- Drugs to treat obesity
- Overview of popular medications for treating obesity
- Digestive blockers – Orlistat (Xenical, Xenalten, Orsothen)
- Hormonal stimulants of insulin production: liraglutide (Victoza, Saxenda)
- Metformin (Glyformin, Glucofage, Siofor, Formitin)
- Baeta, Baeta-Long (exenatide)
- Sibutramine (Meridia, Reduxin, Slimia, Goldline Plus)
- About Prospects and Foreign Drugs
- Rimonabat (Acomplia, Zimulti)
- Lorcaserin (Belvik)
- Xymia (phentermine + topiramate)
*Review of the best according to the editors. About the selection criteria. This material is subjective, is not an advertisement and does not serve as a guide to purchase. It is necessary to consult with a specialist before purchasing.
Which is easier: to put on weight or to lose weight? Of course, it is much harder, and sometimes impossible, to get better. It is easier to increase one’s weight after a serious illness, such as pneumonia or tuberculosis, if one had a higher weight before. The body has a genetic memory. But here if a person was originally thin, and all of his relatives, too, then to gain weight is sometimes very difficult. The organism, according to the second law of thermodynamics, as an open system, tries to go to the state with the least energy. So he tries to get rid of excess energy, without converting it into mass and without expending his own energy. This can be done by an increase in metabolism, a slight increase in body temperature, activation of thyroid hormones, and finally, by reducing absorption in the intestines.
Therefore, compared to those who want to gain weight, those who want to lose weight and cure obesity, in general, in terms of physics, do not need to do anything. Losing weight is much easier than gaining weight. You just need to follow one very important, but simple principle.The daily energy intake should be a little less than its expenditure.
But, alas, obesity is a social scourge of mankind. Obesity is not just a disease or condition, but a global epidemic. By 2010, for example, about 1.5 billion adults were overweight. More than 200 million men and 300 million women have had clinical forms of obesity, and there is a consistent and alarming trend for an increase in the frequency of this pathological condition in civilized population.
It is necessary to treat obesity, but, as in many cases of metabolic disorders, the use of drugs and pills, should be last, after all non-drug methods have been tried. Naturally, one must start with diet and lifestyle modifications, then include an increase in physical activity, and only then turn to drugs and medications against obesity.
Actually, the natural, physiological way and converted excess body weight into energy throughout the history of human civilization. However, the development of medical science was constantly offering improved ways to combat obesity, because people tend not to work on themselves, not to test their willpower, and just apply one or another drug, taking the path of “least resistance.That is why doctors went along with it, gradually began to use laxatives, and then the use of thyroid hormones.
This method of treatment was very crude and consisted in increasing the basic metabolism, but there were significant side effects associated with the emergence of hyperthyroidism clinic. In the thirties there were amphetamines, which are banned in our country, but perfectly suppress appetite and increase physical activity, causing euphoria. However, the use of amphetamines is fraught with subsequent serious disorders, which, above all, manifest themselves in a complete collapse of strength, the development of depression and the formation of addiction.
Research into the effect of various drugs on lipid metabolism in order to find a safe and effective weight-loss drug is ongoing. There are already medicines that can increase metabolism, prevent the absorption of fat, stimulate insulin production, and improve mood. But so far all these drugs allow us to reduce our food intake, or to make the energy intake less advantageous. Still, the cornerstone remains the creation of a substance that would control weight by reducing appetite, and would not cause side effects related to metabolic shifts.
Appetite is not just a feeling or desire.Satisfying hunger is a deep and ancient instinct that, along with the satisfaction of thirst, ranks first among all drives and interests except that of self-preservation. In order to be satiated and survive, a person must take a number of certain actions. So the nervous mechanism underlying appetite and its satisfaction is extremely complex. In clinical practice, drugs have been tested and used that reduced, and even suppressed appetite completely, but all of them had high risks, up to cases of death, and could not be used to treat obesity.
The situation is further aggravated by the fact that the hard-accumulated fat reserves in the human body are protected from irrational use and deposited for reserves. Hormones, enzymes, behavioral modification are on the lookout for our fat reserves.
