Rybelsus is the brand name for the medication semaglutide. It is an oral prescription medication used to treat type 2 diabetes in adults. Semaglutide belongs to a class of drugs called glucagon-like peptide-1 receptor agonists (GLP-1 receptor agonists). These drugs work by helping the body produce more insulin when blood sugar levels are high and also reduce the amount of sugar produced by the liver.
Rybelsus is taken once daily and is often used in combination with diet and exercise to help manage blood sugar levels in people with type 2 diabetes. It may also lead to weight loss in some individuals.
Rybelsus for the treatment of obesity
Semaglutide is used not only in a diabetes treatment program where weight loss was a secondary, albeit desirable, treatment outcome, but also directly to treat obesity in people without diabetes.
The most recent clinical trial program to study the efficacy of semaglutide is the STEP program. Its main goal was to evaluate the effectiveness of semaglutide as a means of reducing body weight. STEP results showed that semaglutide was more effective in reducing body weight than placebo.
In a program of clinical trials comparing different doses of semaglutide, results showed that taking 7 mg of semaglutide resulted in more weight loss than taking 3 mg. The safety profile of semaglutide at a dose of 7 mg was found to be similar to that of semaglutide at a dose of 3 mg orally, with mild to moderate gastrointestinal side effects being the main complaints of study participants.
Cases of hypoglycemia have been reported infrequently, which is encouraging for the use of semaglutide in non-diabetic patients. The study found that in overweight or obese adults, treatment with semaglutide resulted in significant and sustained weight loss compared with placebo.
The main effects of taking Semaglutide:
- reduces glucose concentration;
- reduces insulin resistance;
- reduces the amount of fatty tissue;
- reduces overall body weight;
- reduces cravings for fatty foods.
Pharmacological action – hypoglycemic. Semaglutide is a GLP-1 receptor (GLP-1R) agonist obtained by recombinant DNA biotechnology using a strain of Saccharomyces cerevisiae with subsequent purification.
It has several effects on blood sugar and appetite regulation, as well as on the cardiovascular system. The effect on glucose concentration and appetite is specifically mediated by GLP-1R localized in the pancreas and brain. Pharmacological concentrations of semaglutide reduce blood sugar and body weight. Semaglutide lowers blood glucose by glucose-dependent stimulation of insulin secretion and inhibition of glucagon secretion. Thus, with an increase in blood glucose concentration, insulin secretion is stimulated and glucagon secretion is suppressed. The blood glucose lowering mechanism also involves a slight delay in gastric emptying in the early postprandial phase. In hypoglycaemia, semaglutide reduces insulin secretion and does not reduce glucagon secretion.
Semaglutide reduces total body weight and adipose tissue mass by reducing energy intake. This mechanism includes a general decrease in appetite, including increased satiety signals and reduced hunger cues, as well as better control of food intake and reduced cravings.
Semaglutide is absorbed by specific areas of the brain and improves key satiety signals and dampens key hunger signals. By acting on isolated areas of brain tissue, semaglutide activates neurons associated with satiety and suppresses neurons associated with hunger.
In clinical studies, semaglutide had positive effects on plasma lipids, lower systolic blood pressure and lower inflammation.
Semaglutide inhibits the development of atherosclerosis by preventing further development of aortic plaques and reducing inflammation in the plaques.
Rybelsus, oral semaglutide, is the first of a class of glucagon-like peptide-1 receptor agonists available in oral form. In a clinical program (PIONEER) investigating the effects of oral semaglutide, a dose-dependent effect of the drug was demonstrated, and at a maximum dose of 14 mg, oral semaglutide reduced glycated hemoglobin levels ( HbA1c) of -1.4%, and in body weight – up to 5 kg from the initial level.
Oral semaglutide has been shown to be safe in terms of cardiovascular outcomes. The oral form has its own characteristics of use, which must be taken into account for the maximum effectiveness of the drug, since the effective concentration of the drug depends on the correct observance of these conditions.
The drug should be taken daily on an empty stomach with half a glass of water, half an hour before meals or taking other medications. The most common adverse events associated with semaglutide treatment (nausea, diarrhea and vomiting) characteristic of this class were transient and generally manifested by an increase in the dose of the drug.
Semaglutide – side effects
The most common side effects were gastrointestinal upset, including nausea, diarrhea, and vomiting. In general, these reactions were mild to moderate in intensity and of short duration. Most often, these side effects are observed during the first weeks of treatment.
The frequency of treatment discontinuation due to side effects was 9% in patients receiving the drug. The most common adverse reactions leading to discontinuation of treatment were gastrointestinal disturbances.
Other side effects are rare:
- Immune system – anaphylactic reactions;
- On the part of metabolism and nutrition – hypoglycemia when used with insulin and sulfonylurea derivatives, decreased appetite;
- From the side of the nervous system – dizziness;
- On the part of the organ of vision – complications of diabetic retinopathy;
- From the side of the heart – increased heart rate;
- Gastrointestinal disorders – vomiting, abdominal pain, bloating, constipation, dyspepsia, gastritis, GERD, belching, flatulence, acute pancreatitis;
- Liver and biliary tract – cholelithiasis;
- General ailments – fatigue.