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Incretin Mimetics

Incretin Mimetics For Type 2 Diabetes

Incretin Mimetics For Type 2 Diabetes

Examples Generic Name Brand Name exenatide Bydureon, Byetta liraglutide Victoza Exenatide and liraglutide are a type of medicine called incretin mimetics used to treat people who have type 2 diabetes and who have not been able to control their blood sugar levels with oral medicines. This medicine is given as a shot. This medicine is also known as a glucagon-like peptide 1 (GLP-1) receptor agonist, or GLP-1 agonist. How It Works Incretin is a natural hormone that your body makes. It tells your body to release insulin after you eat. Insulin lowers blood sugar. Incretin mimetics act like (mimic) the incretins in your body that lower blood sugar after eating. Incretin mimetics: Prompt your pancreas to release insulin when blood sugar is rising. Prevent the pancreas from giving out too much glucagon. Glucagon is a hormone that causes the liver to release its stored sugar into the bloodstream. Help to slow the rate at which your stomach empties after eating. This may make you feel less hungry and more satisfied after a meal. Your blood sugar shouldn't get too high too fast after a meal. Why It Is Used These medicines help to keep blood sugar in a target range without causing low blood sugar or weight gain, unless they are taken in combination with medicines that do. Some people feel less hungry and lose weight while taking these medicines. How Well It Works Type 2 diabetes is a disease that can get worse over time, so medicines may need to change. Diabetes medicines work best for people who are being active and eating healthy foods. Studies have suggested that incretin mimetics lower hemoglobin A1c by 0.5% to 1%.1 All medicines have side effects. But many people don't feel the side effects, or they are able to deal with them. Ask your pharmacist about the side effects of each Continue reading >>

Byetta, Januvia/janumet And Victoza

Byetta, Januvia/janumet And Victoza

Posted in Byetta, Januvia/Janumet and Victoza , Defective Drugs Victoza (liraglutide), an injectable Type II diabetes drug, which works by stimulating insulin production by the pancreas, received approval from the U.S. Food and Drug Administration (FDA) in 2010. When taken in high doses (3 milligrams), Victoza, manufactured by Novo Nordisk, has been shown to help individuals lose weight. The drug suppresses an individuals appetite, as well as decreases the absorption of sugar from the digestive system, and slows movement of food through the digestive system. In essence, the individual is likely to feel fuller for a longer period of time when taking Victoza. Accordingly, individuals began reporting weight loss while taking Victoza. Subsequently, in August 2017, the FDA also approved Victoza to reduce the risk of heart attack, stroke, and cardiovascular death, in adults with Type II diabetes and established cardiovascular disease. Posted in Byetta, Januvia/Janumet and Victoza , Defective Drugs As we have previously reported, safety concerns regarding incretin mimetics (such as Byetta, Januvia/Janumet and Victoza), led to more than a thousand lawsuits being filed across the country. Reports suggest that people taking the medications for the treatment of Type 2 diabetes may be at an increased risk of developing pancreatic cancer. In August 2013, those lawsuits were consolidated in a Multi-District Litigation (MDL), before Judge Anthony J. Battaglia, in the United States District Court for the Southern District of California. The litigation suffered an unexpected setback when, in November 2015, the trial court granted summary judgment, essentially dismissing the claims. Posted in Byetta, Januvia/Janumet and Victoza The U.S. Food and Drug Administration (FDA) warned that Typ Continue reading >>