This is why there is still no single, complete remedy that is guaranteed to help you lose weight without changing your lifestyle or diet, and has no contraindications for use. Perhaps closest to this is RDT, or therapeutic fasting. However, there are a number of medications that can be used in short courses, strictly on the doctor’s advice, along with exercise, diet, increased physical activity, and other known methods of weight loss. Very few drugs can be safely used long-term, for a year or longer. Consider some groups of drugs that are used in our country, as well as abroad to reduce body weight.
Drugs to treat obesity
There are very few such drugs, and almost each of them is the only representative of its group. Among medications to treat obesity, or more accurately, to reduce body weight a little, we do not encounter a great abundance of medications. If we turn to pharmacology, there are whole series and generations of drugs, for example, such as non-steroidal anti-inflammatory drugs (NSAIDs). These are meloxicam and nimesulide, ketoprofen and celecoxib, paracetamol and diclofenac. They are all effective, yet completely different.
The same variety can be found among hormonal drugs, among cough medicines, among anti-ulcer drugs and headache medicines. But for the treatment of obesity, unfortunately, we have not yet found the desired abundance. In the case of a drug used in Russia, commercial names are given for it, as well as a price range that is relevant for fall 2019.
All drugs are arranged according to their mechanism of action. There is no ranking in the suggested list, no ranking by possible efficacy. The order is arbitrary.
Before describing the drugs, we should remind you that self-medication is dangerous and trying to use these drugs without a doctor’s prescription can lead to serious illness. In addition, even a doctor, and a specialist in the field of dietetics and the treatment of excess body weight, will certainly try non-drug methods before using medications. And only then, in the absence of results, some of the drugs below may be prescribed.
As with many medications, they have a number of side effects, such as agitation, insomnia, increased blood pressure, a tendency to chronic diarrhea.
Overview of popular medications for treating obesity
|Drugs for the treatment of obesity||1||Digestive blockers – Orlistat (Xenical, Xenalten, Orsothen)||759€|
|2||Hormonal stimulators of insulin production: liraglutide (Victoza, Saxenda)||9 200€|
|3||Metformin (Glyformin, Glucophage, Siofor, Formitin)||168€|
|4||Baeta, Baeta-Long (exenatide)||3 450€|
|Antidepressants||1||Sibutramine (Meridia, Reduxin, Slimia, Goldline Plus)||2 035€|
|About Prospects and Foreign Drugs||1||Rimonabat (Acomplia, Zimulti)||–|
|2||Lorcaserin (Belvic)||18 240€|
Digestive blockers – Orlistat (Xenical, Xenalten, Orsothen)
A remedy that impairs the absorption of fat in the intestine is probably the most harmless of those drugs that are used to treat obesity. For example, in the U.S., you can buy this medicine without a doctor’s prescription, and all other obesity medications would be prescription. What is this medicine? It is Xenical, or Orlistat.
It is known that normally the pancreas produces a special enzyme that breaks down fats (pancreatic lipase), and the bile, which is produced by the liver, helps these fats to emulsify and translate into a convenient phase for the action of lipase. So if you somehow inactivate this lipase, then the fats from the food will not be broken down in the intestine, but will be excreted unchanged in the feces.
If Xenical is used in therapeutic, recommended dosages, then absorption of fat in the intestine is reduced by one-third, and metabolism is not changed in this case. As a result of the reduced intake of fats into the bloodstream, the body’s ability to store them as a reserve in adipose tissue also decreases. There are many clinical studies that have shown that the use of this drug without changing diet and without exercise allowed patients to lose an average of about 6 kg of weight over 4 years. Naturally, this indicates that the drug works, but if a person will watch his diet and increase his physical activity, then the same amount of pounds can be lost not in 4 years, but in 4 months, me and even faster, without affecting health.
Xenical, or Orlistat, has a minor but unpleasant side effect. If fat is not absorbed, it must be excreted with the feces. And if the feces will contain an excessive amount of fat, then the fat, accumulating on the walls of the colon, will cause its mechanical irritation, and the fatty stool will literally slide out on the surface of the intestine. This phenomenon of steatorrhea is well known to patients with chronic pancreatitis. Because of enzyme deficiencies, their stools become very greasy and they constantly have to use a toilet brush, because the fat is not easily flushed out with water.
