Do you want to lose weight? Eat a pill!

Modern medicines for weight loss

Polina Loseva, XX2 century

These are lorcaserin (Belviq) – weight loss pills developed by the American company Arena Pharmaceuticals. In 2012, they were approved by the FDA and recommended for adults with a BMI above 30 (or above 27 if they have type 2 diabetes, hypertension or high cholesterol). On the day when Belviq was approved by the FDA, the developer's shares soared by almost 30%: it was assumed that the need for such a drug was very high and it would be sold for at least $ 1 billion a year. However, sales were disappointing. In 2015, Arena Pharmaceuticals (Belviq is currently its only drug on the market) was forced to lay off 80 employees, in July 2016 – another 100 (more than 73%). A year ago, the company's management announced that it was preparing to sell the rights to Belviq to a Japanese partner.

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Humanity has learned several lessons from the long years of struggle with excess adipose tissue. Firstly, sometimes there is too much of a good person, and then he needs to be treated. Secondly, it is not always enough to run in the morning and give up sweets. Thirdly, not all methods of treatment are equally useful. We have compiled for you a list of officially approved drugs for the treatment of obesity and tell you how and to whom they can help.

We draw your attention to the fact that medicines officially approved by the regulator in one state may not be among those approved for sale in another, or may be directly prohibited. Look carefully at the list of approved in which country a particular drug is listed, and do not try to purchase something that may cause problems with the law. Even if there are positive scientific research data about these substances.

To begin with, let's define what excess weight is. From a medical point of view, weight can be superfluous only for the body and its work, but not at all for the self-esteem of its owner. Therefore, when we talk about obesity, we are not talking about the fact that someone's dress does not fit well. We are talking about the fact that adipose tissue "sits" on someone's organs and prevents them from functioning normally. And this, you will agree, is a much more serious problem. The World Health Organization suggests to believe not the mirror, but the body mass index (BMI). We take the body weight (in kilograms) and divide by the square of height (in meters). You can start to get nervous if the index is greater than 25 – this is recognized as overweight. And only after 30 does real obesity begin.

Let's dig deep and see where the excess weight comes from. To do this, let's run along the path that food takes on the way to fat deposits.

1. Absorption. We're eating.
2. Digestion. In the stomach and intestines, enzymes act on food, splitting it into small parts that can be easily absorbed.
3. Suction. Intestinal cells absorb individual molecules and transport them into the blood.
4. Feeding of cells. The molecules circulate through the blood, from where they are gradually disassembled by the cells of the body.
5. Storage. Liver and adipose tissue cells take the remnants of fats and sugars from the blood to put aside for a rainy day. At the same time, sugar is also converted into fats in adipose tissue.
6. Energy consumption. If the blood sugar level drops, you have to use up supplies. First of all, from the liver, since sugars are stored there, and only then from adipose tissue.

Where can this system fail? The most obvious thing is if the food intake turns out to be more than the energy consumption. In other words, a person eats too much or moves too little. In addition, the mechanisms by which the bodies regulate each other's work may break down. For example, the connection between adipose tissue and the pancreas often collapses. The latter secretes insulin, which stimulates the capture of sugar from the blood. If the body does not produce enough insulin (type 1 diabetes mellitus), people do not get fatter - their adipose tissue does not receive a signal to store food. But with type 2 diabetes, the opposite is true: if a person has too many reserves (obesity), then his tissues may lose sensitivity to insulin, and sugar will accumulate in the blood.

But this is just the tip of the iceberg. Do not forget that all the above-mentioned stages are connected to each other by dozens of signaling molecules. The stomach signals to the brain whether there is enough food. Adipose tissue secretes substances that reduce appetite. And the brain, in turn, gives the command to eat more or digest more intensively. And we still do not take into account the kilograms of bacteria in the intestine, which also have an opinion about our digestion and also actively express it, that is, they secrete signaling substances. Therefore, when we are dealing with obesity, it is sometimes very difficult to say exactly what went wrong. Anything could break.

Since there are many causes of obesity, then it can be treated in different ways. There are simple methods: eat less or spend more energy. This includes all kinds of diets and physical activity. However, it often happens that they do not help. This means that the problem is not in the balance of stocks and expenses, but in the mechanisms of regulation. There are many questionable methods used by people with eating disorders: laxatives (so that food is not absorbed), diuretics (when dehydrated, fats are also often broken down), antidepressants (so that you don't want to eat), etc. These methods, as a rule, are harmful to health, but they still do not solve the problem.

