To reduce weight in bodybuilding, medications are actively used that were not originally intended for this purpose. In particular, Clenbuterol (unofficial name - Clen) is a bronchodilator that reduces swelling in lung diseases. But bodybuilders take it to burn fat during the cutting phase. The lack of androgenic effect characteristic of anabolic steroids allows Clenbuterol to be used for weight loss in women. Girls usually combine it with intense fitness programs, thus losing up to 5 kg per course.
Clenbuterol - for drying and losing weight[edit | edit code]
Clenbuterol - a drug for 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, and is therefore often used by athletes for weight loss and cutting. Clenbuterol courses often include thyroxine and ketotifen to speed up the weight loss process. Clenbuterol is not related to anabolic steroids and belongs to the group of adrenomimetics, which exert their physiological effect by stimulating beta-2 adrenergic receptors, as a result of which the sympathetic nervous system is activated and lipolysis is triggered. A prescription is required to purchase the drug.
Can be prescribed to girls, without the risk of developing androgenic side effects characteristic of anabolic steroids.
Half-life:
36 hours
Doping status[edit | edit code]
Clenbuterol has been banned by WADA for use in sports since 1992. Standard anti-doping tests usually respond to a urine concentration of 5-10 ng/L, which is observed 4-5 days after the last dose. More sensitive tests increase the detection time for clenbuterol to 2-3 weeks or higher (1-2 ng/L). The drug accumulates in adipose tissue and can be more actively released during exercise or competition.
One of the possible ways that clenbuterol enters an athlete’s body may be through meat, since in some countries (China, Mexico) it is used to increase the weight of fattened animals.
Several scientific articles report the frequent inappropriate inclusion of clenbuterol in fat-burning supplements.[1]
Mechanism of action[edit | edit code]
As a beta-2 agonist, clenbuterol acts as a fat burner by binding to type 2 beta receptors in adipose and muscle tissue of the human body. After clenbuterol binds to the receptor, a cascade of biochemical reactions is launched that lead to an increase in the synthesis of cAMP (cyclic adenosine monophosphate). cAMP, in turn, activates enzymes that mobilize fatty acids from adipocytes (fat tissue cells).
Anabolic and anti-catabolic effects of clenbuterol
The action of clenbuterol on beta-2-adrenergic receptors of the presynaptic membrane increases the release of norepinephrine and adrenaline, which have a powerful fat-burning effect. Clenbuterol increases the level of basal metabolism by 20-30% of the initial level.
Clenbuterol inhibits the activity of lipoprotein lipase, as a result of which fat deposition in adipose tissue becomes impossible. Acting on beta-2 adrenergic receptors of the central nervous system, this drug enhances the secretion of thyroid hormones [2] - the body's natural fat burners.
A 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 cutting in bodybuilding. Studies have found that the anti-catabolic effect of the drug is due to blocking Ca2+-dependent and ubiquitin-proteasome proteolysis.[3]
The mechanism of the anabolic action of clenbuterol through the expression of the CRTC2 gene
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 exercise induce CREB-mediated transcription through activation of its obligate coactivators CRTC2 and Crtc3.[5]
In contrast to the catabolic activity typically associated with sympathetic nervous system function, activation of Crtc/Creb proteins in skeletal muscle of transgenic mice results in enhanced anabolic processes and increased protein synthesis. Thus, in animals overexpressing CRTC2, myofibril cross-sectional area increases, intramuscular triglyceride content and glycogen content increase. In addition, there is a significant increase in strength indicators.
Due to the above mechanisms, the drug has a moderate anabolic effect, which has been proven in experiments on humans and practical use in bodybuilding.
Given the fact that the drug has virtually no interaction with beta-1 adrenergic receptors, there is bronchodilation and easier breathing, as well as a much lower incidence of side effects from the cardiovascular system compared to non-selective agonists such as ephedrine.
