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GLP-1 Receptor Agonists (RA) As an addition to oral metformin, injectable forms of GLP-1 Receptor Agonists can help the pancreas release more insulin when glucose levels are high. We've listed several examples below, including short-acting that are cleared from the body in less than a day, and long-acting that may continue to work for up to a week. These medications can slow down glucose absorption during digestion and are used to treat type 2 diabetes only. Liraglutide is also indicated for reducing the risk of major cardiovascular events in patients who have type 2 diabetes and cardiovascular disease. With the exception of an oral form of short-acting GLP-1 RA, oral semoglutide or Rybelsus®, the medications are provided in disposable pen injection devices that we will review later in this presentation. This class of medications may also be added to the initial regimen of metformin (which we will discuss with the oral medications) to improve treatment. Mechanism of Action The GLP-1 receptor agonists decrease blood glucose by increasing the secretion and release of insulin in response to food and decreasing glucagon secretion. The GLP-1 receptor agonists also slow gastric emptying, regulate post-prandial glucagon secretion, and enhance satiety. In addition, GLP-1 RAs can reduce release of glucose by the liver. Side effects of these medications may include early satiety, reduced appetite, nausea, vomiting, and diarrhea, which tend to subside or lessen over time. |
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Oral Diabetes Medications
Sodium-Glucose Co-Transporter Type 2 Inhibitors (SGLT2 Inhibitors)
Available forms
Canagliflozin (Invokana®)
Dapagliflozin (Farxiga®)
Empagliflozin (Jardiance®)
Ertugliflozin (Steglatro®)
Indications for Use
These drugs block some of the glucose in your system from reentering your blood through your kidneys. They also cause your body to get rid of more glucose through your urine. The SGLT2 inhibitors are also prescribed to patients who have type 2 diabetes and are taking metformin to reduce the risk of major cardiovascular events.
Mechanism of Action
SGLT2 inhibitors increase the renal excretion of glucose and lowers plasma glucose. These drugs block some of the glucose in your system from reentering your blood through your kidneys.
Dipeptidyl Peptidase IV (DPP-4) Inhibitors
Available forms
Alogliptin (Nesina®)
Linagliptin (Tradjenta®)
Saxigliptin (Onglyza®)
Sitagliptin (Januvia®)
Indications for Use
The DPP-4 inhibitors can be used as monotherapy along with diet and exercise or in combination with other medications. The effect may be modest, but may also be an important adjunct to metformin, thiazolidinedione, or sulfonylurea, or even as an alternative to metformin for patients who have contraindications or exhibit intolerance to metformin.
Mechanism of Action
These drugs block the breakdown of certain hormones (glucagon-like peptide-1 or GLP-1) in your body, which results in feedback to decrease glucagon production and release and promote production and release of insulin. These drugs also slow your digestion by slowing gastric emptying, which slows the increase of blood glucose. The 2020 Standards of Care note that if oral agents don’t provide adequate blood sugar control, the addition of a glucagon-like peptide 1 receptor agonist is preferred to insulin, if it is possible to use.
DPP-4 inhibitors tend to be body weight neutral and are generally well tolerated.
Side effects may include sore throat, stuffy nose, upset stomach, and diarrhea.
Thiazolidinediones
Available forms
Pioglitazone (Actos®)
Rosaglitazone (Avandia®)
Indications for Use
As an adjunct, along with diet and exercise, to attain glycemic control for patients who have type 2 diabetes.
Mechanism of Action
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hiazolidinediones lower blood glucose by increasing insulin utilization and decreasing insulin resistance.