A drug that until the end of July was admitted only for use in people with type 2 diabetes was approved by the National Administration of Medicines, Food and Medical Technology (ANMAT) to use in people with obesity. The parent drug (semaglutide) is already marketed under the name Ozempic and the remedy to come contains it in higher weights (2 and 4 grams) under the trade name Wegovy. Both remedies are manufactured by the danish lab Novo Nordisk, and are part of a class of drugs called GLP-1 receptor agonists, that since 2017 have radically changed the treatment of both diabetes and obesity. With its light and dark.
And it is that due to the results obtained in scientific studies, they began to sell (first the Ozempic, the second dates from 2021) even without medical prescription and without diabetes involvedto the point that Ozempic came to run out of pharmacies in the countries where it was approved and diabetic people could not buy it because those who only wanted to lose a few kilos of weight had already swept it away. Billionaire Entrepreneurs (Elon Muskcurrent owner of Tesla, SpaceX and the former social network Twitter today called X), artists, influencers, singers and celebrities of all kinds are giving it daily use, to the point that only in 2022 he producer laboratory declared a 50 percent increase in your earnings.
In fact, the global demand its alot higher than production capacity of the laboratory, to such an extent that Wagovy would not arrive in Argentina before mid-2024.
Findings
A little over two decades ago, an experiment was carried out in which healthy individuals were given 50 grams of glucose orally, while another group received 50 grams of glucose intravenously. The initial assumption was that both pathways would equally raise the amount of insulin produced by the pancreas. The researchers found, however, that volunteers given glucose by mouth produced 60% more insulin than healthy people given glucose intravenously. From there it was found that there was something, at the intestinal level, that intervened in the increased insulin levels.
“Were detected two substances produced in the intestine: one was called GLP-1 and the other GIP. The scientists verified that these analogues (technically, intestinal incretins), particularly in the case of GLP-1, helped to produce a greater amount of insulin by beta cells in the presence of glucose at the intestinal level. These substances are naturally produced in the body, but the duration does not normally exceed 3 to 5 minutes -explains the diabetologist Gabriel Lijteroff, director of the scientific committee of the Argentine Diabetes Federation (FAD)-. From there, they began to look for a strategy that would prolong the life of this substance called GLP-1 or that would inhibit its rapid destruction. As a result of the research, two types of drugs emerged. Some, the GLP-1 analogues, could be synthesized in the laboratory to have a longer duration administered subcutaneously”.
In the various studies with GLP-1 analogues, the researchers found that the substances, in addition to helping to produce glucose through a mechanism called glucose-dependent (if the person does not eat, it does not act), help increase weight loss. “And also, over the years, studies have shown that these drugs have a preventive action both on the cardiovascular system and in renal pathology associated with diabetes”, adds Lijteroff, a member of the executive committee of International Diabetes Federation for the South American and Caribbean Region (SACA).
The first analogue of GLP-1 presented in Argentina was exenatide, which is given subcutaneously every 12 hours, and later others appeared that are also being marketed in Argentina, such as liraglutide and lixisenatide. Now there is a new generation of GLP-1 analogs that has the advantage that it can be given, instead of every 12 hours or daily, on a weekly basis, like semaglutide or dulaglutide. A box of any of these remedies does not fall, on average, from the one hundred thousand pesos.
Performance
The action of semaglutide, which is being marketed for type 2 diabetes in doses of 0.5 to 1 gram, is given through various mechanisms. In the case of diabetes, and in the presence of glucose, these GLP-1 analogues are activated, helping the insulin production by the remaining beta cells left in the pancreas of a person with type 2 diabetes. But semaglutide also has a action also at the brain levelthat is to say, cerebral suppress appetite. This mechanism is related to the fact that people, both those with type 2 diabetes and those who are obese, have an increase in a substance called ghrelin on the roof of the stomach, which reduces or slows down the feeling of satiety.
“In such a way that with these GLP-1 analogues, the action of ghrelin can be inhibited, and therefore the person returns to having a normal perception of satiety. Consequently, he eats less than he was eating up to now, the appetite is normalized in this way and by a non-amphetamine mechanism the person manages to lose weight. With the benefit that, being what we call glucose dependent, that is, if the person does not eat, they do not act, the medication minimizes the chances of this person having hypolucemia”, explains Lijteroff, who is also head of diabetology of Hospital Santamarina de Monte GrandeBuenos Aires province.
Another of the effects that these GLP-1 analogues have is that slow down stomach emptying. Normally gastric emptying takes about two hours then, but if this process slows down the person has a feeling of satiety that also helps to reduce appetite and lose weight.
Furthermore, in the USA and in the European Union There is already a presentation of semaglutide in the form of tablets that are taken once a day, with a dosage of three, seven and up to 14 milligrams, under the name Rybelsus.
The average weight loss achieved with these drugs, always accompanied by a healthy diet and physical activity, is 10 percent over at least six months. But that percentage of weight loss depends on the amount of drug the person receives.
In it last American congress on diabetes held in June more drugs were introduced. The tirzepatidas that are currently used for the treatment of diabetes (and that combine GLP-1 with another substance) could be approved for use against obesity next year in the United States, and according to the studies presented by their producing laboratory ( Ely Lilly), allows to obtain a weight loss of 15.7% in adults.
And another one, the portrayed, which is administered orally and is still in phase 2 studies, combines three neutransmitters. “He presented himself at this American congress with a very significant weight loss at 48 weeks, of almost 28% in women and a percentage close to 22% in men with an average drop of 24%”, summarizes Lijteroff.
Precautions
And he warns: “It is important to take into account that these drugs, for use in type 2 diabetes or for obesity have to be prescribed by a doctor, because with respect to type 2 diabetes, the association with certain types of drugs can generate hypoglycemia. Furthermore, it is important to note that They are authorized only for people over 10 or 12 years of age, according to different laws, and only for type 2 diabetes and not for type 1 diabetes or insulin dependent.
The effect of this type of medication is dose dependent, that is, it has been seen that the higher the dose, the more weight loss, but due to the decrease in the speed of gastric emptying, also these side effects such as nausea and fullness increase with dose. For this reason, the dose must be started gradually until the useful or clinically tolerated dose is reached.
“Although the clinical experience did not give problems, in experimentation with animals (rats, specifically) the researchers found that increased thyroid cancer Lijteroff concludes. In such a way that to people who have, although this was not seen in human beings, there is a recommendation that in people who have a history of thyroid cancer in the family must refrain from using it or use it under medical prescription”.
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