Human studies[edit | edit code]
A 2015 study by Lee P. was the first reliable evidence of the effectiveness of beta-agonists in humans. Analogous to 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, and these effects were more pronounced in girls. [6]
In addition, Morten Hostrup (2015) found that the beta-2 adrenergic agonist terbutaline
(10-15 mg/day) causes a statistically significant increase in lean muscle mass, increases strength and endurance at maximum load on an exercise bike.[7]
Effects of clenbuterol[edit | edit code]
- Burning fat and drying muscles
- Increased strength and endurance[8][9]
- Temperature increase
- Decreased appetite
- Psychic activation
- Anti-catabolic effect
- Anabolic effect[10]
The low incidence 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 in large doses clenbuterol may have catabolic effects, but this is not true, due to the lack of any physiological or empirical justification.
Application in bodybuilding
So, let's take a closer look at what clenbuterol helps with when used as a sports nutrition supplement. Its main advantage is its assistance in drying out the athlete. It is used as a fat burner before competitions. However, it is worth noting that in bodybuilding it is considered a doping and traces of its use can be detected in the body within two to three weeks.
This is not a hormonal drug, which means it is suitable for weight loss for both men and girls. The main condition for achieving a great effect is combination with proper nutrition and intense training.
Despite the fact that some athletes use clenbuterol alone, it is recommended to combine it with drugs that can enhance its properties, or prevent the body from getting used to the active substance. There are many recipes for such a combined technique and we will look at them below.
Clenbuterol course: losing weight or cutting[edit | edit code]
In men, the recommended dose of clenbuterol for drying and losing weight is 120 - 140 mcg per day. In women, the average dose of clenbuterol for drying and losing weight is 80-100 mcg per day. The course of clenbuterol has its own subtle features that must be strictly followed to avoid side effects.
The duration of a course of clenbuterol is usually 2 weeks, then addiction develops (receptor tolerance) and effectiveness decreases. After which you need 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 substantiated back in 1990: desensitization of beta-adrenergic receptors develops due to phosphorylation of receptors and through other biochemical modifications at the level of secondary messengers (kinases, G-proteins, etc.). These structures take several days to update.[11]
The duration and effectiveness of the clenbuterol course, as mentioned, can be increased by including ketotifen. Sometimes, to prevent adaptation of receptors, a pulse course is recommended - 2 days of intake, 2 days of rest, but this scheme is less effective.
Do not forget to take enough protein, BCAA and other cortisol blockers during your cycle, this will significantly improve the result. Follow an appropriate diet for weight loss or cutting.
In 2010, a study was conducted that revealed a synergistic effect when combined with anabolic steroids, which confirms the advisability of including the drug at the end of the AC cycle.[12] Many experts do not recommend combining the drug with anabolic steroids, as the risk of cardiac hypertrophy increases.
A course of clenbuterol without ketotifen[edit | edit code]
- day 1: 20 mcg (0.02 mg)
- day 2: 40 mcg (0.04 mg)
- 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
The dose of clenbuterol should be increased progressively during the first week. The optimal time to take clenbuterol is in the morning (so as not to provoke insomnia, and in the morning the effectiveness of the drug is higher). When increasing the dosage, start taking it in 2 doses: morning and afternoon.
Course of clenbuterol + ketotifen[edit | edit code]
Ketotifen
- an antiallergic agent with the 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.[13][14][15] The mechanism of this effect is obviously associated not with histamine receptors, but with inhibition of phosphodiesterase [16], which regulates the cAMP-dependent metabolism of all cells, which allows us to extrapolate the results obtained in work with lymphocytes to adipose tissue.
Similar receptor resensitization effects have been observed with ketotifen and other beta-agonists, which has been supported by a large number of studies.[17][18]
With the help of ketotifen, you can speed up the process of losing weight or drying by 10-20 percent and extend the course up to 8 weeks. In addition, ketotifen will help eliminate mental agitation, tremors of the limbs, insomnia and rapid heartbeat.
- 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 break
Ketotifen is taken at night, clenbuterol - in the morning. The dose distribution is the same as in the previous example.
Combination:
To maximize the effectiveness of the course, clenbuterol is combined with thyroxine. However, in this case the risk of side effects increases.
Course of clenbuterol + T3 + yohimbine[edit | edit code]
Read the main article:
Combination with thyroxine and yohimbine
Compound
The main active ingredient is clenbuterol hydrochloride. The concentration in tablets can vary from 20 to 60 mcg depending on the manufacturer. Most often, tablets are available in a dosage of 40 mg. In addition to the active ingredient, the composition includes gelatin and maltodextrin, which perform auxiliary functions. It is also available in syrup form. However, since the syrup contains sugar, this form of release is not recommended for a bodybuilder, and the effect of its use is lower.
