From the Guidelines
Ozempic (semaglutide) works by mimicking the action of the naturally occurring hormone GLP-1 (glucagon-like peptide-1) in the body, binding to and activating GLP-1 receptors to stimulate insulin secretion, suppress glucagon release, slow gastric emptying, and increase feelings of fullness, leading to decreased food intake and improved blood glucose control. As a GLP-1 receptor agonist, semaglutide has a long half-life of approximately one week, allowing for once-weekly subcutaneous injection dosing 1. This multi-faceted approach to blood glucose control makes Ozempic effective for managing type 2 diabetes and, at higher doses (as Wegovy), for weight management in eligible patients with obesity or overweight with weight-related comorbidities. The mechanism of action of semaglutide involves stimulating insulin secretion from pancreatic beta cells when blood glucose levels are elevated, while simultaneously suppressing glucagon release from pancreatic alpha cells, which helps reduce hepatic glucose production 1. Additionally, semaglutide slows gastric emptying, which delays the absorption of glucose from the gut into the bloodstream, preventing rapid spikes in blood sugar after meals, and acts on the brain's appetite control centers to increase feelings of fullness and reduce hunger, leading to decreased food intake 1.
Some of the key benefits of semaglutide include its ability to reduce cardiovascular events in people with type 2 diabetes who are either at high risk for cardiovascular disease or have cardiovascular disease, as well as its effectiveness in reducing weight and improving weight-related comorbidities in individuals with obesity or overweight 1. However, it is essential to consider the potential side effects and contraindications of semaglutide, including nausea, vomiting, diarrhea, and increased risk of pancreatitis, as well as its use in patients with a history of medullary thyroid cancer or multiple endocrine neoplasia type 2 1.
Overall, the use of semaglutide as a treatment for type 2 diabetes and obesity has been supported by numerous studies, including the STEP trials, which demonstrated significant weight loss and improvement in weight-related comorbidities in individuals with obesity or overweight 1. As such, semaglutide is a valuable treatment option for eligible patients, offering a range of benefits that can improve morbidity, mortality, and quality of life.
From the FDA Drug Label
Semaglutide is a GLP-1 analogue with 94% sequence homology to human GLP-1. Semaglutide acts as a GLP-1 receptor agonist that selectively binds to and activates the GLP-1 receptor, the target for native GLP-1. Semaglutide reduces blood glucose through a mechanism where it stimulates insulin secretion and lowers glucagon secretion, both in a glucose-dependent manner. The mechanism of blood glucose lowering also involves a minor delay in gastric emptying in the early postprandial phase.
The mode of action of Ozempic (semaglutide) is as a GLP-1 receptor agonist, which:
- Stimulates insulin secretion in a glucose-dependent manner
- Lowers glucagon secretion in a glucose-dependent manner
- Causes a minor delay in gastric emptying in the early postprandial phase This results in lowering of blood glucose levels 2.
From the Research
Mode of Action of Ozempic (Semaglutide)
The mode of action of Ozempic (semaglutide) involves stimulating the release of insulin and lowering blood glucose levels 3, 4. Semaglutide is a glucagon-like peptide-1 (GLP-1) receptor agonist that mimics the action of endogenous GLP-1, consequently reversing hyperglycemia and causing weight reduction 5.
Key Mechanisms
- Stimulates the release of insulin 4
- Lowers blood glucose levels 3, 4
- Suppresses glucagon secretion 5
- Decreases hunger 5
- Causes weight reduction 3, 4, 5
Administration and Formulation
Semaglutide is available in both subcutaneous and oral dosage forms 6, 5, 7. The subcutaneous formulation is administered using an injection device, while the oral formulation is the first ingestible GLP-1 receptor agonist 5, 7.