Medications

DPP-4 Inhibitors or Incretin Enhancers

DPP-4 inhibitors are now available from various companies. DPP4 inhibitors work by blocking dipeptidyl peptidase IV (DPP-4), an enzyme that breaks down gut peptides, especially GLP-1. Unlike GLP-1 agonists that increases GLP-1 action, DPP-4 inhibitors work indirectly to raise GLP-1. Blocking DPP-4 makes GLP-1 levels rise and increases insulin release after meals and when glucose levels are high. However, inhibition of DPP-4 also causes levels of GLP-2, GIP, and other gut peptides to rise.

GLP-1 agonist, like Byetta and Bydureon can help treat Type 2 Diabetes.

Amylin

GLP-1 or glucagon-like peptide 1 is one of several naturally occurring incretin compounds that possess biologic activity when released from the gut during digestion. Because of its name, GLP-1 would seem to act like glucagon, which is a hormone that increases glucose production by the liver and raises glucose levels. Rather, GLP-1 lowers both glucagon and glucose levels. Though their actions differ, GLP-1 and glucagon are both derived from the same parent compound called proglucagon, hence the similarity in name.

Prandin and Starlix (Rapid Insulin Releasers)

Two drugs in this class are now available – Prandin, derived from benzoic acid and approved by the FDA in 1997, and Starlix, derived from D-phenylalanine and approved in 2000. They raise insulin levels rapidly by stimulating the beta cells by mechanisms different from the sulfonylureas. They enhance insulin release from the pancreas over a short period of time only when the glucose level is high. Therefore, the risk of hypoglycemia is reduced. Their activity more closely mimics normal first phase insulin release when food is eaten by a person without diabetes.

Actos and Avandia (Glitazones)

Thiazolidinediones or glitazones are the first class of medication designed to reverse the basic problem in Type 2 diabetes of resistance to insulin. Insulin resistance appears to be associated with high blood pressure and the high triglycerides/low HDL cholesterol problem that puts many people with Type 2 diabetes at risk for heart disease.

Precose and Glyset (Starch Blockers)

Alpha-glucosidase inhibitors or starch blockers help control blood sugars by slowing down the digestion of complex carbohydrates. This greatly reduces the spikes that may be seen in blood sugar after meals and, surprisingly, also tends to lower the fasting blood sugar. The two medications in this group, Precose and Glyset, are taken with every meal.

Metformin

Two drugs from the biguanide class, metformin and phenformin, were developed in 1957. Unfortunately, phenformin reached the U.S. market first and resulted in several deaths from lactic acidosis. When this risk surfaced, phenformin was pulled from drugstore shelves worldwide. Metformin was eventually found to be 20 times less likely to cause lactic acidosis, but it was tainted by the history of its cousin. Metformin first became available in France in 1979 and has been widely used in Europe since then, but it was not cleared for use in Type 2 diabetes in the U.S. until 1994.

Sulfonylureas

Sulfonylureas, the first drug group introduced into the U.S. in 1955, stimulates the beta cells to produce more insulin. These drugs have kept many Type 2’s off injected insulin. Sulfonylureas will not work in those with Type 1 diabetes (except for a specific type) nor in anyone with Type 2 whose beta cells no longer produce insulin. Loss of insulin production, indicated by a low C-peptide level in the blood, is found in those with Type 1 diabetes, in many who have Type 1.5 diabetes, and in many others with Type 2 diabetes for more than 6 to 15 years.

The Incretins: GLP-1 Agonists and DPP-4 Inhibitors

by John Walsh, P.A, CDE

In 1902, Researchers first hypothesized that the gut might directly signal the pancreas. The term incretin was first used in 1930 to describe the enhanced glucose lowering effect that was seen when a gut extract was fed to dogs. In the 1960s, researchers discovered that almost twice as much insulin was released when they infused glucose directly into the gut rather than into the blood as an IV solution, renewing interest in a search for compounds produced by the gut that could lower blood glucose levels.

Symlin, An Injectable Form of Amylin

Used to Improve Post Meal Glucose Control (Type 1)
and Weight Loss (Type 1 and possibly Type 2)

Dosing
Post Meal Control
Weight Loss
Stability
Tips On Handling Lows
The Symlin Pen
Summary

Learn About the Basics of Diabetes

Diabetes can be a complicated disease to manage, especially for the newly diagnosed. It affects men, women, and children differently. There are also multiple types of diabetes (Pre-diabetes, Type 1, Type 1.5, Type 2, etc) that have different effects on people. This section of our site gives you a great outline of diabetes diagnosis, treatments and complications. 

Newly Diagnosed

Learn the basics of diabetes, from its diagnosis and types to staying motivated while dealing with the disease.

 

Newsletter

Sign up for the Diabetesnet.com newsletter.