Side effects of clenbuterol[edit | edit code]
Side effects of clenbuterol are listed by frequency of occurrence:
- Palpitations (60%) - eliminated by beta-1 blockers. Take 5 mg of Bisoprolol or 50 mg of Metoprolol in the morning.
- Trembling (20%) - especially pronounced on the first day of use, then gradually fades away. Eliminated by ketotifen.
- Sweating (10%)
- Insomnia (7%) - eliminated with ketotifen
- Anxiety (6%) - eliminated with ketotifen
- Increased blood pressure (6%) - eliminated by beta-1 blockers. Take 5 mg of Bisoprolol or 50 mg of Metoprolol in the morning.
- Abnormal bowel movements - diarrhea (5%) - as a rule, observed only in the first days of taking the drug
- Nausea (3%)
- Convulsions (in case of overdose or at the initial stage of taking the drug)
- In individual cases, a headache is possible, most likely associated with increased blood pressure.
As you can see, many of the side effects of clenbuterol can be prevented with the help of ketotifen and bisoprolol (metoprolol). Also, it should be noted that most side effects are especially pronounced only in the initial stages of the course, and after a few days they subside or completely disappear.
Animal studies have shown that large doses of clenbuterol can be toxic to the myocardium,[19] and testicular tissue.[20][21]
Ostapenko’s book “Anabolic Drugs” contains 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 or practical confirmation of these statements, so they can only be regarded as the author’s guesses. In addition, it has been determined that abdominal enlargement in professional athletes is primarily associated with the use of large doses of growth hormone.
Beta 2 receptors are also found in the kidneys, due to which there is an increase in the secretion of renin, which subsequently leads to the removal of potassium from the body, so additional intake of asparkam is considered advisable.
Clenbuterol slightly increases insulin secretion. By acting on intestinal receptors, it causes its relaxation, which can affect its function: incomplete digestion of food, diarrhea, flatulence, dysbacteriosis.
The information in some instructions about bronchospasm after withdrawal is relevant only for people with asthma in whom the reaction of the bronchial tree is increased.
Caffeine, yohimbine, thyroxine and other stimulants significantly increase the incidence of side effects.
Clenbuterol and alcohol[edit | edit code]
It is not recommended to combine clenbuterol and alcohol, as this may increase nausea and palpitations. Clenbuterol and alcohol increase the load on the cardiovascular system. In addition, alcohol interferes with weight loss and drying. Alcohol destroys muscles. Read the main article:
alcohol and muscles.
Lose weight with the help of "Saltos"
In pharmacies, clenbuterol is sold only in the form of syrup, and the tablets are distributed illegally by special dealers (it is from them that most athletes buy the drug). But there is a complete substitute for clenbuterol - Saltos. The drug has a similar mechanism of action on the body, except for one thing - it is eliminated much faster. Because of this, Saltos for weight loss is taken one tablet three times a day. If the body’s tolerance is good, then the dose can be doubled (that is, take 2 tablets three times a day). In other respects, the course of treatment is no different.
Notes[edit | edit code]
- Parr MK, Koehler K, Clenbuterol marketed as a dietary supplement. Biomed Chromatogr. 2008 Mar;22(3):298-300.
- Katsumata M, Yano H, Miyazaki A. Effect of beta agonist clenbuterol on the body composition of rats with hypothyroidism induced by oral administration of propylthiouracil. J Nutr Sci Vitaminol (Tokyo). 1991 Aug;37(4):411-7.
- Yimlamai T, Dodd SL — Clenbuterol induces muscle-specific attenuation of atrophy through effects on the ubiquitin-proteasome pathway. J Appl Physiol. 2005 Jul;99(1):71-80. Epub 2005 Mar 17.
- Francesca Wannenes, Loretta Magni. In Vitro Effects of Beta-2 Agonists on Skeletal Muscle Differentiation, Hypertrophy, and Atrophy. World Allergy Organization Journal 2012, 5:66-72
- Bruno NE et al. Creb coactivators direct anabolic responses and enhance performance of skeletal muscle //The EMBO journal. – 2014. – T. 33. – No. 9. – pp. 1027-1043.
