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Ketotifen: use in bodybuilding and fitness

In view of the scarce information about Ketotifen, its mode of action, its effect and what is its application in fitness and bodybuilding, we will try to bring some clarity! The information was gathered from various sources, as well as from our own experience with Ketotifen!

What is Ketotifen

Ketotifen belongs to a group of anti-allergic medicines called antihistamines! It is used to treat bronchial asthma and allergies (blocks histamine, which is released in allergies). In addition, it can be prescribed to treat colitis.

When used to treat asthma, weight gain and increased appetite are among the most common side effects. Ketotifen protects cells in the stomach, small intestine and the rest of the gut from a number of toxins. A number of practical examples show that it can be useful for skin problems such as acne. The product also reduces swelling (swelling and puffiness caused by water retention) around wounds.

Why Ketotifen is used by bodybuilders and fitness trainers

Like other drugs used by athletes because of their secondary properties, Ketotifen is well used by fitness trainers! It is gaining popularity for its ability to increase the sensitivity of beta-2-adrenergic receptors, which are suppressed by drugs such as Clenbuterol and Ephedrine.

Those who are aware of Clenbuterol and Ephedrine know that they quickly saturate the receptors and stop working. This is where Ketotifen comes to the rescue. It increases the limit of adaptation to these preparations and allows their use for a longer period in a cycle for relief and reduction of subcutaneous fat.

Another important advantage of taking Ketotifen is that it has the ability to lower the levels of TNF-alpha (Tumor Necrosis Factor-alpha), which is a catabolic hormone. The effect of TNF-alpha is reduced by both testosterone and IGF-1 levels. TNF-alpha also helps increase insulin resistance, which we are certainly not looking for.

This property of Ketotifen, which inhibits TNF-alpha, may make it a valuable tool in post-steroid therapy (PCT).

Ketotifen and Clenbuterol 

Clenbuterol is a beta 2 receptor agonist. It has a mild anabolic effect and is a great thermogenic used to fight fat, and at higher doses has anti-catabolic action. Unfortunately, Clenbuterol quickly saturates the receptors and to be effective it is taken cyclically for 2 weeks with a break of 2 weeks.

Ketotifen regulates beta-receptors and clears them, it does not allow them to be suppressed even during a heavy cycle with Clenbuterol. This means that you can continue to take Maple indefinitely without interruption. Drinking 2-3 mg can regulate even severely clogged receptors within a week.

This means that you do not need to take very high doses of Maple to get the same results. Taking about 30-40% less Maple will be just as effective.

Ketotifen: Intake and Dosage

No studies have been conducted to find the most effective dose, but German researchers use 3-4 mg daily. Our experience has shown that 2 mg every day is sufficient. However, much higher doses have been shown to be completely safe, with no adverse effects other than increased drowsiness and appetite. Higher doses will increase the appetite for bad foods. It is recommended to take it before bedtime, but it can be divided into 2 equal days.

Side effects and toxicity

Ketotifen is virtually non-toxic (although not recommended in patients with epilepsy). Its main side effects are temporary drowsiness, dry mouth, (and other mucuos membranes), stimulating appetite and weight gain.


Hypersensitivity, pregnancy, lactation, children under 3 years (tablets, eye drops) or 6 months (syrup).

Do not take by people with:

Epilepsy, liver failure. During pregnancy and lactation.

The materials on the site are for informational and educational purposes, do not constitute medical advice, incentives or recommendations. The information provided describes well enough the negative effects of doping so that users can make their own decisions in the interests of their health and safety. Consumers should consult a doctor before resorting to any preparations.

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Ways to quickly reduce body fat


In this article we will introduce you to 10 of the most common and most effective means of achieving low body fat and reducing subcutaneous fat. These are tools used by both professional bodybuilders and millions of fitness trainers around the world to quickly reduce body fat, relief – the so-called cleansing, and even weight loss.

Many of you know that bodybuilders have a basic period for growing and gaining muscle mass, followed by a phase / period for relief. You can often find photos of professional bodybuilders during their main period (off season), which clearly shows that they have not avoided fatty foods. But within a few months, even weeks, they pose again in good condition, embossed and free of fat. Of course, diet, exercise and experience play a huge role in their ability to recover from acute diets to reduce body fat, but as many other athletes may find, discipline and will alone are not enough for these dramatic changes in fitness. and bodybuilding trainers.

Although these ways to reduce subcutaneous fat are effective, many of them are an element of risk and should be used under medical supervision. The question follows: why are they still used? The answer is simple: it is the desire to be the best, regardless of cost, risk or ethics.

Stimulants to reduce body fat

Stimulants are medications or supplements that accelerate fat loss by sending a signal to the body. They work by stimulating and releasing a neurotransmitter called norepinephrine (NE) or norepinephrine, prolonging its signal or directly replacing it. There are two classic examples of stimulants that burn subcutaneous fat.

