Secretagogues

Secretagogues are classified as sulfonylureas or non-sulfonylureas (repaglinide). The primary action of secretagogues is to increase the release of insulin from the pancreas.  

1. Therapeutic Considerations with Secretagogues

All information from medication product monographs unless referenced below.

A1c Lowering  1-1.5%1
Hypoglycemia Risk High
Side Effects hypoglycemia, weight gain
Vascular Protection No
Weight May increase 
Cost, Blue Cross coverage;  strengths;  dosing frequency; indications

Visit Secretagogues in the Complete Diabetes Medications Table  

Combination Medications None
Advice for times of dehydration, vomitting, diarrhea To avoid concerns with reduced medication clearance, Diabetes Canada advises this class of medication be stopped until these symptoms are resolved. Adequate hydration should be promoted. 
Other
  • Generally cost less than other classes of diabetes medications (other than Metformin). 
  • Gliclazide, gliclazide MR and glimepiride are associated with less hypoglycemia than glyburide. 
  • Repaglinide is associated with less hypoglycemia in those with irregular or missed meals. 
  • Gliclazide, glimepiride and glyburide are contraindicated in severe renal failure (see Dosing Considerations); however repaglinide can be used at lower doses. 
  • Cardiovascular risk seen with first generation sulfonylreas (ie- tolbutamide) but not with second generation sulfonylureas available now, especially gliclazide that is pancreas specific.2


 2. Dosing Considerations with Secretagogues

  • Refer to Therapeutic Considerations for Renal Impairment, Diabetes Canada for specific brand dosing recommendations in renal impairment. 
  • All brands indicate tablet should be taken with meal. 
  • The daily dose of the secretagogues gliclazide, glimiperide and glybyride is usually adjusted based on overall blood glucose values or A1c. 
  • Individual meal doses of repaglinide may be adjusted based on postprandial glucose levels. The patient may also be taught to vary repaglinide dose based on planned carboyhdrate intake and/or activity level. 

3. Brand Considerations

 

Gliclazide - Diamicron®

Gliclazide Modified Release - Diamcron MR®

  •  See the Complete Diabetes Medication Table for: cost/month; Blue Cross coverage; available strengths;  dosing frequency; Health Canada indications
  • To be taken once a day with breakfast meal. 

Glimepiride - Amaryl® 

  •  See the Complete Diabetes Medication Table for: cost/month; Blue Cross coverage; available strengths;  dosing frequency; Health Canada indications
  • To be taken once a day with breakfast or first meal of the day. 

Glyburide - Diabeta® 

Repaglinide - Gluconorm® 

References:

  1. Inzucchi SE, Bergenstal RM, Buse JB, det al. Management of hyperglycemia in type 2 diabetes: a patient-centred approach. Diabetes Care 2012; 35: 1364-79.  http://care.diabetesjournals.org/content/35/6/1364  (Accessed Feb 26, 2018). 
  2. Schramm TK, Gislason GH, Vaag A, et al. Mortality and cardiovascular risk associated with different insulin secretagogues compared with metformin in type 2 diabetes, with or without a previous myocardial infarction: a nationwide study. Eur Heart J 2011; 32:1900.