Posted on Wednesday, 10th February 2010 by admin
GLP-1 analogues available in the U.S. are exenatide (sold as Byetta) and liraglutide (sold as Victoza). They are sometimes referred to as GLP-1 receptor agonists. They are not considered first-choice drugs, but instead are typically used in combination with other drugs (except insulin).
Remember that drug names vary by country and manufacturer. This is a brief review only; consult your physician or pharmacist for full details.
Fun Fact for the diabetic version of Trivial Pursuit:
Exenatide (Byetta) is a synthesized version of a protein initially discovered in the saliva of a lizard, the Gila monster.
How do they work?
It’s complicated.
First off, you need to know that a small intestine hormone, glucagon-like peptide-1 (GLP-1), is produced in response to a meal. This hormone increases insulin secretion by pancreas beta cells, suppresses glucagon after meals, inhibits emptying of the stomach, and inhibits appetite. Other effects are suppression of glucose production by the liver, and improved glucose uptake by tissues outside the liver. All this tends to lower blood sugar levels after meals.
The problem is that GLP-1 is quickly destroyed by an enzyme called DPP-4. We have available to us now chemicals similar to GLP-1, called GLP-1 analogues, that bind to the GLP-1 receptors and are resistant to degradation by the enzyme DPP-4. They essentially act like GLP-1, and they hang around longer.
GLP-1 levels, by the way, are decreased in type 2 diabetes.
The action of GLP-1 is dependent on blood sugar levels. If blood glucose is not elevated, GLP-1 doesn’t go to work. From a practical viewpoint, this means that GLP-1-based therapies don’t cause hypoglycemia.
We know little about long-term outcomes with these drugs, such as diabetic complications, health-related quality of life, or mortality.
Uses
Exenatide is FDA-approved for adults with type 2 diabetes who are not adequately controlled with metformin, sulfonylurea, or a thiazolidinedione (or a combination of these agents). So it’s an add-on drug, not approved for use by itself. It’s not approved for use with insulin therapy.
Liraglutide is FDA-approved for treatment of type 2 diabetes but is not recommended as initial therapy, although it does seem to be approved for use by itself. It has been used alone and also in combination with metformin, sulfonylurea, and/or thiazolidinediones. It’s not approved for use with insulin therapy.
Dosing
They are available only as subcutaneous injections. Exenatide is twice daily, starting at 5 mcg within 60 minutes prior to a meal. After four weeks, the dose is increased to 10 mcg wtice daily.
Liraglutide is a once daily subcutaneous injection starting at 0.6 mg, increasing to 1.2 mg after one week. It is given without regard to meals. Maximum dose is 1.8 mg/day.
Side Effects
GLP-1 analogues tend to cause nausea, vomiting, and diarrhea in as many as four in 10 users. The nausea typically improves over time. They tend to cause weight loss. Both drugs might cause pancreatitis, which is life-threatening. When used with a sulfonlyurea, hypoglycemia may occur.
Liraglutide might cause thyroid cancer. No risk of hypoglycemia when used as the sole diabetes drug.
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- Drug Review: Dipeptidyl-Peptidase-4 Inhibitors (sitagliptin and saxagliptin)
- Drug Review: Insulin Secretagogues (sulfonylureas, repaglinide, and nateglinide)
- New Drug May Trim Insulin Injections to Just 3 a Week
- How Well Should Diabetes Be Controlled?
Tags: Exenatide, Exenatide Liraglutide
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