Therapeutic Role Of Incretin Mimetics

Therapeutic Role Of Incretin Mimetics

Weight Changes in the 3 Pivotal Exenatide Trials Data adapted from: DeFronzo et al., [12] Buse et al., [13] and Kendall et al. [14] Drucker DJ. Enhancing incretin action for the treatment of type 2 diabetes. Diabetes Care. 2003;26:2929-2940. Abstract Gerich JE. Physiology and pathophysiology of postprandial glucose regulation. Medscape Diabetes & Endocrinology. 2004;6(2). Available at: Accessed June 13, 2005. Vahl TP, D'Alessio DA. Glucagon-like peptide 1: incretin, glucose regulatory hormone and diabetes treatment, part II. Medscape Diabetes & Endocrinology. 2004;6(1). Available at: Accessed June 13, 2005. Perfetti R. The role of GLP-1 in the regulation of islet cell mass. Medscape Diabetes & Endocrinology. 2004;6(2). Available at: Accessed June 13, 2005. Uwaifo GI, Ratner RE. Novel pharmacologic agents for type 2 diabetes. Endocrinol Metab Clin North Am. 2005;34:155-197. Abstract Harris MI, Eastman RC, Cowie CC, et al. Racial and ethnic differences in glycemic control of adults with type 2 diabetes. Diabetes Care. 1999;22:403-408. Abstract Weyer C, Bogardus C, Mott DM, Pratley RE. The natural history of insulin secretory dysfunction and insulin resistance in the pathogenesis of type 2 diabetes mellitus. J Clin Invest.1999;104:787-794. Abstract Nielsen LL, Baron AD. Pharmacology of exenatide (synthetic exendin 4) for the treatment of type 2 diabetes. Curr Opin Investig Drugs. 2003;4:401-405. Abstract Degn KB, Brock B, Juhl CB, et al. Effect of intravenous infusion of exenatide (synthetic exendin 4) on glucose dependent insulin secretion and counterregulation during hypoglycemia. Diabetes. 2004;53:2397-2403. Abstract Kolterman OG, Buse JB, Fineman MS, et al. Synthetic exendin-4 (exenatide) significantly reduces postprandial and fasting plasma glucose in subjects with t Continue reading >>

Side Effects Of Incretin Mimetics (glp-1 Agonists)

Side Effects Of Incretin Mimetics (glp-1 Agonists)

Incretin Mimetics: How they work Incretins are protein hormones produced in the digestive tract after we have eaten a meal. They lead to an increase in insulin secretion, so the sugar from the meal can be delivered from our blood into our cells, reducing blood sugar levels. Incretin mimetics ‘mimic’ the incretin called GLP-1, so they too lower blood sugar. You need inject incretin mimetics, also known as GLP-1 agonists, under your skin, just before a meal. Side effects of Incretin Mimetics or GLP-1 drugs may be the result of the way they work in the human body. Incretin Mimetics lower blood sugar in the human body by: Increasing insulin secretion from the pancreas after a meal Reducing the amount of glucagon secreted from the pancreas. Glucagon is a hormone that signals the liver to release stored sugar into the blood stream Reducing the speed at which food is ‘emptied’ into the intestine. This helps you feel fuller for longer and reduces appetite. Incretin Mimetics: Most Prescribed brands Three incretin mimetics are most prescribed and sold: Exenatide (Immediate Release), which was the first in this class of drugs and sold under the brand name Byetta Exenatide (Long Acting), sold under the brand name Bydueron Liraglutide, sold under the trade name, Victoza Other commonly available brand names are Saxenda and Trulicity. Exenatide is isolated from the saliva of a lizard called Heloderma suspectum. (popularly called the Gila Monster). Exenatide (Immediate Release) or Byetta is sold as as a solution (liquid) in a prefilled dosing pen. You need to inject it just under the skin twice a day, just before meals. It should never be injected after meals. Your doctor will probably start you on a low dose of Exenatide (Immediate Release) and may switch you a higher dose if Continue reading >>

Incretin Mimetics And Dpp-iv Inhibitors: New Paradigms For The Treatment Of Type 2 Diabetes

Incretin Mimetics And Dpp-iv Inhibitors: New Paradigms For The Treatment Of Type 2 Diabetes

