In the pursuit of the perfect body, appetite control remains a cornerstone. Fighting hunger is the most difficult stage for anyone who has been on a diet. Appetite blockers come to the rescue, but what is hidden behind this name? How did they evolve from dangerous stimulants to ‘smart’ peptides that trick the brain? Let’s look at the mechanisms, generations, and hidden risks of these powerful drugs.
Not all blockers are the same: 3 strategies to fight hunger
Before we talk about specific substances, it is important to understand how you can affect your appetite in general.
Mechanical filling. The simplest and oldest way. This includes eating plenty of fiber, bran, or just plain water. The stomach fills up, its walls stretch, and a signal is sent to the brain: ‘I’m full.’ The effect is short-lived and not always effective.
Central exposure (via the central nervous system). A more powerful, but also riskier path. Substances of this group directly affect neurotransmitters in the brain, which are responsible for the feeling of hunger and satiety. These historically include:
Amphetamines and Ephedrine: Dramatically increase the level of dopamineDopamine is a neurotransmitter and hormone that plays a key role in the brain's reward system, motivation, pleasure, learning, and movement regulation.Main functions: Stimulates feelings of pleasure and satisfaction. Involved in motivation and decision-making processes. Regulates motor activity. Affects memory, attention, and mood. and norepinephrine. The result is euphoria, a surge of energy, and a complete loss of appetite. The price is a huge load on the cardiovascular and nervous systems, irritability, tremor, a high risk of addiction and mental disorders.
Sibutramine: Blocks the reuptake of serotonin and norepinephrine. This creates a persistent feeling of fullness. However, its side effects (tachycardia, increased blood pressure, irritability) led to the drug’s ban in most countries.
Hormonal effects (peptideA peptide is a molecule consisting of a chain of amino acids linked together by peptide bonds. Peptides are shorter chains than proteins and usually contain from 2 to 50 amino acids. When the number of amino acids in a chain exceeds 50, such molecules are called proteins. Peptides can perform various functions in the body, including: Hormones, Neuropeptides, Antibiotics, Antioxidants agonists). The most modern and physiological approach. These drugs do not’ break ‘the system, but’ deceive ‘ it, imitating the effect of natural satiety hormonesHormones are biologically active substances that are produced by specialized cells or glands (such as endocrine glands) and regulate various physiological processes in the body. They act as chemical signals that are transmitted through the bloodstream to organs and tissues to control and coordinate a wide range of functions, including metabolism, growth and development, reproduction, mood, and more. Examples include insulin, testosterone, estrogen, and adrenaline. that are released after eating.
Revolution: Peptide agonists or ‘Satiety Hormones’ in the syringe
This is the gold standard of modern pharmacology for weight control. Their work is based on the simulation of incretins – hormones of the gastrointestinal tract.
How does it work? When you eat, your gut releases several hormones, including GLP-1 (glucagon-like peptide-1) and GIP (glucose-dependent insulinotropic polypeptide). They perform several tasks:
They send a signal to the brain (in the hypothalamus) about saturation.
Slow down the emptying of the stomach, prolonging the feeling of satiety.
They stimulate the production of insulin in response to food intake.
Peptide agonists are synthetic analogues of these hormones that are resistant to rapid degradation and work for a long time.
Signal imbalance. There are also receptors in other parts of the intestine. When the signal comes from only one part of the brain, but not from others, the brain receives conflicting information. This leads to neurological side effects: nausea, irritability, ‘alarm’ in the body.
Digestive problems. Greatly slows down the motility of the gastrointestinal tract. Meat and solid food are digested for a very long time, causing a ‘brick’ feeling in the stomach. Constipation occurs, and stagnation can form in the biliary system.
Generation 2: Dual Agonists (Tirzepatide-Munjaro)
Operating principle: They activate two types of receptors at once — GLP-1 and GIP.
Advantages: A more physiological effect, as the natural work of two hormones is imitated. This results in stronger and more comfortable appetite suppression, fewer side effects, and better weight loss results.
An important caveat: Munjaro is not just a’ stronger ‘ Azempik. The . old medical tactic of ‘start with Azempic, and when it stops working, switch to Munjaro’ is incorrect. It is more logical to immediately use a more balanced drug.
Generation 3: Triple Agonists (Retatrutide)
Operating principle: Three receptors are involved-GLP-1, GIP and glucagon. Glucagon is traditionally considered a blood sugar-boosting hormone, but in this bundle it enhances metabolic effects and thermogenesis.