1. Clenbuterol

The use of Clenbuterol will help to quickly reduce body fat and subcutaneous layers. It is a direct beta-agonist, which means that it stimulates exactly the same norepinephrine receptors that help burn and reduce body fat. The main advantage of Clenbuterol is that it is more specific, affecting only beta-2 receptors. This is important because there are two classes of NE receptors in the cell membrane of fat cells – alpha and beta. Alpha-2 receptors cause beta receptors to respond to fat loss. So, Clenbuterol actually creates a stronger signal to release fat from adrenaline, which stimulates both alpha and beta receptors.

Clenbuterol is used to treat asthma! An anabolic effect has been established in clinical trials with animals. But to achieve this effect, humans need too high doses, which will be toxic or possibly deadly, so in practice, Clenbuterol has no anabolic effect. The drug is usually dosed in the range of 10-40 micrograms (not milligrams) per day, although tolerance to it is rapidly developing. The effects of Clenbuterol are short-lived, as beta-receptors decrease within a few weeks, so many users use Clenbuterol for only a short period of time or take and stop it every few days. With long-term use, Ketotifen is used, which increases the sensitivity of beta-2 receptors and allows Clenbuterol to work for a long time.

2. Ephedrine / Caffeine stacks

The use of Ephedrine is an effective way to reduce body fat. These supplements are usually the best-selling in health food stores simply because they work and are effective in reducing body fat. Numerous studies have been published showing that the combination of ephedrine and caffeine effectively accelerates weight loss while maintaining muscle mass. There are many controversies regarding the safety of ephedrine and caffeine supplements due to a number of adverse events reported among consumers. The use of this combination has been associated with a number of hospitalizations and several deaths. However, in controlled-dose clinical trials, subjects did not experience serious adverse reactions and the combination was declared safe.

Bodybuilders use ephedrine / caffeine supplements not only for fat loss, but also because it is mulatto and can help maintain energy and motivation during training.

Unlike clenbuterol, ephedrine does not act directly on beta receptors, but causes the release of norepinephrine, which stimulates both alpha and beta receptors, so the short-term effect of ephedrine is less dramatic.

Hormones to reduce body fat

Hormones in the body are involved in energy balance and changes in the levels of these hormones can directly affect metabolism and fat loss. In addition, other effects of these hormones can alter the rate of fat accumulation. The use of hormones to lose and reduce body fat is especially dangerous, as an excess of any hormone can lead to serious consequences.

3. Anabolic steroids

Testosterone and anabolic steroids are known for their effect on skeletal muscle, they lead to muscle growth and strength gain. By increasing the relative amount of muscle, steroids reduce the percentage of body fat. Also, a number of studies have found that anabolic steroids, such as Anavar (Oxandrolone), Winstrol (Stanozolol), etc., can also have a direct effect on reducing body fat.

4. Growth hormone

Growth hormone (GH) affects many functions in the human body. Recently, it has gained popularity as a powerful agent for increasing muscle mass, while reducing subcutaneous fat. Growth hormone moves nutrients from fat stores to functioning muscles and organs. GH affects growth through another hormone called IGF-1, but its effect on reducing subcutaneous fat is more direct and powerful. Elevated levels of growth hormone interfere with insulin – the main driving force for fat storage, and accelerates the release of fat from fat cells. Growth hormone (GH) is used by bodybuilders and obese people in doses of 4-6 IU / day. GH should not be used without a prescription from a specialist.

5. Aromatase inhibitors

Aromatase inhibitors are drugs that prevent the conversion of androgens to estrogen. Bodybuilders add aromatase inhibitors to their arsenal in order to prevent and reduce estrogenic side effects associated with anabolic steroids. Testosterone and other steroids can be converted to estrogen as a result of aromatase, and high levels of estrogen will lead to water retention, fat accumulation or gynecomastia. Fat cells have receptors that bind to sex hormones, and the presence of estrogen helps increase their numbers, which predisposes them to fat accumulation. Aroma inhibitors reduce the amount of estrogen, which allows bodybuilders to provide more security and a better appearance.

The strongest aromatase inhibitor is Arimidex – Do not take this preparation without the appointment of a specialist.

6. Thyroid hormone (triiodothyronine) – T3

Triiodothyronine, known as T3 or Cytomel, is the strongest agent for reducing subcutaneous fat and weight loss. Triiodthyronin, known as T3 or Cytomel, is a hormone of the thyroid gland. It is a major regulator of the body’s metabolic rate. T3 is an extremely powerful hormone and acts on fat loss by making the body more sensitive to norepinephrine.

High levels of T3 lead to a highly catabolic state, and although weight loss will be significant, a significant portion of weight loss will come from muscle mass. This leads bodybuilders to use it against the background of a good steroid cycle. In addition, excess T3 can make an individual very sensitive to other stimulants, or even the natural release of NEs, leading to dangerous heart rhythms, insomnia and irritability. Consumers should be very careful when combining triiodothyronine with certain stimulants. Using it without anabolic steroids is likely to lead to a solid loss of muscle mass.