Abstract Incretin mimetics are a new class of pharmacological agents with multiple antihyperglycemic actions that mimic several of the actions of incretin hormones originating in the gut, such as glucagon-like peptide (GLP)-1. Dipeptidyl peptidase-IV (DPP-IV) inhibitors suppress the degradation of many peptides, including GLP-1, thereby extending their bioactivity. These agents seem to have multiple mechanisms of action for the treatment of type 2 diabetes mellitus (T2DM), including some or all the following: enhancement of glucose-dependent insulin secretion, suppression of inappropriately elevated glucagon secretion, slowing of gastric emptying, and decreased food intake. Exenatide (BYETTA®) is the first incretin mimetic approved for clinical use by the US Food and Drug Administration. In phase 3 clinical trials, exenatide reduced HbA1c by ∼1% and body weight by ∼2 kg in T2DM patients failing to achieve glycemic control with metformin and/or a sulfonylurea, with mild-to-moderate nausea the most common side effect. Several GLP-1 analogues and DPP-IV inhibitors are in late-stage clinical testing and may soon become available for treating T2DM patients. The use of these agents may provide an opportunity to bring about new improvements in diabetes care. Continue reading >>

Medications: Incretin Mimetics

Medications: Incretin Mimetics

For decades, insulin was the only injectable diabetes medication. But in the past seven years, several more have come on the market, including three incretin mimetics: exenatide (Byetta) , long-acting exenatide (Bydureon), and liraglutide (Victoza). These medications are approved only for the treatment of type 2 diabetes , though they may someday be used by people with type 1 as well ("Incretin Mimetics and Type 1," below). Many have heralded this class of medications as a monumental advance in diabetes care, and indeed their attractive characteristics include promoting weight loss and carrying a low risk for hypoglycemia (low blood glucose) . Here's the skinny on incretin mimetics: how they work, how they differ, and what to consider discussing with your doctor. Incretins are a group of hormones, and all three U.S.-approved incretin mimetics mimic the same incretin hormone, GLP-1. This hormone is made by specialized cells in the small intestine, which release the incretin into the body when they sense food from a meal passing through the intestines. Sources: (for weight loss and A1C reduction): The Lancet, published online June 8, 2009; presentation by John Buse, MD, PhD, at the European Association for the Study of Diabetes 2011 annual meeting Once in the bloodstream, incretins travel around the body, affecting several organs, including the pancreas. Incretins spur cells in the pancreas to make more insulin in response to a rise in blood glucose. The insulin brings blood glucose levels back down after eating. Incretins also suppress the production of glucagon, a hormone that signals the liver to release its glucose stores into the blood. When the liver holds back its stored glucose, blood glucose levels are more likely to remain in the normal range. "Glucagon suppres Continue reading >>

Incretin Mimetics: Pros And Cons, And Emerging Agents In Diabetes Treatment

Incretin Mimetics: Pros And Cons, And Emerging Agents In Diabetes Treatment

Type 2 diabetes mellitus (T2DM) is a huge health problem globally. It affects nearly 25.8 million people in the United States.1 Over 35% of US adults 20 years or older (or 79 million Americans) are currently classified as having prediabetes, which places them at greater risk for developing diabetes. Patients diagnosed with diabetes have a much higher risk of developing heart disease, hypertension, stroke, and kidney disease.1 No optimal medication exists currently for the treatment of T2DM. The American Diabetes Association (ADA) recommends metformin as the preferred initial pharmacologic agent for the treatment of this disease. However, if high doses of noninsulin monotherapy are not successful at achieving a patient’s goal glycated hemoglobin (A1C), then a second oral agent, a glucagonlike peptide-1 (GLP-1) receptor agonist or insulin should be added. Many patients will eventually need to have insulin added to their medication regimen.2 Numerous side effects exist with all medications used for the treatment of T2DM, including hypoglycemia and weight gain, as well as difficulty tolerating therapy.2 Some of the more recent classes of medications for the treatment of T2DM focus on the incretin or GLP-1 system. GLP-1 based therapies have not been studied in patients with type 1 diabetes (T1DM) and therefore should not be used in those patients at this time. The goal in the treatment of patients with T2DM is to restore normoglycemia both fasting and postprandially. Incretin Effect To understand how the medications affecting the incretin system work, it is necessary to first understand the incretin effect. When nondiabetic patients are given oral glucose, their insulin levels increase as much as 3 times greater than when the same patients are given IV glucose to match the Continue reading >>

