat-burning effect. Clenbuterol increases the basal metabolism by 20-30% from baseline.
Clenbuterol inhibits the activity of lipoprotein lipase, it becomes impossible resulting in the deposition of fat in adipose tissue. Acting beta-2-adrenergic receptors of the central nervous system, the drug enhances the secretion of thyroid hormones – zhiroszhigateli natural organism.
A unique feature of Clenbuterol is that it is not only a powerful fat burner, but also has a strong anti-catabolic effect , protecting muscles from breaking down, which is very important during weight loss and drying in bodybuilding. Studies have shown that anti-catabolic effects of the drug caused by blocking Ca 2+ dependent and ubiquitin-proteasome proteolysis.
A study in 2012 (Francesca Wannenes, Loretta Magni) confirms the ability of clenbuterol to block the mechanisms of muscle atrophy. A new study in 2014 showed that β-agonists (catecholamines) released during intense exercise cause CREB-mediated transcription through the activation of its obligate coactivators CRTC2 and Crtc3.
Due to the above-mentioned mechanisms drug has moderate anabolic effect, as evidenced in human experiments and practical application in bodybuilding.
Given the fact that the preparation hardly interacts with beta-1-adrenergic receptors occur expansion and bronchial respiratory relief, as well as a much lower frequency of side effects to the cardiovascular compared with nonselective agonists system, such as ephedrine.
Studies in humans
Study Lee P. 2015 became the first reliable evidence of the effectiveness of beta-agonists in humans. An analogue of the mechanism of action of formoterol ( .beta.2 selective agonist) at a dose of 160 mg/day stimulate anabolism, increased protein synthesis, without causing side effects of the cardiovascular system, while these effects are more pronounced in women.
In addition, in Morten Hostrup (2015) found that the beta-2-agonists terbutaline (10-15 mg/day) causes a statistically significant increase in lean body mass, increases strength and endurance at maximum load on a stationary bike.
- Fat burning and drying of muscles
- Increased strength and endurance
- Temperature increase
- Decreased appetite
- Mental activation
- anti-catabolic effect
- Anabolic action
The low incidence of adverse events (practice shows that irreversible side effects is almost totally absent) and a wide range of positive effects of clenbuterol make one of the best fat burners bodybuilding.
Some writers (Yuri BOMBEL) argue that large doses of clenbuterol may have catabolic effects, but this is not true, in the absence of any physiological or empirical justification.
Cycle clenbuterol: weight loss or drying
In men, the recommended dose of clenbuterol for drying and losing weight is 120 – 140 micrograms per day. In women, the average dose of clenbuterol for drying and losing weight is 80-100 mg per day. clenbuterol cycle has its subtle features that must be followed strictly in order to avoid side effects.
Duration Clenbuterol is usually 2 weeks, then produced addictive (tolerance receptors) and reduced effectiveness. After that you need to do 2 week break with ketotifen , without a break of no use, and then repeat the cycle; ketotifen without a break should be much larger. Need a break scientifically proved in 1990: desensitization of beta-adrenergic receptors developed by phosphorylation of the receptors, and by other biochemical modifications at the level of second messengers (kinases, G-proteins, and others.). In the update of these structures requires several days.
The duration of the cycle and efficiency of clenbuterol, as has been said, can be increased by the inclusion of ketotifen. Sometimes, to prevent receptor adaptation recommended pulse rate – 2 days of reception, 2 rest days, but this scheme is less efficient.
Do not forget during the cycle to take a sufficient amount of protein, BCAA’s and other blockers, cortisol , it will significantly improve the result. Observe proper diet for weight loss or drying .
In 2010, a study, which revealed a synergistic effect when combined with anabolic steroids, which confirms the desirability of placing on the drug at the end of the AU cycle. Many experts do not recommend to combine the drug with anabolic steroids, because the risk of heart hypertrophy.