But there are officially approved medications for weight loss, and they work a little differently. Their list does not match in many countries, and we will start with the USA, where there are significantly more of them than in Of Russia. There are five groups of drugs.

1. Digestive blockers

These include orlistat (Xenical, Alli) – the only weight loss drug that can be purchased in the USA without a doctor's prescription. It blocks lipase, an enzyme that breaks down fats in the intestine. This allows you to reduce their absorption by 30% without affecting the rest of the metabolism. And since fat does not enter the bloodstream, then we cannot store it. According to clinical studies, over 4 years, patients taking orlistat lost, on average, 5.8 kg. In the control group, who took a placebo, – 3 kg. Here we note that usually weight loss medications are recommended to be combined with diet and exercise. Therefore, we can say that part of the weight loss of participants in such trials is almost always provided not by a drug, but by a change in lifestyle. As a side effect of orlistat, steatorrhea (fatty stools) is possible, which can be avoided by eating less fatty foods. In addition, in some cases, the drug had a negative effect on the functioning of the liver, kidneys and pancreas. However, these cases were rare, besides, do not forget that obesity itself is often accompanied by a violation of the internal organs. The beneficial effects include the fact that orlistat reduces the total level of cholesterol and low-density lipoproteins (LDL).

2. Stimulators of insulin production

In America, they use liraglutide (Saxenda, Victoza). It is an analog of glucagon-like peptide 1 (GLP-1), which acts on the pancreas and enhances insulin production. And insulin, in turn, reduces appetite. This drug is designed for people suffering from type 2 diabetes (low sensitivity to insulin), and, unlike the others, is intended for injection. After 56 weeks of daily injections, people dropped up to 8.4 kg. If it is used by people who are not diabetic, hypoglycemia is possible – a decrease in blood sugar levels – which in extreme cases can lead to coma. There may be other side effects from the digestive (diarrhea, constipation, nausea) and nervous (headache, dizziness) systems.

3. Anorexics

Signals between neurons in the brain are transmitted through small molecules – neurotransmitters. Depending on which neurotransmitters are released, different neurons are activated. If the signal goes through sympathetic nerve fibers, a stress response is triggered. The body focuses all its forces on survival, while the heart and lungs are actively working, and digestion, for example, is inhibited. If the signal goes along the parasympathetic fibers, the body relaxes. The heart and lungs work calmly, but more energy is spent on digestion and excretion. Anorexics mimic the work of neurotransmitters and trigger a stress response. This reduces the activity of the hunger center and increases the splitting of energy reserves.

To date , several two types of anorexics are used: 1) lorcaserin (Belvik) – reduces appetite by activating the serotonin receptor, known as the 5-HT2C – i 2 receptor) diethylpropion (Tenuate), phentermine (Adipex), fendimetrazine (Bontril), benzphetamine (Regimenex) – relatives of amphetamines.

Lorcaserin acts mildest of all. He was suspected of provoking cancer and depression, but the fears were not confirmed. According to clinical studies, lorcaserin works better in the first months, and then its effect decreases. On average, over the course of a year on lorcaserin, people suffering from obesity and overweight on the background of diabetes lost about 4.5–5% of their weight (versus 1.5% on placebo).

Unlike lorcaserin, the rest of the anorexics are FDA (FDA) it does not recommend using for a long time, as they are addictive (no wonder they look like amphetamines). Due to addictive behavior and possible serious side effects in case of overdose, anorexics are not sold without a prescription, and their turnover in the United States is under strict state control.

However, not so long ago, a milder option appeared – phentermine + topiramate (Ximia). It is already recommended for long-term use. The exact mechanisms of action of topiramate are still unknown. It has been used before as an anticonvulsant in the treatment of epilepsy, it increases the activity of the inhibitory neurotransmitter GABA (gamma-aminobutyric acid). Probably, this allows you to avoid getting used to phentermine without interfering with its action. For 56 weeks with the help of Ximia, patients lost up to 10 kg of weight. However, for all its softness, Xymia also has unpleasant side effects. It reduces the amount of the female sex hormone ethinyl estradiol in the blood, which worsens the effect of oral contraceptives and increases the likelihood of bleeding. In addition, the frequency of anxiety disorders and depression increases 4-7 times among patients taking Ximia. Therefore, it is not recommended to take it for people prone to depression.