Glucagon-like Peptide-1 Receptor Agonist

Glucagon-like Peptide-1 Receptor Agonist

Glucagon-like peptide-1 receptor agonists also known as GLP-1 receptor agonists or incretin mimetics are agonists of the GLP-1 receptor. This class of drugs is used for the treatment of type 2 diabetes.[1][2] One of their advantages over older insulin secretagogues, such as sulfonylureas or meglitinides, is that they have a lower risk of causing hypoglycemia.[3] There is some concern over the safety profile of these drugs due to proliferative effects in the pancreas. At the same time, diabetes is associated with both acute pancreatitis and pancreatic cancer, and the most recent studies have not found that these drugs can cause either pancreatitis or cancer.[4] Approved GLP-1 agonists: exenatide (Byetta/Bydureon), approved in 2005/2012 liraglutide (Victoza, Saxenda), approved 2010[5] lixisenatide (Lyxumia), approved in 2016[6] albiglutide (Tanzeum), approved in 2014 by GSK[7] dulaglutide (Trulicity), approved in 2014—manufactured by Eli Lilly[8] semaglutide (Ozempic), approved in 2017.[9] Under investigation:[1] taspoglutide, phase III halted Sept 2010 These agents work in the same pathway as DPP-4 inhibitors but are generally considered more potent.[10] As of 2017 it is unclear if they affect a person's risk of death.[11] [edit] Continue reading >>

Incretin Mimetics (glp-1 Agonists)

Incretin Mimetics (glp-1 Agonists)

Tweet Incretin mimetics are a relatively new group of injectable drugs for treatment of type 2 diabetes. The drugs, also commonly known as glucagon-like peptide 1 (GLP-1) receptor agonists or GLP-1 analogues, are normally prescribed for patients who have not been able to control their condition with tablet medication. Drugs in this class In the UK, the following incretin mimetics are available for type 2 diabetic patients - (trade name first, generic name in brackets): Bydureon (Exenatide) - taken once weekly Byetta (Exenatide) - taken twice daily Lyxumia (lixisenatide) - taken once daily Trulicity (Dulaglutide) - taken once weekly Victoza (Liraglutide) - taken once daily Byetta and Bydureon are the same medical drug. The only difference is that Bydureon is long-lasting, requiring only one injection per week, whereas Byetta is taken twice-daily due to its much shorter-term effects. How do they work? They work by copying, or mimicking, the functions of the natural incretin hormones in your body that help lower post-meal blood sugar levels. These functions include: Stimulating the release of insulin by the pancreas after eating, even before blood sugars start to rise. Inhibiting the release of glucagon by the pancreas. Glucagon is a hormone that causes the liver to release its stored sugar into the bloodstream. Slowing glucose absorption into the bloodstream by reducing the speed at which the stomach empties after eating, thus making you feel more satisfied after a meal. These effects are in direct response to the presence of carbohydrate in the gut and therefore the chance of significant hypoglycemia occurring is unlikely, unless used in combination with other hypoglycemic drugs. Benefits of incretin mimetics By increasing insulin secretion and inhibiting glucagon releas Continue reading >>

Incretin Mimetics: A Novel Therapeutic Option For Patients With Type 2 Diabetes A Review

Incretin Mimetics: A Novel Therapeutic Option For Patients With Type 2 Diabetes A Review

