Clenbuterol
Clenbuterol - for drying and weight loss
Clenbuterol (Clenbuterol, "maple") is a drug that is used in medicine to treat bronchial asthma. In recent years, clenbuterol has found widespread use in bodybuilding and fitness due to its ability to burn fat, so it is often used by athletes for weight loss and drying. Clenbuterol courses often include thyroxine and ketotifen to speed up the weight loss process. Clenbuterol is unrelated to anabolic steroids and belongs to the group of adrenomimetics, which exert their physiological effect by stimulating beta-2-adrenoreceptors, as a result of which the sympathetic nervous system is activated and lipolysis is triggered. A prescription is required to purchase the drug.
It can be prescribed to girls without the risk of developing androgenic side effects inherent in anabolic steroids.
Half-life: 36 hours
It can be prescribed to girls without the risk of developing androgenic side effects inherent in anabolic steroids.
Half-life: 36 hours
Doping status
Clenbuterol has been banned by WADA for use in sports since 1992. Standard anti-doping tests usually respond to a concentration of 5-10 ng / l in urine, which is observed 4-5 days after the last intake. More sensitive tests increase the detection time of clenbuterol to 2-3 weeks and above (1-2 ng/l). The drug accumulates in adipose tissue and can be released more actively during exercise or competition.
Meat may be one of the possible ways for clenbuterol to enter the athlete's body, since in some countries (China, Mexico) it is used to increase the weight of fattened animals.
Several scientific articles report the frequent unauthorized inclusion of clenbuterol in sports supplements for fat burning.
Meat may be one of the possible ways for clenbuterol to enter the athlete's body, since in some countries (China, Mexico) it is used to increase the weight of fattened animals.
Several scientific articles report the frequent unauthorized inclusion of clenbuterol in sports supplements for fat burning.
Mechanism of action
Being a beta-2 agonist, clenbuterol acts as a fat burner by binding to type 2 beta receptors in the fat and muscle tissue of the human body. After clenbuterol binds to the receptor, a cascade of biochemical reactions is triggered that lead to an increase in the synthesis of cAMP (cyclic adenosine monophosphate). cAMP, in turn, activates enzymes that mobilize fatty acids from adipocytes (adipose tissue cells).
Anabolic and anti-catabolic effects of clenbuterol
When clenbuterol acts on beta-2-adrenergic receptors of the presynaptic membrane, the release of norepinephrine and adrenaline increases, which have a powerful fat-burning effect. Clenbuterol increases the level of basal metabolism by 20-30% of the initial level.
Clenbuterol suppresses the activity of lipoprotein lipase, as a result of which the deposition of fat in adipose tissue becomes impossible. Acting on beta-2 adrenoreceptors of the central nervous system, this drug enhances the secretion of thyroid hormones[2] - the body's natural fat burners.
The unique feature of clenbuterol is that it is not only a powerful fat burner, but also has a pronounced anti-catabolic effect, protecting muscles from destruction, which is very important during weight loss and drying in bodybuilding. Studies have found that the anti-catabolic effect of the drug is due to the blocking of Ca2+ dependent and ubiquitin-proteasome proteolysis.
Anabolic and anti-catabolic effects of clenbuterol
When clenbuterol acts on beta-2-adrenergic receptors of the presynaptic membrane, the release of norepinephrine and adrenaline increases, which have a powerful fat-burning effect. Clenbuterol increases the level of basal metabolism by 20-30% of the initial level.
Clenbuterol suppresses the activity of lipoprotein lipase, as a result of which the deposition of fat in adipose tissue becomes impossible. Acting on beta-2 adrenoreceptors of the central nervous system, this drug enhances the secretion of thyroid hormones[2] - the body's natural fat burners.
The unique feature of clenbuterol is that it is not only a powerful fat burner, but also has a pronounced anti-catabolic effect, protecting muscles from destruction, which is very important during weight loss and drying in bodybuilding. Studies have found that the anti-catabolic effect of the drug is due to the blocking of Ca2+ dependent and ubiquitin-proteasome proteolysis.