- Lee P. et al. Formoterol, a Highly β 2-Selective Agonist, Induces Gender-Dimorphic Whole Body Leucine Metabolism in Humans //Metabolism. – 2015. – T. 64. – No. 4. – pp. 506-512.
- https://jap.physiology.org/content/early/2015/07/07/japplphysiol.00319.2015
- Thieme D., Hemmersbach P. Doping in sports. – Heidelberg, Germany: Springer, 2010. – Pp. 239
- Hostrup M. et al. Mechanisms underlying enhancements in muscle force and power output during maximal cycle ergometer exercise induced by chronic β2-adrenergic stimulation in men // Journal of Applied Physiology. – 2015. – T. 119. – No. 5. – pp. 475-486.
- https://www.ncbi.nlm.nih.gov/pubmed/25650070
- Hausdorff WP, Caron MG, Lefkowitz RJ Turning off the signal: desensitization of beta-adrenergic receptor function //The FASEB Journal. – 1990. – T. 4. – No. 11. – pp. 2881-2889. https://www.fasebj.org/content/4/11/2881.full.pdf+html
- Ung RV, Rouleau P, Effects of co-administration of clenbuterol and testosterone propionate on skeletal muscle in paraplegic mice. J Neurotrauma. 2010 Jun;27(6):1129-42.
- "Effects of ketotifen and clenbuterol on beta-adrenergic receptor functions of lymphocytes and on plasma TXB-2 levels of asthmatic patients." Huszar E, Herjavecz I, Böszörmenyi-Nagy G, Slapke J, Schreiber J, Debreczeni LA. Z Erkr Atmungsorgane. 1990;175(3):141-6.
- "Effects of ketotifen on the responsiveness of peripheral blood lymphocyte beta-adrenergic receptors." Polson JB, Lockey RF, Bukantz SC, Lowitt S, Krzanowski JJ Jr, Szentivanyi A. - Z Erkr Atmungsorgane. 1990;175(3):141-6.
- "Effects of calcium channel blockers and ketotifen on beta 2 adrenergic receptor regulation in intact human lymphocytes." Hui KK, Yu JL. — Res Commun Chem Pathol Pharmacol. 1989 Jul;65(1):3-19.
- https://www.drugbank.ca/drugs/DB00920
- Brodde OE et al. Terbutaline-induced desensitization of beta 2-adrenoceptor in vivo function in humans: attenuation by ketotifen //Journal of cardiovascular pharmacology. – 1992. – T. 20. – No. 3. – pp. 434-439.
- Pauwels R., Van der Straeten M. The effect of ketotifen on bronchial beta-adrenergic tachyphylaxis in normal human volunteers // Journal of allergy and clinical immunology. – 1988. – T. 81. – No. 4. – pp. 674-680.
- Burniston, J. G., et al. (2002). Myotoxic effects of clenbuterol in the rat heart and soleus muscle. J Appl Physiol. 93:1824-32.
- Blanco, A., et al. (2002). Testicular damage from anabolic treatments with the beta(2)-adrenergic agonist clenbuterol in pigs: a light and electron microscope study. The Veterinary Journal. 163:292-98.
- Blanco, A., et al. (2001). Morphological and quantitative study of the Leydig cells of pigs fed with anabolic doses of clenbuterol. Res in Veterinary Science. 71:85-91.
Workout
The effect of using the drug will be much more noticeable if it is combined with a training system. This is a fat burner that works on its own and the effect of its combination with sports will be stunning. Each athlete decides how to train for cutting based on the characteristics of the body. However, general training requirements include adding cardio to strength training, as well as increasing the number of repetitions by reducing the weight used.
Action
In terms of its action, it belongs to adrenergic agonists, i.e. to drugs that trigger natural fat burning processes in the body. The mechanism of action of clenbuterol for weight loss is to use the athlete’s own body reserves. Excess fat deposits are removed due to the activation of lipolysis - increased processing of subcutaneous fat for energy.
The main component of the drug is clenbuterol hydrochloride. In terms of its action, it does not belong to anabolic steroids, that is, it is not prohibited. In addition to fat burning, the drug affects the body in the following ways:
- Speeds up metabolism, which also has a positive effect on the weight loss process.