Incretin mimetics: a novel therapeutic option for patients with type 2 diabetes a review We are experimenting with display styles that make it easier to read articles in PMC. The ePub format uses eBook readers, which have several "ease of reading" features already built in. The ePub format is best viewed in the iBooks reader. You may notice problems with the display of certain parts of an article in other eReaders. Generating an ePub file may take a long time, please be patient. Diabetes, metabolic syndrome and obesity : targets and therapy Incretin mimetics: a novel therapeutic option for patients with type 2 diabetes a review Katrine B Hansen, Tina Vilsbll, and Filip K Knop Type 2 diabetes mellitus is a metabolic disease associated with low quality of life and early death. The goal in diabetes treatment is to prevent these outcomes by tight glycemic control and minimizing vascular risk factors. So far, even intensified combination regimen with the traditional antidiabetes agents have failed to obtain these goals. Incretin mimetics are a new class of antidiabetes drugs which involve modulation of the incretin system. They bind to and activate glucagon-like peptide-1 (GLP-1) receptors on pancreatic beta-cells following which insulin secretion and synthesis are initiated. Since the compounds have no insulinotropic activity at lower glucose concentrations the risk of hypoglycemia a well-known shortcoming of existing antidiabetes treatments is low. Additionally, incretin mimetics have been shown to be associated with beneficial effects on cardiovascular risk factors such as weight loss, decrease in blood pressure and changes in lipid profile. Current clinical data on the two available incretin mimetics, exenatide and liraglutide, are evaluated in this review, focusing on Continue reading >>

Incretin-based Therapies

Incretin-based Therapies

INTRODUCTION (by M.A.N.) Incretin mimetics and inhibitors of the protease dipeptidyl peptidase (DPP)-4 are new classes of antidiabetic agents first introduced in the years 2005 (exenatide) and 2007 (sitagliptin), respectively. Both use the antidiabetic properties of the incretin hormone, glucagon-like peptide (GLP)-1 (1). This gut-derived peptide hormone not only augments glucose-induced insulin secretion (required to fulfill the definition of an incretin hormone), but does so in a highly glucose-dependent manner (2), thus preventing GLP-1 alone from provoking hypoglycemia. Additional beneficial effects of GLP-1 on endocrine pancreatic islets are that it 1) supports the synthesis of proinsulin to replenish insulin stores in β-cells; 2) reduces the rate of β-cell apoptosis when islets are incubated in a toxic environment (glucotoxicity, lipotoxicity, cytotoxic cytokines); and 3) promotes differentiation of precursor cells with the ability to develop into β-cells and proliferation of β-cell lines, and in whole animals (rodent studies), this leads to an increased β-cell mass within a few days or weeks (1,3). Furthermore, GLP-1 can lower glucagon concentrations, i.e., induce α-cells to respond again to the inhibitory action of hyperglycemia, while leaving the counterregulatory glucagon responses undisturbed, as in the case of hypoglycemia (2,4). Additional activities of GLP-1 are the deceleration of gastric emptying (5), which slows the entry of nutrients into the circulation after meals, a reduction in appetite, and earlier induction of satiety (6), leading to weight reduction with chronic exposure (7). Renal effects (promotion of sodium and water excretion (8), as well as neuro- (9) and cardioprotective (10) properties of GLP-1, have also been described. While GLP-1 Continue reading >>

Incretin Mimetics

Incretin Mimetics

What are Incretin mimetics Incretin mimetics are agents that act like incretin hormones such as glucagon-like peptide-1 (GLP-1). They bind to GLP-1 receptors and stimulate glucose dependent insulin release, therefore act as antihyperglycemics. Incretin mimetics also suppress appetite and inhibit glucagon secretion. They slow gastric emptying and as a result prevent steep rise in post-prandial blood glucose levels. Incretin mimetics are only used to treat type 2 diabetes. List of Incretin mimetics: Filter by: -- all conditions -- Drug Name View by: Brand | Generic Reviews Avg. Ratings Victoza (Pro, More...) generic name: liraglutide 526 reviews 8.0 Byetta (Pro, More...) generic name: exenatide 79 reviews 7.9 Saxenda (Pro, More...) generic name: liraglutide 562 reviews 7.9 Bydureon (Pro, More...) generic name: exenatide 191 reviews 6.9 Trulicity (Pro, More...) generic name: dulaglutide 337 reviews 5.9 Tanzeum (Pro, More...) generic name: albiglutide 11 reviews 4.6 Adlyxin (Pro, More...) generic name: lixisenatide 0 reviews Add rating Bydureon BCise (Pro, More...) generic name: exenatide 1 review Add rating Continue reading >>