But from the use of Xenical there is an additional positive effect, not related to the reduction of body weight. Reducing the amount of absorbed fat leads to a lowering of the total level of cholesterol, and reduces the risk of atherosclerosis. But again, it is much more effective to reduce the risk of atherosclerosis and reduce the concentration of cholesterol in the blood plasma with a diet and increased physical activity.
In the Russian market, Xenical is represented by the Italian company Roche, and a pack of 21 tablets will cost an average of 950 rubles. Orsotene by KRKA will cost a little less, about 800 rubles. It is necessary to apply this remedy in one capsule along with a meal. Therefore, if we assume that a person eats three meals a day, then one package is enough for a week and a monthly course will cost 4000 rubles.
Hormonal stimulants of insulin production: liraglutide (Victoza, Saxenda)
Strictly speaking, among the official indications of liraglutide there is no recommendation to use it for weight loss. It is prescribed to patients with type 2 diabetes to normalize blood sugar levels when other drugs are ineffective. The second indication is to reduce the risk of heart attack and stroke in patients with the same type 2 diabetes in the background of some cardiac pathology, as an adjunctive treatment. But in the U.S., liraglutide is still used to reduce body weight, although also in patients with type 2 diabetes. Unlike other drugs, it is not pills or capsules, or even drops, but a drug for subcutaneous injections.
Liraglutide is similar to human glucagon-like peptide. It took the help of genetic engineering and biotechnology to create it. The corresponding section of human DNA, which encodes the synthesis of this peptide, was embedded in the hereditary material, common yeast, then these yeast multiplied and began to produce this human substance under factory conditions. The result is liraglutide, which, after purification, is 97% similar to human peptide. As a result of its binding to receptors, insulin secretion is stimulated and the barrier of insulin resistance is overcome. This medication must be administered subcutaneously. Self-injected into the shoulder, abdomen, or thigh once a day at home, regardless of food intake. But it is still better to put it at the same time of day.
How much weight loss is possible? According to existing studies, it took more than a year, as much as 14 months, or a gap of 56 weeks, to reliably establish an average weight reduction in diabetic patients of a maximum of 8.5 kg. On the one hand, this figure may indeed amaze and interest. But on the other hand, you should know beforehand about the cost of this drug. For example, Victoza by Novo Nordisk from Denmark costs an average of 10000 rubles ($20000). This is the cost of a two-day treatment. The same drug Saxenda, which is produced by the same company, will cost, on average, 25,000 rubles. For five syringe pens, which is the cost of a five-day treatment. Accordingly, the cost of liraglutide treatment for 56 weeks will cost the patient almost 2 million rubles. So it is still much easier for healthy people to reduce weight at the gym or in the pool, or just limit the amount of fat that comes with food, than to pay such money.
There is another very important circumstance. This drug is only for people with diabetes mellitus. If liraglutide is used by people with normal blood sugar levels, induction of insulin may lead to a drop in blood sugar, development of hypoglycemia, and even a coma. There are a large number of contraindications, drug interactions with other medications, and even the endocrinologist must be trained to work with this drug, and have experience prescribing it.
Metformin (Glyformin, Glucofage, Siofor, Formitin)
The second drug designed for the treatment of type 2 diabetes, which, we emphasize, as a side effect leads to weight loss in patients, is metformin. But, as in the previous case, it can not be used to treat obesity in persons without type 2 diabetes, and furthermore: if a patient takes metformin but is diagnosed with type 1 diabetes, it is simply dangerous to take this medication.
But if a patient with type 2 diabetes has excess body weight, when properly administered metformin begins to work weight loss, with little risk of hypoglycemia, or a drop in blood sugar. Metformin is contraindicated in marked renal pathology and chronic renal failure, in cardiac, hepatic, respiratory failure, dehydration, chronic alcoholism. Siofor 850 mg in tablets, 60 pills (company Berlin Chemi) will cost inexpensive, from 260 to 370 rubles., Domestic Glyformin, produced by the company Akrichin, will cost even cheaper – a maximum of 120 rubles. per package (500 mg #60).
