DPP-4 inhibitors: Difference between revisions

Latest revision as of 18:43, 22 September 2019

Background

Dipeptidyl Peptidase-4 Inhibitors (gliptans) are a class of oral hypoglycemics that block DPP-4. This leads to an increase in the activity of incretins, which inhibit glucagon release, which in turn increase insulin secretion and slow gastric emptying, ultimately decreasing blood glucose levels. These drugs are commonly used in the treatment of type 2 diabetes.
Generally used as second or third line treatment for type 2 diabetes mellitus. They may be used as monotherapy or combined therapy.

FDA Approved DPP-4 Inhibitors

Brand Name	Active Ingredient(s)
Januvia	sitagliptin
Janumet	sitagliptin, metformin
Janumet XR	sitagliptin, metformin ER
Onglyza	saxagliptin
Kombiglyze XR	saxagliptin, metformin ER
Tradjenta	linagliptin
Glyxambi	linagliptin, empagliflozin
Jentadueto	linagiptin, metformin
Nesina	alogliptin
Kazano	alogliptin, metformin
Oseni	alogliptin, pioglitazone

Mechanism of Action

Inhibit DPP-4, an enzyme expressed on surface of most cell types
DPP-4 deacctivates other bioactive peptides, including incretins such as glucagon-like peptide-1 (GLP-1).
GLP-1 is secreted in response to nutrients, stimulating glucose-dependent insulin release from pancreatic beta-cells, which in turn decreases blood sugar levels.
Also decreases gastric emptying and inhibits postprandial glucagon release

Adverse Effects

In controlled studies of sitagliptin (as monotherapy and combination therapy), overall incidence of adverse reactions/discontinuation similar to placebo
Most commonly reported adverse reactions include nasopharyngitis, URI, HA
Postmarketing surveillance found association with sitagliptin and development of acute pancreatitis
- Confounding variables such as diabetes, hypercholesterolemia, hypertriglyceridemia, obesity
Also postmarketing reports of serious allergic reactions (including anaphylactoid reactions, angioedema, SJS)
Studies of other drugs in this class additionally report lymphopenia, cough, peripheral edema, transaminitis, and hypertension.
Other side effects reported in patients taking this class of medication include joint pain

References

Authors:

@@ Line 10: / Line 10: @@
 | Januvia || sitagliptin
 |-
-| Janumet || sitagliptin, metformin
+| Janumet || sitagliptin, [[metformin]]
 |-
-| Janumet XR || sitagliptin, metformin ER
+| Janumet XR || sitagliptin, [[metformin]] ER
 |-
 | Onglyza || saxagliptin
 |-
-| Kombiglyze XR || saxagliptin, metformin ER
+| Kombiglyze XR || saxagliptin, [[metformin]] ER
 |-
 | Tradjenta || linagliptin
@@ Line 22: / Line 22: @@
 | Glyxambi || linagliptin, empagliflozin
 |-
-| Jentadueto || linagiptin, metformin
+| Jentadueto || linagiptin, [[metformin]]
 |-
 | Nesina || alogliptin
 |-
-| Kazano || alogliptin, metformin
+| Kazano || alogliptin, [[metformin]]
 |-
 | Oseni || alogliptin, pioglitazone
@@ Line 32: / Line 32: @@
 ==Mechanism of Action==
-DPP-4 inhibitors inhibit the enzyme DPP-4, which is expressed on the surface of most cell types. DPP-4 deactivates other bioactive peptides, including incretins like glucagon-like peptide-1 (GLP-1). GLP-1 is secreted in the small intestines in response to nutrients, stimulating glucose-dependent insulin release from the pancreatic beta-cells, which then decrease blood sugar levels. Additionally, it decreases gastric emptying and inhibits postprandial glucagon release.
+*Inhibit DPP-4, an enzyme expressed on surface of most cell types
+*DPP-4 deacctivates other bioactive peptides, including incretins such as glucagon-like peptide-1 (GLP-1).
+*GLP-1 is secreted in response to nutrients, stimulating glucose-dependent insulin release from pancreatic beta-cells, which in turn decreases blood sugar levels.
+*Also decreases gastric emptying and inhibits postprandial glucagon release
 ==Adverse Effects==
-In controlled clinical studies of sitagliptin as monotherapy and combination therapy, the overall incidence of adverse reactions and the discontinuation of therapy in those taking sitagliptin was similar to that in those taking the placebo. The most commonly reported adverse reactions include '''nasopharyngitis''', '''upper respiratory tract infection''' and '''headache'''.
+*In controlled studies of sitagliptin (as monotherapy and combination therapy), overall incidence of adverse reactions/discontinuation similar to placebo
+*Most commonly reported adverse reactions include nasopharyngitis, URI, HA
-Postmarketing surveillance found an association between those taking sitagliptin and development of '''acute pancreatitis''', though confounding variables include risk factors such as diabetes, hypercholesterolemia, hypertriglyceridemia and obesity. Approximately 3 months after sitigliptin initiation, there were also reports of '''serious allergic reactions''' including anaphylactoid reactions, angioedema and exfoliate dermatologic reactions such as Stevens-Johnson syndrome.
+*Postmarketing surveillance found association with sitagliptin and development of acute [[pancreatitis]]
+**Confounding variables such as diabetes, hypercholesterolemia, hypertriglyceridemia, obesity
-Studies of other drugs in this class additionally report lymphopenia, cough, peripheral edema, transaminitis, and hypertension.
+*Also postmarketing reports of serious allergic reactions (including anaphylactoid reactions, angioedema, SJS)
+*Studies of other drugs in this class additionally report lymphopenia, cough, peripheral edema, transaminitis, and hypertension.
-Patients taking DPP-4 inhibitors have also been found to develop '''joint pain''', which often ceased within a month of discontinuation of the medication.
+*Other side effects reported in patients taking this class of medication include joint pain
 ==See Also==
@@ Line 50: / Line 53: @@
 [[Category:Pharmacology]]
+[[Category:Endocrinology]]