Posted on Sunday, 7th February 2010 by admin
Insulin secretagogues include sulfonylureas (e.g., glipizide, glimiperide, glyburide) and meglitinides (repaglinide and nateglinide). They are called secretagogues because they make the pancreas beta cells secrete more insulin into the bloodstream.
Sulfonylureas (SUs) in 2010 are still the most widely used drugs for treatment of type 2 diabetes. At least six different SUs are in common usage in the U.S. They are often prescribed for patients who do not respond adequately to lifestyle modification and are intolerant of metformin, the usual first-choice drug.
The meglitinides are also called “glinides.” In the U.S. repaglinide is sold as Prandin, and nateglinide is Starlix. Meglitinides are considerably more expensive than the SUs.
This is a brief review pertinent to type 2 diabetes only—consult your physician or pharmacist for details. Drug names vary by country and manufacturer.
How do they work?
Sulfonylureas increase the pancreas’ production of insulin after a meal (second phase insulin secretion). If the pancreas beta cells are no longer producing any insulin, SUs won’t work. SUs decrease fasting blood sugar by about 20% and hemoglobin A1c by 1 or 2% (absolute, not relative).
Metiglinides have about the same effectiveness as SUs. Repaglinide and nateglinide increase the pancreas’ output of insulin, working faster than sulfonylureas. They don’t last as long as sulfonylureas, which may help avoid hypoglycemia. These two “glinides” work mostly to reduce sugar levels after meals. If the pancreas produces no insulin at all, these drugs won’t work.
We don’t know if these drugs affect death rates.
Uses
May be used alone or in combination with certain other diabetic drugs. Since they have the same mechanism of action, sulfonylureas and meglitinides would not normally be used together. In combination therapy, you want to use drug classes that work by different mechanisms.
Dosing
SU dose depends on the particular one used. Some are taken by mouth once daily, others twice.
Starting dose for repaglinide is 0.5 mg by mouth before each meal. Maximum dose is 4 mg before each meal.
Nateglinide: 120 mg by mouth immediately before each meal.
Side effects
Hypoglycemia is the most severe adverse effect of the sulfonylureas, and may be less common with the meglitinides. The duration of hypoglycemia seen with SUs is often much longer than you would predict by how much drug is in the bloodstream. Hypoglycemia is more common with the longer-acting drugs, such as glyburide and chlorpropamide. There is some concern that sulfonylureas are linked to poorer outcomes after a heart attack. SUs occasionally cause nausea, skin reactions, and elevations of liver function tests.
Weight gain is common with SUs and meglitinides.
When used with insulin or thiazolidinediones, these sulfonylurea adverse effects are more likely to appear: weight gain, fluid retention, congestive heart failure.
Precautions . . .
Sulfonlylureas: Consult your personal physician or pharmacist.
Nateglinide: Use with great caution, if at all, in the setting of severe kidney disease and moderate to severe liver disease.
Repaglinide: Use cautiously in severe kidney and liver disease.
Steve Parker
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Tags: Insulin, Insulin Secretagogues
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