What are GLP-1 receptor agonists?
Glucagon-like peptide 1 (GLP-1) is a hormone released after eating that stimulates insulin secretion and inhibits glucagon secretion from the pancreas in a glucose-dependent manner. GLP-1 receptor agonists are medications that mimic the effects of naturally occurring GLP-1 to regulate blood sugar levels. They work by binding to and activating GLP-1 receptors on pancreatic beta cells and in the brain and small intestine. This leads to increased insulin production and reduced glucagon secretion only when glucose levels are high, thereby lowering the risk of hypoglycemia. GLP-1 receptor agonists also have the potential to reduce appetite and body weight. How do GLP-1 receptor agonists help manage diabetes? GLP-1 receptor agonists lower blood glucose in several ways: - They stimulate the pancreas to release more insulin when blood glucose is high after eating. This helps control post-meal spikes in blood sugar. - They inhibit the pancreas from secreting glucagon when blood glucose levels start to fall. Glucagon normally raises blood glucose, so reducing its levels helps prevent hypoglycemia. - They slow down gastric emptying to reduce the rate at which sugars enter the bloodstream after eating. This also helps smooth out post-prandial blood glucose rises. - In some cases, they may help beta cell function recovery and survival in the pancreas over time by reducing metabolic stress on these cells. - By reducing appetite and food intake, they can aid weight loss which itself contributes to improved blood glucose management. What GLP-1 receptor agonists are available? Several GLP-1 receptor agonists have been approved for treatment of type 2 diabetes: - Exenatide (Byetta): The first GLP-1 Receptor Agonists approved in 2005, it is administered twice daily as injections. - Liraglutide (Victoza): Approved in 2010, it provides once-daily dosing as injections and has a longer duration of action than exenatide. - Dulaglutide (Trulicity): Approved in 2014, it is dosed once weekly as injections. - Lixisenatide (Adlyxin): Approved in 2016, it requires once-daily injections before the largest meal of the day. - Semaglutide (Ozempic/Rybelsus): Approved in 2017 as injections and in 2020 as the only GLP-1 receptor agonist available in oral pill form (Rybelsus). It has a very long duration of action. How effective are GLP-1 receptor agonists? Clinical trials have shown that GLP-1 receptor agonists are highly effective at lowering hemoglobin A1c (HbA1c), a measure of long-term blood glucose control. In head-to-head studies, they performed as well as or better than other non-insulin diabetic medications. Their glucose-lowering efficacy depends on the specific medication and dose. Most GLP-1 receptor agonists can reduce HbA1c by 0.5-1.5% (e.g. from 8% to 6.5-7%) when used either as monotherapy or in combination with other oral medications. In addition, these medications are helpful for weight loss. Participants in clinical studies typically lost 5-10 lbs. on average compared to placebo, and weight loss increased with longer treatment duration. The appetite/satiety effects and slowing of gastric emptying likely contribute to these beneficial metabolic outcomes. Safety and tolerability of GLP-1 receptor agonists The most common side effects reported with GLP-1 receptor agonists include nausea, diarrhea, vomiting and constipation. These side effects are usually mild to moderate in severity and tend to decrease over time as the body adjusts to the medication. In rare cases, inflammation of the pancreas (pancreatitis) has occurred but it is difficult to distinguish whether this is caused by the diabetes itself or the medication. The Food and Drug Administration continues to monitor this potential safety risk. GLP-1 receptor agonists may cause a very small increased risk of thyroid cancer based on rodent studies but no increased risk has been confirmed in human trials or post-marketing data to date. Overall, these medications are generally well-tolerated with minimal risk of hypoglycemia when used as monotherapy or with anti-hyperglycemic agents that do not cause hypoglycemia. Close monitoring is required when used in combination with insulin or insulin secretagogues. Who are candidates for GLP-1 receptor agonist therapy? GLP-1 receptor agonists are a reasonable treatment option for many individuals with type 2 diabetes, especially those who: - Need help with weight loss or have overweight/obesity - Have not achieved glycemic targets on other oral agents - Are at risk of hypoglycemia from their current medications - Have a history of gastrointestinal intolerability with other drugs - Need an injectable therapy with high efficacy on HbA1c and other benefits - Prefer an injectable to an oral medication GLP-1 receptor agonists are effective diabetes medications that promote glycemic control as well as modest weight loss. Their glucose-dependent mechanism of action also offers a relatively low risk of hypoglycemia. Overall, they represent an important treatment approach for selected patients with type 2 diabetes. Get more insights on – GLP-1 Receptor Agonists About Author: Money Singh is a seasoned content writer with over four years of experience in the market research sector. Her expertise spans various industries, including food and beverages, biotechnology, chemical and materials, defense and aerospace, consumer goods, etc. (https://www.linkedin.com/in/money-singh-590844163)
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