Incretin

Incretin

GLP-1 and DPP-4 inhibitors Incretins are a group of metabolic hormones that stimulate a decrease in blood glucose levels. Incretins are released after eating and augment the secretion of insulin released from pancreatic beta cells of the islets of Langerhans by a blood glucose-dependent mechanism. They also slow the rate of absorption of nutrients into the blood stream by reducing gastric emptying and may directly reduce food intake. They also inhibit glucagon release from the alpha cells of the islets of Langerhans. The two main candidate molecules that fulfill criteria for an incretin are the intestinal peptides glucagon-like peptide-1 (GLP-1) and gastric inhibitory peptide (also known as: glucose-dependent insulinotropic polypeptide or GIP). Both GLP-1 and GIP are rapidly inactivated by the enzyme dipeptidyl peptidase-4 (DPP-4); both GLP-1 and GIP are members of the glucagon peptide superfamily.[1][2][3] "Many factors stimulate insulin secretion, but the main one is blood glucose. Incretins, especially GIP and GLP-1 secreted, respectively, by K and L cells in the gut are also important" (Rang and Dale's Pharmacology (2015)). GLP-1 (7-36) amide is not very useful for treatment of type 2 diabetes mellitus, since it must be administered by continuous subcutaneous infusion. Several long-lasting analogs having insulinotropic activity have been developed, and three, exenatide (Byetta) and liraglutide (Victoza), plus exenatide extended-release (Bydureon), have been approved for use in the U.S. The main disadvantage of these GLP-1 analogs is they must be administered by subcutaneous injection. Another approach is to inhibit the enzyme that inactivates GLP-1 and GIP, DPP-4. Several DPP-4 inhibitors that can be taken orally as tablets have been developed. Once weekly dosage of Continue reading >>

Incretin Mimetic Drugs For Type 2 Diabetes

Incretin Mimetic Drugs For Type 2 Diabetes

Drugs in the incretin mimetic class include exenatide (Byetta, Bydureon), liraglutide (Victoza), sitagliptin (Januvia, Janumet, Janumet XR, Juvisync), saxagliptin (Onglyza, Kombiglyze XR), alogliptin (Nesina, Kazano, Oseni), and linagliptin (Tradjenta, Jentadueto). These drugs work by mimicking the incretin hormones that the body usually produces naturally to stimulate the release of insulin in response to a meal. They are used along with diet and exercise to lower blood sugar in adults with type 2 diabetes. Continue reading >>

Incretin Mimetics In The Treatment Of Type 2 Diabetes Mellitus

Incretin Mimetics In The Treatment Of Type 2 Diabetes Mellitus

Incretin Mimetics in the Treatment of Type 2 Diabetes Mellitus European Endocrinology, 2006(1):1-5; DOI: Citation European Endocrinology, 2006(1):1-5; DOI: Incretins are hormones from the gut that augment the postprandial nutrient-induced insulin secretion. The incretin effect is normally quantified by comparing the insulin responses with oral and intravenous glucose administration, where the infusion is adjusted so that the plasma glucose concentrations are similar to those observed after the oral administration. The insulin response to oral glucose is normally much larger than that observed after intravenous (IV) glucose, and in healthy subjects as much as 70% of the insulin response may be attributable to the action of the incretin hormones. An illustration of the power of the incretin effect was provided by Nauck et al.,1 who studied glucose excursions and insulin responses after increasing doses of oral glucose. It turned out that the glucose excursions were identical regardless of the amount of glucose ingested, the explanation being that incretin-induced insulin secretion was augmented progressively, thereby effectively preventing post-challenge hyperglycaemia (see Figure 1). The two most important incretin hormones are glucose-dependent insulinotropic polypeptide (GIP)formerly called gastric inhibitory polypeptideand glucagon-like peptide-1 (GLP-1). Their insulinotropic effects are additive, and together the two hormones can fully explain the incretin effects.2 The secretion of the incretin hormones is also proportional to the size of the ingested nutrient load.3 However, in patients with type 2 diabetes the incretin effects are severely reduced or absent4 and there is little doubt that the lacking incretin effect contributes significantly to the inadequate ins Continue reading >>

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