Clenbuterol cycle without ketotifen
- Day 1: 20 g (0,02mg)
- Day 2: 40 mg (0,04mg)
- Day 3: 60 ug (0,06mg)
- Day 4: 80 g (0,08mg)
- Day 5: 100 mg (0.10 mg)
- Day 6-12: 120 mg (0.12 mg)
- Day 13: 80 mcg (0.08 mg)
- Day 14: 40 micrograms (0,04mg)
Clenbuterol dose should increase progressively during the first week. The optimal time for receiving clenbuterol – in the morning (not to provoke insomnia, also in the morning the effectiveness of the drug above). By increasing the dosage start to take it in 2 divided doses, morning and afternoon.
Cycle clenbuterol + Ketotifen
Ketotifen – antiallergic agent, with the unique ability to restore the sensitivity of beta-2-adrenergic receptors to clenbuterol. This property has been repeatedly demonstrated in the studies. With ketotifen 10-20 percent can accelerate the process of weight loss and prolong the drying rate of up to 8 weeks. Everything else, ketotifen help eliminate mental agitation, tremor of limbs, insomnia, and heart palpitations.
- Day 1: 20 mcg Clenbuterol
- Day 2: 40 mcg Clenbuterol
- Day 3: 60 mcg Clenbuterol
- Day 4: 80 mcg Clenbuterol
- Day 5: 100 mcg Clenbuterol + 1 mg ketotifen
- Day 6-27: 120 mcg Clenbuterol + 2 mg ketotifen
- Day 28: 80 mcg Clenbuterol + 2 mg ketotifen
- Day 29: 50 mcg Clenbuterol + 1-2 mg ketotifen
- Day 30: 33-35 mcg Clenbuterol + 1 mg ketotifen
- at least two weeks interval
Ketotifen is taken at night, clenbuterol – in the morning. Dose distribution is the same as in the previous example.
Combination: To maximize the effectiveness of the cycle Clenbuterol is combined with thyroxine . However, in this case the risk of side effects.
Cycle Clenbuterol + T3 + yohimbine
See main article: The combination with thyroxine and yohimbine
Side effects Clenbuterol
The side effects of clenbuterol are listed by frequency of occurrence:
- Palpitations (60%) – is eliminated beta 1-blockers. Take 5 mg of bisoprolol, or metoprolol 50 mg in the morning.
- Shivers (20%) – is particularly pronounced in the first day of admission, then gradually fades away. Ketotifen is eliminated.
- Sweating (10%)
- Insomnia (7%) – ketotifen is eliminated
- Anxiety (6%) – ketotifen is eliminated
- Increased blood pressure (6%) – eliminated beta 1 blockers. Take 5 mg of bisoprolol, or metoprolol 50 mg in the morning.
- Violation of the chair – diarrhea (5%) – as a rule, is observed only in the first days of dosing
- Nausea (3%)
- Convulsions (with overdose or at the initial stage of the drug)
- In individual cases, possible headache, most likely associated with an increase in blood pressure.
As you can see, many of the side effects of clenbuterol can be prevented with ketotifen and bisoprolol (metoprolol). Also, it should be noted that the majority of side effects are particularly pronounced only in the early stages of the cycle, and they subside or disappear completely within a few days.
The book Ostapenko “Anabolic means” there is information that due to the accumulation of polyamines in cells, clenbuterol can cause malignant process and lead to an increase in the internal organs (such as cardiac hypertrophy), which may explain the pronounced protrusion of the anterior abdominal wall in many of today’s athletes . However, these statements do not have a scientific and practical evidence, so they can only be regarded as the author of the guesswork. In addition, it was determined that an increase in abdominal cavity of professional athletes is primarily due to the use of high doses of growth hormone .
The information in some of the instructions of bronchospasm after cancellation is only valid for people with asthma, bronchial tree whose reaction is increased.
Clenbuterol and alcohol
It is not recommended to combine clenbuterol and alcohol, as this may enhance nausea and palpitations. Clenbuterol alcohol increase and the load on the cardiovascular system. In addition, alcohol interferes with weight loss and drying. Alcohol destroys muscles.