Clenbuterol - a miracle diet pill

People who dream of losing extra pounds give up their favorite foods, exhaust themselves with exercise, and are even ready to take medications to help them lose weight. One of these drugs is clenbuterol.

Who would have known many years ago that this drug, which has been actively used for a long time to treat bronchial asthma, would also turn out to be a powerful fat-burning agent. Therefore, doctors currently use clenbuterol for weight loss.

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]

Lee P.'s 2020 study 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.

Reviews

Despite the potential health risks, clenbuterol is still growing in popularity. Therefore, it would be useful to read a number of reviews about the use of this substance.

The attitude towards the drug is bad. After I started taking it, I immediately started shaking and vomiting. Then a feeling of anxiety. It only went away in the evening, but I still couldn’t fall asleep.

Svetlana, 26 years old (Moscow)

The product dries very well. But in the first week and a half there was trembling throughout the body, the general temperature rose, I often ran to the toilet (diarrhea), and sometimes I had anxious, bad sleep. But then everything went away. I'm pleased with the result. Alexey, 29 years old (Sochi)

Rich Pian's review of Maple is in this video.

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

How to take it correctly

Depending on the dosage regimen, you can take the tablets from two weeks to 30 days, but always 30 minutes before meals. Then follows a break - at least 2 weeks.

For weight loss

There is a misconception that if you take clenbuterol for weight loss like regular vitamins, weight loss will occur. The drug will have an effect only if certain rules are followed.

To increase muscle mass

The scheme is aimed at damaging muscle fibers that begin to grow rapidly after intense training.

Practical recommendations for building muscle:

1. Load only one or two muscle groups in a traumatic mode.
2. Conduct traumatic training once a week.
3. Recommended dosage: on the day of training (7-8 hours before the start) 10 tablets of 40 mcg.
4. On other days the drug is not used.
5. After training, take increased portions of amino acids.

For local fat burning

Many people have so-called “problem areas”, the fat in which does not want to be burned, despite any tricks. Injections of liquid clenbuterol help burn fat exactly in the problem area. A visible result occurs only after a month and a half of regular multiple injections and only against the backdrop of a fairly strict diet.

The recommended drug is Ventipulmin spray syrup (German company Boehringer-Ingelheim).

General rules for Clen injections:

1. You will need an insulin syringe.
2. Add 0.2 ml of solution into it.
3. Make a subcutaneous injection into the problem area.
4. If the body’s reaction is normal during the day, then you can continue to give injections (5-10 pcs. in the same microdoses).
5. It is recommended to give injections on an empty stomach early in the morning.
6. A good effect can be achieved by alternating injections of Clen and Yohimbine.

To improve your training results

Clen, used in small quantities (20-40 mcg) 1-2 hours before training, can significantly increase strength indicators, as well as increase blood flow to the muscles.

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.

Experts' opinion

The use of Clenbuterol for weight loss is condemned by almost all doctors. Its use for weight loss can be fraught with serious heart problems, since the drug causes an increased release of adrenaline into the blood, which negatively affects the functioning of the entire cardiovascular system.

In some cases, taking the drug can lead to the development of a large heart attack.

Losing weight with Clenbuterol is a surefire way to develop health problems. Even if you manage to get rid of extra pounds with its help, the price for this slimness may be too high.

The only safe way to lose weight is a balanced nutrition system, designed for long-term use and reasonable physical activity of moderate intensity.

Notes[edit | edit code]

1. Parr MK, Koehler K, Clenbuterol marketed as a dietary supplement. Biomed Chromatogr. 2008 Mar;22(3):298-300.
2. 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.
3. 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.
4. 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
5. 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.
6. Lee P. et al. Formoterol, a Highly β 2-Selective Agonist, Induces Gender-Dimorphic Whole Body Leucine Metabolism in Humans //Metabolism. – 2020. – T. 64. – No. 4. – pp. 506-512.
7. https://jap.physiology.org/content/early/2015/07/07/japplphysiol.00319.2015
8. Thieme D., Hemmersbach P. Doping in sports. – Heidelberg, Germany: Springer, 2010. – Pp. 239
9. 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. – 2020. – T. 119. – No. 5. – pp. 475-486.
10. https://www.ncbi.nlm.nih.gov/pubmed/25650070
11. 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
12. 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.
13. "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.
14. "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.
15. "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.
16. https://www.drugbank.ca/drugs/DB00920
17. 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.
18. 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.
19. Burniston, J. G., et al. (2002). Myotoxic effects of clenbuterol in the rat heart and soleus muscle. J Appl Physiol. 93:1824-32.
20. 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.
21. 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.

Answers to common questions

Should I take Clenbuterol if I just started working out?

No. At the beginning of training, progress is already taking place by leaps and bounds; there is no need to take Clen.

Can you really lose weight from Clen? If so, how much?

Judging by numerous user reviews, the use of Clenbuterol will help reduce weight from 5 to 8 kg per course. It is important to follow the correct dosage and adhere to the diet.

Is it possible to lose weight with Clenbuterol if you don’t exercise?

The weight loss will be quite insignificant. The drug forces the body to produce a huge amount of energy that needs to be burned, and the best way to do this is through sports. The more intense the training, the better the result.

After completing the course, will I gain the same kilograms?

No. After the Klen course, fat burning slows down a little, you begin to lose weight at the same speed at which you lost weight before the course. But it all depends on your diet and genetic makeup.