Anabolic and anti-catabolic effects of clenbuterol
A 2012 study (Francesca Wannenes, Loretta Magni) confirms the ability of clenbuterol to block the mechanisms of muscle atrophy.[4] A new 2014 study showed that β-agonists (catecholamines) released during intense physical exercise induce CREB-mediated transcription through activation of its obligate coactivators CRTC2 and Crtc3.
Unlike catabolic activity, which is usually associated with the function of the sympathetic nervous system, activation of Crtc/Creb proteins in skeletal muscles of transgenic mice leads to increased anabolic processes and increased protein synthesis. Thus, in animals with overexpression of CRTC2, the cross-sectional area of myofibrils increases, the content of intramuscular triglycerides and the content of glycogen increases. In addition, there is a significant increase in strength indicators.
Due to the above-mentioned mechanisms, the drug has a moderate anabolic effect, which has been proven in human experiments and practical use in bodybuilding.
Given the fact that the drug practically does not interact with beta-1-adrenergic receptors, bronchial dilation and respiratory relief occur, as well as a much lower frequency of side effects from the cardiovascular system compared with non-selective agonists such as ephedrine.
Unlike catabolic activity, which is usually associated with the function of the sympathetic nervous system, activation of Crtc/Creb proteins in skeletal muscles of transgenic mice leads to increased anabolic processes and increased protein synthesis. Thus, in animals with overexpression of CRTC2, the cross-sectional area of myofibrils increases, the content of intramuscular triglycerides and the content of glycogen increases. In addition, there is a significant increase in strength indicators.
Due to the above-mentioned mechanisms, the drug has a moderate anabolic effect, which has been proven in human experiments and practical use in bodybuilding.
Given the fact that the drug practically does not interact with beta-1-adrenergic receptors, bronchial dilation and respiratory relief occur, as well as a much lower frequency of side effects from the cardiovascular system compared with non-selective agonists such as ephedrine.
Механизм анаболического действия кленбутерола через экспрессию гена СRTC2
Human studies
The 2015 Lee P. study was the first reliable evidence of the effectiveness of beta agonists in humans. An analog of the mechanism of action of formoterol (β2 selective agonist) at a dose of 160 mcg / day stimulated anabolism, increased protein synthesis without causing side effects from the cardiovascular system, while these effects are more pronounced in girls. [6]
In addition, the work of Morten Hostrup (2015) found that the beta-2-adrenomimetic terbutalin (10-15 mg/day) causes a statistically significant increase in lean muscle mass, increases strength and endurance at maximum load on an exercise bike.
In addition, the work of Morten Hostrup (2015) found that the beta-2-adrenomimetic terbutalin (10-15 mg/day) causes a statistically significant increase in lean muscle mass, increases strength and endurance at maximum load on an exercise bike.
Effects of Clenbuterol
- Fat burning and muscle drying
- Increased strength and endurance
- Temperature rise
- Decreased appetite
- Mental activation
- Anti-catabolic effect
- Anabolic effect
- Low frequency of side effects (practice shows that irreversible side effects are almost completely absent) and a wide range of positive effects make clenbuterol one of the best fat burners in bodybuilding.
Some authors (Yuri Bombela) claim that clenbuterol can have catabolic effects in high doses, but this is not true, due to the lack of any physiological or empirical justification.
The course of clenbuterol: weight loss or drying
In men, the recommended dose of clenbuterol for drying and weight loss is 120-140 mcg per day. In women, the average dose of clenbuterol for drying and weight loss is 80-100 mcg per day. The course of clenbuterol has its own subtle features that must be strictly observed in order to avoid side effects.
The duration of the course of clenbuterol is usually 2 weeks, then addiction (receptor tolerance) is developed and the effectiveness decreases. After that, it is necessary to take a 2-week break using ketotifen, without it the break is useless, and then repeat the course; without ketotifen, the break should be much longer. The need for a break was scientifically justified back in 1990: desensitization of beta-adrenergic receptors develops due to phosphorylation of receptors and by other biochemical modifications at the level of secondary messengers (kinases, G-proteins, etc.). It takes several days to update these structures.
The duration and effectiveness of the course of clenbuterol, as mentioned, can be increased by including ketotifen. Sometimes, to prevent the adaptation of receptors, a pulse course is recommended - 2 days of admission, 2 days of rest, but this scheme is less effective.
