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Related Concept Videos

Dipeptidyl Peptidase 4 Inhibitors01:23

Dipeptidyl Peptidase 4 Inhibitors

Dipeptidyl peptidase 4 (DPP-4) is a serine protease widely distributed in the body. It's involved in the inactivation of GLP-1 and GIP hormones, which are crucial for insulin regulation. DPP-4 inhibitors, such as sitagliptin (Januvia), saxagliptin (Onglyza), linagliptin (Tradjenta), alogliptin (Nesina), and vildagliptin (Galvus), help increase the proportion of active GLP-1, enhancing insulin secretion. These inhibitors work by competitively binding to DPP-4. This binding causes a significant...
Oral Hypoglycemic Agents: Glinides01:06

Oral Hypoglycemic Agents: Glinides

Repaglinide (Prandin) and Nateglinide (Starlix), known as glinides, are oral insulin secretagogues that stimulate insulin release from pancreatic β cells by closing the ATP-sensitive potassium channels (KATP channel). Repaglinide controls insulin release from pancreatic β cells by managing potassium efflux. It shares two binding sites with sulfonylureas and also has a unique site, indicating overlapping mechanisms of action. With a rapid onset and a 4-7 hour duration, it effectively manages...
Hypoglycemia01:26

Hypoglycemia

Hypoglycemia is a blood glucose level below 70 mg/dL. It commonly occurs in individuals using insulin or insulin-secreting drugs, but may also arise in non-diabetic conditions. People with type 1 diabetes are at the highest risk because they depend on exogenous insulin. People with type 2 diabetes are also at risk, especially when treated with insulin or medications such as sulfonylureas, which increase insulin release regardless of blood glucose levels. It develops when insulin levels exceed...
Oral Hypoglycemic Agents: Biguanides and Glitazones01:26

Oral Hypoglycemic Agents: Biguanides and Glitazones

Biguanides, particularly metformin (Glucophage), are insulin sensitizers that enhance glucose uptake, thereby reducing insulin resistance. Unlike sulfonylureas, metformin doesn't prompt insulin secretion, which helps to curb hypoglycemia risk. Metformin is beneficial in treating conditions like polycystic ovary syndrome due to its insulin-resistance reduction capability. The drug's primary action involves curtailing hepatic gluconeogenesis, a significant contributor to high blood glucose levels...
Hypoglycemia and Glucagon01:15

Hypoglycemia and Glucagon

Without prolonged fasting, healthy individuals maintain blood glucose levels above 3.5 mM due to a well-adapted neuroendocrine counterregulatory system that effectively prevents acute hypoglycemia, a potentially life-threatening condition. The primary clinical scenarios for hypoglycemia encompass diabetes treatment, inappropriate production of endogenous insulin or insulin-like substances by tumors, and the use of glucose-lowering agents in non-diabetic individuals. Notably, hypoglycemia in the...
Glucagon-like Receptor Agonists01:24

Glucagon-like Receptor Agonists

Incretins include glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP), which stimulate insulin secretion post-meals. In type 2 diabetes, GIP's efficacy is reduced, making GLP-1 a viable drug target. GIP originates from preproGIP.
GLP-1, when administered in high doses intravenously, triggers insulin secretion, inhibits glucagon release, slows gastric emptying, reduces food intake, and restores normal insulin secretion. However, its rapid inactivation by the...

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Improving IV Insulin Administration in a Community Hospital
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Published on: June 11, 2012

Hypoglycemia associated with off-label sitagliptin use.

Heather P Whitley1, Kristi Kelley

  • 1Department of Pharmacy Practice, Auburn University Harrison School of Pharmacy, Auburn, AL, USA ; Department of Community and Rural Medicine, University of Alabama School of Medicine, Tuscaloosa, AL, USA.

International Medical Case Reports Journal
|June 8, 2013
PubMed
Summary

Sitagliptin combined with insulin or sulfonylureas can cause hypoglycemia in type 2 diabetes patients. Careful monitoring and dose adjustment are crucial when using sitagliptin off-label with these medications.

Keywords:
DPP-IV inhibitordiabetesdrug-inducedhypoglycemiaoff-labelsitagliptin

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Area of Science:

  • Endocrinology
  • Pharmacology
  • Diabetes Management

Background:

  • Sitagliptin is a dipeptidyl peptidase-4 (DPP-4) inhibitor used for type 2 diabetes.
  • Its mechanism of action does not typically cause hypoglycemia.
  • Off-label use in combination therapies requires careful consideration.

Observation:

  • A case study involving a 55-year-old female with type 2 diabetes.
  • Addition of sitagliptin to metformin, glimepiride, and mixed insulin resulted in hypoglycemia.
  • Symptoms resolved with sulfonylurea discontinuation and insulin dose reduction, recurring upon sitagliptin reintroduction.

Findings:

  • Sitagliptin, when used with hypoglycemia-inducing agents like sulfonylureas or insulin, increases the risk of hypoglycemic events.
  • The risk may also extend to combinations with meglitinides.
  • Reducing meal-time insulin doses can help prevent hypoglycemia in such off-label scenarios.

Implications:

  • Clinicians must exercise caution when prescribing sitagliptin with sulfonylureas or insulin.
  • Vigilant monitoring for hypoglycemia is essential for patients on these combined therapies.
  • Potential insurance coverage issues for off-label sitagliptin combinations should be anticipated.