Unfortunately, T3 is a very specific thyroid hormone, its unauthorized intake is dangerous and can lead to irreversible consequences.


7. Cardio workouts

A good way to reduce body fat is cardio training. Having listed all the stimulants, anabolic steroids and hormones that are most effective at reducing subcutaneous fat, it would be a step backwards, not to mention cardio training.

Cardio is a curse for most bodybuilders! There are many opinions about when and how to do cardio: low or high intensity, daily or infrequent, etc. The effect of cardio training, for fat loss, is to increase the activity associated with burning calories.

It is believed that the body’s minimum need for calories if you do nothing – (resting metabolic rate (RMR)) rises with high intensity workouts although this remains to be proven. Given that greater muscle mass increases RMR, as happens with the use of stimulants such as ephedrine, caffeine and green tea, the argument is insignificant. Every fitness trainer should find the right frequency for cardio workouts, which will be maintained regularly, preferably every other day. The rate of fat burning is higher when exercise is done in the morning, before meals, with plenty of water and caffeine. However, if this is not possible, other forms continue to offer benefits. Also, you need to be careful during a calorie deficit (low carb diet) to avoid injury or muscle catabolism. During a cardio workout, it is good to know how fast your heart rate is, do not exceed 140 beats per minute, because it is believed that above this limit, the body begins to break down muscle tissue.

The diet

8. Ketone diet (Ketogenic diet)

Ketone or ketogenic diet to reduce body fat and relief. This diet is promoted by Dr. Atkins. It is a diet low in carbohydrates and is very effective in reducing body fat and maintaining muscle mass. The ketogenic diet requires a lot of willpower, as it severely limits the amount of carbohydrate foods. This restriction will initially lead to irritability, loss of concentration and strength as one adapts to it, but eventually, nervous behavior and normal training will return to normal.

The purpose of the ketone diet is to reduce the amount of insulin that the body releases when carbohydrates are taken. Insulin is a major anabolic hormone, but unfortunately, it is the main engine of calories in fat cells and prevents the breakdown and excretion of stored fat, which leads to the accumulation of extra pounds in the form of fat. When carbohydrates are limited, there is a large initial weight loss, which is the water associated with glycogen in the liver and muscles. That can be as much as ten pounds in the first week. However, fat loss with a ketone diet is slower and safer.

Without insulin, which blocks the release of fat, fat cells are much more sensitive and react more aggressively to stimulants and other hormones. By properly monitoring calories and the amount of fat in the diet, a good ketogenic diet can lead to dramatic loss of body fat. Muscles can be adversely affected by a ketogenic diet, as insulin also transports nutrients (sugar, amino acids, creatine) into muscle cells and prevents the breakdown of muscle protein. But, in practice, with a ketone diet you can increase lean muscle mass. This type of diet can be followed for a long time, and many of Dr. Atkins’ advocates have adopted a ketogenic diet as a permanent lifestyle.

Other ways to reduce body fat

There are a number of other preparations and ways that promise fat loss and are often used by active and inactive athletes.

9. Yohimbine

Yohimbine is a supplement that is able to block alpha-2 receptors that are responsible for storing and accumulating fat. Its use allows other stimulants to be much more effective and creates a prerequisite for faster burning of subcutaneous fat. In addition, Yohimbine strengthens blood circulation in the waist, hips and thighs, which allows the accumulated fat in these problem areas to be reduced faster.

10. Captopril

Captopril is a medicine used to treat high blood pressure (hypertension). If you already suffer from hypotension, you will have trouble with it! Captopril has the ability to lower alpha-2 receptors, but has no direct effect on them. This is done indirectly by preventing the formation of angiotensin II, as a result of which alpha-2 receptors are reduced. Captopril has weak diuretic properties, and in the long run a side effect of Captopril is weight loss, which is well documented by medical research. Of course, this weight loss may be due to muscle mass, but in reality it is not, the drug has a mild anabolic effect on muscles, which protects them from breakdown. Do not take this preparation without the appointment of a specialist.


Liposuction is a cosmetic operation in which unnecessary fat deposits can be removed and certain areas of the body can be sculpted. Liposuction can be used to shape the body, unfortunately it can not be used for weight loss.

Bodybuilders, but not only them, use extreme measures to achieve extreme weight loss and rapid fat burning. Millions of people apply these methods in an effort to lose weight and look good! But as you can see, most of these ways of burning fat carry risks and many of them would notshould be used without a prescription. None of the methods listed above should be used without greater literacy for the risks it carries.

Body fat in men and women.

original text: Dan Gwartney

The materials on the site are for informational and educational purposes, do not constitute medical advice, incentives or recommendations. The information provided describes well enough the negative effects of doping so that users can make their own decisions in the interests of their health and safety. Consumers should consult a doctor before resorting to any preparations.