Baeta, Baeta-Long (exenatide)
Another analog of glucagon-like peptide can be the drug Baeta-Long, exenatide. The difference between Baeta-Long and liraglutide is the need for once a week rather than daily injections of the drug under the skin. In addition, exenatide may not be used alone, but as an adjunct to metformin. This provides better blood sugar control. The drug Baeta-Long, which is produced by Astra Zeneca, has been used in Europe since 2011, but in the Russian market it appeared only 2 years ago, in 2017.
Despite its subcutaneous injection, the drug is in microspheres, which, once under the skin, gradually dissolve, and the drug is gradually removed from the focus of injection. Nevertheless, there is a risk of developing specific antibodies to this drug, and according to the laws of the immune system, the less frequently the drug is administered, the greater the risk of such neutralizing antibodies, reducing the entire clinical effect. In the case of using the usual short-acting liraglutide once a day, this risk of antibodies is much lower. How much does Baeta-Long cost? In Moscow pharmacies you can buy a pack of 4 for a month for 11000 rubles.
After reading about hormonal drugs, it is likely to sadden people with excess body weight, but without the presence of diabetes mellitus. How to be? Very simply. If your doctor advises it, you can use, though very carefully, strictly on the basis of indications and in the absence of contraindications, drugs from the group of antidepressants. It has long been known that mood medications from the group of especially selective serotonin reuptake inhibitors (SSRIs), such as fluoxetine, paroxetine and others, have as a side effect a decrease in appetite. For some this effect is more pronounced and for some it is less pronounced. One of the leaders in terms of severity of appetite suppression from antidepressants is a drug sibutramine.
Sibutramine (Meridia, Reduxin, Slimia, Goldline Plus)
Despite the fact that this drug acts directly on the main appetite regulation center in the brain, it belongs to the antidepressants, not to the anorectics. That is still considered to be its main antidepressant effect, since it blocks the reuptake of neurotransmitters.
Let’s just say that it has been banned for 9 years in Europe, due to the high risk of cardiovascular complications. It is approved for use in the United States, but with a mandatory caveat from the manufacturer in the instructions that if the patient has a cardiovascular condition, it should not be used. In our country it is sold, although it cannot be bought on the open market, but only with a prescription, and it is included in potent drugs. But if you want to buy it, you can.
Some weight loss fanatics combine the use of sibutramine with the aforementioned metformin to treat type 2 diabetes. This is a categorically contraindicated and harmful combination. Sibutramine has side effects related to the risk of high blood pressure. Constipation, insomnia, irritability, headaches appear. A large number of even fatal outcomes are known, usually associated with self-medication and improper prescribing of the drug.
Sibutramine may be a part of different dietary supplements that are offered for weight loss, and the dosage in these supplements may be many times higher than the maximum allowable, but the fact of sibutramine presence may be hidden. Therefore you should be extremely picky when choosing weight loss drugs, especially those which are on the free market, bought on the internet and brought from China.
One of the most purified drugs is Meridia, which is manufactured by Abbott and sold in 15 mg capsules, in a pack of 28 capsules. It should be prescribed when the body mass index exceeds 27. The results can be seen as a 10% reduction in body weight after 6 months.
Let us briefly list the main official contraindications to taking sibutramine:
- Organic obesity, that is, when the cause is related to a disease;
- The presence of appetite and eating disorders – exhaustion caused by anorexia or the presence of bulimia;
- mental disabilities;
- Taking MAO inhibitors;
- cardiovascular disease or the presence of arterial hypertension;
- Increased thyroid function;
- Chronic kidney and liver failure;
- prostate adenoma, adrenal tumor, glaucoma;
- Childhood, pregnancy and lactation;
- Chronic alcoholism and drug addiction.
Thus, not all obesity can be treated with sibutramine.
Russian sibutramine drugs on the market – Reduxin and Goldline Plus in its composition, in addition to sibutramine, have microcrystalline cellulose. It is not absorbed by the body, has no medicinal effect, but it swells up and creates a false feeling of fullness, like bran or regular fiber. So in case you really want to lose weight, but are rightly afraid of the side effects of sibutramine, just eat plain bran. It is both beneficial and low-cost, and will eventually lead to weight loss.