"Attention" Do not forget to take enough protein, BCAA and other cortisol blockers during the cycle, this will significantly improve the result. Follow an appropriate diet for weight loss or drying.
In 2010, a study was conducted that revealed a synergistic effect when combined with anabolic steroids, which confirms the expediency of including the drug at the end of the course of AS. Many experts do not recommend combining the drug with anabolic steroids, as the risk of heart hypertrophy increases.
The duration of the course of clenbuterol is usually 2 weeks, then addiction (receptor tolerance) is developed and the effectiveness decreases. After that, it is necessary to take a 2-week break using ketotifen, without it the break is useless, and then repeat the course; without ketotifen, the break should be much longer. The need for a break was scientifically justified back in 1990: desensitization of beta-adrenergic receptors develops due to phosphorylation of receptors and by other biochemical modifications at the level of secondary messengers (kinases, G-proteins, etc.). It takes several days to update these structures.
The duration and effectiveness of the course of clenbuterol, as mentioned, can be increased by including ketotifen. Sometimes, to prevent the adaptation of receptors, a pulse course is recommended - 2 days of admission, 2 days of rest, but this scheme is less effective.
"Attention" Do not forget to take enough protein, BCAA and other cortisol blockers during the cycle, this will significantly improve the result. Follow an appropriate diet for weight loss or drying.
In 2010, a study was conducted that revealed a synergistic effect when combined with anabolic steroids, which confirms the expediency of including the drug at the end of the course of AS. Many experts do not recommend combining the drug with anabolic steroids, as the risk of heart hypertrophy increases.
A course of clenbuterol without ketotifen
- day 1: 20 mcg (0.02 mg)
- Day 2: 40 mcg (0.04mg)
- Day 3: 60 mcg (0.06 mg)
- Day 4: 80 mcg (0.08 mg)
- Day 5: 100 mcg (0.10 mg)
- Day 6-12: 120 mcg (0.12 mg)
- Day 13: 80 mcg (0.08 mg)
- day 14: 40 mcg (0.04 mg)
- break
"Attention" The dose of clenbuterol should be progressively increased during the first week. The optimal time to take clenbuterol is in the morning (in order not to provoke insomnia, besides, the effectiveness of the drug is higher in the morning). When increasing the dosage, start taking it in 2 doses: in the morning and after lunch.
The course of clenbuterol + ketotifen
Ketotifen is an antiallergic agent with a unique ability to restore the sensitivity of beta-2-adrenergic receptors to clenbuterol. This property has been repeatedly proven in studies involving not only asthma patients, but also isolated lymphocytes. The mechanism of this effect is obviously not related to histamine receptors, but to the inhibition of phosphodiesterase, which regulates cAMP-dependent metabolism of all cells, which allows extrapolating the results obtained in work with lymphocytes to adipose tissue.
Similar receptor resensitization effects have been observed in ketotifen and in relation to other beta-agonists, which has been confirmed by a large number of studies.
With ketotifen, you can speed up the weight loss or drying process by 10-20 percent and extend the course to 8 weeks. In addition, ketotifen will help eliminate mental agitation, tremor of the limbs, insomnia and palpitations.
Combination: To maximize the effectiveness of the course, clenbuterol is combined with thyroxine. However, in this case, the risk of side effects increases.
Similar receptor resensitization effects have been observed in ketotifen and in relation to other beta-agonists, which has been confirmed by a large number of studies.
With ketotifen, you can speed up the weight loss or drying process by 10-20 percent and extend the course to 8 weeks. In addition, ketotifen will help eliminate mental agitation, tremor of the limbs, insomnia and 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
- for at least two weeks break
Combination: To maximize the effectiveness of the course, clenbuterol is combined with thyroxine. However, in this case, the risk of side effects increases.
Side effects of clenbuterol
The side effects of clenbuterol are listed by frequency of occurrence:
Seizures (in case of overdose or at the initial stage of taking the drug)
In individual cases, a headache is possible, most likely associated with an increase in blood pressure.
As can be seen, many side effects of clenbuterol can be prevented with ketotifen and bisoprolol (metoprolol). Also, it should be noted that most of the side effects are especially pronounced only at the initial stages of the course, and after a few days they subside or disappear completely.