4. Antidepressants

This group includes the drug naltrexone + bupropion (Contrave). Naltrexone blocks opioid receptors – the same ones that are responsible for the invigorating effect of endorphins ("hormones of happiness") and many narcotic substances (morphine, heroin, etc.). Naltrexone is used to treat alcoholism and drug addiction, while patients stop having fun and addiction is removed. Bupropion works differently. When one neuron transmits a signal to another, it releases neurotransmitters, but after a while captures them back. Bupropion interferes with the reuptake of dopamine (a stimulating neurotransmitter) and norepinephrine, therefore it acts as an antidepressant, and the patient is less hungry. With the help of Contrave, the study participants dropped about 5-6% of body weight in 56 weeks (in the control group on placebo – 1.3%). Although there are side effects – nausea, dizziness, dry mouth, and so on.

Now back to Russia. Here the range of available medicines is much smaller. Most of the drugs used in the USA are Belvik, Adipex, Ximia, Contrave, Tenuate – in They are not listed in the State Register of Medicines. And, for example, phentermine (Adipex, Xymia) and diethylpropion (Tenuate) are considered narcotic substances. Let's see what's left on the list.

0. Homeopathic medicines (Dietress, Cefamadar). But we will not consider them, because homeopathy is unscientific and, in principle, cannot work.

1. Orlistat (Xenical, Orsoten, Alli). Allowed in Russia is the same as in the USA. It is suitable in cases when you need to lose a little weight, and when there are no concomitant serious diseases (diabetes, depression, etc.)

2. Sibutramine (Reduxin, Slimia, Lindax, etc.). This is another blocker of the reuptake of neurotransmitters – dopamine, norepinephrine and serotonin. Acts as an antidepressant. However, since 2010, due to the high risk of complications from the cardiovascular system, it has been banned from use in many countries (including Europe; and in In the USA, the FDA required the manufacturer to indicate in the instructions that sibutramine should not be used in patients who have ever had cardiovascular diseases). In Russia, however, it is still on sale, although it is included in the list of potent drugs. In drugs for weight loss, it is sometimes combined with metformin. Metformin was developed as a cure for type 2 diabetes. It enhances the absorption of glucose by tissues and reduces its absorption in the intestine. In the USA, it is not recommended to use it if the patient does not have diabetes. However, some studies have found that people who do not suffer from diabetes lose weight from metformin better than diabetics. The list of side effects of sibutramine is not limited to the cardiovascular system, there is insomnia, rhinitis, and headache. And in complex preparations, the risks associated with metformin are added to them – disorders of the gastrointestinal tract and possible acidosis (acidification of the blood).

3. Antidiabetic drugs. This is metformin, exenatide (Baeta) – analog of liraglutide, and acarbose (Glucobai) – inhibits the digestion of carbohydrates in the intestine. These medications can help people with diabetes (and sometimes, as in the case of metformin, without it), but it is not recommended to use them without special indications or, in any case, without consulting a doctor.

4. Antidepressants (in addition to sibutramine). They are prescribed for obesity associated with disorders of the nervous system, and are also not recommended without indications. Among them are fluoxetine (Prozac), venlafaxine (Velaxine, etc.) and others.

Let's summarize the results. Obesity is a serious disease. It can be pre-diagnosed by body mass index. You can fight it in simple ways by controlling your lifestyle and limiting yourself to food. But if this does not help, you need to start treatment.

Each of the drugs described above has its own characteristics and is not suitable for everyone. Moreover, none of them is a panacea and does not allow you to lose any amount of weight. Some are addictive, side effects, others stop working after the first weeks. Finally, it should be borne in mind that clinical studies have been conducted on people with a body mass index greater than 25-30 (and often diabetic patients). And if their medications helped them lose 5 or 10 kilograms, this does not mean that a healthy person with a normal index who decided to lose a little weight, they will help to the same extent. In any case, before making any changes to your metabolism, it is necessary to consult a doctor.

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