Advantages: To date, this is the most physiological and promising option. It provides mild but very effective appetite suppression without sudden food withdrawal, while demonstrating better performance in improving insulin sensitivity.
Hidden risks and what they don’t say in advertising
Azempic-face and sarcopenia. The biggest danger. Drugs do not have the magical ability to burn only fat. On a caloric deficit, the body looks for light energy. And if you don’t consume enough protein, that energy becomes amino acidsAmino acids are the fundamental building blocks of proteins and play a key role in biological processes. There are a total of 22 standard amino acids used for protein synthesis in living organisms. from your muscles. The result — loss of muscle mass, sagging skin, flabbiness of the face (‘azempik-face’), loss of strength. Solution: Increase protein intake to 2 g per kg of dry weight, use liquid amino acids and proteinsProteins are high-molecular organic substances consisting of alpha-amino acids linked in a chain by a peptide bond. In living organisms, the amino acid composition of proteins is determined by the genetic code. During synthesis, 20 standard amino acids are used in most cases. Many combinations of them determine the great diversity of properties of protein molecules. Proteins play a key role in the immune response and can perform transport, storage, catalytic, structural, and receptor functions. Proteins are an important part of the nutrition of animals and humans. The main sources of proteins are meat, poultry, fish, milk, nuts, legumes, and grains. that are easier to digest.
Formation of antibodies. Peptides are proteins that are foreign to the body. Over time, the immune system begins to produce antibodies against them. This leads to tolerance: the dose stops working, and it has to be increased. After a few months at the maximum dose, the effectiveness may disappear. .: Use a course scheme (for example, 3 months of admission / 3 months of break) to allow the body to clear itself of antibodies.
Psychological dependence. A person gets used to the fact that you can do nothing and not want to eat. After discontinuation of the drug, if the correct eating habits are not formed, the appetite returns with a vengeance, and all the weight is gained back. .: Use the drug as a ‘crutch’ for the duration of active weight loss, while radically changing your diet and lifestyle.
Lack of vitamins and trace elements. Against the background of reduced appetite and difficult digestion, people begin to eat less not only high-calorie, but also healthy food. There are deficiencies of B vitamins, iron, which leads to hair loss, deterioration of the skin and nails. .: Mandatory intake of vitamin and mineral complexes, especially group B.
Application tactics: How to use wisely
Don’t chase after speed. Rapid weight loss (more than 4-5 kg per month) is always a disaster for the metabolism and appearance. Tune in for a slow but stable result.
Start with minimal doses. For sports purposes and comfortable diet compliance, doses 2-3 times lower than the starting ones indicated in the instructions for the treatment of obesity are often sufficient.
Combine with enzymesEnzymes are proteins that accelerate chemical reactions in the body. They ensure the occurrence of metabolic processes such as food digestion, energy release, cell formation, and many others. and choleretics. To improve digestion, use pancreatic enzymes (such as Creon). Ursosan may be useful for preventing bile congestion.
Analyze combinations. Do not mix drugs that affect the central nervous system (for example, Tesofensin) with antidepressants — this can lead to dangerous serotonin syndrome.
Of course, here’s a separate paragraph about microdosing for athletes:
Separately, it is worth highlighting the strategy of using microdoses of peptides, which is popular among athletes. Unlike the clinical approach, where the goal is maximum appetite suppression, here the task is different: not to kill the feeling of hunger completely, but only to dull it, making compliance with a strict diet psychologically comfortable..
Athletes use doses that may be 2-3 times lower than the official starting dose — for example, 100 mcg of Azempic instead of 250 mcg or 1 mg of Munjaro instead of 2.5 mg. Such microdosing does not cause complete rejection of food, which is critical for maintaining energy and performance during training, but it effectively removes the painful feeling of hunger, obsessive thoughts about food and helps to control ‘breakdowns’. This makes it easier to tolerate a caloric deficit, more accurately fit into the planned weight indicators and at the same time maintain muscle mass due to the ability to consume enough protein.
Peptides and drugs for controlling appetite and weight:
Azempic (Semaglutide) – GLP-1 receptor agonist.
Munjaro (Tirzepatide – is a double agonist of GLP-1 and GIP receptors.
Retatrutide is a triple agonist (GLP-1, GIP, glucagon).
Mazudutide is a Chinese analog of Munjaro (GLP-1 + glucagon).
Liraglutide -GLP-1 agonist
Sibutramine is a central appetite blocker (banned).
Tezofensin is a central appetite blocker (triple serotonin, norepinephrine, and dopamine reuptake inhibitor).