In animal experiments, it has been shown that large doses of clenbuterol can be toxic to the myocardium and testicular tissue.[20][21]
In Ostapenko's book "Anabolic agents" there is information that due to the accumulation of polyamines in cells, clenbuterol can cause a malignant process and lead to an increase in internal organs (in particular myocardial hypertrophy), which can explain the pronounced protrusion of the anterior abdominal wall in many modern athletes. However, there is no scientific and practical confirmation of these statements, so they can only be regarded as guesses of the author. In addition, it was determined that abdominal enlargement in professional athletes is primarily associated with the use of high doses of growth hormone.
Beta 2 receptors are also found in the kidneys, due to which there is an increase in renin secretion, which further leads to the excretion of potassium from the body, therefore, additional intake of asparkam is considered advisable.
Clenbuterol slightly increases insulin secretion. Acting on the receptors of the intestine, it causes its relaxation, which can affect its function: incomplete digestibility of food, diarrhea, flatulence, dysbiosis.
The information in some instructions about bronchospasm after withdrawal is relevant only for people with asthma who have an increased bronchial tree reaction.
"Attention" Caffeine, yohimbine, thyroxine and other stimulants significantly increase the frequency of side effects.
Кленбутерол и алкоголь
It is not recommended to combine clenbuterol and alcohol, as this can increase nausea and palpitations. Clenbuterol and alcohol increase the load on the cardiovascular system. In addition, alcohol prevents weight loss and drying. Alcohol destroys muscles. Read the main article: alcohol and muscles.
- Palpitations (60%) - eliminated by beta-1 blockers. Take 5 mg of Bisoprolol or 50 mg of Metoprolol in the morning.
- Trembling (20%) is especially pronounced on the first day of admission, then gradually fades away. It is eliminated by ketotifen.
- Sweating (10%)
- Insomnia (7%) - eliminated by ketotifen
- Anxiety (6%) - eliminated by ketotifen
- An increase in blood pressure (6%) is eliminated by beta-1 blockers. Take 5 mg of Bisoprolol or 50 mg of Metoprolol in the morning.
- Stool disorder - diarrhea (5%) - is usually observed only in the first days of taking the drug
- Nausea (3%)
Seizures (in case of overdose or at the initial stage of taking the drug)
In individual cases, a headache is possible, most likely associated with an increase in blood pressure.
As can be seen, many side effects of clenbuterol can be prevented with ketotifen and bisoprolol (metoprolol). Also, it should be noted that most of the side effects are especially pronounced only at the initial stages of the course, and after a few days they subside or disappear completely.
In animal experiments, it has been shown that large doses of clenbuterol can be toxic to the myocardium and testicular tissue.[20][21]
In Ostapenko's book "Anabolic agents" there is information that due to the accumulation of polyamines in cells, clenbuterol can cause a malignant process and lead to an increase in internal organs (in particular myocardial hypertrophy), which can explain the pronounced protrusion of the anterior abdominal wall in many modern athletes. However, there is no scientific and practical confirmation of these statements, so they can only be regarded as guesses of the author. In addition, it was determined that abdominal enlargement in professional athletes is primarily associated with the use of high doses of growth hormone.
Beta 2 receptors are also found in the kidneys, due to which there is an increase in renin secretion, which further leads to the excretion of potassium from the body, therefore, additional intake of asparkam is considered advisable.
Clenbuterol slightly increases insulin secretion. Acting on the receptors of the intestine, it causes its relaxation, which can affect its function: incomplete digestibility of food, diarrhea, flatulence, dysbiosis.
The information in some instructions about bronchospasm after withdrawal is relevant only for people with asthma who have an increased bronchial tree reaction.
"Attention" Caffeine, yohimbine, thyroxine and other stimulants significantly increase the frequency of side effects.
Кленбутерол и алкоголь
It is not recommended to combine clenbuterol and alcohol, as this can increase nausea and palpitations. Clenbuterol and alcohol increase the load on the cardiovascular system. In addition, alcohol prevents weight loss and drying. Alcohol destroys muscles. Read the main article: alcohol and muscles.
Anabolic drugs may only be used by a doctor's prescription and are contraindicated in children. The information provided does not call for the use or distribution of potent substances and is aimed solely at reducing the risk of complications and side effects.