Gliptins

gliptin basics on how they work

1. Gliptins
background

2. New drugs for DM
•In DM, several pharmacologic interventions
have undesirable side effects, including
hypoglycemia and weight gain.
•Drugs targeting the incretin pathway are
the latest addition to the available
antidiabetes agents.
•Incretin-based therapy is either delivered:
1.orally (dipeptidyl peptidase-4 [DPP-4])
inhibitors or
2.injected subcutaneously (glucagon-like
peptide-1 [GLP-1] mimetics and analogues).

3. India
•Eli Lilly has Byetta (exenatide injection)–
[GLP-1 agonist]
•There are 3 DPP-4 inhibitors currently
available
1.Sitagliptin [JANUVIA – MERCK]
2.saxagliptin, [ONGLYZA - BMS] and
3.Vildagliptin [VILDAGLIPTIN – NOVARTIS]

4. DPP-4
•Dipeptidyl peptidase-4 inhibitors are
effective with a low incidence of
hypoglycemia and no weight gain either as
a single or combination therapy in lowering
1.glycated hemoglobin,
2.fasting and
3.postprandial glucose levels.

5. How DPP-4 works?
•The digestive system breaks down food into
sugar (glucose).
•This increases signals, called incretins.
•Incretins tell the pancreas to release insulin
in response to food.
•In type 2 DM, the pancreas doesn't release
enough insulin or the body's cells may not
use insulin properly.
•This leads to rise in blood sugar level.

6. How DPP-4 works?
•In response to a meal, active glucagon-
like peptide-1 (GLP-1) is secreted by the
L cells of the intestines.
•Without the presence of a gliptin, GLP-1
is rapidly inactivated and degraded by the
enzyme dipeptidyl peptidase IV (DPP4);
•when a gliptin is present, it binds to
DPP4, allowing GLP-1 to remain active.
•Active GLP-1 causes the pancreas to
increase insulin release and decrease
glucagon release.