- It suppresses catabolism, that is, it prevents the body from burning muscles during intense training. And although the effect of clenbuterol as an anti-catabolic is insignificant, it should not be taken into account at all.
- The drug is useful for endurance, strength, and improves mood, which makes it possible to train with greater efficiency.
- Tightens the stomach, allows you to highlight the relief as much as possible.
- Reduces appetite, helps with dieting.
Clenbuterol has virtually no negative effects on the body and can be purchased without a prescription.
Contraindications
The risk of using the drug if there are contraindications is high. The use of even small doses can provoke a heart attack or lead to the development of a pre-infarction condition.
The possibility of using clenbuterol is excluded for the following diseases and conditions:
- myocardial infarction;
- subaortic aortic stenosis;
- heart failure;
- tachyarrhythmia;
- tachycardia;
- endocrine disorders;
- pathologies of the thyroid gland;
- allergic reaction.
For women during breastfeeding or pregnancy, the possibility of prescribing the drug is determined by the doctor. If the potential benefits outweigh the risks, the drug is prescribed with individual dosage selection.
Nutrition
Following a diet when losing weight is a fundamental point in the process of losing weight. The body must receive enough calories to avoid burning muscle, but not enough to store and maintain body fat. Clenbuterol helps in this regard, as it activates the burning of fat in the athlete’s body and prevents the burning of muscle tissue.
A combination of proper nutrition during drying, taking the drug and exhausting strength loads allows you to achieve a sculpted body in the shortest possible time.
Admission results
It is considered a good result to lose 4-8 kilograms of weight in 2 weeks of use. The effectiveness of taking the drug varies greatly depending on the individual characteristics of the body, training regimen, and initial form. However, if your weight loss results are lower, then do not despair, because the drug acts differently on different people.
Once again, it should be noted that the drug is not a “magic pill” that can solve excess weight problems without any effort. To lose weight, clenbuterol must be combined with a proper diet. It doesn’t matter which one, the main thing is that it is effective. In addition, exhausting physical activity will allow the drug to reveal its maximum effect and provide the opportunity to show maximum results. According to reviews of people who have taken clenbuterol, it is possible to lose up to 10 extra pounds after taking one course of the drug.
Where to buy, price, release forms
Clenbuterol from various pharmaceutical companies is present in the assortment of pharmacies. The difficulty of purchasing lies in the fact that this pharmacological drug is included in the category of prescription medications. If you do not have a prescription, you can purchase the drug at any sports pharmacology store.
The cost of clenbuterol depends on the country of manufacture, the form of release and the concentration of the active substance. The average cost of the drug in dollar terms is described in the table below.
Manufacturer | Release form | Price |
Sopharma AD (Bulgaria) | Cardboard packaging of 50 tablets of 0.02 mg. 5 blisters of 10 tablets. | 21$ |
Balkanpharma-Troyan AD | Bottle of 100 tablets of 0.04 mg. | 18$ |
Balkanpharma-Troyan AD | Bottle of 50 tablets of 0.04 mg. | 11$ |
Real reviews of Clenbuterol
- Alexei. Kizilskoye. In the first 10 days there was tremors, restless sleep, fever and stomach upset. Then everything passed. But he dried up normally, although at first it was scary from such symptoms.
- Vitaly. Olenegorsk. Before using the drug, I recommend doing an ECG to check your heart. If there are pathologies, then it is better not to take maple, out of harm’s way. I tried aspirin to reduce the negative effects on the heart. In general, he seems to be alive and well, but it’s better not to take risks. I had only minor deviations in my cardiogram. But I burned the lard, so I don’t really regret it. I really don’t know how this will affect my health in the future.
- Basil. Drakino town. I used Chinese maple for two courses, two weeks each. I did not take it alone, but with potassium orotate. Without much effort and changing my daily routine and diet, I lost 6 kilos. I worked out in the gym, went to training sessions, of course. As a result, the belly shrank noticeably. I was afraid to continue taking it, but I didn’t gain weight after stopping it.
- Marina. Vladivostok. It helped to lose weight, but after the course there was a wild rebound. You can gain more than you lost. Watch your diet!