It should be added that even domestic and not the best in the world preparations of sibutramine, such as Reduxin and Goldline Plus is not cheap. The minimum cost of a package of Reduxin, produced by the domestic company Ozon in the amount of 30 capsules will cost from 1400 rubles.
Of course, there are other drugs from the antidepressant group, such as Prozac (fluoxetine), Velafax (venlafaxine) of the Croatian company Pliva, or Rexetine aka paroxetine, of the Hungarian company Gedeon Richter. These are antidepressants that are used for appropriate indications, to treat anxiety and depression. Reduced appetite, and weight loss would be an appropriate side effect. In free sale, without a prescription, you can not buy them, and this is correct. However, even if these drugs are prescribed for indications, they have specific adverse reactions inherent to the SSRI group. For example, dry mouth, restless legs syndrome at night, and ejaculatory disorders in men.
About Prospects and Foreign Drugs
In countries with advanced health care, new drugs are constantly being tested and studied, as well as different combinations of older drugs that can be used to treat obesity. For example, there is a drug Contraive. In the Russian Federation it is not registered and not sold, but it is used abroad. It is a combination of an opioid receptor blocker, naltrexone, and a serotonin reuptake inhibitor, bupropion. As a result of using Contraive, over a similarly long period of 56 weeks, volunteers lost about 5% of their body weight.
Rimonabat (Acomplia, Zimulti)
There is a promising direction in the use of cannabinoid receptor blockers, which can be used as anorectics, or appetite suppressant medications. But so far, alas, “the first pancake is a cakewalk. The drug Acomplia, or rimonabate, has already been created. This is a pure cannabinoid receptor antagonist, and acts exclusively on the appetite center. Again, it was not without side effects, chief among which was thought to be increased thermogenesis. It was sold in Russia until 2010 under the name Zimulti, but then it was recalled first in Europe and then in Russia because it had even more serious side effects related to neuropsychiatric disorders while taking.
Of the remedies used abroad to reduce appetite, currently the most commonly used is lorcaserin, or Belvik. It is a mild relative of amphetamines, and works best when taken within a few months; if prescribed longer (a year or more), its effectiveness diminishes. Patients with diabetes and obesity are also known to lose about 5% of their body weight over a year of treatment. Lorcaserin is the only anorectic, that is, appetite-reducing drug that can be used for a long time and is not addictive.
There are other drugs, such as Tenuate, Bontril, Regimex – the real relatives of amphetamines. They can already cause true physical and mental dependence, especially if used for a long time. That is why even in the United States the circulation of these drugs is strictly controlled.
Xymia (phentermine + topiramate)
There is a drug called Xymia. This is a combination of the antiepileptic drug topiramate, also recently on the market, with phentermine. In our country it is unlikely that this drug will ever be used, because phentermine is included in list 2 of the list of narcotic and psychotropic drugs and their precursors. Phentermine is a strong psychostimulant, an amphetamine-like substance that strongly suppresses appetite.
Why it is legal in some countries? Because, unlike amphetamines, it does not induce euphoria and therefore does not form a psychological dependence. It is used in the form of the drug Adipex, and in Australia and New Zealand there are prolonged forms of the drug. Combining this substance with topiramate allows increasing the inhibitory activity of gamma-aminobutyric acid, and thus ensures that there will be no addiction after all.
Over a similarly long period of 56 weeks, patients reduced body weight by up to 10 kg, and so far this is an obvious record. But Xymia and its analogues also have side effects. For example, women’s plasma estrogen concentrations drop, and if they use the combined oral contraceptive, it is no longer as effective, and the risk of bleeding increases. The incidence of anxiety and depressive episodes increases significantly with prolonged use, so a full medical examination is necessary before using this drug.
In conclusion we would like to warn our readers against self-treatment of obesity with drugs, and various unregistered questionable dietary supplements, over-the-counter drugs that can be easily purchased in Internet stores. It is dangerous to your health. As shown by numerous clinical studies, 85% of patients, and people in general, with persistent thoughts of losing weight do not need to use drugs. They can reduce their body weight to the ideal weight on their own in a year or two with the help of non-drug methods – diet, physical activity, and lifestyle changes.